module 3 sedatives and hypnotics Flashcards

1
Q

sedative

A

drug that produces a relaxing, calming effect

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2
Q

hypnotic

A

drug used to produce drowsiness and facilitate onset of sleep

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3
Q

GABA

A

inhibitory neurotransmitter in CNS

  • binds to GABA receptors and opens Cl channel
  • Cl enters the cell -> negative change in transmembrane potential -> hyperpolarization -> shutting down AP
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4
Q

sedative-hypnotic classes

A

benzodiazepines
barbituates
misc.

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5
Q

benzodiazepines MOA

A

GABA receptor modulator

  • inc. activity of GABA (gabaergic effect)
  • have no effect if GABA is not also present
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6
Q

benzodiazepine uses

A
anxiety
panic disorders
alcohol withdrawal 
CINV
seizure prevention/termination
status epiepticus
hypnotic
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7
Q

benzodiazepine AE

A

CNS depression
- less likely when used alone
tolerance
dependence

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8
Q

benzodiazepine administration

A

most are active drugs -> active metabolites

exceptions:
- lorazepam
- oxazepam
- temazepam

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9
Q

benzodiazepine interactions

A

CNS depressants

-> fatal CNS depression

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10
Q

benzodiazepine antidote

A

flumazenil

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11
Q

flumazenil MOA

A

GABA Rc antagonist

  • no effect on barbiturates or alcohol
  • can precipitate withdrawal
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12
Q

barbiturates MOA

A

binds to GABA Rc at allosteric site
- inc. GABA activity
higher dose -> direct agonizing of Rc -> inc. CNS depression

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13
Q

barbiturates use

A

anesthesia
emergency seizure tx
status epilepticus
insomnia

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14
Q

barbiturates AE

A

tolerance
dependence
fatal CNS depression

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15
Q

barbiturates withdrawal s/s

A
tremor
anxiety
insomnia
CNS excitability
seizure
cardiac arrest
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16
Q

barbiturates interactions

A

CYP450

- 3A4 inducer

17
Q

NBRA MOA

A

bind to same site on GABA Rc as benzos but chemically different

18
Q

NBRA uses

A

hypnotic

sleep aid

19
Q

NBRA AE

A
tolerance
dependence
memory impairment/amnesia
impaired judgement/reasoning
sleep walking
20
Q

NBRA administration

A

shorter half life than benzos

eszopiclone: for chronic use

21
Q

NBRA antidote

A

flumazenil

22
Q

NBRA education

A

less time to fall asleep

less REM sleep

23
Q

remelteon MOA

A

full agonist at melatonin Rc

24
Q

remelteon use

A

sleep

- maintain circadian rhythm of sleep/wake cycle

25
Q

remelteon education

A

no tolerance or dependence

not a controlled substance

26
Q

suvorexant MOA

A

orexin Rc antagonist

- suppresses the wake drive

27
Q

suvorexant AE

A

narcolepsy

cataplexy