Ramelteon

sleep · endocrine · digestive · Oral

Ramelteon, a sleep compound. Selective MT1 + MT2 melatonin-receptor agonist with ~16× greater MT1 affinity than melatonin. No GABAergic activity… Oral half-life 1.5 h.

Selective MT1 + MT2 melatonin-receptor agonist with ~16× greater MT1 affinity than melatonin. No GABAergic activity → no dependence potential, no scheduling. Modest efficacy on sleep-onset latency (~10 min improvement). CYP1A2 substrate — fluvoxamine contraindicated (>200× AUC rise).

ABSORPTION-RATE PROVENANCE: this value was derived by inverting the one-compartment peak-time relation in 2026-05-26-wave25-ka-from-tmax.ts, whose header claimed every peak time was verbatim from a primary human study. ALL FORTY-FOUR ENTRIES HAVE NOW BEEN CHECKED AND TWENTY-EIGHT FAIL. This one fails because the midpoint of a verbatim "Mean T(max) values of 0.75 to 0.94 hours". It is DISCLOSED RATHER THAN DELETED: a midpoint of a narrow range is usually inside the true spread, and removing it would fall back on the solver default of 1.0 per hour, which is worse for most of these records.

Pharmacokinetics

Sources: PMID:16432265, PMID:15695169