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  • 21
    Electronic Resource
    Electronic Resource
    Inhibitory effect of various iron salts on the absorption of tetracycline in man (1974)
    Springer
    European journal of clinical pharmacology 7 (1974), S. 357-360 
    Details
    ISSN: 1432-1041
    Keywords: Tetracycline absorption ; iron salts ; drug absorption ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The inhibitory effect of various iron salts, all containing 40 mg elemental iron, on the absorption of tetracycline (500 mg) administered simultaneously has been compared in a double-blind cross-over study in 6 healthy human volunteers. On the basis of changes in peak serum tetracycline concentration, area under individual serum tetracycline concentration-time curves and urinary excretion of tetracycline, the following order of inhibition of tetracycline absorption was found: ferrous sulphate 〉 ferrous fumarate, ferrous succinate, ferrous gluconate 〉 ferrous tartrate 〉 ferric sodium edetate. Thus, in addition to different pharmaceutical properties of iron tablets or capsules, the type of iron salt used may significantly influence the absorption of simultaneously ingested tetracycline.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558206
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  • 22
    Electronic Resource
    Electronic Resource
    Effect of oral ferrous sulphate on the half-life of doxycycline in man (1974)
    Springer
    European journal of clinical pharmacology 7 (1974), S. 361-363 
    Details
    ISSN: 1432-1041
    Keywords: Iron ; doxycycline ; drug interaction ; enterohepatic circulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a double-blind cross-over study in seven patients, oral ferrous sulphate (80 mg Fe++) given 3, 7 and 11 h after a daily oral dose of doxycycline, lowered the serum concentration of doxycycline by 20–45%. The half-life of intravenous doxycycline was shortened from 16.6±0.7 h to 11.0±0.4 h by concomitant oral iron therapy. These results are an indirect indication of significant intestinal secretion and reabsorption of doxycycline. The interaction between doxycycline and iron cannot be avoided completely by leaving an interval of 3 h between doses of the two drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558207
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  • 23
    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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  • 24
    Electronic Resource
    Electronic Resource
    Cimetidine-phenytoin interaction: Effect on serum phenytoin concentration and antipyrine test (1981)
    Springer
    European journal of clinical pharmacology 21 (1981), S. 215-220 
    Details
    ISSN: 1432-1041
    Keywords: phenytoin ; cimetidine ; antipyrine test ; drug interaction ; drug metabolism ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a prospective study in nine patients the effects of phenytoin and of cimetidine (1000mg/day) + phenytoin on the antipyrine test and serum phenytoin concentrations were studied. Serum phenytoin increased from the steady state level of 5.7±1.3 mg/l to 9.1±1.4mg/l after three weeks on cimetidine (p〈0.01), and fell to 5.8±1.2 mg/l within two weeks after withdrawal of cimetidine. The protein binding of phenytoin was not changed by cimetidine. After use of phenytoin for 2–4 months, antipyrine clearance increased from 0.67±0.06ml/min/kg to 1.61±0.22 ml/ min/kg, and antipyrine half-live fell from 10.9±1.3h to 4.5±0.6h as compared to the values before phenytoin treatment (p〈0.01). After three weeks combined use of cimetidine and phenytoin, antipyrine clearance was decreased to 1.01±0.07 ml/min/kg and antipyrine half-life was prolonged to 6.1±0.5h, (p〈0.01) compared to the values on phenytoin alone. The distribution volume of antipyrine was not affected by phenytoin nor by cimetidine + phenytoin. The half-life of cimetidine was 2.8±0.3h in the patients on longterm phenytoin treatment. There was a significant positive correlation (p〈0.001) between the increase in serum phenytoin concentration and the prolongation of antipyrine half-life caused by cimetidine. Thus, cimetidine increases serum phenytoin concentration, very probably by inhibiting its metabolism. Care should be taken in the concomitant use of cimetidine and phenytoin, and the dose of phenytoin should be modified according to the clinical symptoms and serum phenytoin concentrations.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00627923
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  • 25
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of chlormethiazole in healthy volunteers and patients with cirrhosis of the liver (1980)
    Springer
    European journal of clinical pharmacology 17 (1980), S. 275-284 
    Details
    ISSN: 1432-1041
    Keywords: chlormethiazole ; cirrhosis of the liver ; antipyrine ; protein binding ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of chlormethiazole after oral and intravenous administration was studied in six healthy volunteers and eight patients with alcoholic cirrhosis of the liver. Plasma concentration-time curve after the intravenous infusion could adequately be described by two- or three-compartment open models both in healthy volunteers and in the patients. Based on the areas under the plasma concentration-time curves, the systemic bioavailability of oral chlormethiazole was about ten times greater in the patients than in healthy controls. The elimination of chlormethiazole was relatively less retarded in the patients, as indicated by a decrease of about 30% in its plasma clearance. In the patients the plasma protein binding of chlormethiazole was decreased, but the volume of distribution and half-life of elimination were unchanged. The increase in bioavailability of chlormethiazole was associated with significant alteration in the serum levels of bilirubin, albumin, alkaline phosphatase, prothrombin-proconvertin activity (P + P) and elimination rate of antipyrine or14C-aminopyrine. The increased bioavailability of oral chlormethiazole was due to impaired first-pass metabolism in the cirrhotic liver. A considerable reduction in dose seems to be indicated if oral chlormethiazole is used in patients with advanced cirrhosis of the liver. A substantial fraction of dose, averaging 15%, was lost during the intravenous infusion, presumably due to adsorption to the infusion tubing.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00625801
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  • 26
    Electronic Resource
    Electronic Resource
    Reduction of absorption of digoxin, phenytoin and aspirin by activated charcoal in man (1978)
    Springer
    European journal of clinical pharmacology 13 (1978), S. 213-218 
    Details
    ISSN: 1432-1041
    Keywords: Activated charcoal ; acute intoxication ; digoxin ; phenytoin ; aspirin ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The inhibitory effect of activated charcoal 50 g suspended in water on the absorption of digoxin, phenytoin and aspirin was studied in six healthy volunteers in a cross-over manner. The absorption of digoxin and phenytoin were almost completely prevented (about 98%) when activated charcoal was ingested immediately after the drug. The total absorption of aspirin was inhibited by 70%, with clear postponement of absorption and partial release of aspirin from the charcoal in the gut: The peak serum concentration of aspirin was reduced by 95% by charcoal. When activated charcoal was ingested 1 hour after the drugs the inhibition of absorption was considerably less. However, since the absorption of larger doses of the drugs is often slow, the administration of an adequate dose of activated charcoal will be of definite value in the treatment of acute intoxication, even if delayed for several hours.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609985
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  • 27
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of metformin after intravenous and oral administration to man (1979)
    Springer
    European journal of clinical pharmacology 16 (1979), S. 195-202 
    Details
    ISSN: 1432-1041
    Keywords: metformin ; biguanides ; pharmacokinetics ; absorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of14C-metformin have been studied in five healthy subjects after oral and intravenous administration. The intravenous dose was distributed to a small central compartment of 9.9±1.61 ( $$\bar X$$ ±SE), from which its elimination could be described using three-compartment open model. The elimination half-life from plasma was 1.7±0.1 h. Urinary excretion data revealed a quantitatively minor terminal elimination phase with a half-life of 8.9±0.7 h. After the intravenous dose, metformin was completely excreted unchanged in urine with a renal clearance of 454±47 ml/min. Metformin was not bound to plasma proteins. The concentration of metformin in saliva was considerably lower than in plasma and declined more slowly. The bioavailability of metformin tablets averaged 50–60%. The rate of absorption was slower than that of elimination, which resulted in a plasma concentration profile of “flip-flop” type for oral metformin.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562061
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  • 28
    Electronic Resource
    Electronic Resource
    Human pharmacokinetics of tolfenamic acid, a new anti-inflammatory agent (1981)
    Springer
    European journal of clinical pharmacology 19 (1981), S. 359-365 
    Details
    ISSN: 1432-1041
    Keywords: tolfenamic acid ; anti-inflammatory agent ; human pharmacokinetics ; bioavailability ; intravenous administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of tolfenamic acid, a new anti-inflammatory agent was studied in six healthy volunteers after an intravenous dose of 100 mg and oral doses of 100, 200, 400 and 800 mg. The disposition of intravenous tolfenamic acid could be described by two-compartment open model, with a central compartment volume (Vdc) of 5.6±0.31 (mean±SE), volume during β-phase (Vdβ) of 31±21, and a total elimination rate constant (k10) 1.6±0.1 h−1. The terminal elimination half-life was 2.5±0.6 h and the total plasma clearance 155±15 ml/min. The elimination occured principally by extrarenal mechanisms, the recovery of unchanged drug together with is glucuronide in urine averaging only 8.8% of the intravenous dose. The binding of tolfenamic acid to plasma proteins averaged 99.7%. The gastrointestinal absorption had a mean half-life of 1.7±0.1 h. Based on comparison of areas under the plasma concentration time-curves after intravenous and oral administration, the biovailability of tolfenamic acid capsules averaged 60%. The rate and extent of absorption and the rate of elimination of tolfenamic acid were independent of dose.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544587
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  • 29
    Electronic Resource
    Electronic Resource
    Prolonged Q-T interval and severe tachyarrhythmias, common features of sotalol intoxication (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 85-89 
    Details
    ISSN: 1432-1041
    Keywords: beta-blockers ; sotalol ; intoxication ; Q-T interval ; tachyarrhythmias
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The findings in six patients admitted to hospital 0.5–4.5 h after the ingestion of an overdose of 2.4–8 g sotalol are described. In addition to bradycardia and hypotension, all patients had a considerably prolonged corrected Q-T interval, up to 172±8% of normal. Severe ventricular tachyarrhythmias occurred in five of the six patients, the risk was greatest up to 20 h after the ingestion of sotalol. The long Q-T interval returned to normal over 3 to 4 days, which is consistent with the long half-life of sotalol. In addition to its beta-blocking action, sotalol has marked electrophysiological properties of a Class III antiarrhythmic drugs, which are likely to be able to account for its observed effects. Special attention should be paid to the risk of severe ventricular arrhythmias in sotalol intoxications.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607142
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  • 30
    Electronic Resource
    Electronic Resource
    Comparison of activated charcoal and ipecac syrup in prevention of drug absorption (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 557-562 
    Details
    ISSN: 1432-1041
    Keywords: drug absorption ; acute intoxication ; activated charcoal ; ipecac syrup ; paracetamol ; tetracycline ; aminophylline
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The efficacy of activated charcoal and ipecac syrup in the prevention of drug absorption was studied in 6 healthy adult volunteers, using a randomized, cross-over design. Paracetamol 1000 mg, tetracycline 500 mg and aminophylline 350 mg were ingested on an empty stomach with 100 ml water. Then, after 5 or 30 min, the subjects ingested, either activated charcoal suspension (50 g charcoal), syrup of ipecac, or, only after 5 min, water 300 ml. Activated charcoal, given either after 5 or 30 min, significantly (p〈0.01 or 〈0.05) reduced the absorption of these 3 drugs measured, for example as AUC0–24h. Syrup of ipecac caused emesis on each occasion, with a mean delay of 15 min. When ipecac was given 5 min after the drugs, its effect on absorption was significant, but when it was given after 30 min only the absorption of tetracycline was reduced. Activated charcoal was significantly (p〈0.05) more effective than ipecac in reducing drug absorption when given at the same time points. In cases of acute intoxication, depending on the quality and quantity of the drugs ingested, the relative efficacy of charcoal and ipecac may be somewhat different from that observed in the present study. Despite its emetic action, however, ipecac syrup is not very effective in preventing drug absorption and, in general, activated charcoal should also be given after induced emesis or gastric lavage.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609903
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