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CNS I > Sedatives I and II > Flashcards

Sedatives I and II Flashcards

1. List the principal criteria for the appropriate use of sedative-hypnotic/anxiolytic agents. 2. List the prototype barbiturates, benzodiazepines, and GABAA-alpha1 selective agonists, describe their clinical uses, their mechanism and site of action, and how their pharmacokinetic differences provide the basis for selection of which agent to use and for what purpose. 3. List the major side effects and abuse potential of the prototype barbiturates, benzodiazepines, and GABAA-alpha1 selective ago

1
Q

Standard reasons to treat anxiety w/drugs

A

1) anxiety
2) not for 8 hours of sleep
3) when it affects quality of life

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2
Q

MOA of Barbiturates

A

not really known, but seem to be GABAA agonist

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3
Q

Long acting barbo class

A

phenobarbital

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4
Q

phenobarbital t 1/2

A

80-120 hrs

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5
Q

pentobarb t 1/2

A

15-48 hrs

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6
Q

intermediate acting barbo

A

pentobarbital

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7
Q

short acting barbo

A

thiopental

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8
Q

clincal use for barbos

A

induction in general anesthesia and seziure disorders

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9
Q

old use for barbos

A

insomnia/anxiety

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10
Q

CNS activity of barbos

A

sedation to coma/death
state resembaling natural sleep
anticonvulsant

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11
Q

sx of barbo OD

A

comatose
bradypnea
marked hypotension
weak rapid pulse

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12
Q

TX for barbo OD

A 
ABC
rule out narcotics
gastric lavage
bicarb
hemodialysis
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13
Q

ways tolerence to barbos comes about

A

induction of P450

cross-tolerence to all CNS depressents

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14
Q

drug class with potentially life-threatening dependance

A

barbos

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15
Q

early stages of barbo withdrawal sx

A

weakness, trembling, insomnia, and abdominal cramps

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16
Q

reversal of early stage barbo withdrawal

A

CNS depressant

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17
Q

when can barbo withdrawal be reversed

A

early only

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18
Q

sx of late stage barbo withdrawal

A

orthostatic hypotension, delirium, convilsions leading to status elipepticus

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19
Q

lenght of barbo withdrawl

A

7-9 days

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20
Q

contraindications of barbos

A

pts with hx or fam hx of acute intermittent porphyria

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21
Q

DOC class for anxiety

A

benzos

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22
Q

DOC for rapid treatment of panic attacks

A

benzos

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23
Q

prototype benzo

A

diazempam

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24
Q

CNS activity of benzos

A 
sedative/hypnotic
anxiolytic
anticonvulsant
muscle relaxant
amnestic
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25
Q

anti anxiety that does not induce P450

A

benzo

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26
Q

advantages of benzos

A

safety, no induction of P450, mild withdrawal

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27
Q

MOA of benzo

A

binds GABAA receptor, increases CL- channel increasing frenquency of openings and release of GABA throughout CNS

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28
Q

GABA receptor that benzos bind to

A

alpha 1,2,3,and 5

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29
Q

GABA receptor mediating sedative properties of benzo

A

a 1, possibly 3

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30
Q

GABA receptor mediating anxiolytic properties of benzo

A

a2, possibly 3

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31
Q

GABA receptor mediating anticonvulsant properties of benzo

A

a3, possibly 1

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32
Q

GABA receptor mediating muscle relaxant properties of benzo

A

a2

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33
Q

benzo antagonist

A

flumazenil

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34
Q

clinical uses of benzos

A

treatment of anxiety

sleep disorders

35
Q

benzos most effective in pts showing

A 
high levels of emotional and somatic sx
low levels of depression
convulsive disorders
neuromusclular disorders
preop meds
treatment of withdrawal from CNS depressents
36
Q

time course of improvement from benzos

A

1-2 weeks

37
Q

sedative that has no peripheral effects

A

benzo

38
Q

only benzo used IM

A

lorazepam

39
Q

benzos with no active metabolite

A

lorazepam, temazepam, triazolam

40
Q

elimanation time for benzos

A

very long

41
Q

sx of benzo withdrawal (low dose)

A

anxiety, rachycardia, palps, anorexia, blurred vision, muscle cramps

42
Q

how to safely withdraw from benzos

A

tapering dose, w/wo switching to long active benzo or phenobarital
propanolol (not for more than 2 weeks)

43
Q

sx of high dose benzo withdrawal

A

anxiety, seizures, psychosis, hyperpyrexia, death

44
Q

prototype benzo

A

diazepam, alprazolam, lorazepam, chloridiazepoxide,

45
Q

longest actiing benzo

A

diazepam, flurazepam

46
Q

benzo with no active metabolites

A

lorazepam

47
Q

danger of flumazenil

A

may precipate benzo withdrawal

48
Q

contraindications for flumazenil

A

hx of seizures

barbo or TCA OD

49
Q

advantages of Benzos for sleep

A 
safety
produce marked sedation
does not disrupt REM sleep
does not induce p450
milder withdrawal syndrome
50
Q

prototype benzos used for sleep

A

flurazepam, larazepam, , temazepam, triazolam

51
Q

long acting benzo that are used for sleep that only the metabolites are active

A

flurazepam

52
Q

IM benzo with no active metabolites

A

lorazepam

53
Q

benzo used for sleep with high abuse potential, no active metabolites short half life

A

triazolam

54
Q

halcion generic

A

triazolam

55
Q

sleep aid drug that can cause bizzare behavior, agitation, hallucination

A

triazolam (halcion)

56
Q

buspirone MOA

A

NOT an GABA drug, may act on serotonin

57
Q

clinical use of buspirone

A

anti-anxiety

58
Q

anti-anxiety drug with NO sedative, anticonvulsant or muscle relaxant effects

A

buspirone

59
Q

anti-anxiety drug with good use in elderly pts

A

buspirone

60
Q

anti-anxiety with good first pass effect

A

buspirone

61
Q

anti-anxiety with no cross-tolerance

A

buspirone

62
Q

anti-anxiety drug that displaces digoxin

A

buspirone

63
Q

GABAA a1 agonists

A

zolpidem, zaleplon, eszopiclone

64
Q

GABAA a1uses

A

decrease sleep latency, decrease total REM sleep and increase Stage 2

65
Q

GABAA a1 effects

A

less anti (anxiety/convulsant/relaxant) effects than benzos

66
Q

ambien

A

zolpidem

67
Q

class of sleep drugs that are metabolized by liver

A

GABAa a1 agonists

68
Q

metabolized by oxidation of methyl group

A

zolipidem

69
Q

metabolized by CYP3A4

A

zaleplon

70
Q

metabolized by CYP3A4 and CYP2E1

A

eszopiclone

71
Q

sleep aids not to be used in sleep apnea

A

GABAA a1

72
Q

glass of sleep aids that can cause residual daytime sedation

A

zolpidem, eszopiclone

73
Q

sleep aid that can cuais dizzyness and GI problems

A

zolpidem

74
Q

sleep aid that can cause birth defects and potential pre/post natal survival

A

zaleplon

75
Q

sleep aid with SE including bad tase, headaches, dizziness and dry mouth

A

eszopiclone

76
Q

GABAA a1 drug with rebound insomnia

A

eszopicline

77
Q

GABAA a1 + SSRI =

A

halluciations

78
Q

inhibitors of CYP3A4 and CYP2E1 can increase serum concentrations of…

A

eszopiclone

79
Q

drug class used for situational anxiety

A

beta blockers

80
Q

antihistamine used for sedative

A

hydroxyzine

81
Q

rationale for hydroxyzine use

A

pts with hx of abusing standard sedatives

82
Q

never ever ever give most sedatives to these pts

A

folks with sleep apnea

83
Q

why don’t you give sedatives to pts with sleep apnea

A

may increase hypoxia and hypercarbia

CNS I (36 decks)

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