Ramelteon

Products

Ramelteon has been approved in the United States since 2005 in the form of film-coated tablets (Rozerem). The drug is not currently registered in many countries. The EMA had rejected approval in the EU because it judged the evidence of efficacy to be insufficient.

Structure and properties

Ramelteon (C16H21NO2, Mr = 259.3 g/mol) exists as an -enantiomer that is very sparingly soluble in water. It is structurally related to the sleep hormone melatonin.

Effects

Ramelteon (ATC N05CH02) has sleep-promoting properties. The effects are due to binding to the melatonin MT1 and melatonin MT2 receptors, which play a central role in the sleep-wake cycle (see under melatonin).

Indications

For the treatment of sleep disorders with difficulty falling asleep. Ramelteon has not yet been approved for other indications (eg, jet lag).

Dosage

According to the expert information. The tablets are taken once daily thirty minutes before bedtime. They should not be given with or immediately after a meal with a high fat content.

Contraindications

  • Hypersensitivity
  • Combination with the CYP inhibitor fluvoxamine

Full precautions can be found in the drug label.

Interactions

Ramelteon is metabolized by CYP1A2, CYP2C, and CYP3A4. Corresponding drug-drug interactions are possible. The potent CYP1A2 inhibitor fluvoxamine is contraindicated because it may inhibit degradation and increase concentrations. Ramelteon should not be combined with alcohol.

Adverse effects

The most common possible adverse effects include drowsiness, dizziness, fatigue, nausea, and worsening of sleep disturbances.