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

Barra, Fabio; Scala, Carolina; Ferrero, Simone

doi:10.1080/17425255.2018.1461840

Cited by 67 publications

(44 citation statements)

References 120 publications

(109 reference statements)

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“…28 Locally, they have been shown to inhibit inflammatory pathways, inhibit angiogenesis, and suppress expression of matrix metalloproteinases, which may also contribute to the growth of endometriotic lesions. 29 Progestins are available in various formulations and are used both alone and in combination with estrogen for treatment of endometriosis-related pain. Progestin monotherapy has been shown to be effective and well tolerated 29,30 and have a decreased risk of thromboembolism compared with CHCs with fewer medical contraindications.…”

Section: Progestinsmentioning

confidence: 99%

“…29 Progestins are available in various formulations and are used both alone and in combination with estrogen for treatment of endometriosis-related pain. Progestin monotherapy has been shown to be effective and well tolerated 29,30 and have a decreased risk of thromboembolism compared with CHCs with fewer medical contraindications. Only norethindrone acetate and depot medroxyprogesterone acetate (DMPA) have been approved by the FDA for use as monotherapy in the treatment of endometriosis.…”

Section: Progestinsmentioning

confidence: 99%

“…Only norethindrone acetate and depot medroxyprogesterone acetate (DMPA) have been approved by the FDA for use as monotherapy in the treatment of endometriosis. 29 The most frequently reported adverse effects of progestins include breakthrough bleeding or spotting, weight gain, breast tenderness, and depression. 31 Each progestin exhibits distinct pharmacokinetics; different affinities for progesterone, estrogen, androgen, and glucocorticoid receptors; and distinct biological activity.…”

Section: Progestinsmentioning

confidence: 99%

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Endometriosis and Female Pelvic Pain

Kim

Han

2018

Semin Reprod Med

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Endometriosis is a nonmalignant gynecologic disorder that can have a significant impact on a woman's quality of life with pelvic pain and possible lasting effects on one's fertility. Symptoms, when present, can be severe and affect many organ systems including the gastrointestinal and urinary systems. Other etiologies of pelvic pain must be ruled out and/or need to be addressed concurrently for optimal patient care. There are numerous medical and surgical treatment options available that have been shown to be beneficial for endometriosis-related pelvic pain. Recurrence is common when medications are discontinued and even after surgical therapy. Ultimately, the treatment approach will be dependent on the needs of the patient, taking into consideration the patient's desire for fertility, symptoms, past treatment, and patient preferences.

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Section: Progestinsmentioning

confidence: 99%

Section: Progestinsmentioning

confidence: 99%

Section: Progestinsmentioning

confidence: 99%

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Endometriosis and Female Pelvic Pain

Kim

Han

2018

Semin Reprod Med

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“…Dienogest binds to the progesterone receptor and, when taken continuously, inhibits systemic gonadotropin secretion and has local antiproliferative and anti-inflammatory effects on endometriotic lesions 17,[21][22][23] . These antiproliferative and antiangiogenic properties of the compound differentiate dienogest from other progestins in the same class 20,23 .…”

Section: Introductionmentioning

confidence: 98%

“…Progestins are recommended as a first-line hormonal therapy for the treatment of endometriosis-related pain and may compare favorably with other treatment options 16 . Dienogest 2 mg daily is a fourthgeneration progestin that first received approval for the treatment of endometriosis in the European Union in 2009 [17][18][19][20] . Dienogest binds to the progesterone receptor and, when taken continuously, inhibits systemic gonadotropin secretion and has local antiproliferative and anti-inflammatory effects on endometriotic lesions 17,[21][22][23] .…”

Section: Introductionmentioning

confidence: 99%

Use of dienogest in endometriosis: a narrative literature review and expert commentary

Murji

Biberoğlu²,

Leng

et al. 2020

Current Medical Research and Opinion

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Objective: Endometriosis affects up to 10% of women of reproductive age, and the main goal of treatment is to relieve symptoms. Progestins have been the mainstay of endometriosis suppression, of which dienogest has become an important option in many parts of the world. This is an expert literature review, with recommendations on the use of dienogest in the context of various clinical considerations when treating endometriosis. Methods: A search of PubMed was conducted for papers published between 2007 and 2019 on the use of dienogest in endometriosis. Experts reviewed these and included those they considered most relevant in clinical practice, according to their own clinical experience. Results: Evidence regarding the long-term use (>15 months) of dienogest for the management of endometriosis is presented, with experts concluding that the efficacy of dienogest should be assessed primarily on its impact on pain and quality of life. Fertility preservation, the option to avoid or delay surgery, and managing bleeding irregularities that can occur with this treatment are also considered. Counseling women on potential bleeding risks before starting treatment may be helpful, and evidence suggests that few women discontinue treatment for this reason, with the benefits of treatment outweighing any impact of bleeding irregularities. Conclusions: Overall, the evidence demonstrates that dienogest offers an effective and tolerable alternative or adjunct to surgery and provides many advantages over combined hormonal contraceptives for the treatment of endometriosis. It is important that treatment guidelines are followed and care is tailored to the woman's individual needs and desires.

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Pharmacokinetics, Bioequivalence, and Safety Evaluation of Dienogest in Healthy Subjects Under Fasting and Fed Conditions

Zhao

Zhang

et al. 2023

Clinical Pharm in Drug Dev

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Dienogest is effective in reducing endometriosis‐related pain symptoms. This study aims to investigate and compare the pharmacokinetic profiles and safety of test formulations to reference formulations of dienogest in healthy Chinese female volunteers under fasting or fed conditions. The purpose of this single‐center, randomized, open‐label, 2‐sequence, 2‐period crossover clinical trial was to evaluate the safety and pharmacokinetic profiles of the 2 formulations under fasting and fed conditions. Additionally, 48 healthy female volunteers were selected and divided at random into the fasting and the fed group. After dosing, the venous blood was collected through indwelling catheters. Dienogest plasma concentrations were measured using liquid chromatography–tandem mass spectrometry after the plasma samples were prepared with the protein precipitation method. Under either fasting or fed conditions, the pharmacokinetic parameters (maximum observed concentration, area under the concentration–time curve [AUC] from time 0 to the last measurable concentration, and AUC from time 0 to infinity) for dienogest between the test and reference products, geometric mean ratio, and 90%CI were all within the range of 80%–125%. The 2 dienogest products were bioequivalent. Based on maximum observed concentration and AUC from time 0 to the last measurable concentration, the generic dienogest was bioequivalent to the original dienogest in this study conducted under fasting and fed conditions in healthy Chinese women (study CTR20190063 on https://chinadrugtrials.org.cn registry).

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

Cited by 67 publications

References 120 publications

Endometriosis and Female Pelvic Pain

Endometriosis and Female Pelvic Pain

Use of dienogest in endometriosis: a narrative literature review and expert commentary

Pharmacokinetics, Bioequivalence, and Safety Evaluation of Dienogest in Healthy Subjects Under Fasting and Fed Conditions

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