Drug reference

Cyproterone acetate

Hormonal Anticancer Agent · Hormone Antagonist

Also known as Androcur, Cyprostat, Cyproterone

Hormonal Anticancer AgentHormone Antagonist

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

—

none in our sources

PREGNANCY

FDA category + note

Mechanism

Cyproterone acetate is an anti-androgen that binds to the androgen receptor, inhibiting the action of androgens. It also inhibits pituitary gonadotrophin secretion, leading to a depression of spermatogenesis and reversible infertility. Additionally, it has progestin activity.

Indications

Severe hypersexuality in malesSexual deviation in malesMetastatic prostate cancer refractory to gonadorelin analogue therapyAdjunct in prostatic cancer (before and after initiation of gonadorelin analogue)Treatment of acne in womenTreatment of hirsutism in womenLong-term palliative therapy for prostate cancer where gonadorelin analogues or orchidectomy are contraindicated, not tolerated, or where oral therapy is preferredHot flushes with gonadorelin analogue therapy or after orchidectomyprecocious puberty (in boys)inappropriate sexual behaviour (in men)acne (in women, usually in combination with an estrogen)hirsutism (in women, usually in combination with an estrogen)metastatic prostate carcinoma (efficacy inferior to other forms of androgen deprivation)

Dosing

Adult: Hyper-sexuality/Sexual deviation: 50 mg twice daily by mouth, to be taken after food. Adjunct in prostatic cancer: 200 mg daily in 2-3 divided doses by mouth for 5-7 days before initiation of gonadorelin analogue, followed by 200 mg daily in 2-3 divided doses for 3-4 weeks after initiation of gonadorelin analogue.…
Hepatic adjustment: Manufacturer advises avoid (unless used for prostate cancer).
Max dose: 300 mg per day (for adjunct in prostatic cancer)

Contraindications

Dubin-Johnson syndrome
Existing or history of thromboembolic disorders
Malignant diseases (except for carcinoma of the prostate)
Meningioma or history of meningioma
Previous or existing liver tumours (not due to metastases from carcinoma of the prostate)
Rotor syndrome
Wasting diseases (except for inoperable carcinoma of the prostate)
Severe depression (when used for hypersexuality)
Severe diabetes with vascular changes (when used for hypersexuality)
Sickle-cell anaemia (when used for hypersexuality)

Side effects

Common

FatigueLassitudeGastrointestinal discomfortMyalgiaFluid imbalanceLipid metabolism changeAbnormal hepatic functionReduced spermatogenesisAbnormal sperm forms

Serious

Hepatic tumours (in animal studies)
Neoplasms
Direct hepatic toxicity (jaundice, hepatitis, hepatic failure, fatalities reported at doses of 100 mg and above)
Adrenocortical suppression
Anaemia
Azoospermia
Thromboembolism
Galactorrhoea
Meningioma
hepatotoxicity