module 3 sedatives and hypnotics Flashcards
sedative
drug that produces a relaxing, calming effect
hypnotic
drug used to produce drowsiness and facilitate onset of sleep
GABA
inhibitory neurotransmitter in CNS
- binds to GABA receptors and opens Cl channel
- Cl enters the cell -> negative change in transmembrane potential -> hyperpolarization -> shutting down AP
sedative-hypnotic classes
benzodiazepines
barbituates
misc.
benzodiazepines MOA
GABA receptor modulator
- inc. activity of GABA (gabaergic effect)
- have no effect if GABA is not also present
benzodiazepine uses
anxiety panic disorders alcohol withdrawal CINV seizure prevention/termination status epiepticus hypnotic
benzodiazepine AE
CNS depression
- less likely when used alone
tolerance
dependence
benzodiazepine administration
most are active drugs -> active metabolites
exceptions:
- lorazepam
- oxazepam
- temazepam
benzodiazepine interactions
CNS depressants
-> fatal CNS depression
benzodiazepine antidote
flumazenil
flumazenil MOA
GABA Rc antagonist
- no effect on barbiturates or alcohol
- can precipitate withdrawal
barbiturates MOA
binds to GABA Rc at allosteric site
- inc. GABA activity
higher dose -> direct agonizing of Rc -> inc. CNS depression
barbiturates use
anesthesia
emergency seizure tx
status epilepticus
insomnia
barbiturates AE
tolerance
dependence
fatal CNS depression
barbiturates withdrawal s/s
tremor anxiety insomnia CNS excitability seizure cardiac arrest
barbiturates interactions
CYP450
- 3A4 inducer
NBRA MOA
bind to same site on GABA Rc as benzos but chemically different
NBRA uses
hypnotic
sleep aid
NBRA AE
tolerance dependence memory impairment/amnesia impaired judgement/reasoning sleep walking
NBRA administration
shorter half life than benzos
eszopiclone: for chronic use
NBRA antidote
flumazenil
NBRA education
less time to fall asleep
less REM sleep
remelteon MOA
full agonist at melatonin Rc
remelteon use
sleep
- maintain circadian rhythm of sleep/wake cycle
remelteon education
no tolerance or dependence
not a controlled substance
suvorexant MOA
orexin Rc antagonist
- suppresses the wake drive
suvorexant AE
narcolepsy
cataplexy
