Frovatriptan: pharmacological differences and clinical results.
Frovatriptan is a 5-HT(1B/1D) agonist demonstrating consistently effective headache relief at a low dose of 2.5 mg. A striking pharmacokinetic characteristic is its long half-life of 25 h. This is balanced by an average Tmax of 2-3 h, a low degree of lipophilicity and a low oral bioavailability of 24-30%. Fifty per cent of the drug is renally excreted and the rest is partially metabolized by P450 CYP 1A2. In three short-term multicentre, double-blind, placebo-controlled phase III trials, the 2 h headache response for 2.5 mg frovatriptan varied from 36 to 46% (placebo 21-27%). The 4 h headache responses were considerably higher--up to 65%. Thirty-five per cent of patients were consistent rapid responders. The recurrence rate was 10-25%. In addition to effective and prolonged relief of head pain, frovatriptan reduced associated migraine symptoms such as nausea, photophobia and phonophobia. There was an excellent tolerability profile with the incidence of adverse events for frovatriptan only slightly higher than placebo. The most commonly reported adverse events for both frovatriptan and placebo were dizziness, nausea, headache and fatigue.
Rapoport
A M
AM
The New England Center for Headache, P.C., Stamford, CT 06902-1251,. nervel@webquill.com
D002227:Carbazoles / Q000494:pharmacology* / Q000627:therapeutic use; D017322:Clinical Trials, Phase II as Topic; D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology* / Q000627:therapeutic use; D014363:Tryptamines
D002227:Carbazoles; D017366:Serotonin Receptor Agonists; D014363:Tryptamines; C108128:frovatriptan