Zolmitriptan


Zolmitriptan, sold under the brand name Zomig among others, is a triptan used in the acute treatment of migraine attacks with or without aura and cluster headaches. It is a selective serotonin receptor agonist of the 1B and 1D subtypes.
It was patented in 1990 and approved for medical use in 1997.

Medical uses

Zolmitriptan is used for the acute treatment of migraines with or without aura in adults. Zolmitriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine.
Zolmitriptan is available as a swallowable tablet, an oral disintegrating tablet, and a nasal spray, in doses of 2.5 and 5 mg. People who get migraines from aspartame should not use the disintegrating tablet, which contains aspartame.
According to a study of healthy volunteers, food intake seems to have no significant effect on the effectiveness of Zolmitriptan in both men and women.

Contraindications and precautions

Zolmitriptan should not be given to patients with ischemic heart disease or to patients who have symptoms or findings consistent with ischemic heart disease, coronary artery vasospasm, including Prinzmetal's angina, or other significant underlying cardiovascular disease.
Zolmitriptan may increase blood pressure, it should not be given to patients with uncontrolled hypertension, should not be used within 24 hours of treatment with another 5-HT1 agonist, or an ergotamine-containing or ergot-type medication like dihydroergotamine or methysergide, and should not be administered to patients with hemiplegic or basilar migraine.
Concurrent administration of MAOI or use of zolmitriptan within 2 weeks of discontinuation of MAO-A inhibitor therapy is contraindicated.

Adverse reactions

The Zomig ZMT dissolvable pill contains aspartame, and should be avoided by anyone sensitive to that ingredient and by those suffering from phenylketonuria.
Rarely, serious cardiac events, including myocardial infarction, have been associated with zolmitriptan.
Reported minor adverse reactions include: hypesthesia, paresthesia, warm and cold sensations, chest pain, throat and jaw tightness, dry mouth, dyspepsia, dysphagia, nausea, somnolence, vertigo, asthenia, myalgia, myasthenia and sweating.
Following administration of cimetidine, the half-life and AUC of zolmitriptan and its active metabolites were approximately doubled. Cimetidine is a histamine H2-receptor antagonist that inhibits the production of acid in the stomach.

Chemistry

Zolmitriptan is a synthetic tryptamine derivative and appears as a white powder that is partially soluble in water.

Economics

Brand names

Zolmitriptan is marketed by AstraZeneca with the brand names Zomig, Zomigon, AscoTop and Zomigoro.

Economics

In 2008, Zomig generated nearly $154 million in sales.
AstraZeneca's U.S. patent on Zomig tablets expired on November 14, 2012, and its pediatric exclusivity extension expired on May 14, 2013. The patent in certain European countries has already expired too, and generic drug maker Actavis released a generic version in those countries, starting in March 2012.

Legal status

In Russia versions of zolmitriptan, which are not registered in the National registry of medications, may be regarded as narcotic drugs.