depressants Flashcards
major inhibitory NT in CNS
GABA
Barbiturates absorption
small intestine
Barbiturates distribution
highly lipid soluble
fast rate of entry into CNS
Barbiturates metabolism
slow
induce hepatic drug-metabolizing enzymes (Rx interactions)
Barbiturates MOA
bind GABA-A receptor
increases duration of channel opening
high conc: directly activate
hella high conc: decrease release of other NTs
Barbiturates effects
CNS depression low therapeutic index hypotension anticonvulsant activity not analgesic reduce REM sleep induce own metabolism
Barbiturates dependence
psychological
physical
status epilepticus
abrupt withdrawal is life-threatening
Methohexital
ultra-short acting BARB
anesthesia
short procedures
Secobarbital
Pentobarbital
short/intermediate acting BARB
sedation
insomnia
Phenobarbital
long acting BARB
epilepsy
Barbiturates SE
CNS depressant
OD: death
contraindicated in acute intermittent porphyria
Barbiturates Rx interactions
additive effects w/CNS depressants
cross-tolerance w/CNS depressants
induction of P450
Ethanol absoprtion
GI tract
Ethanol distribution
cross BBB
cross placenta
Ethanol metabolism
liver
unchanged in urine
sweat