Abirone

Abiraterone acetate

In combination w/ prednisone or prednisolone for newly diagnosed high risk metastatic hormone sensitive prostate cancer (mHSPC) in adult men in combination w/ androgen deprivation therapy; metastatic castration resistant prostate cancer (mCRPC) in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated; mCRPC in adult men whose disease has progressed on or after a docetaxel-based chemotherapy regimen.

1,000 mg (four 250-mg tab) as single daily dose. mHSPC Given w/ prednisone or prednisolone 5 mg daily. mCRPC Given w/ prednisone or prednisolone 10 mg daily. Patient who develops hepatotoxicity during treatment Re-treatment: 500 mg (2 tab) once daily may be given following return of LFTs to patient's baseline.

Should be taken on an empty stomach: Take at least 1 hr before or 2 hr after meals. Swallow whole, do not chew/crush.

Hypersensitivity. Severe hepatic impairment (Child-Pugh class C). Women who are or may potentially be pregnant.

Patients whose underlying medical conditions might be compromised by increases in BP, hypokalaemia (eg, those on cardiac glycosides), or fluid retention (eg, those w/ heart failure, severe or unstable angina pectoris, recent MI or ventricular arrhythmia & those w/ severe renal impairment); w/ history of CV disease. Consider obtaining assessment of cardiac function (eg, ECG) before treating patients w/ significant risk for CHF (eg, history of cardiac failure, uncontrolled HTN, or cardiac events eg, ischaemic heart disease). Treat cardiac failure & optimise cardiac function before treatment. Correct & control HTN, hypokalaemia & fluid retention. Monitor BP, serum K, fluid retention (wt gain, peripheral oedema), & other signs & symptoms of CHF during treatment every 2 wk for 3 mth, then mthly thereafter & correct abnormalities. QT prolongation in patients experiencing hypokalaemia in association w/ treatment. Assess cardiac function as clinically indicated, institute appropriate management & consider discontinuation of treatment if there is a clinically significant decrease in cardiac function. Measure serum transaminase levels prior to starting treatment, every 2 wk for the 1st 3 mth of treatment, & mthly thereafter; immediately if clinical symptoms or signs suggestive of hepatotoxicity develop. Interrupt treatment immediately & closely monitor liver function if at any time ALT/AST rises >5 x ULN. Patients w/ active or symptomatic viral hepatitis. Acute liver failure & hepatitis fulminant. Corticosteroid w/drawal & coverage of stress situations. Monitor for adrenocortical insufficiency if patients are w/drawn from prednisone or prednisolone. Monitor patients for symptoms of mineralocorticoid excess if treatment is continued after corticosteroids are w/drawn. Increase dose of corticosteroids before, during & after stressful situation in patients on prednisone or prednisolone who are subjected to unusual stress. Decreased bone density in men w/ metastatic advanced prostate cancer which increased by treatment in combination w/ glucocorticoid. Lower rates of response in patients previously treated w/ ketoconazole for prostate cancer. Increased hyperglycaemia w/ use of glucocorticoids; measure blood sugar frequently in patients w/ diabetes. Concomitant use w/ cytotoxic chemotherapy. Contains lactose; not to be taken by patients w/ rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Patients on controlled Na diet. Anaemia & sexual dysfunction in men w/ metastatic prostate cancer including those undergoing treatment. Patients concomitantly treated w/ medicinal products known to be associated w/ myopathy/rhabdomyolysis. Avoid strong CYP3A4 inducers during treatment. Discontinue if severe hepatotoxicity develops. Moderate hepatic impairment; not to be used in severe hepatic impairment. Renal impairment. Use condom along w/ another effective contraceptive method if patient is engaged in sexual activity w/ a pregnant woman or woman of childbearing potential. Not for use in women. Childn.

UTI; hypokalaemia; HTN; diarrhoea; increased ALT/AST; peripheral oedema. Sepsis; hypertriglyceridaemia; cardiac failure, angina pectoris, atrial fibrillation, tachycardia; dyspepsia; rash; haematuria; fractures.

Increased absorption w/ food. Decreased mean plasma AUC∞ w/ rifampicin. Avoid use w/ strong CYP3A4 inducers eg, phenytoin, carbamazepine, rifabutin, rifapentine, phenobarb, St. John's wort (Hypericum perforatum). Increased systemic exposure of dextromethorphan. Co-administration w/ CYP2D6-activated/metabolized medicinal products (particularly w/ narrow therapeutic index) eg, metoprolol, propranolol, desipramine, venlafaxine, haloperidol, risperidone, propafenone, flecainide, codeine, oxycodone & tramadol; CYP2C8-metabolized medicinal products w/ narrow therapeutic index. Increased AUC of pioglitazone. May increase conc of medicinal products eliminated by OATP1B1. May prolong QT intervals or induce torsades de pointes w/ class IA (eg, quinidine, disopyramide) or class III (eg, amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic medicinal products, methadone, moxifloxacin, antipsychotics. May increase PSA levels w/ spironolactone.

Cancer Hormone Therapy

L02BX03 - abiraterone ; Belongs to the class of other hormone antagonists and related agents. Used in the treatment of metastatic castration-resistant prostate cancer.

Rx