Benzodiazepines Flashcards
benzos: 5 main pharmacological effects
anxiolysis sedation anterograde amnesia anticonvulsant actions muscle relaxation (spinal level)
what do we use benzos for the most
anxiolysis
benzos and muscle relaxation
no muscle relaxation
do not affect muscle relaxant doses
benzos and hepatic metabolism
do not induce hepatic metabolism
less potential for tolerance/abuse than barbs, opioids
benzos and cerebrovascular response
preserves cerebrovascular response
greater margin of safety
benzos replaced what for premed/MAC cases
barbs
benzos structure
benzene ring with 7 member diazepine ring
benzos mechanism of action
facilitate action of GABAa
increase affinity of GABAa to receptor
do benzos mimic GABAa?
NO, does not directly activate GABAa receptor
what does increase of affinity of GABA mean?
open Cl channel
increase in Cl in cell
hyperpolarizes cel in post synapse
benzos are different in 3 ways
potency, lipid solubility, pharmacokinetics
in general, benzos are
highly lipid soluble, highly bound to albumin
if pt is drunk, do you give benzos?
no, the ETOH is already binding to the GABAa receptors
versed preparation, shape, potency, effect site equilibration time, hepatic effect, % protein bound, redistribution/duration time, elimination T1/2
water soluble imidazole ring 2-3x more potent than diazepam 0.9-5.6 min effect site equilibration, increases with age extensive first pass effect 90-98% protein bound rapid redistribution, short duration T1/2 = 1-6.5 hrs
versed metabolism
extensive first pass effect hydroxylation to water soluble compound 1,4 hydroxymidazolam 1 hydroxymidazolam is an active metabolite conjugated, excreted in urine renal failure does not affect midazolam