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APIs of Zolmitriptan

  • Author:Ray Dean
  • Source:www.oceanchinachem.com
  • Release on :2016-11-13

Zolmitriptan is a selective 5-HTIB / ID receptor agonist. By stimulating intracranial blood vessels (including arteriovenous anastomosis) and the sympathetic nervous system on the 5-HTIB / ID receptor, causing intracranial vasoconstriction and inhibition of pre-inflammatory neuropeptide release. For the treatment of adult or non-aura migraine. Zolmitriptan absorbed rapidly after oral administration. 1 hour peak plasma concentration of up to 75%, followed by plasma concentration of 4 to 6 hours. The average absolute bioavailability of the parent compound was about 40%.

 

Zolmitriptan mainly through the liver biotransformation, and metabolites excreted from the urine. The three main metabolites are: indoleacetic acid (the main metabolite in plasma and urine), N-oxide and N-demethyl metabolite. N-demethyl metabolites are active and other metabolites are inactive. The plasma concentration of the N-demethyl metabolite is approximately half that of the parent drug; therefore, it is expected to contribute to the therapeutic effect of this product. More than 60% of the oral single dose is excreted in the urine (mainly indoleacetic acid metabolites), and about 30% of the parent compound by the prototype excreted by feces. The renal clearance rate of this product is greater than the glomerular filtration rate, suggesting the presence of renal tubular secretion.

 

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