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Rizatriptan, a Novel 5‐HT 1B/1D Agonist for Migraine: Single‐ and Multiple‐Dose Tolerability and Pharmacokinetics in Healthy Subjects
Author(s) -
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.
Publication year - 2000
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/009127000004000110
Subject(s) - rizatriptan , tolerability , pharmacokinetics , medicine , placebo , pharmacology , metabolite , active metabolite , migraine , adverse effect , agonist , anesthesia , sumatriptan , receptor , alternative medicine , pathology
Rizatriptan is a novel 5‐HT 1D/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‐monodesmethyl 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 .