Ramelteon tablets are indicated for the treatment of insomnia characterized by difficulty in sleep onset.

Ramelteon is a melatonin receptor agonist with high affinity for MT1 and MT2 receptors and selectivity over the MT3 receptor. Its action at MT1 and MT2 receptors is believed to promote sleep by influencing the circadian rhythm that regulates the normal sleep–wake cycle. These receptors are normally activated by endogenous melatonin. Ramelteon has no significant affinity for the GABA receptor complex or for receptors associated with neuropeptides, cytokines, serotonin, dopamine, noradrenaline, acetylcholine, or opioid systems.

Adults: One tablet (8 mg) taken within 30 minutes of going to bed. It should not be taken with or immediately after a high-fat meal. Total daily dose should not exceed 8 mg.

Elderly: No overall differences in safety and efficacy between elderly and younger adult subjects.

Children: Safety and effectiveness not established.

• Rifampin: Decreases exposure to ramelteon and reduces its effects.
• Ketoconazole: Increases the AUC of ramelteon.
• Fluconazole: Increases systemic exposure to ramelteon.
• Donepezil: Increases systemic exposure to ramelteon.
• Doxepin: Increases systemic exposure to ramelteon.

Hypersensitivity to any component of this formulation.

The most common adverse effects include somnolence, dizziness, fatigue, nausea, headache, and worsening of insomnia. Hallucinations and behavioral changes such as unusual behavior, agitation, and mania have also been reported. Amnesia, anxiety, and other neuropsychiatric symptoms may occur unpredictably.

Pregnancy Category C. Animal studies suggest possible fetal risk. Ramelteon should be used during pregnancy only if the potential benefit justifies the potential risk. It is not known whether ramelteon is excreted in human breast milk. Caution is advised when administering to breastfeeding women.

Possible risks include angioedema, anaphylaxis, hallucinations, decreased testosterone levels, and increased prolactin levels.

General symptomatic and supportive treatment should be provided. Gastric lavage may be considered if appropriate. Intravenous fluids should be administered as needed. Vital signs such as respiration, pulse, and blood pressure should be closely monitored, along with supportive care.

Miscellaneous sedatives and hypnotics

Store below 30°C, protected from light and moisture. Keep out of reach of children.