anxiolytics - benzos Flashcards
which of the benzos have active metabolites that have a T1/2 up to 100hrs?
CD on Fire
- chlordiazepoxide
- diazepam
- flurazepam
name all the benzodiazepines (7): in order from shortest to longest T1/2:
- midazolam (1.9hr)
- triazolam (2.9hr)
- alprazolam (12hr)
- lorazepam (14hr)
- chlordiazepoxide
- diazepam
- flurazepam
MTAL CD on Fire!
which of the benzos are directly metabolized to inactive glucuronides?
lorazepam (maybe midazolam, triazolam, alprazolam)
which of the benzos have to get oxidized via the P450 microsomal system in the liver, then conjugated to become inactive?
CD on Fire
- chlordiazepoxide
- diazepam
- flurazepam
where do the benzos bind/work?
GABAa receptors (binds btwn a1-y2 subunits); GABAa agonists
which benzos are not use to tx short-term depression, but instead used as an anesthesia (has calming effects, and produces anterograde amnesia)?
midazolam
which benzos is used for anticonvulsant and muscle relaxant, in addition to typical benzo’s use: short-term depression, maintenance of bipolar, severe bipolar?
diazepam, lorazepam
which benzo is typically used for sedation, anticonvulsant, and to PREVENT W/D SEIZURES AND SYMPTOMS IN ALCOHOLICS?
lorazepam
what are the SE’s of benzos?
- daytime sedation and drowsiness
- anterograde amnesia
- synergistic depression of CNS with other drugs
- psychologic and physiologic dependence with chronic use
can u die from benzo OD? why/why not?
no, b/c have ceiling effect. only augments GABA but potentiating Cl- channel opening; does not directly open Cl- channels.
what toxin binds noncompetitively at GABAa Cl- channels and in doing so, produces convulsions?
picrotoxin, GABAa antagonist
drug that is a non-benzo receptor agonist?
zolpidem
BDZ-1 selective agonist
zolpidem
benzodiazepine antagonist and specifically, competitive non-selective antagonist
flumazenil
drug used to produce sedation (calming/anxiolytic) and hypnosis (sleepiness) without muscle relaxation or anticonvulsant activity?
zolpidem
drug used for benzo ODs?
flumazenil
SE: sleep walking/driving/eating, next morning impairment
zolpidem
SE: might have life-threatening w/d sx, and siezures in mixed ODs, nonuniform in reversal of respiratory depression
flumazenil
which disorders do you not use SSRI’s as first line tx (what do you use instead)?
acute anxiety/benzos
for what disorders do you use SSRIs and/or benzos?
GAD, panic disorder
what disorder do you use SSRIs?
OCDs
which drug relieves anxiety (is anxiolytic) without marked sedation?
buspirone
at what receptor does buspirone work on?
partial agonist at 5HT1a receptors;;;;no interaction with GABAa receptor complex
what are the two barbiturates?
- thiopental
2. phenobarbitol
