Insomnia drugs [3] Flashcards
Admin of which drug is most likely to produce memory disturbances such as anterograde amnesia?
(aka which one enhances GABA fxn?)
BDZ: Diazepam (anxiolytic)
Glutamate is active when forming memory
Enhancing GABA indirectly reduces Glu
(note: a1 enhance sleep, a2-5 lessens anxiety)
Phenelzine
MAOI
Monoaminergic cell groups activate cerebral cortex to facilitate PROCESSING of these thalamic inputs:
List the NT these red pathways secrete
- Locus ceruleus
- Raphe
- Tuberomamillary
- VTA
- Basal forebrain
- Locus ceruleus: NE
- Raphe: 5HT
- Tuberomamillary: His
- VTA: DA
- Basal forebrain: ACh
GABA is (select one) Off/ON when you are awake. _____ Enhances GABA and promote sleep.
OFF
BDZ
(GABA released from anterior hypothalamus
High ACh, 5HT, and GABA help you go towards (pick one) wakefulness/sleep
sleep
Z drugs are good at preserving which part of your sleep?
REM (20-25% of your sleep, stage of recall-able dreams)
Which stage of sleep predominates?
Stage 2 (50%) - ligh sleep, EEG slower
BDZ for sleep
Triazolam
Temazepam
Flurazepam
Z drugs for sleep
zolpidem (closest to ideal)
zaleplon
eszopiclone
BDZ effects of stages of sleep
- Sleep latency
- Duration
- 1
- 2
- 3
- 4
- REM
- Sleep latency: ↓
- Duration: ↑
- 1: ↑
- 2: ↑
- 3: ↓
- 4: ↓
- REM: ↓
sleep faster + stay asleep
*note (latency, duration, 1 are like Z drugs)
Z drugs effects of stages of sleep
- Sleep latency
- Duration
- 1
- 2
- 3
- 4
- REM
- Sleep latency: ↓
- Duration: ↑
- 1: ↑
- 2: ↑
- 3: no effect
- 4: no effect
- REM: no effect
sleep faster + stay asleep
diff btwn a1 and a2-5 location effects
a1: cortex
- sleep
- anticonvulsant
a2-5: limbic system + brain stem
- anxiolytic
- myorelaxant
Diff btwn Z drugs and BDZ (triazolam)
for: hypnotic, anticonvulsant, myorelaxant
- quantal vs graded
Z drug:
quantal response: bam you asleep (immediate release)
upping the dose → see anticonvulsant and myorelaxant effects
BDZ:
Graded (gradual)
intially see anticonvulsant and myorelaxant → up the dose and get hypnotic effect
(feel relax b4 sleep unlike Z drug)
Why wont Tamazepam be impaired as you get older?
goes out phase II
metab not affected by age
Hangover effect is least likely seen in drugs with long or short half lives?
short
hangover effect is seen in drugs with long half lives
Which of the Z drugs:
- have the longest half life?
- reduces nocturnal awakenings?
- best for middle of the night awakenings?
- is best for sleep maintanence
Eszopiclone
Zolpidem
Zaleplon (short half life)
Eszopiclone (long half life)
Do BDZ or Z drugs cause anterograde amnesia?
Which has high therapeutic index relative to barbs?
Both (a1)
Both
Trazodone
- MOA
- ADRs
- clinical use
Mixed Serotonin receptor antagonist and reuptake blocker
Oversedation, orthostasis (a1), Priapism
*an antidepressant
Ramelteon
- MOA
- ADRs
- clinical use
Melatonin receptor agonist
dizziness, somnolence, fatigue, nausea
*sedative
Diphenhydramine (benadryl)
- MOA
- clinical use
H1 and muscarinic R antagonist
sedative, hypnotic, anxiolytic
have to get into the brain to cause sleepiness - 1st gen
Quetiapine effects on sleep
(atypical antipsychotic agent)
D2 antagonist
- leave Extrapyramidal side effects alone better than typical
- improve DA release in mesocortical pathway- control negative symp
Can be used as an adjunctive (just like melatonin and diphenhydramine)
which agents used in tx of insomnia are likely to cause anticholinergic side effects?
1st gen antihistamines
(block muscarinic receptors as well as H1)
- Diphenhydramine
- Doxylamine