Ramelteon is a selective MT1/MT2 melatonin receptor agonist, indicated for the treatment of insomnia characterized by difficulty falling asleep.

How to Use Ramelteon

Standard Dosing Regimen

Dosage: The recommended dose is 8 mg, to be taken orally within 30 minutes before bedtime.

Dosage Form: 8 mg film-coated tablets, containing excipients such as lactose and starch; the tablets should be swallowed whole.

Timing of Administration: Administration with a high-fat meal should be avoided (as this can increase AUC by 31% and decrease Cmax by 22%).

Operational Precautions

Missed Dose Handling: If a dose is missed, it should be taken as soon as possible before bedtime, and the original scheduled dosing time should be resumed the next day.

Contraindicated Combinations: Concomitant use with potent CYP1A2 inhibitors (e.g., fluvoxamine) is contraindicated (as this can increase AUC by 190-fold).

Precautions for Ramelteon Use

Dosage Adjustments in Patients with Hepatic Impairment

Mild Hepatic Impairment: No dosage adjustment is required, but careful monitoring is necessary.

Moderate Hepatic Impairment: Use with caution (exposure may increase by more than 10-fold).

Severe Hepatic Impairment (Child-Pugh Class C): Contraindicated.

Management of Adverse Reactions

Common Reactions: Drowsiness (5%), dizziness (5%), and fatigue (4%); usually, no discontinuation of treatment is needed.

Endocrine Effects: Long-term use may increase prolactin levels (with an average increase of 34% in women); attention should be paid to symptoms such as menstrual abnormalities or galactorrhea.

Severe Reactions: If signs of allergy or liver injury (e.g., jaundice, elevated transaminases) occur, treatment should be discontinued immediately.

Drug Interactions

Enzyme Inducers (e.g., rifampicin): May reduce the efficacy of ramelteon; alternative treatment options should be evaluated.

Central Nervous System (CNS) Depressants (e.g., alcohol): May enhance sedative effects; concomitant use should be avoided.

Ramelteon Use in Special Populations

Elderly Patients

Dosage: Same as that for adults (8 mg), but note that AUC may increase by 97% (especially in patients aged ≥ 75 years).

Monitoring: Pay attention to residual effects the next day (e.g., fatigue, memory impairment).

Pregnant and Lactating Women

Pregnancy: Animal studies have shown a teratogenic risk (diaphragmatic hernia at doses ≥ 150 mg/kg); data in humans are limited. Use is only recommended when the potential benefit is significant.

Lactation: Ramelteon is excreted in rat milk; excretion in human milk is unknown. It is recommended to discontinue the drug or stop breastfeeding.

Patients with Respiratory Diseases

Mild to Moderate COPD/Sleep Apnea: May be used, but data on severe cases are lacking.

Severe Sleep Apnea: Use is not recommended.