Description

Abiret Tablet: Each tablet contains Abiraterone Acetate USP 250mg Tablet.

 

Product Features

Product Name	:	Abiret
Generic Name	:	Abiraterone
Formulation	:	Tablet
Available Pack Size	:	120’s Pot
Available Strength	:	250 mg
Registrations	:	Export Only

 

How does abiraterone work?

Abiraterone drug works by inhibiting an enzyme called 17 α-hydroxylase/C17, 20-lyase (CYP17). This enzyme is found in testicular, adrenal, and prostatic tumor tissues and plays a crucial role in androgen production.

 

Specifically, CYP17 facilitates two consecutive reactions: firstly, the conversion of pregnenolone and progesterone into their 17 α-hydroxy derivatives via 17α-hydroxylase activity, and secondly, the subsequent formation of dehydroepiandrosterone (DHEA) and androstenedione through C17, 20 lyase activity.

 

These compounds, DHEA and androstenedione, serve as precursors to testosterone. Abiraterone’s inhibition of CYP17 can lead to increased production of mineralocorticoids by the adrenals.

 

Prostate cancer thrives on androgens. Abiraterone Acetate 250 mg reduces androgen levels effectively, unlike conventional therapies which mainly target testicular androgen production. Abiraterone cuts both testicular and adrenal androgen production. Monitoring testosterone levels isn’t needed during Abiraterone 250 mg treatment, but changes in PSA levels may not always reflect clinical benefits for each patient.

 

Abiraterone acetate side effects

The most common adverse reactions are fatigue, arthralgia, hypertension, nausea, edema, hypokalemia, hot flush, diarrhea, vomiting, upper respiratory infection, cough, and headache.

 

Dosage and Administration

For metastatic castration-resistant prostate cancer (CRPC), doctors typically prescribe 1,000 mg of Abiraterone Acetate orally once daily, in addition to 5 mg of Prednisone orally twice daily.

 

Similarly, for metastatic high-risk castration-sensitive prostate cancer (CSPC), the recommended daily dose of Abiraterone Acetate is 1,000 mg, along with 5 mg of Prednisone orally once a day.

 

Important Instruction

Patients taking Abiraterone Drug should also be receiving a gonadotropin-releasing hormone (GnRH) analog simultaneously or should have undergone bilateral orchiectomy. It’s essential to take Abiraterone Acetate on an empty stomach, either at least one hour before or at least two hours after eating. The tablets must be swallowed whole with water and should not be crushed or chewed.

 

Abiraterone 250 mg Drug Interactions

Abiraterone Acetate interacts with CYP3A4 enzymes. Rifampin, a strong inducer of CYP3A4, reduces Abiraterone 250 mg exposure by 55%. Avoid strong CYP3A4 inducers during treatment; if necessary, increase Abiraterone dose frequency. Ketoconazole, a strong CYP3A4 inhibitor, has no significant effect on Abiraterone pharmacokinetics.

 

Abiraterone inhibits CYP2D6 and CYP2C8 enzymes. Co-administration with CYP2D6 substrates like Thioridazine increases their levels substantially, warranting caution or alternative treatments. Pioglitazone, a CYP2C8 substrate, shows increased levels when taken with Abiraterone, necessitating close monitoring for toxicity.

 

Precaution

Abiraterone Acetate can lead to hypertension, hypokalemia, and fluid retention due to increased mineralocorticoid levels from CYP17 inhibition. Patients should undergo monthly monitoring for these conditions. Hypertension and hypokalemia must be managed before and during Abiraterone 250 mg treatment. Patients should also be watched for signs of adrenocortical insufficiency. Prior to starting Abiraterone, measure serum transaminases (ALT and AST) and bilirubin levels. During the first three months of treatment, check these levels every two weeks, then monthly thereafter.

 

Pediatric Use: The safety and effectiveness in pediatric patients have not been established.
Use in Pregnancy: The safety and efficacy of Abiraterone Acetate have not been established in females. The drug can cause fetal harm and potential loss of pregnancy.
Use in Lactation: There is no information available on the presence of Abiraterone Acetate in human milk, or on the effects on the breastfed child or milk production.

 

Overdose

There is no specific antidote. In the event of an overdose, Abiraterone Drug should be stopped, general supportive measures are undertaken, including monitoring for arrhythmias and cardiac failure and assess liver function.

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