INSOMNIA

Question 1

Selecting a pharmacologic agent for sleep (3)

Answer 1

1. sleep symptom pattern to improve (latency - pick a shorter T1/2, or maintenance - pick a longer T1/2)
2. Patient preference
   - ->sleep improvement - benefit vs side effects - risk
   - -> controlled substance vs Rx vs OTC
   - -> cost
3. Past response

*pick a profile to match the ℅ and situation

Question 2

Benzo - MOA

Answer 2

binds to central GABA receptors via the BZDP binding site and inhibit neurotransmission from CNS

Question 3

2 GABA subunits and their effects

Answer 3

• ->alpha 1 = sedative/hypnotic

- ->alpha 2= anxiolytic/muscle relaxant

Question 4

Why do Non-BZDP have an improved SE profile over BZDP?

Answer 4

higher affinity to alpha 1 (sedative/hypnotic)

Question 5

Which med for insomnia has better anticonvulsant, anxiolytic and muscle relaxant properties?

Answer 5

BZDP

Question 6

BZDP- Side effects

Answer 6

Daytime symptoms - “hangover” effect - drowsiness, mental/motor depression, amnesia
Psych effects - complex sleep related behaviors, worsening depression, behavioral changes (hallucinations, psychosis)
Withdrawal symptoms

Question 7

BZDP vs Non-BZDP - more tolerance?

Answer 7

BZDP

Question 8

BZDP - Precautions

Answer 8

Hx depression, suicidal thoughts
Hx complex sleep-related behaviors
Hepatic disease
Hx drug/ETOH abuse
Use of other CNS depressants
Limitation on planned amount of sleep
Impaired sleep function (apnea, COPD)

Question 9

Estazolam (Prosom), Temazepam (Restoril) and Triazolam (Halcion) - class?

Answer 9

Short or intermediate acting BZDP

*cause less fatigue

Question 10

Flurazepam (Dalmane) and Quazepam (Doral) - class?

Answer 10

Long acting BZDP

*more fatigue

Question 11

Eszopiclone (Lunesta), Zaleplon (Sonata), Zolpidem (Ambien) - class?

Answer 11

Non-BZDP Receptor Agonist

Question 12

Which drugs are potent 3A4 inhibitors?

Answer 12

Amiodarone
Protease Inhibitors
Dilt/Verapamil
E-mycin/Clarithro

Question 13

Non-BZDP Receptor Agonists - DDI

Answer 13

3A4

Question 14

Non-BZDP - education

Answer 14

take at bedtime
not with high fat meal
must have time for enough sleep

Question 15

Ambien Tab vs SL

Answer 15

Tab - longer duration (lasts 8 hrs), women need less (1.75 mg vs 3.5mg) because clear slower (AUC)
SL - for middle of the night waking (lasts 4 hrs)

Question 16

Ambien is a substrate of _____ and _____.

Answer 16

3A4 and 1A2

Question 17

What are the inhibitors of 1A2?

Answer 17

Cipro
Amniodarone
(will increase concentration of meds so need to decrease dose of med)

Question 18

TCA FDA approved for insomnia

Answer 18

Doxepin (Silenor)

Question 19

*Antihistamines for sleep

Answer 19

Benadryl, doxylamine (Aldex) and pyrilamine

Less effective then BZDP

Question 20

*Herbals for sleep

Answer 20

Melatonin, Kava, Valerian Root
MOA - binds to a different subunit then BZDP
*Don’t co-administer with BZDP

Question 21

What antidepressant should be consider for sleep if using SSRI therapy and experiencing insomnia (b/c depression is a CI for sedative-hypnotic)?

Answer 21

Trazodone 25-100mg nightly

Question 22

Zolpidem AkA

Answer 22

Ambien

Question 23

Eszopiclone AKA

Answer 23

Lunesta

Question 24

Temazepam AKA

Answer 24

Restoril

Question 25

Zolpidem AkA

Answer 25

Ambien

Question 26

Zalepion AKA

Answer 26

Sonata

Question 27

*Which NonBZDP GABA agonists are approved for long term (6-12 months) insomnia treatment?

Answer 27

Eszopiclone (Lunesta)

Zolpidem (Ambien)

Question 28

*Typical time frame for short term insomnia treatment?

Answer 28

2-4 weeks

Question 29

*Risk factors for insomnia?

Answer 29

older
female
comorbid conditions (GERD, CHF, Psych)
shift work
unemployed