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Antiandrogens: clinical applications.
J Steroid Biochem Mol Biol. 1990 Nov 20; 37(3):349-62.JS

Abstract

Antiandrogens, preventing androgen action at target tissue level, are used in the treatment of various androgen-dependent diseases. Pharmacologically these substances have either a steroidal structure, like cyproterone acetate (CPA) and spironolactone (SPL), or a non-steroidal structure, like flutamide (FLU). In women with hyperandrogenism (PCO syndrome, idiopathic hirsutism, acne), clinical benefit may be obtained with CPA, which also displays a progestational activity and an antigonadotropic effect. CPA (25-50 mg/day) is used in combination with ethinyl-estradiol (EE) (20-30 micrograms/day) in reversed sequential regimen. SPL, less effective than CPA may be employed in moderate hirsutism and acne at dosages of 100-200 mg/day. During SPL treatment menstrual irregularities are frequent: in this case an association with oral contraceptives is indicated. SPL + bromocriptine (2.5-5 mg/day) has been experienced with success in PCO syndrome. The pure antiandrogen FLU, inducing progressive increase in LH and testosterone secretion, may be used only in combination with oral contraceptives. In men antiandrogens have been tested in BPH and prostatic carcinoma. In BPH the decrease in nuclear receptors and DHT nuclear content during CPA or FLU may represent the rational base of the medical treatment. An improvement in urinary obstructive manifestation has been observed with CPA alone or associated with tamoxifen (100 mg + 100 mg day). In advanced prostatic carcinoma antiandrogens represent a good alternative to estrogen therapy with less side effects and in combination with surgical or medical castration (LH-RH analogues) achieve a complete androgen blockade. An increase in the percentage of remissions and survival has been reported.

Authors+Show Affiliations

Sciarra F
Istituto di V Clinical Medica Generale, University of Rome La Sapienza, Italy.
Toscano V
No affiliation info available
Concolino G
No affiliation info available
Di Silverio F
No affiliation info available

MeSH

Acne VulgarisAdultAndrogen AntagonistsCyproteroneCyproterone AcetateDermatitis, SeborrheicFemaleFlutamideHirsutismHumansMaleProstatic NeoplasmsSpironolactone

Pub Type(s)

Clinical Trial
Comparative Study
Journal Article
Multicenter Study
Randomized Controlled Trial

Language

eng

PubMed ID

2147859

Citation

Sciarra, F, et al. "Antiandrogens: Clinical Applications." The Journal of Steroid Biochemistry and Molecular Biology, vol. 37, no. 3, 1990, pp. 349-62.
Sciarra F, Toscano V, Concolino G, et al. Antiandrogens: clinical applications. J Steroid Biochem Mol Biol. 1990;37(3):349-62.
Sciarra, F., Toscano, V., Concolino, G., & Di Silverio, F. (1990). Antiandrogens: clinical applications. The Journal of Steroid Biochemistry and Molecular Biology, 37(3), 349-62.
Sciarra F, et al. Antiandrogens: Clinical Applications. J Steroid Biochem Mol Biol. 1990 Nov 20;37(3):349-62. PubMed PMID: 2147859.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antiandrogens: clinical applications. AU - Sciarra,F, AU - Toscano,V, AU - Concolino,G, AU - Di Silverio,F, PY - 1990/11/20/pubmed PY - 1990/11/20/medline PY - 1990/11/20/entrez SP - 349 EP - 62 JF - The Journal of steroid biochemistry and molecular biology JO - J Steroid Biochem Mol Biol VL - 37 IS - 3 N2 - Antiandrogens, preventing androgen action at target tissue level, are used in the treatment of various androgen-dependent diseases. Pharmacologically these substances have either a steroidal structure, like cyproterone acetate (CPA) and spironolactone (SPL), or a non-steroidal structure, like flutamide (FLU). In women with hyperandrogenism (PCO syndrome, idiopathic hirsutism, acne), clinical benefit may be obtained with CPA, which also displays a progestational activity and an antigonadotropic effect. CPA (25-50 mg/day) is used in combination with ethinyl-estradiol (EE) (20-30 micrograms/day) in reversed sequential regimen. SPL, less effective than CPA may be employed in moderate hirsutism and acne at dosages of 100-200 mg/day. During SPL treatment menstrual irregularities are frequent: in this case an association with oral contraceptives is indicated. SPL + bromocriptine (2.5-5 mg/day) has been experienced with success in PCO syndrome. The pure antiandrogen FLU, inducing progressive increase in LH and testosterone secretion, may be used only in combination with oral contraceptives. In men antiandrogens have been tested in BPH and prostatic carcinoma. In BPH the decrease in nuclear receptors and DHT nuclear content during CPA or FLU may represent the rational base of the medical treatment. An improvement in urinary obstructive manifestation has been observed with CPA alone or associated with tamoxifen (100 mg + 100 mg day). In advanced prostatic carcinoma antiandrogens represent a good alternative to estrogen therapy with less side effects and in combination with surgical or medical castration (LH-RH analogues) achieve a complete androgen blockade. An increase in the percentage of remissions and survival has been reported. SN - 0960-0760 UR - https://www.unboundmedicine.com/medline/citation/2147859/Antiandrogens:_clinical_applications_ DB - PRIME DP - Unbound Medicine ER -