Bicalutamide

Pronunciation

(bye ka LOO ta mide)

U.S. Brand Names

Casodex®

Synonyms

CDX; ICI-176334

Generic Available

Canadian Brand Names

Casodex®

Use

In combination therapy with LHRH agonist analogues in treatment of advanced prostatic carcinoma

Pregnancy Risk Factor

Lactation

Excretion in breast milk unknown

Contraindications

Hypersensitivity to bicalutamide or any component of the formulation; pregnancy

Warnings/Precautions

Rare cases of death or hospitalization due to hepatitis have been reported postmarketing. Use with caution in moderate to severe hepatic dysfunction. Hepatotoxicity generally occurs within the first 3-4 months of use. Baseline liver function tests should be obtained and repeated regularly during the first 4 months of treatment, and periodically thereafter. Additionally, patients should be monitored for signs and symptoms of liver dysfunction. Bicalutamide should be discontinued if patients have jaundice or ALT is two times the upper limit of normal. May cause gynecomastia in a high percentage of patients.

Adverse Reactions

>10%: Endocrine & metabolic: Hot flashes (8% to 24% in combination with LHRH agonists), gynecomastia (23% to 62%), breast tenderness (25% to 60%)

2% to <5%:

Cardiovascular: Angina pectoris, CHF, edema

Central nervous system: Anxiety, depression, confusion, somnolence, nervousness, fever, chills

Dermatologic: Dry skin, pruritus, alopecia

Endocrine & metabolic: Breast pain, diabetes mellitus, decreased libido, dehydration, gout

Gastrointestinal: Anorexia, dyspepsia, rectal hemorrhage, xerostomia, melena, weight gain

Genitourinary: Polyuria, urinary impairment, dysuria, urinary retention, urinary urgency

Hepatic: Alkaline phosphatase increased

Neuromuscular & skeletal: Myasthenia, arthritis, myalgia, leg cramps, pathological fracture, neck pain, hypertonia, neuropathy

Renal: Creatinine increased

Respiratory: Cough increased, pharyngitis, bronchitis, pneumonia, rhinitis, lung disorder

Miscellaneous: Sepsis, neoplasma

<1%: Diarrhea

Overdosage/Toxicology

Symptoms of overdose include hypoactivity, ataxia, anorexia, vomiting, slow respiration, and lacrimation. Management is supportive. Dialysis is of no benefit.

Drug Interactions

In vitro displacement of warfarin by bicalutamide

Stability

Store at room temperature

Mechanism of Action

Pure nonsteroidal antiandrogen that binds to androgen receptors; specifically a competitive inhibitor for the binding of dihydrotestosterone and testosterone; prevents testosterone stimulation of cell growth in prostate cancer

Pharmacodynamics/Kinetics

Absorption: Rapid and complete

Protein binding: 96%

Metabolism: Extensively hepatic; stereospecific metabolism

Half-life elimination: Up to 10 days; active enantiomer 5.8 days

Excretion: Urine and feces (as unchanged drug and metabolites)

Dosage

Adults: Oral: 50-150 mg/day

Dosage adjustment in renal impairment: None necessary as renal impairment has no significant effect on elimination

Dosage adjustment in liver impairment: Limited data in subjects with severe hepatic impairment suggest that excretion of bicalutamide may be delayed and could lead to further accumulation. Use with caution in patients with moderate to severe hepatic impairment.

Administration

Dose should be taken at the same time each day with or without food; start treatment at the same time as treatment with an LHRH analog

Monitoring Parameters

CBC, ECG, echocardiograms, and serum testosterone and luteinizing hormone (periodically). Liver function tests should be obtained at baseline and repeated regularly during the first 4 months of treatment, and periodically thereafter; monitor for signs and symptoms of liver dysfunction. (discontinue if jaundice is noted or ALT is two or more times the upper limit of normal).

Dietary Considerations

May be taken with or without food.

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take as directed, at the same time each day, with or without food. Do not alter dose or discontinue without consulting prescriber. Void before taking medication. If you have diabetes, monitor serum glucose closely and notify prescriber of changes (this medication may alter glucose levels). May cause dizziness, confusion, or drowsiness (use caution when driving or engaging in tasks that require alertness until response to drug is known); nausea or vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); constipation (increased exercise, fluids, fruit, or fiber may help); hair loss; or impotence. Report easy bruising or bleeding; yellowing of skin or eyes; change in color of urine or stool; unresolved CNS changes (eg, nervousness, chills, insomnia, somnolence); skin rash, redness, or irritation; chest pain or palpitations; respiratory difficulty; urinary retention or inability to void; muscle weakness, tremors, or pain; persistent nausea, vomiting, diarrhea, constipation; or other unusual signs or adverse reactions. Pregnancy/breast-feeding precautions: This drug will cause fetal abnormalities - consult prescriber for effective contraceptives. Consult prescriber if breast-feeding.

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May produce anxiety, depression, and confusion

Mental Health: Effects on Psychiatric Treatment

None reported

Oncology: Emetic Potential

Very low (<10%)

Dosage Forms

Tablet: 50 mg

References

Blackledge GR, Cockshott ID, and Furr BJ, "Casodex (Bicalutamide): Overview of a New Antiandrogen Developed for the Treatment of Prostate Cancer," Eur Urol , 1997, 31(Suppl 2):30-9.

Goa KL and Spencer CM, "Bicalutamide in Advanced Prostate Cancer. A Review," Drugs Aging , 1998, 12(5):401-22

Kennealey GT and Furr BJ, "Use of the Nonsteroidal Antiandrogen Casodex in Advanced Prostatic Carcinoma," Urol Clin North Am , 1991, 18(1):99-110.

Kolvenbag GJ and Blackledge GR, "Worldwide Activity and Safety of Bicalutamide: A Summary Review," Urology , 1996, 47(1A Suppl):70-9.

Kolvenbag GJ and Nash A, "Bicalutamide Dosages Used in the Treatment of Prostate Cancer," Prostate , 1999, 39(1):47-53.

Kolvenbag GJ, Blackledge GR, and Gotting-Smith K, "Bicalutamide (Casodex) in the Treatment of Prostate Cancer: History of Clinical Development," Prostate , 1998, 34(1):61-72.

Mahler C, Verhelst J, and Denis L, "Clinical Pharmacokinetics of the Antiandrogens and Their Efficacy in Prostate Cancer," Clin Pharmacokinet , 1998, 34(5):405-17.

Migliari R, Muscas G, Murru M, et al, "Antiandrogens: A Summary Review of Pharmacodynamic Properties and Tolerability in Prostate Cancer Therapy," Arch Ital Urol Androl , 1999, 71(5):293-302.

Tyrrell CJ, "Casodex: A Pure Nonsteroidal Antiandrogen Used as Monotherapy in Advanced Prostate Cancer," Prostate Suppl , 1992, 4:97-104.

International Brand Names

Androxinon® (AR); Bicalutamida Delta Farma® (AR); Bicaprost® (AR); Bidrostat® (AR); Casodex® (AR, AT, BE, BR, CA, CH, CL, CY, CZ, DE, DK, EC, EG, ES, FI, FR, GB, HR, HU, ID, IE, IL, IT, JO, KW, LB, LU, MT, MX, NL, NO, PL, PT, RO, RU, SE, SG, SI, SY, TH, TR, YU, ZA); Cosudex® (AU); Dimalan® (AR); Gepeprostin® (AR); Imda® (AR); Liberprost® (AR); Lutamidal® (CO); Raffolutil® (AR)

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