Zolmitriptan

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Zomig, Zolmitriptan; Belgium: Zomig; Czech Republic: Zolmiles, Zolmitriptan, Zomig; Denmark: Zomig; Estonia: Zolmitriptan, Zomig; Finland: Zomig; France: Zomig, Zomigoro; Germany: Ascotop, Ozolmotan, Zolmitriptan, Zomig, Zomigoro; Greece: Zolmitriptan, Zomigon; Hungary: Zomig; Ireland: Zolmiles, Zomig; Italy: Zomig; Latvia: Zolmitriptan, Zomig; Lithuania: Zolmitriptan, Zomig; Luxembourg: Zomig; Netherlands: Zomig; Poland: Zolmitriptan, Zomig; Portugal: Zolmitriptano, Zomig; Romania: Zolmitriptan; Slovakia: Zomig; Slovenia: Zomig; Spain: Zomig; Sweden: Zolmitriptan, Zomigon, Zomigoro; UK: Zomig.

North America

Canada: Zomig; USA: Zomig.

Latin America

Argentina: Zomigón; Brazil: Zomig; Mexico: Zomig.

Asia

Japan: Zomig.

Drug combinations

Chemistry

Zolmitriptan: C~16~H~21~N~3~O~2~. Mw: 287.36. (1) 2-Oxazolidinone, 4-[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]-, (S)-; (2)(S)-4-[[3-[2-(Dimethylamino)ethyl]indol-5-yl]methyl]-2-oxazolidinone. CAS-139264-17-8 (1997).

Pharmacologic Category

Antimigraine Agents; Selective Serotonin Agonists. Serotonin 5-HT~1B~, 5-HT~1D~ Receptor Agonist. (ATC-Code: N02CC03).

Mechanism of action

Selective agonist for serotonin (5-HT~1B~ and 5-HT~1D~ receptors) 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 zolmitriptan in pregnant women. Use only if potential benefit to mother outweighs potential risk to fetus. In animal studies, administration associated with embryolethality, fetal abnormalities, and pup mortality. Excretion in breast milk unknown (use caution during lactation).

Unlabeled use

Contraindications

Hypersensitivity to zolmitriptan or any component of the formulation. Ischemic heart disease or vasospastic coronary artery disease, including Prinzmetal’s angina. Uncontrolled hypertension. Symptomatic Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders. Use with ergotamine derivatives (within 24 hours of same). Use within 24 hours of another 5-HT~1~ agonist. Concurrent administration or within 2 weeks of discontinuing an MAOI. Management of hemiplegic or basilar migraine. Additional contraindications with nasal spray: Cerebrovascular syndromes (e.g. stroke, TIA), peripheral vascular disease (including ischemic bowel disease).

Warnings and precautions

Not recommended if patient has risk factors for heart disease (high blood pressure, high cholesterol, obesity, diabetes, smoking, strong family history of heart disease, postmenopausal woman, or male >40 years of age). Cerebral/subarachnoid hemorrhage and stroke reported with 5-HT~1~ agonist administration. Nasal spray contraindicated in cerebrovascular syndromes. Elevated blood pressure reported on rare occasions with and without history of hypertension. Peripheral vascular ischemia and colonic ischemia reported with 5-HT~1~ agonists. Rarely, partial vision loss and blindness (transient and permanent) reported with 5-HT~1~ agonists. Should not be given to patients who have risk factors for CAD (e.g. hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, menopause, male >40 years of age) without adequate cardiac evaluation. Use with caution in hepatic impairment (drug clearance may be reduced leading to increased plasma concentrations). Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may occur with concomitant proserotonergic drugs (e.g. SSRIs/SNRIs or triptans) or agents which reduce metabolism of zolmitriptan. Concurrent use of serotonin precursors not recommended. Some products (tablets) contain phenylalanine. Only indicated for treatment of acute migraine. Not intended to prevent or reduce number of migraine attacks.

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