Eulexin: Advanced Androgen Blockade for Prostate Cancer Control
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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 prostate carcinoma. It works by competitively inhibiting the binding of androgens, like testosterone and dihydrotestosterone (DHT), to their receptors in prostate tumor cells. This targeted action helps suppress tumor growth and disease progression, making it a cornerstone in hormonal treatment strategies for advanced prostate cancer. Eulexin is typically administered alongside a luteinizing hormone-releasing hormone (LHRH) agonist to achieve maximal androgen blockade, offering a comprehensive approach to hormonal control in eligible patients.
Features
- Active ingredient: Flutamide 125 mg
- Pharmaceutical form: Oral tablets
- 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 metabolite (hydroxyflutamide) has a half-life of about 8–10 hours
- Excretion: Primarily renal, with some fecal elimination
Benefits
- Effectively reduces androgen stimulation of prostate cancer cells, slowing tumor progression.
- Used in combination with LHRH agonists, it provides complete androgen blockade, improving response rates.
- Helps manage disease-related symptoms such as bone pain and urinary obstruction in metastatic settings.
- Oral administration allows for convenient outpatient treatment, supporting patient quality of life.
- Well-established efficacy and safety profile based on decades of clinical use and research.
- Contributes to prolonged progression-free survival in appropriately selected patient populations.
Common use
Eulexin is primarily used in combination with a luteinizing hormone-releasing hormone (LHRH) analog, such as leuprolide or goserelin, for the treatment of metastatic prostate cancer (stage D2). This combination is intended to achieve maximal androgen blockade by suppressing both testicular and adrenal androgen production and blocking receptor binding. It may also be used off-label in certain cases of locally advanced disease or as part of neoadjuvant therapy before radical prostatectomy or radiation, though such uses should be guided by specialist evaluation and current clinical evidence.
Dosage and direction
The standard dosage of Eulexin is one 125 mg tablet administered orally three times daily (approximately every 8 hours), for a total daily dose of 375 mg. It must be given concomitantly with an LHRH agonist as prescribed. Tablets can be taken with or without food, though consistency in administration relative to meals may help maintain stable plasma levels. Dosage adjustments are generally not required based on age alone, but renal or hepatic impairment may necessitate careful monitoring and potential modification. Treatment should be continued unless disease progression or unacceptable toxicity occurs. Always follow the specific dosing regimen provided by the treating physician.
Precautions
Regular monitoring of liver function tests (LFTs) is essential before initiation and periodically during therapy, as flutamide has been associated with hepatic injury, including rare cases of fatal hepatitis. Patients should be advised to report symptoms such as nausea, vomiting, abdominal pain, fatigue, dark urine, or jaundice promptly. Blood counts and prostate-specific antigen (PSA) levels should also be tracked to assess response and detect potential hematologic effects. Due to the risk of photosensitivity reactions, patients should use sunscreen and protective clothing when outdoors. Caution is advised in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency due to a theoretical risk of hemolytic anemia. Cardiovascular status should be monitored, especially in those with pre-existing heart disease.
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 (Child-Pugh Class C) or a history of flutamide-induced liver injury. Use is also contraindicated in women, particularly those who are or may become pregnant, due to potential teratogenic effects and lack of indication. It is not recommended for pediatric patients. Concomitant use with certain other hepatotoxic drugs should be avoided unless the potential benefit justifies the risk.
Possible side effect
Common side effects are often related to androgen deprivation and may include hot flashes (up to 60% of patients), loss of libido, impotence, gynecomastia, breast tenderness, nausea, vomiting, diarrhea, and increased liver enzymes. Less frequently, patients may experience drowsiness, confusion, edema, hypertension, or hematologic changes such as anemia or leukopenia. Rare but serious adverse effects include hepatotoxicity (elevated transaminases, jaundice, hepatic necrosis), which requires immediate medical attention, and pulmonary toxicity (interstitial pneumonitis). Photosensitivity reactions and cardiovascular events have also been reported in some cases.
Drug interaction
Flutamide is primarily metabolized by CYP1A2 and may interact with drugs that inhibit or induce this enzyme. Concurrent use with strong CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin) may increase flutamide levels and the risk of toxicity. Warfarin: Flutamide may potentiate anticoagulant effect; monitor INR closely. Other hepatotoxic agents (e.g., acetaminophen in high doses, statins, certain antifungals) may increase the risk of liver injury. LHRH agonists are used concomitantly as part of standard therapy and do not represent an interaction but a intended synergistic effect. Always inform the prescriber of all medications, including over-the-counter drugs and supplements.
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, skip the missed dose and resume the usual dosing schedule. Do not double the dose to make up for a missed one. Maintaining consistent timing helps sustain stable androgen receptor blockade. Patients should be instructed to contact their healthcare provider or pharmacist if unsure about how to manage missed doses, especially if occurring frequently.
Overdose
There is limited experience with flutamide overdose. Symptoms may include exaggerated pharmacological effects such as nausea, vomiting, dizziness, drowsiness, and potential hepatic toxicity. In case of suspected overdose, seek immediate medical attention or contact a poison control center. Supportive and symptomatic treatment is recommended; there is no specific antidote. Gastric lavage or activated charcoal may be considered if ingestion was recent. Monitor vital signs, liver function, and provide supportive care as needed.
Storage
Store Eulexin tablets at room temperature (15–30°C or 59–86°F), in a dry place, protected from light and moisture. Keep the container tightly closed and out of reach of children and pets. Do not use beyond the expiration date printed on the packaging. Proper disposal of unused or expired medication should be done in accordance with local regulations, ideally through a drug take-back program.
Disclaimer
This information is intended for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting, changing, or stopping any medication. Individual patient needs and circumstances may vary. The prescribing physician should be guided by the latest clinical evidence and official prescribing information.
Reviews
Clinical studies and long-term use have established Eulexin as an effective component of combined androgen blockade for metastatic prostate cancer. In pivotal trials, the combination with an LHRH agonist demonstrated improved progression-free and overall survival compared to monotherapy. Most urologists and oncologists regard it as a standard option within its indication, though newer antiandrogens may offer alternative profiles. Patient tolerance is generally acceptable, with hot flashes and gastrointestinal complaints being the most frequently reported issues; hepatic monitoring remains a critical aspect of management. Overall, it continues to be a valuable agent in the armamentarium against advanced prostate cancer.