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Androgen antagonists in androgen target tissues


, : Androgen antagonists in androgen target tissues. Pharmacology & Therapeutics 24(3): 367-400

Most antiandrogens appear to act by binding to the androgen receptor and competitively inhibiting the binding of testosterone and cihydrotestosterone to the receptor. Focusing on those compounds which appear to inhibit androgen receptor mediated responses, this review discusses the chemistry of those antiandrogens which have been studied to the extent that their mechanism of action is at least partially understood, outlines the mechanism of androgen action as it is currently understood and suggests how antiandrogens might fit in with this mechanism, indicates the major metabolites of several important antiandrogens, and discusses the clinical applications of several antiandrogens. Cyproterone acetate has been studied extensively as a potential male contraceptive. Although it was recognized that 100 mg of cyproterone acetate per day inhibited spermatogenesis, that dose also reduced libido and potency. Following the administration of 10 or 20 mg of cyproterone acetate per day to 15 males for 26 weeks, the following observations were made: the number of motile sperm was reduced; the quality of their motion was impaired; and the ability of the sperm to penetrate cervical mucus was decreased. Sperm density was also suppressed, but neither it nor sperm motility were inhibited to the extent necessary for contraception. Antiandrogens have been demonstrated to be beneficial in treating 5 clinical syndromes or diseases: acne, seborrhea, hirsutism with or without menstrual abnormalities; precocious puberty; benign prostatic hypertrophy; cancer of the prostate; and sexual deviates. Since 3 of these conditions are very common, effective and safe treatment would have a large market. At this time, antiandrogens are widely used in Europe for treatment of seborrhea, acne, and hirsutism and a large Veterans Administration Cooperative Study in the US was approved but has not yet been funded to compare antiandrogens with other treatments for cancer of the prostate. Studies to assess antiandrogen interaction with other hormones or drugs have been limited. Side effects in the female have been best evaluated when cyproterone acetate was administered in combination with ethinyl estradiol. In 46 women followed over 317 cycles, side effects were similar to those reported with estrogen-progestin contraceptives. Administration of 10-20 mg of cyrproterone acetate per day to males caused no significant side effects, but 100 mg or more/day has caused loss of libido, impotence, gynecomastia, tiredness, weakness, decreased efficiency, weight gain, drying and desquamation of skin over the legs, and loss of hair on the trunk and pubic area.

US$29.90

PMID: 6205409


Other references

Haeusler, G., 1972: Differential effect of verapamil on excitation contraction coupling in smooth muscle and on excitation secretion coupling in adrenergic nerve terminals. Journal of Pharmacology and Experimental Therapeutics 180(3): 672-682

Singh, D.P.; Sharma, P.; Shinohara, T.; Chylack Jr, L.T.; Fatma, N., 2003: Ledgf regulates expression of sparc, a gene having important biological function in lens. Purpose: LEDGF is a transcriptional survival factor and exerts its cellular survival function against stress by binding to stress response (STRE; A/TGGGG/TA) and heat shock (nGAAn) elements in the stress response genes and activating transcription...

Linton, E., 1915: Cestode Cysts from Muskrat. In this short paper the author describes the occurrence of four cysts in a muskrat-three in the liver and one in the peritoneum-which proved on examination to be Cysticercus fasciolaris.

Itskovich, A.I.; Furtsev, V.I.; Pozdniakova, L.I., 1988: An oxygen regimen in acute pneumonia and bronchitis in children. Pediatriia: 107-107

Williams, R.M.; Martin, S.; Falchuk, K.R.; Trey, C.; Dubey, D.P.; Cannady, W.G.; Fitzpatrick, D.; Noreen, H.; Dupont, B.; Yunis, E.J., 1978: Increased frequency of HLA-DRW4 in chronic active hepatitis. HLA-A, B, C and DRw typing was performed on peripheral blood lymphocytes of 17 adults with the diagnosis of chronic active hepatitis made by liver biopsy as the only criterion for study. An increase in the frequency of HLA-DRw4 (71 vs. 24%, p less...

Komura, M.; Komura, H.; Otani, Y.; Suzuki, K.; Satake, R.; Kodaka, T.; Terawaki, K.; Yonekawa, H.; Ikebukuro, K.; Hoshi, K.; Takato, T.; Tabata, Y.; Komuro, H.; Iwanaka, T., 2016: Tracheoplasty with cartilage-engineered esophagus environments. Our objective was to investigate the feasibility of engineering cartilage on the esophagus layer and outside the esophagus. Moreover, we investigated the feasibility of tracheoplasty with cartilage engineered on the esophagus in rabbits. Chondrocy...

Wood, S.N., 1940: Iodine in Nutrition and Therapy of Livestock. Canadian Journal of Comparative Medicine and Veterinary Science 4(11): 306-315

Hughes, J.N.; Chen, Q., 2011: Reciprocal effects of student-teacher and student-peer relatedness: Effects on academic self efficacy. This study investigated the reciprocal effects between teacher student relationship quality (TSRQ) and two dimensions of classroom peer relatedness, peer liking and peer academic reputation (PAR), across three years in elementary school and the ef...

Leinonen, J.; Laatikainen, L., 2000: The decrease of visual acuity in cataract patients waiting for surgery. To investigate the rapidity of vision loss in eyes waiting for cataract surgery and to estimate what proportion of life expectancy the extended wait for surgery comprised. The visual acuities at the time of referral and on the day before surgery w...

Kalz, M., 1965: The effect of water and electrolyte diuresis on the early phosphate damage to the rat kidney. Early damage to kidneys following 1- and 2-basic Na-phos-phate undergoes marked macroscopical and microscopical change in both localization and gravity, when introducing 50 ml water/kg, 50 ml electrolyte solution after Ringer/kg 400 mg acetazolami...