Sedative Hypnotics Flashcards by Christina Provenza

progression of sedative hypnotics

anxiolysis
sedation
hypnosis
anesthesia
death

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use of barbiturates

induce anesthesia

rarely used

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use of benzodiazepines

anxiety
insomnia
epilepsy

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use of non-benzodiazepines (z drugs)

insomnia

safest for use

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GABA receptor for sedative/hypnotic

alpha1

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GABA receptor for anxiolytic and muscle relaxant

alpha2

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GABA receptor for anticonvulsant

alpha3

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GABA receptor for amnesia

alpha5

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barbiturate action at GABA receptor

increase duration of opening

increases efficacy of GABA

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benzodiazepine action at GABA receptor

increase frequency of opening

increases potency of GABA

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barbiturates to recognize

thiopental
pentobarbital
amobarbital
phenobarbital

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thopental

short acting barbiturate

used for amnesia prior to surgery

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phenobarbital

long acting barbiturate

used for seizures

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side effects of barbiturates

dose dependent respiratory depression
induction of liver enzymes
low margin of safety
increases porphyrin production- do not use with porphyria

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benzodiazepine side effects/toxicity

tolerance to sedation and euphoria
cross tolerance with other CNS depressants
physical dependence- withdrawal symptoms

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advantages of benzo use for insomnia over barbiturates

higher margin of safety than barbiturates- plateaus before bad effects
no cyp induction
milder withdrawal

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therapeutic use of bentos #1

insomnia- reduces time to sleep and increases total sleep time
moderate REM decrease
increase stage 2
decrease stage 4
REM rebound when ended

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flurazepam half life

40-100 (longest)

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flurazepam use

short term mild/moderate insomina

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flurazepam activity

prodrug

peak metabolite plasma concentration 1-3h

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flurazepam delivery/absorption

good absorption orally

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lorazepam half life

10-20hours

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lorazepam use

short term mild/moderate insomnia with anxiety

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lorazepam activity

slow

no active metabolites

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lorazepam delivery/absorption

oral- slow | IM- good

temazepam half life

10-40h

temazepam use

short term severe insomina

temazepam delivery/absorption

slow and erratic oral absorption

temazepam warnings

distorts normal sleep pattern | do not use during pregnancy

triazolam half life

short term acute insomnia (jet lag) | **doesn't work for frequent awakenings

triazolam activity

fast acting- peak plasma levels 1h

triazolam delivery/absorption

good oral

triazolam warnings

higher abuse potential (fast acting) | more severe withdrawal with chronic use

use #2 of benzos

amnesia during anesthesia for procedures

midazolam

benzo for amnesia short term use half life 2-6h

benzo overdose treatment

``` maintain respiration rule out narcotics by giving naloxone gastric lavage hemodialysis flumazenil ```

naloxone

drug for narcotic overdose

flumazenil

benzo antagonist that reverses respiratory depression very short acting- requires close monitoring causes withdrawal symptoms

do not give flumazenil to

seizure history barbiturate or TCA overdose careful with ethanol intoxication

z drugs

benzodiazepine receptor agonsits

insomnia drugs with highest margin of safety

z drugs

MOA of z drugs

interacts with alpha1 receptors

z drug that is non selective

eszopiclone

effects of z drugs

hypnosis with little muscle relaxant or anticonvulsant effects

use of z drugs

decrease latency without affecting sleep cycles

why are z drugs better than benzos

less: anti anxiety, anticonvulsant, muscle relaxant, impact on REM sleep

z drug metabolism

liver | change dose for elderly and liver disease

3 z drugs

zolpidem zaleplon eszopiclone

zolpidem half life

2-2.5h | medium duration

zolpidem form

tablet controlled release tablet sublingual, lingual

zolpidem metabolism

CYP 3A4

zolpidem ADR

dizziness diarrhea GI irritation

zolpidem residual sleepiness

confusion and falls in elderly | memory impairment at high doses

zaleplon half life

1h shorts duration approved for use during night

zaleplon metabolism

aldehyde oxidase- works in patients with liver dysfunction

zaleplon ADR

impaired fertility | color disturbances

zaleplon tolerancee

rebound insomnia at high doses

eszopiclone half life

6h | longest duration

eszopiclone metabolism

CYP 3A4

eszopiclone ADR

taste disturbance | xerostomia

eszopiclone residual sleepiness

next day memory impairment psychomotor impairment rebound insomnia

z drugs causing rebound insomina

zaleplon | eszopiclone

longest duration z drug

eszopiclone

shortest duration z drug

zaleplon

CYP 3A4 metabolized z drugs

zolpidem | eszopiclone

suvorexant

orexin receptor antagonist used for insomina

ramelteon

synthetic melatonin- against at SCM MT1 and MT2 receptors

do not give sedative-hypnotics to

obstructive sleep apnea