Casodex: Advanced Androgen Blockade for Prostate Cancer Control
Casodex
| Product dosage: 50mg | |||
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Synonyms
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Casodex (bicalutamide) is a non-steroidal antiandrogen medication specifically developed for the treatment of prostate cancer. As part of combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog, it provides complete androgen blockade by competitively inhibiting androgen binding at cellular receptor sites. This dual-action approach targets both testicular and adrenal androgen production, offering a comprehensive strategy for metastatic prostate cancer management. Clinical evidence supports its role in improving progression-free survival and overall treatment response when used according to established protocols.
Features
- 50 mg film-coated tablets containing bicalutamide as the active pharmaceutical ingredient
- Selective androgen receptor antagonist with high binding affinity
- Once-daily oral administration regimen
- Bioavailability approximately 90% following oral administration
- Extensive hepatic metabolism primarily via cytochrome P450 (CYP) 3A4 isoenzyme
- Mean elimination half-life of approximately 5.8 days in patients with prostate cancer
- Steady-state concentrations achieved within 4-12 weeks of continuous dosing
- White, circular biconvex tablets with “CASODEX 50” engraved on one side
Benefits
- Provides complementary androgen suppression when combined with LHRH analog therapy
- Reduces testosterone stimulation of prostate cancer cells through receptor-level blockade
- Demonstrates favorable tolerability profile compared to older antiandrogen therapies
- Maintains quality of life through once-daily dosing convenience
- Shows synergistic activity with surgical castration or medical castration therapies
- May delay disease progression in advanced prostate cancer settings
Common use
Casodex is primarily indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D2 metastatic carcinoma of the prostate. This combination approach provides maximal androgen blockade by addressing both testicular androgen production (via LHRH suppression) and peripheral androgen receptor activation. The medication is typically initiated concurrently with LHRH analog therapy or following surgical castration. Clinical studies have demonstrated that this combination therapy can prolong progression-free survival and improve objective response rates compared to monotherapy approaches in appropriately selected patients.
Dosage and direction
The recommended dosage of Casodex is one 50 mg tablet taken orally once daily, preferably at the same time each day. Administration should begin concurrently with LHRH analog therapy or following surgical castration. Tablets should be swallowed whole with water and may be taken with or without food. Treatment should continue until disease progression becomes evident or until unacceptable toxicity occurs. No dosage adjustment is necessary for elderly patients, but careful monitoring is advised. For patients with mild to moderate hepatic impairment, close supervision is recommended, while those with severe hepatic impairment should generally avoid use.
Precautions
Regular monitoring of liver function tests is essential during treatment, particularly during the first 4 months of therapy and periodically thereafter. Patients should be advised about the potential for hepatotoxicity and instructed to report symptoms such as nausea, vomiting, abdominal pain, fatigue, anorexia, flu-like symptoms, dark urine, or jaundice promptly. Periodic assessments of prostate-specific antigen (PSA) levels are necessary to monitor treatment response. Patients should be cautioned about potential visual disturbances and advised against driving or operating machinery if such symptoms occur. Those with pre-existing cardiovascular conditions require careful monitoring due to potential fluid retention effects.
Contraindications
Casodex is contraindicated in patients with known hypersensitivity to bicalutamide or any component of the formulation. It should not be used in women, particularly those who are or may become pregnant, due to potential teratogenic effects. The medication is contraindicated in patients with severe hepatic impairment (Child-Pugh Class C). Concomitant use with terfenadine, astemizole, or cisapride is contraindicated due to potential QT prolongation risks. The medication should not be used as monotherapy for prostate cancer treatment outside of specific clinical circumstances under specialist supervision.
Possible side effect
- Hot flashes (49% of patients)
- Breast pain (38%) and gynecomastia (35%)
- Constipation (12%), nausea (11%), and diarrhea (9%)
- Asthenia (15%) and pain (18%)
- Elevated liver enzymes (transaminases) in approximately 10% of patients
- Decreased libido (9%) and impotence (8%)
- Dyspnea (7%) and peripheral edema (6%)
- Rash (6%) and sweating (5%)
- Less commonly: hepatitis, jaundice, hepatic failure, photosensitivity reactions
- Rare reports: interstitial lung disease, thrombocytopenia, neutropenia
Drug interaction
Casodex undergoes extensive hepatic metabolism primarily through CYP3A4, creating several important interaction considerations. Co-administration with strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir) may increase bicalutamide exposure. Inducers of CYP3A4 (rifampin, carbamazepine, phenytoin) may decrease bicalutamide concentrations. Warfarin co-administration requires careful monitoring of prothrombin time due to potential enhancement of anticoagulant effect. Caution is advised with medications that prolong QT interval (certain antiarrhythmics, antipsychotics, antibiotics). The medication may interact with other highly protein-bound drugs through displacement mechanisms.
Missed dose
If a dose of Casodex is missed, the patient should take it 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. Patients should not take a double dose to make up for a missed dose. Maintenance of consistent dosing is important for therapeutic efficacy, so patients should be advised to establish a routine for daily administration. If multiple doses are missed, medical advice should be sought regarding appropriate management strategy.
Overdose
There is no specific antidote for Casodex overdose. Management should consist of supportive measures and symptomatic treatment. In cases of recent ingestion, gastric lavage may be considered. Since bicalutamide is highly protein-bound, dialysis is unlikely to be beneficial. Liver function should be monitored closely, and appropriate supportive care provided for any clinical manifestations. The extended half-life of bicalutamide necessitates prolonged observation in overdose situations. Cases of intentional overdose should receive psychiatric evaluation in addition to medical management.
Storage
Store Casodex tablets at controlled room temperature between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). Keep the medication in its original container with the lid tightly closed to protect from moisture and light. Keep out of reach of children and pets. Do not use tablets that appear discolored or show signs of deterioration. Properly dispose of any unused medication after treatment completion or expiration date passage according to local regulations. Do not flush medications down the toilet or pour them into drains.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient circumstances. The prescribing physician should be consulted for complete information regarding indications, contraindications, warnings, precautions, and adverse effects. Patients should not alter or discontinue medication without medical supervision. While every effort has been made to ensure accuracy, medical knowledge evolves continuously, and newer information may supersede content presented here.
Reviews
Clinical studies demonstrate that Casodex in combination with LHRH analogs shows significant improvement in progression-free survival compared to monotherapy in metastatic prostate cancer. The combination therapy approach is generally well-tolerated, with hot flashes and breast tenderness being the most frequently reported adverse effects. Many urologists note the convenience of once-daily dosing contributes to treatment adherence. Some studies suggest potential quality of life benefits compared to older antiandrogen therapies, though individual responses vary. Regular monitoring remains essential for optimal management and early detection of potential hepatic complications.