Effects of resins and activated charcoal on the absorption of digoxin, carbamazepine and frusemide.

Neuvonen, Pertti J.; Kivistö, Kari T.; Hirvisalo, E. L.

doi:10.1111/j.1365-2125.1988.tb03295.x

Cited by 46 publications

(19 citation statements)

References 14 publications

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“…A small dose of charcoal (8g) completely prevented (99.5%) the absorption ofa therapeutic dose (40mg) of frusemide (Neuvonen et al 1987). A small dose of charcoal (8g) completely prevented (99.5%) the absorption ofa therapeutic dose (40mg) of frusemide (Neuvonen et al 1987).…”

Section: Diureticsmentioning

confidence: 99%

Oral Activated Charcoal in the Treatment of Intoxications

1988

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Activated charcoal has an ability to adsorb a wide variety of substances. This property can be applied to prevent the gastrointestinal absorption of various drugs and toxins and to increase their elimination, even after systemic absorption. Single doses of oral activated charcoal effectively prevent the gastrointestinal absorption of most drugs and toxins present in the stomach at the time of charcoal administration. Known exceptions are alcohols, cyanide, and metals such as iron and lithium. In general, activated charcoal is more effective than gastric emptying. However, if the amount of drug or poison ingested is very large or if its affinity to charcoal is poor, the adsorption capacity of activated charcoal can be saturated. In such cases properly performed gastric emptying is likely to be more effective than charcoal alone. Repeated dosing with oral activated charcoal enhances the elimination of many toxicologically significant agents, e.g. aspirin, carbamazepine, dapsone, dextropropoxyphene, cardiac glycosides, meprobamate, phenobarbitone, phenytoin and theophylline. It also accelerates the elimination of many industrial and environmental intoxicants. In acute intoxications 50 to 100g activated charcoal should be administered to adult patients (to children, about 1 g/kg) as soon as possible. The exceptions are patients poisoned with caustic alkalis or acids which will immediately cause local tissue damages. To avoid delays in charcoal administration, activated charcoal should be a part of first-aid kits both at home and at work. The 'blind' administration of charcoal neither prevents later gastric emptying nor does it cause serious adverse effects provided that pulmonary aspiration in obtunded patients is prevented. In severe acute poisonings oral activated charcoal should be administered repeatedly, e.g. 20 to 50g at intervals of 4 to 6 hours, until recovery or until plasma drug concentrations have fallen to non-toxic levels. In addition to increasing the elimination of many drugs and toxins even after their systemic absorption, repeated doses of charcoal also reduce the risk of desorbing from the charcoal-toxin complex as the complex passes through the gastrointestinal tract. Charcoal will not increase the elimination of all substances taken. However, as the drug history in acute intoxications is often unreliable, repeated doses of oral activated charcoal in severe intoxications seem to be justified unless the toxicological laboratory has identified the causative agent as not being prone to adsorption by charcoal. The role of repeated doses of oral activated charcoal in chronic intoxication has not been clearly defined.(ABSTRACT TRUNCATED AT 400 WORDS)

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Section: Diureticsmentioning

confidence: 99%

Oral Activated Charcoal in the Treatment of Intoxications

1988

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“…In the publication by Lapatto-Reiniluoto, the authors reported a reduction of absorption of carbamazepine (measured as the AUC 0-24 ) by activated charcoal of 62% [31]. In another publication, the absorption of 400 mg oral carbamazepine was decreased greatly (90%) by activated charcoal [32].…”

Section: Discussionmentioning

confidence: 99%

Seromucosal Transport of Intravenously Administered Carbamazepine Is Not Enhanced by Oral Doses of Activated Charcoal in Rats

Eyer¹,

Jung²,

Neuberger³

et al. 2008

Basic Clin Pharma Tox

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Abstract:The fate of carbamazepine after intravenous injection in rats (n = 24) and the influence of activated charcoal on the kinetics was investigated. After randomization to four groups (n = 6, each), plasma concentration and the quantities of carbamazepine and metabolites excreted into bile, urine and intestine were determined using an in situ perfusion model of the small intestine (Ringer's solution) with or without orally administered activated charcoal (AC + ; AC-) and with or without bile duct cannulation (BD + ; BD -). The cumulative amount of carbamazepine and metabolites exsorbed into the small intestine within 3.5 hr after intravenous injection was about 15% in BD -animals and about 3% in BD + animals. About 20% of the dose was detected in the externalized bile. Activated charcoal did not influence the amount exsorbed into the small intestine. Terminal half-life in plasma ranged from 159 min. to 194 min. within the four treatment groups without statistical significant difference (P = 0.751). Correspondingly, the area under the curve did not vary significantly and ranged between 1.13 and 1.41 g/min./l (P = 0.378). Excretion of carbamazepine and metabolites into urine varied between 3% and 6% of dose within all groups and showed close correlation with diuresis. In an identical experimental approach using a 2-fold intestinal perfusion rate (50 ml/hr; n = 8), no fundamental changes compared to the main experiment regarding pharmacokinetics of carbamazepine were observed. The lack of effect of activated charcoal on the elimination of carbamazepine and metabolites must be contributed to the small amount of the drug being exsorbed into the intestine and may be further influenced by reduced intestinal permeability of carbamazepine and metabolites or inadequate luminal stirring.Activated charcoal is a widely used and generally accepted agent to prevent the absorption of orally ingested drugs, especially in the overdose setting. Although there are no satisfactorily designed clinical studies assessing the benefit from single-dose activated charcoal to recommend this therapy [1], data from literature clearly support the use of multipledose activated charcoal for some toxins such as carbamazepine, dapson, phenobarbital, quinine and theophylline in the case of overdose [2]. Besides the prevention of drug absorption and the possibility of activated charcoal interrupting the enteroenteric circulation, oral administration has also been demonstrated to enhance the clearance of intravenously administered drugs that are exsorbed seromucosally into the intestinal lumen in rats [3][4][5][6][7][8][9][10][11][12]. This process is generally called 'gastrointestinal dialysis' since it was first described in 1982 [13]. Basic pharmacokinetic requirements for clinically relevant seromucosal transport include small size of molecule, intermediate lipophilicity, low protein binding and a small volume of distribution.If a relevant amount of drug would be exsorbed into the intestinal lumen and if orally administered activated charcoa...

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“…Colestipol can affect the bioavailability of gemfibrozil, thiazide diuretics, propranolol, furosemide, tetracycline, and penicillin G [13]. Absorption of digoxin is not affected by colestipol [166]. Colesevelam did not decrease the absorption of digoxin, fenofibrate, lovastatin, warfarin, digoxin, metoprolol, quinidine and valproic [82,167].…”

Section: Adverse Effects and Drug Interactionsmentioning

confidence: 99%

Lipid-Lowering Drugs Acting at the Level of the Gastrointestinal Tract

Filippatos

Mikhailidis²

2009

CPD

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This review considers the hypolipidaemic drugs that act on the gastrointestinal (GI) tract. We searched PubMed up to April 2008 and included randomized controlled trials, original papers, review articles and case reports. Bile acid sequestrants (BAS) have a well-established low density lipoprotein cholesterol (LDL-C) lowering effect, but may increase triglyceride (TG) levels. BAS have no systematic adverse effects, but are associated with increased GI adverse effects and interactions with the absorption of other drugs. Ezetimibe improves LDL-C, high density lipoprotein cholesterol and TG levels, as monotherapy or especially when given with a statin. Ezetimibe has not been associated with serious adverse effects. Ezetimibe has not been evaluated in large clinical trials with cardiovascular disease (CVD) endpoints. Phytosterols are not licensed drugs; they have a well-established LDL-C lowering effect, but there are no large long-term randomized clinical trials investigating their effects on CVD events. Orlistat is an antiobesity drug with a small additional LDL-C lowering effect independent of weight loss. Orlistat-assisted weight loss improves the overall lipid profile, carbohydrate metabolism and transaminase activities. However, its use should be limited to weight reduction. This drug is associated with increased GI adverse effects.

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Effects of resins and activated charcoal on the absorption of digoxin, carbamazepine and frusemide.

Cited by 46 publications

References 14 publications

Oral Activated Charcoal in the Treatment of Intoxications

Oral Activated Charcoal in the Treatment of Intoxications

Seromucosal Transport of Intravenously Administered Carbamazepine Is Not Enhanced by Oral Doses of Activated Charcoal in Rats

Lipid-Lowering Drugs Acting at the Level of the Gastrointestinal Tract

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