Bicalutmide
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Bicalutamide is an anti-androgen drug used to treat prostate cancer. It works by binding to androgen receptors to prevent the activation of genes by androgens like testosterone. It is well absorbed orally and metabolized in the liver. Common side effects include hot flashes, diarrhea, nausea and elevated liver enzymes. It should not be used by pregnant females or those with a hypersensitivity to bicalutamide.
![Chemical name
Systematic (IUPAC) name
N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide.](https://image.slidesharecdn.com/bicalutmide-131224153520-phpapp01/85/Bicalutmide-4-320.jpg)
Bicalutmide
- 1. Bicalutamide
- 2. Objective • • • • • • • • • • • Drug name Chemical name group mechanism of action Pharmacodynamics Pharmacokinetics Pharmacotherapeutics Dosage & administration Side effects Contraindications references
- 3. Drug name • Bicalutamide is marketed by AstraZeneca with the brand names Casodex , Cosudex, Calutide and Kalumid
- 4. Chemical name Systematic (IUPAC) name N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide.
- 5. group • Bicalutamide belongs to a group of medicines known as antiandrogens.
- 6. mechanism of action • Bicalutamide acts as a pure anti-androgen by binding to the androgen receptor (AR) and preventing the activation of the AR and subsequent upregulation of androgen responsive genes by androgenic hormones. • In addition, bicalutamide accelerates the degradation of the androgen receptor.
- 7. pharmacodynamics • bicalutimde blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue.
- 8. pharmacokinetics • Absorption is well-absorbed following oral administration, although the absolute bioavailability is unknown Well absorbed from the GI tract. • Metabolism Extensively hepatic by oxidation and glucuronidation. • Excretion in Urine and faeces. • Half-life 6-7 days.
- 9. pharmacotherapeutics • Bicalutamide is indicated for the treatment of stage D2 metastatic prostate cancer in combination with a luteinizing hormone-releasing hormone analogue or as a monotherapy. • It has also been used in clinical trials for ovarian cancer. • Bicalutamide is currently tested for treatment of androgen receptor positive ER-/PR- metastatic breast cancer.
- 10. Dosage & administration • orally administration. • Bicalutamide (Casodex®) is a tablet, which is taken once a day. It is available in two different strengths: 50mg and 150mg.
- 11. Side effects • • • • • • • • hot flushes gastrointestinal disorders diarrhea & nausea hepatic changes (elevated levels of transaminases, jaundice) pruritus Hot flushes Weakness Weight gain
- 12. Contraindications • is contraindicated in patients who have shown a hypersensitivity reaction to its use. • Bicalutamide is a teratogen and must not be handled by females who are or may become pregnant. It is known to cause fetal harm. • Enhances effect of coumarin anticoagulants.
- 13. references • British National Formulary; 63rd Edition (Mar 2012) British Medical Association and Royal Pharmaceutical Society of Great Britain, London (link to current BNF) • http://www.mims.com/USA/drug. • Sweetman, et al. Martindale: The Complete Drug Reference. 36th edition. 2009. Pharmaceutical Press • http://www.cancerresearchuk.org/cancer-help. • Risbridger ,G.P et al.Breast and prostate cancer more similiar than diffrent .Nature (2010)