Flutamide

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Generic Name of Flutamide - Learn More

Flutamide

Flutamide Precaution - What You Need to Know

Flutamide is an antiandrogen medication primarily used in the treatment of prostate cancer. Caution should be exercised in patients with a history of liver disease, as flutamide is metabolized in the liver, and hepatotoxicity is a well-known adverse effect of this drug. Liver function should be regularly monitored, particularly during the first few months of therapy, as liver failure can occur, manifesting as jaundice, elevated liver enzymes, or right upper abdominal pain. Patients with pre-existing liver conditions should only use flutamide if the benefits outweigh the risks, and they should be closely monitored. Flutamide is also contraindicated in patients with severe liver impairment. In addition, flutamide can cause gynecomastia (enlargement of male breast tissue) and reduced libido due to its antiandrogenic effects, which may be distressing for some men. It is important to monitor for any signs of breast tenderness or enlargement and to address these concerns with patients. Flutamide should be used with caution in patients with a history of depression or psychiatric disorders, as it can exacerbate mood changes. Regular monitoring of blood counts, especially liver function and testosterone levels, is essential throughout treatment to minimize potential risks.

Flutamide Indication - Uses and Benefits

Flutamide is primarily indicated for the treatment of prostate cancer, often as part of a combined therapy with other treatments such as surgery or radiation therapy. It is used to block the effects of androgens (male hormones like testosterone), which can promote the growth of prostate cancer cells. Flutamide works by inhibiting the action of testosterone at the androgen receptors in prostate tissue. This antiandrogenic effect slows or halts the progression of the cancer. Additionally, flutamide is used off-label for conditions like hirsutism (excessive hair growth in women) and acne in women, although other antiandrogens, like spironolactone, are more commonly preferred for these indications. It may also be used in the treatment of gender dysphoria in transgender women to suppress male characteristics by reducing the effects of testosterone. While flutamide is effective at reducing the symptoms associated with high levels of androgens, its use is typically limited to more severe cases, and it is generally combined with other therapies to enhance efficacy and reduce side effects.

Flutamide Contraindications - Important Warnings

Flutamide is contraindicated in patients who are hypersensitive to flutamide or any component of the formulation. It is also contraindicated in patients with severe hepatic impairment or active liver disease, including hepatitis, cirrhosis, or significant liver dysfunction, as the drug can exacerbate liver damage and potentially lead to acute liver failure. Flutamide is not recommended for use in women due to its potential for causing severe liver toxicity, as well as its primary use in male patients with prostate cancer. It should not be used in patients with pre-existing prostate cancer metastases that have spread to the liver, as the treatment can worsen liver function and hinder the therapeutic goals. Pregnant women should avoid flutamide, as it has been classified as a pregnancy category D drug, which indicates potential harm to the fetus, including birth defects and other complications. Due to its strong antiandrogenic properties, flutamide can also cause feminizing effects in male patients, including breast tenderness or enlargement, which may be uncomfortable but are typically reversible upon discontinuation of the drug.

Flutamide Side Effects - What to Expect

Flutamide can cause both common and severe side effects:
- Common side effects: These include gastrointestinal symptoms such as nausea, diarrhea, and vomiting, which may occur during the initiation of therapy. Hot flashes, fatigue, and weakness are also commonly reported. Patients may experience decreased libido, erectile dysfunction, and gynecomastia (breast enlargement in men), which are often reversible upon discontinuation of the drug. These effects are due to the antiandrogenic activity of flutamide.
- Serious side effects: The most concerning side effect of flutamide is hepatotoxicity, which can manifest as jaundice, abdominal pain, dark urine, and elevated liver enzymes. In severe cases, acute liver failure can occur, which is life-threatening. Regular liver function tests should be performed, especially during the first 3 months of treatment. Other serious effects include mental health changes, such as depression, anxiety, and mood swings, which may be exacerbated by the medication. Rarely, flutamide can cause arrhythmias, cardiovascular issues, or edema.
- Long-term use risks: Chronic use of flutamide may also lead to irreversible liver damage if not monitored adequately. It can also contribute to bone density loss over time, particularly when used in conjunction with other androgen-deprivation therapies.
- Managing side effects: Liver function tests should be monitored regularly to detect early signs of liver toxicity. Patients experiencing gynecomastia or libido changes should discuss alternatives with their healthcare provider. If any serious side effects, such as jaundice or significant mood changes, occur, the drug should be discontinued immediately.

Flutamide Pregnancy Category ID - Safety Information

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Flutamide Mode of Action - How It Works

Flutamide exerts its therapeutic effects by blocking the action of androgens, particularly testosterone, at the androgen receptors in target tissues such as the prostate gland. It works by competitively binding to the androgen receptors and preventing testosterone and dihydrotestosterone (DHT) from activating these receptors. By inhibiting androgen receptor activation, flutamide reduces the growth of prostate cancer cells, which rely on androgens for proliferation. This antiandrogenic activity is the reason flutamide is primarily used in the treatment of prostate cancer, where androgen-driven tumor growth is a significant factor in disease progression. Flutamide is a non-steroidal antiandrogen and is distinct from other hormonal therapies in that it specifically targets the androgen receptor without affecting other steroid hormones. This mechanism helps to suppress the effects of testosterone and can reduce symptoms associated with excess androgen activity, such as hirsutism in women.

Flutamide Drug Interactions - What to Avoid

Flutamide has several known drug interactions that can affect its safety and efficacy:
- CYP450 interactions: Flutamide is metabolized by the cytochrome P450 enzyme system, particularly CYP1A2. Drugs that inhibit CYP1A2, such as fluvoxamine or ciprofloxacin, can increase flutamide levels, leading to a higher risk of toxicity, including liver damage. Conversely, drugs that induce CYP1A2, like rifampin, can reduce the efficacy of flutamide by increasing its metabolism.
- Warfarin: Flutamide may enhance the anticoagulant effect of warfarin, leading to an increased risk of bleeding. If flutamide and warfarin must be used together, close monitoring of INR (International Normalized Ratio) is required to avoid bleeding complications.
- Other antiandrogens or hormonal therapies: Combining flutamide with other antiandrogens (e.g., spironolactone) or hormonal therapies may increase the risk of side effects, such as liver toxicity and feminizing effects in men. Caution is needed when combining these medications, and careful monitoring is required.
- Corticosteroids: Concurrent use of flutamide with corticosteroids may enhance the risk of developing side effects like edema, gastrointestinal bleeding, or increased blood pressure. Monitoring of electrolytes and blood pressure may be necessary during therapy.
- Alcohol: Alcohol consumption should be minimized while taking flutamide, as it can exacerbate liver toxicity. Patients are advised to avoid heavy drinking during treatment with flutamide to reduce the risk of hepatic damage.

Flutamide Adult Dose - Recommended Dosage

For the treatment of prostate cancer, the usual dose of flutamide is 250 mg orally three times a day. The drug is typically used in combination with other therapies, such as a luteinizing hormone-releasing hormone (LHRH) agonist, to achieve more comprehensive androgen deprivation. Flutamide should be taken with or without food, and the tablet should be swallowed whole. Patients undergoing therapy should have regular follow-up visits to monitor for adverse effects, especially liver function tests and testosterone levels. If liver toxicity occurs, the medication should be discontinued. The dose may be adjusted based on clinical response and tolerability, but the maximum recommended dose should not exceed 750 mg per day.

Flutamide Child Dose - Dosage for Children

Flutamide is not typically used in pediatric patients. The safety and efficacy of flutamide in children have not been established, and it is generally reserved for the treatment of prostate cancer in adult males. If flutamide is ever prescribed for off-label uses in children (e.g., for severe hirsutism), careful dose adjustment and monitoring for adverse effects should be done. Other more appropriate therapies are generally preferred for pediatric conditions involving excess androgen.

Flutamide Renal Dose - Dosage for Kidney Conditions

Flutamide is not primarily excreted by the kidneys, so renal impairment does not generally necessitate significant dosage adjustments. However, patients with renal insufficiency should still be closely monitored for any potential side effects, particularly liver function, as flutamide may still affect liver metabolism in such patients. In severe renal impairment, the use of flutamide should be approached with caution, and alternative therapies may be considered if necessary.