Co-cyprindiol

Uses

This is used for Acne, Contraception, Hirsutism, Prostatic carcinoma, Libido, Hot flushes

Co-cyprindiol is also used to associated treatment for these conditions: Advanced Prostate Carcinoma, Menstrual Irregularities, Metastatic Hormone Refractory Prostate Cancer, Osteoporosis, Paraphilia, Postmenopausal Osteoporosis, Primary Amenorrhoea, Secondary Amenorrhea, Severe Acne, Hormone Replacement Therapy

How Co-cyprindiol works

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.

Dosage

Co-cyprindiol dosage

Acne, Contraception, Hirsutism: 2 mg/day (with ethinylestradiol) for 21 days of the menstrual cycle.

Palliative treatment for prostatic carcinoma: Initial: 300 mg/day in 2-3 divided doses. Maintenance: 200-300 mg/day.

Control of libido: 50 mg twice daily. Hot flushes 50 mg/day, may increase to 150 mg/day in 3 divided doses if needed.

Side Effects

Inhibits spermatogenesis, reduces volume of ejaculate, causes infertility, produces abnormal spermatozoa, gynecomastia and enlargement of mammary glands; galactorrhoea and benign nodules. Depressive mood changes. Alterations in hair pattern, skin reactions. Fatigue and lassitude, breathlessness, wt changes.

Precaution

Prostate cancer, hepatic impairment, DM, history of depression, familial defects in lipoprotein metabolism, CV diseases. Monitor LFT, adrenocortical function, LDL and HDL levels, and RBC count during treatment. In women: Interrupt treatment if persistent or recurrent bleeding occurs to exclude the possibility of organic diseases. May increase risk of thrombo-embolic diseases. Ineffective for male hypersexuality in chronic alcoholism. May impair ability to drive or operate machinery. Pregnancy, lactation.

Interaction

Metabolism may be reduced by inhibitors of CYP3A4 e.g. ketoconazole, itraconazole, clotrimazole, ritonavir. Inducers of CYP3A4 e.g. rifampicin, phenytoin may reduce the levels of cyproterone.

CYP1A2 and CYP3A4 inducers such as aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together. Altered anticoagulant effect when used with dicoumarol.

Potentially Fatal: Antibiotics (ampicillin, tetracycline, sulphonamides and chloramphenicol) can cause intermenstrual bleeding or failure of contraception. Reduced efficacy of antihypertensives or hypoglycaemic drugs.

Elimination Route

Completely absorbed following oral administration.

Half Life

Elimination Following oral or intramuscular administration, the plasma half-life is 38 and 96 hours, respectively.

Elimination Route

It is excreted approximately 60% in the bile and 33% through the kidneys.

Pregnancy & Breastfeeding use

Pregnancy Category X. Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh potential benefits.

Contraindication

Markedly impaired liver function or cholestasis; Dubin-Johnson or Rotor syndrome, hepatic adenoma; malignant or wasting diseases; severe chronic depression; severe diabetes with vascular changes; sickle-cell anaemia; history of thromboembolic disorders; renal impairment. Youths <18 yr.

Innovators Monograph

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