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Zolmitriptan

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Zolmitriptan
Systematic (IUPAC) name
(S)-4-{3-[2-(Dimethylamino) ethyl] indol-5-ylmethyl} oxazolidin-2-on
Identifiers
CAS number 139264-17-8
ATC code N02CC03
PubChem 441240
DrugBank APRD00376
Chemical data
Formula C16H21N3O2
Mol. weight 287.357 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 25%
Metabolism  ?
Half life 3 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Zolmitriptan is an oral, selective 5-hydroxytryptamine 1B/1D (5-HT 1B/1D ) receptor agonist. It is a second-generation triptan, for acute treatment of migraine attacks with or without aura and cluster headaches.

Zolmitriptan is marketed by AstraZeneca with the brand names Zomig, Zomigon (Greece & Argentina) and AscoTop (Germany). In 2005, AstraZeneca generated $352 million in sales with Zomig.

Contents

[edit] Description

Zolmitriptan is a synthetic indole derivative with the empirical formula is C16H21N3O2. Zolmitriptan is a white to almost white powder that is readily soluble in water.

[edit] Indications and Use

For is indicated for the acute treatment of migraine 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.

[edit] 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 variant 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 MAO-A inhibitors or use of zolmitriptan within 2 weeks of discontinuation of MAO-A inhibitor therapy is contraindicated.

[edit] Adverse Reactions

Serious cardiac events, including myocardial infarction have been associated with zolmitriptan. These are, however, rare.

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.

[edit] Full Prescribing Information

Full prescribing information

[edit] References

MacGregor, E.A. (1998). "Zolmitriptan clinical studies". Drugs Today 34 (12): 1027-1033. DOI:10.1358/dot.1998.34.12.487488.


[edit] External links



Triptans (N02CC) edit

Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Sumatriptan, Zolmitriptan

de:Zolmitriptan


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