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Psych > sedative hypnotics pharm > Flashcards

sedative hypnotics pharm Flashcards

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1
Q

benzodiazepines

A 
alprazolam
clonazepam
diazepam
midazolam
triazolam
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2
Q

benzodiazepine antagonists

A

flumazenil

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3
Q

barbituates

A

phenobarbital

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4
Q

absorption of sedative-hypnotics

A

lipid solubility major determining factor for rate of CNS effects
all cross BBB, placenta, and breast milk

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5
Q

benzos meta

A

liver
cumulative toxicity (especially those w/long half lives)
if pt has hepatic insufficiency should use oxazempam or lorazepam

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6
Q

barbituates meta

A

hepatic
phenobarbital exception that 20-30% excreted unchanged (alkaline urine will increase excretion rate)
can have cumulative toxicity

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7
Q

benzo MOA

A

increase efficiency of GABA
DO NOT substitute for GABA itself, potentiates
increased frequency of ClCh opening

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8
Q

barbituates MOA

A

increase duration of GABA ClCh opening

at high concentations can open Chs w/o GABA

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9
Q

drugs which faciliate GABA actions

A

benzos
eszopiclone
zaleplon
zolpidem

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10
Q

GABA antagonists

A

flumazenil

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11
Q

inverse GABA agonists

A

beta-carbolines

produce anxiety and seizures

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12
Q

sedation

A

suppress CNS
reduce anxiety
benzos also exert dose-dependent anterograde amnesia

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13
Q

anticonvulsant efects

A

benzos and barbituates

zolpidem, zaleplon, and eszopiclone lack anticonvulsant activity

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14
Q

mm relaxation

A

benzos, carbamates

zolpidem, zaleplon, and eszopiclone do not cause mm relaxation

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15
Q

flumazenil MOA

A

binds benzo binding site of GABAR acting as competitive antagonists

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16
Q

flumazenil uses

A

approved for reversing CNS depression from benzo overdose or to shorten recovery from anesthesia

17
Q

flumazenil ADRs

A

agitation, confusion, dizziness, nausea

18
Q

Tx of acute anxiety attacks/panic attacks

A

benzos (no single one has been determined as best)

19
Q

chronic anxiety disorders

A

SSRIs

can combine with benzo until SSRI reaches full effectiveness (4-6wks)

20
Q

benzos advantages for Tx anxiety

A

high therapeutic index
availability of flumazenil for overdose
low risk of DDIs
minimal effects on CV or ANS

21
Q

benzos disadvantages for Tx anxiety

A

risk of dependence
depression of CNS
amnestic effects
additional CNS depression when combined w/other drugs (alcohol)

22
Q

older insomnia drugs

A

barbituates and chloral hydrate

still used, not preferred

23
Q

benzos for insomnia

A

cause day time sedation
risk of tolerance
may have anterograde amnesia problems

24
Q

news insomnia srugs

A

zolpidem, zaleplon, and eszopiclone efficacies similar to older drugs
rapid onset and modest day after effects

25
Q

zolpidem

A

available in biphasic release formula that provides sustained drug levels for sleep maintenance

26
Q

zaleplon

A

acts rapidly, short half life

used to put people to sleep, not keep them there

27
Q

zaleplon, and eszopiclone

A

cause less amnesia or day after somnolence then zolpidem or benzos

28
Q

other uses of sedative-hypnotics

A

seizures
anesthesia
withdrawal from alcohil
Diazepam for mm spasm

29
Q

barbituates CIs

A

any type of porphyria

30
Q

ramelteon MOA

A

agonist at MT1&2

melantonin Rs located in suprachiasmic nuclei

31
Q

ramelteon uses

A

insomnia characterized by difficulty falling asleep

32
Q

ramelteon CIs

A

co administration w/fluvoxamine

33
Q

ramelteon ADRs

A

dizziness
somnolence
fatigue
endocrine chagnes

34
Q

busprinone MOA

A

unknown

maybe effects srotenergic or domipinergic neurons

35
Q

busprinone uses

A

general anxiety disorder

does not cause sedation, hypnotic, euphoric, anitconvulsant or mm relaxant effects

36
Q

busprinone ADRs

A 
tachy and palpitations
nervousness
GI
paresthesias
dose dependent papillary constriction
37
Q

zolpidem, zaleplon, and eszopiclone MOA

A

bind selectively to GABARs acting like benzos to enhance hyperpolarization

Psych (8 decks)

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