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Pharmacokinetics and Safety of Oral Eletriptan during Different Phases of the Menstrual Cycle in Healthy Volunteers
Author(s) -
Shah Ajit K.,
LaBoyGoral Ms. Lucia,
Scott Nicholas,
Morse Ms. Theresa,
Apseloff Glen
Publication year - 2001
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 - 10.1177/00912700122012922
Subject(s) - pharmacokinetics , cmax , luteal phase , dosing , medicine , menstrual cycle , adverse effect , follicular phase , elimination rate constant , pharmacology , hormone , volume of distribution
The purpose of this study was to determine the pharmacokinetics and safety of eletriptan in different phases of the menstrual cycle. Female volunteers (n = 16) with a regular menstrual cycle (28 ± 4 days) received a single oral dose of 80 mg eletriptan during each of the four cycle phases: phase 1 (menses), days 1 to 4; phase 2 (follicular), days 6 to 10; phase 3 (ovulatory), days 11 to 13; and phase 4 (luteal), days 21 to 24. Eletriptan plasma concentrations were determined from serial plasma samples taken during a 24‐hour period after dosing. Blood pressure, pulse rate, and ECG measurements were performed at baseline, 1 and 24 hours after dosing. No significant differences between phases were observed for maximum plasma concentration (C max , range of means = 188–234 ng/ml), time to maximum concentration (t msx , range of means = 1.8‐2.5 h), or systemic exposure (area underthe curve [AUC], range of means = 1194–1514 ng·h/ml). Although there was a statistically significant difference in the terminal phase elimination rate constant (k el ) between phases 1and 2 (0.175/h vs. 0.158/h, p = 0.044), the corresponding difference in terminal phase half‐life (t 1/2 ) (4.0 h vs. 4.4 h) was not considered to be clinicallyrelevant. No clinicallyrelevant differences in blood pressure, pulse rate, or ECG were observed, and the incidence, nature, and severity of adverse events were similar in all phases. The different phases of the menstrual cycle had no clinically significant effect on the pharmacokinetics, safety, or tolerability of oral 80 mg eletriptan in healthy females.