Sedative-hypnotics Flashcards
name the two non-BNZ anxiolytics
buspirone
propranolol
MOA of benzodiazepines?
allosteric agonist at the GABA receptor that potentiates the effects of GABA (increases likelihood of GABA channel opening)
MOA of flumazenil
competitive antagonist at the GABA receptor that blocks the effects of BNZs
which 3 BNZs have a shorter duration of action, simpler metabolism via conjugation and are eliminated in the urine?
lorazepam
alprazolam
oxazepam (not on drug list)
(Lazy Ass Ox)
all of the BNZs undergo hepatic metabolism except which two drug?
lorazepam & oxazepam (not on drug list)
all of the BNZs are what pregnancy category?
Category D
which oral BNZ has a rapid onset of action with a long half life?
dizepam (also administered by injection)
which BNZ has an intermediate onset of action and an intermediate half-life ( and is also administered by injection)
lorazepam
which BNZ has a more severe reaction regarding withdrawal and dependence?
alprazolam (needs to be tapered)
-has shorter half life, but technically considered intermediate half life and onset of action)
what are the symptoms of BNZ withdrawal?
tremor, sweating, REBOUND INSOMNIA, abd. discomfort, tachycardia, systolic HTN, muscle twitching, photo/audio sensitivity
- also rebound anxiety & insomnia
- convulsions possible after protracted high doses
the symptoms of BNZ withdrawal primarily involve what?
autonomic stimulation
which 3 BNZs are used for anxiety for intermittent or limited treatment?
alprazolam
lorazepam
clonazepam
which BNZ is used to treat panic attacks?
responds favorably to alprazolam (possesses antidepressant activity like TCAs)
what is the only BNZ that causes muscle relaxation?
diazepam (the drug inhibits monosynaptic reflexes in the spinal cord)
-other BNZs only do this at supra-clinical doses
which two BNZs would you use for alcohol withdrawal, and what about if the pt has hepatic impairment?
chlordiazepoxide & diazepam
Lorazepam if hepatic impairment (undergoes renal metabolism as well as hepatic)
what are the 1st set of effects that develop tolerance with BNZ therapy?
1st to sedative and hypnotic effects
2nd to anticonvulsant effects
which effect of BNZs rarely develops tolerance?
anxiolytic effects
nonselective BNZs allosterically enhance the inhib. actions of GABA by binding b/w the what subunits?
alpha-1, alpha-2, alpha-3, or alpha-5 and gamma subunits
what are the proposed mechanisms for the development of tolerance with BNZ?
receptor uncoupling
receptor subunit down regulation
sensitization of glutamatergic system
cross talk from other G-protein receptor systems
what do you have to remind the pt of when taking BNZs?
tell pt to accomodate their activities until the full effects of the sedative action are appreciated
excess sedation with BNZs is sometimes associated with what?
respiratory depression
what is the name of the BNZ antagonist that will rapidly restore respiratory function?
flumazenil
what kind of pts can’t tolerate the resp. depression with BNZs?
older pts with COPD
MOA for buspirone
suppresses serotonergic while enhancing noradrenergic and dopaminergic activities
(as effective as BNZs as an anxiolytic, but slow onset-wks)
