Androcur

How does it work?

Androcur tablets contain the active ingredient Cyproterone acetate, which is a type of medicine known as an Anti Androgen. Cyproterone acetate is also available without a brand name, ie as the generic medicine.
Androgens are male hormones such as testosterone. Testosterone is produced by the testicles and is the main hormone essential for normal growth and development of the male sex organs and male sexual characteristics. During adult life, testosterone is essential for the production of sperm, the maintenance of sex drive, erectile potency, and the functioning of the prostate gland and other reproductive structures.
Cyproterone acts on an area of the brain called the hypothalamus and causes a reduction in the amount of testosterone produced by the body. It also prevents testosterone from binding to androgen receptors in other areas of the body. The result of this is a decrease in the amount of testosterone circulating in the body, which can help control sexual desire.
Androcur tablets are used to Anti Androgen in Transgender. Control sex drive in men with severe hypersexuality and or sexual deviation. Sexual deviation refers to men who prefer sexual practices that are biologically abnormal or considered morally wrong or illegal, for example paedophilia or bestiality.

How to used for Transgender?

Cyproterone acetate (Androcur) 50-100 mg/day.
Androcur interfere with receptor binding of androgens have been used success-fully.

What is it used for?

• Anti Androgen in Transgender or Transsexual.
• Controlling sex drive in men with severely increased sex drive (hypersexuality) and/or deviant antisocial sexual behaviour such as bestiality or paedophilia.

Not to be used in

• Women.
• Children or adolescents under 18 years of age.
• Men whose bones or testicles have not fully matured.
• People who have had a meningioma (a tumour in the protective membranes around the brain and spinal cord).
• Liver disease.
• Malignant or cancerous disease (except prostate cancer).
• Men who have ever had a blood clot in a vein (venous thromboembolism), eg in the leg (deep vein thrombosis) or in the lungs (pulmonary embolism).
• Men who have ever had a blood clot in an artery, eg a stroke or mini-stroke (TIA) caused by a blood clot, or a heart attack.
• Hereditary blood disorder called sickle cell anaemia.
• Diabetes with complications affecting the blood circulation, eyes or kidneys.
• Long-term severe depression.

This medicine should not be used if you are allergic to any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy.

If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.

Hormone Treatment in Male-to-Female Transsexuals

Transgender Hormone Treatment in Male-to-Female Transsexuals Annihilation of Male Characteristics

In male-to-female transgender suppression of the original sex characteristics can be obtained by compounds that exert directly or indirectly an antiandrogenic effect. Androgens are for their production dependent on stimulation by the pituitary hormone luteinizing hormone (LH) which, in turn, is stimulated by the hypothalamic hormone luteinizing hormone-releasing hormone (LHRH). The biological action of androgens is contingent on their interaction with hormone receptors in the body's tissue cells. Interference with any of these mechanisms will lead to a decline of the biological action of androgenic hormone. Some of the drugs that will be listed have a dual action in this respect (Table 1).

TABLE 1. Hormones Used in Cross-Gender Hormone Treatment of Transsexualism

Antiandrogens
LHRH analogues
	leuprorelin	Lucrin depotR	3.75 mg/months s.c.
	triptorelin	Decapepty1-CRR	3.75 mg/months i.m
Interference with testosterone or DHT production
	Spironolactone	Aldactone	100-200 mg/day p.o.
	finasteride	not registered
	flutamide	EulexinR	250 mg t.i.d., p.o.
Antigonadotropic
	Cyproterone acetate	Androcur	100-150 mg/day p.o.
	Hydroxyprogesterone	Proluton depot	250 mg/2 weeks to 1000 mg/month i.m.
	medroxyprogesterone	proveraR	5-10 mg/day p.o.
		Depo-ProveraR	150 mg/month i.m.
		FarlutaiR	5-10 mg/day p.o.
		Farlutal depotR	100 mg/month i.m.
Androgen receptor blockers
	Cyproterone acetate	Androcur	100-150 mg/day p.o.
	nilutamide	AnandronR	300 mg/day p.o.
	Spironolactone	Aldactone	100-200 mg/day p.o.
Estrogens
	ethinyl estradiol	Diane 35	100 µg/day p.o.
		Sucee	100 µg/day p.o.
		Yasmin	100 µg/day p.o.
	conjugated estrogens	premarin	5-10 mg/day p.o.
	17ß estradlol	progynova	2-4 mg/day p.o.
		Progynon depot	10 mg/2 weeks to 100 mg/month i.m.
		Estraderm TTSR	50-100 µg/day trans dermally
		Oestrogel	75-150 µg/day trans dermally
	estriol	SynapauseR	4-6 mg/day p.o.
Androgens
	testosterone esters	TestoylronR	250 mg/2 weeks 1.m.
		sustanonR	250 mg/2 weeks i.m.
	testosterone undecanoate	AndrinlR	160-240 mg/day p.o.

1. Suppression of gonadotropins (the pituitary hormones) that stimulate testicular and ovarian hormone production can be achieved by LHRH analogues: triptorelin and leuprorelin 3.75 mg/4 weeks are available as injectables. Their cost is prohibitive; a major side effect is hot flashes of the type that postmenopausal women experience. There is no reported experience with these drugs in transsexuals. Also cyproterone acetate, progestogens and high dose estrogens suppress gonadotropins by their negative feedback action. Progestogens are available in the form of medroxyprogesterone acetate (Provera^R) as a parenteral drug (150 mg/6 weeks) and Hydroxyprogesterone (Proluton) (250 mg/2 weeks) or oral drug (5-10 mg/day). They probably also interfere with the androgen receptor.

2. interference with the production of testosterone or its conversion to the potent metabolite 5alpha-dihydrotestosterone (DHT) can be exercised by drugs like spironolactone (Aldactone) 100-200 mg/day. Finasteride is a potent 5 alpha-reductase inhibitor preventing the conversion of testosterone to DHT and therewith reducing its biological effect.

3. Drugs that interfere with receptor binding of androgens (or in the future with postreceptor mechanisms) have been used success-fully. Cyproterone acetate (Androcur) 100 mg/day orally or 300 mg/month intramuscularly and less effectively medroxyprogesterone acetate have also antigonadotropic action. The "pure" antiandrogens nilutamide (Anandron^R) 300 mg/day and flutamide (Eulexin 250 mg, three times a day) are potent drugs. They are less suited as monotherapy since by their interference with the negative feed-back action of androgens, they stimulate gonadotropin production and subsequently androgen production. Spironolactone has also receptor-blocking properties.

Of all the above drugs side-effects have been reported. Some are inherent in the interference with the biological action of androgens like a reduction of muscle mass and power and of the hemoglobin content. Some patients will complain of loss of energy and vitality to straightforward depression. The antiandrogen we have extensively used is cyproterone acetate (100mg/day). Side effects encountered are those mentioned above. Our alternative drug is spironolactone. Several studies have demonstrated its efficacy in transsexuals and in hirsute women alike. It has also an antihypertensive effect, since the drug was designed as a diuretic.

We have limited experience with nilutamide and LHRH antagonists. Medroxy-progesterone acetate has been widely used in the USA also in sex offenders. It is a satisfactory drug also in the view of the mild side effects and the costs. A randomized double-blind clinical trial to establish the best suited antiandrogen compound in transsexuals has not been performed so far.


Following orchiectomy we try to reduce or terminate antiandrogen therapy. Sexual hair growth is clearly dependent on androgens for its initiation and it would be logical to believe that antiandrogens are redundant following orchiectomy. Though not verified by research data, patients claim that also after orchiectomy their sexual hair growth is still reduced by antiandrogens. Due to the much shorter life cycle of sexual hair on the trunk, arms and legs as compared to the face and the greater density of hair follicles in the beard area, beard growth is not reduced to a cosmetically acceptable degree by antiandrogens. Other measures like depilation by electrolysis are needed. Those subjects who are young enough to have no significant beard development or whose racial background provides them with little or no beard development, are not in need of antiandrogens for this purpose.