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  • activated charcoal  (5)
  • gastrointestinal absorption  (3)
  • 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
    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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  • 3
    Electronic Resource
    Electronic Resource
    Effect of activated charcoal on absorption and elimination of phenobarbitone, carbamazepine and phenylbutazone in man (1980)
    Springer
    European journal of clinical pharmacology 17 (1980), S. 51-57 
    Details
    ISSN: 1432-1041
    Keywords: activated charcoal ; phenobarbitone ; carbamazepine ; phenylbutazone ; absorption ; elimination ; acute intoxication
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of activated charcoal, given as a water suspension, on the absorption and elimination of phenobarbitone 200 mg, carbamazepine 400 mg and phenylbutazone 200 mg, was studied in five healthy volunteers, using a randomized crossover design. Absorption of the drugs was almost completely prevented (more than 95%) when charcoal 50 g was ingested within five minutes of taking the drugs. When activated charcoal was taken one hour after the drugs, the mean inhibition of drug absorption was considerably less and the inhibition was greatly dependent on the individual rate of absorption. The half-life of phenobarbitone was markedly shortened from a control value of 110±23 h to 19.8±1.0 h (P〈0.05), with a corresponding increase in plasma clearance from 4.6 ml/min to 23 ml/min, when activated charcoal 118 g, in five divided doses was given between 10 and 48 h after ingestion of the drug. The half-life of carbamazepine was shortened by 45% (P〈0.05) and the reduction in the half-life of phenylbutazone (30%) by charcoal, too, was statistically significant. The only side effect from use of the charcoal suspension was constipation, which occured in three subjects after repeated doses, and which was easily treated with lactulose if required. Although activated charcoal should be given as soon as possible, even its delayed use may be indicated, due to the slow absorption often seen in acute intoxication. The use of multiple doses of charcoal appears to be indicated as an additional treatment of certain severe intoxications to prevent the release of drugs from charcoal, and to increase their rate of elimination if they are secreted into the gut with subsequent reabsorption.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561677
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  • 4
    Electronic Resource
    Electronic Resource
    Effect of activated charcoal on absorption of tolbutamide and valproate in man (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 243-246 
    Details
    ISSN: 1432-1041
    Keywords: tolbutamide ; valproate ; intoxication ; activated charcoal ; inhibition of absorption ; sulphonylureas ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The claim that activated charcoal should be ineffective or even contraindicated in intoxication due to tolbutamide is based only on limited in vitro studies. To test the claim, the effect of activated charcoal 50 g on the absorption of tolbutamide and, as a reference, of sodium valproate, was studied in 6 healthy volunteers. Each volunteer swallowed tolbutamide 500 mg and sodium valproate 300 mg with 50 ml water 1 h after a light breakfast, and within 5 min they took in randomized order either a suspension of activated charcoal or water. The absorption of tolbutamide, calculated as the peak concentration and the area under the serum drug concentration-time curve during 0–48 h, was reduced by 90% by charcoal (p〈0.001). The absorption of valproate in these conditions was reduced on average by 65% (p〈0.01). In each subject charcoal had a greater effect on the absorption of tolbutamide than of valproate. According to these findings and preliminary in vitro studies on other sulphonylureas high doses of activated charcoal can be recommended for the preventing the absorption of sulphonylureas in acute intoxications. The poor aqueous solubility of these substances at the gastric pH probably delays their gastrointestinal absorption, so that they may be adsorbed on to charcoal even given several hours later.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613825
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  • 5
    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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  • 6
    Electronic Resource
    Electronic Resource
    Activated charcoal in the treatment of hypercholesterolaemia: dose-response relationships and comparison with cholestyramine (1989)
    Springer
    European journal of clinical pharmacology 37 (1989), S. 225-230 
    Details
    ISSN: 1432-1041
    Keywords: hypercholesterolaemia ; cholestyramine ; activated charcoal ; dose-response ; total cholesterol ; LDL ; HDL
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The dose-response relationship of activated charcoal in reducing serum cholesterol was determined and the effects of charcoal and cholestyramine were compared in patients with hypercholesterolaemia. In a cross-over study 7 patients ingested charcoal 4, 8, 16 or 32 g/day, and finally bran, each phase lasting for 3 weeks. Serum total and LDL-cholesterol were decreased (maximum 29% and 41%, respectively) and the ratio of HDL/LDL-cholesterol was increased (maximum 121%) by charcoal in a dose dependent manner. Ten further patients with severe hypercholesterolaemia ingested daily for 3 weeks, in random order, activated charcoal 16 g, cholestyramine 16 g, activated charcoal 8 g + cholestyramine 8 g, or bran. The concentrations of total and LDL-cholesterol were reduced by charcoal (23% and 29%, respectively), cholestyramine (31% and 39%) and their combination (30% and 38%). The ratio of HDL/LDL-cholesterol was increased from 0.13 to 0.23 by charcoal, to 0.29 by cholestyramine, and to 0.25 by their combination. Serum triglycerides were increased by cholestyramine but not by charcoal. Other parameters, including the serum concentrations of vitamin A, E and 25(OH)D3 remained unaffected. The changes in lipids only partly subsided during the 3-week bran phase. In general, the acceptability by the patients and the efficacy of activated charcoal, cholestyramine and their combination were about equal, but there were individual preferences for particular treatments.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00679774
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  • 7
    Electronic Resource
    Electronic Resource
    Effect of magnesium hydroxide on the absorption of tolfenamic and mefenamic acids (1988)
    Springer
    European journal of clinical pharmacology 35 (1988), S. 495-501 
    Details
    ISSN: 1432-1041
    Keywords: tolfenamic acid ; mefenamic acid ; fenamates ; gastrointestinal absorption ; magnesium hydroxide ; aluminium hydroxide ; sodium bicarbonate ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of various antacids on the absorption of tolfenamic and mefenamic acids has been investigated in three separate crossover studies, each consisting of four phases. Single doses of magnesium hydroxide (85 mg, 425 mg and 1700 mg) or of water (150 ml) were given by mouth to 6 healthy volunteers immediately after tolfenamic acid 400 mg (Study 1), and, using an identical study design, after mefenamic acid 500 mg (Study 3). In Study 2 sodium bicarbonate 1 g, aluminium hydroxide 1 g, an antacid preparation containing both aluminium and magnesium hydroxides, or water alone were ingested with tolfenamic acid 400 mg. Plasma concentrations of tolfenamic and mefenamic acids and their cumulative excretion in urine were determined up to 24 h. Magnesium hydroxide greatly accelerated, in a dose-dependent manner the absorption of both tolfenamic and mefenamic acids. The peak times in plasma were shortened by about 1 h by 425 mg and 1700 mg magnesium hydroxide, and the peak plasma concentrations of both fenamates were elevated up to 3-fold. The area under the plasma concentration-time curve between 0 and 1 h of tolfenamic acid was increased up to 7-fold and that of mefenamic acid up to 3-fold. The total bioavailability of tolfenamic and mefenamic acids was only slightly increased. Aluminium hydroxide alone and in combination with magnesium hydroxide significantly retarded the absorption and lowered the peak plasma concentration of tolfenamic acid. Sodium bicarbonate had no significant effect on its absorption. The interaction with magnesium hydroxide leads to higher and earlier peak plasma concentrations of the fenamates. Aluminium hydroxide prevents this effect of magnesium hydroxide. If rapid onset of the analgesic effect of the fenamates is required, concomitant ingestion of the fenamates with an antacid containing magnesium but not aluminium hydroxide is recommended.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558244
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  • 8
    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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