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Bicalutamide (Bicalutamide) - Warnings and Precautions

 
 



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 Tablets, USP. 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 Tablets, USP patients in controlled clinical trials.

Serum transaminase levels should be measured prior to starting treatment with Bicalutamide Tablets, USP, 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 Tablets, USP should be immediately discontinued with close follow-up of liver function.

Gynecomastia and Breast Pain

In clinical trials with Bicalutamide Tablets, USP 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.

Glucose Tolerance

A reduction in glucose tolerance has been observed in males receiving LHRH agonists. This may manifest as diabetes or loss of glycemic control in those with pre-existing diabetes. Consideration should therefore be given to monitoring blood glucose in patients receiving Bicalutamide Tablets, USP in combination with LHRH agonists.

Laboratory Tests

Regular assessments of serum Prostate Specific Antigen (PSA) may be helpful in monitoring the patient's response. If PSA levels rise during Bicalutamide Tablets, USP therapy, the patient should be evaluated for clinical progression. For patients who have objective progression of disease together with an elevated PSA, a treatment-free period of antiandrogen, while continuing the LHRH analog, may be considered.

USE IN SPECIFIC POPULATIONS

Pregnancy

PREGNANCY CATEGORY X [see Contraindications]. Based on its mechanism of action, Bicalutamide Tablets, USP may cause fetal harm when administered to a pregnant woman. Bicalutamide Tablets, USP are 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.

While there are no human data on the use of Bicalutamide Tablets, USP in pregnancy and Bicalutamide Tablets, USP are not for use in women, it is important to know that maternal use of an androgen receptor inhibitor could affect development of the fetus.

In animal reproduction studies, male offspring of rats receiving doses of 10 mg/kg/day (approximately 2/3 of clinical exposure at the recommended dose) and above, were observed to have reduced anogenital distance and hypospadias. These pharmacological effects have been observed with other antiandrogens. No other teratogenic effects were observed in rabbits receiving doses up to 200 mg/kg/day (approximately 1/3 of clinical exposure at the recommended dose) or rats receiving doses up to 250 mg/kg/day (approximately 2 times the clinical exposure at the recommended dose).

Nursing Mothers

Bicalutamide Tablets, USP are not indicated for use in women.

Pediatric Use

The safety and effectiveness of Bicalutamide Tablets, USP in pediatric patients have not been established.

Labeling describing pediatric clinical studies for bicalutamide is approved for AstraZeneca Pharmaceuticals LP's bicalutamide tablet. However, due to AstraZeneca Pharmaceuticals LP's marketing exclusivity rights, a description of those clinical studies is not approved for this bicalutamide labeling.

Geriatric Use

In two studies in patients given 50 or 150 mg daily, no significant relationship between age and steady-state levels of total bicalutamide or the active R-enantiomer has been shown.

Hepatic Impairment

Bicalutamide Tablets, USP should be used with caution in patients with moderate-to-severe hepatic impairment. Bicalutamide Tablets, USP are extensively metabolized by the liver. Limited data in subjects with severe hepatic impairment suggest that excretion of Bicalutamide Tablets, USP may be delayed and could lead to further accumulation. Periodic liver function tests should be considered for hepatic-impaired patients on long-term therapy [see Warnings and Precautions].

No clinically significant difference in the pharmacokinetics of either enantiomer of bicalutamide was noted in patients with mild-to-moderate hepatic disease as compared to healthy controls. However, the half-life of the R-enantiomer was increased approximately 76% (5.9 and 10.4 days for normal and impaired patients, respectively) in patients with severe liver disease (n=4).

Renal Impairment

Renal impairment (as measured by creatinine clearance) had no significant effect on the elimination of total bicalutamide or the active R-enantiomer.

Women

Bicalutamide has not been studied in women.

Page last updated: 2010-11-16

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