Abiraterone acetate oral
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Oral formulations of abiraterone
Drugs List
Therapeutic Indications
Uses
Metastatic castration-resistant prostate cancer
Metastatic hormone sensitive prostate cancer
Indicated for use with prednisone or prednisolone for the treatment of:
Newly diagnosed high risk metastatic hormone sensitive prostate cancer in combination with androgen deprivation therapy.
Metastatic castration-resistant prostate cancer where the disease has progressed on or after a docetaxel-based chemotherapy regimen.
Metastatic castration-resistant prostate cancer patients who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy where chemotherapy is not yet indicated.
Dosage
Whilst the doses stated below are those recommended by the manufacturer, local cancer network protocols for the relevant indication should be consulted.
Adults
Metastatic hormone sensitive prostate cancer: 1g once daily, taken with 5mg dose prednisone or prednisolone.
Metastatic castration-resistant prostate cancer: 1g once daily, taken with 10mg dose prednisone or prednisolone.
Additional Dosage Information
Hepatotoxicity
ALT or AST greater than 5 times ULN:
Interrupt treatment until liver function tests have returned to baseline; re-administer abiraterone acetate at a reduced dose of 500mg once daily.
If hepatotoxicity reoccurs at this reduced dose, treatment should be discontinued.
ALT or AST greater than 20 times ULN:
Discontinue treatment.
Grade 3 or greater toxicities
Suspend treatment and initiate appropriate medical management. Re-initiate once symptoms resolve to grade 1 or baseline.
Contraindications
Galactosaemia
Long QT syndrome
Severe hepatic impairment
Torsade de pointes
Uncontrolled hypertension
Precautions and Warnings
Family history of long QT syndrome
Fluid retention
Restricted sodium intake
Cardiac failure
Diabetes mellitus
Electrolyte imbalance
Glucose-galactose malabsorption syndrome
Hepatitis B
Hepatitis C
History of cardiovascular disorder
History of torsade de pointes
Hypertension
Lactose intolerance
Moderate hepatic impairment
Recent myocardial infarction
Severe angina
Severe renal impairment
Unstable angina
Ventricular arrhythmias
Consider supplementary corticosteroids if subject to stress or surgery
Contains more than 1 mmol (23 mg) sodium per dose
Control cardiac failure before starting treatment
Correct electrolyte disorders before treatment
Ensure hypertension is controlled prior to treatment
Treat concurrently with a corticosteroid
Treatment to be prescribed under the supervision of a specialist
Contains lactose
Advise patient to have no food for 2 hours before and 1 hour after dose
Consult local policy on the safe use of oral anti-cancer drugs
Staff: Not to be handled by pregnant staff
Correct hypokalaemia before treatment
Monitor serum transaminases before treatment
CCF risk: Monitor BP, serum K+ & fluid retention every 2 weeks for 3months
If hypokalaemia occurs, maintain serum potassium at or above 4 mmol/l
Monitor blood glucose closely in patients with diabetes mellitus
Monitor blood pressure, serum potassium and fluid retention monthly
Monitor ECG in patients at risk of QT prolongation
Monitor serum electrolytes
Monitor serum transaminases every 2 weeks for 3 months, then monthly
Consider discontinuing therapy if significant cardiac failure develops
May cause loss of bone mineral density
May affect results of some laboratory tests
Discontinue permanently if AST or ALT level exceeds 20 x ULN
Interrupt therapy if hepatic transaminases > 5 times upper limit of normal
Interrupt treatment for any grade 3 toxicity
Advise patient not to take St John's wort concurrently
Male: Additional contraception required in addition to barrier method
Male: Use of condoms advised if partner pregnant or may become pregnant
Patients previously treated with ketoconazole for prostate cancer may have a lower rate of response to abiraterone acetate.
Medical castration with LHRH analogue should be continued during treatment in patients not surgically castrated.
Before starting treatment, patients with a significant risk of congestive cardiac failure should be considered for an assessment of cardiac function (e.g. echocardiogram). Cardiac failure should be treated and cardiac function optimized. During treatment, blood pressure, serum potassium and fluid retention should be monitored every 2 weeks for the first 3 months and monthly thereafter.
Cases of myopathy and rhabdomyolysis have been reported within the first 6 months of treatment, and recovered after withdrawing treatment.
Cases of QT prolongation have been observed in patients experiencing hypokalaemia associated with abiraterone acetate.
Pregnancy and Lactation
Pregnancy
Abiraterone is not indicated for use in women.
Lactation
Abiraterone is not indicated for use in women.
Counselling
Advise patient if a dose of either abiraterone acetate, prednisone or prednisolone is missed, treatment should be resumed the following day with the usual daily dose.
Advise patient a condom is required if engaging in sexual activity with a pregnant woman. If engaging in sexual activity with a women of child bearing potential then a condom and another effective method of contraception is required.
Side Effects
Acute hepatic failure
Adrenal cortex insufficiency
Allergic alveolitis
Anaphylactic reaction
Angina pectoris
Arrhythmias
Atrial fibrillation
Cardiac failure
Congestive cardiac failure
Decreased ejection fraction
Diarrhoea
Dyspepsia
Fractures
Fulminant hepatitis
Haematuria
Hypertension
Hypertriglyceridaemia
Hypokalaemia
Increase in ALT level
Increase in AST level
Myocardial infarction
Myopathy
Peripheral oedema
Prolongation of QT interval
Rash
Rhabdomyolysis
Sepsis
Serum bilirubin increased
Tachycardia
Urinary tract infections
Ventricular dysfunction
Effects on Laboratory Tests
Spironolactone binds to the androgen receptor and may increase prostate specific antigen (PSA) levels.
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: September 2022
Reference Sources
Summary of Product Characteristics: Zytiga 500 mg film coated tablets. Janssen-Cilag Ltd. Revised December 2020.
Summary of Product Characteristics: Abiraterone 1000mg film-coated tablets. Sandoz Limited. Revised June 2021.
Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
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