Alcohol, Anxiolytics, & Sedative Hypnotics Flashcards
Fomepizole MOA
inhibits alcohol DH
Disulfram MOA
inhibits aldehyde DH
product of alcohol DH?
acetaldehyde
product of aldehyde DH
acetate
alcohol MOA (4)
binds to GABAa receptor to increase Cl- influx
increases DA in mesolimbic pathway
inhibits the effect of glutamate on NMDA receptor
increases NMDA receptors
naltrexone contraindication
liver failure
naltrexone MOA
opioid antagonist- blocks alcohol’s ability to stimulate the reward pathway
acamprosate (camprel EC) MOA
structural analogue of GABA- restores balance of GABA and glutamate
antidote for MeOH poisoning
fomepizole- alcohol DH inhibitor
short-acting barbiturate used for anesthesia induction
thiopental (pentothal)
long-acting barbiturate, used as anticonvulsant
phenobarbital (Luminal)
barbiturate contraindications (3)
porphyria
pulmonary insufficiency
alcohol
short-acting benzo
midazolam
long-acting benzos (4)
diazepam
prazepam
clorazepate
fluzepam
short-acting benzos (3)
alprazolam
triazolam
lorazepam
benzo MOA (2)
bind to the GABAa receptor
increase affinity of the receptor to GABA, prolonging its action
benzo tx insomnia (2)
flurazepam
temazepam
helpful for people who can’t fall asleep
benzo tx status epilepticus (2)
diazepam
lorazepam
benzo sedation/anesthesia
midazolam
benzo for muscle spasm
diazepam
benzo for EtOH withdrawl (3)
taper w/
chlordiazepoxide
diazepam
lorazepam
benzo contraindications? (2)
pregnancy
sleep apnea
benzo antagonist & MOA
flumazenil
antagonist- competes for GABA receptor
reverses effects of benzos
flumazenil contraindication
hx seizures
“Z drugs” & MOA
Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta)
bind to the BZ1 subtype of the GABA receptor to increase GABA mediated inhibition
eszopiclone use?
long-half life, long-term tx
Ramelteon (Rozerem) MOA
melatonin analogue, promotes sleepiness w/ no GABA effect
GABA independent- no ceiling effect
Buspirone (BuSpar) MOA & use
partial agonist at post-synaptic serotonin receptor –> inhibition of cell signaling, decreased 5-HT release
relieves anxiety w/o sedation. takes 2 weeks to feel effects
low addiction potential