Current understanding on pharmacokinetics, clinical efficacy and safety of progestins for treating pain associated to endometriosis

Fabio Barra, Carolina Scala, Simone Ferrero
Expert opinion on drug metabolism & toxicology · 2018 · vol. 14(4) , pp. 399–415 · doi:10.1080/17425255.2018.1461840 · PMID:29617576 · W2795797649
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This review explores the pharmacokinetics, clinical efficacy, and safety of progestins, including FDA-approved NETA and DMPA, for treating endometriosis-associated pain.

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Abstract

INTRODUCTION: Endometriosis is a chronic estrogen and progestogen responsive inflammatory disease associated with pain symptoms and infertility. The medical therapy of endometriosis aims to induce decidualization within the hormonally dependent ectopic endometrium, and it is often administered to ameliorate women' pain symptoms or to prevent post-surgical disease recurrence. A variety of progestins have been used in monotherapy for the medical management of women with endometriosis. Areas covered: This review aims to offer the reader a complete overview of pharmacokinetic (PK) and clinical efficacy of progestins for the treatment of endometriosis. Expert opinion: Each progestin has a distinct PK parameters and pharmacodynamics affinity not only for progesterone receptor, but also for other steroid receptors, such as estrogen, androgen, and glucocorticoid. Moreover, progestins can also be delivered in different formulations. All these characteristics influence their final biological effect. Randomized, controlled, non-blinded studies support the use of oral progestin-only treatment for pelvic pain associated with endometriosis. Currently, the only two progestins approved by Food and Drug Administration (FDA) for the treatment of endometriosis are norethindrone acetate (NETA) and depot medroxyprogesterone acetate (DMPA).

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Condition tags

endometriosischronic_pelvic_paininfertility

MeSH descriptors

Endometriosis Pelvic Pain Progestins Administration, Oral Endometriosis Endometriosis Endometriosis Female Humans Medroxyprogesterone Acetate Medroxyprogesterone Acetate Norethindrone Norethindrone Norethindrone Norethindrone Acetate Pelvic Pain Pelvic Pain Progestins Progestins Progestins

Citation neighborhood

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

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Cited by (50)

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