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  • 1
    Electronic Resource
    Electronic Resource
    Effect of magnesium hydroxide on the absorption and efficacy of tolbutamide and chlorpropamide (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 675-679 
    Details
    ISSN: 1432-1041
    Keywords: Tolbutamide ; Magnesium hydroxide ; chlorpropamide ; gastrointestinal absorption ; drug interaction ; healthy volunteers ; plasma glucose ; plasma insulin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of magnesium hydroxide on the absorption and efficacy of tolbutamide and chlorpropamide was examined in a total of 32 healthy volunteers in two separate, randomized parallel-group studies, with 16 subjects in each study. After an overnight fast, the first group of 8 volunteers ingested 500 mg tolbutamide or 250 mg chlorpropamide with 150 ml water, and the second group the same doses of the active drugs with 150 ml water containing 850 mg magnesium hydroxide. Magnesium hydroxide increased the area under the plasma tolbutamide concentration-time curve (AUC) from 0 to 1 h and from 0 to 2 h by 5-fold and 2.5-fold, respectively. The peak plasma concentration, peak time and total AUC were not significantly altered. The incremental insulin area and the decremental glucose area from 0 to 1.5 h were significantly larger in the magnesium hydroxide group than in the controls. The maximum insulin response to tolbutamide was increased fourfold by coadministration of magnesium hydroxide, and it occurred about 1 h earlier than in the control group. In addition, the maximum fall in plasma glucose concentration was attained about 1 h earlier in the antacid group. A tendency to an increased rate of chlorpropamide absorption was observed after magnesium hydroxide, but it did not appear to affect the insulin and glucose responses to chlorpropamide. It is concluded that magnesium hydroxide increased the early bioavailability of tolbutamide, resulting in enhanced insulin and glucose responses. A tendency toward accelerated chlorpropamide absorption by magnesium hydroxide was also observed, but the efficacy of chlorpropamide was unaffected.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00265936
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  • 2
    Electronic Resource
    Electronic Resource
    Effect of zinc sulphate on the absorption of tetracycline and doxycycline in man (1975)
    Springer
    European journal of clinical pharmacology 9 (1975), S. 131-134 
    Details
    ISSN: 1432-1041
    Keywords: Drug interaction ; drug absorption ; zinc sulphate ; tetracycline ; doxycycline
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A possible interaction between zinc sulphate and tetracycline or doxycycline was examined in a cross-over study in seven volunteers. A single dose of zinc sulphate (45 mg Zn++) was given simultaneously with tetracycline hydrochloride (500 mg) or doxycycline chloride (200 mg). The serum concentration of tetracycline, the area under the serum tetracycline concentration-time curve and the excretion of tetracycline in urine were reduced by about 30% (p〈0.05) from the respective control values. The absorption of doxycycline was not influenced significantly by zinc sulphate. The clinical significance of the zinc-tetracycline interaction seems to be of limited importance.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614009
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  • 3
    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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  • 4
    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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  • 5
    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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  • 6
    Electronic Resource
    Electronic Resource
    Effect of dose of charcoal on the absorption of disopyramide, indomethacin and trimethoprim by man (1984)
    Springer
    European journal of clinical pharmacology 26 (1984), S. 761-767 
    Details
    ISSN: 1432-1041
    Keywords: drug absorption ; intoxication ; activated charcoal ; disopyramide ; indomethacin ; trimethoprim ; healthy volunteers ; adsorption capacity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The efficacy of various charcoal-to-drug ratios for the absorption of drugs was studied in 6 healthy volunteers and in vitro at two pHs. Disopyramide 200 mg, indomethacin 50 mg and trimethoprim 200 mg were ingested on an empty stomach with 100 ml water. After 5 min the subjects ingested a charcoal suspension in 300 ml — 2.5 g, 10 g, 25 g or 50 g of Norit A, or 10 g of PX-21, or water 300 ml only. Increasing the dose of activated charcoal from 2.5 g to 50 g reduced the gastrointestinal absorption of disopyramide and indomethacin from 30–40% to 3–5%, and that of trimethoprim from 10% to 1% of the respective controls. Disopyramide and trimethoprim were best adsorbed by charcoal in vitro at neutral and indomethacin at acid pH, but saturation of the adsorption capacity was apparent at charcoal-to-drug ratios less than 7.5. Combining the in vitro and in vivo results it can be concluded that the dose of activated charcoal to be given in acute intoxication should be as large as possible, because the drug history is often unknown.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541939
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  • 7
    Electronic Resource
    Electronic Resource
    Differential effects of sodium bicarbonate and aluminium hydroxide on the absorption and activity of glipizide (1991)
    Springer
    European journal of clinical pharmacology 40 (1991), S. 383-386 
    Details
    ISSN: 1432-1041
    Keywords: Glipizide ; gastrointestinal absorption ; sodium bicarbonate ; aluminium hydroxide ; glucose ; drug interaction ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of sodium bicarbonate and aluminium hydroxide on the absorption and activity of glipizide have been studied in healthy volunteers in two randomized cross-over trials. After an overnight fast, 5 mg glipizide was given either with 150 ml water or with water containing 3.0 g sodium bicarbonate or 1.0 g aluminium hydroxide. Sodium bicarbonate significantly increased the AUC of plasma glipizide from 0 to 0.5 h, 0 to 1 h, and from 0 to 2 h (six-, four- and twofold, respectively). The time to peak concentration (tmax) fell from 2.5 h during the control phase to 1.0 h during the sodium bicarbonate phase. The absorption half-life (t1/2a), lag time and mean residence time (MRT) were also significantly decreased. No significant change in peak plasma concentration (Cmax), total AUC or elimination half-life (t1/2) was noted. The decremental plasma glucose areas from 0 to 1 h and 0 to 2 h were significantly larger (80% and 50%, respectively) than during the control phase. The maximal decrease in glucose was 50% greater during the sodium bicarbonate phase, and the time to reach it was reduced by 35 min. Aluminium hydroxide had no significant effects on the rate or extent of absorption of glipizide, and the glucose response also remained unaffected. It is concluded that the concomitant ingestion of sodium bicarbonate and glipizide may result in accelerated absorption of glipizide and an increased effect on glucose. A common dose of aluminium hydroxide did not appear to affect the absorption of glipizide.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00265848
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