Comparative Pharmacology
Head-to-head clinical analysis: RAMELTEON versus TASIMELTEON.
Peer-Reviewed Evidence
Head-to-head clinical analysis: RAMELTEON versus TASIMELTEON.
RAMELTEON vs TASIMELTEON
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Tasimelteon is a selective melatonin MT1 and MT2 receptor agonist that mimics the natural sleep-promoting effects of melatonin by modulating circadian rhythms. It binds to MT1 receptors to promote sleep onset and to MT2 receptors to phase-shift the circadian clock.
8 mg orally once daily within 30 minutes of bedtime.
20 mg orally once daily at bedtime, taken within 30 minutes of retiring and at the same time each night. Not to be taken with or immediately after a high-fat meal.
MODERATE Risk
MODERATE Risk
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.
1.3 hours (range 0.5–2.0 h); short half-life consistent with use for sleep initiation without residual sedation.
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.
Primarily hepatic metabolism via CYP1A2 and CYP3A4; <0.1% excreted unchanged in urine; fecal excretion accounts for ~80% of total clearance as metabolites.
Category C
Category C
Melatonin Receptor Agonist
Melatonin Receptor Agonist
"The metabolism of Cyclosporine can be decreased when combined with Ramelteon."