The Effects of Pharmaceuticals, Environmental, and Occupational Agents on Sperm Motility
Claude Gagnon in Controls of Sperm Motility, 2020
Cyproterone acetate (6-chloro-17-hydroxy l-alpha-2-alpha methylenepregna-4,6-diene 3,20-dione acetate), an antiandrogenic steriod, is used in the treatment of hypersexuality, sexual deviations (sex offenders), and male precocious puberty, and to alleviate the symptoms of prostatic carcinoma. Cyproterone acetate is also one of the antiandrogens that have been considered as a potential male contraceptive. In the lower dosage range (10 to 20 mg daily), it lowers the depth of sperm penetration into a column of midcycle cervical mucus in vitro (Kremer test) and reduces the sperm density in human semen, while lowering the levels of circulating testosterone and gonadotropins.63,64 At higher doses (100 mg daily), cyproterone can also cause immobilization of the spermatozoa in addition to the decrease in sperm count.65
The practical management of hormonal treatment in adults with gender dysphoria
James Barrett in Transsexual and Other Disorders of Gender Identity, 2017
Cyproterone acetate is a potent androgen receptor-blocking drug. It is derived from progesterone and is metabolised in the liver. Its use is associated with hepatic dysfunction, and although this rarely leads to discontinuation of the drug it does require regular monitoring of liver function.32,34 More importantly there is a significant incidence of depression associated with the use of cyproterone in up to 30% of users.32 In this patient population depression is a significant problem, and cyproterone acetate can often exacerbate these symptoms. The same problems occur with the use of finasteride; both depression and liver function disturbance have been described with the use of this drug.35–37 Antiandrogens have been necessary in the past, as many patients fail to suppress their production of testosterone with estrogen therapy. Now we have the availability of GnRH analogues. These drugs work by over-stimulating the LH receptors on the gonadotrophin cells of the pituitary, which become downregulated decreasing LH release which leads to reduced testosterone production. There has been extensive experience in using these drugs both in the treatment of prostate cancer and infertility, and they have an excellent side-effect profile.
Urological Anti-cancer Agents
Karl H. Pang, Nadir I. Osman, James W.F. Catto, Christopher R. Chapple in Basic Urological Sciences, 2021
Cyproterone acetateDual mechanism of action:Inhibition of prostate cells AR.Negative feedback effect on the hypothalamus and pituitary gland.Side effects: similar to LHRH antagonists:Depressed mood, dyspnoea, fatigue, gynaecomastia, hepatic disorders, hot flush, hyperhidrosis, nipple pain, restlessness, weight change
Androgen receptor modulators: a review of recent patents and reports (2012-2018)
Published in Expert Opinion on Therapeutic Patents, 2019
Shinya Fujii, Hiroyuki Kagechika
Since AR activation is closely related to aggravation of prostate cancer, AR antagonists are used clinically for the treatment of prostate cancer [18–21]. Cyproterone acetate (7) is a steroidal AR antagonist used in the treatment of androgen-dependent disorders including prostate cancer (Figure 3) [22,23]. Oxendolone (8) is used in the treatment of enlarged prostate in Japan [24]. However, steroidal antagonists exhibit side effects due to cross-activity with other steroid hormone receptors, and therefore various nonsteroidal AR antagonists (nonsteroidal antiandrogens, NSAAs) have been developed. Flutamide (9) is one of the first-generation nonsteroidal AR antagonists; it was discovered in 1967 and has been in clinical use since the 1980s [25,26]. Flutamide (9) has also been a lead compound for the development of various novel nonsteroidal AR antagonists. Two other first-generation NSAAs, the hydantoin derivative nilutamide (10) [27,28] and the sulfone derivative bicalutamide (11) [29,30], have been in clinical use since the 1990s. Bicalutamide (11) is the most potent of the three, having the highest receptor affinity and a superior ADMET profile [31], and is, therefore, the most widely used first-generation NSAA for prostate cancer. Topilutamide (12) is also a first-generation NSAA used for the treatment of pattern hair loss in the Czech Republic and Slovakia [32].
Spherical agglomeration to improve dissolution and micromeritic properties of an anticancer drug, Bicalutamide
Published in Drug Development and Industrial Pharmacy, 2019
Hitesh Dalvadi, Komal Parmar, Suryabali Yadav
Bicalutamide (BCT) is a nonsteroidal antiandrogen that is used widely in the treatment therapy of prostate cancer. It stops testosterone from reaching the cancer cells. It is not reported to cause any side effects associated with steroidal antiandrogens like cyproterone acetate and shows the absence of any known progestational activities. Elimination half-life of BCT is about one week and thus is compatible with once-daily dosing. BCT is a lipophilic drug with log P octanol/water value of 2.92, where P is the partition coefficient and depicts a very low solubility in water (<5 mg/L). Various researchers have investigated different approaches to improve the dissolution properties of BCT [16–18]. Heretofore, there is no work reported whereby micromeritic and dissolution properties of BCT have been improved by spherical crystal agglomeration technique. Hence, the authors endeavor to study the influence of processing conditions and formulation parameters on the formation of BCT agglomerates and its properties viz. micromeritic and dissolution. Principal component analysis and Box-Behnken experimental design were utilized to optimize the prepared agglomerates of BCT.
Effect of orlistat during individualized comprehensive life-style intervention on visceral fat in overweight or obese PCOS patients
Published in Gynecological Endocrinology, 2022
Min Min, Xiangyan Ruan, Husheng Wang, Jiaojiao Cheng, Suiyu Luo, Zhongting Xu, Meng Li, Alfred Otto Mueck
Because in our team’s earlier study with cyproterone acetate/EE the 3-monthly duration was effective [12, 14], so results could be expected choosing this time of duration. Hormonal oral contraception was started in both groups during menstrual cycle day 5 using DRSP/EE (Bayer Healthcare Co. Ltd, 28 tablets/box, 24 active pills each containing 20 μg ethinyl estradiol (EE) and 3 mg drospirenone (DRSP), followed by 4 placebo tablets; trade name YAZ). This “24 + 4” schedule was performed in group-1 together with orlistat (Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd, 0.12 g/tablet), using 3 tablets/day during meals or within half an hour after meals. Group-2 only used DRSP/EE.
Related Knowledge Centers
- Acne
- Antiandrogen
- Estrogen
- Hirsutism
- Precocious Puberty
- Prostate Cancer
- Progestogen
- Androgen-Dependent Condition
- Feminizing Hormone Therapy
- Oral Contraceptive Pill