Cyproterone is a derivative of progesterone; its combination of structural similarities and differences results in the following:
• Competition with testosterone for receptors in target peripheral organs (but not causing féminisation as do oestrogens); it reduces spermatogenesis even to the level of azoospermia (reverses over about 4 months after the drug is stopped); abnormal sperm occurs during treatment.
• Competition with testosterone in the central nervous system, reducing sexual drive and thoughts, and causing impotence.
• Some agonist progestogenic activity on hypothalamic receptors, inhibiting gonadotrophin secretion, which also inhibits testicular androgen production.
Uses. Cyproterone is used for reducing male hypersexuality and in prostatic cancer and severe female hirsutism. A formulation of cyproterone plus ethinylestradiol (Dianette) is offered for this latter purpose as well as for severe acne in women; this preparation acts as an oral contraceptive but does not have a UK licence, and should not be used primarily for this purpose. Plainly, long-term use of the drug poses both medical and ethical problems.3 It is even advised that for management of male hypersexuality formally witnessed written consent be obtained.
Cyproterone causes hepatomas in rats.
Cyproterone is plainly unsuitable for male contraception (see actions above).
Flutamide and bicalutamide are nonsteroidal antiandrogens available for use in conjunction with the gonadorelins (e.g. goserelin) in the treatment of prostatic carcinoma. Finasteride (p. 544), which inhibits conversion of testosterone to dihydro-testosterone, has localised antiandrogen activity in tissues where dihydrotestosterone is the principal androgen: this makes it a useful drug in the treatment of benign prostatic hypertrophy.
Spironolactone (p. 534) also has antiandrogen activity and may help hirsutism in women. Androgen secretion may be diminished by continued use of a gonadorelin (LH-RH) analogue (see p. 714).
Ketoconazole (antifungal) interferes with androgen and corticosteroid synthesis and may be used in prostatic carcinoma.
Androgens are effective protein anabolic agents, but their clinical use for this purpose is limited by the amount of virilisation that women will tolerate. Attempts made to separate anabolic from androgenic action have been only partially successful and
3 Individual problems can be quite trying and revealing. A 26-year-old woman with severe facial hirsutism was prescribed cyproterone from days 5 to 15 of each menstrual cycle. After 4 months, she reported to her doctor that her male Rottweiler would not leave her alone and repeatedly tried to mount her during these 10 days of each month. The patient managed to keep her Rottweiler and lose her hair by having the dog castrated (Cotterill J A1992 Lancet 340: 986).
all anabolic steroids also have androgenic effects. They have been used to treat osteoporosis in women but are no longer recommended for this purpose.
The itching of chronic biliary obstruction may be relieved by stanozolol 5-15 mg/day There remains, however, a risk of increasing the degree of jaundice (see p. 653).
They benefit some patients with aplastic anaemia.
Hereditary angioedema (lack of inhibition of the complement CI esterase) may be prevented by androgens (stanozolol and danazol are used).
Anabolic steroids can prevent the calcium and nitrogen loss in the urine that occurs in patients bedridden for a long time and they have therefore been used in the treatment of some severe fractures. The use of anabolic steroids in conditions of general wasting despite nutritional support may be justifiable in extreme debilitating disease, such as severe ulcerative colitis, and after major surgery. In the later stages of malignant disease they may make the patient feel and look less wretched. Their general use as tonics is scandalous, as is their use in sport (see Index).4
Anabolic steroids do not usefully counter the unwanted catabolic effects of the adrenocortical hormones.
None of these agents is free from virilising properties in high doses; acne and greasy skin may be the early manifestation of virilisation (see also, Adverse effects of androgens, p. 714; and Drugs and sport).
Administration should generally be intermittent in courses of 3-12 weeks with similar intervals, to reduce the occurrence of unwanted effects, especially liver injury.
There is little to choose between the principal available drugs, nandrolone (Durabolin) (i.m. once a week) and stanozolol (Stromba) (orally), except that the latter is contraindicated in liver disease.
4 While the misuse of anabolic steroids in sport is well known (infamous), a report has drawn attention to the practice among some teenagers of using the drugs to improve their appearance and handsomeness, giving themselves the 'macho' look which they think girls like. (Nilsson S 1995 Androgenic anabolic steroid use among male adolescents in Falkenberg. European Journal of Clinical Pharmacology 48: 9-11).
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