Drug information of Zolmitriptan

Zolmitriptan

Drug group:

Zolmitriptan is a headache medicine that narrows blood vessels around the brain. Zolmitriptan also reduces substances in the body that can trigger headache pain, nausea, sensitivity to light and sound, and other migraine symptoms.
Zolmitriptan is used to treat migraine headaches. Zolmitriptan will only treat a headache that has already begun. It will not prevent headaches or reduce the number of attacks.

Mechanism of effect

The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

Pharmacodynamic

Zolmitriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors

Pharmacokinetics

Zolmitriptan is well absorbed after oral administrationMean absolute oral bioavailability is approximately 40%. Food has no affect on the rate and extent of absorption. Protein binding: 25%. Metabolism: Hepatic. The mean elimination half-life of zolmitriptan and of the active N-desmethyl metabolite is 3 hours. Total radioactivity recovered in urine and feces was 65% and 30% of the administered dose, respectively. About 8% of the dose was recovered in the urine as unchanged Zolmitriptan

Dosage

Usual Adult Dose for Migraine Oral:
-Initial dose: 1.25 or 2.5 mg orally once (may break the scored 2.5 mg tablet in half to obtain 1.25 mg dose); may repeat in 2 hours if migraine has not resolved or returns after a transient improvement
-Maintenance Dose: Adjust dose based on individual response
Maximum single dose: 5 mg Maximum daily dose: 10 mg in a 24-hour period

Alerts

Overuse of acute migraine drugs (e.g. ergotamine, triptans, opioids, or a combination of drugs for 10 or more days per month) may lead to exacerbation of headache (medication overuse headache).

Points of recommendation

1- Take Zolmitriptan exactly as your doctor tells you to take it.
2- If your headache comes back after your first dose, you may take a second dose anytime after 2 hours of taking the first dose.
For any attack where the first dose did not work, do not take a second dose without talking with your doctor. Do not take more than a total of 10 mg of Zolmitriptan tablets (tablets or spray combined) in any 24 hour period.

Pregnancy level

C

Related drugs

Rizatriptan , Almotriptan , eletriptan


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