Casodex

Casodex (bicalutamide) is a nonsteroidal antiandrogen medication 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. It functions by competitively inhibiting androgen binding at cellular receptor sites, thereby interrupting the hormone-driven proliferation of prostate cancer cells. This targeted mechanism offers a sophisticated approach to hormonal manipulation in advanced prostate cancer management, providing clinicians with a valuable tool for comprehensive androgen deprivation therapy.

Features

• Contains 50 mg bicalutamide as the active pharmaceutical ingredient
• White, film-coated tablets with “CDX” and “50” engraved on opposite sides
• Available in calendar blister packs of 28 tablets
• Demonstrated high affinity for androgen receptors with prolonged receptor binding
• Long elimination half-life (approximately 5.8 days) allowing once-daily dosing
• Extensive hepatic metabolism primarily via cytochrome P450 (CYP) 3A4 isoenzyme
• High plasma protein binding (96%) primarily to albumin

Benefits

• Effectively suppresses testosterone stimulation of prostate cancer growth when combined with LHRH therapy
• Delays disease progression in metastatic prostate cancer
• Maintains quality of life through oral administration convenience
• Demonstrates predictable pharmacokinetics with once-daily dosing
• Provides complementary androgen blockade when used with medical castration
• Offers favorable tolerability profile compared to some alternative antiandrogens

Common use

Casodex is primarily prescribed as part of combined androgen blockade for advanced prostate cancer. It is initiated concurrently with an LHRH analog (such as leuprolide or goserelin) to provide immediate receptor blockade while the LHRH analog achieves chemical castration over 2-4 weeks. This combination approach prevents the initial testosterone surge that can occur with LHRH monotherapy. The medication is typically continued long-term unless disease progression or unacceptable toxicity occurs. Some clinicians may use Casodex monotherapy in specific cases where LHRH analogs are contraindicated, though this represents an off-label application.

Dosage and direction

The recommended dosage is one 50 mg tablet taken orally once daily, preferably at the same time each day. Administration should begin concurrently with LHRH analog therapy and continue throughout treatment. Tablets should be swallowed whole with water and may be taken with or without food, though consistency in administration relative to meals is recommended to maintain stable pharmacokinetics. No dosage adjustment is typically required for elderly patients, but hepatic impairment necessitates careful monitoring and potential dosage reduction. Treatment duration is determined by therapeutic response and tolerability, often continuing until disease progression.

Precautions

Regular monitoring of liver function tests (ALT, AST, bilirubin) is essential, particularly during the first 4 months of therapy and periodically thereafter. Patients should be advised about potential hepatotoxicity signs including jaundice, dark urine, or abdominal pain. Blood glucose monitoring may be warranted in diabetic patients due to potential effects on glycemic control. Patients should use caution when driving or operating machinery until their response to therapy is established, as fatigue and dizziness may occur. Regular bone density assessment may be considered due to accelerated bone mineral density loss associated with androgen deprivation therapy.

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 during pregnancy, due to potential teratogenic effects and disruption of normal hormonal function. Concurrent use with terfenadine, astemizole, or cisapride is contraindicated due to potential QT prolongation risks. The medication is contraindicated in patients with severe hepatic impairment (Child-Pugh Class C) unless no alternative exists and benefits clearly outweigh risks.

Possible side effects

Common adverse reactions (≥10% incidence) include hot flashes (49%), pain (general) (18%), constipation (12%), asthenia (15%), nausea (15%), and diarrhea (12%). Gynecomastria (38%) and breast pain (39%) occur frequently due to altered estrogen-androgen balance. Less common but clinically significant effects include hepatic changes (elevated transaminases in 6-9%, jaundice in <1%), cardiovascular effects (hypertension 7%, heart failure 2%), and hematological changes (anemia 7%). Rare but serious adverse events include hepatitis, hepatic necrosis, and pulmonary fibrosis. Most side effects are dose-dependent and may diminish with continued therapy.

Drug interaction

Casodex undergoes extensive hepatic metabolism primarily via CYP3A4, creating potential interactions with inhibitors and inducers of this enzyme. Strong CYP3A4 inhibitors (ketoconazole, ritonavir) may increase bicalutamide exposure, while inducers (rifampin, carbamazepine) may decrease efficacy. Warfarin requires careful INR monitoring due to potential protein binding displacement. The medication may enhance effects of other QT-prolonging drugs. Concurrent use with other hepatotoxic agents increases risk of liver injury. Calcium channel blockers and statins may require dosage adjustment due to competitive protein binding.

Missed dose

If a dose 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. Doubling doses to make up for a missed dose is not recommended due to increased risk of adverse effects. Patients should maintain a consistent dosing schedule to ensure stable androgen receptor blockade. If multiple doses are missed, medical consultation is recommended to assess appropriate management strategy.

Overdose

No specific antidote exists for Casodex overdose. Management should be supportive and symptomatic. Given the drug’s extensive protein binding, dialysis is unlikely to be effective. Symptoms may include enhanced pharmacological effects such as increased hepatic enzyme elevations, gastrointestinal distress, and dizziness. Liver function should be monitored closely, and appropriate supportive care instituted. Cases of accidental ingestion should be reported to poison control centers for appropriate management guidance.

Storage

Store at controlled room temperature (20-25°C or 68-77°F) with excursions permitted between 15-30°C (59-86°F). Protect from light and moisture. Keep in original packaging until administration. Keep out of reach of children and pets. Do not use beyond the expiration date printed on packaging. Properly dispose of unused medication through take-back programs or according to local regulations to prevent environmental contamination.

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. Full prescribing information including boxed warnings should be consulted before initiating therapy. Dosage and administration may vary based on clinical context and regional prescribing guidelines. Patients should report any adverse effects to their healthcare provider promptly.

Reviews

Clinical studies demonstrate that Casodex 50 mg in combination with LHRH analogs provides effective androgen suppression with generally favorable tolerability. The combination shows equivalent efficacy to orchidectomy with the advantage of reversibility. Many urologists appreciate the convenience of oral administration and the mitigation of initial testosterone flare when combined with LHRH therapy. Patient-reported outcomes indicate acceptable quality of life maintenance despite expected side effects of androgen deprivation. Ongoing research continues to evaluate optimal sequencing and combination strategies in evolving prostate cancer treatment paradigms.