Pharmacologic profile and clinical efficacy of rizatriptan

Rizatriptan is a recently developed, potent, and selective 5-HT1B/1D receptor agonist, effective in the treatment of acute attacks of migraine. It has a favorable pharmacological profile characterized by a high bioavailability after oral administration (approximately 45%) and rapid absorption (T-max approximately 1 hour). Rizatriptan 10 mg provides rapid and consistent relief of headache. Results of double-blind, placebo-controlled studies indicate that 2 hours after 10 mg of rizatriptan, from 67% to 77% of patients experienced headache relief (grade 3/2 to 1/0) and up to 44% became headache-free (grade 3/2 to 0). Headache recurrence, which occurs in about one third of patients within 24 hours after administration of the initial dose, is effectively treated with a second dose of rizatriptan. Rizatriptan also restores the ability of patients to function normally. In the treatment of multiple attacks, 93% of patients experience headache relief during the first or second attack when treated with 10 mg of rizatriptan. In a direct comparison trial with oral sumatriptan (100 mg), rizatriptan (10 mg) showed an earlier onset of effect and a greater effectiveness in relieving pain at 1 hour, as well as in improving the ability of the patients to function normally. Moreover, investigations on the effects of long-term treatment for up to 1 year carried out in approximately 40000 attacks, show that rizatriptan has a high and consistent response rate as well as a marked superiority over "standard care." Taken together, the data obtained in phase 2 and 3 studies indicate that rizatriptan is a valuable addition to the pharmacological armamentarium for the management of migraine.