Bicamed 50

Bicamed 50

bicalutamide

Manufacturer:

Hetero Labs

Distributor:

Medicell Pharma
Full Prescribing Info
Contents
Bicalutamide.
Description
Each film coated tablet contains 50 mg of Bicalutamide.
Bicalutamide Tablets contain 50 mg of bicalutamide, a non-steroidal androgen receptor inhibitor with no other known endocrine activity. The chemical name is propanamide, N [4 cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]- 2-hydroxy-2-methyl-,(+-).
Bicalutamide is a racemate with its antiandrogenic activity being almost exclusively exhibited by the R-enantiomer of bicalutamide; the S-enantiomer is essentially inactive.
The inactive ingredients of Bicalutamide Tablets are Lactose monohydrate, Crospovidone, Povidone, Magnesium stearate and Opadry White (HPMC 2910/ Hypromellose 5 cp (E464) 62.500% w/w,Titanium dioxide (E171), Macrogol/PEG 400).
Action
Pharmacotherapeutic group: Antiandrogen. ATC code: L02 B B03.
Pharmacology: Pharmacodynamics: Bicalutamide is a non-steroidal antiandrogen, devoid of other endocrine activity. It binds to androgen receptors without activating gene expression, and thus inhibits the androgen stimulus. Regression of prostatic tumours results from this inhibition. Clinically, discontinuation of Bicalutamide can result in antiandrogen withdrawal syndrome in a subset of patients.
Bicalutamide is a racemate with its antiandrogenic activity being almost exclusively in the (R)-enantiomer.
Pharmacokinetics: Bicalutamide is well absorbed following oral administration. There is no evidence of any clinically relevant effect of food on bioavailability.
The (S)-enantiomer is rapidly cleared relative to the (R)-enantiomer, the latter having a plasma elimination half-life of about 1 week.
On daily administration of Bicalutamide, the (R)-enantiomer accumulates about 10 fold in plasma as a consequence of its long half-life.
Steady state plasma concentrations of the (R)-enantiomer of approximately 9 microgram/ml are observed during daily administration of 50 mg doses of Bicalutamide. At steady state the predominantly active (R)-enantiomer accounts for 99% of the total circulating enantiomers.
The pharmacokinetics of the (R)-enantiomer are unaffected by age, renal impairment or mild to moderate hepatic impairment. There is evidence that for subjects with severe hepatic impairment, the (R)-enantiomer is more slowly eliminated from plasma.
Bicalutamide is highly protein bound (racemate 96% (R)-enantiomer>99%) and extensively metabolised (via oxidation and glucuronidation): Its metabolites are eliminated via the kidneys and bile in approximately equal proportions.
In a clinical study the mean concentration of R-bicalutamide in semen of men receiving Bicalutamide 150 mg was 4.9 microgram/ml. The amount of bicalutamide potentially delivered to a female partner during intercourse is low and by extrapolation possibly equates to approximately 0.3 microgram/kg. This is below that required to induce changes in offspring of laboratory animals.
Toxicology: Preclinical safety data: Bicalutamide is a potent antiandrogen and a mixed function oxidase enzyme inducer in animals. Target organ changes, including tumour induction, in animals, are related to these activities. None of the findings in the preclinical testing is considered to have relevance to the treatment of advanced prostate cancer patients.
Indications/Uses
Treatment of advanced prostate cancer in combination with LHRH analogue therapy or surgical castration.
Dosage/Direction for Use
Adult males including the elderly: one tablet (50 mg) once a day.
Treatment with Bicalutamide should be started at the same time as treatment with an LHRH analogue or surgical castration.
Children: Bicalutamide is contraindicated in children.
Renal impairment: no dosage adjustment is necessary for patients with renal impairment.
Hepatic impairment: no dosage adjustment is necessary for patients with mild hepatic impairment. Increased accumulation may occur in patients with moderate to severe hepatic impairment (see Precautions).
Overdosage
There is no human experience of overdosage. There is no specific antidote; treatment should be symptomatic. Dialysis may not be helpful, since Bicalutamide is highly protein bound and is not recovered unchanged in the urine. General supportive care, including frequent monitoring of vital signs, is indicated.
Contraindications
Bicalutamide is contraindicated in females and children (see Use in Pregnancy & Lactation).
Bicalutamide must not be given to any patient who has shown a hypersensitivity reaction to the active substance or to any of the excipients of this product.
Co-administration of terfenadine, astemizole or cisapride with Bicalutamide is contraindicated (see Interactions).
Special Precautions
Initiation of treatment should be under the direct supervision of a specialist.
Bicalutamide is extensively metabolised in the liver. Data suggests that its elimination may be slower in subjects with severe hepatic impairment and this could lead to increased accumulation of Bicalutamide. Therefore, Bicalutamide should be used with caution in patients with moderate to severe hepatic impairment.
Periodic liver function testing should be considered due to the possibility of hepatic changes. The majority of changes are expected to occur within the first 6 months of Bicalutamide therapy.
Severe hepatic changes and hepatic failure have been observed rarely with Bicalutamide, and fatal outcomes have been reported (see Adverse reactions). Bicalutamide therapy should be discontinued if changes are severe.
A reduction in glucose tolerance has been observed in males receiving LHRH agonists. This may manifest as diabetes or loss of glycaemic control in those with pre-existing diabetes. Consideration should therefore be given to monitoring blood glucose in patients receiving Bicalutamide in combination with LHRH agonists.
Bicalutamide has been shown to inhibit cytochrome P450 (CYP 3A4), as such caution should be exercised when co-administered with drugs metabolised predominantly by CYP 3A4 (see Contraindications and Interactions).
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on Ability to Drive and Use Machines: Bicalutamide is unlikely to impair the ability of patients to drive or operate machinery. However, it should be noted that occasionally somnolence may occur. Any affected patients should exercise caution.
Use In Pregnancy & Lactation
Bicalutamide is contraindicated in females and must not be given to pregnant women or nursing mothers.
Adverse Reactions
In this section, undesirable effects are defined as follows: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (< 1/10,000); not known (cannot be estimated from the available data). (See table.)

Click on icon to see table/diagram/image

Rare cardiovascular effects such as angina, heart failure, conduction defects including PR and QT interval prolongations, arrhythmias and non-specific ECG changes have been observed.
Thrombocytopenia has been reported uncommonly.
In addition, the following adverse experiences were reported in clinical trials (as possible adverse drug reactions in the opinion of investigating clinicians, with a frequency of ≥1%) during treatment with bicalutamide plus an LHRH analogue.
No causal relationship of these experiences to drug treatment has been made and some of the experiences reported are those that commonly occur in elderly patients: Cardiovascular system: heart failure.
Gastrointestinal system: anorexia, dry mouth, dyspepsia, constipation, flatulence.
Central nervous system: dizziness, insomnia, somnolence, decreased libido.
Respiratory system: dyspnoea.
Urogenital: impotence, nocturia.
Haematological: anaemia.
Skin and appendages: alopecia, rash, sweating, hirsutism.
Metabolic and nutritional: diabetes mellitus, hyperglycaemia, oedema, weight gain, weight loss.
Whole body: abdominal pain, chest pain, headache, pain, pelvic pain, chills.
Drug Interactions
There is no evidence of any pharmacodynamic or pharmacokinetic interactions between Bicalutamide and LHRH analogues.
In vitro studies have shown that R-bicalutamide is an inhibitor of CYP 3A4, with lesser inhibitory effects on CYP 2C9, 2C19 and 2D6 activity.
Although clinical studies using antipyrine as a marker of cytochrome P450 (CYP) activity showed no evidence of a drug interaction potential with Bicalutamide, mean midazolam exposure (AUC) was increased by up to 80%, after co-administration of Bicalutamide for 28 days. For drugs with a narrow therapeutic index such an increase could be of relevance. As such, concomitant use of terfenadine, astemizole and cisapride is contraindicated (see Contraindications) and caution should be exercised with the co-administration of Bicalutamide with compounds such as ciclosporin and calcium channel blockers. Dosage reduction may be required for these drugs particularly if there is evidence of enhanced or adverse drug effect. For ciclosporin, it is recommended that plasma concentrations and clinical condition are closely monitored following initiation or cessation of Bicalutamide therapy.
Caution should be exercised when prescribing Bicalutamide with other drugs which may inhibit drug oxidation e.g. cimetidine and ketoconazole. In theory, this could result in increased plasma concentrations of Bicalutamide which theoretically could lead to an increase in side effects.
In vitro studies have shown that Bicalutamide can displace the coumarin anticoagulant, warfarin, from its protein binding sites. It is therefore recommended that if Bicalutamide is started in patients who are already receiving coumarin anticoagulants, prothrombin time should be closely monitored.
Storage
Store below 30°C and protect from moisture.
ATC Classification
L02BB03 - bicalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.
Presentation/Packing
FC tab 50 mg (white colored, round shaped, biconvex, debossed with 2 on one side and H on the other side) x 30's.
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