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Progestin Androgenic Activity

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1. Comparing the Effects of Combined Oral Contraceptives Containing Progestins With Low Androgenic and Antiandrogenic Activities on the Hypothalamic-Pituitary-Gonadal Axis in Patients With Polycystic Ovary Syndrome: Systematic Review and Meta-Analysis (Full text)

Comparing the Effects of Combined Oral Contraceptives Containing Progestins With Low Androgenic and Antiandrogenic Activities on the Hypothalamic-Pituitary-Gonadal Axis in Patients With Polycystic Ovary Syndrome: Systematic Review and Meta-Analysis Different products of combined oral contraceptives (COCs) can improve clinical and biochemical findings in patients with polycystic ovary syndrome (PCOS) through suppression of the hypothalamic-pituitary-gonadal (HPG) axis.This systematic review (...) and meta-analysis aimed to compare the effects of COCs containing progestins with low androgenic and antiandrogenic activities on the HPG axis in patients with PCOS.We searched PubMed, Scopus, Google Scholar, ScienceDirect, and Web of Science databases (1980-2017) to identify randomized controlled trials or nonrandomized studies investigating the effect of COCs containing progestins with low androgenic and antiandrogenic activities, including the products containing desogestrel, cyproterone acetate

2018 JMIR Research Protocols PubMed abstract

2. Progestin Androgenic Activity

Progestin Androgenic Activity Progestin Androgenic Activity Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Progestin Androgenic (...) Activity Progestin Androgenic Activity Aka: Progestin Androgenic Activity , Androgenic Activity II. General Unbound testosterone increases with androgenicity III. Characteristics Conditions associated with high Androgenic Activity ( ) (or weight gain) Nervousness Lowered HDL-2 Conditions associated with low Androgenic Activity Decreased libido IV. Progestins with most potent Androgenic Activity Methyltestosterone (50): Upper limit reference (8.6) (8.3) dl- (4.2) (3.4) V. Progestins with least

2018 FP Notebook

3. Comparing the androgenic and estrogenic properties of progestins used in contraception and hormone therapy (Full text)

and efficacies of selected progestins from different generations determined in parallel. We show that the progestins bind to the androgen receptor (AR) with similar affinities to each other and progesterone, while none bind estrogen receptor (ER)-β, and only norethisterone acetate, levonorgestrel and gestodene bind ERα. Comparative dose-response analysis revealed that progestins from the first three generations display similar androgenic activity to the natural androgen dihydrotestosterone (...) Comparing the androgenic and estrogenic properties of progestins used in contraception and hormone therapy Progestins used in endocrine therapies bind to multiple steroid receptors and are associated with several side-effects. It is thus important to understand the relationship between steroid receptor cross-reactivity and the side-effect profile of progestins. In cell lines that express negligible levels of steroid receptors, we report for the first time the binding affinities, potencies

2017 Biochemical and biophysical research communications PubMed abstract

4. Harnessing Androgen-Receptor Pathway Activation for Targeted Alpha Particle Radioimmunotherapy of Breast Cancer. (Full text)

Harnessing Androgen-Receptor Pathway Activation for Targeted Alpha Particle Radioimmunotherapy of Breast Cancer. The impact of androgen receptor (AR) activity in breast cancer biology is unclear. We characterized and tested a novel therapy to an AR-governed target in breast cancer.Experimental Design: We evaluated the expression of prototypical AR gene products human kallikrein 2 (hK2) and PSA in breast cancer models. We screened 13 well-characterized breast cancer cell lines for hK2 and PSA (...) production upon in vitro hormone stimulation by testosterone [dihydrotestosterone (DHT)]. AR-positive lines were further evaluated by exposure to estrogen (17β-Estradiol) and the synthetic progestin D-Norgestrel. We then evaluated an anti-hK2-targeted radiotherapy platform (hu11B6), labeled with alpha (α)-particle emitting Actinium-225, to specifically treat AR-expressing breast cancer xenografts under hormone stimulation.D-Norgestrel and DHT activated the AR pathway, while 17β-Estradiol did

2018 Clinical Cancer Research PubMed abstract

5. Colorectal tumor prevention by the progestin medroxyprogesterone acetate is critically dependent on postmenopausal status (Full text)

chemopreventive activity. The effect of MPA on colorectal carcinogenesis has been difficult to study in animal models. Most models are not affected by either depleting female hormones by ovariectomy or treatment with MPA. Importantly, an ovariectomy fails to reproduce one of the hall marks of the postmenopausal state in women with intact ovaries. That is, the continued production of androgens by the atrophic postmenopausal ovaries. Here we show that adenoma incidence is increased in the vinyl cylcohexene (...) Colorectal tumor prevention by the progestin medroxyprogesterone acetate is critically dependent on postmenopausal status The large randomized placebo controlled trials of the Women's Health Initiative have shown that the combination of estrogen and progestin medroxyprogesterone acetate (MPA) protects from colorectal cancer in postmenopausal women. No effect was observed in women treated with estrogen alone. This suggests that progesterone, or more specifically the progestin MPA may have

2018 Oncotarget PubMed abstract

6. Progestin Androgenic Activity

Progestin Androgenic Activity Progestin Androgenic Activity Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Progestin Androgenic (...) Activity Progestin Androgenic Activity Aka: Progestin Androgenic Activity , Androgenic Activity II. General Unbound testosterone increases with androgenicity III. Characteristics Conditions associated with high Androgenic Activity ( ) (or weight gain) Nervousness Lowered HDL-2 Conditions associated with low Androgenic Activity Decreased libido IV. Progestins with most potent Androgenic Activity Methyltestosterone (50): Upper limit reference (8.6) (8.3) dl- (4.2) (3.4) V. Progestins with least

2015 FP Notebook

7. Nestorone® (NES) a Novel Progestin for Non-oral Contraception: Structure-activity Relationships and Brain Metabolism Studies. (Full text)

Nestorone® (NES) a Novel Progestin for Non-oral Contraception: Structure-activity Relationships and Brain Metabolism Studies. Nestorone® (NES) is a potent nonandrogenic progestin being developed for contraception. NES is a synthetic progestin that may possess neuroprotective and myelin regenerative potential as added health benefits. In receptor transactivation experiments, NES displayed greater potency than progesterone to transactivate the human progesterone receptor (PR). This was confirmed (...) by docking experiments where NES adopts the same docking position within the PR ligand-binding domain (LBD) as progesterone and forms additional stabilizing contacts between 17α-acetoxy and 16-methylene groups and PR LBD, supporting its higher potency than progesterone. The analog 13-ethyl NES also establishes similar contacts as NES with Met909, leading to comparable potency as NES. In contrast, NES is not stabilized within the human androgen receptor LBD, leading to negligible androgen receptor

2016 Endocrinology PubMed abstract

8. Review: Understanding the role of androgens and placental AR variants: Insight into steroid-dependent fetal-placental growth and development. (Abstract)

Review: Understanding the role of androgens and placental AR variants: Insight into steroid-dependent fetal-placental growth and development. The role of steroids throughout pregnancy and their effect on placental physiology is well established, especially for estrogens, progestogens, and glucocorticoids; however, the role of androgens - particularly within the context of placental physiology - remains largely unexplored. Androgens are often defined as the male sex-steroids and are fundamental (...) and activity of factors involved in androgen biosynthesis and bioavailability, with males consistently demonstrating greater degrees of altered protein and gene expression when compared with females. Understanding the placental androgen axis is essential as many pregnancy comorbidities are associated with elevated concentrations of androgens and perturbed intrauterine development or growth. Indeed, it appears that specific pathophysiologies of pregnancy can modulate the activity of key factors involved

2019 Placenta

9. Third Generation Progestin

. Ontology: Levonorgestrel (C0023566) Definition (NCI) The levorotatory form of norgestrel and synthetic progestogen with progestational and androgenic activity. Levonorgestrel binds to the progesterone receptor in the nucleus of target cells, thereby stimulating the resulting hormone-receptor complex, initiating transcription, and increasing the synthesis of certain proteins. This results in a suppression of luteinizing hormone (LH) activity and an inhibition of ovulation, as well as an alteration (...) Generation Progestin Aka: Third Generation Progestin , Norgestrel , Levonorgestrel II. Class 19 Nor-Testosterone : Gonane III. Preparation: dl-Norgestrel Relative : 2.6 : 0 : 4.2 : 2.6 Anti- : Active Anabolic: Active Preparations (0.3/30) Ovral (0.5/50) ( ) (0.075) IV. Preparation: Levonorgestrel Relative : 5.3 : 0 : 8.3 : 5.1 Anti- : Active Anabolic: Active Preparations with (0.1/20) (0.15/30) (0.15/30) (0.15/30) (0.05/30 - 0.075/40 - 0.125/30) (0.15/30) - seasonal (0.09/20) - continuous V. Adverse

2018 FP Notebook

10. First Generation Progestin

Generation Progestin Aka: First Generation Progestin , Norethindrone , Norethynodrel II. Class 19 Nor-Testosterone : Estrane III. Norethindrone Relative : 1.0 : 1.0 : 1.0 : 1.0 Anti- : Active Preparations or (0.5/35) (0.4/35, 1/50) or Biphasic (0.5-1.0/35) Triphasic (0.5-0.75-1.0/35) Triphasic (0.5-1.0-0.5/35) (50 mcg is equivalent to 35 mcg estradiol) 1/50 Ortho-Novum 1/50 1/50 -1 (UK) -only ( ) , (0.35) IV. 50 µg Mestranol (equivalent to 35 µg Ethinyl Estradiol) V. 1000 µg Norethindrone (UK: Norinyl-1 (...) prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See for financial assistance information. Ontology: Norethindrone (C0028356) Definition (NCI) A synthetic progestational substance with some anabolic, estrogenic, and androgenic properties. Norethindrone binds to the progesterone intracellular receptors in the reproductive system and the resultant activated complex interacts with specific DNA sites. This leads to an alteration in protein synthesis and results

2018 FP Notebook

11. Androgen Therapy in Women (Full text)

these immunoassays and liquid chromatography mass spectrometry was poor ( , ); thus, caution should be taken with regard to published absolute values of this steroid ( ). Changes in DHEAS across the lifespan Although androstenedione, DHEAS, and dehydroepiandrosterone (DHEA) are often referred to as adrenal androgens, they are not. They are prohormones, which do not activate the androgen receptor but rather may be converted to active androgens. Cross-sectional studies have reported a linear decline (...) transition, or late transition) ( ). This late perimenopausal rise in DHEAS was also seen in 81 women who had undergone bilateral oophorectomy ( ). The physiological role of changes in DHEAS during this transition is unclear. Androgens and prohormones in tissues Although all the preceding discussions are centered on plasma androgens, ultimately hormone action takes place in cells. Dihydrotestosterone (DHT), rather than T, is the active androgen in three important target tissues in women, including skin

2014 The Endocrine Society PubMed abstract

12. Kaempferol Exhibits Progestogenic Effects in Ovariectomized Rats (Full text)

Kaempferol Exhibits Progestogenic Effects in Ovariectomized Rats Progesterone (P4) plays a central role in women's health. Synthetic progestins are used clinically in hormone replacement therapy (HRT), oral contraceptives, and for the treatment of endometriosis and infertility. Unfortunately, synthetic progestins are associated with side effects, including cardiovascular disease and breast cancer. Botanical dietary supplements are widely consumed for the alleviation of a variety (...) , the ability of kaempferol to block genistein action in the uterus was investigated. Analyses of proliferation, steroid receptor expression, and induction of well-established PR-regulated targets Areg and Hand2 were completed using histological analysis and qPCR gene induction experiments. In addition, kaempferol in silico binding analysis was completed for PR. The activation of estrogen and androgen receptor signalling was determined in vitro.Molecular docking analysis confirmed that kaempferol adopts

2014 Journal of steroids & hormonal science PubMed abstract

13. Circulating Androgen Levels Are Not Affected by the Administration of Vaginal Micronized Progesterone for Withdrawal Bleeding in Patients With Polycystic Ovarian Syndrome

the measurement of basal levels of androgens and 17-hydroxyprogesterone (17-OHP), which are generally used to establish the presence of hyperandrogenemia. In general, these levels are obtained during the follicular phase to maintain sampling uniformity and avoid spurious increases due to corpus luteum function. However, because most hyperandrogenic patients are oligo/amenorrheic, it is frequently necessary to administer a progestogen to induce withdrawal bleeding and properly time the blood sampling. Several (...) medications have been described to properly induce withdrawal bleeding , with medroxyprogesterone acetate (MPA) being the most widely use. However, synthetic compounds as MPA do not replicate precisely the constellation of biologic activities of the parent hormone and results in a temporary, albeit clinically relevant, suppression in ovarian function and circulating androgen levels , in addition of several adverse side effects . In this study, it is hypothesized that the administration of natural

2017 Clinical Trials

14. An androgen receptor mutation in the MDA-MB-453 cell line model of molecular apocrine breast cancer compromises receptor activity. (Full text)

An androgen receptor mutation in the MDA-MB-453 cell line model of molecular apocrine breast cancer compromises receptor activity. Recent evidence indicates that the estrogen receptor-α-negative, androgen receptor (AR)-positive molecular apocrine subtype of breast cancer is driven by AR signaling. The MDA-MB-453 cell line is the prototypical model of this breast cancer subtype; its proliferation is stimulated by androgens such as 5α-dihydrotestosterone (DHT) but inhibited by the progestin (...) medroxyprogesterone acetate (MPA) via AR-mediated mechanisms. We report here that the AR gene in MDA-MB-453 cells contains a G-T transversion in exon 7, resulting in a receptor variant with a glutamine to histidine substitution at amino acid 865 (Q865H) in the ligand binding domain. Compared with wild-type AR, the Q865H variant exhibited reduced sensitivity to DHT and MPA in transactivation assays in MDA-MB-453 and PC-3 cells but did not respond to non-androgenic ligands or receptor antagonists. Ligand binding

2012 Endocrine-Related Cancer PubMed abstract

15. First Generation Progestin

Generation Progestin Aka: First Generation Progestin , Norethindrone , Norethynodrel II. Class 19 Nor-Testosterone : Estrane III. Norethindrone Relative : 1.0 : 1.0 : 1.0 : 1.0 Anti- : Active Preparations or (0.5/35) (0.4/35, 1/50) or Biphasic (0.5-1.0/35) Triphasic (0.5-0.75-1.0/35) Triphasic (0.5-1.0-0.5/35) (50 mcg is equivalent to 35 mcg estradiol) 1/50 Ortho-Novum 1/50 1/50 -1 (UK) -only ( ) , (0.35) IV. 50 µg Mestranol (equivalent to 35 µg Ethinyl Estradiol) V. 1000 µg Norethindrone (UK: Norinyl-1 (...) prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See for financial assistance information. Ontology: Norethindrone (C0028356) Definition (NCI) A synthetic progestational substance with some anabolic, estrogenic, and androgenic properties. Norethindrone binds to the progesterone intracellular receptors in the reproductive system and the resultant activated complex interacts with specific DNA sites. This leads to an alteration in protein synthesis and results

2015 FP Notebook

16. Third Generation Progestin

. Ontology: Levonorgestrel (C0023566) Definition (NCI) The levorotatory form of norgestrel and synthetic progestogen with progestational and androgenic activity. Levonorgestrel binds to the progesterone receptor in the nucleus of target cells, thereby stimulating the resulting hormone-receptor complex, initiating transcription, and increasing the synthesis of certain proteins. This results in a suppression of luteinizing hormone (LH) activity and an inhibition of ovulation, as well as an alteration (...) Generation Progestin Aka: Third Generation Progestin , Norgestrel , Levonorgestrel II. Class 19 Nor-Testosterone : Gonane III. Preparation: dl-Norgestrel Relative : 2.6 : 0 : 4.2 : 2.6 Anti- : Active Anabolic: Active Preparations (0.3/30) Ovral (0.5/50) ( ) (0.075) IV. Preparation: Levonorgestrel Relative : 5.3 : 0 : 8.3 : 5.1 Anti- : Active Anabolic: Active Preparations with (0.1/20) (0.15/30) (0.15/30) (0.15/30) (0.05/30 - 0.075/40 - 0.125/30) (0.15/30) - seasonal (0.09/20) - continuous V. Adverse

2015 FP Notebook

17. Evaluation of Risk-Minimization Activities for Cyproterone Acetate 2 mg/Ethinylestradiol 35 µg: A Cross-Sectional Physician Survey (Full text)

Evaluation of Risk-Minimization Activities for Cyproterone Acetate 2 mg/Ethinylestradiol 35 µg: A Cross-Sectional Physician Survey Cyproterone acetate 2 mg/ethinylestradiol 35 µg, an estrogen/progestogen treatment with anti-androgenic properties, shares a thromboembolism risk with combined hormonal contraceptives. Educational materials (i.e., direct healthcare professional communication, patient information card, prescriber checklist) were distributed to physicians to increase risk

2017 Pharmaceutical medicine PubMed abstract

18. Androgen Excess (Treatment)

, van de Velde CJ. Identification of virilizing adrenal tumors in hirsute women. N Engl J Med . 1994 Oct 13. 331(15):968-73. . Latronico AC, Chrousos GP. Extensive personal experience: adrenocortical tumors. J Clin Endocrinol Metab . 1997 May. 82(5):1317-24. . Wu CH. Plasma androgens, progestins, and prolactin in hirsutism. Eur J Obstet Gynecol Reprod Biol . 1982 Sep. 13(6):377-87. . Hagag P, Hertzianu I, Ben-Shlomo A, Weiss M. Androgen suppression and clinical improvement with dopamine agonists (...) Androgen Excess (Treatment) Androgen Excess Treatment & Management: Medical Care, Surgical Care, Consultations Edition: No Results No Results Please confirm that you would like to log out of Medscape. If you log out, you will be required to enter your username and password the next time you visit. https://profreg.medscape.com/px/getpracticeprofile.do?method=getProfessionalProfile&urlCache=aHR0cHM6Ly9lbWVkaWNpbmUubWVkc2NhcGUuY29tL2FydGljbGUvMjczMTUzLXRyZWF0bWVudA== processing > Androgen Excess

2014 eMedicine.com

19. Androgen Excess (Overview)

and organs, causing variable clinical features such as acne, hirsutism, virilization, and reproductive dysfunction. [ ] Sources and types of androgens in women The endocrine glands secrete 5 androgens through a similar pathway: testosterone, dehydroepiandrosterone sulfate (DHEAS), dehydroepiandrosterone (DHEA), androstenedione, and androstenediol, the latter of which has both androgenic and estrogenic activity. Testosterone and its biologically active metabolite dihydrotestosterone (DHT) are the only (...) androgens with direct androgenic activity. DHEAS, DHEA, and androstenedione are all precursors of testosterone. Androgen secretion pathway in adrenal glands and ovaries. Ovarian androgens The ovaries produce 25% of circulating testosterone, which is dependent on luteinizing hormone (LH) secreted by the anterior pituitary. The ovaries also secrete 50% of the androstenedione and 20% of DHEA. Testosterone is used as a marker of ovarian androgen secretion. However, the adrenals also contribute

2014 eMedicine.com

20. Androgen Excess (Follow-up)

estrogen/progestogen-induced breast cell proliferation in postmenopausal women. Menopause . 2007 Mar-Apr. 14(2):183-90. . Bulun SE, Mahendroo MS, Simpson ER. Polymerase chain reaction amplification fails to detect aromatase cytochrome P450 transcripts in normal human endometrium or decidua. J Clin Endocrinol Metab . 1993 Jun. 76(6):1458-63. . Tuckerman EM, Okon MA, Li T, Laird SM. Do androgens have a direct effect on endometrial function? An in vitro study. Fertil Steril . 2000 Oct. 74(4):771-9 (...) SK, Meinders AE, Haak HR, van de Velde CJ. Identification of virilizing adrenal tumors in hirsute women. N Engl J Med . 1994 Oct 13. 331(15):968-73. . Latronico AC, Chrousos GP. Extensive personal experience: adrenocortical tumors. J Clin Endocrinol Metab . 1997 May. 82(5):1317-24. . Wu CH. Plasma androgens, progestins, and prolactin in hirsutism. Eur J Obstet Gynecol Reprod Biol . 1982 Sep. 13(6):377-87. . Hagag P, Hertzianu I, Ben-Shlomo A, Weiss M. Androgen suppression and clinical improvement

2014 eMedicine.com

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