Name: Sumatriptan (Imitrex)
Class: Anti-Migraine (Serotonin Agonist)
Mechanism: Stim 5-HT1D receptors ® cranial vasoconstriction ® resistance in carotid arteriovenous anastomoses and shunts w/minor effects on systemic and coronary artery vasculature.
Absorption: Subcut. (96% bioavailability) ® peak plasma conc. in 5-20 min. Response in 10-30 min; 10-13 hour duration. Oral (14% bioavailability) ® clinical response in 30-60 min.
Dist.:
Metabolism.: 80% Metabolism.
Excretion, t½: 2 hr.
Toxicity/S.E.s: Pain, swelling, redness at injection site. Feeling of heaviness, tightness in chest (injection). Neuro symptoms (tingling, warm/burning sensation). Rare vasospasm in patients w/coronary artery disease (® angina, MI). 34-46% headaches recur in 24-48 hr.
Utility: Partial/complete relief of migraine headache in 80% w/in 2 hr (subcut). Relieves n/v, photophobia, phonophobia.
Special Features: Oral effective, w/few side effects at lowest doses. Expensive.