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Pharmacologic class: CYP17 inhibitor
Therapeutic class: Antineoplastic
Pregnancy risk category X
Converts from abiraterone acetate in vivo to abiraterone, an androgen biosynthesis inhibitor that inhibits 17α-hydroxylase/C17,20-lyase (CYP17), an enzyme that's expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis, thereby causing androgen-sensitive prostatic carcinoma to respond to such treatment that decreases androgen levels
Tablets: 250 mg
Indications and dosages
➣ Metastatic castration-resistant prostate cancer in combination with prednisone in patients who have received prior chemotherapy containing docetaxel
Adults: 1,000 mg P.O. daily in combination with prednisone 5 mg P.O. b.i.d.
• Baseline moderate hepatic impairment (Child-Pugh Class B)
• Women of childbearing age
Use cautiously in:
• mild to moderate hepatic disease, mineralocorticoid excess, adrenocortical insufficiency, CV disease
• co-administration of CYP2D6 substrates with a narrow therapeutic index (avoid use or if alternative treatments can't be used, consider a dosage reduction of the concomitant CYP2D6 substrate)
• co-administration of strong inhibitors and inducers of CYP3A4 (avoid or use with caution)
• breastfeeding women
• children (safety and efficacy not established).
☞ Be aware that pregnant women and women of childbearing age shouldn't handle drug without wearing gloves.
• Control hypertension and correct hypokalemia before starting drug.
• Give tablets whole and be aware that patient shouldn't eat for at least 2 hours before drug is administered and for at least 1 hour after drug is administered.
☞ Don't use in patients with baseline severe hepatic impairment (Child-Pugh Class C).
• Withhold drug in patients who develop hepatotoxicity during treatment until recovery. May restart drug at a reduced dosage.
☞ Discontinue drug if patient develops severe hepatotoxicity.
• Be aware that safety isn't established in patients with left ventricular ejection fraction less than 50% or New York Heart Association Class III or IV heart failure.
CV: hypertension, arrhythmia, heart failure
GI: diarrhea, dyspepsia
GU: urinary tract infection, urinary frequency, nocturia
Metabolic: hypokalemia, mineralocorticoid excess with fluid retention, adrenocortical insufficiency,
hyperosmolar coma or death Musculoskeletal: joint swelling or discomfort, muscle discomfort, fractures, musculoskeletal and connective tissue disorders
Respiratory: cough, upper respiratory tract infection
Other: fluid retention, edema, hot flushes, chest pain or discomfort
Drug-drug. CYP2D6 substrates with a narrow therapeutic index (such as thioridazine): increased CYP2D6 substrate Cmax and area under the curve (AUC) CYP3A4 inducers (such as carbamazepine, phenobarbital, phenytoin, rifabutin, rifapentine, rifampin): unknown effects Strong CYP3A4 inhibitors (such as atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole): unknown effects
Drug-diagnostic tests. ALT, AST, triglycerides, total bilirubin): increased levels
Potassium: reduced level
Drug-food. Any food: increased abiraterone AUC
• Monitor hepatic function tests closely and modify, interrupt, or discontinue dosing as prescribed.
• Monitor blood pressure, serum potassium level, and signs and symptoms of fluid retention at least monthly.
• Monitor patient for signs and symptoms of adrenocortical insufficiency (such as hypoglycemia, hypotension, orthostatic hypotension, dehydration, weight loss, and nausea and vomiting); be aware that increased dosage of corticosteroids may be indicated before, during, and after stressful situations.
• Tell patient to swallow tablets whole with water on an empty stomach (don't eat for at least 2 hours before taking drug and for at least 1 hour after taking drug).
• Instruct patient to take drug with prednisone as prescribed and not to interrupt or stop either drug without consulting prescriber.
• Instruct patient to report joint or muscle discomfort, urinary or respiratory tract infection, urinating more frequently or during the night, dizziness on standing, extreme thirst, or weight loss.
☞ Advise pregnant women and women of childbearing age not to handle drug without wearing gloves.
• Advise male patient of child-producing age to use a condom and another effective contraceptive during therapy if having sex with a woman of childbearing potential.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and food mentioned above.
Lockerbie Bomber's cancer drugA popular term for an anti-androgenic agent which results in a 36% increase in average survival and reduced pain in men with advanced castration-resistant metastatic prostate cancer.
Joint swelling and discomfort, hypokalaemia, oedema, muscle discomfort, hypophosphataemia, hot flushing, diarrhoea, urinary tract infection, cough.