Generic
Ramelteon
1 brands available in the market
At a glance
Ramelteon is a melatonin receptor agonist used for the treatment of insomnia characterized by difficulty with sleep onset. It has high affinity for melatonin MT1 and MT2 receptors and helps maintain circadian rhythm.
Description
Ramelteon is a melatonin (MT) receptor agonist with high affinity for melatonin MT1 and MT2 receptors and selectivity over the MT3 receptor. Its activity at MT1 and MT2 receptors is believed to contribute to its sleep-promoting properties. Ramelteon has no appreciable affinity for the GABA receptor complex or for receptors that bind to neuropeptides, cytokines, serotonin, dopamine, noradrenaline, acetylcholine, and opiates.
Indications
- Insomnia characterized by difficulty with sleep onset
Therapeutic class
Miscellaneous sedatives & hypnotics
Pharmacological class
Melatonin Receptor Agonist
Pharmacology
Ramelteon acts as an agonist at melatonin MT1 and MT2 receptors, which help maintain circadian rhythm when activated by endogenous melatonin. It does not bind to GABA receptors or other neurotransmitter receptors, distinguishing it from other hypnotics and reducing dependence risk.
Mechanism of action
Regulates sleep-wake cycle by activating melatonin receptors.
Dosage
Adult Dose (Oral):
- 8 mg taken within 30 minutes of going to bed
- Total daily dose should not exceed 8 mg
- Do not take with or immediately after a high-fat meal
Administration
- Take within 30 minutes of going to bed
- Do not take with high-fat meals
- Take at the same time each day
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, skip it and continue with your normal schedule; do not double the dose.
Side effects
Common Side Effects:
- Somnolence
- Dizziness
- Fatigue
- Nausea
- Headache
- Exacerbated insomnia
- Hallucinations
- Behavioral changes
- Amnesia
Precautions & warnings
- May affect driving ability; do not drive if drowsy or dizzy
- Avoid alcohol
- Discontinue if angioedema, anaphylaxis, hallucinations occur
- May decrease testosterone and increase prolactin
- Inform doctor if no improvement in sleep after 7-10 days
Contraindications
- Hypersensitivity to ramelteon or any ingredient
- Severe hepatic impairment
- Patients who develop angioedema should not be re-challenged
Drug interactions
- Rifampin (strong CYP inducer): Decreases exposure and effects
- Ketoconazole (strong CYP3A4 inhibitor): Increases AUC; administer with caution
- Fluconazole (CYP2C9 inhibitor): Increases systemic exposure; administer with caution
- Donepezil: Increases systemic exposure; monitor closely
- Doxepin: Increases systemic exposure; monitor closely
- Alcohol: Additive psychomotor impairment; should not be used in combination
Food interactions
Alcohol consumption with Ramelteon is unsafe.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects; use only if clearly needed.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited human data suggests drug may pass into breast milk; monitor baby for sleepiness, weight gain, and developmental milestones.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
No overall differences in safety and efficacy between elderly and younger adult subjects.
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; no dose adjustment needed; consult your doctor.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed; not recommended in severe liver disease; consult your doctor.
Overdose effects
Overdose: General symptomatic and supportive measures; gastric lavage; IV fluids; monitor vital signs.
Storage conditions
Store below 30°C, away from light and moisture; keep out of reach of children.
Chemical structure
Ramelteon