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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
anti anxiety that does not induce P450
benzo
26
advantages of benzos
safety, no induction of P450, mild withdrawal
27
MOA of benzo
binds GABAA receptor, increases CL- channel increasing frenquency of openings and release of GABA throughout CNS
28
GABA receptor that benzos bind to
alpha 1,2,3,and 5
29
GABA receptor mediating sedative properties of benzo
a 1, possibly 3
30
GABA receptor mediating anxiolytic properties of benzo
a2, possibly 3
31
GABA receptor mediating anticonvulsant properties of benzo
a3, possibly 1
32
GABA receptor mediating muscle relaxant properties of benzo
a2
33
benzo antagonist
flumazenil
34
clinical uses of benzos
treatment of anxiety | sleep disorders
35
benzos most effective in pts showing
``` high levels of emotional and somatic sx low levels of depression convulsive disorders neuromusclular disorders preop meds treatment of withdrawal from CNS depressents ```
36
time course of improvement from benzos
1-2 weeks
37
sedative that has no peripheral effects
benzo
38
only benzo used IM
lorazepam
39
benzos with no active metabolite
lorazepam, temazepam, triazolam
40
elimanation time for benzos
very long
41
sx of benzo withdrawal (low dose)
anxiety, rachycardia, palps, anorexia, blurred vision, muscle cramps
42
how to safely withdraw from benzos
tapering dose, w/wo switching to long active benzo or phenobarital propanolol (not for more than 2 weeks)
43
sx of high dose benzo withdrawal
anxiety, seizures, psychosis, hyperpyrexia, death
44
prototype benzo
diazepam, alprazolam, lorazepam, chloridiazepoxide,
45
longest actiing benzo
diazepam, flurazepam
46
benzo with no active metabolites
lorazepam
47
danger of flumazenil
may precipate benzo withdrawal
48
contraindications for flumazenil
hx of seizures | barbo or TCA OD
49
advantages of Benzos for sleep
``` safety produce marked sedation does not disrupt REM sleep does not induce p450 milder withdrawal syndrome ```
50
prototype benzos used for sleep
flurazepam, larazepam, , temazepam, triazolam
51
long acting benzo that are used for sleep that only the metabolites are active
flurazepam
52
IM benzo with no active metabolites
lorazepam
53
benzo used for sleep with high abuse potential, no active metabolites short half life
triazolam
54
halcion generic
triazolam
55
sleep aid drug that can cause bizzare behavior, agitation, hallucination
triazolam (halcion)
56
buspirone MOA
NOT an GABA drug, may act on serotonin
57
clinical use of buspirone
anti-anxiety
58
anti-anxiety drug with NO sedative, anticonvulsant or muscle relaxant effects
buspirone
59
anti-anxiety drug with good use in elderly pts
buspirone
60
anti-anxiety with good first pass effect
buspirone
61
anti-anxiety with no cross-tolerance
buspirone
62
anti-anxiety drug that displaces digoxin
buspirone
63
GABAA a1 agonists
zolpidem, zaleplon, eszopiclone
64
GABAA a1uses
decrease sleep latency, decrease total REM sleep and increase Stage 2
65
GABAA a1 effects
less anti (anxiety/convulsant/relaxant) effects than benzos
66
ambien
zolpidem
67
class of sleep drugs that are metabolized by liver
GABAa a1 agonists
68
metabolized by oxidation of methyl group
zolipidem
69
metabolized by CYP3A4
zaleplon
70
metabolized by CYP3A4 and CYP2E1
eszopiclone
71
sleep aids not to be used in sleep apnea
GABAA a1
72
glass of sleep aids that can cause residual daytime sedation
zolpidem, eszopiclone
73
sleep aid that can cuais dizzyness and GI problems
zolpidem
74
sleep aid that can cause birth defects and potential pre/post natal survival
zaleplon
75
sleep aid with SE including bad tase, headaches, dizziness and dry mouth
eszopiclone
76
GABAA a1 drug with rebound insomnia
eszopicline
77
GABAA a1 + SSRI =
halluciations
78
inhibitors of CYP3A4 and CYP2E1 can increase serum concentrations of...
eszopiclone
79
drug class used for situational anxiety
beta blockers
80
antihistamine used for sedative
hydroxyzine
81
rationale for hydroxyzine use
pts with hx of abusing standard sedatives
82
never ever ever give most sedatives to these pts
folks with sleep apnea
83
why don't you give sedatives to pts with sleep apnea
may increase hypoxia and hypercarbia

CNS I (36 decks)

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