Description

Simple

A medication used to treat insomnia.

Clinical

A melatonin receptor agonist used to treat insomnia.

Overview

Ramelteon is the first in a new class of sleep agents that selectively binds to the melatonin receptors in the suprachiasmatic nucleus (SCN). It is used for insomnia, particularly delayed sleep onset. Ramelteon has not been shown to produce dependence and has shown no potential for abuse.

Pharmacology

Indication

For the treatment of insomnia characterized by difficulty with sleep onset.

Pharmacodynamic

Ramelteon is the first selective melatonin agonist. It works by mimicking melatonin (MT), a naturally occuring hormone that is produced during the sleep period and thought to be responsible for the regulation of circadian rhythm underlying the normal sleep-wake cycle. Ramelteon has a high affinity f... Read more

Mechanism of action

Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors, and lower selectivity for the MT3 receptor. Melatonin production is concurrent with nocturnal sleep, meaning that an increase in melatonin levels is related to the... Read more

Absorption

Rapid, total absorption is at least 84%.

Protein binding

~82% (in human serum)

Volume of distribution

73.6 L

Clearance

Information currently not available.

Half life

~1-2.6 hours

Route of elimination

Following oral administration of radiolabeled ramelteon, 84% of total radioactivity was excreted in urine and approximately 4% in feces, resulting in a mean recovery of 88%.
Less than 0.1% of the dose was excreted in urine and feces as the parent compound.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Regions: US
  • With Drugs Coadmin:
      • Name: Fluvoxamine
      • Drugbank Id: DB00176
  • Regions: US
  • Patient Conditions:
      • Name: Development of angioedema
      • Drugbank Id: DBCOND0108117
  • With Therapies:
      • Name: Upon initiation of drug therapy
      • Drugbank Id: DBCOND0108116
  • Regions: US
  • Patient Conditions:
      • Name: Severe Sleep Apnea
      • Drugbank Id: DBCOND0086432
      • Modification Of:
        • Base:
          • Name: Sleep Apnea
          • Drugbank Id: DBCOND0030087
        • Severity:
          • Includes:
            • severe
  • Regions: US
  • Patient Conditions:
      • Name: Severe Hepatic Impairment
      • Drugbank Id: DBCOND0070791
      • Modification Of:
        • Base:
          • Name: Heptic Impairment
          • Drugbank Id: DBCOND0072269
        • Severity:
          • Includes:
            • severe
  • Regions: US
  • Patient Conditions:
      • Name: Development of complex sleep behaviors
      • Drugbank Id: DBCOND0108118
  • With Therapies:
      • Name: Upon initiation of drug therapy
      • Drugbank Id: DBCOND0108116

Food Interactions

  • Avoid alcohol.
  • Do not take with or immediately after a high-fat meal.

Interactions

Type in a drug name to check for interaction with Ramelteon
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Ramelteon.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Ramelteon.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Ramelteon is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Ramelteon is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Ramelteon is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Ramelteon is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Ramelteon.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Ramelteon is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Ramelteon is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Ramelteon.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Ramelteon.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Ramelteon.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Ramelteon.
Abacavir
Ramelteon may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Ramelteon can be increased when combined with Abatacept.
Abiraterone
The serum concentration of Ramelteon can be increased when it is combined with Abiraterone.
Acarbose
Acarbose may decrease the excretion rate of Ramelteon which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Ramelteon which could result in a higher serum level.
Acefylline
The metabolism of Acefylline can be decreased when combined with Ramelteon.
Acemetacin
Acemetacin may decrease the excretion rate of Ramelteon which could result in a higher serum level.
6 References
  1. 1 . Karim A, Tolbert D, Cao C: Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia. J Clin Pharmacol. 2006 Feb;46(2):140-8.PubMed: 16432265
  2. 2 . Miyamoto M: Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders. CNS Neurosci Ther. 2009 Winter;15(1):32-51. doi: 10.1111/j.1755-5949.2008.00066.x.PubMed: 19228178
  3. 3 . Pandi-Perumal SR, Srinivasan V, Spence DW, Moscovitch A, Hardeland R, Brown GM, Cardinali DP: Ramelteon: a review of its therapeutic potential in sleep disorders. Adv Ther. 2009 Jun;26(6):613-26. doi: 10.1007/s12325-009-0041-6. Epub 2009 Jun 30.PubMed: 19568703
  4. 4 . Borja NL, Daniel KL: Ramelteon for the treatment of insomnia. Clin Ther. 2006 Oct;28(10):1540-55.PubMed: 17157111
  5. 5 . Roth T, Stubbs C, Walsh JK: Ramelteon (TAK-375), a selective MT1/MT2-receptor agonist, reduces latency to persistent sleep in a model of transient insomnia related to a novel sleep environment. Sleep. 2005 Mar;28(3):303-7.PubMed: 16173650
  6. 6 . Simpson D, Curran MP: Ramelteon: a review of its use in insomnia. Drugs. 2008;68(13):1901-19.PubMed: 18729542