Rizatriptan, a Novel 5-HTlB/lD Agonist for Migraine: Single- and Multiple-Dose Tolerability and Pharmacokinetics in Healthy Subjects.

Autor: Goldberg, Michael R., Lee, Yih, Vyas, Kamlesh P., Slaughter, Donald E., Panebianco, Deborah, Ermlich, Susan J., Shadle, Craig R., Brucker, Mary Jo, McLoughlin, Debra A., Olah, Timothy V.
Zdroj: Journal of Clinical Pharmacology; Jan2000, Vol. 40 Issue 1, p74-83, 10p
Abstrakt: Rizatriptan is a novel 5-H1D,1B agonist for relief of migraine headache. The pharmacokinetics, metabolite profiles, and tolerability of rizatriptan were examined in a multiple-dose study in healthy subjects. Rizatriptan (N = 24) (orplacebo, N = 12) was administered as a single 10 mg dose, followed 48 hours later by administration of one 10 mg dose every 2 hours for three doses on 4 consecutive days, corresponding to the maximum daily dose for a migraine attack. The AUC of rizatriptan and its active N-monodesinethyl metabolite after three 10 mg doses was approximately threefold greater than the plasma concentrations following a single 10 mg dose. Metabolite profiles were similar after single and multiple doses. Adverse events during rizatriptan were mild and transient; similar events occurred during placebo, with a somewhat reduced incidence. Diastolic blood pressure tended to increase compared with placebo (-5 mmHg), particularly on the first multiple-dose day (p < .01 vs. placebo). In conclusion, rizatriptan is well tolerated by healthy subjects during multiple-dose administration, with no unexpected accumulation of drug in plasma. [ABSTRACT FROM PUBLISHER]
Databáze: Complementary Index