Sutrip Mechanism of Action

Pharmacological Classification: Antimigraine (Selective Serotonin (5HT1) Agonist).
Pharmacology: Mechanism of Actions: Sumatriptan is a selective serotonin agonist that acts at 5-HT1 receptors and produces vasoconstriction of cranial arteries. Drugs like sumatriptan, which are commonly known as triptans, are believed to act mainly at 5-HT1B and 5-HT1D subtype receptors and are therefore sometimes referred to as 5HT1B/1D-receptor agonists.
Pharmacokinetics: Sumatriptan is rapidly but incompletely absorbed when given orally and undergoes first-pass metabolism, resulting in a low absolute bioavailability of about 14%.
Peak plasma concentrations after oral doses are achieved in about 2 hours. Bioavailability is much higher (96%) after subcutaneous doses with peak concentrations occurring within 25 minutes. Bioavailability after intranasal doses is 16% of that achieved subcutaneously, with peak concentrations occurring in about 1.5 hours. Plasma protein binding is low at about 14 to 21%. The elimination half-life of sumatriptan is about 2 hours. Sumatriptan is extensively metabolised in the liver predominantly by monoamine oxidase type A and is excreted mainly in the urine as the inactive indole acetic acid derivative and its glucuronide. Sumatriptan and its metabolites also appear in the faeces. Small amounts of sumatriptan are distributed into breastmilk.