Pharmacology of Progestogens

Journal für Reproduktionsmedizin und Endokrinologie - Journal of Reproductive Medicine and Endocrinology 2011; 8 (Sonderheft 1): 157-177

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Keywords: pharmacodynamics,  pharmacokinetics,  progestogens

This review comprises the pharmacokinetics and pharmacodynamics of natural and synthetic progestogens used in contraception and therapy. The paper describes the historic development of progestogens, their mechanisms of action, the relation between structure and hormonal activity, differences in hormonal pattern and potency, peculiarities in the properties of certain compounds, tissue-specific effects, and metabolism. The influence of the route of administration on pharmacokinetics, hormonal activity and metabolism is discussed. The various types of progestogens including tibolone, their receptor interaction, hormonal pattern and the hormonal activity of certain metabolites are described in detail. The structural formula, serum concentrations, binding affinities to steroid receptors and serum binding globulins, and the relative potencies of the available progestins are presented. The different pathways of aromatization of natural androgens as compared to that of norethisterone and tibolone are discussed. Differences in the tissue-specific effects of the various compounds and regimens and their potential implications with the risks and benefits of treatment are described.