From the Guidelines
Abiraterone acetate should be administered orally at a dose of 250 mg once daily, taken after a low-fat breakfast, or 1000 mg once daily, taken on an empty stomach, in combination with prednisone or methylprednisolone to prevent mineralocorticoid excess side effects. The choice of dose and administration method depends on the patient's ability to tolerate the medication and their financial situation, as the lower dose with food has been shown to be non-inferior to the standard dose on an empty stomach 1. The tablets should be swallowed whole with water and not crushed or chewed. Patients should continue taking abiraterone until disease progression or unacceptable toxicity occurs. Regular monitoring of liver function tests, serum potassium, blood pressure, and signs of fluid retention is necessary during treatment. Dose modifications may be required for patients with hepatic impairment or those experiencing toxicity. Abiraterone works by inhibiting CYP17, an enzyme required for androgen biosynthesis, thereby reducing testosterone levels and slowing prostate cancer growth. This medication is contraindicated in patients with severe hepatic impairment and requires caution in those with cardiovascular disease or a history of adrenal insufficiency.
Some key points to consider when administering abiraterone include:
- The importance of concurrent steroid administration to prevent mineralocorticoid excess side effects
- The need for regular monitoring of liver function, potassium and phosphate levels, and blood pressure readings
- The potential for dose modifications in patients with hepatic impairment or those experiencing toxicity
- The contraindication in patients with severe hepatic impairment and the need for caution in those with cardiovascular disease or a history of adrenal insufficiency
It is also important to note that the fine-particle formulation of abiraterone can be used as an alternative to the standard formulation, and that abiraterone can be given in combination with methylprednisolone instead of prednisone 1. However, the most recent and highest quality study recommends the use of abiraterone at a dose of 250 mg once daily, taken after a low-fat breakfast, or 1000 mg once daily, taken on an empty stomach, in combination with prednisone or methylprednisolone 1.
From the FDA Drug Label
The recommended dose of abiraterone acetate tablets is 1,000 mg (two 500 mg tablets or four 250 mg tablets) orally once daily with prednisone 5 mg orally twice daily. Abiraterone acetate tablets must be taken as a single dose once daily on an empty stomach. Do not eat food 2 hours before and 1 hour after taking abiraterone acetate tablets. The tablets must be swallowed whole with water. Do not crush or chew tablets.
The administration method for Abiraterone (Abiraterone acetate) is oral. The tablets should be taken once daily on an empty stomach, swallowed whole with water, and not crushed or chewed.
- Dose: 1,000 mg (two 500 mg tablets or four 250 mg tablets)
- Administration: Orally once daily
- Conditions: On an empty stomach, with prednisone 5 mg orally twice daily 2 2 2
From the Research
Administration Method
- Abiraterone acetate is administered orally 3
- The recommended Phase II dose of abiraterone acetate is 1000 mg orally daily in combination with prednisone 5 mg twice daily 3
Dosage and Combination Therapy
- Abiraterone is often prescribed with low-dose prednisone to suppress adrenocorticotropic hormone (ACTH) 4
- The addition of prednisone (10mg daily) to abiraterone was not able to prevent mineralocorticoid excess syndrome in many cases 5
- A study found that patients receiving 5 mg of prednisone twice daily had a statistically significant decrease in cumulative hazard for experiencing at least one mineralocorticoid excess syndrome event (hypertension and/or hypokalemia) 6
Management of Side Effects
- Mineralocorticoid excess symptoms can be managed with a selective mineralocorticoid antagonist, such as eplerenone, or low-dose corticosteroids 3
- Glucocorticoids and mineralocorticoid receptor (MR) antagonists can be used in the management of abiraterone-induced mineralocorticoid excess syndrome 5
- Amiloride is suggested for managing residual mineralocorticoid activity 4