section name header

Pronunciation

ra-MEL-tee-on

Classifications

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: melatonin receptor agonists

Indications

REMS


Action

  • Activates melatonin receptors, which promotes maintenance of circadian rhythm, a part of the sleep-wake cycle.
Therapeutic effects:
  • Easier onset of sleep.

Pharmacokinetics

Absorption: Well absorbed (84%), but bioavailability is low (1.8%) due to extensive first pass liver metabolism. Absorption by a high-fat meal.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Extensively metabolized by the liver primarily by the CYP1A2 isoenzyme and to a lesser extent by the CYP2C9 and CYP3A4 isoenzymes. Metabolites are excreted mostly in urine (88%); 4% excreted in feces.

Half-Life: 1–2.6 hr.

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
POrapid30–90 minunknown





Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Endo: prolactin levels, testosterone levels

GI: nausea

Neuro: abnormal thinking, behavior changes, dizziness, fatigue, hallucinations, headache, insomnia (worsened), sleep-driving

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions

Drug-drug:

Route/Dosage

Availability

(Generic available)

Assessment

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Rozerem