Zolmitriptan (zolmitriptan)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Zolmitriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors (''triptan'').
Zolmitriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. Zolmitriptan is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists (e.g., almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan). Because the mechanisms involved in the pathogenesis of migraine are not clearly understood, the precise mechanism of action of 5-HT1 receptor agonists in the management of migraine has yet to be established.
However, current data suggest that 5-HT1 receptor agonists, including zolmitriptan, may ameliorate migraine through selective constriction of certain intracranial blood vessels, inhibition of neuropeptide release, and/or reduced transmission in the trigeminal pain pathway.
Zolmitriptan undergoes hepatic metabolism to form 3 principal metabolites, including N-desmethyl zolmitriptan, which exhibits 5-HT1B/1D potency that is 2-6 times that of the parent drug and which may contribute substantially to the observed effects of zolmitriptan. The other principal metabolites (N-oxide and indole acetic acid derivatives) are inactive. In vitro studies suggest that formation of N-desmethyl zolmitriptan may depend on cytochrome P-450 (CYP) isoenzyme 1A2, while monoamine oxidase-A (MAO-A) appears to be responsible for further metabolism of this metabolite.
Following oral administration of a single dose of radiolabeled zolmitriptan, 65 and 30% of the dose is recovered in urine and feces, respectively, as unchanged drug and metabolites. Approximately 8% of the dose is recovered in urine as unchanged zolmitriptan, while the indole acetic acid, N-oxide, and N-desmethyl metabolites account for about 31, 7, and 4% of the dose recovered in urine, respectively. Zolmitriptan and its active metabolite have elimination half-lives of approximately 3 hours in healthy individuals following oral or intranasal administration.
USES: Zolmitriptan is used to treat migraines. It helps to relieve headache, pain, and other migraine symptoms (including nausea, vomiting, sensitivity to light/sound). Prompt treatment helps you return to your normal routine and may decrease your need for other pain medications.
Zolmitriptan belongs to a class of drugs known as triptans. It affects a certain natural substance (serotonin) that causes narrowing of blood vessels in the brain. It may also relieve pain by affecting certain nerves in the brain.
Zolmitriptan does not prevent future migraines or lessen how often you get migraine attacks.
Generic name: zolmitriptan
Pronunciation: (ZOLE-mi-TRIP-tan)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Zolmitriptan
Indications
The following indications are listed for Zolmitriptan:
- Migraine
Dosing
No dosing information is available for this tab.
No dosing information is available for this tab.
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Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Ischemic heart disease (e.g., angina pectoris, myocardial infarction, silent ischemia), coronary vasospasm (e.g., Prinzmetal variant angina), Wolff-Parkinson-White syndrome or cardiac arrhythmias associated with other accessory pathway conduction disorders, uncontrolled hypertension, other serious underlying cardiovascular disease, history of stroke or transient ischemic attack, peripheral vascular disease, or ischemic bowel disease. Basilar or hemiplegic migraine. Treatment within the previous 24 hours with another 5-HT1 receptor agonist or with an ergot alkaloid (e.g., ergotamine, dihydroergotamine, methysergide (no longer commercially available in the US)). Concurrent or recent (within 2 weeks) treatment with a monoamine oxidase-A (MAO-A) inhibitor. Known hypersensitivity to zolmitriptan or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 2% or more of patients receiving orally administered zolmitriptan and more frequently (by at least 2 percentage points) with zolmitriptan than with placebo include dizziness, paresthesia, neck/throat/jaw/chest symptoms (e.g., pain, tightness, pressure, heaviness), other sensations of heaviness/pressure/tightness, nausea, somnolence, warm or cold sensation, asthenia, dry mouth, dyspepsia, dysphagia, vertigo, and sweating.
Adverse effects occurring in 2% or more of patients receiving intranasal zolmitriptan and more frequently with zolmitriptan than with placebo include paresthesia, hyperesthesia, unusual taste, throat pain, pain of specified location, nausea, somnolence, disorder or discomfort of the nasal cavity, asthenia, tightness of the throat, and dry mouth.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of zolmitriptan have not been established in children younger than 18 years of age. Randomized, placebo-controlled studies in adolescents 12-17 years of age with migraine headaches failed to demonstrate efficacy of the drug. Adverse effects reported in adolescents were similar to those reported in adults. Serious adverse events have been reported during postmarketing experience in a limited number of pediatric patients receiving 5-HT1 receptor agonists, including zolmitriptan. Zolmitriptan has not been studied in children younger than 12 years of age,
Category C. (See Users Guide.)
Zolmitriptan is distributed into milk in rats. It is not known whether zolmitriptan is distributed into milk in humans. A decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Experience in patients 65 years of age and older is insufficient to determine whether they respond differently than younger adults; dosage in geriatric patients should be selected with caution.
Pharmacokinetic profile of zolmitriptan in geriatric patients is similar to that in younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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