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Rizatriptan: profile and news
Other information Indication For treatment of acute migraine attacks. Pharmacology Rizatriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Rizatriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Rizatriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT1D family) having only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Rizatriptan also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Rizatriptan in humans. Mechanism Of Action Rizatriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction. Drug Category Anti-migraine Agents; Vasoconstrictor Agents; Anti-inflammatory Agents; Selective Serotonin Agonists; ATC:N02CC04 Brand Names/Synonyms CHEMBANK1748; MK-0462; Maxalt; Maxalt-Mlt; Mk 462 Free Base; Risatriptan; Rizatriptan; Rizatriptan Benzoat; Rizatriptan Benzoate Dosage Forms WAFER Absorption 90%, with oral Interactions Interactions for Rizatriptan: Propranolol: Rizatriptan 5 mg should be used in patients taking propranolol, as propranolol has been shown to increase the plasma concentrations of rizatriptan by 70%. Ergot-containing drugs: Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because there is a theoretical basis that these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and rizatriptan within 24 hours is contraindicated. Other 5-HT1 agonists: The administration of rizatriptan with other 5-HT1 agonists has not been evaluated in migraine patients. Because their vasospastic effects may be additive, coadministration of rizatriptan and other 5-HT1 agonists within 24 hours of each other is not recommended. Selective serotonin reuptake inhibitors (SSRIs): SSRIs (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline) have been reported, rarely, to cause weakness, hyperreflexia, and incoordination when coadministered with 5-HT1 agonists. If concomitant treatment with rizatriptan and an SSRI is clinically warranted, appropriate observation of the patient is advised. No clinical or pharmacokinetic interactions were observed when Rizatriptan 10 mg was administered with paroxetine. Monoamine oxidase inhibitors: Rizatriptan should not be administered to patients taking MAO-A inhibitors and non-selective MAO inhibitors; it has been shown that moclobemide (a specific MAO-A inhibitor) increased the systemic exposure of rizatriptan and its metabolite. Drug/Laboratory Test Interactions: Rizatriptan is not known to interfere with commonly employed clinical laboratory tests. Chemical IUPAC Name N,N-dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]-ethanamine Chemical Formula C15H19N5 Half Life 2-3 hours Drug Type Approved Drug # Accession No APRD00008 CAS Registry Number 145202-66-0 |
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