sedative hypontic drugs Flashcards Preview

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Flashcards in sedative hypontic drugs Deck (38)
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1

barbituate vs benzos dose response relationship curves

barb: linear

benzo: non-linear (safer)

2

benzodiazepines MOA

bind GABA(a) - between alpha and gamma subunit (BZ1 and BZ2)

GABA(a) is a chloride channel - activated by inhibitory GABA

increase in FREQUENCY of chloride influx

allosteric enhancement of GABA effect

3

benzo receptor agonist, antagonist, inverse agonist

agonist: **positive allosteric modulators

antagonist: flumazenil (blocks benzo action)

inverse agonist: negative allosteric modulators of GABA (oppose GABA - cause anxiety and seizures) - only experimental drugs

4

benzo actions

reduce anxiety
sedative and hypnotic actions
anticonvulsant
muscle relaxant
anesthesia

5

benzo PK

lipophilic
various duration of actions
short, intermediate, long acting

6

diazepam: short, intermed, long acting?

long 1 -3 days

7

flurazepam: short, intermed, long acting?

long 1 - 3 days

8

alprazolam: short, intermed, long acting?

intermediate: 10-20 hours

9

lorazepam: short, intermed, long acting?

intermediate: 10-20 hours

10

temazepam: short, intermed, long acting?

intermediate: 10-20 horus

11

oxazepam: short, intermed, long acting?

short 3-8 hours

12

triazolam: short, intermed, long acting?

short 3-8 hours

13

all benzo's undergo phase 1 by CYP3A4 except which 3 drugs

oxazepam
lorazepam
temazepam

good to use in pt with poor liver function or those with poor P450 function

14

desmethyldiazepam

t 1/2 of >40 hours = active metabolite of several benzo's

metabolized into oxazepam

15

flurazepam

oxidized by liver enzymes to active metabolites with long half lifes (30-100 hours)

16

diazepam use

muscular disorder

17

benzo use for seizures

clonazepam

lorazepam and diazepam: status epilepticus

18

tx drug withdrawal

diazepam
oxazepam

for etoh withdrawal

19

benzo use for sleep disorders

flurazepam - long acting
temazepam - intermediate
triazolam - short

20

benzo AE

drowsiness/confusion
ataxia
cognitive impariment

pysch effects = irritable, hostile, paranoia

dependence - withdrawal = confusion, agitation, insomnia

21

flumazenil

only benzo receptor antagonist

reverses CNS depressant effects of benzo OD

22

flumazenil PK

rapid onset, short duration (half life 1 hour)

for OD tx = keep giving flumazenil to maintain reversal

may precipitate withdrawal

23

barbituates

less used b/c AE - tolerance, P450 inducers, coma

24

barbituate MOA

(not as selective as benzo's)

GABA(a) receptors - enhance transmission

increase DURATION of opening of chloride channels

also block glutamate receptors and sodium channels

25

barbituate dose vs action

low - sedation

high - hypnosis

-- anesthesia, coma, death

26

barbituate action

resp depression: suppress hypoxic and chemoreceptor response to CO2

induces P540

anesthesia: thiopental

anticonvulsant: phenobarbital

27

barbituate AE

drowsiness
paradoxical excitement
hypersensitivity
resp depression

*may worsen pain
*severe withdrawal

28

zolpidem

non-benzo benzodiazepine receptor agonist

short duration - 1.5 - 3.5 hr half life

use: short term tx of insomnia

29

zaleplon

non-benzo benzodiazepine receptor agonist

half life - 1 hour

use: short term insomnia tx

30

eszopliclone

non-benzo benzodiazepine receptor agonist

s-enantiomer of zopiclone

tx: insomnia - decreases sleep latency AND improves sleep maintenance

half life - 6 hours (longer half life of z drugs)