cyproterone

No form of cyproterone acetate is available in the United States.

The pharmacokinetics of cyproterone are complicated due to its lipophilic nature.

The drug cyproterone acetate has been commonly used for chemical castration throughout Europe.

Thus the sudden withdrawal of cyproterone acetate may result in undesirable androgenic effects.

In such cases, withdrawal of cyproterone results in a reduction in cancer growth, rather than the opposite.

Cyproterone has been associated with depressive mood changes in some patients, presumably due to androgen deprivation.

These altered androgen receptors can be stimulated, rather than inhibited, by cyproterone.

Use during pregnancy is contraindicated, and for women of childbearing age, cyproterone should be administered with a combined oral contraceptive.

Screening of chemical libraries for AR blockers led to the discovery of cyproterone.

Cyproterone is a topical agent in a lipid suspension that has anti-androgenic activity at the pilosebaceous unit.

Though, cyproterone has also been shown to inhibit 17α-hydroxylase and 17,20-lyase, enzymes in the androgen biosynthesis pathway, which may offset this.

Indeed, finasteride is a substantially weaker antiandrogen in comparison to conventional antiandrogens like spironolactone and cyproterone.

In New Zealand, the antilibidinal drug cyproterone acetate is sold under the name Androcur.

Cyproterone acetate has approximately three times the anti-androgenic activity of cyproterone.

These non-steroidal antiandrogens eventually crossed the blood-brain barrier, like cyproterone, leading to a subsequent increase in serum testosterone levels.

The antiandrogen cyproterone acetate was a gift from C. Sonnenschein (Tufts University).

An acetate group was then added to cyproterone creating cyproterone acetate.

Treatment is with drugs that suppress gonadal steroidogenesis, such as cyproterone acetate, ketoconazole, spironolactone, and testolactone.

More specifically, it is a derivative of pregna-4,6-diene structurally related to the progestogen chlormadinone and the androgen antagonist cyproterone.

Therefore, use of cyproterone acetate in combination with substances which inhibit CYP3A4 may increase the progestational effects.

In treatment of prostate cancer, cyproterone is often co-administered with a GnRH agonist and a 5-alpha-reductase inhibitor.

Dexamethasone is an agonist, and RU486 and cyproterone are antagonists of the GR.

Patients taking cyproterone should have their cortisol levels and electrolytes monitored, and if hyperkalemia develops, reduce the consumption of food having a high potassium content.

The latter causes the limitations of cyproterone acetate, which are central effects on androgen secretion, with subsequent loss of libido and sexual potency.

Compared to cyproterone acetate, spironolactone is considerably less potent as an antiandrogen by weight and binding affinity to the androgen receptor.