Biomaterial Database

Interaction of loperamide and diphenoxylate with ethanol and methohexital. 1978

J L Mcguire, and F Awouters, and C J Niemegeers

The antidiarrheal drugs loperamide and diphenoxylate were tested for their ability to potentiate central nervous system depression induced by ethanol in mice and nethohexital in rats. Oral diphenoxylate potentiated the loss of righting reflex (hypnosis) at 10 mg/kg in mice and at 5 mg/kg in rats, doses which were considerably lower than those required to induce morphine-like behavior in mice and rats. Oral loperamide did not potentiate hypnosis. Increased incidence and duration of hypnosis was observed with loperamide only at very high, nearly toxic doses (100 mg/kg in mice and 80 mg/kg in rats) and these doses induced only nonspecific central nervous system depression. The failure of loperamide to potentiate the action of hypnotics confirms data from clinical trials which showed that loperamide is essentially free of central depressant effects when given orally.

UI	MeSH Term	Description	Entries
D006993	Hypnotics and Sedatives	Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.	Hypnotic,Sedative,Sedative and Hypnotic,Sedatives,Hypnotic Effect,Hypnotic Effects,Hypnotics,Sedative Effect,Sedative Effects,Sedatives and Hypnotics,Effect, Hypnotic,Effect, Sedative,Effects, Hypnotic,Effects, Sedative,Hypnotic and Sedative
D007540	Isonipecotic Acids		Acids, Isonipecotic
D008139	Loperamide	One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.	Imodium,Loperamide Hydrochloride,Loperamide Monohydrochloride,R-18553,Hydrochloride, Loperamide,Monohydrochloride, Loperamide,R 18553,R18553
D008297	Male		Males
D008723	Methohexital	An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.	Methohexitone,Brevimytal Natrium,Brevital,Brietal,Brietal-Sodium,Methohexital Sodium,Methohexital, Monosodium Salt,Brietal Sodium,Monosodium Salt Methohexital,Natrium, Brevimytal,Sodium, Methohexital
D010880	Piperidines	A family of hexahydropyridines.
D012018	Reflex	An involuntary movement or exercise of function in a part, excited in response to a stimulus applied to the periphery and transmitted to the brain or spinal cord.
D004157	Diphenoxylate	A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.	Diphenoxylate Hydrochloride,Diphenoxylate Monohydrochloride,Hydrochloride, Diphenoxylate,Monohydrochloride, Diphenoxylate
D004347	Drug Interactions	The action of a drug that may affect the activity, metabolism, or toxicity of another drug.	Drug Interaction,Interaction, Drug,Interactions, Drug
D000431	Ethanol	A clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in ALCOHOLIC BEVERAGES.	Alcohol, Ethyl,Absolute Alcohol,Grain Alcohol,Alcohol, Absolute,Alcohol, Grain,Ethyl Alcohol