Determination of the adsorption of tramadol hydrochloride by activated charcoal in vitro and in vivo

Although tramadol is one of the most widely used centrally acting analgesics worldwide, no literature is available regarding adsorption of tramadol HCl powder or tablets (Ultram; 50 mg tramadol HCl per tablet) by activated charcoal (AC) for use as potential adjunct treatment of overdose. The present...

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Published inJournal of pharmacological and toxicological methods Vol. 43; no. 3; pp. 205 - 210
Main Authors Raffa, Robert B, Wu, Chunyu, Stone, Dennis J, Borenstein, Michael R, Codd, Ellen E, Coogan, Timothy P
Format Journal Article
LanguageEnglish
Published United States Elsevier Inc 01.05.2000
Subjects
Activated charcoal
Adsorption
Animals
Antidotes - chemistry
Antidotes - therapeutic use
Calibration
Charcoal - chemistry
Dose-Response Relationship, Drug
Drug overdose
Lethal Dose 50
Male
Method
Mice
Mice, Inbred ICR
Narcotics - chemistry
Narcotics - toxicity
Pain Measurement - drug effects
Spectrophotometry, Ultraviolet
Suspensions
Tablets
Tramadol
Tramadol - chemistry
Tramadol - toxicity
Mice
Method
Drug overdose
Activated charcoal
Tramadol
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Summary:Although tramadol is one of the most widely used centrally acting analgesics worldwide, no literature is available regarding adsorption of tramadol HCl powder or tablets (Ultram; 50 mg tramadol HCl per tablet) by activated charcoal (AC) for use as potential adjunct treatment of overdose. The present study incorporated a novel combination of in vitro and in vivo methods to investigate this question. Based on a binding curve of tramadol UV absorbance (UV a; 225 nm) plotted against the amount of AC, the ratio of amount of tramadol completely adsorbed by AC was 0.05 mg/mg. Also based on UV a, no tramadol was detected in filtrate of slurries in which up to 62 tablets of Ultram were mixed with 50 g AC; 4.6% of unbound tramadol was detected when 100 tablets of Ultram were mixed with AC. The ratio of amount of tramadol completely adsorbed by AC in this test was 0.10. In vivo, co-administration of 0.1 g/ml of AC produced a 13- to 14-fold rightward shift in tramadol's antinociceptive dose–response curve and a 1.6-fold rightward shift in tramadol's lethality dose–response curve.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
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ISSN:1056-8719
1873-488X
DOI:10.1016/S1056-8719(00)00091-5