pharmacology: sedative-hypnotic-anxiolytic drugs Flashcards Preview

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Flashcards in pharmacology: sedative-hypnotic-anxiolytic drugs Deck (22):
1

what are the sedative-hypnotic-anxiolytic drugs?

benzodiazepines, barbiturates, alcohols

2

what is the GABA binding site? benzo? barbiturate?

GABA: alpha
benzo: gamma
barbiturate: beta

3

what are the increasing CNS effects of benzos/barbiturate/alcohols?

paradoxical disinhibition --> sedation--> anxiolysis --> anticonvulsant and muscle relaxing --> hypnosis --> anesthesia --> medullary depression --> coma/death

4

how do benzo/barbiturates/alcohol cause paradoxical disinhibition (excitement, drunk)?

inhibiting an inhibitory neuron (causing excitation instead)

5

GABA A activation causes

increased Cl- influx

6

GABA B activation causes

increased K+ efflux

7

benzodiazepine mechanism

potentiate GGABA, increased frequency of CL opening with NO GABA mimetic activity!

8

what are the benzodiazepines?

alprazolam, diazepam, lorazepam, midazolam, temazepam, oxazepam

9

which benzodiazepines have a short half life? implication/clinical use?

temazepam and oxazepam - used in sleep disorders

10

which benzos have a long half life? implication/clinical use?

alprazolam, diazepam, lorazepam, midazolam
-used in anxiety

11

which benzo is used in panic/phobias?

alprazolam

12

which benzo is used in withdrawal states?

diazepam

13

which benzo is used in status epilepticus?

lorazepam

14

which benzo is used in anesthesia?

midazolam

15

what is used in benzodiazepine overdose? mechanism?

BZ receptor antagonist flumazenil

16

barbiturates mechanism

prolong GABA activity by increasing DURATION of Cl- channel opening and have GABA mimetic activity

17

what are the barbiturates? uses?

phenobarbital for seizures (long acting)
thiopental for induction of anesthesia (short acting)

18

what is the contraindication for barbiturates?

porphyrias - blocks enzyme used in heme synthesis D-ALA synthase (buildup of chemicals related to RBC proteins)

19

withdrawal signs for BZs vs withdrawal signs of barbiturates and alcohol

BZs: rebound insomnia, anxiety, seizures when used as antiepileptic or high doses
Barbiturates/ethanol: anxiety, agitation, life-threatening seizures (delirium tremens with alcohol)

20

drug interactions with GABA A drugs

1. additive with other CNS depressants such as anesthetics, antihistamines, opiates, beta blockers
2. barbiturates induce metabolism of most lipid-soluble drugs such as oral contraceptives, carbamazepine, phenytoin, warfarin

21

what are the non-BZ drugs?

1. zolpidem and zaleplon (BZ1 receptor agonist instead of BZ2) - used in sleep disorders
2. buspirone (no effect on GABA - 5-HT1A partial agonist - used in anxiety disorders)

22

what is used for generalized anxiety disorders?

buspirone!