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  • Electronic Resource  (33)
  • 2020-2022
  • 1985-1989
  • 1975-1979  (33)
  • 1977  (33)
  • pharmacokinetics
  • 1
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of paracetamol (acetaminophen) after intravenous and oral administration (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 283-286 
    Details
    ISSN: 1432-1041
    Keywords: Paracetamol ; Acetaminophen ; pharmacokinetics ; first-pass elimination ; intravenous administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma paracetamol concentrations were measured in 6 volunteers after single intravenous (1000 mg) and oral (500 mg, 1000 mg and 2000 mg) doses of the drug. Paracetamol levels declined multiphasically with a mean clearance after intravenous administration of 352±40 ml/min. A two-compartment open model appeared to describe the decline adequately. Comparison of the areas under the plasma concentration-time curves (AUC) indicated that oral bioavailability increased from 0.63±0.02 after 500 mg, to 0.89±0.04 and 0.87±0.08 after 1000 mg and 2000 mg, respectively. As a consequence of the incomplete bioavailability of paracetamol, as well as its multicompartmental distribution, accurate estimates of its distribution volume and clearance cannot be obtained if the drug is given orally. However, an estimate of its total plasma clearance may be derived from the AUC after a 500 mg oral dose.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607678
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  • 2
    Electronic Resource
    Electronic Resource
    Distribution and elimination of digoxin in infants (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 329-335 
    Details
    ISSN: 1432-1041
    Keywords: Digoxin ; pharmacokinetics ; two-compartment model ; radioimmunoassay ; neonates ; infants
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The distribution and elimination of intravenous digoxin were investigated in seven neonates and infants with heart failure. Serum digoxin concentrations during a 24 h period were determined by radioimmunoassay, using125I as tracer. The serum values declined biexponentially after the injection and could be fitted to a two-compartment open model by non-linear least-squares regression. The calculated mean half-lives of the distribution (alpha) phase in neonates and infants were 37 and 28 min, respectively. The mean half-life of the elimination (beta) phase in neonates was 44 h, as compared to 19 h in infants. The mean volume of the central compartment and the mean volume of distribution at steady-state were calculated to be 1.3 and 9.9 l/kg, respectively; no significant differences between neonates and infants were found. The relation between these volumes indicates that digoxin is extensively distributed in tissues. The steady-state distribution volumes of digoxin in neonates and infants exceed those reported in adults. The larger volume of distribution might explain in part why infants with cardiac insufficiency require larger doses of digoxin than adults (on a mg/kg body weight basis) to obtain the same serum concentrations. Elimination of digoxin from the body was slower in neonates than in infants.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00566529
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  • 3
    Electronic Resource
    Electronic Resource
    Individual variation in the response to phenprocoumon (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 351-358 
    Details
    ISSN: 1432-1041
    Keywords: Phenprocoumon ; protein binding ; pharmacokinetics ; pharmacodynamics ; drug therapy ; myocardial infarction ; chronic disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In nine patients, the synthesis rate Rsyn of the vitamin K-dependent clotting factors was calculated from changes in prothrombin-complex activity after intravenous administration of a synthesis-blocking dose of phenprocoumon (PPC). The biological half-life of PPC was between 2.70 and 7.01 days. No correlation was found between the level of the free fraction of this strongly protein-bound drug and its biological half-life. There was a positive correlation (p〈0.01) between the size of the free fraction of PPC and the apparent volume of distribution of the drug. Four of the patients had had an acute myocardial infarction and they showed increased sensitivity to PPC. In them the plasma level of PPC sufficient to reduce Rsyn to 50% of R°syn was significantly lower, and the depression of individual vitamin K-dependent coagulation factors was more pronounced and prolonged, than in five other patients with chronic disease. The degradation rate of coagulation factors was also found to be higher in the patients with acute myocardial infarction. In four patients with chronic disease, anticoagulant therapy with PPC was continued in the out-patient clinic. The calculated oral maintenance dose of PPC, assuming complete absorption, first-order elimination kinetics and a linear relationship between the pharmacological effect and the logarithm of the PPC-plasma concentration, showed good agreement with the dose actually found to produce the desired PP% level.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00566532
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  • 4
    Electronic Resource
    Electronic Resource
    Biotransformation and pharmacokinetics of acenocoumarol (Sintrom®) in man (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 367-375 
    Details
    ISSN: 1432-1041
    Keywords: Acenocoumarol ; excretory balance man ; pharmacokinetics ; biotransformation ; plasma protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption, biotransformation and elimination of the anticoagulant acenocoumarol, 3-[α- (4′-nitrophenyl)-β-acetylethyl]-4-hydroxycoumarin, have been studied by oral administration of 12 mg of a14C-labelled preparation to two male volunteers. Absorption from the gastro-intestinal tract was rapid and the plasma concentration of unchanged drug reached a maximum of 169 and 412 ng/ml, respectively, after 3 hours. The elimination half-life in the two subjects, calculated from the decline between 6 and 24 h, was 8.7 and 8.2 hours. A constant proportion of 98.7% of the drug was bound in vitro to serum proteins over a concentration range of 0.021–8.34 µg/ml, with little interindividual variation. The major portion of the binding was to human serum albumin (97.5%) at two classes of binding sites: association constant K1=1.04×105 l/mole (n1=1) and K2=5.55×103 l/mole (n2=4). In addition to unchanged acenocoumarol, four metabolites were determined in plasma by isotope dilution techniques: the amino-, acetamido-, alcohol1- and alcohol2-metabolites. Of them, the amino-metabolite showed the highest concentration, namely 278 ng/ml, after 6 h in Subject A, and 163 ng/ml after 10 hours in Subject B. Judged from the integrated concentrations, the compounds analyzed accounted for 76 and 89%, respectively, of the total radioactivity in plasma. All the metabolites detected in plasma showed anticoagulant activity when tested in mice. The quantities of the metabolites excreted in urine from 0–120 hours were (Subject A/Subject B): acenocoumarol 0.3/0.2%, amino-metabolite 12.3/7.7%, acetamido-metabolite 19.0/11.1%, alcohol1-metabolite 4.6/9.0%, alcohol2-metabolite 1.7/4.4%, 6-hydroxy-metabolite 6.9/18.3% and 7-hydroxy-metabolite 14.0/22.2%.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00566534
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  • 5
    Electronic Resource
    Electronic Resource
    Pharmacokinetic aspects of protriptyline plasma levels (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 51-56 
    Details
    ISSN: 1432-1041
    Keywords: Antidepressive agent ; protriptyline ; plasma concentration ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma levels of protriptyline have been determined in 30 depressed female patients undergoing antidepressant therapy. After 3 1/2 weeks treatment at dosage levels of 40 mg/day, protriptyline plasma levels ranged from 430 to 1430 nmol/l. During this period only two-thirds of the subjects had definitely achieved asymptotic concentrations. Single dose studies in 5 volunteers suggest that the volume of distribution of protriptyline shows little intersubject variation. The half life of the drug, however, may vary appreciably from subject to subject, ranging from 54 to 198 h. The effects of two sedatives on mean protriptyline plasma levels have been determined. Mean plasma levels for nitrazepam recipients are indistinguishable from those for patients receiving no night sedation. The mean plasma levels for a group of patients receiving sodium amylobarbitone were significantly reduced. The problem of choice and early adjustment of dosages in order to achieve satisfactory plasma levels is discussed. For practical purposes it is suggested that early values may be of predictive significance in allowing early dosage adjustments to be made.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561788
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  • 6
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of salicylate and indomethacin in coeliac disease (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 473-477 
    Details
    ISSN: 1432-1041
    Keywords: Salicylate ; aspirin ; indomethacin ; pharmacokinetics ; coeliac disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma concentrations of salicylate and indomethacin were measured after a single oral dose of aspirin (600 mg) and indomethacin (50 mg) in twelve starved normal subjects and twelve adult patients with coeliac disease. The absorption of salicylate in the coeliac patients was faster than in the normal subjects. The plasma concentration/time curve of indomethacin in both groups was similar during the absorption phase, but there were significant differences between the groups in its elimination. The abnormal absorption pattern of salicylate in coeliac disease does not appear to be related to its pKa. Possible causes of the difference in salicylate absorption include changes in gastric emptying or altered small intestinal permeability.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562942
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  • 7
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of hydrochlorothiazide in man (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 297-303 
    Details
    ISSN: 1432-1041
    Keywords: Hydrochlorothiazide ; pharmacokinetics ; dose/response relationship ; natriuresis ; kaliuresis ; calciuresis ; magnesiuresis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Hydrochlorothiazide (hct) was administered orally in four different doses (12.5, 25, 50 and 75 mg), to eight healthy volunteers. Plasma and urine concentrations of hct were determined by GLC. Maximal plasma levels were found at 1.5–5 h, and averaged 70, 142, 260 and 376 ng × ml−1 respectively. The peak plasma levels and AUC0→9h of hct were highly correlated (p〈0.001) with the dose. The decline in the plasma curve was biphasic in those experiments in which the plasma levels of hct could be determined for at least 24 h. The half life of the slower phase lay between 5.6 and 14.8 h. The urinary recovery of hct, which represented the gastrointestinal absorption, averaged 65 to 72 per cent of the dose. The mean renal plasma clearance did not vary with the dose and averaged 319 to 345 ml × min−1. The diuresis during the 10 h after hct 12.5 mg exceeded that after placebo by a mean of 800 ml. The diureses was not increased further after higher doses of hct. The maximal natriuretic effect (+ 100 mmol), too, was found after the 12.5 mg dose. The excretion of potassium, however, rose with increasing doses; the maximal increment, after 75 mg hct, averaged 25 mmol. The excretion of calcium was significantly increased after 50 mg hct (+ 0.6 mmol). The maximal effect on magnesium excretion occurred after 25 mg hct (+ 0.5 mmol). In healthy volunteers there was no correlation between peak plasma level of hct or AUC0→9h and the renal excretion of water and electrolytes.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607430
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  • 8
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of phenobarbital in childhood (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 305-310 
    Details
    ISSN: 1432-1041
    Keywords: Phenobarbital ; pharmacokinetics ; neonates ; infancy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 14 neonates 1–4 weeks old, 30 babies aged 1–12 months, and 7 infants of 1–5 years of age, the serum levels of phenobarbital were determined by a gas chromatographic micro-method after intravenous injection of phenobarbital 5–10 mg per kg body weight. It was possible to calculate the pharmacokinetic parameters using a two compartment open model. The distribution volumes within the individual age groups and the rate constants k12 and k21 showed no significant differences, but the elimination half-life was significantly longer in neonates (118.6±16.1 h) than in babies (62.9±5.2 h) or infants (68.5±3.2 h).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607431
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  • 9
    Electronic Resource
    Electronic Resource
    Comparison of the pharmacodynamic effects of furosemide and BAY g 2821 and correlation of the pharmacodynamics and pharmacokinetics of BAY g 2821 (muzolimine) (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 341-344 
    Details
    ISSN: 1432-1041
    Keywords: Muzolimine ; pharmacodynamics ; pharmacokinetics ; furosemide ; saluresis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a biometrically planned, double-blind study on 12 Oedema-free male patients the saluretic effect of muzolimine 30 mg was compared with furosemide 40 mg. The plasma level of muzolimine was determined and correlated with its pharmacodynamics. In terms of excretion during the 12-hour observation period muzolimine 30 mg had as great a cumulative effect as furosemide 40 mg. There was a significant difference in the time-response curve. During the first two hours furosemide 40 mg had more saluretic effect than muzolimine 30 mg. Between two and four hours there was no significant difference between the two substances. Between four and six hours, however, muzolimine was somewhat more effective than furosemide, although the difference did not reach the level of significance. After 6 h there was no longer any difference between the two compounds. The half-life of the fall in concentration of muzolimine in plasma was 3.7 up to 10 h after its administration. The time-response curve of the increased urine excretion correlated well with the time course of the concentration of muzolimine in plasma.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562448
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  • 10
    Electronic Resource
    Electronic Resource
    Behaviour of glibenclamide on repeated administration to diabetic patients (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 19-25 
    Details
    ISSN: 1432-1041
    Keywords: Diabetes mellitus ; sulfonylurea ; glibenclamide ; pharmacokinetics ; repeated administration ; deep compartment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Six maturity onset diabetic patients took glibenclamide 5 mg by mouth, every morning 10 min before a standard breakfast. Serum levels of immunoreactive glibenclamide, glucose and immunoreactive insulin were measured repeatedly on the first and 15th days of treatment. Measured glibenclamide blood levels were in close agreement with an analogue computer simulation of data obtained from healthy volunteers: there was no accumulation of drug in the blood, but there was strong evidence for the existence of a slowly equilibrating “deep” compartment. Considerable insulin release and correction of the breakfast-induced hyperglycaemia were observed immediately after administration of the drug, as well as 5 h later, at lunch time. The clinical significance of blood levels of glibenclamide, as well as the correlation of pharmacokinetics with pharmacodynamics, are discussed in the light of these results.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561783
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  • 11
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of methyldopa in healthy man (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 117-123 
    Details
    ISSN: 1432-1041
    Keywords: Methyldopa ; radioactive label ; pharmacokinetics ; metabolism ; healthy volunteers ; intravenous and oral administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of 2-14C-L-α-methyldopa have been investigated in five healthy volunteers following intravenous and oral administration. In the intravenous study a bi-phasic plasma concentration curve was found both for chemically determined α-methyldopa and for radioactivity. The plasma level of radioactivity differed significantly from chemically determined drug, a pattern which was also found in urine. This suggests the presence of unidentified metabolite(s). The difference between plasma disappearance and urine recovery of α-methyldopa and radioactivity during the first 4 h after injection suggests distribution to an extravascular compartment. Plasma half-lives of total radioactivity and of unchanged drug were calculated. In three subjects, pharmacokinetic parameters for a two-compartment open body model were calculated from urine and plasma data. Urinary recovery of radioactivity was almost complete within 48 h after intravenous administration. After oral administration, however, only about 40 per cent of the radioactive dose was recovered in the urine, and it contained approximately equal amounts of unconjugated methyldopa, acid-labile conjugated methyldopa and unidentified metabolite(s). The acid-labile conjugate was found only after oral administration, which supports the theory of a mucosal conjugation process. The lack of acid-labile conjugated drug either in the plasma or urine after intravenous injection indicates that there is no enterohepatic circulation of this drug.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00645132
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  • 12
    Electronic Resource
    Electronic Resource
    Transfer of nitrazepam across the human placenta (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 355-357 
    Details
    ISSN: 1432-1041
    Keywords: Nitrazepam ; placental transfer ; pharmacokinetics ; plasma levels ; protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Six women from 14 to 17 weeks pregnant, and 12 woman from 36 to 40 weeks pregnant, were given nitrazepam 5 mg orally about 12 h before legal abortion by hysterotomy in the former group and elective caesarean section in the latter group. The concentration of nitrazepam was determined by gas-liquid chromatography. Binding to plasma proteins was evaluated by separation of the protein-free fraction by ultracentrifugation. In the first group (early pregnancy) the level of nitrazepam was found to be lower in the fetal than in the maternal circulation. The concentration in amniotic fluid was still lower. In the latter group (late pregnancy) the concentration both of unbound and total nitrazepam in maternal and fetal plasma were in equilibrium, which indicated an increase in transplacental transfer in late pregnancy. The percentage of unbound nitrazepam in both cases was 12%.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562451
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  • 13
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of tolmetin with and without concomitant administration of antacid in man (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 421-428 
    Details
    ISSN: 1432-1041
    Keywords: Tolmetin ; pharmacokinetics ; bioavailability ; antacid ; oral dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The purpose of this study was to determine whether a concomitant single dose of antacid or multiple doses of antacid administered prior to, and with tolmetin, alter the pharmacokinetics of tolmetin when the drug was administered as a commercially available tablet containing tolmetin sodium. The possible effects of the antacid on plasma concentrations and urinary excretion of tolmetin and its major metabolite were evaluated following administration of: (a) tolmetin sodium alone; (b) antacid four time a day for three days prior to a single dose of tolmetin sodium, with continuation of the antacid during the day tolmetin was given; and (c) co-administration of single doses of tolmetin sodium and antacid. The twenty-four subject study was of the crossover type. There were no significant differences among treatment means for: (i) peak plasma concentrations of both tolmetin and metabolite, (ii) AUC 0–8 h and AUC 0-∞ for both tolmetin and metabolite, (iii) time to peak plasma concentration for both tolmetin and metabolite, (iv) plasma concentrations of both tolmetin and the metabolite at all sampling times (except for tolmetin at 2 h), (v) renal clearance of both tolmetin and its metabolite, and (vi) the amount of metabolite excreted in the 0–24 h urine. There were small, but significant, differences among amounts of tolmetin excreted in the 0–24 h urine. Semilogarithmic plots of both tolmetin and metabolite plasma concentrations past the peak concentrations were curved over the entire 8-h observation period; although the elimination half-life of tolmetin has been reported to be about one hour, the half-life most probably exceeds 2.6 h in most subjects. The results of this study indicate a lack of a significant drug-drug interaction between the non-steroidal anti-inflammatory agent, tolmetin sodium, and a commonly used antacid, which is a mixture of magnesium and aluminium hydroxides.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561061
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  • 14
    Electronic Resource
    Electronic Resource
    Antiarrhythmic and electrocardiographic effects of single oral doses of disopyramide (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 91-99 
    Details
    ISSN: 1432-1041
    Keywords: Disopyramide ; plasma concentration ; cardiodepressant drugs ; ventricular arrhythmia ; ventricular tachycardia ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Ten patients with various heart diseases and ventricular arrhythmia received a single oral dose of disopyramide (DE) 200 mg. The ECG was recorded continuously for about 50 h from 2–4 h before drug administration. A statistically significant reduction in the number of ventricular ectopic beats (VEBs) was seen 1.0–3.5 h after drug intake; the average number of VEBs per 30 min decreased from 317 during the control period to 92 by 1.0–3.5 h after treatment and if one patient who did not respond is excluded, the corresponding figures were 272 and 14, respectively. Consecutive VEBs were seen in seven patients before DE was given and decreased significantly (p〈0.05) 1.5–5.5 h after drug administration. There was no change in the PQ interval, the QRS interval showed a slight increase, whereas the QT interval was prolonged 0.5–4 h after administration of DE. A specific gas chromatographic method was used for DE assay in plasma and urine. Absorption was rapid in all patients. Urinary excretion during the first 48 h after drug intake varied between 35 and 75%. The lowest effective antiarrhythmic concentration estimated in six patients ranged from 1.4 to 7.0 µg/ml. β-Phase half-life in five patients was between 10.3 and 22.1 h.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562898
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  • 15
    Electronic Resource
    Electronic Resource
    Fluorometric determination of hydroflumethiazide in human plasma and urine after its oral administration (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 149-154 
    Details
    ISSN: 1432-1041
    Keywords: Hydroflumethiazide ; spectrofluorometry ; pharmacokinetics ; plasma half life ; renal excretion ; renal disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A spectrofluorometric method for determination of hydroflumethiazide in human plasma and urine has been developed. The limit of detection was 10 ng/ml plasma and 100 ng/ml urine. The plasma concentration of hydroflumethiazide was determined for 9–11 hours and excretion in urine for 24–37 hrs after oral administration of about 1 mg/kg body weight to 7 subjects. Plasma half life in healthy subjects was 1.9–2.1 h, and 2.7–8.6 h in patients during the period 4–9 hrs after dosing. Cumulative excretion in urine was 67–79% of the dose during 31–37 hrs in 6 subjects; one patient with renal disease was found to excrete only 25.8% of dose during 24 hours. Renal clearance of hydroflumethiazide was higher in the healthy subjects (0.29–0.44 1 h−1 kg−1) than in the patients (0.040–0.15 l h−1 kg−1). Plasma half life of hydroflumethiazide was not closely correlated with renal clearance of the drug, which suggests that other factors may play a role in determining plasma half life.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562907
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  • 16
    Electronic Resource
    Electronic Resource
    Model independent derivation of general equations for the “first-pass” effect and extra-hepatic drug elimination (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 57-64 
    Details
    ISSN: 1432-1041
    Keywords: General equation ; pharmacokinetics ; first pass effect ; extra-hepatic drug elimination
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A general expression for the ratio of areas below the blood concentration-time curves after intravenous and oral drug administration is derived. This derivation does not require the assumption of a specific compartmental model to describe drug distribution within the body. Similarly an expression for the amount of drug metabolised in the liver is derived. The latter expression is used to estimate the extent of extra-hepatic drug elimination from the body.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561789
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  • 17
    Electronic Resource
    Electronic Resource
    Dose-dependence of the pharmacokinetics of quinidine (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 73-76 
    Details
    ISSN: 1432-1041
    Keywords: Quinidine ; pharmacokinetics ; non-linearity ; dose-dependent pharmacokinetics ; steady state plasma level ; oral administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Quinidine was administrated orally to five healthy male volunteers. Doses of 0.2 g t. i. d., 0.3 g t. i. d. and 0.4 g t. i. d. were given for five days with at least four weeks between each test period. The plasma concentration of quinidine was measured before the morning dose on Days 2–5 of treatment, and 1, 2, 4 and 8 h after the morning dose on the 5th day. There was not a linear relationship between the increase in dose and the increase in plasma concentration of quinidine. A dose increase of 50% from 0.6 to 0.9 g quinidine sulphate per day resulted in an increase in steady state concentration of 94%. A further 33% increase in dose, from 0.9 to 1.2 g daily, resulted in a 55% increase in the steady stae concentration of quinidine. The results demonstrate dose-dependent pharmacokinetics for quinidine. Possible explanations for the nonlinear pharmacokinetics are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561409
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  • 18
    Electronic Resource
    Electronic Resource
    Plasma level of chlormethiazole and two metabolites after oral administration to young and aged human subjects (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 137-145 
    Details
    ISSN: 1432-1041
    Keywords: Chlormethiazole ; pharmacokinetics ; metabolites ; oral administration ; young and elderly human subjects ; quantitative gas chromatographymass spectrometry ; whole blood distribution
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma concentration of chlormethiazole and two of its metabolites has been measured in three young and three aged human subjects following administration of a single oral dose of chlormethiazole. A sensitive analytical method based on gas chromatography-mass spectrometry using the selective ion monitoring mode of operation was developed to permit quantitation of the plasma levels. The time course of the plasma concentration of chlormethiazole and metabolites showed wide inter-subject variation, particularly between the young and elderly subjects. Absorption of chlormethiazole was rapid in the subjects of both groups as assessed by the time taken to reach the peak plasma concentration. The mean peak plasma level of chlormethiazole was more than five times greater in the elderly (2.90±1.56 µg/ml) than in the young (0.55±0.58 µg/ml) subjects. The plasma level of chlormethiazole was consistently higher in the aged subjects and this was reflected by the larger area under the plasma curve in aged (7.62±5.37 µg.h/ml) than in young (0.94±0.66 µg.h/ml) individuals. Decreased pre-systemic elimination by the liver has been suggested as an important factor contributing to the higher plasma level in the elderly. Estimates of absolute systemic availability, calculated by reference to previous intravenous studies, were greater for the elderly subjects. The distribution of chlormethiazole in whole blood from six young and six elderly human subjects was investigated in vitro. The unbound fraction of chlormethiazole in plasma increased significantly from 0.308±0.035 in young subjects to 0.403±0.067 in the elderly. Distribution of the drug in whole blood was different for the two age groups; the fraction of drug distributed to plasma water was significantly greater and the fraction in blood cells was significantly less in the aged.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00645135
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  • 19
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of tolamolol in the treatment of hypertension (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 171-174 
    Details
    ISSN: 1432-1041
    Keywords: Tolamolol ; hypertension ; pharmacokinetics ; mean steady-state concentration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Tolamolol was administered in a “double-blind” study to fifteen hypertensive patients by dose-titration against arterial blood pressure. Mean steady-state plasma tolamolol concentrations (Css) were determined for each patient from the area under the plasma concentration — time curve during a dosage interval whilst patients were receiving optimal tolamolol doses. No significant correlation was observed between daily tolamolol dose and Css; the relationship between fall in lying mean arterial pressure and Css also failed to reach conventional levels of statistical significance, but Css was observed to be correlated with the fall in standing pressure. The results suggest that plasma concentrations in excess of 200 ng/ml may be required to achieve an effective hypotensive response with the drug.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609855
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  • 20
    Electronic Resource
    Electronic Resource
    Human experience of cetiedil, a new vasodilator with anticholinergic properties (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 205-208 
    Details
    ISSN: 1432-1041
    Keywords: Cetiedil ; vasodilator ; anticholinergic drug ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Cetiedil, a new vasodilating drug with anticholinergic properties, was shown to be metabolised very rapidly in man after intravenous and oral administration of the14C-compound. Higher concentrations of labelled compound after oral than after intravenous administration at the same sampling time, and proportional differences in urinary excretion, suggest that metabolic handling of the drug differs depending on the route of administration. Experiments in which inhibition of saliva secretion was measured indicated that (an) active metabolite(s) probably was (were) responsible for the action of the drug. As an anticholinergic drug, cetiedil is at least 400 times weaker than atropine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609862
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  • 21
    Electronic Resource
    Electronic Resource
    The pharmacokinetics of cefuroxime after intravenous injection (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 221-227 
    Details
    ISSN: 1432-1041
    Keywords: Cefuroxime ; cephalosporin antibiotics ; intravenous injection ; pharmacokinetics ; volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Cefuroxime, a new cephalosporin antibiotic which is stable to most β-lactamases produced by Gram-negative bacteria, was given by bolus intravenous injection to six volunteers in doses of 500 mg and 750 mg. The concentrations of cefuroxime in serum and urine were measured at pre-determined times after injection and the data analysed by a two-compartment open system model. A serum concentration of 8 µg/ml was exceeded for 100.3 min (±18.3) after a 500 mg dose and for 144.5 min (±19.8) after 750 mg. The ultimate serum half-life was 1.1 h. Excretion of cefuroxime in the urine was almost complete in 24 h, the clearance being 150 ml/min/1.73 m2. About 45% was excreted through the renal tubules. The injections were well tolerated and no changes in haematological or biochemical values were seen. The resulting data are compared with those published for some other cephalosporins. It is concluded that the favourable pharmacokinetics, especially the high concentrations of unbound cefuroxime in the serum, are likely to aid effective therapy of human infection caused by sensitive bacteria.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609865
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  • 22
    Electronic Resource
    Electronic Resource
    Human pharmacokinetics and bioavailability of temazepam administered in soft gelatin capsules (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 383-386 
    Details
    ISSN: 1432-1041
    Keywords: Benzodiazepine ; temazepam ; pharmacokinetics ; bioavailability ; hard and soft gelatine capsules
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma levels of temazepam were determined in healthy subjects after single oral administration of soft and hard gelatin capsules, and after 7 consecutive night-time doses in soft capsules. Absorption from soft gelatin capsules was significantly faster and produced earlier and higher peak plasma levels. The two pharmaceutical forms did not show any significant difference in relative availability. The apparent half-life of temazepam after night-time administration was significantly shorter than after morning administration, but no change in half-life was observed between the first and seventh night-time doses.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562455
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  • 23
    Electronic Resource
    Electronic Resource
    Disposition of valproic acid in man (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 125-132 
    Details
    ISSN: 1432-1041
    Keywords: Valproic acid ; pharmacokinetics ; saliva concentration ; urinary excretion ; serum protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of valproic acid (VPA) have been studied in 6 healthy subjects following a single 600 mg dose, and after multiple doses over 12 days (1200 mg daily) of enteric-coated sodium valproate. A time lag before absorption of 1 to 2 h was observed in each subject, and then absorption was rapid, peak concentrations being recorded 3 to 4 h after administration of the dose. The plasma level decline was biphasic with a terminal half-life of 15.9±2.6 h in the single dose and 17.3±3.0 h in the multiple dose experiments. There was no evidence of dose dependent kinetics or autoinduction. Total plasma clearance was 0.0064±0.0011 l/kg×h. The apparent volume of distribution was small at 0.15±0.2 l/kg. The mean steady state plasma concentration (Css) reached after 4 days was 81.3±13.0 µg/ml. Css observed was lower than Css predicted (99.2±14.7 µg/ml) from single dose kinetics (p〈0.001). The difference was probably due to a reduction in plasma protein binding at higher concentrations. VPA concentration in saliva was between 0.4 and 4.5% of the total plasma concentration and was not equal to the concentration of unbound drug in plasma (6.7±0.8% unbound). 3.2% of the dose was excreted in urine as the parent drug and 21.2% as conjugated metabolites.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00645133
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  • 24
    Electronic Resource
    Electronic Resource
    Overall pharmacokinetics during prolonged treatment of healthy volunteers with digoxin andβ-methyldigoxin (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 387-392 
    Details
    ISSN: 1432-1041
    Keywords: Digoxin ; β-methyldigoxin ; prolonged administration ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Five healthy volunteers received digoxin 0.4 mg or β-methyldigoxin 0.4 mg i. v., daily for 14 days, in a randomized cross-over arrangement. By monitoring minimal plasma concentrations during multiple dosing, it was found that the steady state pharmacokinetics of digoxin and β-methyldigoxin could be estimated even better by a one-compartment than by a two-compartment model. The following mean parameters were calculated: the half life of digoxin of 1.54±0.31 days was significantly shorter than the half life of 2.29±0.34 days for β-methyldigoxin. The distribution volume of 807±187 liters for digoxin was not significantly larger than the 735±227 liters for β-methyldigoxin. Renal digoxin clearance of 191±25 ml/min was significantly higher than both the renal clearance of β-methyldigoxin of 111±23 ml/min and also the creatinine clearance, which indicates tubular secretion of digoxin. There was a 2.8-fold accumulation of β-methyldigoxin injected once a day, which was significantly higher than the 1.8-fold accumulation of digoxin.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562456
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  • 25
    Electronic Resource
    Electronic Resource
    The pharmacokinetics of carbamazepine (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 451-456 
    Details
    ISSN: 1432-1041
    Keywords: Bioavailability ; carbamazepine ; elimination ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The time-courses of plasma carbamazepine concentrations were followed in six apparently healthy adult subjects who, at different times, took single oral drug doses of 200, 400, 500, 600, 700, 800 and 900 mg. There were some suggestions of impaired bioavailability of the drug when given in tablet form. The following values were obtained for various pharmacokinetic parameters:k abs =0.176±0.209 h−1;k=0.0203±0.0055 h−1; T1/2=37.5±13.1 h; VD=0.825±0.1041 · kg−1; Clearance=0.0163±0.0061 l · kg−1. The elimination rate constant showed a statistically significant increase with increasing drug dose. This may help explain the clinical observation that the rate of rise of steady state plasma carbamazepine concentrations tends to decrease with dose increase in patients taking carbamazepine alone.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561065
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  • 26
    Electronic Resource
    Electronic Resource
    Effect of exercise on the serum level and urinary excretion of tetracycline, doxycycline and sulphamethizole (1977)
    Springer
    European journal of clinical pharmacology 12 (1977), S. 367-373 
    Details
    ISSN: 1432-1041
    Keywords: Sulphamethizole ; tetracycline ; doxycycline ; rest ; exercise ; pharmacokinetics ; excretion ; absorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The serum level and urinary excretion of sulphamethizole, tetracycline and doxycycline were studied in healthy volunteers subjected to intensive exercise and bed rest in a cross-over trial. Each group consisted of 7–8 subjects. The exercise or bed rest began 15 min before oral administration of the drug and was continued for the following 4 hours. During exercise serum drug concentration and the area under the serum concentration-time curve for each agent was significantly higher (p〈0.05) than the corresponding values at rest. Exercise greatly suppressed the renal excretion of tetracycline and doxycycline, but the decrease alone appeared insufficient to account for the pronounced increase in serum drug concentration. Total drug excretion in urine was unchanged. Thus, it seemed most unlikely that overall absorption from the gastrointestinal tract had been altered by exercise. However, the rate of absorption appeared to be more rapid in the exercise than in the rest period. Marked haemoconcentration was not produced by the exercise. In addition to changes in absorption and elimination rates, alteration in the volume of distribution might contribute to the higher serum drug concentration during exercise. Therefore, the level of physical activity should be considered in the interpretation of pharmacokinetic data both in clinical practice and in pharmacokinetic studies.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562453
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  • 27
    Electronic Resource
    Electronic Resource
    Influence of sampling on drug kinetics in liver perfusion (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 335-358 
    Details
    ISSN: 1573-8744
    Keywords: pharmacokinetics ; perfusion models ; sampling ; parameter estimation ; computer program ; Org GB 94 ; mianserin ; Org GC 94
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A mathematical treatment of the influence of sampling on drug kinetics in liver perfusion is presented. Based on the derived equations, a Fortran IV computer program (PERFUS) is given, by which the time course of drug concentrations can be simulated for any sampling scheme. The simulations show that the withdrawal of large samples from the reservoir, i.e., larger than 5% of the reservoir volume, results in substantially biased parameters for drugs that are rapidly distributed and/or metabolized. For the fitting of empirical data, a Fortran IV computer program is given, based on BMDX85 nonlinear least squares by Gauss-Newton iterations. This program (PERFIT) estimates model parameters corrected as if no sampling had occurred, no matter how distorted the drug disappearance curve mày be as a result of sampling or due to degeneration of the two-compartment model into a one-compartment model. The conditions under which this degeneration occurs are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01061695
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  • 28
    Electronic Resource
    Electronic Resource
    Pharmacokinetic and biopharmaceutic profile of chlordiazepoxide HCl in healthy subjects: Single-dose studies by the intravenous, intramuscular, and oral routes (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 3-23 
    Details
    ISSN: 1573-8744
    Keywords: chlordiazepoxide ; benzodiazepine ; two-compartment model, biopharmaceutics ; pharmacokinetics ; single dose ; routes of administration ; intravenous ; intramuscular ; oral
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Single 30- mg doses of chlordiazepoxide HCl were administered to six healthy human subjects by the intravenous, oral, and intramuscular routes. Plasma concentration- time curves following intravenous administration were satisfactorily described by a biexponential equation consistent with a two-compartment open model system. Mean values of half-lives for the so-called distribution and elimination phases were 0.252 and 9.39 hr, respectively. The mean values for the volume of the central compartment (V 1) and volume of distribution $$(V_{d_\beta } )$$ were 18.0 and 30.9% of body weight, respectively. Following oral administration, the drug was rapidly and completely absorbed. Absorption was first order (t1/2≈27 min), and three of the six subjects showed a discernible lag time of approximately 20 min. Drug absorption following intramuscular administration was comparatively slow. A two- compartment “muscle model” comprised of precipitated and solubilized drug in the muscle was found to satisfactorily characterize the absorption process following administration by this route.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01064806
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  • 29
    Electronic Resource
    Electronic Resource
    A pharmacokinetic model for high-dose methotrexate infusions in man (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 421-433 
    Details
    ISSN: 1573-8744
    Keywords: methotrexate ; pharmacokinetics ; model ; computer ; cancer
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The infusion of high doses of methotrexate followed by folinic acid rescue is clinically useful against a variety of tumors. We studied the plasma pharmacokinetics of high-dose methotrexate infusions in patients with advanced cancer and devised a compartmental, kinetic model. our model is based on an earlier, mathematical model which describes the pharmacokinetics of moderate- to- high-dose methotrexate given as a single, intravenous injection. Mathematical equations for our model were solved on a UNIVAC1108 computer with the SAAM program. Seven compartments represent the distribution spaces for methotrexate and its metabolites. The transport of drug into and out of compartments is described by first-order differential equations. A nonlinear, concentration-dependent function is used for renal excretion with saturation of secretory and reabsorption mechanisms by methotrexate. Our model accurately depicts the pharmacokinetics of nine courses of therapy in five patients. The model can also be used to simulate the kinetics of methotrexate for patients with impaired renal function.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01061726
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  • 30
    Electronic Resource
    Electronic Resource
    Hepatic clearance of local anesthetics in man (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 111-122 
    Details
    ISSN: 1573-8744
    Keywords: hepatic clearance ; extraction ratio ; local anesthetics ; pharmacokinetics ; lidocaine ; bupivacaine ; etidocaine ; cardiovascular effects of local anesthetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Two independent methods of calculating hepatic drug clearance were applied to data from studies of the human pharmacokinetics of lidocaine, bupivacaine, and etidocaine. Within experimental limitations, agreement was good between estimates obtained by measurement of areas under blood drug concentration-time curves after rapid intravenous injection and by direct measurement of arterial and hepatic venous drug concentrations. Apparent hepatic extraction ratios of the agents followed the order etidocaine (∼0.73)/s〉lidocaine (∼0.68〉bupivacaine (∼0.37).Pharmacokinetic implications of increases in hepatic blood flow induced by the agents are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01066215
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  • 31
    Electronic Resource
    Electronic Resource
    Pharmacokinetic and biopharmaceutic profile of chlordiazepoxide HCl in healthy subjects: Multiple-dose oral administration (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 25-39 
    Details
    ISSN: 1573-8744
    Keywords: chlordiazepoxide ; benzodiazepine ; two-compartment model ; multiple dosing ; pharmacokinetics ; biopharmaceutics ; metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Eight healthy male volunteers received chlordiazepoxide HCl orally at a dosage of 10 mg every 8 hr over a period of 21 days. On day 22, the regimen was changed to 30 mg every 24 hr for an additional 15 days. Plasma concentrations of chlordiazepoxide and its metabolites desmethyl-chlordiazepoxide, demoxepam, and desoxydemoxepam were measured during 14 of the 36 treatment days. Chlordiazepoxide plasma concentration- time data were consistent with first-order absorption and complete bioavailability. The harmonic mean absorption half-life was 12.3 min. Disposition of chlordiazepoxide was described by a two-compartment open model with a harmonic mean terminal exponential half-life of 10.1 hr. Average steady — state plasma levels of chlordiazepoxide, desmethylchlordiazepoxide, and demoxepam were approximately 0.75, 0.54, and 0.36 μg/ml, respectively.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01064807
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  • 32
    Electronic Resource
    Electronic Resource
    Curve fitting and modeling in pharmacokinetics and some practical experiences with NONLIN and a new program FUNFIT (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 513-531 
    Details
    ISSN: 1573-8744
    Keywords: pharmacokinetics ; nonlinear regression ; curve fitting ; computer program ; time sharing ; modeling ; weighting ; least squares ; parameter estimation ; discrimination between models
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The problems of curve fitting and modeling in pharmacokinetics are discussed. A new nonlinear regression program FUNFIT, written for interactive time sharing, is presented which should be more reliable than programs based on the Gauss-Newton or other related gradient methods. The new program and the well-established program NONLIN were tested on two linear models using human plasma drug level data. FUNFIT found a substantially better solution than NONLIN in the majority of the cases.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01061732
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  • 33
    Electronic Resource
    Electronic Resource
    Gentamicin disposition and tissue accumulation on multiple dosing (1977)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 559-577 
    Details
    ISSN: 1573-8744
    Keywords: gentamicin ; tissue distribution ; pharmacokinetics ; two-compartment modeling
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Gentamicin pharmacokinetics was examined in a group of 47 patients with stable renal function treated an average of 10 days for severe infection. Serum concentrations rose continually during treatment, and declined in two phases after the drug was stopped, with a mean half-life of 112hr (range 27–693 hr) in the second phase. A two-compartment model was used to describe the biphasic decline in serum concentrations and to calculate the amount of drug in the tissue compartment at all times during and after treatment. Predicted tissue amounts of gentamicin rose continually on multiple dosing in all patients. In six patients who died, postmortem tissues were obtained to quantitate recovery. In all cases, the predicted amount of gentamicin in tissues was in close agreement with the amount recovered at autopsy. Tissue distribution and accumulation constitute a major reason for variability in gentamicin pharmacokinetics and explain both the rising peak and trough serum concentrations and the prolonged detection of gentamicin in serum and urine after the drug is stopped.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01059684
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