Eulexin: Advanced Androgen Blockade for Prostate Cancer Control
Eulexin
| Product dosage: 250mg | |||
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Synonyms
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Eulexin (flutamide) is a nonsteroidal antiandrogen medication indicated for use in combination therapy for the management of metastatic prostatic carcinoma. It works by competitively inhibiting the uptake and binding of androgens, like dihydrotestosterone (DHT), to their receptors in target tissues, including prostate tumor cells. When administered alongside a luteinizing hormone-releasing hormone (LHRH) agonist, such as leuprolide, Eulexin provides a comprehensive androgen blockade, significantly reducing tumor growth stimulation. This combination is a cornerstone in the treatment of advanced prostate cancer, helping to control disease progression, alleviate symptoms, and improve quality of life. Its targeted mechanism offers a critical therapeutic option within multimodal treatment regimens.
Features
- Active ingredient: Flutamide 125 mg
- Pharmaceutical form: Oral capsules
- Mechanism: Nonsteroidal antiandrogen; competitive inhibitor at androgen receptor sites
- Bioavailability: Well-absorbed orally, with extensive first-pass metabolism
- Half-life: Approximately 5–6 hours for flutamide; active hydroxylated metabolite has a longer half-life
- Excretion: Primarily renal, with some fecal elimination
Benefits
- Effectively suppresses androgen-driven prostate cancer cell proliferation
- Reduces tumor size and slows metastatic spread when combined with LHRH agonists
- Helps alleviate cancer-related symptoms such as bone pain and urinary obstruction
- Contributes to prolonged progression-free survival in appropriate patient populations
- Supports improved quality of life through symptomatic control
- Oral administration allows for convenient outpatient treatment
Common use
Eulexin is used in combination with a luteinizing hormone-releasing hormone (LHRH) agonist for the treatment of metastatic prostate carcinoma (stage D2). It is not used as monotherapy. The combination is intended to achieve total androgen blockade by suppressing testicular androgen production (via LHRH agonist) and blocking the action of adrenal androgens and any residual androgens at the receptor level (via flutamide). This approach is standard in advanced disease to delay progression and manage symptoms.
Dosage and direction
The recommended dosage is one 125 mg capsule three times daily (every 8 hours), for a total daily dose of 375 mg. Eulexin should be initiated concurrently with an LHRH agonist, such as leuprolide or goserelin. Administration with or after food may help reduce gastrointestinal upset. Capsules should be swallowed whole with water. Dosage adjustments are generally not required for elderly patients, but hepatic impairment necessitates caution and potential dose reduction or discontinuation.
Precautions
Regular monitoring of liver function tests (ALT, AST, bilirubin) is mandatory before starting and periodically during treatment, as flutamide is associated with hepatotoxicity. Patients should be advised to report symptoms such as nausea, vomiting, abdominal pain, fatigue, dark urine, or jaundice immediately. Blood counts should also be monitored. Due to the risk of photosensitivity reactions, patients should use sunscreen and protective clothing when outdoors. Eulexin may cause dizziness or visual disturbances; caution is advised when driving or operating machinery.
Contraindications
Eulexin is contraindicated in patients with known hypersensitivity to flutamide or any component of the formulation. It should not be used in patients with severe hepatic impairment. It is not indicated for use in women, particularly pregnant or breastfeeding women, due to potential teratogenic effects and lack of safety data. It must not be used as monotherapy in the treatment of prostate cancer.
Possible side effects
Common side effects may include hot flashes, loss of libido, impotence, diarrhea, nausea, vomiting, and breast tenderness or enlargement (gynecomastia). Less frequently, skin rash, photosensitivity, and increased liver enzymes are observed. Rare but serious adverse effects include hepatotoxicity (ranging from transaminase elevations to hepatic necrosis), cholestatic jaundice, and hemolytic anemia. Any signs of liver dysfunction require immediate medical evaluation.
Drug interactions
Eulexin is metabolized primarily by CYP1A2. Concomitant use with strong CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin) may increase flutamide plasma concentrations and the risk of toxicity. It may potentiate the effects of warfarin, necessitating close monitoring of INR. Concurrent use with other hepatotoxic drugs (e.g., acetaminophen in high doses, certain statins) should be avoided or closely supervised. LHRH agonists are used in combination but do not exhibit significant pharmacokinetic interactions.
Missed dose
If a dose is missed, it should be taken as soon as remembered, unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Doubling the dose to make up for a missed one is not recommended. Consistent dosing is important to maintain stable androgen blockade.
Overdose
There is no specific antidote for flutamide overdose. Symptoms may include exaggerated pharmacological effects such as nausea, vomiting, dizziness, and potential hepatic toxicity. Gastric lavage or activated charcoal may be considered if ingestion was recent. Treatment is supportive and symptomatic, with particular attention to monitoring and supporting liver function. Hemodialysis is not likely to be effective due to high protein binding.
Storage
Store at room temperature (15–30°C or 59–86°F) in a dry place, protected from light and moisture. Keep the container tightly closed. Do not freeze. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging.
Disclaimer
This information is intended for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider for any health-related decisions or before starting, changing, or stopping any medication. Dosage and suitability are determined by a physician based on individual patient factors.
Reviews
(Simulated expert commentary)
“Eulexin, in combination with LHRH therapy, remains a validated option for achieving complete androgen blockade in metastatic prostate cancer. Clinical trials and long-term use have demonstrated its efficacy in reducing PSA levels, delaying disease progression, and palliating symptoms. The hepatotoxicity risk, while serious, is manageable with vigilant monitoring. It is a well-established agent in the urological oncology armamentarium.” – Clinical Oncologist
“Patient tolerance is generally acceptable, with hot flashes and gastrointestinal complaints being the most frequently reported issues. The three-times-daily dosing requires adherence, but the oral form is convenient compared to intravenous alternatives. The benefits in controlling advanced disease often outweigh the side effect profile when monitored appropriately.” – Urology Specialist