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T&D II exam 1 > Sleep > Flashcards

Sleep Flashcards

1
Q

Benzodiazepines

what does it do?

A

Dec sleep latency
dec number of awakenings
inc awakening threshold

Time in stage 2 inc, time in stages 3 and 4 dec

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2
Q

BDZ

net effect

how

A

inc in sleep time

by ALTERED sleep architecture

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3
Q

SE of BDZ

A

Dev of tolerance

rebound of REM w/ discont.

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4
Q

Examples of BDZ

A 
Flurazepam(long)
Temazepam(mid)
Triazolam(short)
Quazepam
Estazolam
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5
Q

Flurazepam

A

dec in sleep-induction time
dec in number of awakenings

LONG ACTING

little rebound

DAY TIME SEDATION AND ACCUMULATION OF DRUG - long half life

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6
Q

Temazepam

A

for pts who exp FREQUENT WAKENING

give couple of hours before desired bedtime

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7
Q

Triazolam

A

short action

used to INDUCE sleep - ptns w/ recurring insomnia

TOLERANCE devs fast! - use intermittently!

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8
Q

Zolpidem

A

non-BDZ
most commonly used?
acts at BDZ RECEPTOR

quick onset

PRESERVES SLEEP STRUCTURE

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9
Q

Zaleplon

A

Binds BDZ receptor

short duration, rapid onset

half life of 1 hr: used in middle of night for broken sleep

Abuse potential

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10
Q

Eszopicione

A

longer half life

BDZ like

not for short term use

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11
Q

Barbiturates

A

once used as sedative hypnotics

use minimized bc of

  • drug tolerance
  • inc CYP activity
  • physical dependence
  • withdrawal sx
  • Coma at toxic doses
  • no antidote
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12
Q

Low vs high conc of BARBs

A

low: depress CNS activity
high: Depress nerve, sk muscle and smooth and cardiac muscle

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13
Q

MOA BARBs

A

open channel for longer periods than BDZs

inh release of excitatory transmitters

depress Ca2+/Ca dep release of NT

Stabilize membrane

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14
Q

BARBs mimic _____ at high doses

A

GABA

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15
Q

Induction of Anesthesisa

A

BARBs

Specifically: THIOPENTAL

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16
Q

Therapeutic use of BARBs

A
  • antagonize CNS stimulants
  • sedation
  • anticonvulsant
  • induction of anesthesia
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17
Q

how does BARBs affect REM cycles/time spent in it

A

Decreases

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18
Q

Effect of BARBs on

  1. respiration
  2. cardio
  3. hepatic
  4. Pregnant women/breast feeding
A
  1. depress neurogenic drive
  2. minimal effect
  3. contraindicated for acute/intermittent PORPHYRIA - bc of delta-aminolevulinic acid synthetase activation causing porphyria exacerbation
  4. crosses placenta, appears in br milk
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19
Q

Does tolerance occur with BARBs

A

yes

even cross tolerance to other CNS depressants

and withdrawal rxns

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20
Q

is analgesia produced with BARBs?

A

No

but HYPERALGESIA in response to painful stimuli

21
Q

Truth Serum

route of admn

A

narcotherapy

IV
Sedation
“inhibitions are removed”

22
Q

Truth serum

A

Amobarbital
pentobarpital
thiopental

23
Q

Is there an antidote for acute toxicity of BARBs

A

no

you have to remove unabsorbed drug by lavage
artificial ventilation
hemodialysis
charcoal

24
Q

Chronic use of BARBs

A

downregulates GABA receptors – inc cholinergic activity – elevates glutamate receptors: EXCITEMENT (upon withdrawal)

ABSTIENCE SYNDROME

life threatening

25
Q

an example of barbiturate like sedative

A

Chloral hydrate

26
Q

Chloral hydrate

A
  • short active
    GI irritation

Prodrug. active met: trichloroethanol

enhances effects of CNS depressants:
-w/ alcohol – “knock out drops”

mild insomnia, less effective than BDZ

27
Q

Diphenhydramine

Doxylamine

A
  • histamine antagonist
  • tx of mild insomnia
  • less effective than BDZ
28
Q

Synthesis of melatonin

when is it secreted

A

pineal gland from tryptophan

inc in late evening, peaks in the middle of the night, dec in morning
diurnal rhythm

29
Q

Ramelton

A
  • melatonin receptor agonist

rapid onset
minimal rebound

NO abuse potential (good for adolescents)

30
Q

EtOH

A

CNS depressant

positive allosteric modulator of GABA receptor

Dec sodium and Calcium influx

31
Q

use of ethanol

A

methanol or ethylene glycol intoxication - greater affinity of alc dehydrogenase for ethanol

dec formation of toxic metabolites
methanol -**- formaldehyde – formate

32
Q

used as treatment of alcoholism

A

Disulfiram

accumulation of acetaldehyde – causes:

  • flushing
  • tachycardia
  • hyperventilation
  • nausea
33
Q

disulfiram acts on

A

aldehyde dehydrogenase (inhibits)

34
Q

Treatment of withdrawal/relapse

A

Naltrexone

Acamprosate

35
Q

MOA Naltrexone

A

opioid receptor antagonist

reduces craving/blunts pleasurable effects

DEC Dopamine release in nucleus accumbens

36
Q

Major side effect of Naltrexone

A

Nausea

37
Q

MOA Acamprosate

A

structural analog of GABA

dec glutamate neurotransmission during alcohol withdrawal

38
Q

Major side effect of Acamprosate

A

Diarrhea

39
Q

How do most meds improve sleepiness

A

enhance dopamine signaling

40
Q

how do most cataplexy-suppressing meds work

A

inc NE or Serotonin signaling

41
Q

Narcolepsy

Excessive daytime sleepiness

A

Modafinil
Methylphenidate
Amphetamines

42
Q

Narcolepsy

Cataplexy

A

Antidepressants

Gamma hydroxybutyrate

43
Q

Narcolepsy

Disrupted nighttime sleep

A

Zolpidem

Gammahydroxybutyrate

44
Q

Modafinil

A
  • Dopamine transporter blocking activity

Narcolepsy, Shift work sleep disorder, obstructive sleep apnea (adjunct)

45
Q

when do you admn Modafinil

  • Narcolepsy
  • shift worker
A
  • narc: in the morning

- shift worker: 1 hr before shift

46
Q

most comon SE with Modafinil

A

Rhinitis

don’t give to kids!

47
Q

Gamma hydroxybutyrate

A

natural product formed from GABA

better night time sleep = reduces cataplexy during the day

Interacts with GHB receptor, GABAb receptor
- effect on slow-wave sleep

48
Q

“date rape drug”, CNS depressant

A

Gamma hydroxybutyrate

49
Q

most common SE of Gamma hydroxybutyrate

A

Vomiting

T&D II exam 1 (8 decks)

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