Diane 35 is an antiandrogens and progestin medication and progesterone
is Cyproterone acetate (CPA). Cyproterone acetate sold
alone is under the brand name Androcur but mainly with ethinylestradiol under the brand on Diane
or Diane-35 :
CPA
was discovered in 1961. It was originally developed as a
progestin. In 1965, the antiandrogenic effects of CPA were
discovered. CPA was first marketed, as an antiandrogen, in 1973, and was
the first antiandrogen to be introduced for medical use. A few years later, in
1978, CPA was introduced as a progestin in a birth control pill It has
been described as a "first-generation" progestin. CPA is
available widely throughout the world The
indications A) in the treatment of
androgen-dependent conditions in women like acne, excessive hair growth, CPA blocks the effects of androgens like testosterone in
the body, which it does by preventing them from interacting with their biological
target, the androgen receptor (AR),
and by reducing their production by the gonads and hence
their concentrations in the body. In addition, it has progesterone-like
effects by activating the progesterone receptor (PR). CPA is
used to treat such conditions both at low doses as a birth control pill and on
its own at higher doses. A birth control pill containing low-dose CPA in
combination with ethinylestradiol to treat acne has been
found to result in overall improvement in 75 to 90% of women, with responses
approaching 100% improvement other medications with
antiandrogenic effects are used to treat androgen-dependent conditions instead CPA
is used as an antiandrogen to treat high androgen
levels and associated symptoms such
as masculinization due to conditions
like polycystic ovary syndrome (PCOS)
and congenital adrenal hyperplasia (CAH)
in women. It is almost always combined with an estrogen, such as ethinylestradiol,
when it is used in the treatment of PCOS in women. CPA has been investigated
for use in reducing aggression and self-injurious
behavior via its antiandrogenic effects in conditions
like autism spectrum disorders, dementias like Alzheimer's disease, and psychosis. CPA
may be effective in the treatment of obsessive–compulsive disorder (OCD). In
very limited clinical research, it has been reported to be
"considerably" effective in the treatment of OCD in women. CPA
has been studied in the treatment of cluster
headaches in men.
CPA
were no more effective or only marginally more effective in the treatment of
severe hirsutism in women than the birth control pill alone.
Type
I:- CPA is used with ethinylestradiol as a combined
birth control pill to prevent pregnancy. This birth control
combination has been available since 1978. The formulation is taken once
daily for 21 days, followed by a 7-day free interval.
The
other combinations of Oestrogens :
A)CPA has also been available in combination with estradiol valerate (brand
name Femilar) as a combined birth control pill in Finland since
1993.
B)Cyclical high dose CPE say 100 mg fro day 5-day 14 and EE 30
mcg or Lynoral O.03 mg fro day 5 to day 25.
High-dose CPA tablets have a
contraceptive effect and can be used as a form of birth control, although they
are not specifically licensed as such. CPA has typically been combined with
ethinylestradiol, but it can alternatively be used in combination with hormone replacement therapy dosages
of estradiol instead.
C)
Ethinylestradiol/cyproterone
acetate Randomized controlled trials have
found that higher dosages of CPA (e.g., 20 mg/day or 100 mg/day)
added cyclically to a birth control pill containing ethinylestradiol and
2 mg/day
D)
CPA at a dosage of 50 mg/day in
combination with 100 μg/day transdermal estradiol patches has been found
to be effective in the treatment of hirsutism similarly to the combination of
CPA with ethinylestradiol.
What are the other anti-androgens available
?? Examples of such medications
include 1) gonadotropin-releasing hormone
modulators (GnRH modulators) like leuprorelin and degarelix, 2)
nonsteroidal
antiandrogens like flutamide and bicalutamide, 3) the diuretic and steroidal antiandrogen spironolactone,
the 4) progestin medroxyprogesterone acetate, and 6) the 5α-reductase inhibitors finasteride and dutasteride.
The
steroidal antiandrogen and progestin chlormadinone acetate is used as an
alternative to CPA in Japan, South Korea, and a few other countries. Maintenance therapy with lower doses of CPA, such as
25 mg/day, has been found to be effective in preventing relapse of
symptoms of hirsutism. Side effects of CPA in general include hypogonadism (low
sex-hormone levels) and associated symptoms such
as demasculinization, sexual dysfunction, infertility,
and osteoporosis (fragile bones); breast changes
such as breast tenderness, breast enlargement, and ; emotional changes such as fatigue and depression;
and other side effects such as vitamin B12 deficiency, weak glucocorticoid effects,
and elevated liver enzymes. Weight gain can
occur with CPA when it is used at high doses. Some of the side effects of
CPA can be improved or fully prevented if it is combined with an estrogen to
prevent estrogen deficiency.
..What is Cyproterone acetate (CPA), CPA
is used as an antiandrogen to treat androgen-dependent skin and hair conditions such as acne, seborrhea, hirsutism (excessive
hair growth), scalp hair loss, and hidradenitis suppurativa in
women. These conditions are worsened by the presence of androgens, and by
suppressing androgen levels and blocking their actions, CPA improves the
symptoms of these conditions..sold alone under the brand name Androcur or
early puberty, and prostate
cancer, as a component of feminizing hormone therapy for transgender
women, and in birth control pills. It is formulated and
used both alone and in combination with an estrogen and is available for use
both by mouth and by injection into muscle.
CPA
is taken by mouth one to three times per day or given by injection once or
twice per week.
Common side effects of
high-dose CPA in men include gynecomastia (breast
development) and feminization. In both men and women,
possible side effects of CPA
include low sex
hormone levels, reversible infertility, sexual dysfunction, fatigue, depression, weight gain,
and elevated liver enzymes. At very high
doses in older individuals, significant cardiovascular complications
can occur. Rare but serious adverse reactions of CPA include blood clots, liver damage,
and certain types of benign brain tumors.
CPA can also cause adrenal insufficiency as a withdrawal effect
if it is discontinued abruptly from a high dosage. CPA blocks the effects
of androgens like testosterone in
the body, which it does by preventing them from interacting with their biological
target, the androgen
receptor (AR), and by reducing their production by
the gonads and
hence their concentrations in the body. In addition, it has progesterone-like
effects by activating the progesterone receptor (PR). It can
also produce weak cortisol-like effects at very high doses.
CPA
alone is used as progestin and antiandrogen in hormonal birth control and in the
treatment of androgen-dependent conditions.
Specifically, CPA is used in combined birth control pills, in the
treatment of androgen-dependent skin and hair conditions such
as acne, seborrhea, excessive
hair growth, and scalp hair
loss, high androgen levels, in transgender hormone therapy, to
treat prostate cancer, to reduce sex drive in sex offenders or
men with paraphilias or hypersexuality,
to treat early puberty, and for other uses. It
is used both at low doses and at higher doses.
.
High-dose CPA alone likewise has been found to improve
symptoms of acne by 75 to 90% in women. Discontinuation of CPA has been
found to result in marked recurrence of symptoms in up to 70% of
women. CPA is one of the most commonly used medications in the treatment
of hirsutism, hyperandrogenism, and polycystic ovary syndrome in women
throughout the world.
Higher
dosages of CPA are used in combination with an estrogen specifically at doses
of 25 to 100 mg/day cyclically in the treatment of hirsutism in women. The
efficacy of such dosages of CPA in the treatment of hirsutism in women appear
to be similar to that of spironolactone, flutamide,
and finasteride.
The
efficacy of the combination of an estrogen and CPA in the treatment of
hirsutism in women appears to be due to marked suppression of total and
free androgen levels
as well as additional blockade of the androgen
receptor.
CPA
has been found to be effective in the treatment of acne in males, with marked
improvement in symptoms observed at dosages of 25, 50, and 100 mg/day in
different studies. It can also halt further progression of scalp hair loss in
men. Increased head hair and decreased body hair has been observed with CPA in
men with scalp hair loss. However, its side effects in men, such as demasculinization, gynecomastia, sexual dysfunction, bone density loss, and
reversible infertility, make the use of CPA in males
impractical in most cases. In addition, lower dosages of CPA, such as
25 mg/day, have been found to be better-tolerated in men. But such doses
also show lower effectiveness in the treatment of acne in men.
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