abiraterone
Brand: Zytiga
(a- bir- a'ter- one)
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
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