Ramelteon (Rozerem) is a potent and selective activator of melatonin (MT-1 and MT2) receptors. It is used in the treatment of patients with insomnia and delirium in ICU patients.

Ramelteon Uses:

• Insomnia:

  • It is indicated for the treatment of insomnia in patients who have difficulty falling asleep.

• Off Label Use of Ramelteon in Adults:

  • For the prevention of ICU-related delirium.

Ramelteon (Rozerem) Dose in Adults

Ramelteon (Rozerem) Dose in the treatment of Insomnia:

• 8 mg orally once a day administered within 30 minutes of bedtime.
• The maximum dose is 8 mg/day.

Ramelteon (Rozerem) Dose in the treatment of ICU-related delirium (off-label):

• 8 mg once a day at bedtime.

Use in Children:

Not indicated.

Pregnancy Risk Category: C

• Animal reproduction studies have shown adverse pregnancy outcomes. It can cause hormonal abnormalities, such as a change of libido or menstrual irregularities.

Use while breastfeeding

• It is unknown if the drug is excreted into breastmilk. It is recommended that breastfeeding mothers use it with caution, weighing both the risks and benefits.
• If breastfeeding is continued, it should be checked for signs of somnolence or feeding problems.
• Alternatively, nursing mothers may be asked to breastfeed their infants for as long as possible.

Dose in Kidney Disease:

No dosage adjustment is necessary.

Dose in Liver disease:

• Mild impairment:
  • There are no dosage adjustments provided in the manufacturer’s labeling.
• Moderate impairment:
  • There are no dosage adjustments provided in the manufacturer’s labeling;
  • It should be used with caution.
• Severe impairment:
  • Avoid using it in severe hepatic impairment.

Side Effects of Ramelteon (Rozerem):

• Central Nervous System:

  • Dizziness
  • Somnolence
  • Fatigue
  • Insomnia Worsened
  • Depression

• Endocrine & Metabolic:

  • Serum Cortisol Decreased

• Gastrointestinal:

  • Nausea
  • Taste Perversion

• Neuromuscular & Skeletal:

  • Myalgia
  • Arthralgia

• Respiratory:

  • Upper Respiratory Infection

• Miscellaneous:

  • Influenza

Contraindications to Ramelteon (Rozerem):

• Patients who have angioedema from previous ramelteon therapy should not be rechallenged.
• Concurrent use with fluvoxamine

Warnings and precautions

• Abnormal thinking and behavior changes:

  • The use of hypnotic or sedative drugs has been linked to abnormal thinking and behavior such as aggression, agitation, decreased inhibition, bizarre behavior and depersonalization.
  • These symptoms may appear suddenly in patients who have not previously been diagnosed with a psychiatric disorder.

• Depression in the CNS:

  • CNS depression can occur, which may lead to impairments in mental and physical abilities. People who are required to be alert for mental tasks, such as driving or operating heavy machinery, should be cautious.

• Hyperprolactinemia

  • It can increase serum prolactin levels. Patients undergoing treatment for prolactin should be viewed carefully to avoid unnecessary investigations or treatment.

• Hypersensitivity reactions

  • Rarely have allergic reactions including angioedema been reported. The drug should be avoided by patients in the future.

• Activities that are sleep-related:

  • It has been linked to dangerous sleep-related activities. It has been reported that individuals have used it to cook, eat, drive, make phone calls, and have sex.
  • Other neuropsychiatric symptoms include anxiety, amnesia, and even anxiety.
  • The risk of developing these conditions may be increased by the use of sedatives or other CNS depressants drugs, such as alcohol, in combination with sedatives.
  • If the patient reports complex sleep-related problems, it is best to stop treatment.

• Depression

  • Patients suffering from depression should be cautious when taking the drug. It should not be used in patients with severe depression.
  • Suicidal thoughts have been linked to the use of hypnotics.

• Hepatic impairment

  • Patients with mild-to-moderate liver disease should use it with caution. It should not be used in severe liver disease.

• Respiratory disease

  • Patients suffering from chronic respiratory conditions like asthma, COPD or sleep Apnea should be cautious about using the drug. The drug should not be used in patients suffering from severe symptoms, such as severe sleep apnea or impending respiratory failure.