Abiraterone

Cytostatic · Oral anti-androgen

Indications

With prednisolone for metastatic castration-resistant prostate cancer, in men who are asymptomatic or mildly symptomatic and in whom chemotherapy is not yet indicated, or men whose disease has progressed during or after docetaxel treatment.

Dosage

Adults: 1 gm once daily, at least 1 hr before and 2 hr after food. Children: Not applicable.

Adverse Effects

UTI, hypokalaemia, hypertriglyceridaemia, cardiac failure, angina, arrhythmia, hypertension, increased ALT/AST peripheral oedema, diarrhoea, dyspepsia, haematuria, fractures, rash, myopathy.

Risk Factor (Pregnancy/Lactation)

Contraindications: Active or symptomatic viral hepatitis, severe hepatic impairment. Precautions: Heart failure, severe or unstable angina, recent MI or ventricular arrhythmia or arterial thrombotic event. Severe renal impairment, moderate hepatic impairment. Previous ketoconazole treatment. Continue LHRH analogue in patients not surgically castrated. Correct hypokalaemia, control hypertension and fluid retention and optimise cardiac function before starting treatment. Monitor BP, serum potassium and fluid levels before and during treatment and monthly thereafter (every 2 weeks for first 3 months in patients at risk of CHF). Perform LFTs before treatment, every 2 weeks for first 3 months and monthly thereafter: withdraw if ALT/AST >5 x ULN and do not restart if ALT/AST >20 x ULN. Withhold if grade >3 toxicity occurs. Condoms should be worn by men whose partners are pregnant and an…

Interactions

Cardiac glycosides, CYP2D6 substrates, ketoconazole, other potent inhibitors or inducers of CYP3A4, drugs that cause myopathy or rhabdomyolysis.

Advice to Patient

Take atleast 1 hour before or 2 hours after meals. Do not chew or crush tablets, swallow whole. If a dose is missed, skip it and return to normal schedule. Do not take double dose. Contact prescriber if there is bone pain, signs of infection (fever, chills, sore throat), injury, sudden asthma attack. Keep all doctors and lab appointments. Abiraterone acetate is taken along with prednisone. Use caution if doctor tells you to discontinue prednisone or to reduce the dose, or if you experience events that cause physical stress.

Pharmacokinetics

Absorption: Increased systemic exposure with food. Metabolism: Hepatic. Half-life elimination: 14.4-16.5 hrs. Time to peak, plasma: Approx. 2 hrs. Excretion: Faeces (approx. 88%). Urine (approx. 5%).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.