Bicalutamide

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[edit] BRAND NAMES

[edit] STRUCTURE

Bicalutamide.jpg

[edit] MECHANISM OF ACTION

Prostatic carcinoma is known to be androgen sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen.

Bicalutamide is a non-steroidal antiandrogen that binds to androgen receptors preventing testosterone stimulation of cell growth in prostate cancer

[edit] INDICATIONS

Bicalutamide is indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog also known as gonadotrophin-releasing hormone (GnRH) agonists such as goserelin, leuprorelin and triptorelin, for the treatment of Stage D2 metastatic carcinoma of the prostate.

Long-acting luteinising hormone-releasing hormone (LHRH), suppress testosterone production to castration levels within 2–3 weeks of treatment initiation. However, LHRH agonist treatment causes an initial increase in testosterone, known as a surge, which can lead to a flare in clinical symptoms. Bicalutamide decrease incidence of clinical flare

[edit] DOSAGE

Usual dose is one 50 mg tablet once daily (morning or evening), with or without food. Start treatment at the same time with LHRH analog. Take at the same time daily without regards to food

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to Bicalutamide
  • Pregnancy

[edit] WARNINGS AND PRECAUTIONS

  • Hepatitis: Cases of death or hospitalization due to severe liver injury (hepatic failure) have been reported post-marketing in association with the use of Bicalutamide. Hepatotoxicity in these reports generally occurred within the first three to four months of treatment. Hepatitis or marked increases in liver enzymes leading to drug discontinuation occurred in approximately 1% of Bicalutamide patients in controlled clinical trials. Serum transaminase levels should be measured prior to starting treatment with Bicalutamide, at regular intervals for the first four months of treatment, and periodically thereafter. If clinical symptoms or signs suggestive of liver dysfunction occur (e.g., nausea, vomiting, abdominal pain, fatigue, anorexia, “flu-like” symptoms, dark urine, jaundice, or right upper quadrant tenderness), the serum transaminases, in particular the serum ALT, should be measured immediately. If at any time a patient has jaundice, or their ALT rises above two times the upper limit of normal, Bicalutamide should be immediately discontinued with close follow-up of liver function.
  • Gynecomastia and Breast Pain: In clinical trials with Bicalutamide 150 mg as a single agent for prostate cancer, gynecomastia and breast pain have been reported in up to 38% and 39% of patients, respectively.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category X (US). Bicalutamide may cause fetal harm when administered to a pregnant woman. Bicalutamide is contraindicated in women, including those who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus.

[edit] SIDE EFFECTS

Possible adverse reactions in patients receiving Bicalutamide plus an LHRH-Agonist include: hot flashes, pain (including general, back, pelvic and abdominal), asthenia, constipation, infection, nausea, peripheral edema, dyspnea, diarrhea, hematuria, nocturia, anemia, decreased libido and leg cramps.

Bicalutamide may also cause dizziness, confusion, or drowsiness (patients who experience this symptom should observe caution when driving or operating machines)

[edit] RELATED LINKS

Hormone Therapy for Prostate Cancer

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Androgens
Agonists Androstanolone   Dihydrotestosterone   Fluoxymesterone   Mesterolone   Methyltestosterone   Testosterone
Antiandrogens Androgen antagonists Bicalutamide   Chlormadinone acetate   Cyproterone acetate   Dienogest   Drospirenone   Flutamide   Nilutamide   Spironolactone
5α reductase inhibitors Dutasteride (Avodart)   Finasteride (Proscar)