Bicalutamide: Anti-Androgen Prostate Cancer Hormone Treatment

Indications for Bicalutamide

Anti-androgen hormone treatment of prostate cancer with bicalutamide is a therapeutic option against prostate cancer in the following situations:

Hormonal treatment of metastatic prostate cancer
Adjuvant therapy of advanced prostate cancer after external beam radiation therapy (EBRT) or radical prostatectomy.
Conservative treatment of locally advanced prostate cancer with lower urinary tract symptoms (LUTS)
Reduction of prostate volume before brachytherapy of prostate cancer

Mechanism of Action of Bicalutamide

Bicalutamide is a nonsteroidal anti-androgen drug, which shows competitive antagonism in relation to the androgen receptor.

Pharmacokinetics of Bicalutamide

Good absorption after oral ingestion
Over 95% plasma protein binding
Hepatic metabolism, renal and biliary excretion. Elimination half life: 1.3 days. Metabolites from bicalutamide are pharmacologically active and lead to an effective half life of 7 days for active metabolites.

Side Effects of Bicalutamide

Bicalutamide shows typical side effects of antiandrogens: gynecomastia, hot flushes, decreased libido, decreased erectile function. Sexual side effects are less pronounced than with LHRH treatment.
Abdominal pain, diarrhea or nausea (15%), rarely vomiting.
Increased liver enzymes (7%) or jaundice.
Fluid retention, cardiac decompensation
Anemia (frequently), rarely leukopenia, thrombocytopenia
Allergic reactions

Interactions with Bicalutamide

Warfarin (displacement from the plasma protein binding), terfenadine or cisapride (inhibition of cytochromes).

Contraindications for Bicalutamide

Increased liver enzymes warrant dose reduction and regular laboratory monitoring. Bicalutamide should be stopped in progressive elevation of liver transaminases without evidence of liver metastases. Further contraindications are allergy, bicalutamide has no indications in women and children.

Dosage of Bicalutamide

In Germany, two dosages of bicalutamide are approved: 50 mg p.o. 1-0-0 or 150 mg 1-0-0 p.o:

150 mg/d bicalutamide is recommended for antiandrogenic monotherapy (as an alternative to LHRH-treatment).

50 mg bicalutamide 1-0-0 p.o. is sufficient to prevent the testosterone flare at the start of LHRH therapy or in combination with LHRH treatment (maximal androgen blockade, MAB).

Flutamide

Index

Cephalosporins

Index: 1–9 A B C D E F G H I J K L M N O P Q R S T U V W X Y Z

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References

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Deutsche Version: Bicalutamid

Last update:

Dr. med. Dirk Manski (E-Mail)