Zolmitriptan (oral): Difference between revisions
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'''''For patient information about Zolmitriptan, click [[Zolmitriptan (patient information)|here]].''''' | '''''For patient information about Zolmitriptan, click [[Zolmitriptan (patient information)|here]].''''' | ||
{{SB}} | {{SB}} ZOLMIPTRIPTAN | ||
==Overview== | ==Overview== |
Revision as of 03:08, 10 February 2014
Clinical data | |
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Pregnancy category | |
Routes of administration | Oral, nasal spray |
ATC code | |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Bioavailability | 40% (oral) |
Protein binding | 25% |
Elimination half-life | 3 hours |
Excretion | Renal (65%) and fecal (35%) |
Identifiers | |
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CAS Number | |
PubChem CID | |
DrugBank | |
E number | {{#property:P628}} |
ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
Chemical and physical data | |
Formula | C16H21N3O2 |
Molar mass | 287.357 g/mol |
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
For patient information about Zolmitriptan, click here.
Synonyms / Brand Names: ZOLMIPTRIPTAN
Overview
Zolmitriptan is an oral, selective Serotonin receptor agonist, of the serotonin receptor 1B/1D (5-HT1B/1D). It is a second-generation 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 (Greece & Argentina), AscoTop (Germany) and Zomigoro (France). In 2005, AstraZeneca generated $352 million in sales with Zomig.
Category
FDA Package Insert
ZOLMIPTRIPTAN (zolmitriptan) tablet, orally disintegrating
Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages
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 comes in both a swallowable and oral disintegrating tablet. People who get migraines from aspartame should not use the disintegrating tablet (Zomig ZMT), which contains aspartame.
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.
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.
Mechanism of Action
Zolmitriptan is a selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cerebral arteries and trigeminal sensory nerves. It causes vasoconstriction and reduces inflammation associated with antidromic neuronal transmission and has been used in the management of acute migraine attacks.
References
- MacGregor, E.A. (1998). "Zolmitriptan clinical studies". Drugs Today. 34 (12): 1027–1033. doi:10.1358/dot.1998.34.12.487488.
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