Sedative-hypnotics

Question 1

name the two non-BNZ anxiolytics

Answer 1

buspirone

propranolol

Question 2

MOA of benzodiazepines?

Answer 2

allosteric agonist at the GABA receptor that potentiates the effects of GABA (increases likelihood of GABA channel opening)

Question 3

MOA of flumazenil

Answer 3

competitive antagonist at the GABA receptor that blocks the effects of BNZs

Question 4

which 3 BNZs have a shorter duration of action, simpler metabolism via conjugation and are eliminated in the urine?

Answer 4

lorazepam
alprazolam
oxazepam (not on drug list)

(Lazy Ass Ox)

Question 5

all of the BNZs undergo hepatic metabolism except which two drug?

Answer 5

lorazepam & oxazepam (not on drug list)

Question 6

all of the BNZs are what pregnancy category?

Answer 6

Category D

Question 7

which oral BNZ has a rapid onset of action with a long half life?

Answer 7

dizepam (also administered by injection)

Question 8

which BNZ has an intermediate onset of action and an intermediate half-life ( and is also administered by injection)

Answer 8

lorazepam

Question 9

which BNZ has a more severe reaction regarding withdrawal and dependence?

Answer 9

alprazolam (needs to be tapered)

-has shorter half life, but technically considered intermediate half life and onset of action)

Question 10

what are the symptoms of BNZ withdrawal?

Answer 10

tremor, sweating, REBOUND INSOMNIA, abd. discomfort, tachycardia, systolic HTN, muscle twitching, photo/audio sensitivity

• also rebound anxiety & insomnia
• convulsions possible after protracted high doses

Question 11

the symptoms of BNZ withdrawal primarily involve what?

Answer 11

autonomic stimulation

Question 12

which 3 BNZs are used for anxiety for intermittent or limited treatment?

Answer 12

alprazolam
lorazepam
clonazepam

Question 13

which BNZ is used to treat panic attacks?

Answer 13

responds favorably to alprazolam (possesses antidepressant activity like TCAs)

Question 14

what is the only BNZ that causes muscle relaxation?

Answer 14

diazepam (the drug inhibits monosynaptic reflexes in the spinal cord)
-other BNZs only do this at supra-clinical doses

Question 15

which two BNZs would you use for alcohol withdrawal, and what about if the pt has hepatic impairment?

Answer 15

chlordiazepoxide & diazepam

Lorazepam if hepatic impairment (undergoes renal metabolism as well as hepatic)

Question 16

what are the 1st set of effects that develop tolerance with BNZ therapy?

Answer 16

1st to sedative and hypnotic effects

2nd to anticonvulsant effects

Question 17

which effect of BNZs rarely develops tolerance?

Answer 17

anxiolytic effects

Question 18

nonselective BNZs allosterically enhance the inhib. actions of GABA by binding b/w the what subunits?

Answer 18

alpha-1, alpha-2, alpha-3, or alpha-5 and gamma subunits

Question 19

what are the proposed mechanisms for the development of tolerance with BNZ?

Answer 19

receptor uncoupling
receptor subunit down regulation
sensitization of glutamatergic system
cross talk from other G-protein receptor systems

Question 20

what do you have to remind the pt of when taking BNZs?

Answer 20

tell pt to accomodate their activities until the full effects of the sedative action are appreciated

Question 21

excess sedation with BNZs is sometimes associated with what?

Answer 21

respiratory depression

Question 22

what is the name of the BNZ antagonist that will rapidly restore respiratory function?

Answer 22

flumazenil

Question 23

what kind of pts can’t tolerate the resp. depression with BNZs?

Answer 23

older pts with COPD

Question 24

MOA for buspirone

Answer 24

suppresses serotonergic while enhancing noradrenergic and dopaminergic activities
(as effective as BNZs as an anxiolytic, but slow onset-wks)

Question 25

what is the name of the beta blocker that is useful for performance anxiety or stage fright?

Answer 25

propanolol (suppresses somatic & autonomic symptoms of anxiety but doesn’t alter emotional symptoms)

Question 26

which benzo do you give to a pt in an acute psychotic episode?

Answer 26

lorazepam (it has favorable pharmacokinetics)