Rizatriptan


Description

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

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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... Read more

Mechanism of action

Three distinct pharmacological actions have been implicated in the antimigraine effect of the tripta... Read more

Absorption

Rapid following oral administration. Bioavailability is 45%. Food has no effect on the bioavailabili... 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 excrete... Read more

Toxicity

Symptoms of overdose include dizziness, fainting, heart and blood vessel problems, high blood pressu... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Neurological side effects US
  • adult
  • Kind: experimental
    • Percent: 14-20%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Digestive side effects US
    • adult
  • Kind: experimental
    • Percent: 9-13%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 4-9%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Pain and other pressure sensations US
    • adult
  • Kind: experimental
    • Percent: 6-9%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: 4-8%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Asthenia/fatigue US
    • adult
  • Kind: experimental
    • Percent: 4-7%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 4-6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Paresthesia US
    • adult
  • Kind: experimental
    • Percent: 4-5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Chest pain (tightness, pressure, and/or heaviness) US
    • adult
  • Kind: experimental
    • Percent: <2-3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dry Mouth US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Pain (location unspecified) US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <2%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Pain, tightness, or pressure in the neck/throat/jaw US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Regional pain (tightness, pressure, and/or heaviness) US
    • adult
  • Kind: experimental
    • Percent: <1-2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Warm sensations US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Palpitation US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Hypoesthesia US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Disorientation US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Confusion US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Agitation US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Gait abnormality US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Memory Impairment US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Myalgia US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Muscle Weakness US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Stiffness US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Vertigo US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Muscle cramp/spasm US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Dyspepsia US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Bradycardia US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Cold extremities US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Abdominal distension US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Tongue edema US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Tremor US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Euphoria US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Tachycardia US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Flushing US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Dyspnea US
    • adult
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Attention disturbance US
    • pediatric
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Presyncope US
    • pediatric
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Hallucination US
    • pediatric
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Abdominal Discomfort US
    • pediatric
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Hypoacusis US
    • pediatric
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Abnormal Coordination US
    • pediatric
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Fatigue US
    • pediatric
  • Kind: experimental
    • Percent: >1%
  • Clinical Trial
    Urticaria US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Rash US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Sweating US
    • adult
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial

    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

    Type in a drug name to check for interaction with Rizatriptan

    The risk or severity of adverse effects can be increased when Rizatriptan is combined with (R)-warfarin.
    The risk or severity of adverse effects can be increased when Rizatriptan is combined with (S)-Warfarin.
    The risk or severity of hypertension can be increased when Rizatriptan is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
    The risk or severity of hypertension can be increased when Rizatriptan is combined with 1-benzylimidazole.
    The risk or severity of serotonin syndrome can be increased when Rizatriptan is combined with 2,5-Dimethoxy-4-ethylamphetamine.
    The risk or severity of adverse effects can be increased when Rizatriptan is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The risk or severity of adverse effects can be increased when Rizatriptan is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The risk or severity of adverse effects can be increased when Rizatriptan is combined with 4-hydroxycoumarin.
    The metabolism of Rizatriptan can be decreased when combined with 4-Methoxyamphetamine.
    The risk or severity of adverse effects can be increased when Rizatriptan is combined with 5-methoxy-N,N-dimethyltryptamine.
    The risk or severity of adverse effects can be increased when Rizatriptan is combined with 7-Nitroindazole.
    The metabolism of Rizatriptan can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
    Rizatriptan may decrease the excretion rate of Abacavir which could result in a higher serum level.
    The risk or severity of hypertension can be increased when Rizatriptan is combined with Abediterol.
    Acarbose may decrease the excretion rate of Rizatriptan which could result in a higher serum level.
    Rizatriptan may decrease the antihypertensive activities of Acebutolol.
    Aceclofenac may decrease the excretion rate of Rizatriptan which could result in a higher serum level.
    Acemetacin may decrease the excretion rate of Rizatriptan which could result in a higher serum level.
    The risk or severity of adverse effects can be increased when Rizatriptan is combined with Acenocoumarol.
    The risk or severity of adverse effects can be increased when Rizatriptan is combined with Acepromazine.

    References

    • 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 . Wellington K, Jarvis B: Spotlight on rizatriptan in migraine. CNS Drugs. 2002;16(10):715-20. [PubMed: 12269863]
    • 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 . 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 . 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]

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