Zolmitriptan

What it is and how it works

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-HT1A receptors. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are 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.

Mechanism class: Serotonin 1b Receptor Agonists · Serotonin 1d Receptor Agonists

Indications

is indicated for the acute treatment of migraine with or without aura in adults and pediatric patients 12 years of age and older. Limitations of Use Only use ZOLMITRIPTAN NASAL SPRAY if a clear diagnosis of migraine has been established. If a patient has no response to ZOLMITRIPTAN NASAL SPRAY treatment for the first migraine attack, reconsider the diagnosis of migraine before ZOLMITRIPTAN NASAL SPRAY is administered to treat any subsequent attacks. ZOLMITRIPTAN NASAL SPRAY is not indicated for the prevention of migraine attacks. Safety and effectiveness of ZOLMITRIPTAN NASAL SPRAY have not been established for cluster headache. Not recommended in patients with moderate or severe hepatic impairment .

Dosage and administration (summary)

Recommended starting dose: 2.5 mg Maximum single dose: 5 mg May repeat dose after 2 hours if needed; not to exceed 10 mg in any 24-hour period Dosing Information The recommended starting dose for ZOLMITRIPTAN NASAL SPRAY in adult and pediatric patients 12 years of age and older is 2.5 mg. As the individual response to ZOLMITRIPTAN NASAL SPRAY may vary, the dose should be adjusted on an individual basis. The maximum recommended single dose of ZOLMITRIPTAN NASAL SPRAY is 5 mg. If the migraine has not resolved by 2 hours after taking ZOLMITRIPTAN NASAL SPRAY, or returns after a transient improvement, another dose may be administered at least 2 hours after the previous dose.

Contraindications

Zolmitriptan is 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 Wolff-Parkinson-White Syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders History of stroke, transient ischemic attack (TIA) or history of hemiplegic or basilar migraine because th…

Warnings and precautions

Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina: Perform cardiac evaluation in patients with multiple cardiovascular risk factors Arrhythmias: Discontinue dosing if occurs Chest/throat/neck/jaw pain, tightness, pressure, or heaviness: Generally not associated with myocardial ischemia.

Pregnancy

Pregnancy Risk Summary There are no adequate data on the developmental risk associated with the use of zolmitriptan in pregnant women. In reproductive toxicity studies in rats and rabbits, oral administration of zolmitriptan to pregnant animals resulted in embryolethality and fetal abnormalities (malformations and variations) at clinically relevant…

Storage and supply

The ZOLMITRIPTAN NASAL SPRAY device is a blue-colored plastic device with a gray protection cap, labeled to indicate the nominal dose. Each ZOLMITRIPTAN NASAL SPRAY device administers a single dose of ZOLMITRIPTAN NASAL SPRAY. ZOLMITRIPTAN NASAL SPRAY is supplied as a clear to pale yellow solution of zolmitriptan, buffered to a pH 5.0.

Source: Zolmitriptan (Zolmitriptan) — US FDA prescribing information, 2019-04-30, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.