Drugs of abuse I Flashcards
definition: pharmacokinetic tolerance
increased drug metabolism results in decrease in the amount of available drug or duration of drug action at the target site
definition: pharmacodynamic tolerance
CNS responds and adapts to presence of drug - desensitization, down regulation, and / or internalization of receptors
what are the molecular targets of abusive drugs?
GPCRs
inotropic channels
dopamine transporters
which brain area houses the dopaminergic neurons responsible for addiction / reward?
ventral tegmental area
opioids, THC, GHB act on what receptor? what NT is involved?
GPCRs
GABA
cocaine, amphetamine, MDMA act on what receptor?
DA transporters
benzodiazapines, nicotine, ethanol act on what receptor?
inotropic channels
what is the relative risk of addiction of CNS depressants and sedatives / hypnotics?
3 (scale 0-5)
ethanol follows what type of elimination kinetics?
zero order (independent of time and concentration)
which enzyme is involved in the rate limiting step of alcohol metabolism?
alcohol dehydrogenase
what is the function of disulfiram? what is its clinical use?
inhibits ALDH alcohol addiction treatment - triggers unpleasant symptoms of hangover to discourage further use
what is the MOA of ethanol? what is the result?
potentiates effects of GABA at GABAa receptors results in increased chloride ion flux and neuronal hyperpolarization
what is the molecular basis for ethanol induced blackouts?
upregulation of NMDA receptors
what contributes to withdrawal effects of ethanol?
excess NMDA receptors
what are the signs and symptoms of wernicke korsakoff syndrome?
ocular disturbances
changes in mental state
memory impairment
movement difficulties
