Zolmitriptan

Zolmitriptan is a triptan medication used for the acute treatment of migraines with or without aura in adults. It functions by constricting blood vessels around the brain and reducing substances in the body that can trigger migraine symptoms such as headache, nausea, sensitivity to light and sound, and other symptoms associated with migraine attacks. Zolmitriptan does not prevent future migraines or lessen how often you get migraine attacks.

Medical Uses

Zolmitriptan is indicated for the acute treatment of migraine attacks with or without aura. It is not intended for the prophylactic therapy of migraine or for the management of cluster headaches. The effectiveness of zolmitriptan for the treatment of migraines in adolescents has not been established.

Mechanism of Action

Zolmitriptan works by binding to serotonin (5-HT) receptors in the brain, specifically the 5-HT1B and 5-HT1D receptors. This action leads to vasoconstriction of the intracranial blood vessels and inhibition of pro-inflammatory neuropeptide release, which in turn helps to alleviate migraine symptoms.

Pharmacokinetics

After oral administration, zolmitriptan is well absorbed from the gastrointestinal tract. The bioavailability of zolmitriptan is approximately 40%, and its peak plasma concentrations are reached in about 1-2 hours. Zolmitriptan is metabolized in the liver primarily by the enzyme CYP1A2 to an active metabolite. The elimination half-life of zolmitriptan is about 2.5 to 3 hours. It is excreted primarily in the urine, with a small amount excreted in the feces.

Adverse Effects

Common adverse effects of zolmitriptan include dizziness, drowsiness, dry mouth, and throat or chest discomfort. Less common but more serious side effects may include heart attack, stroke, high blood pressure, and serious allergic reactions. Patients with certain cardiovascular conditions, uncontrolled hypertension, or history of stroke should not use zolmitriptan.

Contraindications

Zolmitriptan is contraindicated in patients with:

• A history of coronary artery disease (CAD), angina, myocardial infarction, or other significant underlying cardiovascular disease.
• Uncontrolled hypertension.
• Hemiplegic or basilar migraine.
• Severe hepatic impairment.
• Known hypersensitivity to zolmitriptan or any of its components.

Drug Interactions

Zolmitriptan can interact with several other medications, including monoamine oxidase inhibitors (MAOIs), other 5-HT1 agonists (other triptans), and selective serotonin reuptake inhibitors (SSRIs). These interactions can increase the risk of serotonin syndrome, a potentially life-threatening condition.

Dosage and Administration

Zolmitriptan is available in oral tablets, orally disintegrating tablets, and nasal spray forms. The recommended dose for adults is 2.5 mg, which can be repeated after 2 hours if the migraine persists. The maximum recommended dose in a 24-hour period is 10 mg.

Conclusion

Zolmitriptan is an effective medication for the acute treatment of migraines. However, it is not suitable for all patients, particularly those with certain cardiovascular conditions or severe hepatic impairment. Patients should discuss their medical history and potential drug interactions with their healthcare provider to ensure zolmitriptan is safe for them.

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  Chemical structure of Zolmitriptan

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  3D model of Zolmitriptan

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  Zolmitriptan