bicalutamide (Casodex)
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Introduction
Tradename: Casodex.
Indications
- prostate cancer
- used in combination with GnRH analogue goserelin (Zoladex)
Dosage
Pharmacokinetics
- well absorbed orally
- unaffected by food
- no dosage adjustment for renal failure
- use with caution in patients with hepatic impairment
elimination via liver
1/2life = 6 days
Monitor
- baseline & every 3 months
- 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
- common (> 10%)
- hot flashes (49%), facial flushing exacerbated by EtOH
- gynecomastia & breast pain (38-39%)
- 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
- uncomon (< 1%)
- 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
- androgen antagonist
- competitively blocks nuclear androgen receptors
- compensatory increases in LH & testosterone may occur
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ AHFS Drug Information, American Society of Health-System Pharmacists, Bethesda, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com