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bicalutamide (Casodex)

Tradename: Casodex. Indications: 1) prostate cancer 2) used in combination with GnRH analogue goserelin (Zoladex) Dosage: 50 mg PO QD. Pharmacokinetics: 1) well absorbed orally 2) unaffected by food 3) no dosage adjustment for renal failure 4) use with caution in patients with hepatic impairment Monitor: 1) baseline & every 3 months - serum prostate-specific antigen (PSA) - serum alkaline phosphatase - serum acid phosphatase - prostate exam - bone scan - liver scan - chest X-ray 2) baseline & periodically - complete blood count (CBC) - liver function tests (LFTs) - more frequently during 1st 4 months of therapy [4] - electrocardiogram (EKG) - echocardiogram - serum testosterone - serum luteinizing hormone (LH) Adverse effects: 1) common (> 10%) - hot flashes (49%), facial flushing exacerbated by EtOH - gynecomastia & breast pain (38-39%) 2) less common (2-5%) - angina pectoris, congestive heart failure (CHF), edema, anxiety, depression, confusion, somnolence, nervousness, fever/chills, dry skin, pruritus, alopecia, hyperglycemia, decreased libido, dehydration, gout, anorexia, dyspepsia, rectal hemorrhage, dry mouth, melena, weight gain, urinary frequency, dysuria, urinary retention, urinary urgency, increased alkaline phosphatase, myasthenia, arthritis, myalgia, pathologic fracture, neck pain, hypertonia, neuropathy, increased serum creatinine, cough, pharyngitis, bronchitis, pneumonia, rhinitis 3) uncomon (< 1%) - diarrhea 4) other - testicular interstitial cell adenoma - hepatotoxicity - monitor liver function - discontinue (in the absence of liver metastases) if: - transaminases > 2 X upper limit of normal - jaundice - tumor flare can occur - nocturia - dyspepsia Drug interactions: may enhance activity of warfarin Mechanism of action: 1) androgen antagonist 2) competitively blocks nuclear androgen receptors 3) compensatory increases in LH & testosterone may occur

Related

goserelin (Zoladex)

General

androgen receptor antagonist; androgen receptor signaling inhibitor (ARSI) antineoplastic endocrine agent

Properties

INHIBITS: androgen receptor MISC-INFO: elimination route LIVER 1/2life 6 DAYS

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. AHFS Drug Information, American Society of Health-System Pharmacists, Bethesda, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com