Pharmacokinetics Characteristics of Clomiphene Citrate in Patients with Polycystic Ovary Syndrome (PCOS)

There are no pharmacokinetic data on CC isomers zuclomiphene (Zu) and enclomiphene (En) in patients receiving the drug, mainly women with polycystic ovary disease (PCOS). Thus, the main purpose of this study was to characterize the pharmacokinetics of Zu and En isomers and their intersubject variability, for the first time, in anovular patients with PCOS after a single oral administration of CC. Nine women with infertility and PCOS who referred to the infertility clinic were included in this study. After getting consent of patients and ethical approval from the University ethics committee, they received clomiphene citrate 50 mg on the first day of their menstrual cycle. LH, FSH and prolactin levels were measured before and after medication. Plasma concentrations of Zu and En were measured in the patients from the second day of their menstrual cycle (day 1 of dosing) up to 21 days. The mean (± coefficient of variation) of Cmax, tmax, and AUC of Zu was 15±41 ng/mL, 7±87 h, and 1289±34 ng/mL.h (AUC0-456 h), and that of En was 15±18 ng/mL, 3±68 h, and 65±35 ng/ml.h (AUC0-72 h), respectively. These parameters appeared to be different for Zu from those reported previously in healthy participant; the pharmacokinetic parameters of En in patients with polycystic ovary syndrome were not generally different from the healthy subjects.