Zolmitriptan (3 brand names, 3 dosage forms, 2 routes)
Available dosage forms: TABLET, SPRAY, TABLET, ORALLY DISINTEGRATING.
Routes of administration: ORAL, NASAL.
Brand Names
- ZOLMITRIPTAN
- ZOMIG
- ZOMIG-ZMT
Indications and Usage
Zolmitriptan tablets are indicated for the acute treatment of migraine with or without aura in adults. Limitations of Use Only use zolmitriptan tablets if a clear diagnosis of migraine has been established. If a patient has no response to zolmitriptan tablets treatment for the first migraine attack, reconsider the diagnosis of migraine before zolmitriptan tablets are administered to treat any subsequent attacks. Zolmitriptan tablets are not indicated for the prevention of migraine attacks. Safety and effectiveness of zolmitriptan tablets have not been established for cluster headache.
Contraindications
Zolmitriptan tablets are contraindicated in patients with: Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), other significant underlying cardiovascular disease, or coronary artery vasospasm including Prinzmetal’s angina [see Warnings and Precautions ( 5.1) ] Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see Warnings and Precautions ( 5.2) ] History of stroke, transient ischemic attack (TIA), or history of hemiplegic or basilar migraine because these patients are at a higher risk of stroke [see Warnings and Precautions ( 5.4) ] Peripheral vascular disease (PVD) [see Warnings and Precautions ( 5.5) ] Ischemic bowel disease [see Warnings and Precautions ( 5.5) ] Uncontrolled hypertension [see Warnings and Precautions ( 5.8) ] Recent use (i.e., within 24 hours) of another 5-HT 1agonist, ergotamine-containing medication, or ergot-type medication (such as dihydroergotamine or methysergide) [see Drug Interactions ( 7.1, 7.3) ] Concurrent administration of a monoamine oxidase (MAO)-A inhibitor or recent use of a MAO-A inhibitor (that is within 2 weeks) [see Drug Interactions ( 7.2) and Clinical Pharmacology ( 12.3) ] Known hypersensitivity to zolmitriptan tablets (angioedema and anaphylaxis seen) [see Adverse Reactions ( 6.2) ]
Adverse Reactions
The following adverse reactions are described elsewhere in other sections of the prescribing information: Myocardial Ischemia, Myocardial Infarction, and Prinzmetal Angina [see Warnings and Precautions ( 5.1) ]. Arrhythmias [ see Warnings and Precautions ( 5.2) ]. Chest and or Throat, Neck and Jaw Pain/Tightness/Pressure [see Warnings and Precautions ( 5.3) ]. Cerebrovascular Events [see Warnings and Precautions ( 5.4) ]. Other Vasospasm Reactions [see Warnings and Precautions ( 5.5) ]. Medication Overuse Headache [see Warnings and Precautions ( 5.6) ]. Serotonin Syndrome [see Warnings and Precautions ( 5.7) ]. Increase in Blood Pressure [see Warnings and Precautions ( 5.8) ].
Mechanism of Action
Zolmitriptan binds with high affinity to human recombinant 5-HT 1D and 5-HT 1B receptors, and moderate affinity for 5-HT 1A receptors. The N-desmethyl metabolite also has high affinity for 5-HT 1B/1D and moderate affinity for 5-HT 1A receptors. Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT 1B/1Dreceptors on intracranial blood vessels (including the arteriovenous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
Overdosage
There is no experience with acute overdose of zolmitriptan. Clinical study subjects who received single 50 mg oral doses of zolmitriptan commonly experienced sedation. There is no specific antidote to zolmitriptan. In cases of severe intoxication, intensive care procedures are recommended, including establishing and maintaining a patent airway, ensuring adequate oxygenation and ventilation, and monitoring and support of the cardiovascular system. The elimination half-life of zolmitriptan is 3 hours [see Clinical Pharmacology ( 12.1) ]; therefore, monitor patients after overdose with zolmitriptan for at least 15 hours or until symptoms or signs resolve. It is unknown what effect hemodialysis or peritoneal dialysis has on the plasma concentrations of zolmitriptan.