Pharmacologic profile and clinical efficacy of rizatriptan

Research output: Contribution to journalArticle

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Abstract

Rizatriptan is a recently developed, potent, and selective 5-HT(1B/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 40 000 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.

Original languageEnglish (US)
JournalHeadache
Volume39
Issue number7 SUPPL. 1
StatePublished - 1999

Fingerprint

Headache
Aptitude
Migraine Disorders
rizatriptan
Receptor, Serotonin, 5-HT1D
Pharmacology
Receptor, Serotonin, 5-HT1B
Sumatriptan
Biological Availability
Oral Administration
Therapeutics
Placebos
Recurrence
Pain

Keywords

  • Pharmacokinetics
  • Rizatriptan

ASJC Scopus subject areas

  • Clinical Neurology
  • Neuroscience(all)

Cite this

Pharmacologic profile and clinical efficacy of rizatriptan. / Lipton, Richard B.

In: Headache, Vol. 39, No. 7 SUPPL. 1, 1999.

Research output: Contribution to journalArticle

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abstract = "Rizatriptan is a recently developed, potent, and selective 5-HT(1B/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 40 000 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.",
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