Abiraterone Acetate

Name: Abiraterone Acetate

Stability

Storage

Oral

Tablets

20–25°C (may be exposed to 15–30°C).1

Uses of Abiraterone Acetate

  • It is used to treat prostate cancer.
  • It may be given to you for other reasons. Talk with the doctor.

What do I need to tell my doctor BEFORE I take Abiraterone Acetate?

  • If you have an allergy to abiraterone or any other part of abiraterone acetate.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you have any of these health problems: Liver disease or low potassium levels.
  • If you have high blood pressure.
  • If you are a woman. This medicine is not approved for use in women. If you are a woman using this medicine, talk with your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding.

This is not a list of all drugs or health problems that interact with abiraterone acetate.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

If OVERDOSE is suspected

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Brand Names U.S.

  • Zytiga

Off Label Uses

Prostate cancer, metastatic or high-risk locally advanced, castration-sensitive

Data from a large, multinational, randomized, controlled phase III study supports the use of abiraterone (in combination with prednisone and androgen-deprivation therapy [ADT]) in patients with newly diagnosed metastatic prostate cancer that is castration-sensitive.[Fizazi 2017] Data from a large, multicenter, randomized multi-stage phase II/III study also supports the use of abiraterone (in combination with prednisolone and long-term ADT) in patients with newly diagnosed metastatic or high-risk locally advanced prostate cancer.[James 2017]

Contraindications

Women who are or may become pregnant

Canadian labeling: Additional contraindication (not in the US labeling): Hypersensitivity to abiraterone acetate or any component of the formulation or container

Dosing Adjustment for Toxicity

Hepatotoxicity: Refer to Dosing: Hepatic Impairment.

Drug Interactions

Amodiaquine: CYP2C8 Inhibitors may increase the serum concentration of Amodiaquine. Avoid combination

Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Bosentan: CYP2C9 Inhibitors (Moderate) may increase the serum concentration of Bosentan. Management: Concomitant use of both a CYP2C9 inhibitor and a CYP3A inhibitor or a single agent that inhibits both enzymes with bosentan is likely to cause a large increase in serum concentrations of bosentan and is not recommended. See monograph for details. Monitor therapy

Cannabis: CYP2C9 Inhibitors (Moderate) may increase the serum concentration of Cannabis. More specifically, tetrahydrocannabinol serum concentrations may be increased. Monitor therapy

Choline C 11: Antiandrogens may diminish the therapeutic effect of Choline C 11. Monitor therapy

CloZAPine: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of CloZAPine. Monitor therapy

Codeine: CYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine. Monitor therapy

CYP1A2 Substrates: Abiraterone Acetate may increase the serum concentration of CYP1A2 Substrates. Monitor therapy

CYP2C8 Substrates: Abiraterone Acetate may increase the serum concentration of CYP2C8 Substrates. Monitor therapy

CYP2C9 Substrates: CYP2C9 Inhibitors (Moderate) may decrease the metabolism of CYP2C9 Substrates. Monitor therapy

CYP2D6 Substrates: Abiraterone Acetate may increase the serum concentration of CYP2D6 Substrates. Management: Avoid concurrent use of abiraterone with CYP2D6 substrates that have a narrow therapeutic index whenever possible. When concurrent use is not avoidable, monitor patients closely for signs/symptoms of toxicity. Consider therapy modification

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Abiraterone Acetate. Management: Avoid whenever possible. If such a combination cannot be avoided, increase abiraterone acetate dosing frequency from once daily to twice daily during concomitant use. Avoid combination

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

DOXOrubicin (Conventional): CYP2D6 Inhibitors (Moderate) may increase the serum concentration of DOXOrubicin (Conventional). Management: Seek alternatives to moderate CYP2D6 inhibitors in patients treated with doxorubicin whenever possible. One U.S. manufacturer (Pfizer Inc.) recommends that these combinations be avoided. Consider therapy modification

Dronabinol: CYP2C9 Inhibitors (Moderate) may increase the serum concentration of Dronabinol. Monitor therapy

Eliglustat: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Eliglustat. Management: Reduce the eliglustat dose to 84 mg daily. Avoid use of eliglustat in combination with a moderate CYP2D6 inhibitor and a strong or moderate CYP3A4 inhibitor. Consider therapy modification

Fesoterodine: CYP2D6 Inhibitors may increase serum concentrations of the active metabolite(s) of Fesoterodine. Monitor therapy

Indium 111 Capromab Pendetide: Antiandrogens may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Avoid combination

Metoprolol: CYP2D6 Inhibitors may increase the serum concentration of Metoprolol. Management: Consider an alternative for one of the interacting drugs in order to avoid metoprolol toxicity. If the combination must be used, monitor response to metoprolol closely. Metoprolol dose reductions may be necessary. Consider therapy modification

Nebivolol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Nebivolol. Monitor therapy

Perhexiline: CYP2D6 Inhibitors may increase the serum concentration of Perhexiline. Management: Consider alternatives to this combination if possible. If combined, monitor for increased perhexiline serum concentrations and toxicities (eg, hypoglycemia, neuropathy, liver dysfunction). Perhexiline dose reductions will likely be required. Consider therapy modification

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Spironolactone: May diminish the therapeutic effect of Abiraterone Acetate. Monitor therapy

St John's Wort: May decrease the serum concentration of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

Tamoxifen: CYP2D6 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Tamoxifen. Specifically, CYP2D6 inhibitors may decrease the metabolic formation of highly potent active metabolites. Management: Consider alternatives with less of an inhibitory effect on CYP2D6 activity when possible. Consider therapy modification

Tetrahydrocannabinol: CYP2C9 Inhibitors (Moderate) may increase the serum concentration of Tetrahydrocannabinol. Monitor therapy

Thioridazine: CYP2D6 Inhibitors may increase the serum concentration of Thioridazine. Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

TraMADol: CYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of TraMADol. These CYP2D6 inhibitors may prevent the metabolic conversion of tramadol to its active metabolite that accounts for much of its opioid-like effects. Monitor therapy

Monitoring Parameters

ALT, AST, and bilirubin prior to treatment, every 2 weeks for 3 months and monthly thereafter; if baseline moderate hepatic impairment (Child-Pugh class B), monitor ALT, AST, and bilirubin prior to treatment, weekly for the first month, every 2 weeks for 2 months then monthly thereafter. If hepatotoxicity develops during treatment (and only after therapy is interrupted and liver function tests have returned to safe levels), monitor ALT, AST, and bilirubin every 2 weeks for 3 months and monthly thereafter. Monitoring of testosterone levels is not necessary. Serum potassium (prior to treatment and at least monthly).

Monitor for signs and symptoms of adrenocorticoid insufficiency; if clinically indicated, consider appropriate diagnostics to confirm adrenal insufficiency. Monitor blood pressure and for fluid retention (prior to treatment and at least monthly). Monitor adherence.

Abiraterone acetate Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

  • Bladder pain
  • bloody or cloudy urine
  • blurred vision
  • body aches or pain
  • chills
  • cough
  • difficult, burning, or painful urination
  • dizziness
  • ear congestion
  • fainting
  • fast, slow, or irregular heartbeat
  • fever
  • frequent urge to urinate
  • headache
  • loss of voice
  • lower back or side pain
  • nasal congestion
  • nervousness
  • pounding in the ears
  • runny nose
  • slow or fast heartbeat
  • sneezing
  • sore throat
  • swelling
  • trouble breathing
  • unusual tiredness or weakness

Less common

  • Chest pain or discomfort
  • decreased urine output
  • dilated neck veins
  • extreme tiredness or weakness
  • irregular breathing
  • tightness in the chest
  • weight gain

Incidence not known

  • Clay-colored stools
  • dark urine
  • diarrhea
  • general feeling of discomfort or illness
  • itching, rash
  • loss of appetite
  • muscle cramp, spasm, pain, or stiffness
  • nausea
  • stomach pain, continuing
  • thickening of bronchial secretions
  • unpleasant breath odor
  • vomiting
  • vomiting of blood
  • yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Bruise
  • constipation
  • falls
  • feeling of warmth
  • fractures
  • groin pain
  • increased urge to urinate during the night
  • joint swelling or discomfort
  • redness of the face, neck, arms, and occasionally, upper chest
  • trouble sleeping
  • waking to urinate at night

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

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