Drug information of Ramelteon

Ramelteon


Mechanism of effect

Melatonin receptor agonist with high affinity for MT1 & MT2 receptors.

Pharmacokinetics

Absorption: 84%

Bioavailability: 1.8%

Protein bound: 82%

Extensive first-pass metabolism; mostly by hepatic CYP1A2

Excretion

Urine: 84%

Feces: 4%

Onset of Action:30 minutes

Time to Peak: Median: 0.5 to 1.5 hours

Distribution: 74 L

Drug indications

-Insomnia: Treatment of insomnia characterized by difficulty with sleep onset

-Off Label Uses: Delirium (prevention), ICU related

Dosage

Insomnia: Oral: 8 mg once daily administered within 30 minutes of bedtime. Maximum dose: 8 mg/day.

Delirium (prevention), ICU related (off-label use): 8 mg once daily at bedtime

Drug contraindications

Hypersensitivity

Severe hepatic impairment

Concomitant fluvoxamine

Side effects

Dizziness ,somnolence , fatigue , insomnia worsened , depression ,Serum cortisol decreased, Nausea , taste perversion ,Myalgia , arthralgia ,Upper respiratory infection Influenza ,Anaphylaxis, angioedema, complex sleep-related behavior (sleep-driving, cooking or eating food, making phone calls), prolactin levels increased, testosterone levels decreased

Alcohol, Alizapride, Azelastine (Nasal), Blonanserin, Brexanolone, Brimonidine (Topical), Bromopride, Bromperidol, Buprenorphine, Cannabidiol, Cannabis, Chlormethiazole, Chlorphenesin Carbamate, CNS Depressants, CYP1A2 Inhibitors (Moderate), CYP1A2 Inhibitors (Strong), CYP3A4 Inducers (Strong), CYP3A4 Inhibitors (Strong), Dimethindene (Topical), Doxylamine, Dronabinol, Droperidol, Esketamine, Fluconazole, Flunitrazepam, HYDROcodone, HydrOXYzine, Kava Kava, Lofexidine, Magnesium Sulfate, Melatonin, Methotrimeprazine, MetyroSINE, Minocycline (Systemic), Nabilone, Opioid Agonists, Orphenadrine, Oxomemazine, OxyCODONE, Paraldehyde, Perampanel, Piribedil, Pramipexole, ROPINIRole, Rotigotine, Rufinamide, Selective Serotonin Reuptake Inhibitors, Sodium Oxybate, Suvorexant, Tapentadol, Tetrahydrocannabinol, Tetrahydrocannabinol and Cannabidiol, Thalidomide, Trimeprazine, Zolpidem

Alerts

Moderate hepatic impairment

Concomitant CYP1A2 inhibitors

Potential for cognitive & behavioral changes

May impair ability to drive/perform hazardous tasks

Hyperprolactinemia: May increase prolactin levels.

Hypersensitivity reactions

Depression: Use with caution in patients with depression; worsening of depression, including suicidal ideation has been reported with the use of hypnotics

Respiratory disease: Use with caution in patients with respiratory compromise, COPD or sleep apnea. Use is not recommended in patients with severe sleep apnea (has not been studied).

Points of recommendation

-Appropriate use: Symptomatic treatment of insomnia should be initiated only after careful evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7 to 10 days may indicate psychiatric and/or medical illness.

- Rapid onset: Because of the rapid onset of action, administer immediately prior to bedtime.

-patients must be cautioned about performing tasks, which require mental alertness

 

Pregnancy level

Pregnancy Category: Adverse events were observed in some animal reproduction studies. May cause disturbances of reproductive hormonal regulation (eg, disruption of menses or decreased libido).

Available data from postmarketing reports with use in pregnant women have not identified drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

Breast feeding warning

Lactation: There are no data regarding presence of drug or metabolites in human milk, effects on breastfed infant, or on milk production

Infants exposed to drug through breastmilk should be monitored for somnolence and feeding problems; a lactating woman may consider interrupting breastfeeding and pumping and discarding breast milk during treatment and for 25 hours (approximately 5 elimination half-lives) after drug administration in order to minimize drug exposure to a breastfed infant

Related drugs

Melatonin , Triazolam

Drug forms

Rozerem

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