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Neuro Pt 4 > Insomnia Pharm > Flashcards

Insomnia Pharm Flashcards

1
Q

Phenelzine

A

MOA inhibitor

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2
Q

Antimuscarinic drugs and sleep

A

Act through ACh
Off when asleep
Helps put you to sleep
Pedunculopontine Tegmental

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3
Q

Antidepressants and sleep

A

Increase serotinin activity
Help with sleep
Dorsal Raphe

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4
Q

Amphetamines and sleep

A

Dopamine and NE increase wakefulness

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5
Q

Antihistamines and sleep

A

Help you sleep

Posterior hypothalamus

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6
Q

Benzodiazepines and sleep

A

Enhance GABA and promote sleep

Anterior hypothalamus

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7
Q

Orexin antagonists and sleep

A

promote sleep by blocking excitatory actions of orexin on NE-5HT neurons

Lateral Hypothalamus

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8
Q

Adenosine antagonists and sleep

A

ex Caffeine
increase alertness
Basal forebrain

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9
Q

Stages of sleep

A

Non-REM (70-75%):
Stage I- transition phase; EEG like wakefullness
Stage II- Light sleep EEG slower
Stage III and IV (delta)- EEG very slow, deepest level of sleep (described as “best”); stage where somnambulism and night terrors can occur

REM sleep (25-30%): Occurrence of rapid eye movements, decreased muscle tone, increased blood pressure, pulse, and respiration; stage of most recallable dreams

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10
Q

Benzodiazepines and Non-Benzodiazepine Receptor Agonists mechanism of action

A

facilitating the action of GABA at the GABAA receptor-chloride channel complex

GABA appears to interact with alpha or beta subunits triggering chloride channel opening with resultant membrane hyperpolarization

Bind to GABA-chloride channels with both α1 and α2/α5 subunits and result in both sleep and anxiolysis

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11
Q

GABA receptors with alpha 1 subunits

A

highly expressed in the cortex

Mediate sedative (sleep), amnestic, and anticonvulsant actions of benzodiazepines

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12
Q

GABA receptors with alpha-2/alpha-5 subunits

A

highly expressed in the limbic system /brain stem

Mediate myorelaxant, motor impairing, anxiolytic, and ethanol-potentiating effects of benzodiazepines

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13
Q

“z-drugs”

A

(zolpidem, zaleplon, eszopiclone)

Non-benzodiazepines - bind only to GABA-chloride channels with α1 subunits resulting in sleep without anxiolysis (reduced potential for dependence)

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14
Q

Name the 3 major Benzodiazepines used for sleep aid

A

Triazolam
Temazepam
Flurazepam

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15
Q

Triazolam

A

A benzodiazepine

Sleep aid

Eliminated within 1 dosing cycle (t1/2: 1.5-5 hrs),

less daytime sedation (hangover)

use cautiously in elderly with dose reduction

rapidly absorbed

Can see rebound insomnia next day due to rapid elimination

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16
Q

Temazepam

A

A benzodiazepine

Sleep aid

Intermediate t1/2 (9-13 hrs)

slowly absorbed

peak concentration at 2-3 hrs

minimal effect on latency to sleep onset

17
Q

Flurazepam

A

A benzodiazepine

Sleep aid

Long t1/2 with active metabolite (75-90 hrs),

see effect at same dose for 28 consecutive days (i.e., little tolerance).

Can accumulate in elderly due to impaired hepatic clearance leading to daytime sedation (“hangover”) / overdosage (t1/2 extended to 120-160 hrs).

18
Q

“Z-drugs” (name them!)

A

Zolpidem

Zaleplon

Eszopiclone

19
Q

Zolpidem

A

A “z-drug” for sleep aid

Short durations of action (6-8 hours) and half-life (zolpidem: 2-2.5 hrs).

Rapid oral absorption.

Effective for reducing sleep latency and nocturnal awakenings with an increase in total sleep time and efficiency.

20
Q

Zaleplon

A

A “z-drug” for sleep aid

Short durations of action (6-8 hours) and half-life (zaleplon: 1 hr).

Rapid oral absorption.

Best suited for use as a sleep aid for middle-of-the-night awakenings

Decreasing time to sleep onset

21
Q

Eszopiclone

A

A “z-drug” for sleep aid

Structurally different from zolpidem or zaleplon with longer t1/2 (∼ 6 hrs)

safe for long term use with little or no suggestion for development of tolerance

22
Q

Adverse effects of benxodiazepines

A

In general, very safe and fatal overdoses are rare unless they are taken in combination with other CNS depressants or alcohol.

Daytime sedation and performance impairment

Anterograde amnesia, rebound insomnia, Psychologic and Physical Dependence

23
Q

What schedule are Benzodiazepines?

A

schedule IV

24
Q

Adverse effects of “Z-drugs”

A

Zolpidem: Drowsiness, amnesia, dizziness, headache and GI complaints. Does not appear to have significant effects on next-day psychomotor performance. Rebound effects and withdrawal and tolerance with prolonged use appear minimal, but are possible.

Zaleplon: Most common side effects are dizziness, headache, and somnolence. Like zolpidem, no next-day psychomotor impairment or rebound insomnia

Eszopiclone: Similar to zolpidem but longer half-life associated with increased incidence of next day psychomotor impairment with higher doses - FDA required lower dose for initiation [2014]

25
Q

What schedule are z-drugs?

A

schedule IV

26
Q

Trazodone

A

Non-GABA-Benzodiazepine Receptor mechanism

Complex effects on 5HT neurons, including weak but specific inhibition of reuptake and both agonist and antagonist receptor actions

Antidepressant

Watch out in elderly (Oversedation and orthostasis)

27
Q

Tricyclic Antidepressants (TCADs)

A

Non-GABA-Benzodiazepine Receptor mechanism

Block of reuptake of serotonin and/or norepinephrine

Adverse rxn: Antimuscarinic activity

28
Q

Ramelteon

A

Non-GABA-Benzodiazepine Receptor mechanism

Agonist at melatonin MT1 (induce sleepiness) and MT2 receptors (regulation of circadian rhythms) in suprachiasmatic nucleus of hypothalamus. Decreases mean latency to sleep

29
Q

Antihistamines

A

Non-GABA-Benzodiazepine Receptor mechanism

example: Diphenhydramine

Antagonist action at histamine H1 and muscarinic cholinergic receptors in the CNS resulting in sedating properties

Less effective than benzodiazepines

NOT recommended

May be useful short-term

30
Q

Chloral Hydrate

A

Non-GABA-Benzodiazepine Receptor mechanism

Old drug (1800’s), may be effective hypnotic for a few nights for transient insomnia. Continued use often leads to physical dependence.

31
Q

Which class of drugs for sleep aid decreases delta and REM sleep?

A

Benzodiazepines

32
Q

What is the tolerance like for benzodiazepines and z-drugs

A

BZD: if used for more than one week, get tolerance

Z-drugs: little tolerance

33
Q

Flumazenil

A

antagonist that binds to same site as BDZs and “Z”-drugs

Used in treatment of benzodiazepine overdose toxicity

NOT effective for BARB or ethanol toxicity

Neuro Pt 4 (25 decks)

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