Drugs for Insomnia

Question 1

Temazepan

benzodiazepine

Answer 1

MOA: binds to allosteric site on GABA-A receptor to enhance the action of GABA

Use: Insomnia

SE: depresses REM sleep

Metabolized by CYP3A4
CI: grapefruit juice

Question 2

Eszopiclone (Lunesta)

Non-benzodiazepine

Answer 2

MOA: selective binding to and activation of GABA-A receptors containing a1 subunits – only have sedative effects

Use: Insomnia – decrease sleep latency and increase total sleep time without affecting REM sleep

PK: longest duration of action, metabolized by CYP3A4

*additive effects with other CNS depressants

Question 3

Zolpidem (Ambien)

Answer 3

MOA: selective binding to and activation of GABA-A receptors containing a1 subunits – only have sedative effects

Use: Insomnia

SE: confusion, ataxia, delirium, psychotic reactions, HA

PK: metabolized by CYP3A4

Question 4

Zalepon (Sonata)

Answer 4

MOA: selective binding to and activation of GABA-A receptors containing a1 subunits – only have sedative effects

Use: Insomnia

SE: back and chest pain, migraines, GI effects, difficulty concentrating

PK: metabolized by CYP3A4; shortest duration of action

Question 5

Ramelteon

Melatonin receptor agonist

Answer 5

MOA: binds with high affinity to MT1 and MT2 receptors in the SCN of hypothalamus

Use: shortens sleep latency but does not prolong maintenance

SE: somnolence, fatigue, dizziness

PK: metabolized by CYP1A2; CI fluoxetine (inhibits CYP1A2)