Progress in Pharmacokinetics of Progesterone and Its Derivatives

Progesterone is a progestogen drug that has significant protective effect on the endometrium in women. Progesterone and its derivatives have been widely used in various gynecological diseases such as endometrial hyperplasia, dysfunctional uterine bleeding, endometriosis, premenstrual tension syndrome, corpus luteum insufficiency and so on. However, some progesterone derivatives have androgenic activity that may have teratogenic effects, and are limited in the treatment of infertility. Progesterone has no androgenic activity and can be widely used in the field of assisted reproduction. However, long-term treatment is required, and clinical efficacy of different progesterone dosage forms varies greatly. Therefore, clinical treatment largely depends on the choice of route of administration. This article reviews the in vivo pharmacokinetic parameters of progesterone and its derivatives in different dosage forms as well as the effect of the route of administration, dosage and dosing frequency on pharmacokinetics, so as to provide reference for the clinical formulation of a reasonable dosing regimen.