Pharmacokinetics, metabolism and serum concentrations of progestins used in contraception

Many different forms of hormonal contraception are used by millions of women worldwide. These contraceptives differ in the dose and type of synthetic progestogenic compound (progestin) used, as well as the route of admin-istration and whether or not they contain estrogenic compounds. There is an increasing awareness that different forms of contraception and different progestins have different side-effect profiles, in particular their cardiovascu-lar effects, effects on reproductive cancers and susceptibility to infectious diseases. There isa need to develop new methods to suit different needs and with minimal risks, especially in under-resourced areas. This requires a better understanding of the pharmacokinetics, metabolism, serum and tissue concentrations of progestins used in con-traception as well as the biological activities of progestins and their metabolites via steroid receptors. Here we review the current knowledge on these topics and identify the research gaps. We show that there is a paucity of research on most of these topics for most progestins. We find that major impediments to clear conclusions on these topics include a lack of standardized methodologies, comparisons between non-parallel clinical studies and variability of data on serum concentrations between and within studies. The latter is most likely due, at least in part, to differences in intrinsic characteristics of participants. The review highlights the importance of insight on these topics in order to provide the best contraceptive options to women with minimal risks. (c) 2020 Elsevier Inc. All rights reserved.

Automated summary

This study discusses the impact of different forms of hormonal contraception and progestins on side effects, reproductive cancers, and susceptibility to infectious diseases. The research highlights the lack of study on progestins used in hormonal contraception and emphasizes the need for greater understanding of these topics.