Pharm - sedative/hypnotics

Question 1

benzodiazepam moa

Answer 1

allosteric agonist at the BNZ binding site, potentiating the effects of GABA

Question 2

flumazenil moa

Answer 2

competitive antagonist, blocking the effects of benzodiazepines

Question 3

benzos converted to nordiazepam

Answer 3

clorazepate, diazepam, chlordiazepoxide, prazepam, halazepam

Question 4

benzos that are rapidly conjugated and eliminated in the urine

Answer 4

lorazepam, alprazolam, and oxazepam

Question 5

benzos with rapid onset

Answer 5

diazepam, triazolam, flurazepam, chlorazepate

Question 6

diazepam pharmacokinetics

Answer 6

rapid onset, long half life

Question 7

lorazepam pharmacokinetics

Answer 7

intermediate onset, long half like

Question 8

benzo pregnancy category

Answer 8

D

Question 9

abrupt discontinuation of BNZ treatment

Answer 9

withdrawal symptoms - tremor, sweating, insomnia, abdominal discomfort, tachycardia, systolic HTN, muscle twitching, photo/audio sensitivity; rebound anxiety and insomnia

Question 10

best benzos for anxiety

Answer 10

alprazolam, lorazepam, and clonazepam

Question 11

best benzo for panic attacks

Answer 11

alprozolam - possess antidepressant activity like TCAs

Question 12

best benzos for muscle relaxation

Answer 12

only diazepam inhibits monosynaptic reflexes in the spinal cord

Question 13

best benzo for alcohol withdrawal

Answer 13

chlordiazepoxide and diazepam; lorazepam if hepatic impairment (no cup metab)

Question 14

order of benzo tolerance development

Answer 14

1st: sedative and hypnotic effects
2nd: anticonvulsant effects
rarely if ever to anxiolytic effects

Question 15

mechanism of benzo tolerance

Answer 15

receptor uncoupling, down regulation, up-regulation of the fast-acting and opposing stimulatory glutamate, cross talk from other G-protein receptor systems (DA, ACh, 5-HT)

Question 16

benzo side effects

Answer 16

nausea, xerostomia, confusion, headache, or indifference; avoid use with alcohol or other CNS depressants

Question 17

buspirone moa

Answer 17

suppresses serotonergic while enhancing noradrenergic and dopaminergic activities
as effective as BNZs as anxiolytic, but with slow onset

Question 18

propranolol use

Answer 18

useful for performance anxiety or stage fright; suppresses somatic and autonomic symptoms of anxiety but does not alter emotional symptoms