Avitriptan (BMS-180048) is a 5-HT1-like receptor agonist for the treatment of
migraine. This double-blind, placebo-controlled, randomized, parallel-group study evaluated the pharmacokinetics, safety, and preliminary efficacy of
avitriptan in patients with
migraine during migrainous and
pain-free states. Patients met the IHS criteria for
migraine with or without
aura and suffered one to six
migraines per month for at least 1 year. Patients in a clinic experiencing a
migraine headache received
avitriptan 75 mg, 150 mg, or 200 mg or matching placebo capsules. Blood samples were obtained before and 0.25, 0.75, 1, 1.5, 2, 2.5, 3, 4, 5, and 6 hours after dosing.
Headache intensity was rated before and up to 6 hours after dosing. Seven to 30 days after the inclinic treatment, patients returned in a
pain-free state for the same study medication. All pharmacokinetic and safety measures were repeated. Forty-eight patients (9 men and 39 women) participated. Peak plasma concentrations of
avitriptan were achieved 1 to 2 hours following dosing in
migraine and
pain-free states for all doses. The pharmacokinetics of
avitriptan were proportional to dose during a
migraine attack over the 75- to 200-mg dose range. The 150- and 200-mg doses of
avitriptan demonstrated a greater decrease in
headache intensity scores at 2 hours postdose. The most common adverse event was
paresthesia. Thus,
avitriptan was rapidly absorbed, well tolerated, and demonstrated preliminary efficacy in this population.