Description

Simple

A medication used to treat migraines.

Clinical

A 5-HT1B/1D receptor agonist used to treat migraines.

Overview

Rizatriptan is a triptan drug used for the treatment of migraine headaches. It is a selective 5-hydroxytryptamine1 receptor subtype agonist.

Pharmacology

Indication

For treatment of acute migraine attacks with or without aura.

Pharmacodynamic

Rizatriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists and has only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors... Read more

Mechanism of action

Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D recept... Read more

Absorption

Rapid following oral administration. Bioavailability is 45%. Food has no effect on the bioavailability of rizatriptan. However, administering rizatriptan with food will delay by 1 hour the time to reach peak plasma concentration. The rate of absorption is not affected by the presence of a migraine a... Read more

Protein binding

14%

Volume of distribution

140 L [male]110 L [female]

Clearance

Information currently not available.

Half life

2-3 hours

Route of elimination

Approximately 14% of an oral dose is excreted in urine as unchanged rizatriptan while 51% is excreted as indole acetic acid metabolite, indicating substantial first pass metabolism.

Toxicity

Symptoms of overdose include dizziness, fainting, heart and blood vessel problems, high blood pressure, loss of bowel and bladder control, slow heartbeat, and vomiting.

Adverse Effects

Contraindications

  • Time Period: within 24 hours
  • Regions: US
  • With Categories Coadmin:
      • Name: Selective Serotonin 5-HT1 Receptor Agonists
      • Drugbank Id: DBCAT002224
  • Time Period: within 24 hours
  • Regions: US
  • With Categories Coadmin:
      • Name: Ergot Alkaloids and Derivatives
      • Drugbank Id: DBCAT000606
      • Mesh Id: D004876

Food Interactions

    Information currently not available.

Interactions

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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 risk or severity of adverse effects can be increased when Rizatriptan is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of adverse effects can be increased when Rizatriptan is combined with (S)-Warfarin.
1-benzylimidazole
The risk or severity of hypertension can be increased when Rizatriptan is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when Rizatriptan is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Rizatriptan is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Rizatriptan is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
The risk or severity of adverse effects can be increased when Rizatriptan is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The metabolism of Rizatriptan can be decreased when combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Rizatriptan is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Rizatriptan is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The metabolism of Rizatriptan can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Abacavir
Rizatriptan may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abediterol
The risk or severity of hypertension can be increased when Rizatriptan is combined with Abediterol.
Acarbose
Acarbose may decrease the excretion rate of Rizatriptan which could result in a higher serum level.
Acebutolol
Rizatriptan may decrease the antihypertensive activities of Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Rizatriptan which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Rizatriptan which could result in a higher serum level.
Acenocoumarol
The risk or severity of adverse effects can be increased when Rizatriptan is combined with Acenocoumarol.
Acepromazine
The risk or severity of adverse effects can be increased when Rizatriptan is combined with Acepromazine.
Aceprometazine
The risk or severity of adverse effects can be increased when Rizatriptan is combined with Aceprometazine.
5 References
  1. 1 . Wellington K, Plosker GL: Rizatriptan: an update of its use in the management of migraine. Drugs. 2002;62(10):1539-74.PubMed: 12093318
  2. 2 . Wellington K, Jarvis B: Spotlight on rizatriptan in migraine. CNS Drugs. 2002;16(10):715-20.PubMed: 12269863
  3. 3 . Ikemoto F, Toru T, Aijima H, Natsumeda Y: [Rizatriptan (Maxalt), a new entity of triptan for migraine: pharmacology and therapeutic relevance]. Nihon Yakurigaku Zasshi. 2004 Apr;123(4):295-302.PubMed: 15056946
  4. 4 . Villalon CM, Centurion D, Valdivia LF, De Vries P, Saxena PR: An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.PubMed: 12434581
  5. 5 . Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87.PubMed: 11152011