Abuse potential of loperamide. 1980

J H Jaffe, and M Kanzler, and J Green

Effects of the currently marketed form of loperamide (Imodium capsules) that might relate to abuse potential were examined. Study I was a double-blind "dose run-up" in adult male subjects with a history of illicit drug use but no history of opioid addiction. Subjective responses to doses of loperamide ranging from 12 to 60 mg were compared with responses to 120 mg codeine sulfate (96 mg base) and to placebo. Based on study I, loperamide (60 mg) was used in study II and its effects were compared with those of codeine (96 mg base) and placebo in an exaddict subject group. Study II subjects had had extensive opioid experience but were not actively addicted at the time of this double-blind, inpatient study. In study II, as in study I, unlike loperamide and placebo, codeine induced pupillary constriction. Loperamide (60 mg) induced a detectable subjective effect in somewhat over half the subjects, was "liked" little or not at all, and was identified as "dope" at a frequency less than that for a threshold dose of oral codeine. It was concluded that in its present form, i.e., capsules containing loperamide mixed with magnesium stearate, loperamide poses little threat of potential abuse.

UI MeSH Term Description Entries
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
D009270 Naloxone A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors. MRZ 2593-Br,MRZ-2593,Nalone,Naloxon Curamed,Naloxon-Ratiopharm,Naloxone Abello,Naloxone Hydrobromide,Naloxone Hydrochloride,Naloxone Hydrochloride Dihydride,Naloxone Hydrochloride, (5 beta,9 alpha,13 alpha,14 alpha)-Isomer,Naloxone, (5 beta,9 alpha,13 alpha,14 alpha)-Isomer,Narcan,Narcanti,Abello, Naloxone,Curamed, Naloxon,Dihydride, Naloxone Hydrochloride,Hydrobromide, Naloxone,Hydrochloride Dihydride, Naloxone,Hydrochloride, Naloxone,MRZ 2593,MRZ 2593 Br,MRZ 2593Br,MRZ2593,Naloxon Ratiopharm
D010880 Piperidines A family of hexahydropyridines.
D011680 Pupil The aperture in the iris through which light passes. Pupils
D003061 Codeine An opioid analgesic related to MORPHINE but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough. Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-, (5alpha,6alpha)-,Ardinex,Codeine Phosphate,Isocodeine,N-Methylmorphine,N Methylmorphine
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D019966 Substance-Related Disorders Disorders related to substance use or abuse. Chemical Dependence,Drug Abuse,Drug Addiction,Drug Dependence,Drug Habituation,Drug Use Disorder,Drug Use Disorders,Organic Mental Disorders, Substance-Induced,Substance Abuse,Substance Dependence,Substance Related Disorder,Substance Use,Substance Use Disorder,Substance Use Disorders,Prescription Drug Abuse,Substance Addiction,Abuse, Drug,Abuse, Prescription Drug,Abuse, Substance,Addiction, Drug,Addiction, Substance,Chemical Dependences,Dependence, Chemical,Dependence, Drug,Dependence, Substance,Dependences, Chemical,Disorder, Drug Use,Disorder, Substance Related,Disorder, Substance Use,Disorders, Substance Related,Drug Abuse, Prescription,Habituation, Drug,Organic Mental Disorders, Substance Induced,Related Disorder, Substance,Related Disorders, Substance,Substance Abuses,Substance Uses,Use, Substance

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