Bicatero

White coloured, round shaped, biconvex, film-coated tablets debossed with '2' on one side and 'H' on other side.
For the use of Registered Medical Practitioner or a Hospital or a Laboratory only.
Each film-coated tablet contains Bicalutamide 50 mg.

Pharmacology: Pharmacodynamics: Bicalutamide is a nonsteroidal androgen receptor inhibitor. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. 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.
Pharmacokinetics: Absorption: Rapid and complete; unaffected by food.
Protein binding: 96%.
Metabolism: Extensively hepatic; glucuronidation and oxidation of the R (active) enantiomer to inactive metabolites; the S enantiomer is inactive.
Half-life elimination: Active enantiomer: ~6 days, ~10 days in severe liver disease.
Time to peak, plasma: Active enantiomer: ~31 hours.
Excretion: Urine (36%, as inactive metabolites); feces (42%, as unchanged drug and inactive metabolites).

Treatment of metastatic prostate cancer (in combination with an LHRH analogue therapy or surgical castration).

Oral: Adults: Prostate cancer, metastatic: One tablet (50 mg) once daily (in combination with an LHRH analogue).
Dosage adjustment in renal impairment: No adjustment required.
Dosage adjustment in hepatic impairment: No adjustment required for mild, moderate, or severe hepatic impairment; use caution with moderate-to-severe impairment. Discontinue if ALT >2 times ULN or patient develops jaundice.
Administration: Dose should be taken at the same time each day with or without food. Treatment for metastatic cancer should be started concomitantly with an LHRH analogue.

Treatment: There is no specific antidote; treatment of an overdose should be symptomatic.
In this patient population, multiple drugs may have been taken. Dialysis is not likely to be helpful since bicalutamide is highly protein bound and is extensively metabolized. General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated.

Hypersensitivity to bicalutamide or any component of the formulation; use in women and children; co-administration with terfenadine, astemizole or cisapride.
Use in Children: Safety and effectiveness of bicalutamide in children have not been established, and its use in children is contraindicated.

Hepatitis: Rare cases of death or hospitalization because of severe liver injury have been reported during postmarketing in association with the use of bicalutamide. Hepatotoxicity in these reports generally occurred within the first 3 to 4 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.
Measure serum transaminase levels prior to starting treatment with bicalutamide, at regular intervals for the first 4 months of treatment, and periodically thereafter. If clinical symptoms or signs suggestive of liver dysfunction occur (eg, nausea, vomiting, abdominal pain, fatigue, anorexia, flu-like syndromes, dark urine, jaundice, or right upper quadrant tenderness), measure the serum transaminases, in particular the serum ALT, immediately. If at any time a patients has jaundice or their ALT rises above 2 times the upper limit of normal (ULN), immediately discontinue bicalutamide, 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.
Glucose tolerance: A reduction in glucose tolerance has been observed in men receiving LHRH agonists. This may manifest as diabetes or loss of glycemic control in those with preexisting diabetes. Therefore, give careful consideration to monitoring blood glucose in patients receiving bicalutamide in combination with LHRH agonists.
Hypersensitivity reactions: Hypersensitivity reactions, including angioneurotic edema and urticaria, have been reported.
Hepatic function impairment: Use bicalutamide with caution in patients with moderate to severe hepatic impairment. Bicalutamide is extensively metabolized by the liver. Limited data in subjects with severe hepatic impairment suggest that excretion of bicalutamide may be delayed and could lead to further accumulation. Consider periodic liver function tests for hepatically impaired patients on long-term therapy.

Pregnancy: Pregnancy Category X.
Bicalutamide may cause fetal harm when administered to a pregnant woman. Bicalutamide is contraindicated in women, including those who are or may become pregnant. There are no studies in pregnant women using bicalutamide. If this drug is used during pregnancy or if the patient becomes pregnant while taking this drug, apprise the patient of the potential hazard to the fetus.
While there are no human data on the use of bicalutamide in pregnancy and bicalutamide is not for use in women, it is important to know that maternal use of an androgen receptor inhibitor could affect development of the fetus.
Lactation: Bicalutamide is not indicated for use in women, and its use in women is contraindicated.

Adverse reaction percentages reported as part of combination regimen with an LHRH analogue unless otherwise noted.
Incidence >10%: Cardiovascular: Peripheral edema.
Central nervous system: Pain.
Endocrine & metabolic: Hot flashes, breast pain, gynecomastia.
Gastrointestinal: Constipation, nausea, diarrhea, abdominal pain.
Genitourinary: Pelvic pain, hematuria, nocturia.
Hematologic: Anemia.
Neuromuscular & skeletal: Back pain, weakness.
Respiratory: Dyspnea.
Miscellaneous: Infection.
Incidence ≥2% to 10%: Cardiovascular: Chest pain, hypertension, angina pectoris, cardiac arrest, CHF, edema, MI, coronary artery disorder, syncope.
Central nervous system: Dizziness, headache, insomnia, anxiety, depression, chills, confusion, fever, nervousness, somnolence.
Dermatologic: Rash, alopecia, dry skin, pruritus, skin carcinoma.
Endocrine & metabolic: Hyperglycemia, dehydration, gout, hypercholesterolemia, libido decreased.
Gastrointestinal: Dyspepsia, weight loss, anorexia, flatulence, vomiting, weight gain, dysphagia, gastrointestinal carcinoma, melena, periodontal abscess, rectal hemorrhage, xerostomia.
Genitourinary: Urinary tract infection, impotence, polyuria, urinary retention, urinary impairment, urinary incontinence, dysuria, urinary urgency.
Hepatic: LFTs increased, alkaline phosphatase increased.
Neuromuscular & skeletal: Bone pain, paresthesia, myasthenia, arthritis, pathological fracture, hypertonia, leg cramps, myalgia, neck pain, neuropathy.
Ocular: Cataract.
Renal: BUN increased, creatinine increased, hydronephrosis.
Respiratory: Cough, pharyngitis, bronchitis, pneumonia, rhinitis, asthma, epistaxis, sinusitis.
Miscellaneous: Flu-like syndrome, diaphoresis, cyst, hernia, herpes zoster, sepsis.

Anticoagulants: In vitro studies have shown bicalutamide can displace coumarin anticoagulants, such as warfarin, from their protein-binding sites. It is recommended that if bicalutamide is started in patients already receiving coumarin anticoagulants, closely monitor prothrombin times and adjust the anticoagulant dose if necessary.
Cytochrome P-450 system: R-bicalutamide is an inhibitor of CYP3A4. Coadministration with midazolam has shown mean midazolam levels increased 1.5-fold (for maximum plasma concentration) and 1.9-fold (for area under the curve). Exercise caution when bicalutamide is coadministered with CYP3A4 substrates.

Storage and Handling: Store below 30°C and protect from moisture.

Cancer Hormone Therapy

L02BB03 - bicalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.

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