Pharm, sedatives/hypnotics, Kinder Flashcards

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1
Q

What benzos are used as sedatives

A
alprazolam
clonazepam
diazepam
midazolam
triazolam
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2
Q

benzo antagonist

A

flumazenil

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3
Q

barbituate used for sedative hypnotic

A

phenobarbital

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4
Q

mis sedative hypnotic drugs

A
busiprone
eszopiclone
ramelteon
zaleplon
zolpidem
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5
Q

misc sedative hypnotic drugs

A
busiprone
eszopiclone
ramelteon
zaleplon
zolpidem
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6
Q

sedative vs hypnotic

A

sedative: reduce anxiety and exerts calming effect
hypnotic: drowsiness and facilitates onset and maintenance of state of sleep

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7
Q

MAO benzos

A

promote binding of GABA to R

enhances GAG induced ion currents (inc freq Cl opening)

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8
Q

effects benzo as sedative/hypnotic

A

sedation, hypnosis, muscle relaxation, anxiolytic and anticonvulsant effects

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9
Q

MOA barbituate

A

bind GABA a R and potentiate Cl Ch (inc duration Cl opening)

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10
Q

effects barbituates as sedative/hypnotic

A

mild sedation to anesthesia
anxiolytic
hypnotic and anticonvulsant effects

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11
Q

MOA eszopiclone and zaleplon and zolpidem

A

agonist effects at benzo side on GABAa R

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12
Q

MOA remelteon

A

activate melatonin R MT1 MT2

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13
Q

MOA remelteon

A

activate melatonin R MT1 MT2

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14
Q

Absorption distribution sedative hypnotics

A

lipid solubility determines rates and rates of onset

all cross CNS, placental barrier and breast milk

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15
Q

metabolism benzos

A

hepatic

CYP3A4

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16
Q

which benzos more likely to cause excessive drowsiness

A

benzos with long half life

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17
Q

relative CI to benzos

A

hepatic insufficiency

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18
Q

metabolism barbituates

A

hepatic metabolism and excreted in urine as glucuronide conjugates

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19
Q

new hypnotic metabolism

A

CYP3A4

short half life

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20
Q

what can increase elimnatino of phenobarbital in urine

A

alkalinization

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21
Q

better choice benzo if have hepatic insufficiency

A

lorazepam and oxazepam

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22
Q

3 types binding sites of Benzos

A

agonist- facilitate GABA
antagonist- block actions benzo
inverse agonists- negative allosteric modulators– produce anxiety and seizures

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23
Q

what are the benzo agonists

A

benzos, eszoplicone, zalplon and zolpidem

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24
Q

what are the benzo antagonists

A

flumazenil

25
Q

what are the inverse agonists to benzo R

A

beta carboline class

26
Q

which drug class exerts dose dependent anterograde amnesic effects

A

benzos

27
Q

which drug increases total sleep time

A

eszopiclone

28
Q

which drugs decrease time to fall asleep

A

newer sedative hypnotics at high doses

29
Q

which sedative hypnotics can cause anesthesia

A

thipental and methohexital

diazepam, lorazepam and midazolam

30
Q

which benzos are used for seizures

A

clonzepam nitrazepam lorazepam diazepam

phenobarbital too

31
Q

which benzos are used as muscle relaxants

A

diazepam

32
Q

Respiratory effects sedative hypnotics

A

significant dose dependent respiratory depression in patients with pulm disease
depress medullary respiratory center can cause death in overdose
most marked when given IV

33
Q

CV effects sedative hypnotics

A

depression in diseases that impair CV function like HF hypovolemia (depression medullary vasomotor center)
dec contractility and tone at toxic doses
most marked when given IV

34
Q

Cross tolerance

A

between sedative hypnotics of same class and with ethanol

35
Q

tolerance

A

decreased R

increased hepatic CYP

36
Q

class schedule of sedative hypnotics

A

III or IV
III: mod to low potential physical dependence, high for psychologic dependence
IV: limited potential for dependence

37
Q

class schedule of sedative hypnotics

A

III or IV
III: mod to low potential physical dependence, high for psychologic dependence
IV: limited potential for dependence

38
Q

physiologic dependence

A

inc anxiety, insomnia, CNS excitability may progress to convulsions

39
Q

Sx withdawal from psychologic dependence

A

cravings, irritability, insomnia, depression, anorexia

40
Q

Sx withdawal from psychologic dependence

A

cravings, irritability, insomnia, depression, anorexia

41
Q

MOA flumenazil

A

binds benzo site on GABAa and is competitive antagonist

blocks actions of benzos and zolpidem zaleplon and eszopiclone

42
Q

use of flumenazil

A

approved for reversing CNS depressant effect of benzos overdose and to shorten recovery following benzo anesthetic and diagnostics procedures

43
Q

adverse effects to flumenazil

A

agitaiton, confusion, dizziness, nausea

can precipitate abstinence syndrome in those with physiologic dependence

44
Q

adverse effects to flumenazil

A

agitaiton, confusion, dizziness, nausea

can precipitate abstinence syndrome in those with physiologic dependence

45
Q

benzo for panic disorders and agoraphobia

A

alprazolam

lorazepam and clonazepam also useful in panic disorders

46
Q

benzos for anxiety

A

since SSRIs and SNRI now more effective

use concomitant with SSRI util SSRI becomes effective then wean off benzo

47
Q

advantage of using benzo for anxiety

A

high therapeutic index
have flumazenil for overdose
low risk interactions
minimal effects CV and ANS

48
Q

disadvantage benzo for anxiety

A

risk dependence
depress CNS
amnestic effects
additional CNS depression when combined with other drugs (ethanol)

49
Q

newer agents to treat sleep problems

A

zolpidem zaleplon and eszopiclone

rapid onset few effects next day

50
Q

what drug is for those who wake up early and cannot get enough sleep

A

eszopiclone

51
Q

failure of insomnia to remit after 7-10 days of Tx could indicate what

A

primary psychiatric or medical illness that needs to be evaluated

52
Q

patients with increased sensitivity to sedative hypnotics

A

CV disease
resp disease
hepatic impairment in older patients

53
Q

drugs most frequently used in planned overdose

A

sedative hypnotics

54
Q

barbituates CI in who

A

Hx of acute intermittent porphyria because enhance porphyrin synthesis

55
Q

DDI with ramelteon

A

AARI fluvoxamine because CYP1A2

56
Q

adverse effect ramelton

A

dizziness, somnolence, fatigue, endocrin changes: dec cortisol, dec testosterone and inc PRL

57
Q

ramelton used for

A

Tx insomnia with difficulty sleep onset

58
Q

buspirone used for

A

generalized anxiety disorder

59
Q

adverse effect buspirone

A

tachy, palpitations, nervousness, GI distress, paresthesias and dose dependent papillary constriction