Zomitan 2.5

Zolmitriptan is a selective 5-hydroxytryptamine (5-HT) 1B/1D receptor agonist of the triptan class, with moderate affinity for 5-HT1A receptors as well. It is available as tablets and nasal spray, and should be taken only after a migraine attack has already begun.

Indicated for the acute treatment of migraines with or without aura in adults. Not used for migraine prevention or to reduce the frequency of attacks.

5-HT Agonists

Selective 5-HT1B/1D receptor agonist (Triptan class)

Migraines are likely due to local cranial vasodilatation and/or the release of sensory neuropeptides through nerve endings in the trigeminal system. The therapeutic activity of Zolmitriptan is thought to be due to agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system, resulting in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

Zolmitriptan binds to and activates 5-HT1B and 5-HT1D receptors located on intracranial blood vessels and perivascular nerve endings of the trigeminal system. This induces vasoconstriction of intracranial blood vessels and inhibits the release of pro-inflammatory neuropeptides such as CGRP, VIP, and substance P from trigeminal nerve endings, reducing pain signal transmission to the brain and relieving migraine symptoms.

Tablet: The recommended starting dose is 2.5 mg. Maximum single dose is 5 mg. If the migraine has not resolved 2 hours after taking the dose, or returns after transient improvement, a second dose may be taken at least 2 hours after the first. Maximum daily dose is 10 mg in any 24-hour period. Nasal Spray: Administer one dose of 5 mg nasal spray for acute migraine. If headache returns, the dose may be repeated after 2 hours. Maximum daily dose should not exceed 10 mg in any 24-hour period. A single 5 mg dose administered into one nostril has been shown effective for acute migraine in adults. Doses lower than 5 mg can only be achieved with the oral formulation; choice of dose and route should be individualized. Safety of treating an average of more than 4 headaches in a 30-day period has not been established.

Take only after a migraine attack has already begun, not as a preventive measure. Tablets should be taken orally with water; food has no significant effect on efficacy. Nasal spray is for nasal use only, administered as one dose into one nostril. If a second dose is needed, wait at least 2 hours between doses.

This medicine is taken as needed when a migraine attack occurs, not on a fixed schedule, so a missed dose situation does not apply. Take as needed without exceeding the maximum daily dose of 10 mg in 24 hours.

The most common adverse reactions were: Neck/throat/jaw pain or pressure Dizziness Paresthesia Asthenia (weakness) Somnolence Warm/cold sensation Nausea Heaviness sensation Dry mouth

There have been rare reports of serious cardiac adverse reactions, including acute myocardial infarction, occurring within a few hours following administration. Sensations of tightness, pain, and pressure may occur in the chest, throat, neck, and jaw after treatment - these are usually not cardiac in origin, but should be evaluated promptly if they occur. Overuse (more than 10 days/month) may lead to medication-overuse headache. Before treating patients with atypical migraine symptoms, exclude other potentially serious neurological conditions. Clearance is reduced in patients with severe renal impairment (CrCl 5-25 mL/min); use with caution. Use with caution and adjusted dosing in moderate to severe hepatic impairment.

Patients with ischemic coronary artery disease Patients with a history of stroke Concurrent or recent use of a monoamine oxidase inhibitor (MAOI) Known hypersensitivity to Zolmitriptan Wolff-Parkinson-White syndrome or arrhythmias associated with cardiac accessory conduction pathway disorders Ischemic or vasospastic arterial disease

MAO inhibitors: Contraindicated - significantly increases zolmitriptan and its active metabolite levels. Cimetidine: Approximately doubles the half-life and AUC of zolmitriptan; dose should be limited (max 2.5 mg/dose, 5 mg/day). Propranolol: Increases Cmax and AUC of zolmitriptan by about 1.5-fold, without significant change in blood pressure or pulse. Other triptans or ergotamine-type drugs: Concomitant use may increase vasospasm risk and should be avoided. SSRIs/SNRIs: May increase the risk of serotonin syndrome.

Food has no significant effect on the bioavailability of zolmitriptan, so it can be taken with or without food.

Pregnancy Category C. Zolmitriptan should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, and only under a physician's advice.

Pregnancy Category: C — always consult a doctor before taking during pregnancy.

It is not known whether Zolmitriptan is excreted in human milk. A decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Not recommended for use in patients under 18 years of age, as safety and effectiveness have not been established in this age group.

No specific dosage adjustment is provided by the manufacturer for elderly patients; however, given the higher relative risk of cardiovascular disease in this population, it should be used with caution and under medical supervision.

Clearance of Zolmitriptan is reduced in patients with severe renal impairment (CrCl 5-25 mL/min); use with caution. In moderate to severe hepatic impairment, zolmitriptan blood levels may increase and some patients have shown significant blood pressure elevation, so the dose should be adjusted and administered with caution.

There is limited clinical experience with acute overdose of Zolmitriptan. Subjects who received single 50 mg oral doses commonly experienced sedation. There is no specific antidote to Zolmitriptan. In cases of severe intoxication, intensive care procedures are recommended, including maintaining a patent airway, ensuring adequate oxygenation and ventilation, and monitoring and supporting the cardiovascular system. The elimination half-life of Zolmitriptan is approximately 3 hours; monitor patients after overdose for at least 15 hours or until symptoms resolve. Seek emergency medical care immediately if overdose is suspected.

Protect from light and moisture, store below 30C. Keep the medicine out of the reach of children.

Chemically, Zolmitriptan is (S)-4-[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]-2-oxazolidinone. Its molecular formula is C16H21N3O2, with a molecular weight of approximately 287.36. It is a white to almost white powder that is readily soluble in water. Zolmitriptan belongs to the triptan class and acts as a selective 5-HT1B/1D receptor agonist.

Q: What is Zolmitriptan used for? A: It is used to relieve an already-started acute migraine attack, with or without aura, in adults. It does not prevent migraines. Q: What is the maximum dose in a day? A: Up to a maximum of 10 mg in 24 hours, with at least 2 hours between doses. Q: Can I take this medicine if I have heart disease? A: No, it is contraindicated in patients with ischemic coronary artery disease or a history of stroke, as it constricts blood vessels. Q: Is Zolmitriptan safe during pregnancy? A: It is Pregnancy Category C. It should not be used during pregnancy without a doctor's advice. Q: Can this medicine be given to children? A: No, safety and effectiveness have not been established in patients under 18 years of age.