Rizatriptan
- Atc Codes:N02CC04
- CAS Codes:145202-66-0#144034-80-0#159776-67-7
- PHARMGKB ID:145202-66-0#144034-80-0#159776-67-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Maxalt; Belgium: Maxalt; Bulgaria: Maxalt; Denmark: Maxalt; Estonia: Maxalt;Finland: Maxalt; France: Maxalt; Germany: Maxalt; Greece: Maxalt; Italy: Maxalt, Rizaliv, Trizadol RPD; Lithuania: Maxalt; Luxembourg: Maxalt; Netherlands: Maxalt, Rizatan, Rizatriptan; Poland: Maxalt; Portugal: Maxalt; Romania: Maxalt; Slovakia: Maxalt, Rizatriptan; Spain: Maxalt; Sweden: Maxalt, Rizatriptan; UK: Maxalt.
North America
Canada: Maxalt; USA: Maxalt.
Latin America
Brazil: Maxalt.
Asia
Japan: Maxalt.
Drug combinations
Chemistry
Rizatriptan Benzoate: C~15~H~19~N~5~ C~7~H~6~O~2~. Mw: 391.47. (1) 1H-Indole-3-ethanamine, N,N-dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-,monobenzoate; (2) 3-[2-(Dimethylamino)ethyl]-5-(1H-1,2,4-triazol-1-ylmethyl)indole monobenzoate. CAS-145202-66-0; CAS-144034-80-0 (rizatriptan)(1996).
Rizatriptan Sulfate: (C~15~H~19~N~5~)~2~ H~2~SO~4~ H~2~O. Mw: 654.78. (1) 1H-Indole-3-ethanamine, N,N-dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-, sulfate (2:1), monohydrate; (2) 3-[2-(Dimethylamino)ethyl]-5-(1H-1,2,4-triazol-1-ylmethyl)indole sulfate (2:1), monohydrate. CAS-159776-67-7 (1996).
Pharmacologic Category
Antimigraine Agents; Selective Serotonin Agonists; Serotonin 5-HT~1B~, 5-HT~1D~ Receptor Agonist. (ATC-Code: N02CC04).
Mechanism of action
Selective agonist for serotonin (5-HT~1D~ receptor) in cranial arteries to cause vasoconstriction and reduce sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine.
Therapeutic use
Acute treatment of migraine with or without aura.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies using rizatriptan in pregnant women. Use only if potential benefit to mother outweighs potential risk to fetus. Decreased weight gain, developmental toxicity and increased mortality in offspring, observed in some animal studies. Teratogenic effects not observed. Excretion in breast milk unknown (use with caution in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to rizatriptan or any component of the formulation. Documented ischemic heart disease or Prinzmetal’s angina. Uncontrolled hypertension. Basilar or hemiplegic migraine. During or within 2 weeks of MAOIs. During or within 24 hours of treatment with another 5-HT~1~ agonist, or ergot-containing or ergot-type medication (e.g. methysergide, dihydroergotamine).
Warnings and precautions
Coronary artery vasospasm, transient ischemia, MI, ventricular tachycardia/fibrillation, cardiac arrest, cerebral/subarachnoid hemorrhage, stroke and death reported with 5-HT~1~ agonist administration. Significant elevation in blood pressure, including hypertensive crisis, also reported on rare occasions in patients with and without history of hypertension. Peripheral vascular ischemia and colonic ischemia reported with 5-HT~1~ agonist. Should not be given in risk factors for CAD without adequate cardiac evaluation. Use with caution in hepatic impairment (drug clearance may be reduced leading to increased plasma concentrations), and in dialysis patients. Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may occur with concomitant proserotonergic drugs (i.e. SSRIs/SNRIs or triptans) or agents which reduce metabolism of rizatriptan. Concurrent use of serotonin precursors (e.g. tryptophan) not recommended. Only indicated for treatment of acute migraine.