Rozerem

Rozerem is the brand name for ramelteon, a prescription sleep medication approved for adults with insomnia characterized by difficulty falling asleep. It is a melatonin receptor agonist marketed for the treatment of sleep-onset insomnia and is not intended for sleep maintenance. Ramelteon is not a controlled substance in the United States and is typically prescribed to adults after assessment for sleep disorders.

Mechanism of action

Ramelteon is a selective agonist of the MT1 and MT2 melatonin receptors. By activating these receptors in the suprachiasmatic nucleus, it helps regulate circadian timing and promotes sleep onset without acting on GABA receptors, distinguishing it from benzodiazepine and non-benzodiazepine hypnotics.

Dosage, pharmacokinetics, and interactions

Ramelteon is administered orally, with a common dose of 8 mg taken about 30 minutes before bedtime. It has a relatively short elimination half-life and is rapidly absorbed. The drug is extensively metabolized by hepatic cytochrome P450 enzymes, particularly CYP1A2, with contributions from CYP2C9 and CYP3A4. Because of this metabolism, ramelteon can interact with strong CYP1A2 inhibitors (for example, fluvoxamine) and inducers (such as rifampin). Food does not appear to have a major effect on overall exposure, but timing relative to meals may be considered when scheduling doses.

Safety and indications

Common adverse effects include somnolence, dizziness, fatigue, nausea, and headache. Rare reactions can include allergic responses such as angioedema. Ramelteon is not associated with a significant abuse potential and does not carry a boxed warning. It should be used with caution in hepatic impairment, and safety in pregnancy and lactation has not been established.