ramelteon


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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.
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References in periodicals archive ?
Reddy's Laboratories Launches Ramelteon Tablets, in the US Market
(27,28) A recent study by Wei Zhou et al was the first of its kind to evaluate the effects of melatonin and a melatonin receptor agonist Ramelteon against Porphyromonas gingivalis.
It also raises the possibility that treatments for sleep disturbances with such agents as Ramelteon may have dual benefits on inflammation as well as sleep [43].
Yeni ajanlarin arasinda primer uykusuzlugun tedavisi icin onaylanan melatonin reseptorlerini hedef alan ramelteon ve dusuk doz doxepin bulunmaktadir.
In addition, this recommendation is classified as "weak," and the associated evidence "low-quality." Medications reviewed included eszopiclone, zaleplon, Zolpidem, orexin receptor antagonist, melatonin, ramelteon, and benzodiazepines.
Ramelteon: This drug binds with melatonin receptors in the brain to promote sleepiness.
US Food and Drug Administration (FDA)-approved hypnotic medications fall into 5 families (TABLE 2(40)): benzodiazepines (BDZs), benzodiazepine agonists (BDZAs, sometimes called "Z drugs"), melatonin agonists (eg, ramelteon), tricyclic antidepressants (eg, low-dose doxepin), and orexin antagonists (eg, suvorexant).
The acquired products include Buprenorphine HCl/Naloxone HCl Sublingual Film, Ethinyl estradiol/Ethonogestrel Vaginal Ring, Ezetimibe/Simvastatin Tablets, Metformin HCl/Saxagliptin ER Tablets, Tobramycin Inhalation Solution, Phentermine HCl/Topiramate ER Capsules, Imiquimod Topical Cream and Ramelteon Tablets.
26% Prescribe ramelteon, 8 mg/d, at bedtime, for insomnia, and refer Ms.
Sparse data on the new hypnotics (eszopiclone, zaleplon, zolpidem, and ramelteon) suggest an increased risk of cancer, which is supported by studies demonstrating a carcinogenic effect in rodents.[sup][22]
Preventive effects of ramelteon on delirium: a randomized placebo-controlled trial.
Ramelteon (Rozerem[C]): a non-selective (MT1/MT2) melatonin receptor agonist,