General
Description & Use
Used for prostate cancer treatment. Also used as an effective
anti androgen to supress male hormones in M2F transsexuals.
It
is a synthetic 17-lactone drug which is a renal competitive aldosterone
antagonist in a class of pharmaceuticals called potassium-sparing
diuretics, used primarily to treat heart failure, ascites in patients
with liver disease, low-renin hypertension, hypokalemia, and Conn's
syndrome as well as high blood pressure. On its own, spironolactone
is only a weak diuretic, but it can be combined with other diuretics.
About one person in one hundred with hypertension has elevated
levels of aldosterone; in these persons the antihypertensive effect
of spironolactone may exceed that of complex combined regimens
of other antihypertensives.
Cyproterone
acetate
Cyproterone acetate has weak progestational activity (e.g., it
acts like progesterone) and can be used to treat hot flushes.
As part of some combined oral contraceptive pills (Dianette in
UK and Diane-35®,
Estelle and Ginette in other countries) it decreases acne and
hirsutism (male-pattern hair growth). Cyproterone acetate (Androcur,
Cyprostat, Cyproteron, Procur, Cyprone, Cyprohexal, Ciproterona,
Cyproteronum, Neoproxil, Siterone) is an antiandrogen, i.e. it
suppresses the actions of testosterone (and its metabolite dihydrotestosterone)
on tissues. It acts by blocking androgen receptors which prevents
androgens from binding to them and suppresses luteinizing hormone
(which in turn reduces testosterone levels) Due to its anti-androgen
effect, it can also be used to treat hirsutism, and is a common
component in hormone therapy for male-to-female transgender people.
Due
to its anti-androgen effect, it can also be used to treat hirsutism,
and is a common component in hormone therapy for male-to-female
transsexual and transgendered people. It is also used for treating
hair loss and acne in women and can be used as a topical medication
for treatment of male baldness..
Side
effects of Cyproterone acetate
The most serious potential side effect is liver toxicity, and
patients should be monitored for changes in liver enzymes, especially
if taking a high dose (200-300 mg/day). Toxicity is dose-dependent
and the low doses used in birth control pills (2 mg) such as Diane-35®
not appear to represent a significant risk.
Suppression
of adrenal function and reduced response to ACTH have been reported.
Low cortisol levels may impair carbohydrate metabolism, and patients
with diabetes mellitus may require adjustments in insulin dosage.
Low aldosterone levels may lead to salt loss and hyperkalemia
(excess potassium). 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.
Used
alone, cyproterone acetate does not appear to have a significant
effect on blood clotting factors, however in combination with
ethinylestradiol (as in combined oral contraceptive pills) presents
an increased risk of deep vein thrombosis. There are conflicting
reports as to whether there is a significant difference in the
risk of thrombosis between oral contraceptives containing cyproterone
acetate versus other types of combined oral contraceptives.
Cyproterone
has been associated with depressive mood changes in some patients,
presumably due to androgen deprivation. However, others have reported
significant antidepressant effects. This may be due to its effect
on adrenal hormones, as similar antidepressant effects have been
observed with other adrenal suppressants, such as metyrapone.
Cyproterone acetate suppresses production of estrogen due to its
antigonadotrophic effect, and long-term use without estrogen replacement
may result in osteoporosis.
Side-effects
in men which directly result from its antiandrogenic action include
gynecomastia (breast growth), galactorrhea (milk outflow), and
erectile dysfunction.
We
are currently unable to supply this medication.
However we can suggest an alternative anti androgen medication
such as Spironolactone (marketed under the trade names Aldactone,
Novo-Spiroton, Spiractin, Spirotone, Verospiron, Berlactones,
Aladactide 25, Spironolact/ Hydroflumethiazide, and Lasilactone)
see:- Aladactide
25 (Spironolact/ Hydroflumethiazide) And also see
under Spirotone
and Lasilactone
A
combination medication containing cyproeterone/ estradiol and
widely used by M2F transsexuals is Diane-35®
