section name header

Pronunciation

tas-i-MEL-tee-on

Classifications

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: melatonin receptor agonists

Indications

REMS


Action

  • Acts as an agonist at melatonin MT1 and MT2 receptor sites, which are involved in regulation or circadian rhythm.
Therapeutic effects:
  • Improved circadian rhythm with improved sleep/wake patterns.

Pharmacokinetics

Absorption: 38% absorbed following oral administration, plasma concentrations in female patients.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP1A2 and CYP3A4 isoenzymes. Primarily excreted in urine as metabolites.

Half-Life: 1.3 hr.

Time/Action Profile

(establishment of circadian rhythm/sleep cycle)

ROUTEONSETPEAKDURATION
POwks–mosunknownunknown





Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

GI: liver enzymes

Neuro: headache, nightmares/unusual dreams

Interactions

Drug-drug:

Route/Dosage

Non-24-Hour Sleep-Wake Disorder

Nighttime Sleep Disturbances in Smith-Magenis Syndrome

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Hetlioz, Hetlioz LQ