Biomaterial Database

Pharmacokinetic considerations in abuse liability evaluation. 1991

M Farré, and J Camí

Institut Municipal d'Investigació Mèdica, Barcelona, Spain.

The behavioral effects of a drug are related to three factors: its intrinsic pharmacological activity, its physicochemical properties, and its pharmacokinetic parameters. In many cases differences in absorption, distribution, metabolism, and elimination may explain the different abuse liability profiles of drugs from within the same pharmacological class. Rapid absorption rate and high lipid solubility are the most important factors contributing to early drug concentrations in the brain. Differences in drug metabolism may be related to dose-dependent kinetics, first-pass metabolism, and variations in genetic traits (e.g. poor or extensive metabolizers). Metabolic pathways may produce active metabolites with similar or greater pharmacological activity than the parent substance. Drugs with a rapid elimination rate have been associated with greater self-administration and with early emergence of withdrawal symptoms. More pharmacokinetic studies are needed in human drug abuse liability evaluations. Knowledge of the plasma concentrations of drugs and their pharmacokinetic parameters can be essential to interpret differences among similar drugs in human abuse liability assessments.

UI	MeSH Term	Description	Entries
D011619	Psychotropic Drugs	A loosely defined grouping of drugs that have effects on psychological function. Here the psychotropic agents include the antidepressive agents, hallucinogens, and tranquilizing agents (including the antipsychotics and anti-anxiety agents).	Psychoactive Agent,Psychoactive Agents,Psychoactive Drug,Psychopharmaceutical,Psychopharmaceuticals,Psychotropic Drug,Psychoactive Drugs,Agent, Psychoactive,Agents, Psychoactive,Drug, Psychoactive,Drug, Psychotropic,Drugs, Psychoactive,Drugs, Psychotropic
D004341	Drug Evaluation	Any process by which toxicity, metabolism, absorption, elimination, preferred route of administration, safe dosage range, etc., for a drug or group of drugs is determined through clinical assessment in humans or veterinary animals.	Evaluation Studies, Drug,Drug Evaluation Studies,Drug Evaluation Study,Drug Evaluations,Evaluation Study, Drug,Evaluation, Drug,Evaluations, Drug,Studies, Drug Evaluation,Study, Drug Evaluation
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D012307	Risk Factors	An aspect of personal behavior or lifestyle, environmental exposure, inborn or inherited characteristic, which, based on epidemiological evidence, is known to be associated with a health-related condition considered important to prevent.	Health Correlates,Risk Factor Scores,Risk Scores,Social Risk Factors,Population at Risk,Populations at Risk,Correlates, Health,Factor, Risk,Factor, Social Risk,Factors, Social Risk,Risk Factor,Risk Factor Score,Risk Factor, Social,Risk Factors, Social,Risk Score,Score, Risk,Score, Risk Factor,Social Risk Factor
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