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Zolmitriptan
Systematic (IUPAC) name
(S)-​4-​({3-​[2-​(dimethylamino)​ethyl]-​1H-​indol-​5-​yl}​methyl)-​1,3-​oxazolidin-​2-​one
Identifiers
CAS number 139264-17-8
ATC code N02CC03
PubChem 60857
DrugBank APRD00376
Chemical data
Formula C16H21N3O2 
Mol. mass 287.357 g/mol
Pharmacokinetic data
Bioavailability 40% (oral)
Protein binding 25%
Metabolism Hepatic (CYP1A2-mediated, to active metabolite)
Half life 3 hours
Excretion Renal (65%) and fecal (35%)
Therapeutic considerations
Pregnancy cat. B3(AU) C(US)
Legal status -only (US)
Routes Oral, nasal spray
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Zolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is a triptan, used in the acute treatment of migraine attacks with or without aura and cluster headaches.

Zolmitriptan is marketed by AstraZeneca with the brand names Zomig, Zomigon (Argentina, Canada & Greece), AscoTop (Germany) and Zomigoro (France). In 2008, Zomig generated nearly $154 million in sales.[1]

Contents

Description

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

Indications

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 (Zomig ZMT), which contains aspartame.[2]

Contraindications and precautions

Zolmitriptan should not be given to patients with ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia) 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.

Rarely, serious cardiac events, including myocardial infarction, have been associated with zolmitriptan.

Reported minor adverse reactions include: hypesthesia, paresthesia (all types), warm and cold sensations, chest pain, throat and jaw tightness, dry mouth, dyspepsia, dysphagia, nausea, somnolence, vertigo, asthenia, myalgia, myasthenia and sweating.

Drug Interactions: see Zomig package insert for complete list: [1]

Following administration of cimetidine, the half-life and AUC of zolmitriptan and its active metabolites were approximately doubled (see CLINICAL PHARMACOLOGY in product pamphlet). Cimetidine (INN) (pronounced /sɨˈmɛtɨdiːn/, /saɪˈmɛtɨdiːn/) is a histamine H2-receptor antagonist that inhibits the production of acid in the stomach.

References

  1. ^ "2008 Top 200 generic drugs by retail dollars" PDF (332 KB). Drug Topics (May 26, 2009). Retrieved on August 25, 2009.
  2. ^ Newman LC, Lipton RB (2001). "Migraine MLT-Down: An Unusual Presentation of Migraine in Patients With Aspartame-Triggered Headaches" (abstract). Headache: The Journal of Head and Face Pain 41 (9): 899–901. doi:10.1046/j.1526-4610.2001.01164.x. 

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