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Psychopharmacology > Lecture 19: Sedative-Hypnotics > Flashcards

Lecture 19: Sedative-Hypnotics Flashcards

1
Q

first two sleep-inducing agents

A

bromide and chloral hydrate

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2
Q

what drug was introduced in 1912?

A

phenobarbitol

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3
Q

2 drugs introduced in 1950s

A

meprobamate (equanil) and carisoprodol (soma)

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4
Q

first benzo

A

librium

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5
Q

3 benzos

A

valium, xanax, ativan

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6
Q

where do most act?

A

GABAa

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7
Q

3 nonbenzo BZRAs

A

zolpidem (ambien)
zaleplon (sonata)
eszopiclone (lunesta)

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8
Q

4 general anesthetics

A

nitrous oxide
halothane
isoflurane
ketamine

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9
Q

5HT1-A agonist

A

buspirone

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10
Q

BZRA

A

benzodiazepine receptor agonist

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11
Q

3 brain regions associated with anxiety response

A
  1. amygdala
  2. OF cortex
  3. insula
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12
Q

how many beta subunits?

A

3

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13
Q

how many alpha subunits?

A

6

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14
Q

how many gamma subunits?

A

3

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15
Q

bicuculline

A

deadly convulsant; competitive antagonist at GABA site

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16
Q

newer drugs are named by ___

A

receptors they bind to or that underlie major clinical actions

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17
Q

BZRAs include both ___

A

BZs and nonBZs

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18
Q

BZs act on GABA neurons in ___

A

limbic system

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19
Q

what happens when GABAergic function is blocked?

A

anxiety, seizures

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20
Q

what does hypofunctional GABAa receptor activity do?

A

sensitizes amygdala to anxiogenic responses

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21
Q

what is the general action of BZs on brain?

A

may reset threshold of amygdala to more normal level of responsiveness

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22
Q

what is an alcohol-induced blakout?

A

drug-induced, reversible, organic brain syndrome (state of bementia)

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23
Q

how many barbs between 1912 and 1950?

A

50 different

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24
Q

half life of barbs

A

3 min - 48 hours

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25
Q

ultrashort acting barb

A

thiopental

26
Q

why is thiopental so short?

A

extremely lipid soluble, crossing BBB rapidly

27
Q

longer acting barb; why?

A

amobarbital; more water soluble, slower to penetrate CNS

28
Q

are barbs analgesic?

A

no

29
Q

what do barbs due to REM sleep?

A

REM sleep and dreaming is suppressed; vivid and excessive dreaming during withdrawal

30
Q

what kind of tolerance produced by barbs?

A

metabolic: induce enzymes that metabolize them
cell: adaptation of neurons to drug presence

31
Q

4 reasons barbs are not widely used

A
  1. lethal in overdose
  2. narrow therapeutic range
  3. high potential for dependence/abuse
  4. dangerous interactions with other drugs
32
Q

4 symptoms of barb withdrawal

A
  1. hallucinations
  2. restlessness
  3. disorientation
  4. life threatening convulsions
33
Q

effects of barbs in pregnancy

A

possible risk of developmental abnormalities

34
Q

are nonbarb sedative hypnotics safer than barbs?

A

no

35
Q

methaqualone

A

quaaludes

36
Q

BZ MoA

A

GABA agonists, increase chloride ion influx; allosteric modulators that increase GABA binding to GABAa receptor binding site

37
Q

5 uses of BZs

A
  1. anxiolytic
  2. anticonvulsant
  3. insomnia
  4. central muscle relaxants
  5. potentiation of CNS depressants (anesthesia)
38
Q

% of dependent users of BZs; comorbid depressive disorders?

A

10%; 34%

39
Q

peak plasma conc of BZs

A

1 hour

40
Q

3 negative effects of BZs on elderly

A
  1. dementing
  2. depressive
  3. increased falls
41
Q

metabolite of diazepam

A

nordiazepam

42
Q

half life of nordiazepam

A

60 hours

43
Q

metabolite of lorazepam

A

glucoronide conjugated metabolite (inactive)

44
Q

2 short acting benzos

A
  1. halcion (triazolam)

2. xanax (alprazolam)

45
Q

intermediate acting BZ

A

lorazepam (ativan)

46
Q

2 long acting BZs

A
  1. chlordiazepoxide (librium)

2. diazepam (valium)

47
Q

6 limits of BZs

A
  1. poorly relieve stress
  2. limited anticonvulsant use
  3. complicate cog behav therapies (memory/cog problems)
  4. dementing
  5. rebounding symptoms w withdrawal
  6. addictive
48
Q

1mg xanax impairs driving comparable to BAC of ___

A

0.15

49
Q

ambien half life

A

2-2.5 hrs

50
Q

sonata half life

A

1 hour

51
Q

lunesta half life

A

5-7 hrs

52
Q

Z drugs are more selective for GABARs with ___

A

a1 subunits

53
Q

3 benefits of BZs

A
  1. safe
  2. do not induce metabolic enzymes
  3. act only on CNS
54
Q

what kind of memory is impaired with BZs?

A

episodic memory

55
Q

common users and abusers of BZs

A

older women

young male drug users

56
Q

benefit of ketamine as anesthetic

A

doesn’t reduce blood pressure

57
Q

ramelteon

A

selective meltaonin receptor agonist; very modest effect

58
Q

buspar

A

selective weak 5HT1a agonist

59
Q

what specific risk do barbs have for children?

A

trigger hyperactivity and learning problems

60
Q

antiepileptic drug problem for pregnancy

A

higher rates of stillbirth and infant mortality; 7% risk of birth defect

Psychopharmacology (22 decks)

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