Abiraterone Acetate

Introduction

Abiraterone Acetate is a medication used in the treatment of prostate cancer. It is an androgen biosynthesis inhibitor that reduces the levels of androgens, such as testosterone and dihydrotestosterone, which fuel the growth of prostate cancer cells. Abiraterone is used particularly in patients with castration-resistant prostate cancer (CRPC) who have progressed despite conventional hormone therapy.

Uses

Abiraterone Acetate is primarily used for:

• Treating metastatic castration-resistant prostate cancer (CRPC) in combination with prednisone or prednisolone.
• It is used in both pre- and post-chemotherapy settings for patients whose disease has progressed despite other treatments.

Brand Name	Abiraterone Acetate
Type
Weight
Generic	Abiraterone Acetate
Manufacturer
Available in	English বাংলা

Mechanism of Action

Abiraterone Acetate works by inhibiting the enzyme CYP17A1, which is crucial in the biosynthesis of androgens. By blocking this enzyme, Abiraterone reduces the production of testosterone and other androgens not only in the testes but also in the adrenal glands and tumor tissue. This results in lower levels of circulating androgens, which can slow down or stop the growth of prostate cancer cells that depend on these hormones.

How Long Does It Take to Work?

Patients may start to see clinical benefits within a few weeks of starting treatment, but it can take several months to observe the full therapeutic effects. The time to response varies based on individual patient factors and the extent of disease progression.

Absorption

Abiraterone Acetate is well absorbed from the gastrointestinal tract. The absolute bioavailability of Abiraterone is approximately 38% when taken with food. The presence of food does not significantly affect the drug’s absorption, but it is recommended to take Abiraterone on an empty stomach to optimize absorption.

Route of Elimination

Abiraterone is primarily metabolized in the liver. It undergoes extensive metabolism via the CYP3A4 enzyme pathway, producing inactive metabolites. The drug and its metabolites are excreted primarily via the feces, with a smaller amount eliminated in the urine.

Dosage

Adults:

• The usual dose of Abiraterone Acetate is 1,000 mg taken orally once daily, in combination with 10 mg of prednisone or prednisolone taken twice daily.
• Dosage adjustments may be required in cases of hepatic impairment or based on other patient-specific factors.

Geriatric Use:

• Dosage adjustments are not generally required for elderly patients, but they should be monitored closely for adverse effects and tolerability.

Administration

Abiraterone Acetate should be taken orally, once daily, on an empty stomach. The tablets should be swallowed whole with water and not crushed, chewed, or broken. It is important to follow the prescribed dosing schedule and take the medication at the same time each day.

Side Effects

Common side effects of Abiraterone Acetate include:

• Fatigue
• Joint pain
• Hot flashes
• Diarrhea
• Hypertension
• Elevated liver enzymes

Less common but more serious side effects may include adrenal insufficiency, liver toxicity, and cardiovascular events.

Toxicity

Symptoms of toxicity may include severe liver dysfunction, high blood pressure, and severe electrolyte imbalances. In cases of suspected overdose or severe adverse effects, discontinuation of the medication and supportive care may be necessary, including management of liver function and electrolyte abnormalities.

Precautions

Precautions include monitoring for signs of adrenal insufficiency, liver dysfunction, and hypertension. Regular blood tests are necessary to monitor liver enzymes, potassium levels, and blood pressure during treatment. Patients should also be monitored for signs of cardiovascular problems.

Interaction

Abiraterone Acetate can interact with other medications, particularly those that affect CYP3A4 enzyme activity. These interactions can affect the metabolism and efficacy of Abiraterone. Important interactions include:

• Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) – may increase Abiraterone levels and risk of side effects.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine) – may decrease Abiraterone levels and effectiveness.

Disease Interaction

Abiraterone should be used with caution in patients with pre-existing liver conditions, adrenal insufficiency, or hypertension. Regular monitoring is required to manage and adjust treatment in these patients as needed.

Drug Interaction

Drug interactions may include:

• Anticoagulants – increased risk of bleeding or altered effectiveness.
• Other anticancer agents – potential for additive or synergistic effects, which may require dose adjustments.

Food Interactions

Food does not significantly affect the absorption of Abiraterone, but it is generally recommended to take the medication on an empty stomach to maximize absorption. Avoiding excessive alcohol consumption is also advised, as it may exacerbate side effects.

Pregnancy Use

Abiraterone Acetate is classified as a Category X drug for pregnancy. It is contraindicated during pregnancy due to the potential for fetal harm. Women who are pregnant or planning to become pregnant should not use Abiraterone, and effective contraception should be used during treatment.

Lactation Use

It is not known if Abiraterone Acetate is excreted in human breast milk. Due to potential risks to a nursing infant, breastfeeding is generally not recommended while taking Abiraterone. Patients should discuss alternative feeding options with their healthcare provider.

Acute Overdose

In the event of an acute overdose, symptoms may include severe liver dysfunction, electrolyte imbalances, and hypertension. Treatment should be supportive and may include measures to manage liver function and correct any metabolic abnormalities. Immediate medical attention is required.

Contraindication

Abiraterone Acetate is contraindicated in patients with severe hepatic impairment. It should not be used in pregnant women or in patients with hypersensitivity to the drug or any of its components.

Use Direction

Patients should follow the prescribed dosage and administration instructions carefully. Abiraterone should be taken once daily on an empty stomach, with prednisone or prednisolone as directed. Regular monitoring and follow-up appointments are necessary to assess treatment efficacy and manage side effects.

Storage Conditions

Abiraterone Acetate should be stored at room temperature, between 20°C to 25°C (68°F to 77°F), in a tightly closed container. Keep the medication away from moisture and direct light, and out of reach of children.

Volume of Distribution

The volume of distribution of Abiraterone is approximately 100 L. This reflects its distribution into various tissues and its ability to cross cellular membranes.

Half Life

The plasma half-life of Abiraterone is approximately 12 to 15 hours. Its long half-life contributes to its dosing schedule of once daily administration.

Clearance

Abiraterone is primarily cleared through hepatic metabolism. Its clearance rate can be affected by liver function, and dosage adjustments may be necessary in patients with liver impairment.

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Some Frequently Asked Questions About Abiraterone Acetate

1. What is Abiraterone Acetate ?

Abiraterone Acetate is a medication used in the treatment of metastatic castration-resistant prostate cancer (mCRPC). It works by inhibiting androgen production, which helps to slow cancer growth.

2. How does Abiraterone Acetate work?

It works by blocking the enzyme CYP17A1, which is involved in the production of androgens like testosterone. Reducing androgen levels can slow the growth of prostate cancer cells.

3. What is Abiraterone Acetate used for?

It is primarily used to treat prostate cancer that has spread and is resistant to traditional hormonal treatments.

4. What is the usual dosage of Abiraterone Acetate ?

The typical dosage is 1,000 mg once daily, taken on an empty stomach with water, followed by a glucocorticoid such as prednisone or prednisolone.

5. How should I take Abiraterone Acetate ?

Swallow the tablet whole, and avoid eating for at least 2 hours before and 1 hour after taking the medication to ensure its proper absorption.

6. Can I take Abiraterone Acetate with food?

No, it should be taken on an empty stomach for better absorption. Avoid food for at least 2 hours before and after taking it.

7. What should I do if I miss a dose of Abiraterone Acetate ?

If you miss a dose, take it as soon as you remember, unless it's almost time for your next dose. In that case, skip the missed dose and continue with your regular schedule.

8. What are the common side effects of Abiraterone Acetate ?

• Fatigue
• Joint pain
• Hot flashes
• Diarrhea
• Low potassium levels (hypokalemia)

9. Can Abiraterone Acetate cause high blood pressure?

Yes, Abiraterone can cause high blood pressure (hypertension) as a side effect.

10. Can I take Abiraterone Acetate if I have liver problems?

If you have liver problems, your doctor may need to adjust the dosage or monitor your liver function more closely while taking Abiraterone.

11. Is Abiraterone Acetate safe during pregnancy?

No, it is not safe for use during pregnancy and should not be used by pregnant women as it can harm the fetus.

12. Is Abiraterone Acetate safe while breastfeeding?

No, it is not recommended to take Abiraterone while breastfeeding as it can pass into breast milk.

13. Can I drive while taking Abiraterone Acetate ?

Abiraterone can cause dizziness and fatigue, so you should avoid driving if you feel these side effects.

14. Can Abiraterone Acetate interact with other medications?

Yes, it can interact with medications like blood thinners, corticosteroids, and certain antifungals, so inform your doctor about all medications you are taking.

15. Can Abiraterone Acetate cause weight gain?

Yes, some individuals may experience weight gain as a side effect of Abiraterone.

16. How does Abiraterone Acetate affect testosterone levels?

Abiraterone lowers testosterone levels, which helps in controlling prostate cancer growth.

17. Can Abiraterone Acetate be used to treat breast cancer?

No, Abiraterone is specifically used for prostate cancer and is not approved for the treatment of breast cancer.

18. What is the recommended glucocorticoid to take with Abiraterone?

Prednisone or prednisolone is typically prescribed to be taken alongside Abiraterone to reduce side effects related to adrenal insufficiency.

19. How long should I take Abiraterone Acetate ?

Abiraterone is usually taken until the prostate cancer becomes resistant to the drug, as determined by your doctor.

20. Can I stop taking Abiraterone Acetate suddenly?

No, you should not stop taking Abiraterone without consulting your doctor. Gradual adjustment may be necessary.

21. Can Abiraterone Acetate cause nausea?

Yes, nausea is a potential side effect, although it is not common.

22. How does Abiraterone Acetate affect bone health?

Abiraterone can cause bone thinning (osteoporosis), so your doctor may monitor your bone health and recommend supplements.

23. Can I take Abiraterone Acetate with a vitamin D supplement?

Yes, but you should inform your doctor if you are taking any vitamin D supplements.

24. Does Abiraterone Acetate lower my immune system?

Yes, it can lower your immune system by affecting adrenal gland function.

25. Can Abiraterone Acetate affect my fertility?

Abiraterone may affect fertility in men, so it is advised to consult a doctor about the potential impact on reproductive health.

26. Can I take Abiraterone Acetate if I have diabetes?

Abiraterone can affect blood sugar levels, so diabetics should monitor their levels carefully while on this medication.

27. Can Abiraterone Acetate cause dizziness?

Yes, dizziness is a possible side effect, especially when standing up quickly.

28. Is Abiraterone Acetate available over the counter?

No, Abiraterone Acetate is a prescription medication and should be taken under a doctor's supervision.

29. How does Abiraterone Acetate compare to other prostate cancer treatments?

Abiraterone is often used when other treatments like chemotherapy or traditional hormonal therapy fail to control prostate cancer.

30. Can Abiraterone Acetate be used for early-stage prostate cancer?

It is typically used for advanced or metastatic prostate cancer, not early-stage prostate cancer.

31. Can I take Abiraterone Acetate if I have heart disease?

If you have heart disease, consult your doctor before taking Abiraterone, as it can cause high blood pressure and affect your heart.

32. Can Abiraterone Acetate be taken with antihypertensive medications?

Yes, but it is important to monitor your blood pressure regularly, as Abiraterone can cause hypertension.

33. What should I do if I experience severe side effects?

If you experience severe side effects, such as chest pain, difficulty breathing, or severe fatigue, seek immediate medical attention.

34. Can Abiraterone Acetate cause kidney problems?

Abiraterone may affect kidney function, so kidney function should be monitored during treatment.

35. What are the long-term effects of taking Abiraterone Acetate ?

Long-term use may lead to side effects like osteoporosis, liver issues, and adrenal insufficiency, which require ongoing monitoring.

36. Can Abiraterone Acetate affect my skin?

Yes, skin rashes or changes in skin texture can sometimes occur with Abiraterone use.

37. Can I drink alcohol while taking Abiraterone Acetate ?

It's best to avoid alcohol as it may exacerbate side effects like dizziness and liver strain.

38. Can Abiraterone Acetate be used after chemotherapy?

Yes, Abiraterone is commonly used after chemotherapy to manage advanced prostate cancer.

39. Does Abiraterone Acetate require regular blood tests?

Yes, regular blood tests are necessary to monitor liver function, blood pressure, and potassium levels.

40. Can Abiraterone Acetate cause depression?

Yes, some users may experience mood changes, including depression.

41. Can Abiraterone Acetate be used for other types of cancer?

It is specifically approved for prostate cancer and is not used for other types of cancer.

42. Can Abiraterone Acetate cause fatigue?

Yes, fatigue is one of the more common side effects.

43. How do I know if Abiraterone Acetate is working?

Your doctor will monitor your PSA (prostate-specific antigen) levels and other signs to determine if the medication is effective.

44. Can Abiraterone Acetate be taken with aspirin?

Consult your doctor, as aspirin can affect blood clotting and interact with certain cancer treatments.

45. Can I take Abiraterone Acetate for pain management?

Abiraterone is not used for pain management, but it helps control the growth of cancer cells.

46. What should I do if I accidentally overdose on Abiraterone Acetate ?

Seek immediate medical attention if you suspect an overdose.

47. Can Abiraterone Acetate cause hair loss?

Hair loss is not a common side effect but may occur in some patients.

48. Can Abiraterone Acetate cause digestive problems?

Yes, some people experience symptoms like nausea, diarrhea, or constipation.

49. Can I take Abiraterone Acetate with other cancer medications?

Yes, but always consult your oncologist to avoid potential drug interactions.

50. How long will I need to take Abiraterone Acetate ?

The duration depends on how well the drug controls your cancer and your doctor's recommendation.