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Pronunciation:

(sye PROE ter one)

Synonyms:

Cyproterone Acetate

Generic Available:

Yes (Canada)

Canadian Brand Names:

Alti-CPA; Androcur®; Androcur® Depot; Gen-Cyproterone

Use:

Palliative treatment of advanced prostate carcinoma

Restrictions:

Not available in U.S.

Pregnancy Risk Factor:

Not indicated for use in women

Pregnancy Implications:

In males, sperm count and volume of ejaculate will be reduced. After ~2 months of treatment, infertility may be noted.

Contraindications:

Hypersensitivity to cyproterone or any component of the formulation; active liver disease or hepatic dysfunction; renal impairment

Warnings/Precautions:

Cyproterone has been associated with hepatic toxicity (jaundice, hepatitis, hepatic failure); typically this toxicity develops after several months of therapy. Monitor hepatic function and consider discontinuation of therapy in patients with evidence of hepatic injury.

Use caution in patients with a history of depression. Cyproterone has been associated with an increased incidence of depression, particularly early in the course of therapy (initial 6-8 weeks). Use with caution in patients with diabetes or impaired glucose tolerance, may cause alterations in glucose metabolism. Use with caution in conditions that may be aggravated by fluid retention, or cardiovascular disease. May increase the risk of thromboembolism and/or alter lipid profiles.

Adverse Reactions:

Frequency not defined.

Cardiovascular: Heart failure, hemorrhage, hypotension, MI, stroke, shock, stroke, syncope, tachycardia, thrombosis (DVT, pulmonary embolism, retinal vein thrombosis)

Central nervous system: Libido increased, lassitude, fatigue, weakness, dizziness, encephalopathy, depression, headache

Dermatologic: Dry skin (sebum reduction), patchy loss of body hair, eczema, urticaria, erythema nodosum, rash, exfoliative dermatitis, photosensitivity, scleroderma, pruritus, hirsutism, skin discoloration

Endocrine & metabolic: Hyperglycemia, negative nitrogen balance, gynecomastia, hot flashes, benign nodular breast hyperplasia, galactorrhea, inhibition of spermatogenesis, impotence, adrenal suppression (dose related), hypercalcemia, diabetes mellitus, weight gain/loss

Gastrointestinal: Constipation, diarrhea, dyspepsia, nausea, anorexia, pancreatitis, glossitis, vomiting

Genitourinary: Hematuria, urinary frequency, bladder carcinoma

Hematologic: PT decreased, fibrinogen increased, thrombocytopenia, anemia, hemolytic anemia, leukopenia, leukocytosis

Hepatic: Hepatic dysfunction (dose related), hepatitis, transaminases increased, cholestatic jaundice, cirrhosis, hepatic failure, hepatic necrosis, ascites, hepatic coma, hepatomegaly, hepatoma, hepatic carcinoma

Local: Injection site reaction

Neuromuscular and skeletal: Weakness, myasthenia, osteoporosis

Ocular: Optic neuritis, optic atrophy, abnormal accommodation, abnormal vision, retinal disorder, blindness

Renal: Serum creatinine increased, renal failure

Respiratory: Asthma, bronchospasm, cough, dyspnea, pulmonary embolism, pulmonary fibrosis

Miscellaneous: Allergic reaction

Overdosage/Toxicology:

Toxicity is unlikely following single exposures of excessive doses. Any treatment following emesis and charcoal administration should be supportive and symptomatic.

Ethanol/Nutrition/Herb Interactions:

Ethanol: May reduce the effect of cyproterone (not established in the treatment of prostatic carcinoma); avoid concurrent use.

Stability:

Store at controlled room temperature of 25°C (77°F).

Mechanism of Action:

Cyproterone is a steroidal compound with anti-androgenic, anti-gonadotropic, and progestin-like activity.

Pharmacodynamics/Kinetics:

Absorption: Oral: Rapid and complete

Metabolism: Hepatic, some metabolites have activity

Half-life elimination: Oral: 38 hours; Depot injection: 4 days

Time to peak, plasma: Oral: 3-4 hours; Depot injection: 3 days

Excretion: Urine (35%, as metabolites); feces (60%)

Dosage:

Adults: Males: Prostatic carcinoma (palliative treatment):

Oral: 200-300 mg/day in 2-3 divided doses; following orchiectomy, reduce dose to 100-200 mg/day; should be taken with meals

I.M. (depot): 300 mg (3 mL) once weekly; reduce dose in orchiectomized patients to 300 mg every 2 weeks

Dosage adjustment in renal impairment: Use is contraindicated

Dosage adjustment in hepatic impairment: Use is contraindicated with hepatic impairment or active liver disease

Administration:

Administer at the same time each day. Take with meals.

Monitoring Parameters:

Liver function tests should be performed at baseline and periodically thereafter, or whenever signs or symptoms suggestive of hepatotoxicity are noted. Adrenal function should be monitored periodically.

Dental Health: Effects on Dental Treatment:

Key adverse event(s) related to dental treatment: Glossitis.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Dosage Forms:

Injection, solution, as acetate (Androcur® Depot): 100 mg/mL (3 mL) [contains benzyl benzoate and castor oil]

Tablet, as acetate (Androcur®): 50 mg

International Brand Names:

Alti-CPA (CA); Androcur® (CA); Androcur® Depot (CA); Gen-Cyproterone (CA)

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