ZIB

101

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Modification in the pharmacokinetics of amikacin during development (1982)

Lanao, J. M. ; Dominguez-Gil, A. ; Dominguez-Gil, A. A. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 155-160

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ISSN: 1432-1041

Keywords: amikacin ; pharmacokinetics ; development ; neonate ; infant ; child

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The disposition kinetics of a single i.v. dose of amikacin was studied in 6 neonates (6–25 days old), 10 infants (4–18 months) and 8 young children (3–11 years). There was a progressive change in the distribution and elimination kinetics during development. The distribution coefficient of the antibiotic averaged of 0.429, 0.320 and 0.210 l/kg in the newborns, infants and young children, respectively and serum half-life (t1/2 β) in these three groups averaged 2.812, 1.803 and 1.196 h, respectively. Significant differences in certain pharmacokinetic parameters were found between the values in paediatric patients and in adults receiving the same dose. A linear relationship was established between the distribution volume of the antibiotic and the weight of the patients, as defined by the following equation: $${\text{Vd}}_{{\text{ss}}} \left( 1 \right) = 0.976 + 1.140 \cdot {\text{TBW}}\left( {{\text{kg}}} \right);r = 0.954$$ The results suggest that a regimen of very frequent administrations should be employed in infants and young children in order to maintain a therapeutic level throughout treatment.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00545971

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102

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Clinical pharmacokinetics of high dose mebendazole in patients treated for cystic hydatid disease (1982)

Braithwaite, P. A. ; Roberts, M. S. ; Allan, R. J. ; [et al.]

Springer

European journal of clinical pharmacology 22 (1982), S. 161-169

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ISSN: 1432-1041

Keywords: mebendazole ; hydatid disease ; Echinococcus granulosus ; hepatic disease ; pharmacokinetics

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The plasma concentrations of mebendazole and its metabolites have been monitored in twelve patients after receiving a 10 mg/kg dose for cystic hydatid disease. The mebendazole plasma concentration-time profiles differed considerably between patients; elimination half-lives ranged from 2.8–9.0 h, time to peak plasma concentration after dosing ranged from 1.5–7.25 h and peak plasma concentrations ranged from 17.5 to 500 ng/ml. The mean peak plasma concentration of mebendazole after an initial dose (69.5 ng/ml) was lower than found in patients during chronic therapy (137.4 ng/ml). The plasma AUCTs for the major metabolites of mebendazole (methyl 5-(α-hydroxybenzyl)-2-benzimidazole carbamate and 2-amino-5 benzoylbenzimidazole) were about five times the plasma AUCT found for mebendazole in patients on chronic therapy. It is suggested that the slower clearance of these polar metabolites relative to mebendazole results from enterohepatic recycling. Since mebendazole is also highly plasma protein bound, caution should be observed in administering mebendazole to patients with liver disease. Concentrations of mebendazole found in the tissue and cyst material collected from two patients during surgery ranged from 59.5 to 206.6 ng/g wet weight.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00542462

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103

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Pharmacokinetics of parenteral and oral melperone in man (1982)

Borgström, L. ; Larsson, H. ; Molander, L.

Springer

European journal of clinical pharmacology 23 (1982), S. 173-176

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ISSN: 1432-1041

Keywords: melperone ; neuroleptic drug ; dose dependent kinetics ; i.m. injection ; i.v. injection ; pharmacokinetics ; oral application

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics of melperone (Buronil®, Ferrosan, Sweden) was studied after administration of various parenteral and oral doses to man. After parenteral administration, the data could be fitted to a two-compartment model, but after oral dosing the distribution phase could not be separated from the elimination phase, and so an one-compartment model gave the best fit. The half-lives were about 3–4 h, except after intramuscular injection, when the half-life was about 6 h. The bioavailability of oral doses was about 60% of the intravenous injection. After the highest oral dose of 100 mg, the pharmacokinetics, expressed as AUC or Cmax, showed non-linearity, possibly due to saturation of the hepatic elimination system.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00545974

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104

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Distribution of oral ketoconazole to vaginal tissue (1982)

Heykants, J. J. P. ; Woestenborghs, R. J. H. ; Bisschop, M. P. J. M. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 331-333

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ISSN: 1432-1041

Keywords: ketoconazole ; vaginal candidosis ; oral antimycotic ; distribution ; pharmacokinetics ; vaginal tissue concentrations

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Plasma samples and biopsies of vaginal tissue were obtained from 23 healthy women undergoing operative sterilization, 1 to 6 h after a single oral dose of ketoconazole 200 mg. Drug concentrations in plasma and tissue, were measured by a specific gas chromatographic method. The vaginal tissue concentration averaged 2.4 times less than the corresponding plasma levels. Equilibrium between tissue, and plasma was established within 1 h after dosing, when vaginal tissue levels exceeded 1 µg/g. Ketoconazole concentrations decayed monoexponentially over the time interval studied (1–6 h), with the similar half-lives of 1.2 and 1.4 h in plasma and tissue, respectively. Following an oral 200 mg dose, a tissue concentration not less than 0.01 µg/ml was maintained over a 12 h period. This concentration has been shown to prevent outgrowth of the invasive (pseudo) mycelial form ofCandida albicans. Hence, a b.i.d. or t.i.d. dosage schedule of ketoconazole in vaginal candidosis would give continuously effective levels at the site of infection. Ketoconazole concentrations in vaginal fluid are thought to be much higher than in the tissue because of ion-trapping. The present data may explain the efficacy of oral ketoconazole in the treatment of vaginal candidosis.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00613615

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105

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In vivo effect of methylmercury on protein synthesis in peripheral nervous tissues of the rat (1982)

Omata, Saburo ; Momose, Yasunori ; Ueki, Hiroshi ; [et al.]

Springer

Archives of toxicology 49 (1982), S. 203-214

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ISSN: 1432-0738

Keywords: Methylmercury ; Protein synthesis ; Peripheral nerve ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract The in vivo rates of protein synthesis in the peripheral nervous tissues of methylmercury-treated rats (10 mg/kg/day, for 7 days) have been estimated with improved methods by the injection of a large amount of [l-14C]valine of low specific activity. Protein synthesis activity in the dorsal root ganglia was inhibited to the extent of 60% of the control as early as day 5 and this continued to the symptomatic period (day 15) on which crossing of hind limbs, a typical sign of organomercurial poisoning, was observed in the animals. The sciatic nerves and dorsal roots increased protein synthesis by 56% at the symptomatic period. These increases in protein synthesis may be due to the stimulation of reactivity of Schwann's cells. On the contrary, the protein synthesis in the ventral roots showed a gradual decrease as the intoxication proceeded and decreased to 73% of the control at the symptomatic period, being similar to the case of the brain. The double-labeling studies with sodium dodecyl sulfate/polyacrylamide gel electrophoresis exhibited that methylmercury inhibited the synthesis of the dorsal root ganglion proteins non-uniformly in various apparent molecular sizes, especially on day 10.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00347868

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106

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Ontogenic changes in selenite metabolism in rats (1982)

Ošťádalová, I. ; Babický, A. ; Kopoldová, J.

Springer

Archives of toxicology 49 (1982), S. 247-252

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ISSN: 1432-0738

Keywords: Selenite metabolism ; Selenite toxicity ; Trimethylselenoniumion ; Ontogeny ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract Radioselenium concentration and excretion was studied after administration of 75Se-labelled selenite to male rats during ontogeny. The concentration of radioselenium in individual organs decreases with increasing age. The largest differences between young and adults were in the quantity and quality of excreted substances. During 2 h after the administration of 20 μmol selenite/kg young rats excreted 2.4% of the dose, essentially in the urine only, whilst adults excreted a total of 11%, distributed equally in breath and urine. The part excreted as methylated metabolites was 0.1% of the administered dose in young and 6.3% in adult rats. These results support the hypothesis that the differences in the sensitivity to the toxic action of selenite between young and adult rats can be due to ontogenic differences in selenium metabolism.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00347872

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107

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Endogenous metal binding proteins in relation to the differences in absorption and distribution of mercury in newborn and adult rats (1982)

Webb, M. ; Holt, Daphne

Springer

Archives of toxicology 49 (1982), S. 237-245

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ISSN: 1432-0738

Keywords: Rat ; Adult ; Newborn ; Intestinal copper-complex ; Hepatic zinc-(metallo)-thionein ; Mercury distribution

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract Both in the intestinal copper complex and hepatic zinc-thionein of the newborn rat provide immediately available, high-affinity binding sites for Hg2+. Retention of orally administered Hg2+ in the gastrointestinal tract is much greater in the 5-day old rat than in the weanling and accounts for most (70–90%) of the body burden at 18 h. At a dose level of 790 μg Hg2+/kg body weight, 41% of the Hg2+ retained in the gastrointestinal tract of the newborn animal is located in the soluble fraction of the mucosa and 48% of this is bound by the copper-complex. This complex, therefore, seems to limit the transfer of Hg2+ from the mucosa to the serosa. It does not appear, however, to be a primary acceptor of Hg2+ in the neonatal intestine since, after administration of 100 μgHg2+/kg body weight, its binding of Hg2+ is less (33% of the soluble Hg2+) than that (67% of the soluble Hg2+) of the high molecular weight protein fraction. At 18 h after the intraperitoneal administration of Hg2+ (790 μg Hg2+/kg body weight), whole body retention is greater in the adult (80% of the dose) than in the suckling or weanling animal (63–68% of the dose). In the suckling animal the inter- and intra-organ distributions of the retained Hg2+ also differ from those in the weanling and/or adult rat. Thus the ratio of the renal: hepatic Hg2+ contents, after either intragastric or intraperitoneal doses of Hg2+, increases with age. Also most (approximately 90%) of the Hg2+ retained in the liver of the newborn animal after an intragastric dose is bound by the metallothionein whereas, in the adult liver, only 4% of the total Hg2+ is in this form. The presence of the metallothionein, however, is not the cause of the increased Hg2+ uptake in the former, since induction of hepatic zinc-thionein in the adult by pretreatment with Zn2+ does not affect the distribution of Hg2+ between the liver and kidneys. These findings are discussed in relation to the known differences in intestinal absorption and tissue distribution of Cd2+ and Hg2+ in newborn and adult animals and the greater resistance of the former to Hg2+ nephrotoxicity.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00347871

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108

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Phthalate esters I: effects on cytochrome P-450 mediated metabolism in rat liver and lung, serum enzymatic activities and serum protein levels (1982)

Walseth, Frode ; Toftgård, Rune ; Nilsen, Odd G.

Springer

Archives of toxicology 50 (1982), S. 1-10

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ISSN: 1432-0738

Keywords: Phthalate esters ; Liver ; Lung ; Blood ; Rat ; Enzymatic activities

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract Dimethylphthalate (DMP), dibutylphthalate (DBP) and di(2-ethylhexyl)phthalate (DEHP) were given i.p. (3.8 mM/kg) to Sprague Dawley rats for 5 days. DBP increased significantly the liver concentration of cytochrome P-450, but decreased the lung concentration by about 40%. DBP decreased the lung concentration of cytochrome b5 and NADPH-cytochrome-c-reductase activity by about 30%. Only minor effects were seen after treatment with DMP and DEHP. The direction of B(a)P metabolism was changed and the formation of 2- and 3-hexanol metabolites were increased in liver microsomes after DBP treatment. All phthalate esters decreased the lung metabolism of B(a)P. The cytochrome P-450 enzyme system in the lung was ten times more effective than that in the liver as far as metabolism of n-hexane was concerned. Only minor effects were observed in serum enzyme activities, but a significant decrease in the serum level of albumin was observed after treatment with DBP. No relationship was found between the carbon chain length of the investigated chemicals and effects on microsomal enzymatic activities.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00569231

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109

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Biodegradation of beta-hexachlorocyclohexane (1982)

Macholz, R. M. ; Knoll, R. ; Lewerenz, H. -J. ; [et al.]

Springer

Archives of toxicology 50 (1982), S. 85-88

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ISSN: 1432-0738

Keywords: Hexachlorocyclohexane ; Metabolism ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract Urine and organe of rats were examined for metabolites after oral dosage of thebeta-isomer of hexachlorocyclohexane (HCH).Beta-HCH was converted to 2,3,4- and 2,4,6-trichlorophenol (TCP), to other isomers of TCP, and to 2,3,4,6-tetrachlorophenol.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00569240

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110

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The comparative renotoxicology of phenylmercury and mercuric chloride (1982)

Magos, L. ; Sparrow, S. ; Snowden, R.

Springer

Archives of toxicology 50 (1982), S. 133-139

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ISSN: 1432-0738

Keywords: Phenylmercury ; Mercuric chloride ; Renal mercury ; Alkaline phosphatase ; Proximal tubular damage ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract The acute renotoxicity of HgCl2 and phenylmercuric acetate (PhHgAc) was compared at two intraperitoneal dose levels: 0.5 and 1.0 mg Hg/kg. There was no difference in the type of proximal tubular damage caused by the two mercurials, but 1.0mg Hg/kg as PhHgAc produced approximately the same degree of damage as 0.5 mg Hg/kg as HgCl2. At the selected dose levels only HgCl2, but not PhHgAc increased the urinary excretion of alkaline phosphatase. At 12 and 24 h after PhHgAc the content of mercury was higher in blood and lower in the kidneys and urine than after the administration of equimolar doses of HgCl2. As the difference in the renal mercury contents of HgCl2 and PhHgAc treated groups declined with time, difference in renotoxicity seems to relate only to renal mercury taken up within 24 h of administration. It is suggested that the slower renal extraction of mercury — as in regenerating kidneys (Tandon and Magos 1980) — was responsible for the lower degree of renotoxicity in phenylmercury treated rats.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00373395

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111

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Kanamycin induced ototoxicity in the laboratory rat (1982)

Astbury, P. J. ; Read, N. G.

Springer

Archives of toxicology 50 (1982), S. 267-278

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ISSN: 1432-0738

Keywords: Rat ; Scanning electron microscopy ; Organ of Corti ; Auditory threshold ; Kanamycin ; Preyer reflex

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract Two comparative experiments on the behavioural, audiometric and histological effects of kanamycin-induced cochleotoxicity in the Wistar rat are reported. In the first experiment kanamycin 400–1,500 mg/kg/day was injected subcutaneously for 20 days and the morphological damage to the organ of Corti assessed. In the second experiment the progression of damage to the organ of Corti was examined in animals given kanamycin 700 mg/kg/day for 4–20 days. Behavioural audiometric studies of threshold shift were undertaken throughout both experiments. In the first study, all the animals were killed after a recovery period of 20 days from the last injection, i.e., day 40, and in the second study groups of animals were killed at 4-day intervals between days 4 and 20 of dosing. One cochlea from each animal was critical point-dried, dissected to expose the organ of Corti and examined by scanning electron microscopy. A vertical section through the contralateral cochlea was examined by light microscopy. The results of the morphological examination of the cochleas were collated with the behavioural audiometry. The morphological damage to the organ of Corti followed a stereotyped pattern of degeneration, the extent of which appeared to be determined both by the number and concentration of the kanamycin administrations. The collateral audiometric examinations indicated that extensive damage had taken place before a shift in the behavioural auditory threshold could be detected by observation of the Preyer reflex.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00310859

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112

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Neonatal exposure to zearalenone causes persistent anovulatory estrus in the rat (1982)

Kumagai, Susumu ; Shimizu, Tsutomu

Springer

Archives of toxicology 50 (1982), S. 279-286

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ISSN: 1432-0738

Keywords: Zearalenone ; Rat ; Neonatal administration ; Persistent estrus ; Anovulation

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract The effect of neonatal administration of zearalenone on the female reproductive system was studied in the rat. A single subcutaneous injection of 1.0 mg zearalenone to 3- or 5-day-old rats caused persistent vaginal estrus in adulthood. Ovaries in these animals contained many large follicles but no newly formed corpora lutea. The same effects were observed in rats which had received 100 μg estradiol-17β in the neonatal period. Most rats which had received 100 μg zearalenone or 10 μg estradiol-17β showed regular 4-day estrous cycles and had newly formed corpora lutea in their ovaries. These results demonstrate that neonatal exposure to zearalenone produces persistent anovulatory estrus in the rat, the potency being about one tenth that of estradiol-17β.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00310860

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113

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Cellular responses to trialkylphosphorothioate-induced injury in rat lung (1982)

Dinsdale, D. ; Verschoyle, R. D. ; Cabral, J. R. P.

Springer

Archives of toxicology 51 (1982), S. 79-89

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ISSN: 1432-0738

Keywords: Trialkylphosphorothioates ; Rat ; Lung ; Ultrastructure

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract Various trialkylphosphorothioates occur as impurities in many organophosphorus pesticides. In addition to the immediate, cholinergic symptoms usually associated with the toxicity of organophosphorus compounds an oral LD50 dose of O,S,S-trimethyl phosphorodithioate or O,O,S-triethyl phosphorothioate to rats, resulted in the delayed development of lung lesions and often death within 4 days. This study attributes the late crisis to impaired lung function resulting from massive alveolar oedema and cellular responses to the selective destruction of type I pneumocytes. Proliferation of type II pneumocytes produced an epithelium of very large cells which resulted in a thick blood/alveolus barrier and also occluded much of the alveolar lumen. Debris from the type I pneumocytes was liberated into the alveolar lumen resulting in leukocytic infiltration of the interstitial tissue and an increase in the number of alveolar macrophages. The lung morphology of animals surviving the crisis period returned to normal within a further 4 days with the transformation of many hypertrophic type II pneumocytes into type I alveolar lining cells.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00279323

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114

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The carcinogenic action of aristolochic acid in rats (1982)

Mengs, U. ; Lang, W. ; Poch, J. -A.

Springer

Archives of toxicology 51 (1982), S. 107-119

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ISSN: 1432-0738

Keywords: Aristolochic acid ; Toxicology ; Chronic toxicity ; Carcinogenicity ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract Male and female Wistar rats treated orally with 0.1, 1.0 or 10.0 mg/kg/day aristolochic acid as its sodium salt (AA) developed a high incidence of tumours dependent on dose and time. After 3 months' treatment 1.0 and 10.0 mg/kg AA led to severe papillomatosis of the forestomach with occasional signs of malignancy. Three to 6 months later without further treatment the rats developed squamous cell carcinomas in the forestomach with formation of metastases. At the same time anaplasia of the tubular epithelium and mainly adenomas appeared in the renal cortex. The transitional epithelium of the renal pelvis and the urinary bladder showed hyperplasia, papillomas or carcinomas. For the low dose (0.1 mg/kg) the treatment with AA varied between 3 and 12 months. No tumours were observed in the first 6 months of the study. After 12 and 16 months, however, papillomas or squamous cell carcinomas also occurred in the forestomach. In addition, hyperplasia of the transitional epithelium of the renal pelvis was found while the renal cortex and the urinary bladder remained normal.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00302751

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115

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Distribution and elimination of di-2-ethylhexyl phthalate (DEHP) and mono-2-ethylhexyl phthalate (MEHP) after a single oral administration of DEHP in rats (1982)

Oishi, Shinshi ; Hiraga, Kogo

Springer

Archives of toxicology 51 (1982), S. 149-155

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ISSN: 1432-0738

Keywords: Di-2-ethylhexyl phthalate ; Mono-2-ethylhexyl phthalate ; Simultaneous determination ; Distribution and elimination ; Biological half-life ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract The distribution and elimination of di-2-ethylhexyl phthalate (DEHP) and mono-2-ethylhexyl phthalate (MEHP) after a single oral administration of DEHP (25 mmol/kg) were studied. A gas-liquid Chromatographic method was used for the simultaneous determination of MEHP and DEHP. The compounds were extracted with methylene chloride and the monoester was alkylated to the hexyl derivative by solid-liquid phase transfer catalysis in methylethyl ketone. The coefficients of variation of this method for determination of DEHP and MEHP were 8.3% and 11.4% respectively. The concentration of DEHP and MEHP in blood and tissues increased to maximum within 6–24 h after dosing, while the highest levels observed in the heart and lungs occurred within 1 h. At 6 h after administration, the highest ratio of MEHP/DEHP (mol%) were recorded in testes (210%) while the other tissues exhibited less than 100%. MEHP disappeared exponentially with t 1/2 values ranging from 23 to 68 h; DEHP t 1/2 ranged from 8 to 156 h and the t 1/2 values of MEHP in several tissues were slightly longer than DEHP. The t 1/2 values in blood were 23.8 h and 18.6 h for MEHP and DEHP, respectively.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00302755

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116

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Methylmercury-induced changes in the activities of neurotransmitter enzymes in nervous tissues of the rat (1982)

Omata, Saburo ; Hirakawa, Eihime ; Daimon, Yoshie ; [et al.]

Springer

Archives of toxicology 51 (1982), S. 285-294

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ISSN: 1432-0738

Keywords: Methylmercury ; Neurotransmitter ; Enzyme ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract The activities of neurotransmitter-metabolizing enzymes were determined in the nervous tissues of rats treated with methylmercury chloride (10 mg/kg/day, for 7 days). The activity of choline acetyltransferase was lowered consistently in the cytosol and synaptosomal fractions of the brain in methylmercury-treated rats, while changes in acetylcholinesterase activity in the brain subcellular fractions were small. In peripheral nerves, decreases in activities of choline acetyltransferase in the sciatic nerve and of acetylcholinesterase in the dorsal root were most profound. Decreases in these enzyme activities started at an early phase and increased markedly with the progress of intoxication. The activity of acetylcholinesterase in the dorsal root ganglion and in the sciatic nerve was also inhibited significantly at the latent period and more profoundly at the symptomatic period at which time crossing of hind limbs, a typical sign of organomercurial poisoning, was observed in the animals. Activities of tyrosine hydroxylase and monoamine oxidase were elevated in the brain homogenate and especially in the synaptosomal fraction with respect to the former enzyme after methylmercury treatment. Effects of methylmercury in vitro on the activities of these enzymes revealed that a much higher amount of methylmercury was required to produce in vitro an inhibitory action equivalent to that observed in vivo. These results suggest that the neurotoxic action of methylmercury could be mediated, at least in part, through the level of neurotransmitter enzymes.

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URL: http://dx.doi.org/10.1007/BF00317007

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117

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Investigation of the acute toxicity of some trimethyl and triethyl phosphorothioates with particular reference to those causing lung damage (1982)

Verschoyle, R. D. ; Cabral, J. R. P.

Springer

Archives of toxicology 51 (1982), S. 221-231

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ISSN: 1432-0738

Keywords: Trimethylphosphorothioates ; Triethylphosphorothioates ; Rat ; LD50 ; Lung damage

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Abstract The acute toxicity of trimethyl and triethylphosphorothioates present as impurities in technical organophosphorus insecticides has been examined in rats. Although the majority of these compounds caused cholinergic signs, in some a second phase of toxicity affecting the lung was also seen. Rats after recovering from the cholinergic phase of poisoning showed respiratory distress and died 3–6 days after dosing with a massive increase in lung weight, associated with progressive diffuse interstitial thickening maximal on day 4. For two compounds no cholinergic toxicity was observed and narcosis was the predominant sign of poisoning. Pretreatment with phenobarbitone, piperonyl butoxide or SKF525A protected rats against lung toxicity caused by trimethylphosphorothioate and dithioate but only phenobarbitone was effective against OOS-triethylphosphorothioate lung toxicity. Direct intrabronchial instillation of OSS-trimethylphosphorodithioate and OOS-triethylphosphorothioate, both of which had been shown to cause lung damage after other routes of dosing, did not greatly increase the toxicity of these two compounds, suggesting that they are not directly toxic to the lung and probably require metabolism.

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URL: http://dx.doi.org/10.1007/BF00348854

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118

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Kinetics of furosemide in children with chronic renal failure undergoing regular haemodialysis (1982)

Riva, E. ; Fossali, E. ; Bettinelli, A.

Springer

European journal of clinical pharmacology 21 (1982), S. 303-306

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ISSN: 1432-1041

Keywords: furosemide ; renal failure ; haemodialysis ; pharmacokinetics ; children ; dosage schedule

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Furosemide was measured by gas-liquid chromatography in blood and dialysis fluid from 7 children with chronic renal failure, undergoing regular haemodialysis. It was administered chronically, in two or three daily doses (4.2–9.4 mg/kg). Two children received 1 mg/kg intravenously for determination of the pharmacokinetics. The half-life was longer than in adults and in anephric patients on haemodialysis. Systemic and renal clearance were also much lower. Plasma protein binding in 2 out of 6 cases was reduced as campared to normal adults. The data do not suggest any need to modify the present dosage schedule despite the 4–5 fold increase in the half-life of furosemide. The contribution of haemodialysis to drug clearance was minimal, and accounted for less than 10% of the total clearance.

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URL: http://dx.doi.org/10.1007/BF00637617

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The pharmacokinetics of diclofenac sodium in patients with active rheumatoid disease (1982)

Crook, P. R. ; Willis, J. V. ; Kendall, M. J. ; [et al.]

Springer

European journal of clinical pharmacology 21 (1982), S. 331-334

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ISSN: 1432-1041

Keywords: diclofenac sodium ; rheumatoid disease ; healthy subjects ; serum albumin ; pharmacokinetics

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Pharmacokinetic data for diclofenac sodium has been well established in healthy volunteers, whereas in patients with rheumatoid arthritis very little information is available in the literature. A single oral dose of enteric-coated diclofenac sodium was given to 10 patients with active rheumatoid disease, adopting the same procedures used for a group of 10 healthy volunteers in whom pharmacokinetic data was already available. Plasma specimens were collected over a period of 8h following administration and concentrations of diclofenac determined by GLC. Resulting plasma concentration curves were similar to those obtained in the healthy subjects in that areas under curves and terminal half-lives were comparable. However, peak concentrations of diclofenac were significantly reduced in the rheumatoid patients. The lower peak concentrations were correlated with the lower serum albumin levels in the patients which are associated with active rheumatoid disease.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00637622

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Pharmacokinetic aspects of caffeine in premature infants with apnoea (1982)

Gorodischer, R. ; Karplus, M.

Springer

European journal of clinical pharmacology 22 (1982), S. 47-52

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ISSN: 1432-1041

Keywords: apnoea ; caffeine ; premature infants ; pharmacokinetics

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics of caffeine was examined in 13 premature infants (gestational age 25–34 weeks, birth weight 920–2060 g, postnatal age 1–42 days) who received the drug for treatment of opnoea. Caffeine (1% aqueous solution) was given i.v. in single doses; guided by the clinical response infants received between one and seven (mean 2.6) doses of 15 mg/kg. Mean (± SE; range) Clb was extremely slow − 8.5 ml/kg/h (±0.4; 5.8–12.2), t1/2 was prolonged − 65.0 h (±3.7; 48.2–87.5 h) and Vd was 0.781/kg (±0.04; 0.47–1.01). No significant correlation was found between Clb, t1/2 and postnatal age in the whole group or in individual infants. Effective plasma concentrations varied over a wide range (12–36 µg/ml) and overlapped with subtherapeutic concentrations (⩽24 µg/ml). Single doses of 15 mg/kg i.v. or p.o. prevented apnoea in most cases, if necessary followed by additional doses. Monitoring the blood level of caffeine in infants receiving frequent repeated doses is necessary to prevent toxicity.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00606424

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Pharmacokinetics of chlorpheniramine after intravenous and oral administration in normal adults (1982)

Huang, S. M. ; Athanikar, N. K. ; Sridhar, K. ; [et al.]

Springer

European journal of clinical pharmacology 22 (1982), S. 359-365

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ISSN: 1432-1041

Keywords: chlorpheniramine ; pharmacokinetics ; oral absorption ; half-life ; bioavailability ; volume of distribution

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Plasma and urinary levels of chlorpheniramine (CPM) and its 2 demethylated metabolites were measured by HPLC after i.v. and oral dosing. In 5 mg (maleate) i.v. bolus studies in 2 subjects, plasma CPM levels were fitted to triexponential equations with terminal half-lives (t 1/2) of 23 and 22 h and area of 3.6 and 3.21/kg, respectively. Intravenous data predicted hepatic blood extraction ratios for the 2 subjects to be 0.06 and 0.07, respectively. Absolute bioavailability from oral solution (10 mg) was 59 and 34%, and from tablets (8 mg) 44 and 25%, respectively, indicating extensive gut first-pass metabolism. Mean t 1/2 from 7 oral fasting studies in 5 subjects was 28 h (19–43 h). Mean absorption lag time was 0.7 h (0.4–1.3 h), and mean peak time was 2.8 h (2–4 h). In 2 subjects, 6 mg solutions were given every 12 h for 9 doses; good correlation between single and multiple dose kinetics was found. Significant accumulation was demonstrated in simulation studies with frequent daily dosing. Estimated accumulation ratios vary from 4.1 to 9.4 (mean 6.5). The t 1/2 from urinary data (collected for 12 days) was consistent with plasma data. The above results suggest the need to reexamine the current practice of frequent daily dosing and the use of sustained or controlled release dosage forms of this drug. The possible cause of reduced plasma clearance of CPM in renal patients is discussed.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00548406

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The clinical pharmacology of tolmesoxide (1982)

O'Boyle, C. P. ; Laher, M. ; O'Brien, E. T. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 93-97

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ISSN: 1432-1041

Keywords: tolmesoxide ; vasodilator ; hypertension ; pharmacokinetics ; haemodynamics ; plasma renin activity

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The haemodynamic response and pharmacokinetics of single dose oral tolmesoxide were studied at various dose levels in 4 patients with severe hypertension. There was a reproducible fall in mean arterial pressure from baseline of 24.2% and a rise in heart rate of 37.6% following administration of tolmesoxide. The onset of antihypertensive action occurred within 1 h, with a peak effect at 3 h after dosing. The mean duration of action was up to 12.0 h. Tolmesoxide had a mean half-life of 3.0 h. It was rapidly absorbed with a mean peak plasma level occurring at 1.0 h. Plasma levels correlated well with the doses administered. Side-effects included mild nausea, facial flushing and postural symptoms.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00545961

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123

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Variability of beta-blocker pharmacokinetics in young volunteers (1982)

Jack, D. B. ; Quarterman, C. P. ; Zaman, R. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 37-42

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ISSN: 1432-1041

Keywords: metoprolol ; propranolol ; oxprenolol ; pharmacokinetics ; acetubolol ; diacetolol ; oral contraceptive

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Plasma concentrations of metoprolol, propranolol oxprenolol, acebutolol and its metabolite diacetolol were measured after single oral doses in young healthy volunteers. In order to assess the inter-and intra-subject variability the following pharmacokinetic parameters were compared: AUC o 24 , Cmax, tmax and t1/2. The smallest variation in inter-subject variability was seen with oxprenolol and acebutolol: intrasubject variability was more uniform. Female volunteers taking an oral contraceptive generally had higher AUC o 24 and Cmax values than those not. This finding reached statistical significance only for metoprolol AUC o 24 .

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01061375

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Clinical pharmacokinetics of verapamil in patients with atrial fibrillation (1982)

Anderson, P. ; Bondesson, U. ; Sylvén, C.

Springer

European journal of clinical pharmacology 23 (1982), S. 49-57

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ISSN: 1432-1041

Keywords: verapamil ; norverpamil ; pharmacokinetics ; atrial fibrillation ; oral administration ; i.v. administration

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetic parameters and oral bioavailability of the antiarrhythmic drug verapamil were determined in six patients with atrial fibrillation. Plasma samples were taken following i.v. injection of verapamil 10 mg (Isoptin® 2 ml), and oral verapamil 80 mg (Isoptin® 2 tablets of 40 mg). Verapamil and its N-demethylated metabolite, norverapamil, were analyzed to 1 ng/ml plasma by gas chromatography-mass spectrometry using deuterated standards. Following intravenous injection, the disposition of verapamil followed a biexponential pattern with a fast distribution phase and a slower elimination phase (t1/2β=5.79 h), corresponding to a plasma clearance of 0.26 1/kg/h. After oral administration, only an elimination phase was evident, with the same elimination rate (t1/2β=5.53 h). The oral bioavailability was 10.5%±7.5%. The norverapamil formed after i.v. and oral administration of verapamil had plasma half-lives of 5.86 h and 6.77 h, respectively. The elimination of verapamil in patients with atrial fibrillation was decreased compared to that in healthy young volunteers and the oral bioavailability was lower. Very good correlation between the percentage reduction in heart rate and the log plasma concentration of verapamil was found in every patient during the elimination phase, irrespective of the route of administration. There was also a high correlation when the plasma concentration — effect data from all the patients were pooled (r=0.59,n=71;p〈0.0005).

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01061377

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Pharmacokinetics of theophylline in infants with bronchiolitis (1982)

Franko, T. G. ; Powell, D. A. ; Nahata, M. C.

Springer

European journal of clinical pharmacology 23 (1982), S. 123-127

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ISSN: 1432-1041

Keywords: theophylline ; bronchiolitis ; infants ; pharmacokinetics ; single dose ; multiple doses ; HPLC

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Theophylline pharmacokinetics were studied in 12 infants (age 3 weeks–6.5 months) with bronchiolitis. 9 of the 12 patients received a single dose of aminophylline (5.0–8.5 mg/kg) whereas the remainder were at steady-state receiving multiple doses (2.5–5.0 mg/kg) of aminophylline. The dose was administered IV over 0.5–1.0 h. An HPLC method was used to measure theophylline concentrations in serum and urine. Peak serum concentrations of theophylline measured by HPLC ranged from 8.48–21.6 µg/ml. Total, renal and nonrenal clearance of theophylline ranged from 4.66 to 19.25, 1.07 to 5.76 and 3.59 to 16.83 ml/min/m2, respectively. Mean apparent volume of distribution and elimination half-life were 8.75 l/m2 and 11.38 h, respectively. Although no significant correlation was observed between age and theophylline kinetic parameters, clearance appeared to increase and half-life decrease with age. Our patients had a substantially lower clearance and longer half-life as compared to published data in children 〉1 year of age. A five-fold variation in theophylline clearance demonstrates the need for monitoring theophylline serum concentration to minimize the risk of potential toxicity.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00545965

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Effect of chronic oral contraceptive steroids on theophylline disposition (1982)

Tornatore, K. M. ; Kanarkowski, R. ; McCarthy, T. L. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 129-134

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ISSN: 1432-1041

Keywords: theophylline ; ethinylestradiol ; oral contraceptives ; pharmacokinetics

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The effect of chronic oral contraceptive (OC) usage on the disposition of theophylline was examined. Aminophylline solution (4 mg/kg) was given orally to 8 healthy female non-OC users and to 8 healthy women who were chronic (〉6 months) OC users. The OC user group had a significantly lower total plasma clearance of theophylline than women not using OC (35.1±5.6 vs. 53.1±14.5 ml/h/kg). The t1/2 was also significantly prolonged in the OC group (9.79±1.43 vs. 7.34±1.75 h) while the volume of distribution was similar between the 2 groups. The serum ethinylestradiol (EE) concentrations after oral OC administration were measured simultaneously. The apparent clearance of EE was about 30% lower in the OC users. A significant positive correlation was found between the apparent clearance of EE and the plasma clearance of theophylline. The effects of OC are predominantly due to chronic use with decreased elimination of both theophylline and EE.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00545966

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Pharmacokinetics of ticarcillin in man (1982)

Davies, B. E. ; Humphrey, M. J. ; Langley, P. F. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 167-172

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ISSN: 1432-1041

Keywords: ticarcillin ; probenecid ; excretion ; pharmacokinetics ; automated chemical assay method

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The excretion of radioactivity has been investigated in 3 healthy volunteers following rapid intravenous administration of 5 g of [35S]-ticarcillin. The radioactive dose was rapidly and completely excreted, since within 4 days 98.5% was recovered, 95% in the urine and 3.5% in faeces. All the urine radioactivity was accounted for as ticarcillin and its penicilloic acid. Plasma and urine samples collected from the volunteers at frequent intervals during the first 6 h of the experiment were assayed for penicillin by an automated chemical method and also for radioactivity. The results obtained by the chemical autoanalyser method were in excellent agreement with the plasma levels of radioactivity. From the data it was possible to calculate the renal clearance of the penicillin, a mean value of 104 ml/min was observed in the 3 volunteers. A further three volunteers were dosed intravenously with a 5 g bolus of non-radiolabelled ticarcillin in a cross-over study with and without predosing with probenecid. Serum samples were analysed by the chemical method for penicillin and the data subjected to pharmacokinetic analysis using a two compartment open model. The results indicate a shift of the distribution equilibrium of ticarcillin from the serum into the peripheral compartment after predosing with probenecid. Furthermore, the mean half-life of ticarcillin in the serum of the three volunteers was significantly increased from 1.3 h to 2.1 h by predosing with probenecid.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00545973

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Pharmacokinetics of oral dipyridamole (Persantine®) and its effect on platelet adenosine uptake in man (1982)

Dresse, A. ; Chevolet, C. ; Delapierre, D. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 229-234

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ISSN: 1432-1041

Keywords: dipyridamole ; platelets ; plasma levels ; pharmacokinetics ; adenosine uptake

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Two preparations of dipyridamole have been studied by oral administration to 11 normal volunteers. The plasma levels of dipyridamole and its glucuronide were determined simultaneously by high performance liquid chromatography. The instant form (I.F., 100 mg) was administered four times daily and the slow release preparation (SRP, 200 mg) twice daily, for 3 days. Multiple blood samples were collected on Days 1–4 to provide plasma for assay, and simulteneously, platelet rich plasma was prepared for ex vivo study of the effect of dipyridamole on platelet uptake of adenosine. The pharmacokinetics of absorption and distribution of dipyridamole were described using a two compartment model with lag time and prolonged absorption. Strong inhibition of the platelet adenosine uptake was observed at therapeutic plasma levels. The inhibition of platelet adenosine uptake may be related to some of the pharmacological properties of dipyridamole.

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URL: http://dx.doi.org/10.1007/BF00547559

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Pharmacokinetics and tolerance of slow-release indomethacin tablets in rheumatoid arthritis (1982)

Kaarela, K. ; Lehtinen, K. ; Mäkisara, P. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 349-351

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ISSN: 1432-1041

Keywords: indomethazine ; rheumatoid arthritis ; pharmacokinetics ; tolerance ; side effects ; slow-release tablets

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics, efficacy and tolerance of a new formulation of slow-release indomethacin tablet were compared with those of a conventional indomethacin capsule in 30 patients with rheumatoid arthritis. The slow-release tablet was absorbed more slowly than the capsule (tmax 3.7 h and 〈 2 h, respectively) and produced more even serum drug levels in 10 subjects. Side-effects, especially dizziness and diarrhoea, were less frequent after the slow-release tablet than during the capsule period.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00613619

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Pharmacokinetics of3H-phenylephrine in man (1982)

Hengstmann, J. H. ; Goronzy, J.

Springer

European journal of clinical pharmacology 21 (1982), S. 335-341

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ISSN: 1432-1041

Keywords: phenylephrine ; pharmacokinetics ; bioavailability ; first-pass metabolism ; phenolic conjugates ; m-hydroxymandelic acid ; intravenous ; oral

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary 7-3H-phenylephrine was given to 15 volunteers by a short-infusionn=4) or p.o. (10 volunteers, 1 patient with porto-caval anastomosis). Analysis of serum for free3H-phenylephrine and fractionation of urinary radioactivity was performed by ion-exchange and thin-layer chromatography. As almost the same3H-activity was excreted in urine after i.v. and p.o. administration, 86% and 80% of the dose respectively, complete enteral absorption can be assumed. A considerable difference was seen in the fraction of free phenylephrine, i.v. 16% of the dose versus p.o. 2.6%, which suggested reduced bioavailability. This was confirmed by comparison of the areas under the serum curve, which showed a bioavailability factor of 0.38. The result for the patient with porto-caval anastomosis was comparable to that in the normal volunteers. The biological half-life of 2 to 3h was comparable to that of structurally related amines, as were the total clearance of 2 1/h, and the volume of distribution of 340l. Metabolism to phenolic conjugates mainly after oral ingestion, and tom-hydroxymandelic acid after i.v. injection, again demonstrated thatm-hydroxylated amines are predominantly conjugated during the “first-pass” metabolism.

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URL: http://dx.doi.org/10.1007/BF00637623

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Pharmacokinetics of furosemide in patients with hepatic cirrhosis (1982)

González, G. ; Arancibia, A. ; Rivas, M. I. ; [et al.]

Springer

European journal of clinical pharmacology 22 (1982), S. 315-320

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ISSN: 1432-1041

Keywords: furosemide ; cirrhotic patients ; ascitic fluid ; diuretic effect ; pharmacokinetics ; healthy volunteers

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics of furosemide was studied in 7 patients with diagnosed liver cirrhosis and in 7 healthy subjects. Furosemide in plasma and ascitic fluid was analyzed spectrofluorometrically. After a single intravenous dose, the cirrhotic patients showed lower initial plasma concentrations of furosemide because of the larger volume of distribution. The mean half-life in cirrhotic patients was significantly greater than in healthy volunteers. The longer half-life was associated with a reduction in the serum clearance of furosemide. Ascitic fluid volume in the patients ranged from 4.6 to 7.71. There was no significant amount of furosemide in the fluid. The diuretic interchange between this fluid and plasma was slow, as peak concentrations ranged from 0.3 to 0.5 µg/ml within 3 to 5 h after bolus administration of furosemide. Diuresis and urinary sodium excretion, 5 h after furosemide injection, were similar in both groups; larger potassium excretion was found in the cirrhotic patients.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00548399

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Pharmacokinetics of cimetidine and its sulphoxide metabolite during haemodialysis (1982)

Larsson, R. ; Erlanson, P. ; Bodemar, G. ; [et al.]

Springer

European journal of clinical pharmacology 21 (1982), S. 325-330

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ISSN: 1432-1041

Keywords: cimetidine ; renal failure ; cimetidine sulphoxide ; pharmacokinetics ; haemodialysis

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary A single intravenous dose of cimetidine 200mg was administered to 6 patients with severe chronic renal failure one hour prior to haemodialysis. The plasma concentrations of cimetidine and its sulphoxide metabolite at the start of haemodialysis were 2.74±0.12 and 0.76±0.08 µg/ml, and after dialysis for 4h 1.08±0.10 and 0.51±0.08 µg/ml, respectively (mean ± SE). The average haemodialysis clearance (ClHDa) of cimetidine during dialysis was 46–92ml/min at a dialysate flow rate of 320ml/min and blood flow rates in the 6 patients between 160–240ml/min. The mean ClHDa of the sulphoxide metabolite was 44% higher than that of cimetidine, and ranged between 49–148ml/min. During haemodialysis the mean plasma elimination half-life (t1/2) of cimetidine was 3.24h (range 2.08–5.08) and of the sulphoxide metabolite 9.49h (range 4.70–14.39). There was a significant relationship between the elimination rate constant (β) and ClHDa of the sulphoxide metabolite (p〈0.01), but no such relationship was found between β and ClHDa of cimetidine. However, there was a tendency to a relationship between β of cimetidine and the capacity to metabolise the drug, expressed as the ratio between the plasma concentrations of the sulphoxide metabolite and cimetidine after dialysis for 4h. These ratios ranged between 0.23–0.76, and the lowest ratio was seen in the patient with the lowest β value of cimetidine. Thus, the large variations in the plained by differences in their capacity to metabolise the drug. The mean total amount of cimetidine eliminated during dialysis was 27.3mg (range 17.9–31.8), which was 9.0–15.9% of the given dose. Between 12.2–21.2mg (mean 15.3) of the sulphoxide metabolite was eliminated in the dialysate. Major adjustment of the dose of cimetidine on days of dialysis is not necessary.

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URL: http://dx.doi.org/10.1007/BF00637621

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Distribution of lithium elimination rates in a selected population of psychiatric patients (1982)

Thornhill, D. P. ; Field, S. P.

Springer

European journal of clinical pharmacology 21 (1982), S. 351-354

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ISSN: 1432-1041

Keywords: lithium ; plasma level decay curve ; elimination ; pharmacokinetics ; psychiatric patients

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Chronic treatment with conventional lithium carbonate was interrupted in a selected group of 40 psychiatric patients of mixed sex and race. All patients had normal renal function. Serum samples were taken 12, 24, 36 and 48 h after the last dose and lithium was assayed by atomic absorption spectrophotometry. Decay rates calculated for the 12–24 h and 36–48 h periods yielded different values. This was ascribed to the presence of an incomplete redistribution phase during the earlier period. The distribution of elimination rates determined during the later period gave a more symmetrical spread and approximated a normal distribution. The mode, median, mean and standard deviation of the lithium elimination half-lives were 12.5, 14, 18.2 and 7.3 h and 22.5, 24.5, 29.8 and 10.1 h for the two periods, respectively. The results contrast sharply with another report of the distribution spread of elimination half-lives in a much larger sample. The current values have implications for dosage prediction, serum level monitoring and dosage formulation, especially sustained-release preparations. The evidence was against the possibility that some individuals ‘retain’ lithium.

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URL: http://dx.doi.org/10.1007/BF00637625

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Pharmacokinetics of propranolol and sotalol in hyperthyroidism (1982)

Aro, A. ; Anttila, M. ; Korhonen, T. ; [et al.]

Springer

European journal of clinical pharmacology 21 (1982), S. 373-377

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ISSN: 1432-1041

Keywords: propranolol ; sotalol ; thyrotoxicosis ; bioavailability ; serum tri-iodothyronine ; pharmacokinetics

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The elimination and bioavailability of two beta-blocking agents, propranolol and sotalol, were studied in 10 thyrotoxic patients, both before and after treatment with iodine-131. Each subject received in random order propranolol 160 mg and sotalol 160mg as single oral doses both while hyperthyroid and after euthyroidism had been achieved. The pharmacokinetics of sotalol was not affected by hyperthyroidism, whereas serum propranolol concentrations were significantly lower during hyperthyroidism than in the euthyroid state. During hyperthyroidism, the bioavailability of propranolol was significantly reduced (p〈0.05) and its clearance was increased (p〈0.005), whereas there was no difference in its serum t1/2. This indicates that the bioavailability of propranolol in hyperthyroidism is reduced by a mechanism which may depend on increased first-pass metabolism in the liver, or on an increased distribution volume of the drug. Both propranolol and sotalol caused a slight decrease in serum tri-iodothyronine concentration. As the effects of beta-blocking agents on the symptoms of hyperthyroidism are correlated with the serum concentration of the drugs, sotalol, with its long half-life and unaltered elimination in hyperthyroidism, has certain advantages over propranolol in the treatment of thyrotoxicosis.

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URL: http://dx.doi.org/10.1007/BF00542321

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Studies of the different metabolic pathways of antipyrine in man (1982)

Danhof, M. ; Zuilen, A. ; Boeijinga, J. K. ; [et al.]

Springer

European journal of clinical pharmacology 21 (1982), S. 433-441

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ISSN: 1432-1041

Keywords: antipyrine ; antipyrine metabolites ; drug metabolism ; route of administration ; healthy volunteers ; urinary excretion ; pharmacokinetics

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics of antipyrine in plasma and saliva, and urinary excretion of its major metabolites, were studied following i.v. and oral administration of antipyrine 500 mg to 6 healthy volunteers. Data from both plasma and saliva showed that the oral bioavailability of antipyrine given as an aqueous solution was complete. The saliva/plasma concentration ratio was constant with time from about 3 h onwards, with a mean value of 0.87 after oral and 0.91 after i.v. administration. It is concluded that the pharmacokinetic parameters of antipyrine can be satisfactorily established on the basis of salivary data, although the volume of distribution and clearance values are then slightly too high. After i.v. administration, 3.8±1.9% of the dose was excreted in urine as unchanged antipyrine in 48h, 24.9±6.3% as 4-hydroxyantipyrine, 16.5±3.2% as norantipyrine, 13.0±2.2% as 3-hydroxymethyl-antipyrine and 5.8±1.0% as 3-carboxy-antipyrine. No significant differences were observed following oral administration. The half-lives calculated from the linear part of the urinary excretion rate curves of the metabolites were about the same for oral and i.v. administration, and were of the same order of magnitude as the elimination half-life of parent drug in plasma and saliva. It is important for determination of the ultimate metabolite ratio that urine is collected for at least 36h, because there is a delay in the excretion of 3-hydroxymethyl-antipyrine in urine.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00542332

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Relationship between the plasma concentration of clomipramine and desmethylclomipramine in depressive patients and the clinical response (1982)

Vandel, B. ; Vandel, S. ; Jounet, J. M. ; [et al.]

Springer

European journal of clinical pharmacology 22 (1982), S. 15-20

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ISSN: 1432-1041

Keywords: clomipramine ; desmethylclomipramine ; depressive syndrome ; plasma level ; pharmacokinetics ; clinical response ; benzodiazepines

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Thirty one in-patients suffering from depression were treated orally with clomipramine (Cl) at various dosage, for 28 days, after a “wash-out” period of three days. In 17 patients receiving 75 mg per day of Cl, steady state plasma levels of Cl were reached at Day 14, and steady state plasma levels of its active metabolite, desmethylclomipramine (DMCl), were reached at Day 21. In contrast, in 7 other patients receiving a dosage increasing to 150 mg per day at Day 7, mean plasma levels of Cl and DMCl continued to rise during the entire treatment period. At the steady state, a correlation was found between Cl dosage expressed as mg kg body weight and the plasma concentration of Cl and DMCl. Factors such as tobacco and alcohol consumption seem to modify the Cl/DMCl ratio. A comparison of clinical response with plasma levels of Cl, DMCl and Cl + DMCl showed a significant negative linear correlation.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00606419

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Kinetics of allopurinol after single intravenous and oral doses (1982)

Breithaupt, H. ; Tittel, M.

Springer

European journal of clinical pharmacology 22 (1982), S. 77-84

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ISSN: 1432-1041

Keywords: allopurinol ; oxipurinol ; benzbromarone ; hydrochlorothiazide ; pharmacokinetics ; bioavailability ; interaction

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary An high-pressure liquid chromatographic method was used to measure allopurinol and oxipurinol in plasma and urine in 6 healthy volunteers after a single intravenous or oral dose of allopurinol. The influence of coadministrated benzbromarone and hydrochlorothiazide on the pharmacokinetics of allopurinol and oxipurinol was also investigated. After intravenous injection of allopurinol 300 mg the plasma disappearance was biexponential, with a mean distribution half-life of 2.32±1.08 min $$(\bar x \pm SD)$$ and an elimination half-life of 47.8±10.6 min. The total clearance of allopurinol was 11.37±2.70 ml/min/kg, whereas its renal clearance was only 1.73±0.79 ml/min/kg. Oxipurinol disappeared monoexponentially from plasma ith a mean half-life of 12.2±2.6 h. Its renal clearance was 0.42±0.091 ml/min/kg. After oral administration of allopurinol 300 mg the peak plasma concentration of 2.1±0.6 µg/ml (1.5×10−5 M) was reached within 30 to 120 min. The peak level of oxipurinol of 5.8±1.5 µg/ml (3.8×10−5 M) was found within 2 to 5 h after intravenous and oral allopurinol. The bioavailability of oral allopurinol computed from plasma data was 90.4±8.7%. The total recovery from urine was 77% (allopurinol 8%, oxipurinol 69%) after oral and 88% after i.v. administration. It was concluded that about 10% of the oral dose was not absorbed and that 12% was eliminated by an unknown mechanism, presumably as riboside. The pharmacokinetics of allopurinol and oxipurinol were not significantly influenced by coadministration of benzbromarone or hydrochlorothiazide.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00606429

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Pharmacokinetics of methadone during maintenance treatment: Adaptive changes during the induction phase (1982)

Nilsson, M. -I. ; Änggård, E. ; Holmstrand, J. ; [et al.]

Springer

European journal of clinical pharmacology 22 (1982), S. 343-349

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ISSN: 1432-1041

Keywords: methadone ; opiate addicts ; pharmacokinetics ; single and multiple doses ; stable isotope technology ; methadone maintenance therapy ; deuterium technique

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Deuterated methadone (M-d30) and GC-MS were used to study the pharmacokinetics of methadone (M) during the induction stage of methadone maintenance treatment (MMT). A pulse dose of M-d3 was given on Days 1 and 25 of two dosage regimens, one with a continuous 30 mg dose (n=6), and the other with 30 mg for 10 days, followed by 60 mg as the maintenance dose (n=6). Plasma and urinary levels of M and M-d3 were measured throughout and plasma half-lives, oral bioavailabilities and volumes of distribution were calculated from the data of Days 1–2 and 24–26. The oral bioavailability of a methadone solution was found to be between 81 and 95%; elimination half-life in the β-phase varied between 19 and 58 h; the volume of distribution was 4.1±0.65 l/kg; and total body clearance of M was 54–195 ml/min and its renal clearance 3.4–34 ml/min. A consistent finding was a lower urinary pH and increased renal clearance during the first days of MMT as compared with after one month. In 4/12 of the patients dispositional tolerance was developed to methadone during the first month of treatment. The shorter elimination half-lives in those patients probably caused unacceptably high fluctuation in the body content of M during the 24 h dosage interval, and may have interfered therefore, with its therapeutic effectiveness

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00548404

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Pharmacokinetic and pharmacodynamic studies of tienilic acid in healthy volunteers (1982)

Kerremans, A. L. M. ; Gribnau, F. W. J. ; Tan, Y. ; [et al.]

Springer

European journal of clinical pharmacology 22 (1982), S. 515-521

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ISSN: 1432-1041

Keywords: tienilic acid ; uricosuria ; pharmacokinetics ; pharmacodynamics ; uric acid ; diuretic ; plasma level assay

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary A simple and reliable HPLC method for the determination of tienilic acid ((TA) Selacryn®, Selcryn®, Diflurex®, Ticrynafen®) and its alcoholic metabolite in plasma and urine has been developed. In 8 healthy adult volunteers the plasma and urinary levels of tienilic acid and its alcoholic metabolite, and plasma and urinary levels of sodium, creatinine and uric acid were measured after oral administration of tienilic acid 250 mg. The pharmacokinetic parameters found differed only slightly from those reported in the literature, as there was faster absorption and a shorter half-life. TA is probably excreted by a saturable renal tubular transport mechanism. The pharmacodynamic effects of tienilic acid developed quickly, the uricosuric effect being very impressive and the natriuretic effect moderate. These effects disappeared in about 8 h. An inverse relationship was found between the starting plasma uric acid level in an individual and the maximal uric acid clearance — the higher the plasma uric acid level, the lower was the maximum effect. Plasma tienilic acid level and natriuretic effect were correlative within individuals and intra-individually (p〈0.05). Urinary tienilic acid level and natriuretic effect were correlated, too (p〈0.05 top〈0.001), but only intraindividually. No correlation between drug level and uricosuric effect was found.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00609624

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140

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Pharmakokinetic properties of noscapine (1982)

Dahlström, B. ; Mellstrand, T. ; Löfdahl, C. -G. ; [et al.]

Springer

European journal of clinical pharmacology 22 (1982), S. 535-539

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ISSN: 1432-1041

Keywords: noscapine ; pharmacokinetics ; absorption ; bioavailability ; intravenous application ; oral application ; ion exchange resin tablet

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Noscapine was administred to five healthy volunteers in a randomized crossover design, as an intravenous infusion of 66 mg, and as an oral 150 mg dose of either rapidly dissolving tablets or a tablet containing ion exchange resin-bound noscapine. After i.v. administration, the disposition of noscapine was bi-exponential with an elimination half-life of 2.6 h; the total plasma clearance was 22 ml/min/kg and the volume of distribution (Vdarea) was 4.7 l/kg. The absolute oral bioavailability was 30%, with a 3.6-fold interindividual variation. There was no pharmacokinetic evidence to support a prolonged action of the ion exchange resin tablet.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00609627

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Pharmacokinetics of theophylline in patients following short-term intravenous infusion (1982)

Steinijans, V. W. ; Eicke, R. ; Ahrens, J.

Springer

European journal of clinical pharmacology 22 (1982), S. 417-422

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ISSN: 1432-1041

Keywords: theophylline ; aminophylline ; obstructive airways disease ; short-term i.v. infusion ; log-normal distribution ; pharmacokinetics ; serum concentrations

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Serum theophylline concentrations after intravenous administration of a new short-term infusion (Euphyllin® Kurzzeitinfusion) were measured in 50 out-patients with chronic obstructive airways disease (COAD). An intravenous infusion of theophylline ethylenediamine 480 mg (corresponding to approximately 350 mg anhydrous theophylline) in 50 ml isotonic solution was given in 20 min. Blood samples were taken beforehand and 25 to 30 min and 1, 3 and 6 h after starting the infusion. 86% of the patients had a one-hour serum level in the therapeutic range of 8–20 mg/l, and 2 h later, this was true of 64% of the patients. The short-term infusion was well tolerated, even in cases with unknown high pre-infusion serum levels. Pertinent pharmacokinetic parameters were determined, such as total body clearance, apparent volume of distribution, and half-life of elimination. Geometric mean and 95%-confidence limits, derived from the log-normal distribution of these parameters, were: Cl=0.044 (0.018–0.109) l/h/kg ideal body weight, Vd=0.451 (0.258–0.789) l/kg ideal body weight, and t1/2(el)=7.1 (2.6–19.1) h.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00542546

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Pharmacokinetics of bacmecillinam and pivmecillinam in volunteers (1982)

Josefsson, K. ; Bergan, T. ; Magni, L. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 249-252

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ISSN: 1432-1041

Keywords: mecillinam ; bacmecillinam ; pivmecillinam ; pharmacokinetics ; pro-drug ; healthy volunteers ; bioavailability

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics of bacmecillinam and pivmecillinam were studied in healthy fasting volunteers given tablets in a cross-over, randomized order. The mean (±SD) peak levels of plasma mecillinam were 1.43±0.34, 2.73±0.43, and 4.62±1.41 mg/l after bacmecillinam 100, 200, and 400 mg and 2.38±0.65 mg/l after pivmecillinam 400 mg. The corresponding areas under plasma Vs time curves (AUC) were 2.21±0.19, 3.99±0.63, and 7.74±1.38 mg·h·l−1 for bacmecillinam and 5.35±0.93 mg·h·l−1 for pivmecillinam. The elimination half-lives were 0.8–1.1h for bacmecillinam and 0.7h for pivmecillinam. The 12 h urinary recovery of unchanged mecillinam after the 400 mg doses was 41% for bacmecillinam and 30% for pivmecillinam. The 400 mg dose of bacmecillinam gave a significantly higher plasma peak (p〈0.001), AUC (p〈0.001) and urinary recovery (p〈0.001) than did pivmecillinam 400 mg. The plasma peaks appeared earlier and the rate of absorption was higher after bacmecillinam than after pivmecillinam (p〈0.05). In conclusion, bacmecillinam had a better bioavailability than pivmecillinam in the tablet formulations studied. The AUC increased linearly with increasing doses of bacmecillinam.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00547563

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Pharmacokinetics of terodiline in human volunteers (1982)

Karlén, B. ; Andersson, K. -E. ; Ekman, G. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 267-270

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ISSN: 1432-1041

Keywords: terodiline ; human volunteers ; pharmacokinetics ; serum clearance ; bioavailability

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics of terodiline HCl was studied in nine healthy volunteers given 12.5 mg i.v. and p.o. or 20 mg i.v. and 25 mg p.o. on two different occasions. The serum concentrations were measured by gas chromatography — mass spectrometry, using deuterated terodiline HCl as the internal standard. After i.v. administration the kinetics could be described by a two-compartment model with a mean distribution half life of 0.3 h and a mean elimination half life of 63 h. The serum clearance and apparent volume of distribution varied about 4-fold with mean values of 4.8 l/h and 417 l, respectively. After oral administration, the mean half life of absorption was 0.7 h and that of elimination 65 h. The absolute bioavailability varied between 64% and 105% with a mean of 92%. The long serum half life of terodiline should permit its once daily administration.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00547566

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Pharmacokinetics of pancuronium in man: A linear system (1982)

Duvaldestin, P. ; Demetriou, M. ; D'Hollander, A.

Springer

European journal of clinical pharmacology 23 (1982), S. 369-372

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ISSN: 1432-1041

Keywords: neuromuscular blockade ; pancuronium ; non-depolarizing neuromuscular blocking agent ; pharmacokinetics

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Pancuronium in bolus doses of 40 to 350 µg/kg was administered to surgical patients in order to evaluate the linearity of its pharmacokinetics. The profile of the plasma decay curve and of its urinary elimination were compared with reference to the administered dose. It was possible to superimpose the dose-normalized plasma decay-curves. The parameters of the two compartment-open model used to describe the pharmacokinetics of pancuronium were not influenced by the dose. The elimination half-life was 89±20 min and the plasma clearance was 1.84±0.38 ml/min/kg. The profiles of cumulative urinary excretion were also dose-independent. After 6 and 24 h, 57% and 69% of the administered dose, respectively, had been excreted in the urine. The results indicate that the pharmacokinetics of pancuronium is linear.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00613623

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Influence of acetylator phenotype on the pharmacokinetics of a new vasodilator antihypertensive, endralazine (1982)

Reece, P. A. ; Cozamanis, I. ; Zacest, R.

Springer

European journal of clinical pharmacology 23 (1982), S. 523-527

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ISSN: 1432-1041

Keywords: endralazine ; acetylator phenotype ; hydralazine ; pharmacokinetics ; plasma concentrations

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Five and 10 mg single oral doses of a new vasodilator antihypertensive, endralazine (E) were given on separate occasions to 17 normal male volunteers (8 slow, 7 heterozygous fast and 2 homozygous fast acetylators). The homozygous fast acetylators were excluded from statistical comparisons. Only small differences were observed in the pharmacokinetics of E between the phenotypes and there was no evidence of non-linearity at the 2 dose levels studied. Terminal half-lives ranged from 2.59 to 7.14 h with a mean of 4.30±1.08 h for the 5 mg dose and 4.25±1.09 h for the 10 mg dose. There was no significant difference in half-lives between slow and heterozygous fast acetylators. The mean area under the plasma level-time curve (AUC 0 ∞ ) was 18.2% lower (p〈0.05) in the heterozygous fast acetylators than in the slow acetylators following the 5 mg dose and 11.0% lower (p〉0.05) following the 10 mg dose. Extremely rapid absorption of the drug precluded accurate estimation of absorption rates. The AUC 0 ∞ of the acetylation metabolite (methyltriazoloendralazine) was small compared to that of E although higher in the heterozygous fast acetylators than in the slow acetylators (p〈0.01).

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00637500

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Estimation of absorption ratios and their variation for orally administered drugs (1982)

Betzien, G. ; Kaufmann, B. ; Schneider, B.

Springer

European journal of clinical pharmacology 22 (1982), S. 265-272

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ISSN: 1432-1041

Keywords: pharmacokinetics ; variation of absorption ratios ; bioavailability ; dissection of variation due to absorption and intermediate processes ; oral drug application

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Differences in the plasma concentrations of drugs after oral administration are caused by two main factors: variation in absorption ratios and in the distribution processes in the body. A new method for the dissection of both types of factors is discussed. The method uses a reference regression of the AUC-values to the corresponding values after intravenous infusion of graded doses. The reference regression is estimated from an appropriate trial. Deviation of the determined AUC-values from the regression curve afford an estimate of the residual variance due to varying distribution volumes or similar random biological effects. For the estimation of absorption ratios after oral administration the drug is given orally to another sample of subjects and their AUC-values are calculated. The deviation of these AUC values due to the above mentioned random effects are simulated using the residual variance of the reference regression, and are subtracted from the observed AUC-values. Then, the differences in the corresponding absorbed doses are transformed by inverting the reference regression. From these doses the empirical distribution function and statistical parameters (e.g. quantiles) are determined. The method has the advantage that no restrictive assumptions are required, such as first order processes, dose linearity, homogeneity of variance or normal distribution of absorption ratios. Its applicability to substances with qualitative differences in their pharmacokinetics is demonstrated by appropriate examples.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00545226

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Effect of urinary pH on the disposition of methadone in man (1982)

Nilsson, M. -I. ; Widerlöv, E. ; Meresaar, U. ; [et al.]

Springer

European journal of clinical pharmacology 22 (1982), S. 337-342

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ISSN: 1432-1041

Keywords: methadone ; pharmacokinetics ; urinary pH ; RBC level ; saliary level ; mass fragmentography

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The influence of urinary pH on the acute disposition of methadone in man was studied in five healthy volunteers. A cross-over experiment was performed in each subject. In the first experiment the subjects were treated with ammonium chloride (urinary pH ≈ 5.2) and in the other the urine was made alkaline (pH ≈ 7.8) by treatment with sodium hydrogen carbonate. d, 1-Methadone-HCl 10 mg (M) was administered intramuscularly on each occasion and blood, saliva and urine levels of M were determined by mass fragmentography. Plasma half-lives, volumes of distribution and body clearances of M were calculated in both experiments. The plasma half-lives in the β-phase were 19.5±3.6 h (acidic urine) and 42.1±8.8 h (alkaline urine), respectively (p〈0.001). The volumes of distribution were increased when the pretreatment was changed from ammonium chloride to sodium bicarbonate, namely from 3.51±0.41 l/kg to 5.24±0.83 l/kg (p〈0.01). The body clearance decreased from 134±21 ml/min (acidic) to 91.9±9.1 ml/min (alkaline urine) (p〈0.01). The ration Mplasma/MRBC was about 2.3 and the elimination of M from RBCs was in good agreement with the plasma kinetics of M under both experimental conditions. The salivary levels of M did not reflect the plasma kinetics and considerable variation was seen in the ratio Msaliva/Mplasma (0.26–2.98). Thus, the present experiments demonstrate that pretreatment either with ammonium chloride or bicarbonate had profound effects on both the distribution and elimination kinetics of methadone.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00548403

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Should erythromycin dose be altered in haemodialysis patients? (1982)

Iliopoulou, A. ; Downey, K. ; Chaput de Saintonge, D. M. ; [et al.]

Springer

European journal of clinical pharmacology 23 (1982), S. 435-440

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ISSN: 1432-1041

Keywords: erythromycin ; haemodialysis ; dosage adjustment ; pharmacokinetics ; protein-binding

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Erythromycin kinetics were studied in 17 patients with end stage renal failure treated with maintenance haemodialysis and 9 normal volunteers to discover if dialysis patients needed a modified dose. The elimination half life in dialysis patients (on dialysis days) was similar to that reported in normal subjects. Only small amounts of drug appeared in the dialysate, no patient loosing more than 9 mg in one dialysis. Both patients and volunteers had similar plasma concentrations 8 h after the end of a 5-day course. Protein-binding did not change significantly during dialysis and was similar to that reported in normal subjects. We conclude that dialysis patients requiring 1.5 g of erythromycin stearate daily or less can be given normal doses.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00605994

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Covalent protein binding of reactive adriamycin metabolites in rat liver and rat heart microsomes (1982)

Scheulen, M. E. ; Kappus, H. ; Nienhaus, Anne ; [et al.]

Springer

Journal of cancer research and clinical oncology 103 (1982), S. 39-48

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ISSN: 1432-1335

Keywords: Adriamycin ; Cardiotoxicity ; Covalent protein binding ; Metabolic activation ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary Covalent binding of 3H-labeled adriamycin metabolites to bovine serum albumin and microsomal protein is demonstrated in an aerobic incubation system with rat liver and rat heart microsomes, respectively, using exhaustive organic solvent extraction and gel chromatography. Covalent protein binding was dependent on active microsomes, NADPH, and oxygen and was inhibited by reduced glutathione and other sulfhydryl compounds. The anthracycline moiety was spectrophotometrically evidenced in the adriamycin metabolite(s) covalently bound to protein. Thus, enzymatic activation of adriamycin in the heart with consecutive covalent protein binding of reactive adriamycin semiquinone radicals may contribute to adriamycin cardiotoxicity.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00410304

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150

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Distribution of the liver carcinogen methapyrilene in fischer rats and its interaction with macromolecules (1982)

Lijinsky, W. ; Muschik, G. M.

Springer

Journal of cancer research and clinical oncology 103 (1982), S. 69-73

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ISSN: 1432-1335

Keywords: Methapyrilene ; Liver tumor ; Rat ; Interaction ; Radioactivity

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary The anti-histaminic drug methapyrilene hydrochloride, which induces liver tumors in rats, was labeled with tritium by exchange and administered at a dose of 21 mg containing 700 μCi to each of 15 male Fischer rats. At 1 h, 6 h, 14 h, 24 h, and 44 h after treatment three rats were killed and their livers, pancreas, kidneys, and lungs were removed. The pooled organs were homogenized and DNA, RNA, and soluble protein were isolated from each. The extent of interaction of radioactive methapyrilene with liver nucleic acids was exceedingly small and did not differ significantly from the binding to nucleic acids in kidney, lung, or pancreas, which are not target organs of this carcinogen in rats. Binding of radioactivity to soluble proteins of the liver was considerable and substantially greater than in the other organs. If the mechanism of carcinogenic action of methapyrilene involves covalent interaction with DNA this must be at a very low and highly specific level.

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URL: http://dx.doi.org/10.1007/BF00410307

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151

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Minor role of lipid peroxidation in acute bleomycin toxicity in rats (1982)

Muliawan, H. ; Burkhardt, A. ; Scheulen, M. E. ; [et al.]

Springer

Journal of cancer research and clinical oncology 103 (1982), S. 135-143

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ISSN: 1432-1335

Keywords: Bleomycin ; Lipid peroxidation ; Lung toxicity ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary Bleomycin was injected i.p. in rats, and the amount of expired ethane which indicateds lipid peroxidation was followed up for 78 h. Compared to controls neither 1x30 mg/kg and 2x30 mg/kg nor 1x70 mg/kg bleomycin led to increased ethane expiration, although body weight loss indicated toxicity. That pulmonary toxicity had been developed due to the acute bleomycin treatment could be demonstrated by histological examinations of lungs of the animals of the highest dosage group. The combined treatment of rats with bleomycin and ferrous ions neither resulted in an increase of ethane expired compared to that of the ferrous iontreated animals. Rather a decrease was observed. Our results indicate that acute bleomycin toxicity is not associated with increased lipid peroxidation. Furthermore, our data suggest that the bleomycin-ferrous-complex does not initiate lipid peroxidation in vivo.

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URL: http://dx.doi.org/10.1007/BF00409644

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Experimental chemotherapy with N′N′-bis(2-chloroethyl)-N-nitrosourea (BCNU) in autochthonous neurogenic tumors of the rat transplacentally induced by ethylnitrosourea (1982)

Fiebig, H. H. ; Strobel, H. ; Schmähl, D.

Springer

Journal of cancer research and clinical oncology 104 (1982), S. 89-98

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ISSN: 1432-1335

Keywords: Autochthonous primary neurogenic tumors ; Rat ; Transplacental induction ; Chemotherapy ; BCNU

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary Autochthonous neurogenic tumors of the rat induced by transplacental application of ethylnitrosourea were used for the first time to study their suitability as tumor models for experimental chemotherapy. Of 189 transplacentally treated rats, 87% developed neurogenic tumors. After the initial clinical diagnosis of a neurogenic tumor, additional malignant tumors often occurred. The mean number of neurogenic tumors from 62 untreated control rats increased from 1.0 per rat at the time of randomization to 1.2 as revealed by autopsy and 1.5 tumors by histological examinations. Out of all neurogenic tumors, tumors of the brain were observed in 31%, tumors of cranial nerves in 36% (90% tumors of trigeminal nerve), tumors of spinal cord in 21%, and tumors of peripheral nerves in 10%. The median survival time until natural death of 62 control rats was 228 days. Rats with tumors of peripheral nerves lived shortest, followed by rats with tumors of cranial nerves, tumors of the spinal cord, and brain tumors. Brain tumors were mainly astrocytomas and oligodendrogliomas. The survival time of untreated rats from randomization to natural death was longest for those with brain tumors, followed by tumors of peripheral nerves, cranial nerves, and tumors of the spinal cord. There was great variation in survival time from a few days to more than 6 months. To study the responsiveness to chemotherapy, 62 rats received BCNU as a single intravenous dose of 9 and later 10 mg/kg. Sixty-two untreated control rats had a median survival time of 36 days (95% confidence interval 26–52 days), the treated rats 43.5 days (26–62 days) The difference was not statistically significant. BCNU produced a remission or a no change of neurologic symptoms in 60% (37 out of 62) in comparison to 39% (24 out of 62) in the control group (p〈0.05). The advantages and disadvantages of the present models are discussed. Due to methodical problems and the marginal response to BCNU, autochthonous neurogenic tumors of the rat are not suitable as models for chemotherapeutic studies.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00402057

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Histamine stimulates renin release from the isolated perfused rat kidney (1982)

Schwertschlag, Ullrich ; Hackenthal, Eberhard

Springer

Naunyn-Schmiedeberg's archives of pharmacology 319 (1982), S. 239-242

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ISSN: 1432-1912

Keywords: Renin ; Histamine ; Kidney ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary The renal effects of histamine, histamine receptor agonists and antagonists were studied in the isolated rat kidney, which was perfused with a synthetic medium at constant perfusion pressure in a single pass system. Histamine induced a concentration-dependent increase of renin release ranging from a two-fold increase at 0.5 μM to a four-fold increase at 10 μM. No change in renal vascular resistance, glomerular filtration rate and sodium excretion occurred. Histamine-H2-antagonists (ranitidine and cimetidine) were more effective to block the response to histamine than was the histamine H1-antagonist diphenhydramine. Histamine-H2-agonists (impromidine and dimaprit, 2.5 μM each) were potent stimulators of renin release, their effect was blunted by H2-antagonists. The histamine-H1-agonist pyridyl-2-ethylamine had a low stimulatory activity at 10 μM final concentration, which may reflect partial H2-agonistic effects. It is concluded that histamine stimulates renin release via H2-receptor activation.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00495872

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Effect of X-ray irradiation on primary mineralization in rat alveolar bone (1982)

Sela, J. ; Deutsch, D. ; Bodner, L. ; [et al.]

Springer

Virchows Archiv 398 (1982), S. 11-18

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ISSN: 1432-2307

Keywords: Bone ; Irradiation ; Matrix-vesicles ; Osteoblast ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary The effect of X-ray irradiation on the process of primary mineralization in bone was studied by biochemical and ultrastructural methods. A single dose of 1500R was administered to the head region of rats. The animals were examined immediately after irradiation and 1, 2 and 3 weeks later. Fractions of isolated cells and extracellular matrix vesicles were prepared from the maxillary alveolar bone of irradiated and untreated rats by collagenase digestion and differential centrifugation. The protein content and activities of vesicular phosphatases were determined in both fractions. A continuous decrease in the activity of alkaline phosphatase could be observed in both cell and matrix vesicle fractions during a three-week follow up after irradiation. Acid phosphatase activity decreased only in the vesicle fraction. Transmission electron microscopy of irradiated bone tissue revealed that many matrix vesicles were devoid of intact membranes and apatite crystals. Calcifying nodules were abundant in the matrix without their apparent fusion into larger mineralized structures. It is suggested that irradiation interferes with enzymatic processes associated with primary mineralization.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00585609

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155

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The effect of beta-adrenergic receptor blockade on intramuscular glycogen mobilization during exercise in the rat (1982)

Górski, Jan ; Pietrzyk, Krystyna

Springer

European journal of applied physiology 48 (1982), S. 201-205

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ISSN: 1439-6327

Keywords: Exercise ; Muscle glycogen ; Muscle types ; Beta-adrenergic blockade ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary The effect of beta-adrenergic receptor blockade (with propranolol) on exercise-induced glycogen mobilization in rat skeletal muscles was studied. Treatment with propranolol either fully or partly prevented glycogen mobilization or had no effect at all on the process. The effects of propranolol depended on the intensity and duration of exercise and on the fiber composition of the muscle studied.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00422981

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156

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Time course of blood ethanol in rats during alcohol dependence and withdrawal (1982)

Burov, Yu. V. ; Vlasova, N. V. ; Rodionov, A. P.

Springer

Bulletin of experimental biology and medicine 94 (1982), S. 1069-1071

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ISSN: 1573-8221

Keywords: pharmacokinetics ; alcohol ; alcohol abstinence

Source: Springer Online Journal Archives 1860-2000

Topics: Biology , Medicine

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00830715

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157

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A model of the kinetics of blood levels of phenazepam and its metabolite 3-hydroxyphenazepam in cats (1982)

Zherdev, V. P. ; Ékonomov, A. L. ; Brestkina, L. M. ; [et al.]

Springer

Bulletin of experimental biology and medicine 94 (1982), S. 1373-1375

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ISSN: 1573-8221

Keywords: pharmacokinetics ; phenazepam ; 3-hydroxyphenazepam ; cats ; blood ; metabolic model

Source: Springer Online Journal Archives 1860-2000

Topics: Biology , Medicine

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00827203

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Pharmacokinetics of ethanol in narcotic doses and endogenous ethanol levels in female rats (1982)

Andronova, L. M. ; Ushakova, M. M. ; Kudryavtsev, R. V. ; [et al.]

Springer

Bulletin of experimental biology and medicine 94 (1982), S. 1689-1692

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ISSN: 1573-8221

Keywords: ethanol preference ; endogenous ethanol ; pharmacokinetics ; estrous cysle

Source: Springer Online Journal Archives 1860-2000

Topics: Biology , Medicine

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00838911

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159

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Clinical pharmacokinetics of disopyramide (1982)

Karim, Aziz ; Nissen, Catherine ; Azarnoff, Daniel L.

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 465-494

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ISSN: 1573-8744

Keywords: disopyramide ; pharmacokinetics ; bioavailability ; metabolite ; half-life ; protein binding ; disease states ; drug-drug interaction

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract Current information on the pharmacokinetics of disopyramide is reviewed with emphasis on the implications for antiarrhythmic therapy. The absolute bioavailability, the disposition half-life, the plasma clearance, and the renal clearance for normal subjects and patients are discussed. Drug-drug interactions are discussed, and a new flexible intravenous dosing schedule is proposed.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01059032

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Literature growth in pharmacokinetics (1982)

Boxenbaum, Harold

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 335-348

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ISSN: 1573-8744

Keywords: pharmacokinetics ; bioavailability ; growth ; literature growth ; logistic function

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract The literature growth in pharmacokinetics and bioavailability between the years 1964 and 1980 is analyzed. During much of this period, the literature doubled approximately every 1.6 years. However, during the period 1978–1980, little or no growth was observed. During the period 1950–1967, the total chemical literature increased exponentially with a half-life of 8.28 years; between 1968 and 1980, the half-life was 12.4 years. Thus, the pharmacokinetic literature increased at a much more rapid pace than did the total chemical literature in general. The subject of growth is considered in a general context, particularly as influenced by psychological, sociological, political, and economic factors. It is concluded that while mathematical functions may adequately describe past literature trends, they have little if any utility in predicting future trends in specific research areas such as pharmacokinetics.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01059265

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Pharmacokinetics of intravenous chloramphenicol sodium succinate in adult patients with normal renal and hepatic function (1982)

Burke, J. T. ; Wargin, W. A. ; Sherertz, R. J. ; [et al.]

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 601-614

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ISSN: 1573-8744

Keywords: chloramphenicol-3-monosuccinate ; chloramphenicol-1-monosuccinate ; chloramphenicol ; bioavailability ; pharmacokinetics ; intravenous administration ; adult patients

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract The pharmacokinetics of chloramphenicol (CAP) and total chloramphenicol succinate (CAPS) were studied in eight hospitalized adult patients with normal renal and hepatic function receiving intravenous chloramphenicol sodium succinate therapy. The steady-state peak concentrations of CAP (8.4–26.0 μg/ml) occurred at an average of 18.0 min (range 5.4–40.2) after cessation of the chloramphenicol sodium succinate infusion. Unhydrolyzed CAPS prodrug, representing 26.0±7.0% of the dose, was recovered unchanged in the urine indicating that the bioavailability of CAP from a dose of intravenous chloramphenicol succinate is not complete. A pharmacokinetic model was developed for simultaneous fitting of CAP and CAPS plasma concentration data. Pharmacokinetic parameters determined by simultaneous fitting were: V, 0.81±0.18 liters/kg; t1/2, 3.20 ±1.02 hr; CLB, 3.21±1.27 ml/min/kg for chloramphenicol; and V, 0.38±0.13 liters/kg; t1/2, 0.57±0.12hr; CLB, 7.72±1.87 ml/min/kg for total chloramphenicol succinate.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01062543

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162

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Pharmacokinetics and pharmacodynamics of the antiarrhythmic compound MD750819 in dogs with experimentally induced arrhythmias (1982)

Dow, James ; Laquais, Bernard ; Tisne-Versailles, Jacky ; [et al.]

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 283-296

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ISSN: 1573-8744

Keywords: antiarrhythmic compound ; experimental arrhythmia ; pharmacokinetics ; three compartment model ; pharmacological response ; combined pharmacokinetic pharmacodynamic model

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract Pharmacokinetics and pharmacodynamics were studied in three dogs with interventricular coronary artery ligatures (ligature of Harris) and in three control animals. Weighted nonlinear analysis was used to fit equations describing two and three compartment open models to the experimental data, obtained after intravenous injection (5 mg/kg) of the drug. The three compartment model gave a reduction in the weighted sum of squared residuals and an improvement in the randomness of scatter of the experimental points about the theoretical curve. The postdistribution elimination half-life was longer, the area under the plasma elimination curve larger, and the total body plasma clearance and apparent volume of distribution was reduced in the animals with arrhythmias. The pharmacological response was assessed by recording the ECG and calculating the percentage of normal sinus rhythm/min. A combined pharmacokinetic-pharmacodynamic model was used to analyze data from individual animals. ke0, a measure of the lag time of pharmacological response behind changes in plasma concentration, and Ce (50), a measure of the sensitivity of the cardiac site of action of the drug, were determined.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01059262

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163

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Pharmacokinetics and bioavailability of intravenous, oral, and rectal nitrazepam in humans (1982)

Jochemsen, R. ; Hogendoorn, J. J. H. ; Dingemanse, J. ; [et al.]

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 231-245

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ISSN: 1573-8744

Keywords: nitrazepam ; i.v. ; oral ; rectal administration ; protein binding ; pharmacokinetics ; bioavailability

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract The pharmacokinetics and bioavailability of nitrazepam following intravenous, oral (tablet), and rectal (solution) administration were studied in seven healthy, young male volunteers. Nitrazepam plasma concentrations were determined by electron-capture GLC; pharmacokinetic evaluations were made by compartmental analysis (NONLIN) and compared with the results obtained by a less stringent modelling of the data. The plasma concentration-time profile was similar for all three routes of administration. Mean kinetic parameters as obtained by compartmental analysis of i.v. nitrazepam were: distribution half-life 17 min; volume of distribution after equilibrium 2.14 liters/kg; total plasma clearance 61.6 ml/min; elimination half-life 29.0 h. The mean protein unbound fraction of nitrazepam in plasma was 12.3% and the clearance of the unbound fraction was 506 ml/min. Absorption of oral nitrazepam started after the elapse of a lag time (mean value 12 min) and occurred as an apparent first-order process in all but one subject, with a mean absorption half-life of 16 min. Distribution and elimination half-lives were comparable with those following i.v. administration. Following rectal administration of the nitrazepam solution, rapid first-order absorption occurred with a mean lag time of 4 min and a mean absorption half-life of 9 min. Peak times (median 18 min) were significantly shorter than following oral administration (median 38 min), but there was little difference in peak concentrations. The distribution half-life was similar to i.v. and oral administration, but the elimination half-lives were longer with a mean value of 33.1 h. Following i.v. administration a good agreement was found between the results obtained by compartmental analysis using NONLIN and those obtained by a less stringent modelling of the data. Following oral and rectal administration, a good agreement between the two procedures was found for the elimination half-life; estimation of bioavailability, however, was higher by compartmental analysis. The mean bioavailability data showed that absorption is complete when nitrazepam is given orally and almost 20% lower when it is given rectally, but considerable interindividual differences were observed.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01059259

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164

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Pharmacokinetics of sulfaethidole in the rat: Nonlinear multicompartment solution (1982)

Kekki, Matti ; Julkunen, Risto J. K. ; Pohjanpalo, Hannu

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 27-51

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ISSN: 1573-8744

Keywords: pharmacokinetics ; models ; plasma protein binding ; nonlinear processes ; Sulfaethidole

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract Sulfaethidole distribution and elimination in the rat was studied over a 90-fold dose range. This experimental design produced marked nonlinearity in the binding of Sulfaethidole to proteins in both interstitial fluid and plasma. Using a multicompartmental model consisting of binding of Sulfaethidole to plasma and interstitial fluid proteins, Sulfaethidole distribution in the body could be simulated. Urinary and biliary elimination of Sulfaethidole depended on the unbound drug mass in the plasma and urine flow. The results confirm the central role of the unbound species in the distribution and elimination of drugs with marked binding to plasma proteins.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01059182

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165

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Analytical approximations of sensitivities of steady state predictions to errors in parameter estimation (1982)

Gonda, Igor

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 559-574

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ISSN: 1573-8744

Keywords: pharmacokinetics ; steady state predictions ; sensitivity analysis ; parameter estimates ; optimum sampling strategies

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract The sensitivity theory is applied to derive a linear approximation to the functional dependence of some steady state quantities of therapeutic significance on pharmacokinetic parameters obtained from the biexponential response to a single drug dose. The error of a steady state prediction depends in general on two terms. The first one may be viewed as an approximate sensitivity of the prediction to the parameter errors, and this depends solely on the algebraic relation between the prediction and the parameters. The second term is the relative error in parameters, and this may be affected by experimental design and the method of data analysis. Comparisons are made with Monte Carlo simulations and “a posteriori”estimates of variance of a prediction.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01059038

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166

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Intraindividual variability in theophylline pharmacokinetics: Statistical verification in 39 of 60 healthy young adults (1982)

Upton, Robert A. ; Thiercelin, Jean-Francois ; Guentert, Theodor W. ; [et al.]

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 123-134

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ISSN: 1573-8744

Keywords: theophylline ; pharmacokinetics ; variability ; disposition rate constant ; man

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract After administering a single 300 mg dose of theophylline in oral solution to 12 healthy adults, the dose-normalized area under the plasma concentration-time curve was 97.2±20.1 % (mean±SD) of that after giving a 500 mg dose and statistically indistinguishable. Similarly, these areas multiplied by the individual's terminal disposition rate constant (β) were statistically indistinguishable between 300 and 500mg doses (99.1±10.3%), giving no evidence of dose-dependence for theophylline kinetics at the levels below 15 μg/ml observed in these individuals. After an intravenous dose, a shortlived distribution phase (t1/2α) is sometimes seen. An a phase, however, is hardly discernible in over 250 profiles arising from oral doses administered during five single dose bioavailability studies. Almost all such profiles appear to follow single-compartment model predictions. With precautions to avoid a potential a phase, a terminal log-linear slope can be fitted by least squares analysis with a relative standard error in the slope determination almost always less than 6%. Covariance analysis confirms statistically that 39 of the 60 participating individuals varied in their β on the different occasions each was required to take a dose during the course of a crossover bioavailability trial. In one study, even though each individual was observed on only two occasions, 9 out of 12 showed statistically identifiable variation in β. Fluctuations in β of 60% can be seen. Changes of 30% or greater are common and can occur within 3 or 4 days. Thus real, large, and potentially frequent changes in β of theophylline have been identified in a majority of normal subjects. These changes do not appear to be confined to either sex, to smokers or nonsmokers, or to heavier or lighter individuals. No chronological pattern has, as yet, been recognized in the intraindividual variability in β.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01062330

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Effect of dose size on the pharmacokinetics of intravenous hydrocortisone during endogenous hydrocortisone suppression (1982)

Toothaker, R. D. ; Welling, Peter G.

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 147-156

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ISSN: 1573-8744

Keywords: intravenous hydrocortisone ; blood concentrations ; pharmacokinetics ; endogenous hydrocortisone suppression

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract The pharmacokinetics of hydrocortisone were examined following single intravenous doses of 5, 10, 20, and 40 mg hydrocortisone, as the sodium succinate salt, to healthy male volunteers. Endogenous hydrocortisone was suppressed by administration of 2 mg dexamethasone the night before hydrocortisone injection. Plasma samples obtained serially during 8 h after hydrocortisone injection were assayed by reversephase HPLC using a fixed wavelength (254 nm) ultraviolet detector. Initial concentrations of hydrocortisone in plasma were proportional to dose size. The subsequent decline in hydrocortisone concentrations was biphasic, and individual data sets were adequately described in terms of the pharmacokinetic two-compartment open model. Values of pharmacokinetic parameters were similar from the 5, 10, and 20 mg doses. Following the 40 mg dose, the overall elimination rate constant decreased, while the distribution volume, Vdss,and plasma clearance increased, in comparison with the values obtained from lower doses. Changes in the pharmacokinetics of hydrocortisone at high doses may be related to drug concentrationdependent changes in the binding of hydrocortisone to plasma proteins. Previously reported dosedependent changes in some pharmacokinetic parameters following oral hydrocortisone are attributed to absorption rather than distribution or elimination effects.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01062332

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168

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Pharmacokinetics of cefroxadin (CGP 9000) in man (1982)

Gerardin, André ; Lecaillon, Jean B. ; Schoeller, Jean P. ; [et al.]

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 15-26

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ISSN: 1573-8744

Keywords: cefroxadin ; pharmacokinetics ; man

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract The pharmacokinetics of cefroxadin have been studied after the administration of single oral and intravenous doses to healthy volunteers. Cefroxadin was assayed by HPLC. The kinetics in plasma following i.v. administration were described by using a three-compartment model. An additional disposition phase was observed following oral administration that could not be detected after the low i.v. dose. The terminal half-life was 1.03 h. The apparent volume of distribution at the steady state was consistent with a diffusion of the antibiotic in all extracellular fluids. The AUCafter oral administration was linearly related to the dose. The urinary excretion amounted to 95% of the dose with virtually complete absorption of orally administered drug.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01059181

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The effect of saturable binding to plasma proteins on the pharmacokinetic properties of disopyramide (1982)

Giacomini, Kathleen M. ; Swezey, Sarah E. ; Turner-Tamiyasu, Kathleen ; [et al.]

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 1-14

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ISSN: 1573-8744

Keywords: disopyramide ; pharmacokinetics ; antiarrhythmic, healthy subjects

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract Disopyramide exhibits saturable binding to plasma proteins in the therapeutic plasma concentration range. Because of this property, controversy exists in the literature regarding the pharmacokinetic properties of the drug. The purposes of this study were to reassess the pharmacokinetic properties of disopyramide in humans, taking into consideration both total and unbound concentrations and to use disopyramide as a model compound to study the effect of drug binding on the renal clearance of both total and unbound drug. A single intravenous dose of disopyramide (1.5 mg/kg) was administered to eight normal volunteers. Blood and urine samples were collected for 36h. Total concentrations of disopyramide in plasma and urine were determined by high pressure liquid chromatography. Binding of disopyramide to plasma proteins was determined by equilibrium dialysis. In all subjects, the binding of disopyramide to plasma proteins was saturable, but there were considerable differences in binding between subjects. The volume of distribution, total body clearance, and renal clearances of both total and unbound drug were calculated. Because only the total body clearance and renal clearance of unbound compound are not dependent upon unbound fraction (α), these are the only parameters which can be reported without qualification as to the concentration. The mean ± SD total body clearance of unbound drug in the eight subjects was 5.40± 2.80 ml/min/kg. About 50% of this was due to renal elimination. A statistically significant negative correlation of the renal clearance of total disopyramide with time was observed in seven of eight subjects, whereas a significant correlation between the renal clearance of unbound disopyramide and time was observed in only one subject. This suggests that the renal clearance of unbound disopyramide is independent of α, while the renal clearance of total disopyramide is dependent upon α.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01059180

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170

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Interspecies scaling, allometry, physiological time, and the ground plan of pharmacokinetics (1982)

Boxenbaum, Harold

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 201-227

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ISSN: 1573-8744

Keywords: interspecies variations ; scaling ; heterogony ; allometry ; pharmacokinetics ; physiological time ; pharmacokinetic time ; maximum lifespan potential

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract Interspecies variation in pharmacokinetics is considered and treated as a property and consequence of body size (allometry). Consequently, it is possible to reference (scale) pharmacokinetic parameters to the organism's individual anatomy, biochemistry, and/or physiology in such a manner that differences between species are nullified. Thus, in the mouse, rat, dog, monkey, and human, methotrexate plasma clearance always equals 133% of creatinine clearance and as such becomes invariant. Pharmacokinetic time (a variable in terms of chronological time) is shown to be a form of physiological time in which a pharmacokinetic event becomes the independent variable, e.g., disposition halflife. A relationship between pharmacokinetic time and body size is demonstrated. It is suggested that man's lesser quantitative ability to metabolize many drugs may be correlated with his enhanced longevity.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01062336

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171

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The pharmacokinetics and pharmacodynamics of bumetanide in normal subjects (1982)

Marcantonio, Laurence A. ; Auld, William H. R. ; Skellern, Graham G. ; [et al.]

Springer

Journal of pharmacokinetics and pharmacodynamics 10 (1982), S. 393-409

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ISSN: 1573-8744

Keywords: diuretic ; bumetanide ; pharmacokinetics ; pharmacodynamics ; normals

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology

Notes: Abstract The pharmacokinetics and pharmacodynamics of bumetanide (1 mg) administered either orally or intravenously were studied in a group of normal subjects using high-pressure liquid chromatography. A two-compartment model adequately fitted the intravenous data. Renal clearance (85 ml min−1 contributed 65% to the total elimination of bumetanide irrespective of whether a model-dependent or model-independent method was used. Oral administration of bumetanide elicited a greater and a more prolonged pharmacological response than did intravenous bumetanide. An attempt is made to relate the pharmacokinetics of the drug to its pharmacodynamics.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01065171

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172

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Gallensäurenreflux nach operativen Eingriffen am Rattenmagen (1982)

Hellerer, O. ; Rath, H. ; Falter, E. ; [et al.]

Springer

Langenbeck's archives of surgery 356 (1982), S. 159-166

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ISSN: 1435-2451

Keywords: Bile acid ; Reflux ; Stomach surgery ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Description / Table of Contents: Zusammenfassung Am standardisierten Tiermodell an der Ratte wurde die Höhe des duodenogastrischen Refluxes acht Monate nach SPV mit und ohne Pyloroplastik untersucht. Zur Bestimmung des Refluxes diente die enzymatische Messung der Gallensäurenkonzentration im intraoperativ entnommenen Mageninhalt. Als Vergleichsgruppen dienten Laparotomie, alleinige Pyloroplastik und als obligates Refluxmodell die Resektion nach BII ohne Enteroanastomose. Die Höhe des duodenogastrischen Refluxes war nach SPV mit und ohne Pyloroplastik signifikant niedriger als in der Kontrollgruppe. Tiere mit alleiniger Pyloroplastik zeigten einen signifikant erhöhten Reflux. Die BIIGruppe hatte einen fünffach höheren Wert als die Kontrollgruppe. Aufgrund der Pyloroplastik als Drainageoperation kommt es am Rattenmagen nach SPV nicht zur Retention von Speiseresten, die man nach SPV ohne Pyloroplastik beobachtet. Aber wegen der verzögerten Magenmotilität legt sich eingedickter Speisebrei vor den Magenausgang und reduziert so den duodenogastrischen Reflux. Nach unseren Ergebnissen kann ein vermehrter duodenogastrischer Reflux nach SPV mit und ohne Pyloroplastik keine morphologischen Veränderungen der Magenmucosa verursachen.

Notes: Summary Using rats in a standardized animal experiment, the extent of duodenogastric reflux was studied eight months postoperatively following SPV with and without pyloroplasty. The reflux was determined by enzymatically testing the concentration of bile acid secretion withdrawn from the stomach intraoperatively. Serving as comparison were laparotomies, simple pyloroplasties, and the obligatory reflux models: resection after Bll without enteroanastomosis. After SPV with and without pyloroplasty, the extent of duodenogastric reflux was less than in the control group. Specimens with simple pyloroplasty displayed a significantly greater reflux. The Bll group had a fivefold higher reflux than the control group. Since pyloroplasty can be considered a drainage operation, there is no retention of food particles in the stomach of the rat following SPV - an occurrence expected after SPV without pyloroplasty. However, due to the retarded stomach motility, the thickened chyme tends to linger at the opening of the stomach, thus reducing the duodenogastric reflux. According to our investigations, an increased duodenogastric reflux following SPV with or without pyloroplasty does not induce changes in the mucosa of the stomach.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF01261753

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311. Eine neue und einfache Methode der auxilliären Lebertransplantation in der Ratte (1982)

Müller, G. ; Morris, P. J.

Springer

Langenbeck's archives of surgery 358 (1982), S. 582-582

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ISSN: 1435-2451

Keywords: Liver transplantation ; Rat ; Technique ; Lebertransplantation ; Ratte ; Technik

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Description / Table of Contents: Zusammenfassung Eine einfache Technik wurde für vascularisierte Lebertransplantate entwickelt: Der Pfortaderkreislauf wurde unter Verwendung der renalen Gefäße hergestellt und die Galle in den Ureter drainiert; Nierenarterie zu Pfortader unter Verwendung eines Stent, Nierenvene End-zu-End zu inferior Vena Cava mittels fortlaufender Naht, 10-0 Nylon. Ureter zu Gallengang unter Verwendung eines Stent. Das neue Modell ermöglicht geringe Letalität, kurze Operations- und Ischämiezeiten und war in mehr als 100 Transplantationen für immunologische Untersuchungen erfolgreich.

Notes: Summary A simple technique was developed for vascularized liver grafts in order to provide consistent reproducibility. Portal circulation was established using the host's renal vessels and ureter for bile drainage: renal vein to inferior vena cava end to end, using continuous 10-0 nylon; renal artery to portal vein using a stent and bile duct to ureter using a stent. The new model provides low mortality, short operation time and ischemia time and was successful in more than 100 transplants for immunological studies.

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URL: http://dx.doi.org/10.1007/BF01272057

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312. Organtransplantation in der Ratte — Nieren, Herz, Leber und Pankreastransplantationen unter Verwendung der Nierengefäße (1982)

Müller, G. ; Fairbrother, B. ; Morris, P. J.

Springer

Langenbeck's archives of surgery 358 (1982), S. 582-583

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ISSN: 1435-2451

Keywords: Rat ; Organ transplantation ; Technique ; Ratte ; Organtransplantation ; Technik

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Description / Table of Contents: Zusammenfassung Über 3000 Transplantationen wurden unter Verwendung der renalen Gefäße für Herz, Nieren, Leber und Pankreastransplantationen durchgeführt: Empfänger Herz Niere Leber Pankreas a. coeliaca carotis comm. a. renalis a. coeliaca a. coeliaca v. renalisa. pulmonalis v. renalis vena cava vena portae ureter - ureter duct chol. duct chol. Die Verwendung der renalen Gefäße erwies sich als geeignete Methode mit niedriger Empfängermortalität, sie ermöglicht „End zu End”-Anastomosen, die sicherer sind als „End-zu-Seit”.

Notes: Summary More than 3000 transplants were performed using the renal vessel for heart, kidney, liver, and pancreas: Recipient Heart Kidney Liver Pancreas Renal artery Common carotis Renal artery Coeliac artery Coeliac artery Renal vein Pulmonal artery Renal vein I.V.C. Portal vein Ureter - Ureter Bile duct Bile duct The use of the renal vessels provides a convenient and accessible site with low recipient mortality for simple end-to-end anastomoses, which are safer then end to side.

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URL: http://dx.doi.org/10.1007/BF01272058

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Tierexperimentelle Untersuchungen zur Carcinomgefährdung des Magens nach Vagotomie (1982)

Schlag, P. ; Weber, E. ; Meister, H. ; [et al.]

Springer

Langenbeck's archives of surgery 357 (1982), S. 105-116

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ISSN: 1435-2451

Keywords: Vagotomy ; Gastric cancer ; Bacteria ; Nitrite ; N-Nitroso compounds ; Rat

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Description / Table of Contents: Zusammenfassung Der Einfluß einer trunculären Vagotomie in Kombination mit verschiedenen Drainageoperationen (Pyloroplastik, Gastroenterostomie ohne Enteroanastomose, Y-Roux-Gastroenterostomie) wurde im Hinblick auf eine Carcinomgefährdung des vagotomierten Magens tierexperimentell an männlichen Wistarratten untersucht. Es wurde überprüft, inwieweit hiernach im Vergleich zu einer nicht-vagotomierten Kontrollgruppe Schleimhautveränderungen auftreten, die unter Exposition mit dem Carcinogen MNNG zeitlich früher und häufiger zur Carcinomentstehung prädisponieren. Als mögliche wichtige cocarcinogene Faktoren wurden zusätzlich die intragastrale Bakterienflora und Nitrit-Konzentration der einzelnen Versuchsgruppen untereinander verglichen. Es zeigte sich, daß der Schweregrad gefundener Magenschleimhautveränderungen, sowie das Ausmaß der bakteriellen Besiedlung und die Nitrit-Konzentration im Magensaft neben der durch Vagotomie angestrebten Säurereduktion vor allem durch Störung der Magenmotilität oder einen enterogastrischen Reflux verstärkt wird. Die Ergebnisse der Untersuchungen sprechen dafür, daß nach Vagotomie, soweit eine ausreichende Magenentleerung gesichert und diese nicht durch einen enterogastrischen Reflux (Gastroenterostomie) erkauft wird, das Risiko für ein Operationsfolgecarcinom gering anzusehen ist.

Notes: Summary To assess the possible risk of cancer in the operated stomach, the influence of truncal vagotomy combined with different operative drainage procedures (pyloroplasty, gastro-enterostomy without entero-anastomosis, Roux-en-Y gastro-enterostomy) was studied in animal experiments. The aim of the study was to determine whether, compared to controls an earlier and higher incidence of precancerous epithelial lesions or cancers in the stomach occurs in vagotomized animals after oral administration of carcinogens (MNNG). To consider conditions, that may predispose to in vivo formation of carcinogenicN-nitroso compounds, bacterial flora and intragastric nitrite concentration were measured and compared in the various operative groups. The severity of induced epithelial lesions and the quantity of bacterial growth and nitrite concentration in the gastric juice were influenced, apart from the reduction of acid output after vagotomy, mainly by prolonged gastric stasis or the degree of enterogastric reflux. The results suggest that there is probably no increased risk of cancer following vagotomy, if sufficient gastric clearance is guaranted and enterogastric reflux is largely excluded.

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URL: http://dx.doi.org/10.1007/BF01237456

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Reduced sedimentation equilibrium time by two-step initial loading (1982)

Todd, G. Peter ; Haschemeyer, Rudy H.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 17-24

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ISSN: 0006-3525

Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: Computer simulation shows that the time required to attain near sedimentation equilbrium is dramatically reduced by a two-step initial loading in which a macromolecular solution at low or zero concentration is layered above one at a higher concentration. To achieve the minimum time requires a good estimate of the molecular weight, but at least a 50% reduction in time can be achieved if the molecular weight of the macromolecule is known only within a factor of 2. Numerical solutions to the differential equation of the ultracentrifuge are calculated using the finite element method. An efficient Gaussian elimination algorithm can be used to minimize calculation time and computer storage requirements.

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Fluorescent-labeled crosslinks in collagen: Pyrenebutyrylhydrazine (1982)

Shambaugh, Nathaniel ; Fujimori, Eiji

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 79-88

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The aldehydes present in acid-soluble type I collagen react with pyrenebutyrylhydrazine to form various types of complexes under different reaction conditions. These complexes exhibit one or more of three different pyrene fluorescence bands: monomer, excimer, and aggregate fluorescence. Collagen, whose aldehydes have been reduced with NaBH4, does not react with this fluorescent hydrazine, confirming that the hydrazine reacts specifically with aldehyde groups to form hydrazones. The absence of a reaction with pepsin-treated collagen also shows that the fluorescent labels are primarily in the nonhelical terminal telopeptides. Upon dialysis, the pyrene label bound to a saturated aldehyde in an α-chain is lost; whereas that bound to an unsaturated aldehyde remains on the protein. The pyrene monomer fluorescence in the β-chain of old collagen is stronger than that of young collagen. The formation of the pyrene excimer fluorescence implies the proximity of two pyrene molecules, probably attached to two adjacent aldehydes. Upon changing from acidic to neutral pH, both excimer and aggregate fluorescence bands disappear within a few seconds, revealing a very rapid alteration at the telopeptides.

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A stereospecific complex of poly(I) with ammonium ion (1982)

Howard, Frank B. ; Miles, H. Todd

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 147-157

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: We describe conditions which lead to complete helix formation of poly(I) in the presence of NH4+. Binding of NH4+ is shown to be specific in the presence of Li+, which does not by itself support helix formation under these conditions. The NH4+-poly(I) complex is characterized by uv, CD, and ir spectroscopy. The CD spectrum is strikingly different from those of the Na+ or K+ complexes, the first extremum being changed from negative for the metal ions to positive for NH4+. A stereospecific model is proposed for the NH4+-poly(I) helix in which the N of NH4+ is located on the axis of the four-stranded helix, midway between planar tetramers formed by the bases. The model is consistent with the tetrahedral symmetry of NH4+, the requirement for four acceptable hydrogen bonds, the observed stability of the helix, and the accepted geometry of the backbone.

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The δ-function counterion condensate around a line charge derived from the Fuoss, Katchalsky, and Lifson polyelectrolyte theory (1982)

Lampert, Murray A.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 159-167

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: It has recently been proven that the counterion condensate around an isolated line charge in an electrolyte, as characterized by nonlinear Poisson-Boltzmann theory, is an encapsulating δ-function. Here the identical result is shown to hold in the framework of the polyelectrolyte theory of Fuoss, Katchalsky, and Lifson. The proof fully exploits analytic solutions to the differential equation which are not available for the nonlinear, cylindrical Poisson-Boltzmann equation.

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Interactions of DNA with divalent metal ions. II. Proton relaxation enhancement studies (1982)

Granot, Joseph ; Kearns, David R.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 203-218

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The extent and modes of binding of the divalent metal ions Mn2+ and Co2+ to DNA and the effects of salt on the binding have been studied by measurements of the effects of these paramagnetic metal ions on the longitudinal and transverse relaxation rates of the protons of the solvent water molecules, a technique that is sensitive to overall binding. The number of water molecules coordinated to the DNA-bound Mn2+ and Co2+ is found to be between five and six, and the electron spin relaxation times and the electron-nuclear hyperfine constants associated with Mn2+ and Co2+ are little or not affected by the binding. These observations indicate little disturbance of the hydration sphere of Mn2+ and Co2+ upon binding to DNA. An average 2-3-fold reduction in the exchange rate of the water of hydration of the bound metal ions and an order-of-magnitude increase in their rotational correlation time are attributed to hydrogen-bond formation with the DNA. The binding constants of Mn2+ to DNA, at metal concentrations approaching zero, are found to be inversely proportional to the second power of the salt concentration, in agreement with the predictions of Manning's polyelectrolyte theory. A remarkable quantitative agreement with the polyelectrolyte theory is also obtained for the anticooperativity in the binding of Mn2+ to DNA, although the experimental results can be well accounted for by another simple electrostatic model. The various modes of binding of divalent metal ions to DNA are discussed.

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Polyelectrolyte complexes of glycol chitosan with some polysaccharides. II. Electrical conductivity (1982)

Srinivasan, R. ; Kamalam, R.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 265-275

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The dc electrical conductivity of films of the polyelectrolyte complexes of glycol chitosan (GlChi) with the sodium salts of dextran sulfate (DS), carboxymethyl cellulose (CMC), polygalacturonic acid (GalUA)n, and alginic acid (AlgA) was measured at temperatures above and below room temperature. The maximum field strength in the thinnest film used amounted to 3 × 104 V/cm. A plot of normalized current against the reciprocal of the absolute temperature revealed two regions with different slopes, and activation energies in these two regions have been obtained for all the complexes. The activation energies in the high-temperature region vary from 0.85 to 1.18 eV and in the low-temperature region from 0 to 0.22 eV. Reasons are given to show that the conductivity is probably ionic. Near room temperature, the current-voltage relation is almost linear in the GlChi-DS complex, while in the other three complexes the current varies as a power n of the voltage with the value of n ranging from 1.7 to 2.5. A rise in temperatures causes an increase in the slope of the log I vs log V plot in GlChi-DS and GlChi-CMC complexes. The nonlinear current-voltage relation is ascribed to a space-charge-limited conductivity.

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URL: http://dx.doi.org/10.1002/bip.360210203

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Crystallization behavior of glucomannan (1982)

Chanzy, H. D. ; Grosrenaud, A. ; Joseleau, J. P. ; [et al.]

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 301-319

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: Five different glucomannan samples were recrystallized from dilute solution. Depending on the experimental conditions, the crystals obtained could be identified as corresponding to the mannan I (anhydrous precipitate of more or less regular lozenge-shaped crystals) or mannan II (hydrated gel-forming pseudo-fibrillar precipitate). High-molecular-weight material, low temperature of crystallization, or a polar crystallization medium favored the mannan II polymorph, whereas a low-molecular weight, a high temperature of crystallization, and a crystallization medium of low polarity yielded the mannan I polymorph. Since the base-plane unit-cell dimensions are fairly constant with respect to variation of glucose, it is likely that isomorphous replacement of mannose by glucose occurs in glucomannan crystallization; the data also indicate that perfection of the glucomannan crystals was reduced in specimens having a high glucose:mannose ratio. The oriented crystallization of glucomannan on cellulose microfibrils was also studied under conditions where the mannan I polymorph was obtained. This gave shish-kebab structures that were characterized.

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Thermodynamic functions of biopolymer hydration. I. Their determination by vapor pressure studies, discussed in an analysis of the primary hydration process (1982)

Lüscher-mattli, Madeleine ; Rüegg, Max

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 403-418

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The primary hydration process of native biopolymers is analyzed in a brief review of the literature, pertaining to various aspects of biopolymer-water systems. Based on this analysis, a hydration model is proposed that implies that the solution conformation of native biopolymers is stable at and above a critical degree of hydration (hp′ = 0.06-0.1 g H2O/g polymer). This water content corresponds to the fraction of strongly bound water, and amounts to ∼20% of the primary hydration sphere. In order to test this model, detailed sorption-desorption scanning experiments were performed on a globular protein (α-chymotrypsin). The results obtained are consistent with the proposed hydration model. They show that under certain experimental conditions, sorption isotherms can be obtained that do not exhibit hysteresis. These data represent equilibrium conditions and are thus accessible to thermodynamic treatment. Valid thermodynamic functions, pertinent to the interaction of water with biopolymers in their solution state, can be obtained from these sorption experiments.

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Light scattering of bovine serum albumin solutions: Extension of the hard particle model to allow for electrostatic repulsion (1982)

Minton, Allen P. ; Edelhoch, H.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 451-458

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The light scattering of bovine serum albumin (BSA) has been measured at protein concentration up to 90 g/L and at pH values between 4.4 and 7.6. The dependence of scattering on both protein concentration and pH may be quantitatively accounted for by a simple extension of the hard-sphere model for protein solutions [Ross, P. D. & Minton, A. P. (1977) J. Mol. Biol. 112, 437-452] allowing for electrostatic repulsions between molecules. According to the extended model, the radius of the effective hard spherical particle representing BSA varies with the net electrical charge of the BSA molecule in a manner which may be calculated from electrostatic theory.

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URL: http://dx.doi.org/10.1002/bip.360210215

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Comprehensive conformational analysis of (Gly-Pro-Pro)n and (Gly-Pro-Hyp)n related to collagen (1982)

Tumanyan, Vladimir G. ; Esipova, Natalia G.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 475-497

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: A complete analysis of all possible conformations with correct hydrogen bonds of the collagen II type was performed on the basis of developed simultaneous equations. Using a unimodal search (by varying Ψ3), the energetically favorable structure was obtained. No other energetically satisfactory structural solutions are possible. The next aim was to obtain a precise model of the molecule. The program used includes a subroutine for continual deformation of the pyrrolidine rings. The set of parameters determining the structure consists of 14 independent variables (8 dihedral and 6 bond angles). As starting points for the energy optimization, conformations produced by scanning and some structures from previous work were used. The final structures (practically the same for both polymers) have helix parameters h = 0.285 nm and t = 52°, which are in excellent agreement with the 7/2 symmetry of diffraction data. The conformations of the pyrrolidine rings are of the B type, i.e., C2-Cβ-exo-Cγ-endo. For both polypeptides, the conformations of imino acids in position 3 of the triplet are the same; in position 2, however, they are slightly different. The difference in diffraction patterns for the 7/2 and 10/3 helices is discussed.

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The chiroptical properties of proteins. III. Adenylate kinaseTaken in part from the Ph.D. dissertation of Robert W. Snyder. (1982)

Snyder, Robert W. ; Hooker, Thomas M.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 547-563

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The CD spectrum of the enzyme adenylate kinase has been investigated. Theoretical calculations, based on the x-ray crystal structure, have been carried out by means of an origin independent matrix formalism. The entire molecule was included in the calculations in the sense that essentially all electronic transitions that occur at wavelengths longer than 185 nm were included in the basis set. A linear dielectric function was utilized to evaluate the intertransition coupling potentials. The results of the theoretical calculations were in reasonable agreement with experimental CD spectra of the molecule.

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Interactions of molecules with nucleic acids. VI. Computer design of chromophoric intercalating agents (1982)

Miller, Kenneth J. ; Newlin, Donald D.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 633-652

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The mode of action of many antitumor agents entails the inhibition of nucleic acid synthesis. Because many of the drugs can intercalate, it is assumed that intercalation is an important step in the mechanism of biological activity. As intercalants contain a planar chromophore as an ingredient essential for intercalation, chromophores that should fit into DNA are desired. This is the main theme of this investigation. Binding to DNA of fundamental moieties, protonated pyridine, aniline, phenol, quinone, and 4H-thiopyran-4-one, is studied to determine their optimum placement in DNA. The optimum orientations for each moiety are superimposed to form polyaromatic systems that can intercalate in a manner in which functional groups on these chromophores are oriented as in the moieties themselves. Ideal intercalants proposed contain three and four fused ring system, have protonated ring nitrogen atoms located to maximize the electrostatic interactions with DNA, hydroxy and amino groups that can hydrogen bond to the OII and O5′ phosphate backbone atoms, and carbonyl and sulfur groups in the central position of the ring system to provide variations in the chromophore and to interact with the relatively positive region in the intercalation site. The optimum orientation occurs when the chromophore and the base pairs overlap to the maximum extent. The ideal intercalants are fundamentally of the type:

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Factors affecting the kinetics of DNA reassociation in phenol-water emulsion at high DNA concentrations (1982)

Wieder, Robert ; Wetmur, James G.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 665-677

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

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Notes: DNA reassociation kinetics using the phenol emulsion reassociation technique (PERT) [Kohne, D. E., Levison, S. A. & Byers, M. J. (1977) Biochemistry 16, 5329-5341] has been investigated at high DNA concentrations using an endonuclease S1 assay of reaction progress. Apparent second-order rate constants fall on two intersecting straight lines when presented as a function of DNA concentrations on a log-log plot. In the low DNA concentration range, the rate constants drop about 10-fold when concentration increases 1000-fold. In the high DNA concentration range, the rate constants drop more than 10-fold when concentration increases 10-fold. The slopes of these lines are the same in different solvents and at different temperatures. The intersection between the lines occurs when the available catalytic surface is saturated. At high DNA concentrations, high-complexity heterologous denatured DNA apparently competes 2-4 times better for the surface than homologous DNA because it does not participate in a reassociation reaction. Native and partially native DNA molecules cannot compete with single-stranded DNA for a saturated surface. At high DNA concentrations, reactions using PERT become dependent on the single-strand DNA length. Increasing length lowers reassociation rates.

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Normal vibrations of proteins: GlucagonThis is paper number 13 in a series, “Vibrational Analysis of Peptides, Polypeptides, and Protein,” of which Ref. 8 is paper number 12. (1982)

Tasumi, M. ; Takeuchi, H. ; Ataka, S. ; [et al.]

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 711-714

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ISSN: 0006-3525

Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Additional Material: 2 Ill.

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URL: http://dx.doi.org/10.1002/bip.360210318

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Correlation between sugar pucker and the orientation around the C3′—O3′ bond (Φ′) in 3′-mononucleotides (1982)

Dhingra, M. M. ; Saran, Anil

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 859-872

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: Classical potential functions (CPF) calculations on 3′-mononucleotides, the building blocks of nucleic acids, predict a correlation between the sugar ring pucker and the torsion angle Φ′ around the C3′—O3′ bond. In ribonucleotides, the value of Φ′ depends on the sugar pucker, viz. the C2′-endo sugar pucker is associated with Φ′ = 210° and 270°, while the C3′-endo sugar pucker favors only Φ′ = 210°. On the other hand, in deoxyribonucleotides, both sugar puckers show a preference for Φ′ = 180°. These theoretical predictions are fully corroborated by the results obtained from x-ray and nmr studies on mono-, di-, and polynucleotides.

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URL: http://dx.doi.org/10.1002/bip.360210411

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Influence of surfactants on the conformation of β-lactoglobulin B using circular dichroismPresented in part at the 1981 Joint Meeting of the Central and Great Lakes ACS Regions of the American Chemical Society, Dayton, Ohio, May 20-22, 1981. (1982)

Damon, Amy Jo Hillquist ; Kresheck, Gordon C.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 895-908

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The effect of several surfactants on the secondary structure of bovine β-lactoglobulin B was determined from the circular dichroism spectra. The spectra were measured at several concentrations of surfactant ranging from 1 mg/mL to the critical micelle concentration. The surfactants studied were sodium dodecyl, decyl, and octyl sulfate, sodium dodecyl sarcosinate, dodecyltrimethylammonium bromide. The data were analyzed using the method of Chen et al. [Biochemistry (1974) 13, 3350-3359] to determine the percentage of α-helix, β-sheet, and unordered form at each surfactant concentration. In every case, an increase in structured form and a 20-25% decrease in the amount of unordered form was noted when the surfactant concentration reached the critical micelle concentration. However, the relative amounts of the two structured forms present depend on the surfactant used. The profile of the secondary structure of the protein also varied from surfactant to surfactant as the protein was titrated, probably reflecting the delicate balance between ionic and nonionic forces that governs the secondary structure of β-lactoglobulin and most other globular proteins in aqueous solution.

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URL: http://dx.doi.org/10.1002/bip.360210504

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Proline-containing β-turns in peptides and proteins. II. Physicochemical studies on tripeptides with the Pro-Gly sequenceFor Paper I of this series, see Ref. 8. (1982)

Brahmachari, Samir K. ; Rapaka, Rao S. ; Bhatnagar, Rajendra S. ; [et al.]

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 1107-1125

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: Amino acids are known to differ in their individual preferences for each of the four positions of the β-turn conformation formed by tetrapeptide segments. Proline and glycine show relatively high preferences for positions 2 and 3, respectively, of the β-turn. Using tripeptides of the type N-acetyl-Pro-Gly-X-OH, where X = Gly, Ala, Leu, Ile, and Phe, we have sought to study the influence of the 4th residue X on the stability of the β-turn conformation in these tripeptides. Our nmr and CD results show that the β-turn stability is quite significantly governed by the nature of the amino acid residue at this position in the following order: Leu 〉 Ala 〉 Ile, Gly 〉 Phe.

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URL: http://dx.doi.org/10.1002/bip.360210608

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Cyclodextrin-adamantanecarboxylate inclusion complexes: A model system for the hydrophobic effect (1982)

Harrison, John C. ; Eftink, Maurice R.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 1153-1166

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: Thermodynamic studies of the binding of adamantanecarboxylate to cyclodextrins have been made as a function of temperature and added organic cosolvent (methanol) using flow microcalorimetry. The negative heat capacity change associated with the adamantanecar-boxylate/β-cyclodextrin interaction and the fact that the interaction is weakened by the addition of methanol implicate the binding process as being a hydrophobically driven one. The negative enthalpy change (ΔH0 = -5.5 kcal/mol) and near-zero entropy change (ΔS0 = 1.5 cal/mol deg) are quite different from the values normally expected for a hydrophobic bond, indicating that other bonding forces are important in addition to the hydrophobic effect. The relative contribution of the hydrophobic effect and other bonding forces (most likely van der Waals forces) to the overall binding was judged from an analysis of the dependence of the thermodynamics of the association process on the surface tension of the water-methanol mixtures following a model for “solvophobic” bonding described by Sinanoglu [Molecular Associations in Biology (1968) Academic Press, New York, pp. 427-445]. From this analysis, adamantane-carboxylate/cyclodextrin complex formation is found to be driven to the extent of -1.9 kcal/mol by the hydrophobic effect. Furthermore, the hydrophobic driving force is found to be characterized by a positive ΔS0 of 10 cal/mol deg. The remaining free energy of binding (and the ΔH0 of binding of ∼-6 kcal/mol) is then due to the intrinsic (surface-tension-independent) van der Waals interaction between the ligand and cyclodextrin cavity.

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URL: http://dx.doi.org/10.1002/bip.360210611

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Masthead (1982)

New York : Wiley-Blackwell

Biopolymers 21 (1982)

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1002/bip.360210701

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Type II β-turn conformation of pivaloyl-L-prolyl-α-aminoisobutyryl-N-methylamide: Theoretical, spectroscopic, and X-ray studies (1982)

Prasad, B. V. Venkataram ; Balaram, Hemalatha ; Balaram, P.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 1261-1273

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: Pivaloyl-L-Pro-Aib-N-methylamide has been shown to possess one intramolecular hydrogen bond in (CD3)2SO solution, by 1H-nmr methods, suggesting the existence of β-turns, with Pro-Aib as the corner residues. Theoretical conformational analysis suggests that Type II β-turn conformations are about 2 kcal mol-1 more stable than Type III structures. A crystallographic study has established the Type II β-turn in the solid state. The molecule crystallizes in the space group P21 with a = 5.865 Å, b = 11.421 Å, c = 12.966 Å, β = 97.55°, and Z = 2. The structure has been refined to a final R value of 0.061. The Type II β-turn conformation is stabilized by an intramolecular 4 → 1 hydrogen bond between the methylamide NH and the pivaloyl CO group. The conformational angles are φPro = -57.8°, ψPro = 139.3°, φAib = 61.4°, and ψAib = 25.1°. The Type II β-turn conformation for Pro-Aib in this peptide is compared with the Type III structures observed for the same segment in larger peptides.

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URL: http://dx.doi.org/10.1002/bip.360210702

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Equilibrium folding and unfolding pathways for a model protein (1982)

Miyazawa, S. ; Jernigan, R. L.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 1333-1363

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ISSN: 0006-3525

Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The folding-unfolding process of reduced bovine pancreatic trypsin inhibitor was investigated with an idealized model employing approximate free energies. The protein is regarded to consist of only Cα and Cβ atoms. The backbone dihedral angles are the only conformational variables and are permitted to take discrete values at every 10°. Intraresidue energies consist of two terms: an empirical part taken from the observed frequency distributions of (φ,ψ) and an additional favorable energy assigned to the native conformation of each residue. Interresidue interactions are simplified by assuming that there is an attractive energy operative only between residue pairs in close contact in the native structure. A total of 230,000 molecular conformations, with no atomic overlaps, ranging from the native state to the denatured state, are randomly generated by changing the sampling bias. Each conformation is classified according to its conformational energy, F; a conformational entropy, S(F) is estimated for each value of F from the number of samples. The dependence of S(F) on energy reveals that the folding-unfolding transition for this idealized model is an “all-or-none” type; this is attributable to the specific long-range interactions. Interresidue contact probabilities, averaged over samples representing various stages of folding, serve to characterize folding intermediates. Most probable equilibrium pathways for the folding-unfolding transition are constructed by connecting conformationally similar intermediates. The specific details obtained for bovine pancreatic trypsin inhibitor are as follows: (1) Folding begins with the appearance of nativelike medium-range contacts at a β-turn and at the α-helix. (2) These grow to include the native pair of interacting β-strands. This state includes intact regular secondary conformations, as well as the interstrand sheet contacts, and corresponds to an activated state with the highest free energy on the pathway. (3) Additional native long-range contacts are completely formed either toward the amino terminus or toward the carboxyl terminus. (4) In a final step, the missing contacts appear. Although these folding pathways for this model are not consistent with experimental reports, it does indicate multiple folding pathways. The method is general and can be applied to any set of calculated conformational energies and furthermore permits investigation of gross folding features.

Additional Material: 10 Ill.

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URL: http://dx.doi.org/10.1002/bip.360210706

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Aggregation of apolar peptides in organic solvents. Concentration dependence of 1H-nmr parameters for peptide NH groups in 310 helical decapeptide fragment of suzukacillin (1982)

Iqbal, M. ; Balaram, P.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 1427-1433

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: Peptide NH chemical shifts and their temperature dependences have been monitored as a function of concentration for the decapeptide, Boc-Aib-Pro-Val-Aib-Val-Ala-Aib-Ala-Aib-Aib-OMe in CDCl3 (0.001-0.06M) and (CD3)2SO (0.001-0.03M). The chemical shifts and temperature coefficients for all nine NH groups show no significant concentration dependence in (CD3)2SO. Seven NH groups yield low values of temperature coefficients over the entire range, while one yields an intermediate value. In CDCl3, the Aib(1) NH group shows a large concentration dependence of both chemical shift and temperature coefficient, in contrast to the other eight NH groups. The data suggest that in (CD3)2SO, the peptide adopts a 310 helical conformation and is monomeric over the entire concentration range. In CDCl3, the 310 helical peptide associates at a concentration of 0.01M, with the Aib(1) NH involved in an intermolecular hydrogen bond. Association does not disrupt the intramolecular hydrogen-bonding pattern in the decapeptide.

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URL: http://dx.doi.org/10.1002/bip.360210711

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Low-frequency modes in the Raman spectra of proteins (1982)

Painter, P. C. ; Mosher, L. E. ; Rhoads, C.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 1469-1472

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Additional Material: 2 Ill.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1002/bip.360210715

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Proline ring conformations corresponding to a bistable jump model from 13C spin-lattice relaxation times (1982)

Shekar, S. C. ; Easwaran, K. R. K.

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 1479-1487

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: A formalism for extracting the conformations of a proline ring based on the bistable jump model of R. E. London [(1978) J. Am. Chem. Soc. 100, 2678-2685] from 13C spin-lattice relaxation times (T1) is given. The method is such that the relaxation data are only partially used to generate the conformations; these conformations are constrained to satisfy the rest of the relaxation data and to yield acceptable ring geometry. An alternate equation for T1 of 13C nuclei to that of London is given. The formalism is illustrated through an example.

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URL: http://dx.doi.org/10.1002/bip.360210802

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Broadline proton magnetic resonance study of cellulose, pectin, and bean cell walls (1982)

MaCkay, Alex L. ; Bloom, Myer ; Tepfer, Mark ; [et al.]

New York : Wiley-Blackwell

Biopolymers 21 (1982), S. 1521-1534

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Keywords: Chemistry ; Polymer and Materials Science

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: We have used broadline proton magnetic resonance to study molecular motion in cellulose, a sodium pectate solution, a calcium pectate gel, and isolated bean cell walls. All samples were prepared in D2O to minimize the contribution of water to the observed signals. For each sample, a free induction decay was obtained, and the second moment, spin-lattice relaxation, and dipolar relaxation were measured. Our results show that the large majority of protons in cellulose are immobile. Rigid and mobile domains were also observed in the pectate samples. We have shown that gelation induces large-scale changes in the free induction decay, the second moment, and the relaxation behavior of the pectate. As with the other samples, rigid and more mobile domains were found in bean cell walls. The fraction in the rigid domains is much larger than the fraction of cellulose in the sample, suggesting that the noncellulosic wall components are also organized into rigid and mobile domains.

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URL: http://dx.doi.org/10.1002/bip.360210805

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