CYPROTERONE ACETATE (CPA) Uses, Side Effects, and More

 CYPROTERONE ACETATE (CPA)

BRAND NAME:- GINETE -35 ,DINAC - 35 .

CYPROTERONE ACETATE is a steroid used in combination with ethinyl estradiol to treat women with severe acne and symptoms of androgenization. Also used alone at much higher doses for palliative treatment of patients with prostate cancer.

PHARMACODYNAMIC:- 

CPA has antiandrogenic activity,progestogenic activity, weak partial glucocorticoid activity, weak steroidogenesis inhibitor activity, and agonist activity at the pregnane X receptor. It has no estrogenic or antimineralocorticoid activity. In terms of potency, CPA is described as a highly potent progestogen, a moderately potent antiandrogen, and a weak glucocorticoid.Due to its progestogenic activity, CPA has antigonadotropic effects, and is able to suppress fertility and sex-hormone levels in both males and females.

PHARMACOKINETICS:-

CPA can be taken by mouth or by injection into muscle. It has near-complete oral bioavailability, is highly and exclusively bound to albumin in terms of plasma protein binding, is metabolized in the liver by hydroxylation and conjugation, has 15β-hydroxycyproterone acetate (15β-OH-CPA) as a single major active metabolite, has a long elimination half-life of about 2 to 4 days regardless of route of administration, and is excreted in feces primarily and to a lesser extent in urine.

MECHANISM OF ACTION:-

The direct antiandrogenic effect of cyproterone is blockage of the binding of dihydrotestosterone to the specific receptors in the prostatic carcinoma cell. In addition, cyproterone exerts a negative feed-back on the hypothalamo-pituitary axis, by inhibiting the secretion of luteinizing hormone resulting in diminished production of testicular testosterone.

 USED:- 

treatment of moderate to severe acne related to androgen-sensitivity (with or without seborrhea) and/or hirsutism, in women of reproductive age.used alone at much higher doses for palliative treatment of patients with prostate cancer.

SIDE EFFECTS:- 

breast tenderness and swelling.

•Tiredness and weakness (fatigue)

•Depression or mood changes.

•Hot flushes or sweats.

•Swelling in parts of the body (fluid build up)

•Weight changes.

•Liver changes (you will have regular blood tests to check for this)

•Shortness of breath.

DOSE :- 2mg OD.