Sedative Hypnotics Flashcards
How do benzos work?
allosteric agonists of GABA-a receptor. Potentiates effects of GABA, does NOT mimic them.
What is the competitive antagonist of GABA-a receptors used to reverse the effects of benzos?
Flumazenil
Why do clorazepate, diazepam, chlordiazepoxide, prazepam, and halazepam have such long duration of clinical action?
They are all metabolized to nordiazepam, which has a long 1/2 life and is still active.
What are the benzos w/ a short duration of action?
Describe their elimination.
lorazepam, alprazolam, oxazepam
Eliminated in urine.
Benzos are Cat ___ for pregnant women?
D
Greater onset and severity of withdrawal symptoms from benzos are related to those with longer or shorter durations of action?
shorter duration of action = more severe withdrawal symptoms
Pt is having a panic attack. Give them this benzo:
Alprazolam
Pt is having muscle spasms, give them this benzo:
Diazepam
Which benzos used for EtOH withdrawal?
What about in the case of hepatic impairment?
chlordiazepoxide
diazepam
Lorazepam for hepatically impaired
Talk to me about the tolerance that develops to Benzos and their effects.
Describe how this tolerance occurs.
Tolerance first develops to sedative and hypnotic effects.
Then to anticonvulsant effects.
Rarely if ever to anxiolytic effects.
Great for tx of anxiety!
Receptor uncoupling, downregulation. Then upregulation of the fast-acting and opposing stimulatory neurotransmitter glutamate (cancels out effects of GABA).
Then maybe G-protein cross-talk.
Give benzos to old people w/ COPD?
Fuck no- respiratory depressive effects.
Also watch out for us w/ EtOH and other CNS depressants.
Non-benzo anxiolytics. What are they? What do they NOT do that benzos DO DO.
Buspirone- but no anticonvulsant/muscle relaxant/sedative effects seen w/ benzos
and Propranolol
How does Buspirone work?
Suppresses 5-HT while enhancing NE and DA
