Dosing & Uses
Dosage Forms & Strengths
tablet (Zytiga)
- 250mg
- 500mg
ultramicronized tablet (Yonsa)
- 125mg
Prostate Cancer
Metastatic castration-resistant prostate cancer
-
Zytiga
- Indicated in combination with prednisone for patients with metastatic castration-resistant prostate cancer (CRPC)
- 1000 mg (two 500-mg tablets or four 250-mg tablets) PO qDay with prednisone 5 mg PO q12hr
-
Yonsa
- Indicated in combination with methylprednisolone for the treatment of patients with metastatic CRPC
- 500 mg (four 125-mg tablets) PO qDay in combination with methylprednisolone 4 mg PO BID
Metastatic high-risk castration-sensitive prostate cancer
-
Zytiga
- Indicated in combination with prednisone for patients with metastatic high-risk castration-sensitive prostate cancer (CSPC)
- 1000 mg (two 500-mg tablets or four 250-mg tablets) PO qDay with prednisone 5 mg PO q12hr
Dosage Modifications
Strong CYP3A4 inducers
- Coadministration with strong CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital): Avoid if possible; if strong CYP3A4 inducer must be administered, increase abiraterone dosage frequency of abiraterone Reduce dose back to the previous dose and frequency, if the concomitant strong CYP3A4 inducer is discontinued
-
Yonsa
- Increase from 500 mg qDay to 500 mg BID
-
Zytiga
- Increase from 1000 mg qDay to 1000 mg BID
Hepatic impairment (Zytiga)
-
Baseline LFTs
- Mild (Child-Pugh A): No dosage adjustment necessary
- Moderate (Child-Pugh B): Reduce starting dose to 250 mg PO qDay; monitor ALT, AST, and bilirubin prior to start of treatment, qWeek for the first month, q2Weeks for the following 2 months of treatment and monthly thereafter
- If elevations in ALT and/or AST >5x ULN or total bilirubin >3x ULN occur in patients with baseline moderate hepatic impairment, discontinue abiraterone and do not retreat patients
- Severe (Child-Pugh C): Do not use
-
Increased LFTs during treatment
- ALT and/or AST >5x ULN or total bilirubin >3x ULN: Interrupt treatment; reinitiate at reduced dose of 750 mg PO qDay following return of LFTs to baseline or to AST/ALT ≤2.5x ULN and total bilirubin ≤1.5x ULN
- For patients who resume treatment, monitor serum transaminases and bilirubin at least q2Weeks for 3 months, and then monthly thereafter
- If hepatotoxicity recurs at 750 mg/day, may restart at 500 mg/day (after LFTs decrease as above)
- If hepatoxicity recurs at reduced dose of 500 mg/day, discontinue treatment
- Permanently discontinue treatment for patients who develop a concurrent elevation of ALT >3x ULN and total bilirubin >2x ULN in the absence of biliary obstruction or other causes responsible for the concurrent elevation
Hepatic impairment (Yonsa)
-
Baseline
- Moderate (Child-Pugh Class B): Reduce recommended dose to 125 mg PO qDay; monitor ALT, AST, and bilirubin prior to the start of treatment, every week for the first month, q2Weeks for the following 2 months of treatment and monthly thereafter
- If elevations in ALT and/or AST >5x ULN or total bilirubin >3x ULN occur in patients with baseline moderate hepatic impairment: Discontinue treatment and do not retreat patients with abiraterone
- Severe (Child-Pugh Class C): Do not use
-
Increased LFTs during treatment
- ALT and/or AST >5x ULN or total bilirubin >3x ULN): Interrupt treatment; restart at a reduced dose of 375 mg qDay following return of liver function tests to the patient’s baseline or to AST and ALT ≤2.5x ULN and total bilirubin ≤1.5x ULN
- For patients who resume treatment, monitor serum transaminases and bilirubin at least q2Weeks for 3 months, and then monthly thereafter
- If hepatotoxicity recurs on 375 mg/day, may be restart at a reduced dose of 250 mg/day (after LFTs decrease as above)
- If hepatotoxicity recurs 250 mg/day, discontinue treatment
- Permanently discontinue for patients who develop a concurrent elevation of ALT >3x ULN and total bilirubin >2x ULN in the absence of biliary obstruction or other causes responsible for the concurrent elevation
- Retreatment in patients who develop AST or ALT ≥20x ULN and/or bilirubin ≥10x ULN is unknown
Renal impairment
- Mild-to-severe: No dosage adjustment necessary
Dosing Considerations
Inform patients that Yonsa tablets are not interchangeable with other abiraterone acetate products
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (2)
- mavacamten
abiraterone will increase the level or effect of mavacamten by affecting hepatic enzyme CYP2C19 metabolism. Contraindicated. Strong or moderate CYP2C19 inhibitors may increase mavacamten systemic exposure, resulting in heart failure due to systolic dysfunction.
- ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)
abiraterone will increase the level or effect of ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) by decreasing metabolism. Contraindicated. Strong CYP2C8 inhibitors are shown to increase dasabuvir plasma concentrations (~10-fold), and therefore increase risk of QT prolongation
Serious - Use Alternative (11)
- apalutamide
apalutamide will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- bosutinib
abiraterone increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- edoxaban
abiraterone will increase the level or effect of edoxaban by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Dose adjustment may be required with strong P-gp inhibitors. DVT/PE treatment: Decrease dose to 30 mg PO once daily. NVAF: No dose reduction recommended
- ivosidenib
ivosidenib will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- metoclopramide intranasal
abiraterone will increase the level or effect of metoclopramide intranasal by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Concurrent use of metoclopramide intranasal and strong CYP2D6 inhibitors is not recommended since the metoclopramide intranasal dose cannot be adjusted.
- palifermin
palifermin increases toxicity of abiraterone by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- pomalidomide
abiraterone increases levels of pomalidomide by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- spironolactone
spironolactone increases toxicity of abiraterone by pharmacodynamic synergism. Contraindicated. Spironolactone binds to androgen receptor and may increase prostate-specific antigen (PSA) levels in abiraterone-treated prostate cancer patients.
- topotecan
abiraterone will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance
- tucatinib
abiraterone will increase the level or effect of tucatinib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of tucatinib (a CYP2C8 substrate) with a strong or moderate CYP2C8 inhibitors increases tucatinib plasma concentrations and risk of toxicities.
- venetoclax
abiraterone will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
Monitor Closely (117)
- amitriptyline
abiraterone increases levels of amitriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- amobarbital
amobarbital will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- amoxapine
abiraterone increases levels of amoxapine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- apalutamide
abiraterone will increase the level or effect of apalutamide by Other (see comment). Use Caution/Monitor. Coadministration of apalutamide with strong CYP2C8 inhibitors does not require initial dosage modification; however, dose reduction may be needed based on tolerability.
- aripiprazole
abiraterone increases levels of aripiprazole by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- atomoxetine
abiraterone increases levels of atomoxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Reduced initial doses of atomoxetine are recommended with strong CYP2D6 inhibitors.
- belzutifan
belzutifan will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.
- betaxolol
abiraterone increases levels of betaxolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- betrixaban
abiraterone increases levels of betrixaban by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Decrease betrixaban dose to 80 mg PO once, then 40 mg PO qDay if coadministered with a P-gp inhibitor.
- bosentan
bosentan decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- butabarbital
butabarbital will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- butalbital
butalbital will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cannabidiol
abiraterone will increase the level or effect of cannabidiol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the cannabidiol dose when coadministered with a moderate CYP2C19 inhibitor.
- captopril
abiraterone increases levels of captopril by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- carbamazepine
carbamazepine decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- carvedilol
abiraterone increases levels of carvedilol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- cenobamate
cenobamate will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- ceritinib
abiraterone increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- chlordiazepoxide
abiraterone increases levels of chlordiazepoxide by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- chloroquine
abiraterone increases levels of chloroquine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- chlorpromazine
abiraterone increases levels of chlorpromazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- cinacalcet
abiraterone increases levels of cinacalcet by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- citalopram
abiraterone increases levels of citalopram by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- clobazam
abiraterone will increase the level or effect of clobazam by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Dosage adjustment may be required; CYP2C19 inhibitors may result in increased exposure to N-desmethylclobazam (active metabolite).
- clomipramine
abiraterone increases levels of clomipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- codeine
abiraterone increases levels of codeine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- crizotinib
abiraterone increases levels of crizotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution should be exercised with concomitant use of moderate CYP3A inhibitors. .
- dabigatran
abiraterone will increase the level or effect of dabigatran by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Atrial fibrillation: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <30 mL/min. DVT/PE treatment: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <50 mL/min
- dabrafenib
dabrafenib decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- desipramine
abiraterone increases levels of desipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- deutetrabenazine
abiraterone will increase the level or effect of deutetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Strong CYP2D6 inhibitors increase the systemic exposure to the active dihydro-metabolites of deutetrabenazine by approximately 3-fold. Do not exceed 18 mg/dose and 36 mg/day of deutetrabenazine if coadministered with strong CYP2D6 inhibitors.
- dexamethasone
dexamethasone decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- dextroamphetamine transdermal
abiraterone will increase the level or effect of dextroamphetamine transdermal by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Initiate with lower doses and monitor patients for signs and symptoms of serotonin syndrome, particularly during dextroamphetamine initiation and after a dosage increase. If serotonin syndrome occurs, discontinue dextroamphetamine transdermal and CYP2D6 inhibitor.
- dextromethorphan
abiraterone increases levels of dextromethorphan by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- diazepam intranasal
abiraterone will increase the level or effect of diazepam intranasal by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Strong or moderate CYP2C19 inhibitors may decrease rate of diazepam elimination, thereby increasing adverse reactions to diazepam.
- dichlorphenamide
dichlorphenamide and abiraterone both decrease serum potassium. Use Caution/Monitor.
- doxepin
abiraterone increases levels of doxepin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- doxepin cream
abiraterone increases levels of doxepin cream by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- doxorubicin
abiraterone increases levels of doxorubicin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- doxorubicin liposomal
abiraterone increases levels of doxorubicin liposomal by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- duloxetine
abiraterone increases levels of duloxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- efavirenz
efavirenz decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- elagolix
elagolix will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.
- eluxadoline
abiraterone increases levels of eluxadoline by decreasing metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2C8 inhibitors.
- encorafenib
encorafenib, abiraterone. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- enzalutamide
enzalutamide decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily
- etravirine
etravirine decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- flecainide
abiraterone increases levels of flecainide by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- fluoxetine
abiraterone increases levels of fluoxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- fluphenazine
abiraterone increases levels of fluphenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- fluvoxamine
abiraterone will increase the level or effect of fluvoxamine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. If therapy cannot be avoided, exercise caution and consider a dose reduction of CYP2D6 substrate
- fosphenytoin
fosphenytoin decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- gallium Ga 68 PSMA-11
abiraterone will decrease the level or effect of gallium Ga 68 PSMA-11 by unspecified interaction mechanism. Modify Therapy/Monitor Closely. Androgen deprivation therapy and other therapies targeting the androgen pathway may result in changes in the uptake of gallium Ga 68 PSMA-11 in prostate cancer. The effect of ADT on the performance of gallium Ga 68 PSMA-11 is unknown.
- glecaprevir/pibrentasvir
abiraterone will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- haloperidol
abiraterone increases levels of haloperidol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- ifosfamide
abiraterone will decrease the level or effect of ifosfamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Use of a CYP3A4 inhibitor may decrease metabolism of ifosfamide, potentially reducing ifosfamide therapeutic effects.
- iloperidone
abiraterone increases levels of iloperidone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- imipramine
abiraterone increases levels of imipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- indacaterol, inhaled
indacaterol, inhaled, abiraterone. QTc interval. Use Caution/Monitor. Drugs that are known to prolong the QTc interval may have an increased the risk of ventricular arrhythmias.
- ivosidenib
abiraterone will increase the level or effect of ivosidenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration with moderate CYP3A4 inhibitors may increase ivosidenib plasma concentrations, thus increasing the risk of QTc prolongation. Monitor for increased risk of QTc interval prolongation.
- lenacapavir
lenacapavir will increase the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- lofexidine
abiraterone will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.
- lorlatinib
lorlatinib will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- maprotiline
abiraterone increases levels of maprotiline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- metaxalone
abiraterone increases levels of metaxalone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- methamphetamine
abiraterone increases levels of methamphetamine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- methohexital
methohexital will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- metoprolol
abiraterone increases levels of metoprolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- mexiletine
abiraterone increases levels of mexiletine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- mirtazapine
abiraterone increases levels of mirtazapine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- mitotane
mitotane decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.
- nafcillin
nafcillin decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- naldemedine
abiraterone increases levels of naldemedine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor naldemedine for potential adverse effects if coadministered with P-gp inhibitors.
- nebivolol
abiraterone increases levels of nebivolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- nevirapine
nevirapine decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- nintedanib
abiraterone increases levels of nintedanib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. If nintedanib adverse effects occur, management may require interruption, dose reduction, or discontinuation of therapy .
- nortriptyline
abiraterone increases levels of nortriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- oliceridine
abiraterone will increase the level or effect of oliceridine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If concomitant use is necessary, may require less frequent oliceridine dosing. Closely monitor for respiratory depression and sedation and titrate subsequent doses accordingly. If inhibitor is discontinued, consider increase oliceridine dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal.
- olodaterol inhaled
abiraterone and olodaterol inhaled both increase QTc interval. Use Caution/Monitor. Drugs that prolong the QTc interval and may potentiate the effects of beta2 agonists on the cardiovascular system; increased risk of ventricular arrhythmias
- oxcarbazepine
oxcarbazepine decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- paroxetine
abiraterone increases levels of paroxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- pentobarbital
pentobarbital will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- perphenazine
abiraterone increases levels of perphenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- phenobarbital
phenobarbital decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- phenytoin
phenytoin decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- pindolol
abiraterone increases levels of pindolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- pitolisant
abiraterone will increase the level or effect of pitolisant by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If coadministered with strong CYP2D6 inhibitors, initiate pitolisant at 8.9 mg/day and increase after 7 days to maximum of 17.8 mg/day. For patients currently taking pitolisant, reduce pitolisant dose by half upon initiating strong CYP2D6 inhibitors.
- primidone
primidone decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- procainamide
abiraterone increases levels of procainamide by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- promethazine
abiraterone increases levels of promethazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- propafenone
abiraterone increases levels of propafenone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- propranolol
abiraterone increases levels of propranolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- protriptyline
abiraterone increases levels of protriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- rifabutin
rifabutin decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- rifampin
rifampin decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- rifapentine
rifapentine decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- rifaximin
abiraterone increases levels of rifaximin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- risperidone
abiraterone increases levels of risperidone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- secobarbital
secobarbital will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- selexipag
abiraterone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- sertraline
abiraterone increases levels of sertraline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- siponimod
siponimod and abiraterone both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- St John's Wort
St John's Wort decreases levels of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of abiraterone with strong CYP3A4 inducers; if a strong CYP3A4 inducer must be used, increase abiraterone dosage frequency from once daily to twice daily.
- stiripentol
stiripentol, abiraterone. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
- tamoxifen
abiraterone, tamoxifen. affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. CYP2D6 inhibition decreases metabolism of tamoxifen to hydroxytamoxifen, and N-desmethyl tamoxifen to endoxifen (active metabolites with 100-fold greater affinity for estrogen receptor); decreased endoxifen levels may result in poor clinical outcome.
- tamsulosin
abiraterone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- tazemetostat
tazemetostat will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- teniposide
abiraterone will increase the level or effect of teniposide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tetrabenazine
abiraterone increases levels of tetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- thioridazine
abiraterone increases levels of thioridazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- tolterodine
abiraterone increases levels of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- tramadol
abiraterone increases levels of tramadol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider increasing tramadol dose if clinically appropriate; if abiraterone is discontinued, consider reducing tramadol dose and frequently monitor for signs of respiratory depression and sedation.
- trimipramine
abiraterone increases levels of trimipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
- vemurafenib
abiraterone increases levels of vemurafenib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- venlafaxine
abiraterone increases levels of venlafaxine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.
Minor (4)
- acetazolamide
acetazolamide will increase the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
Adverse drug reactions are for abiraterone with prednisone
>10% (All grades)
Hypertriglyceridemia (63%)
Hyperglycemia, nonfasting (57%)
Increased ALT (11-46%)
Fatigue (39%)
Lymphopenia (20-38%)
Increased AST (15-37%)
Hypertension (8.5-37%)
Hypernatremia (33%)
Joint swelling/discomfort (30%)
Hypokalemia (17-30%)
Edema (25-27%)
Muscle discomfort (26%)
Hypophosphatemia (24%)
Constipation (23%)
Hot flush (15-22%)
Diarrhea (18-22%)
Hot flush (19%)
Cough (6.5-17%)
Increased total bilirubin (6.6-16%)
Insomnia (14%)
Contusion (13%)
Upper respiratory tract infection (5.4-13%)
Urinary tract infection (7-12%)
Dyspnea (12%)
Nasopharyngitis (11%)
Dyspepsia (6.1-11%)
>10% (Grade 3 or 4)
Hypertension (1.3-20%)
1-10%
All grades
- Hematuria (10%)
- Pyrexia (8.7%)
- Rash (8.1%)
- Headache (7.5%)
- Urinary frequency (7.2%)
- Arrhythmia (7.2%)
- Groin pain (6.6%)
- Nocturia (6.2%)
- Falls (5.9%)
- Fractures (5.9%)
- Chest pain or chest discomfort (3.8%)
- Cardiac failure (2.3%)
Grade 3 or 4
- Lymphopenia (4.1-8.7%)
- Hypophosphatemia (7.2%)
- Hyperglycemia, nonfasting (6.5%)
- Increased ALT (1.4-6.1%)
- Hypokalemia (2.8-10%)
- Increased AST (2.1-4.4%)
- Joint swelling/discomfort (2-4.2%)
- Muscle discomfort (3%)
- Dyspnea (2.4%)
- Fatigue (2.2%)
- Urinary tract infection (1-2.1%)
- Edema or cardiac failure(1.9%)
- Fractures (1.4%)
- Hematuria (1.3%)
- Arrhythmias (1.1%)
<1%
Grade 3 or 4
- Diarrhea (0.6-0.9%)
- Pyrexia (0.6%)
- Chest pain or discomfort (0.5%)
- Hypertriglyceridemia (0.4%)
- Groin pain (0.4%)
- Constipation (0.4%)
- Edema (0.4%)
- Hyponatremia (0.4%)
- Urinary frequency (0.3%)
- Hot flush (0.2-0.3%)
- Headache (0.3%)
- Upper respiratory tract (0.2%)
- Insomnia (0.2%)
- Increased total bilirubin (0.1-0.2%)
Postmarketing Reports
Respiratory, thoracic and mediastinal disorders: Noninfectious pneumonitis
Musculoskeletal and connective tissue disorders: Myopathy, including rhabdomyolysis
Hepatobiliary disorders: Fulminant hepatitis, including acute hepatic failure and death
Immune system disorders: Hypersensitivity, anaphylactic reactions (severe allergic reactions including difficulty swallowing or breathing, swollen face, lips, tongue or throat, or an itchy rash
Warnings
Contraindications
None
Cautions
Caution in patients with a history of cardiovascular disease; safety in patients with LVEF <50% or NYHA Class III or IV heart failure is not established
Hypertension, hypokalemia, and fluid retention may result from increased mineralocorticoid due to CYP17 inhibition; control hypertension and correct hypokalemia before treatment; monitor blood pressure, serum potassium, and symptoms of fluid retention at least monthly
Closely monitor patients with medical conditions that might be compromised by increased blood pressure, hypokalemia, or fluid retention (eg, heart failure, recent MI, cardiovascular disease, ventricular arrhythmia)
QT prolongation and Torsades de Pointes observed in patients who develop hypokalemia during postmarketing surveillance and additional clinical trials
Adrenocortical insufficiency reported in patients receiving abiraterone in combination with prednisone, following interruption of daily steroids and/or with concurrent infection or stress; monitor for symptoms and signs of adrenocortical insufficiency; increased corticosteroid dosage may be indicated before, during, and after stressful situations; concurrent infection or interruption of daily corticosteroids associated with adrenocortical insufficiency
In postmarketing experience, severe hepatic toxicity, including fulminant hepatitis, acute liver failure and deaths occurred
Drug plus prednisone/prednisolone not recommended for use in combination with radium 223 dichloride outside clinical trials; increased incidences of fractures (and deaths observed in patients who received drug plus prednisone/prednisolone in combination with radium Ra 223 dichloride compared to placebo in combination with drug plus prednisone/prednisolone
Based on animal studies and mechanism of action, may cause fetal harm and loss of pregnancy
Drug interactions overview
- See Dosage Modifications
-
Drugs that inhibit or induce CYP3A4
- Strong CYP3A4 inducers (eg, rifampin) decreased systemic exposure of abiraterone; avoid coadministration; if unable to avoid, increase abiraterone dose frequency; reduce dose back to previous dose and frequency, if concomitant strong CYP3A4 inducer is discontinued
- Ketoconazole, a strong CYP3A4 inhibitor, had no clinically meaningful effect when coadministered with abiraterone
-
Effects of abiraterone on drug metabolizing enzyme
- Abiraterone inhibits CYP2D6 and CYP2C8
- In a CYP2D6 drug-drug interaction trial, peak plasma concentration and AUC of dextromethorphan (CYP2D6 substrate) were increased 2.8- and 2.9-fold, respectively, when dextromethorphan was given with abiraterone acetate 1,000 mg qDay and prednisone 5 mg PO BID
- In a CYP2C8 drug-drug interaction trial in healthy subjects, the AUC of pioglitazone (CYP2C8 substrate) was increased by 46% when pioglitazone was coadministered with a single dose of 1,000 mg abiraterone
- Avoid coadministration with substrates of CYP2D6 with a narrow therapeutic index (eg, thioridazine); if alternative treatments cannot be used, consider a dose reduction of the concomitant CYP2D6 substrate drug
- Closely monitor for signs of toxicity related to a CYP2C8 substrate with a narrow therapeutic index if used concomitantly with abiraterone
- Severe hypoglycemia has been reported when administered to patients with pre-existing diabetes receiving medications containing thiazolidinediones (including pioglitazone) or repaglinide; monitor blood glucose in patients with diabetes during and after discontinuation of treatment; assess if antidiabetic drug dosage needs to be adjusted to minimize risk of hypoglycemia
Pregnancy & Lactation
Pregnancy
Based on findings from animal studies and mechanism of action, abiraterone is contraindicated for use in pregnant women because drug can cause fetal harm and potential loss of pregnancy
Not indicated for use in females
There are no human data regarding use in pregnant women
In animal reproduction studies, oral administration of abiraterone acetate to pregnant rats during organogenesis caused adverse developmental effects at maternal exposures ~≥0.03 times the human exposure (AUC) at the recommended dose
Contraception
- Advise males with female partners of reproductive potential to use effective contraception during treatment and for 3 weeks after the final dose of abiraterone
Infertility
- Based on animal studies, may impair reproductive function and fertility in males of reproductive potential
Lactation
Not indicated for women
No information available on the presence of abiraterone acetate in human milk, or on the effects on the breastfed child or milk production
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Androgen biosynthesis inhibitor that inhibits 17 alpha-hydroxylase/C17, 20-lyase (CYP17); this enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis
Inhibition of CYP17 by abiraterone can also result in increased mineralocorticoid production by the adrenal glands
Absorption
Peak plasma time: 2 hr
Peak plasma concentration
- Zytiga: 226 ng/mL ng/mL (at steady state); increases up to 17-fold when administered with high-fat meal
- Yonsa: 73 ng/mL (single-dose); increases up to 6.5-fold when administered with high-fat meal
AUC
- Zytiga: 993 ng·hr/mL (at steady state); increases up to 10-fold when administered with high-fat meal
- Yonsa: 373 ng·hr/mL (single dose); increases up to 4.4-fold when administered with high-fat meal
Distribution
Protein bound: >99% (albumin, alpha-1 acid glycoprotein)
Vd: 19,669 L (at steady state)
P-glycoprotein (P-gp) inhibitor
Metabolism
Hydrolyzed to abiraterone (active metabolite); hydrolysis is likely via esterase activity and is not CYP mediated
CYP3A4 and SULT2A1 enzymes are involved in the formation of 2 inactive metabolites, N-oxide abiraterone sulphate and abiraterone sulphate
Strong inhibitor of CYP1A2 and CYP2D6; moderate inhibitor of CYP2C9, CYP2C19, and CYP3A4
Excretion
Excretion: Feces (88%), urine (5%)
Half-life: 12 hr (prolonged by hepatic impairment to 18-19 hr)
Administration
Oral Administration
Patients receiving abiraterone should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy
Swallow tablets whole with water; do not chew, crush, or split
Zytiga
- Take once daily in combination with prednisone
- Must take on empty stomach; do not eat food 2 hr before and 1 hr after taking medication
Yonsa
- Take once daily with methylprednisone twice daily
- Take with or without food
Missed dose
- If patient misses a dose of abiraterone or corticosteroid (ie, methylprednisolone or prednisone), take normal dose the following day
- If more than one dose per day is skipped, contact healthcare provider
Storage
Tablet: Store at 20-25°C (68-77°F); excursions permitted in the range from 15-30°C (59-86°F)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| abiraterone oral - | 250 mg tablet |  | |
| abiraterone oral - | 250 mg tablet |  | |
| abiraterone oral - | 250 mg tablet |  | |
| abiraterone oral - | 250 mg tablet |  | |
| abiraterone oral - | 500 mg tablet |  | |
| abiraterone oral - | 250 mg tablet |  | |
| abiraterone oral - | 250 mg tablet |  | |
| abiraterone oral - | 250 mg tablet |  | |
| abiraterone oral - | 250 mg tablet |  | |
| Zytiga oral - | 500 mg tablet |  | |
| Zytiga oral - | 250 mg tablet | |
Copyright © 2010 First DataBank, Inc.
Patient Handout
abiraterone oral
ABIRATERONE - ORAL
(A-bir-A-ter-one)
COMMON BRAND NAME(S): Zytiga
USES: This medication is used to treat prostate cancer. Abiraterone belongs to a class of drugs known as anti-androgens (anti-testosterone). Testosterone, a natural hormone, helps prostate cancer to grow and spread. Abiraterone works by blocking the production of testosterone, thereby slowing the growth and spread of prostate cancer.This medication should not be given to women or children.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking abiraterone and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Different brands of this medication may have different dosing directions. Do not change brands of this medication without your doctor's direction.Take this medication by mouth on an empty stomach (at least 1 hour before or 2 hours after food) as directed by your doctor, usually once daily. Taking abiraterone with food greatly increases the amount of this drug in your body and increases the risk of side effects. Swallow the tablets whole. Do not crush or chew the tablets.The dosage is based on your medical condition, lab results, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. Do not stop any medications for your prostate cancer unless told to do so by your doctor. Stopping your medications could allow the cancer to spread more rapidly.Tell your doctor if your condition lasts or gets worse (such as urination becomes more difficult, bone pain increases).Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.
SIDE EFFECTS: Headache, hot flushes, joint pain, heartburn or cold-like symptoms may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high. Your doctor may control your blood pressure with medication.Tell your doctor right away if you have any serious side effects, including: increased urination, painful urination, muscle cramps/weakness, leg pain, swelling in legs/feet, bone fractures.Get medical help right away if you have any very serious side effects, including: chest pain, feeling short of breath while at rest, fast/irregular heartbeat, severe dizziness, fainting, symptoms of liver disease (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking abiraterone, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: previous heart attack, high blood pressure, liver problems, diabetes.Abiraterone may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using abiraterone, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using abiraterone safely.Using corticosteroid medications for a long time along with abiraterone can make it more difficult for your body to respond to physical stress. Before having surgery or emergency treatment, or if you get a serious illness/injury, tell your doctor or dentist that you are using this medication or have used this medication within the past 12 months. Tell your doctor right away if you develop unusual/extreme tiredness or weight loss. If you will be using this medication for a long time, carry a warning card or medical ID bracelet that identifies your use of this medication.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).This medication should not be used by women, especially during pregnancy or breast-feeding. It may harm an unborn or breast-feeding baby. Men with female partners of childbearing age should use reliable form(s) of birth control while taking this medication and for at least 3 weeks after stopping treatment. Consult your doctor for more details.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.A product that may interact with this drug is: radium Ra 223.Other medications can affect the removal of abiraterone from your body, which may affect how abiraterone works. Examples include drugs used to treat seizures (such as carbamazepine, phenytoin, phenobarbital, primidone), St. John's wort, among others.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as blood pressure, potassium levels, liver function, blood PSA test) should be done before you start taking this medication and while you are taking it. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up. If you miss more than one dose, talk to your doctor right away.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised January 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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- View the formulary and any restrictions for each plan.
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