Intro Drugs of Abuse (Kruse) Flashcards
__ is a drug that decreases CNS activity, moderates excitement, and calms the recipient. It is Anxiolytic and fast-acting compared to SSRIs
sedative
__ is a drug that produces drowsiness and facilitates the onset and maintenance of sleep and from which the recipient can be aroused easily. The effects involve more pronounced depression of CNS, which can be achieved with many drugs (not all) in this class by increasing the dose
hypnotic
__ bind to GABAa receptor and enhance GABAs effects (shifts dose response curve to left).
Benzodiazepines
Benzo’s effects on: Chloride ion influx? polarization? action potentials?
increase Cl influx
increase hyper polarization
decrease # APs
Metabolism of benzos? Excretion?
metabolism=Hepatic; CYP3A4 (phase1) and glucuronidation (phase2); Cumulative toxicity
Renal excretion
which benzos are intm to long acting?
(DLC)
Diazepam
Lorazepam
Clonazepam
The rest are short to intm acting
consequence of benzo’s with long 1/2 lives?
more likely to cause cumulative effects (excessive drowsiness, etc) with multiple doses
__ binds to the GABAa receptor, increases duration of GABA-gated channel openings
barbiturates
increase Cl influx, increase hyper polarization, decrease #APs (CNS depression)
phenobarbital, amobarbital, and secobarbital are examples of __
barbiturates
MOA of newer hypnotics (sleep aids), i.e., eszopiclone (lunesta), zolpidem (ambien), and zaleplon (sonata)?
bind to GABAa receptors that contain the a1-subunit
antagonist available for overdose of anti-anxiety meds?
flumazenil –> competitive antagonist
these drugs for tx of insomnia are highly effective, have rapid onset with minimal hangover effects
zolpidem, zaleplon, and eszopiclone
__-sleep aid with biphasic release formulation for sustained sleep maintenance
__-sleep aids that act rapidly
__-sleep aid that has longer 1/2 life
zolpidem
zaleplon and zolpidem
eszopiclone
this drug for insomnia is an agonist at MT1 and MT2 melatonin receptors
Ramelteon
why do you want to avoid coadministration of Ramelteon with Fluvoxamine?
Fluvoxamine is an SSRI and CYP1A2 inhibitor
Ramelteon parent drug metabolized by CYP1A2 to active metabolite
adverse effects of Ramelteon?
dizziness, somnolence, fatigue, endocrine changes –> decrease T and increase prolactin
__ is approved for tx of generalized anxiety disorder, its anxiolytic effects may take more than 1 week to become established, does NOT cause sedation, hypnotic, euphoric, anticonvulsant, or muscle relaxant effects
Buspirone
metabolism of Buspirone?
CYP3A4
kinetics of ethanol metabolism?
Zero order
Memory loss that occurs with high levels of alcohol (blackouts) most likely results from inhibition of __ receptor activation
NMDA
Alcohol inhibits ability of glutamate to open cation channel of NMDA receptor and leads to increased depression of CNS
Alcohols effect on GABA receptors?
enhances the effects of GABA on GABAa receptor and leads to increased depression of CNS (additive CNS depression)
major pharmacological objective in acute alcohol withdrawal syndrome?
prevent seizures, delirium, and arrhythmias, electrolyte rebalancing, thiamine therapy
can be life-threatening, can use Benzos
MOA and use for Naltrexone?
MOA: mu opioid receptor antagonist (long-acting)
Approved for tx of alcohol and opiate dependence
Reduces craving for etoh and rate of relapse to either drinking or eton dependence for short term (12 weeks)
MOA and use for Acamprosate?
MOA: weak NMDA-receptor antagonist and GABAa receptor agonist (also effects serotonergic, noradrenergic, and dopaminergic systems)
reduces short-term and long-term relapse rates (>6 mos)
