Rozerem

ramelteon

Rozerem

Pharmacologic class: Melatonin receptor agonist

Therapeutic class: Hypnotic

Pregnancy risk category C

Action

Promotes sleep through activity at melatonin MT1 and MT2 receptors, which are thought to be involved in maintaining circadian rhythm underlying normal sleep-wake cycle

Availability

Tablets: 8 mg

Indications and dosages

Insomnia marked by difficulty with sleep onset

Adults: 8 mg P.O. within 30 minutes of going to bed

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:

• sleep apnea, chronic obstructive pulmonary disease, hepatic impairment

• concurrent use of fluvoxamine

• pregnant or breastfeeding patients

• children (safety and efficacy not established).

Administration

• Give within 30 minutes of patient's bedtime.

• Don't give with or immediately after a high-fat meal.

Adverse reactions

CNS: headache, somnolence, fatigue, dizziness, exacerbated insomnia, depression

GI: nausea, diarrhea

Musculoskeletal: myalgia, arthralgia

Respiratory: upper respiratory tract infection

Other: altered taste, influenza

Interactions

Drug-drug. Fluconazole, fluvoxamine, ketoconazole: increased ramelteon blood level

Rifampin: decreased ramelteon efficacy

Drug-diagnostic tests. Blood cortisol: decreased

Drug-food. High-fat meals: altered ramelteon absorption

Drug-herbs. American elder, bishop's weed, cat's claw, devil's claw, eucalyptus, feverfew, ginkgo, kava, licorice, pomegranate: increased ramelteon blood level

Valerian: additive sedation, increased ramelteon blood level

Drug-behaviors. Alcohol use: additive psychomotor impairment

Patient monitoring

• Monitor prolactin and testosterone levels, if ordered, in patient who develops unexplained amenorrhea, galactorrhea, decreased libido, or fertility problems.

• Evaluate patient for physical and psychiatric disorders before and during therapy. Worsening of insomnia or onset of new behavioral or cognitive symptoms could signal underlying psychiatric disorder.

Patient teaching

• Instruct patient to take drug within 30 minutes of going to bed.

• Advise patient not to take drug with or immediately after a high-fat meal.

• Caution patient to avoid driving and other hazardous activities until drug effects are known.

• Advise patient to contact prescriber if insomnia worsens.

• Instruct patient to report menses cessation, excessive or spontaneous lactation, decreased libido, or fertility problems.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, tests, food, herbs, and behaviors mentioned above.

ramelteon

(ra-mel-tee-on) ,

Rozerem

(trade name)

Classification

Therapeutic: sedative hypnotics
Pharmacologic: melatonin receptor agonists
Pregnancy Category: C

Indications

Treatment of insomnia characterized by difficult sleep onset.

Action

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

Therapeutic effects

Easier onset of sleep.

Pharmacokinetics

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 and 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.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POrapid30–90 minunknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity;History of angioedema with previous use;Severe hepatic impairment;Concurrent use of fluvoxamine; Lactation: Lactation; Pediatric: Safety not established.
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; Obstetric: Use only if maternal benefit outweighs fetal risk.

Adverse Reactions/Side Effects

Central nervous system

  • abnormal thinking
  • behavior changes
  • dizziness
  • fatigue
  • hallucinations
  • headache
  • insomnia (worsened)
  • sleep—driving

Gastrointestinal

  • nausea

Endocrinologic

  • ↑ prolactin levels
  • ↓ testosterone levels

Miscellaneous

  • angioedema (life-threatening)

Interactions

Drug-Drug interaction

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.

Route/Dosage

Oral (Adults) 8 mg within 30 min of going to bed.

Availability (generic available)

Tablets: 8 mg

Nursing implications

Nursing assessment

  • Assess sleep patterns before and periodically throughout therapy.

Potential Nursing Diagnoses

 (Indications)
Risk for injury (Side Effects)

Implementation

  • 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.
  • Oral: Administer 30 min prior to going to bed.

Patient/Family Teaching

  • 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.

Evaluation/Desired Outcomes

  • Relief of insomnia.
Mentioned in ?
References in periodicals archive ?
(BSE: 500124) (NSE: DRREDDY) (NYSE: RDY) has launched Ramelteon Tablets, 8 mg, a therapeutically equivalent generic version of Rozerem (ramelteon, 8 mg) Tablets, approved by the US Food and Drug Administration (USFDA), the company said.
Jul 26, 2013: Takeda Pharma Receives FDA Approval for Rozerem 89
According to the company, the generic version of Buprenorphine HCl/Naloxone HCl Sublingual Film's is Suboxone sublingual film; Ethinyl estradiol/Ethonogestrel Vaginal Ring's is NuvaRing; Ezetimibe/Simvastatin Tablets' is Vytorin; Metformin HCl/Saxagliptin ER Tablets' is Kombiglyze XR; Tobramycin Inhalation Solution's is Tobi; Phentermine HCl/Topiramate ER Capsules' is Qsymia; Imiquimod Topical Cream's generic is Zyclara 3.75% Cream and Ramelteon Tablets' is Rozerem.
The latest compound to enter the marketplace is Rozerem, a melatonin agonist receptor.
"Products that don't represent major safety concerns are likely to see a switch." Mahecha expects Japanese pharmaceutical company Takeda's Rozerem to be a likely switch candidate in the sleep aid segment.
An exception is two melatonin antagonists, approved by the Food and Drug Administration, Rozerem and Tasimelteon, strictly used for insomnia (23, 24, 25).
** Ramelteon (Rozerem) is a prescription drug that works differently from the other hypnotic medications used to treat insomnia.
The Z-drugs, along with short-to intermediate-acting benzodiazepines and ramelteon (Rozerem), are first-line options for insomnia, according to American Academy of Sleep Medicine guidelines (J.
The Z-drugs, along with short- to intermediate-acting benzodiazepines and ramelteon (Rozerem), are first-line options for insomnia, according to American Academy of Sleep Medicine guidelines (J.
New medications, including doxepin (Silenor) 3 to 6 mg, Lunesta in tapering doses 3-2-1 mg, Rozerem 8 mg, and Saphris (for anxiety stabilization and sleep effect), are quite useful in stabilizing individuals.
Mainstream prescription drugs for sleep include Ambien, Lunesta, Sonata, and Rozerem. Doxepin (Silenor), a drug that was initially developed to treat depression, was approved by the FDA last year for treatment of insomnia characterized by waking frequently or waking too early and not being able to return to sleep.
When generic Ambien (zolpidem) went off patent, within a fortnight its market share of nonbarbiturate sleep aids fell from 42.4% to 12.5%.7 Unlike Lipitor, however, even as branded Ambien's market share fell dramatically, the market share fell moderately for Rozerem (to 0.9% of the market) and Lunesta (6.7%), and only within several years (Figure 2).(8)