ra-MEL-tee-on

• Insomnia characterized by difficult sleep onset.

• Activates melatonin receptors, which promotes maintenance of circadian rhythm, a part of the sleep-wake cycle.

• Easier onset of sleep.

Absorption: Well absorbed (84%), but bioavailability is low (1.8%) due to extensive first pass liver metabolism. Absorption ↑ by a high fat meal.

Distribution: Widely distributed to body tissues.

Metabolism/Excretion: Extensively metabolized by the liver; mainly by CYP1A2 enzyme system. Metabolites are excreted mostly in urine (88%); 4% excreted in feces.

Half-life: 1–2.6 hr.

Contraindicated in:

• Hypersensitivity
• History of angioedema with previous use
• Severe hepatic impairment
• Concurrent use of fluvoxamine.

Use Cautiously in:

• Depression or history of suicidal ideation
• Moderate hepatic impairment
• Concurrent use of CYP3A4 inhibitors, such as ketoconazole
• Concurrent use of CYP2C9 inhibitors, such as fluconazole
• OB: Use during pregnancy only if potential maternal benefit outweighs potential fetal risk.
• Lactation: Use while breastfeeding only if potential maternal benefit outweighs potential risk of somnolence in infant
• Pedi: Safety and effectiveness not established in children.

Endo: ↑prolactin levels, ↓ testosterone levels.

GI: nausea.

Neuro: abnormal thinking, behavior changes, dizziness, fatigue, hallucinations, headache, insomnia (worsened), sleep — driving.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA).

Drug-Drug:

• Blood levels and effects are ↑ by fluvoxamine; concurrent use is contraindicated.
• Levels and effects may be ↓ by rifampin.
• Concurrent use of CYP3A4 inhibitors, such as ketoconazole, may ↑ levels and effects; use cautiously.
• Concurrent use of CYP2C9 inhibitors, such as fluconazole, may ↑ levels and effects; use cautiously.
• Donepezil and doxepin may ↑ levels.
• ↑risk of excessive CNS depression with other CNS depressants including alcohol, benzodiazepines, opioids, and other sedative/hypnotics.

• PO (Adults): 8 mg within 30 min of going to bed.

• Do not confuse Rozerem (ramelteon) with Razadyne (galantamine).
• Do not administer with or immediately after a high-fat meal.
  • Before administering, reduce external stimuli and provide comfort measures to increase effectiveness of medication.
• PO: Administer 30 min prior to going to bed.

Rozerem

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: melatonin receptor agonists

(Generic available)

• Tablets: 8 mg;

(blood levels)

• Assess sleep patterns before and periodically throughout therapy.

• (Indications).
• Risk for injury (Side Effects).

• Instruct patient to take ramelteon as directed, within 30 min of going to bed and to confine activities to those necessary to prepare for bed. Instruct patient to read the Medication Guide before starting and with each Rx refill; changes may occur.
• Causes drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
• Caution patient that complex sleep-related behaviors (sleep-driving, making phone calls, preparing and eating food, having sex, sleep walking) may occur while asleep. Inform patient to notify health care professional if sleep-related behaviors (may include sleep-driving — driving while not fully awake after ingestion of a sedative-hypnotic product, with no memory of the event) occur.
• Advise patient to notify health care professional immediately if signs of anaphylaxis (swelling of the tongue or throat, trouble breathing, and nausea and vomiting) or angioedema (severe facial swelling) occur; may occur as early as the first time the product is taken.
• Caution patient to avoid concurrent use of alcohol or other CNS depressants.
• Advise female patients to notify health care professional if pregnancy is planned or suspected or if breast feeding.

• Relief of insomnia.

NDC Code^*

• 0591- Actavis Pharma, Inc.
  • 0591-2191- Ramelteon
    • 0591-2191-01- 100 TABLET in 1 BOTTLE (0591-2191-01)

• 0591- Actavis Pharma, Inc.
  • 0591-2191- Ramelteon
    • 0591-2191-30- 30 TABLET in 1 BOTTLE (0591-2191-30)

• 43598- Dr.Reddys Laboratories Inc
  • 43598-741- Ramelteon
    • 43598-741-01- 100 TABLET in 1 BOTTLE (43598-741-01)

• 43598- Dr.Reddys Laboratories Inc
  • 43598-741- Ramelteon
    • 43598-741-10- 1000 TABLET in 1 BOTTLE (43598-741-10)

• 43598- Dr.Reddys Laboratories Inc
  • 43598-741- Ramelteon
    • 43598-741-30- 30 TABLET in 1 BOTTLE (43598-741-30)

• 63629- Bryant Ranch Prepack
  • 63629-8264- Ramelteon
    • 63629-8264-1- 30 TABLET in 1 BOTTLE (63629-8264-1)

• 64764- Takeda Pharmaceuticals America, Inc.
  • 64764-805- Rozerem
    • 64764-805-10- 100 TABLET, FILM COATED in 1 BOTTLE (64764-805-10)

• 64764- Takeda Pharmaceuticals America, Inc.
  • 64764-805- Rozerem
    • 64764-805-22- 6 CARTON in 1 TRAY (64764-805-22) > 1 BLISTER PACK in 1 CARTON > 2 TABLET, FILM COATED in 1 BLISTER PACK

• 64764- Takeda Pharmaceuticals America, Inc.
  • 64764-805- Rozerem
    • 64764-805-30- 30 TABLET, FILM COATED in 1 BOTTLE (64764-805-30)

• 70710- Zydus Pharmaceuticals (USA) Inc.
  • 70710-1344- Ramelteon
    • 70710-1344-1- 100 TABLET in 1 BOTTLE (70710-1344-1)

• 70710- Zydus Pharmaceuticals (USA) Inc.
  • 70710-1344- Ramelteon
    • 70710-1344-3- 30 TABLET in 1 BOTTLE (70710-1344-3)

• 70710- Zydus Pharmaceuticals (USA) Inc.
  • 70710-1344- Ramelteon
    • 70710-1344-5- 500 TABLET in 1 BOTTLE (70710-1344-5)

• 70771- Cadila Healthcare Limited
  • 70771-1495- Ramelteon
    • 70771-1495-1- 100 TABLET in 1 BOTTLE (70771-1495-1)

• 70771- Cadila Healthcare Limited
  • 70771-1495- Ramelteon
    • 70771-1495-3- 30 TABLET in 1 BOTTLE (70771-1495-3)

• 70771- Cadila Healthcare Limited
  • 70771-1495- Ramelteon
    • 70771-1495-5- 500 TABLET in 1 BOTTLE (70771-1495-5)