Hormones 2016

Cyproterone Acetate
Note
Bicalutamide is extensively metabolised in the liver. Data suggests that
its elimination may be slower in people with severe hepatic impairment
and this could lead to increased accumulation of bicalutamide. Therefore,
bicalutamide should be used with caution in patients with moderate to
severe hepatic impairment.
Periodic liver function testing should be considered due to possibility of
hepatic changes. The majority of changes are expected to occur within the
first 6 months of bicalutamide therapy.
Severe hepatic changes and hepatic failure have been observed rarely with
bicalutamide, and fatal outcomes have been reported. Bicalutamide therapy
should be discontinued if changes are severe.
Warning
Bicalutamide is a teratogen and must not be handled by females who are or
may become pregnant. It is known to cause foetal harm.
Cyproterone Acetate
What is it?
Cyproterone acetate, sometimes abbreviated as CPA, and sold under
brand names such as Androcur and Cyprostat, is a synthetic steroidal
antiandrogen drug with additional progestogen and antigonadotropic
properties (Neumann and Topert, 1986). Its primary action is to suppress
the activity of the androgen hormones such as testosterone and its more
potent metabolite dihydrotestosterone (DHT) in the body, effects which
it mediates via competitive antagonism of the androgen receptor and
inhibition of enzymes in the androgen biosynthesis pathway. The main
therapeutic indications of cyproterone acetate are prostate cancer, benign
prostatic hyperplasia, priapism, hypersexuality (e.g., as a form of chemical
castration), and other conditions in which androgen action maintains the
disease process. In addition, it can also be used to treat acne and hirsutism
in females, and is a common component in hormone therapy for transsexual
women.
An anti-androgen that, in the form of its acetate (cyproterone acetate), also
has progestational properties. It is used in the treatment of hypersexuality
in males, as a palliative in prostatic carcinoma, and, in combination
with oestrogen, for the therapy of severe acne and hirsutism in females
(drugbank, 2014a).
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Version 2016.3576– – Document LATEXed – 1st May 2016
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