Name: Methysergide (Sansert)
Class: Anti-Migraine (Serotonin Agonist)
Mechanism: Partial agony at 5-HT2 vascular receptors & partial agonist at a-adrenergic receptors (can act as a blocker) ® vasoconstriction (cerebral vasc. most sensitive), uterine smooth muscle contraction, n/v, diarrhea.
Absorption:
Dist.:
Metabolism.:
Excretion, t½:
Toxicity/S.E.s: Weight gain, peripheral edema, fibrosis (retroperitoneal, pleuropericardial, subendocardial). Concurrent use of ergot alkaloids, b adrenergic blockers, erythromycin, or dopamine ® risk of arterial spasm & occlusion. Occasional central stim. & hallucinations.
Utility: Migraine prevention. Reserved for recurrent, refractory, severe migraine, as fibrosis is assoc. w/prolonged use.
Special Features: Relatively ineffective in treatment of impending/active migraines. Useful as a prophylactic.