Ramelta

Indications

Ramelteon is prescribed for the management of insomnia, particularly when difficulty initiating sleep is the primary issue.
Note: Use this medication as advised by a registered healthcare professional.

Pharmacology

Ramelteon acts as a melatonin receptor agonist, exhibiting high affinity for both the MT1 and MT2 receptors, with a lower affinity for the MT3 receptor. Melatonin naturally increases at night, promoting sleepiness and enhancing the tendency to fall asleep. The MT1 receptors play a key role in regulating sleepiness and facilitating sleep onset, while MT2 receptors help shift the body’s circadian rhythm. Notably, MT3 receptors have a different function and are not involved in the sleep-wake cycle. Ramelteon does not interact with GABA receptors or other neurochemical receptors (such as serotonin, dopamine, norepinephrine, etc.).

Dosage & Administration

• Adult dose: 8 mg, taken 30 minutes before bedtime.
• Avoid taking with or immediately after a high-fat meal.
• Do not exceed 8 mg per day.
  Note: Follow your healthcare provider’s guidance on dosage.

Drug Interactions

• Rifampin (strong CYP enzyme inducer): Reduces the effectiveness of Ramelteon.
• Ketoconazole (strong CYP3A4 inhibitor): May increase the AUC of Ramelteon; caution is advised.
• Fluconazole (CYP2C9 inhibitor): Can increase the systemic exposure of Ramelteon; use cautiously.
• Donepezil and Doxepin: May increase Ramelteon’s systemic exposure; close monitoring is required when combined.
• Alcohol: Can intensify psychomotor impairment; avoid combining with alcohol.

Contraindications

• History of angioedema during previous Ramelteon use.
• Fluvoxamine (strong CYP1A2 inhibitor): Increases the AUC of Ramelteon and should not be used together.

Side Effects

Common side effects (more than 3% of users) include:

• Drowsiness
• Dizziness
• Fatigue
• Nausea
• Worsening insomnia

Pregnancy & Lactation

• Pregnancy: Animal studies suggest potential fetal harm. Only use if the benefits outweigh the risks.
• Breastfeeding: Use cautiously when nursing.

Precautions & Warnings

• Anaphylactic reactions: Includes angioedema and anaphylaxis; avoid re-challenging if such reactions occur.
• Insomnia persistence: If symptoms persist beyond 7-10 days, reassess for other underlying conditions.
• Behavioral changes: May include complex behaviors such as “sleep-driving” and hallucinations. Any new onset behavioral changes should be evaluated immediately.
• Depression: Worsening of depression or suicidal thoughts may occur.
• CNS Effects: May impair alertness and coordination; avoid operating machinery or driving after use.
• Reproductive effects: Can lead to decreased testosterone and elevated prolactin. The impact on the developing human reproductive axis is unknown.
• Severe sleep apnea: Ramelteon is not recommended for patients with severe sleep apnea.

Use in Special Populations

• Pediatric use: Safety and effectiveness have not been established.
• Geriatric use: No significant differences in safety or efficacy between elderly and younger adults.
• Hepatic impairment: Use with caution in moderate liver impairment; not recommended in severe cases.

Therapeutic Class

Miscellaneous sedatives and hypnotics.

Storage Conditions

Store at 25°C, with permitted temperature variations between 15° to 30°C. Keep the container tightly closed and protect from moisture and humidity.