Updated May 30, 2026, 4:23 PM
Androgen inhibitorUS FDA Database Verified

abiraterone

Brand: Zytiga

(a- bir- a'ter- one)

Pregnancy Category: X

Pharmacological Action

Converted to abiraterone, which inhibits CYP17, the enzyme required for androgen biosynthesis; androgen- sensitive prostate cancer responds to treatment that decreases androgens

Therapeutic outcome: Decreases spread of malignancy

Uses

Metastatic castration- resistant prostate cancer in combination with prednisone in patients who have received prior chemotherapy containing docetaxel

Contraindications

Pregnancy (X), women, children

Precautions: Adrenal insufficiency, cardiac disease, MI, heart failure, hepatic disease, hypertension, hypokalemia, infection, surgery, ventricular dysrhythmia

Dosage & Routes

Adult

Males: PO 1000 mg q day with predniSONE 5 mg bid Hepatic dose Adult

Males: (Child- Pugh B, 7- 9) PO 250 mg q day with predniSONE; (Child- Pugh C, >10 do not use

Available forms: Tab 250 mg

Implementation Give whole, on empty stomach two hrs before or 1 hr after meals with full glass of water Women who are pregnant or may become pregnant should not touch tabs without gloves Storage of tabs at room temperature

Adverse Effects

CV: Angina, dysrhythmia exacerbation, atrial flutter/fibrillation/tachycardia, AV block, chest pain, edema, heart failure, MI, hypertension, QT prolongation, sinus tachycardia, supraventricular tachycardia, ventricular tachycardia

ENDO: Hot flashes

GI: Diarrhea, dyspepsia

GU: Increased urinary frequency, nocturia, urinary tract infection

META: Adrenocortical insufficiency, hyperbilirubinemia, hypertriglyceridemia, hypokalemia, hypophosphatemia

MS: Arthralgia, myalgia

RESP: Cough, upper respiratory infection

SYST: Infection

Pharmacokinetics

Absorption: Food increases effect; give on empty stomach; increased effect in hepatic disease

Distribution: 99% protein binding

Metabolism: Converted to abiraterone (active metabolite)

Excretion: 88% (feces), 5% (urine)

Half-life: Mean terminal half-life 7-17 hr

Pharmacodynamics

Onset: Unknown

Peak: Unknown

Duration: Unknown

Interactions

Drug classifications CYP3 A4 inhibitors (clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole, ketoconazole, itraconazole); CYP3 A4 inducers (carBAMazepine, phenytoin, rifampin, rifabutin, rifapentine, PHENobarbital): avoid use with this product CYP2 D6 substrate (dextromethorphan, thioridazine): increased action of these products; dose of these products should be reduced

Nursing Considerations

Assessment Monitor prostate specific antigen (PSA), serum potassium, serum bilirubin Monitor liver function tests (AST/ALT) baseline and every 2 wk for 3 mo and monthly thereafter in those with no known hepatic disease; interrupt treatment in patients without known hepatic disease at baseline who develop ALT/AST >5 times ULN or total bilirubin >3 times ULN; in baseline moderate hepatic disease, measure ALT, AST, and bilirubin before the start of treatment, every week for the first month, every 2 weeks for the following 2 months, and monthly thereafter; if elevations in ALT and/or AST >5 times ULN or total bilirubin >3 times ULN occur in patients with baseline moderate hepatic impairment, discontinue and do NOT restart. Measure serum total bilirubin, AST, and ALT if hepatotoxicity is suspected. Elevations of AST, ALT, bilirubin from baseline should prompt more frequent monitoring. Monitor musculoskeletal pain, joint swelling, discomfort: Arthritis, arthralgia, joint swelling, and joint stiffness, some severe. Muscle discomfort that included muscle spasms, musculoskeletal pain, myalgia, musculoskeletal discomfort, and musculoskeletal stiffness may be relieved with analgesics Assess for signs and symptoms of adrenocorticoid insufficiency; monthly for hypertension, hypokalemia, and fluid retention Monitor ECG for QT prolongation, ejection fraction in those with cardiac disease, small increases in the QTc interval such as < 10 ms have occurred; monitor for arrhythmia exacerbation such as sinus tachycardia, atrial fibrillation, supraventricular tachycardia (SVT), atrial tachycardia, ventricular tachycardia, atrial flutter, bradycardia, AV block complete, conduction disorder, and bradyarrhythmia

Patient/family education Teach patient that women must not come in contact with tabs, wear gloves if product needs to be handled, pregnancy (X) Instruct patient to report chest pain, swelling of joints, burning/pain when urinating

Evaluation

Positive therapeutic outcome: Decrease in B/P

Reference

Mosby's Drug Guide; Davis Drug Guide

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