Zolmitriptan is a medication commonly used in the treatment of migraines. Here's an overview of its pharmacology, indications, and dosage and administration:
Pharmacology:
Mechanism of Action: Zolmitriptan binds to serotonin 5-HT 1B/1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system. This action results in cranial vessel constriction and the inhibition of pro-inflammatory neuropeptide release. These effects help alleviate the symptoms of a migraine attack.
Absorption: Zolmitriptan is well absorbed when taken orally (PO).
Peak Plasma Levels: Peak plasma levels are typically reached at around 2 hours after oral administration.
Elimination: The elimination half-life (t1/2) of both zolmitriptan and its active metabolite is approximately 3 hours.
Excretion: Zolmitriptan and its metabolites are excreted in the feces and urine.
Indications:
Zolmitriptan is indicated for the acute treatment of migraines, both with or without an aura. It is not intended for the prophylactic (preventative) treatment of migraines.
Dosage and Administration:
The recommended dosage of Zolmitriptan for the treatment of a migraine attack is 2.5 mg. If the symptoms persist or return within 24 hours, a second dose of 2.5 mg has been shown to be effective. If a second dose is needed, it should not be taken within 2 hours of the initial dose.
For patients who do not achieve satisfactory relief with 2.5 mg doses, subsequent migraine attacks can be treated with 5 mg doses of Zolmitriptan. Significant efficacy is typically apparent within 1 hour of dosing. Zolmitriptan can be effective whenever taken during a migraine attack, but it is advisable to take it as early as possible after the onset of a migraine headache.
In the event of recurrent attacks, it is recommended that the total intake of Zolmitriptan in a 24-hour period should not exceed 15 mg.
Special Populations:
Use in Children: The safety and efficacy of Zolmitriptan in pediatric patients have not been established.
Use in Patients Aged Over 65 Years: Safety and efficacy in individuals aged over 65 years have not been systematically evaluated.
Patients with Hepatic Impairment: There is no clinical or pharmacokinetic experience in patients with hepatic impairment treated with Zolmitriptan. Therefore, caution may be necessary in such cases.
It's important to use Zolmitriptan as directed by a healthcare professional and to discuss any concerns or potential contraindications with your healthcare provider. This information is based on my knowledge up to September 2021, and there may have been updates or changes in recommendations since then.
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