Comparative Pharmacology
Head-to-head clinical analysis: HETLIOZ versus RAMELTEON.
Peer-Reviewed Evidence
Head-to-head clinical analysis: HETLIOZ versus RAMELTEON.
HETLIOZ vs RAMELTEON
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Melatonin receptor agonist; selective agonist at MT1 and MT2 receptors in the suprachiasmatic nucleus, regulating circadian rhythms.
Selective melatonin receptor agonist with high affinity for MT1 and MT2 receptors in the suprachiasmatic nucleus; promotes sleep by mimicking the effects of endogenous melatonin.
20 mg orally once daily at bedtime, take within 30 minutes of bedtime, with or without food.
8 mg orally once daily within 30 minutes of bedtime.
None Documented
None Documented
Terminal elimination half-life is approximately 1.3-1.5 hours. No clinically relevant accumulation with daily dosing.
Clinical Note
moderateRamelteon + Tenofovir disoproxil
"The metabolism of Tenofovir disoproxil can be decreased when combined with Ramelteon."
Clinical Note
moderateRamelteon + Sulfisoxazole
"The serum concentration of Sulfisoxazole can be increased when it is combined with Ramelteon."
Clinical Note
moderateRamelteon + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Ramelteon."
Clinical Note
moderateRamelteon + Cyclosporine
1-2.6 hours. The terminal half-life is short (mean ~1.3 hours) with no accumulation upon repeated dosing. Clinical context: Rapid clearance supports once-nightly dosing for sleep onset insomnia.
Primarily hepatic metabolism; 77-88% excreted in feces as metabolites, 13-23% in urine as metabolites. <1% excreted unchanged.
Ramelteon is extensively metabolized, primarily via CYP1A2 and to a lesser extent CYP2C9 and CYP3A4. Approximately 84% of the dose is excreted in urine as metabolites, with 4% as unchanged drug. Fecal excretion accounts for about 4% of the dose.
Category C
Category C
Melatonin Receptor Agonist
Melatonin Receptor Agonist
"The metabolism of Cyclosporine can be decreased when combined with Ramelteon."