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(a-bi-ra-te-rone) ,


(trade name)


Therapeutic: antineoplastics
Pharmacologic: enzyme inhibitors
Pregnancy Category: X


With prednisone in the treatment of metastatic castration-resistant prostate cancer.


Inhibits the enzyme 17α-hydroxylase/C17,20–lyase, which is required for androgen production. May also result in increased mineralocortocoid production.

Therapeutic effects

Decreased androgen production with decreased spread of androgen-sensitive prostate cancer.


Absorption: Hydrolyzed to its active compound following oral administration.
Distribution: Unknown.
Protein Binding: >99%.
Metabolism and Excretion: Metabolized by esterases to inactive compounds; eliminated primarily in feces as unchanged drug and metabolites; 5% excreted in urine.
Half-life: 12 hr.

Time/action profile (blood level)

POunknown2 hr 12 hr


Contraindicated in: Severe hepatic impairment (Child-Pugh Class C); Obstetric: Pregnancy or potential to become pregnant (may cause fetal harm); Lactation: Lactation.
Use Cautiously in: Cardiovascular disease (safety not established if LVEF <50% or NYHA Class III or IV heart failure;Recent myocardial infarctionVentricular arrhythmiasElectrolyte abnormalities or hypertension (correct/treat prior to initiation);Pre-existing liver disease (dose modification required for Child-Pugh Class B);Stress, infection, trauma, acute disease process (may result in adrenocortical insufficiency requiring additional corticosteroids).

Adverse Reactions/Side Effects

Noted for combination treatment with prednisone


  • cough


  • arrhythmia
  • edema
  • hypertension


  • hepatotoxicity (life-threatening)
  • diarrhea
  • dyspepsia


  • hot flush


  • adrenocortical insufficiency (due to concurrent prednisone)

Fluid and Electrolyte

  • hypokalemia


  • nocturia
  • urinary frequency


  • fracture
  • joint pain/discomfort


Drug-Drug interaction

Acts as an inhibitor of the CYP2D6 enzyme system; avoid concurrent use with agents that are substrates of CYP2D6, especially those with narrow therapeutic indices, including thioridazine and dextromethorphan; if concurrent use is necessary, dosage ↓ of substrate may be required. Abiraterone is a substrate of the CYP3A4 enzyme system. Concurrent use of strong CYP3A4 inducers including carbamazepine, phenobarbital, phenytoin, rifabutin, rifapentine, or rifampin should be avoided or undertaken with caution.


Oral (Adults) 1000 mg once daily used in combination with 5 mg prednisone twice daily; Concurrent use of strong CYP3A4 inducer—1000 mg twice daily.

Hepatic Impairment

Oral (Adults) Child-Pugh Class B—250 mg once daily with 5 mg prednisone twice daily.


Tablets: 250 mg

Nursing implications

Nursing assessment

  • Monitor BP and assess for fluid retention at least monthly. Control hypertension during therapy.
  • Monitor for signs and symptoms of adrenocortical insufficiency (hypotension, weight loss, weakness, nausea, vomiting, anorexia, lethargy, confusion, restlessness), especially in patients under stress or who are withdrawn from or have decreased prednisone dose. Symptoms may be masked by abiraterone.
  • Lab Test Considerations: Monitor AST, ALT, and bilirubin prior to, every 2 wks for 3 mo, and monthly thereafter. If AST and/or ALT ↑ >5 times upper limit of normal or bilirubin ↑ >3 times upper limit of normal in patients with baseline moderate hepatic impairment, interrupt abiraterone. Following return of liver function to baseline or AST and ALT ↑ >2.5 times upper limit of normal or bilirubin ↑ >1.5 times upper limit of normal may re-start at a reduced dose of 750 mg once daily. Monitor serum transaminases and bilirubin every 2 wks for 3 mo and monthly thereafter. If hepatotoxicity recurs, may restart at 500 mg once daily following return to baseline or AST and ALT ↑ >2.5 times upper limit of normal or bilirubin ↑ >1.5 times upper limit of normal. If hepatotoxicity recurs at 500 mg dose, discontinue therapy.
    • Monitor serum potassium and sodium at least monthly during therapy. May cause hypokalemia; control during therapy.
    • May cause ↑ triglycerides and ↓ phosphorous.

Potential Nursing Diagnoses

Activity intolerance


  • Control hypertension and correct hypokalemia prior to starting therapy.
  • Oral: Administer twice daily with prednisone on an empty stomach at least 2 hrs before or 1 hr after meals; food increases absorption. Swallow tablets whole with water; do not crush, break, or chew.

Patient/Family Teaching

  • Instruct patient to take medication as directed and not to stop abiraterone or prednisone without consulting health care professional. If a dose is missed, take the following day. If more than 1 dose is missed, consult health care professional. Do not share medication with others, even if they have the same symptoms; may be dangerous.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Advise patient to notify health care professional of side effects that are bothersome or persistent.
  • Advise female patient to use effective contraception during therapy and for 1 wk after therapy and to notify health care professional immediately of pregnancy is suspected or if breast feeding. Male patients should use a condom and another form of contraception during sex with a women of child-bearing potential during and for 1 wk after therapy. Pregnant women should not touch the tablets without wearing gloves.
  • Explain need for continued follow-up exams and lab tests to assess possible side effects.

Evaluation/Desired Outcomes

  • Decreased spread of androgen-sensitive prostate cancer.
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References in periodicals archive ?
In the Phase 1/2 clinical trial, ESSA intends to demonstrate the safety, tolerability, maximum tolerated-dose, pharmacokinetics, and efficacy of EPI-506 in prostate cancer patients who have failed abiraterone or enzalutamide or both, the current standard-of-care drugs in mCRPC.
We have summarized the Systemic Therapy in Advanced or Metastatic Prostate Cancer: Evaluation of Drug Efficacy--Androgen Suppression-Based Therapy Alone or Combined With Zoledronic Acid, Docetaxel, Prednisolone, Celecoxib, Abiraterone, Enzalutamide and/or Radiotherapy in Treating Patients With Locally Advanced or Metastatic Prostate Cancer (STAMPEDE) and Phase III Randomized Study of Adjuvant Radiotherapy With Versus Without Concurrent Goserelin in Patients Who Have Undergone Surgery for Recurrent or Refractory Prostate Cancer CGETUG) trials providing further evidence of the benefit of early docetaxel added to hormone therapy in advanced prostate cancer.
The Scottish Medicines Consortium rejected pleas for the drug abiraterone to be approved for use before chemotherapy.
He was previously prescribed abiraterone in yet another attempt to fight the disease, but he was unaware that this would later deem him ineligible for NHS access to enzalutamide.
Experts from The Institute of Cancer Research said abiraterone should be offered before they undergo chemo.
Previous draft guidance sparked an outcry when Nice said it should be recommended, but stipulated patients could take it only if they had not previously used the drug abiraterone.
Nice chief executive Sir Andrew Dillon said: "Clinical specialists told the committee that radium-223 would be used as an alternative treatment option to docetaxel as an initial treatment, and abiraterone as a second-line treatment when the disease has progressed.
In January, Nice, which vets the cost-effectiveness of NHS treatments, published draft guidance saying men should not qualify for the medicine if they have previously been treated with another prostate cancer drug, abiraterone.
This trend continued in 2011 and 2012, when 3 therapies, the CYP17 inhibitor abiraterone acetate (Zytiga; Janssen Biotech) (7), the bone-targeting agent [sup.
The Institute of Cancer Research, London, and its partner hospital The Royal Marsden NHS Foundation Trust jointly led the new Phase III trial of enzalutamide and the Phase III trials of two other drugs, cabazitaxel and abiraterone.
COLNE Valley MP Jason McCartney has welcomed an announcement by the National Institute for Health and Clinical Excellence that the breakthrough prostate cancer drug - abiraterone - will now be made available on the NHS.
The medication, abiraterone acetate -- marketed as Zytiga -- also delayed the development of pain and deterioration of the patients' overall condition.