post-title portfolio-title Bicalutamide Tablets USP 50mg Taj Pharma 2020-01-21 09:12:52 no no
  1. NAME OF THE MEDICINAL PRODUCT

Bicalutamide Tablets USP 50mg Taj Pharma
Bicalutamide Tablets USP 150mg Taj Pharma

  1. QUALITATIVE AND QUANTITATIVE COMPOSITION

a) Each film-coated tablet contains:
Bicalutamide USP? ? ? ? ? ? ? ? ? ? ? ? ? ? ??50mg
Excipients? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ?q.s
Colour: Titanium Dioxide USP

b) Each film-coated tablet contains:
Bicalutamide USP? ? ? ? ? ? ? ? ? ? ? ? ? ? ??150mg
Excipients? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ?q.s
Colour: Titanium Dioxide USP

For the full list of excipients, see section 6.1

  1. PHARMACEUTICAL FORM

Film-coated tablet.

  1. CLINICAL PARTICULARS

4.1 Therapeutic indications

Treatment of advanced prostate cancer in combination with luteinizing hormone-releasing hormone (LHRH) analogue therapy or surgical castration.

4.2 Posology and method of administration

Posology

Adult males including the elderly: one tablet (50mg) once a day.

Treatment with Bicalutamide Tablets 50mg should be started at least 3 days before commencing treatment with an LHRH analogue, or at the same time as surgical castration.

Paediatric population: Bicalutamide is contraindicated for use in children (see section 4.3 ).

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 Section 4.4).

4.3 Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

Use in females, children and adolescents is contraindicated (see section 4.6).

Co-administration of terfenadine, astemizole or cisapride with Bicalutamide is contra-indicated (see section 4.5).

4.4 Special warnings and precautions for use

Initiation of treatment should be under the direct supervision of a specialist.

Bicalutamide is extensively metabolized 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 Section 4.8).

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 Sections 4.3 and 4.5.

Androgen deprivation therapy may prolong the QT interval.

In patients with a history of or risk factors for QT prolongation and in patients receiving concomitant medicinal products that might prolong the QT interval (see section 4.5) physicians should assess the benefit risk ratio including the potential for Torsade de pointes prior to initiating Bicalutamide tablets.

Antiandrogen therapy may cause morphological changes in spermatozoa. Although the effect of bicalutamide on sperm morphology has not been evaluated and no such changes have been reported for patients who received Bicalutamide tablets, patients and/or their partners should follow adequate contraception during and for 130 days after Bicalutamide therapy.

Patients with rare hereditary problems of galactose intolerance, the total lactase deficiency or glucose-galactosemalabsorption should not take this medicinal product.

An increased Prothrombin Time (PT) and International Normalised Ratio (INR)have been reported in patients receiving bicalutamide and coumarin anticoagulants concomitantly.. Some cases have been associated with risk of bleeding. Close monitoring of PT/INR is advised and anticoagulant dose adjustment should be considered (see sections 4.5).

4.5 Interaction with other medicinal products and other forms of interaction

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 contra-indicated (see Section 4.3) and caution should be exercised with the co-administration of bicalutamide with compounds such as cyclosporin and calcium channel blockers. Dosage reduction may be required for these drugs particularly if there is evidence of enhanced or adverse drug effect. For cyclosporin, 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. There have been reports of increased Prothrombin Time (PT) and International Normalised Ratio (INR) when co-administered with bicalutamide. It is therefore recommended that if bicalutamide is administered in patients who are already receiving coumarin anticoagulants, PT/INR should be closely monitored.and adjustments of anticoagulant dose considered (see sections 4.4).

Since androgen deprivation treatment may prolong the QT interval, the concomitant use of Bicalutamide tablets with medicinal products known to prolong the QT interval or medicinal products able to induce Torsade de pointes such as class IA (e.g. quinidine, disopyramide) or class III (e.g. amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic medicinal products, methadone, moxifloxacin, antipsychotics, etc. should be carefully evaluated (see section 4.4).

Paediatric population

Interaction studies have only been performed in adults.

4.6 Fertility, pregnancy and lactation

Pregnancy

Bicalutamide is contra-indicated in females and must not be given to pregnant women.

Breast-feeding

Bicalutamide is contraindicated during breast-feeding.

Fertility

Reversible impairment of male fertility has been observed in animal studies (see section 5.3). A period of subfertility or infertility should be assumed in man.

4.7 Effects on ability to drive and use machines

Bicalutamide is unlikely to impair the ability of patients to drive or operate machinary. However, it should be noted that occasionally somnolence may occur. Any affected patients should exercise caution.

4.8 Undesirable effects

In this section, undesirable effects are defined as follows: very common (?1/10); common (?1/100, < 1/10); uncommon (?1/1,000, < 1/100); rare (?1/10,000, < 1/1,000); very rare (< 1/10,000); not known (cannot be estimated from the available data).

Table 1 Frequency of Adverse Reactions

System Organ Class Frequency Event
Blood and lymphatic system disorders Very common Anaemia
Immune system disorders Uncommon Hypersensitivity, angioedema and urticaria
Metabolism and nutrition disorders Common Decreased appetite
Psychiatric disorders Common Decreased libido depression
Nervous system disorders Very common Dizziness
Common Somnolence
Cardiac disorders Common Myocardial infarction (fatal outcomes have been reported)4, Cardiac failure4
Not known QT prolongation (see sections 4.4 and 4.5)
Vascular disorders Very common Hot flush
Respiratory, thoracic and mediastinal disorders Uncommon Interstitial lung disease5?(fatal outcomes have been reported).
Gastrointestinal disorders Very common Abdominal pain

constipation

nausea

Common Dyspepsia

flatulence

Hepato-biliary disorders Common Hepatotoxicity, jaundice, hypertransaminasaemia1
Rare Hepatic failure2?(fatal outcomes have been reported).
Skin and subcutaneous tissue disorders Common Alopecia

hirsutism/hair re-growth

dry skin

pruritus rash

Rare Photosensitivity reaction
Renal and urinary disorders Very common Haematuria
Reproductive system and breast disorders Very common Gynaecomastia and breast tenderness3
Common Erectile dysfunction
General disorders and administration site conditions Very common Asthenia oedema
Common Chest pain
Investigations Common Weight increased
  1. Hepatic changes are rarely severe and were frequently transient, resolving or improving with continued therapy or following cessation of therapy
  2. Listed as an adverse drug reaction following review of post-marketed data. Frequency has been determined from the incidence of reported adverse events of hepatic failure in patients receiving treatment in the open-label bicalutamide arm of the 150 mg EPC studies.
  3. May be reduced by concomitant castration.
  4. Observed in a pharmaco-epidemiology study of LHRH agonists and anti-androgens used in the treatment of prostate cancer. The risk appears to be increased when bicalutamide was used in combination with LHRH agonists but no increase in risk was evident when bicalutamide was used as a monotherapy to treat prostate cancer.
  5. Listed as an adverse drug reaction following review of post-marketed data. Frequency has been determined from the incidence of reported adverse events of interstitial pneumonia in the randomised treatment period of the 150 mg EPC studies.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product.

4.9 Overdose

There is no human experience of overdosage. There is no specific antidote; treatment should be symptomatic. Dialysis is 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.

  1. PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Hormone antagonists and related agent,Antiandrogens

Mechanism of action

Bicalutamide is non steroidalantiandrogen, devoid of other endocrine activity. It binds to androgen receptors without activating gene expression, and thus inhibits the androgen stimulus. Regression of prostatic tumors 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.

5.2 Pharmacokinetic properties

Absorption

Bicalutamide is well absorbed following oral administration. There is no evidence of any clinically relevant effect of food on bioavailability.

Distribution

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.

Biotranformation

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 Tablets 50mg, 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 Tablets. At steady state the predominantly active (R)-enantiomer accounts for 99% of the total circulating enantiomers.

Elimination

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.

Special Populations

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.

5.3 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. Atrophy of seminiferous tubules of the testes is a predicted class effect with antiandrogens and has been observed for all species examined. Reversal of testicular atrophy occurred 4 months after the completion of dosing in a 6-month rat study. No recovery was observed at 24 weeks after the completion of dosing in a 12-month rat study. Following 12-months of repeated dosing in dogs (at doses of approximately 7 times human therapeutic concentrations at the recommended human dose of 50 mg), the incidence of testicular atrophy was the same in dosed and control dogs after a 6 month recovery period. In a fertility study, male rats had an increased time to successful mating immediately after 11 weeks of dosing; reversal was observed after 7 weeks off-dose.

  1. PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Core tablet:Lactose monohydrate, Sodium starch glycolate,Povidone, Magnesium stearate

Coating:Hypromellose,Macrogol, Titanium dioxide.

6.2 Incompatibilities

Not applicable

6.3 Shelf life

2 years

6.4 Special precautions for storage

This medicinal product does not require any special storage conditions

6.5 Nature and contents of container

Tablets are packed in Bottle/Alu-Alu blisters

Pack Size of: 7, 14, 28, 30, 50, 90, 100 or 200 tablets.

Not all pack sizes may be marketed.

6.6 Special precautions for disposal and other handling

Any unused medicinal product or waste material should be disposed of in accordance with local requirements.

7.Manufactured in India By:
TAJ PHARMACEUTICALS LIMITED
at SURVEY NO.188/1 TO 189/1,190/1 TO 4,
ATHIYAWAD, DABHEL, DAMAN- 396210 (INDIA).

Bicalutamide Tablets USP 50mg/150mg Taj Pharma
(Bicalutamide)

Package leaflet: Information for the user

Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.

  • Keep this leaflet. You may need to read it again.
  • If you have any further questions, ask your doctor or pharmacist.
  • This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
  • If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet (see section 4).

What is in this leaflet:

  1. What bicalutamide is and what it is used for
    2. What you need to know before you take bicalutamide
    3. How to take bicalutamide
    4. Possible side effects
    5. How to store bicalutamide
    6. Contents of the pack and other information

 

  1. WHAT BICALUTAMIDE IS AND WHAT IT IS USED FOR

Bicalutamide 50mg film-coated Tablets (called bicalutamide throughout this leaflet) are used for the treatment of advanced prostate carcinoma. It is taken together with a drug known as a Luteinising Hormone-Releasing Hormone (LHRH) analogue – an additional hormone treatment – or with surgical removal of the testicles.

Bicalutamide is one of a group of medicines known as the non-steroidal anti-androgens. The active substance bicalutamide blocks the undesired effect of the male sex hormones (androgens) and inhibits cell growth in the prostate.

In a daily dose of 50 mg:

It is used in combination with other treatments such as drugs that reduce the androgen levels in the body.

  1. WHAT YOU NEED TO KNOW BEFORE YOU TAKE BICALUTAMIDE

Do not take bicalutamide:

  • if you are allergic to the active substance or to any of the other ingredients of this medicine (listed in section 6)
  • if you take terfenadine or astemizole (for hay fever or allergy) or cisapride (for stomach problems)
  • Bicalutamide should not be given to women, including pregnant women or nursing mothers or to children or adolescents.

Warnings and precautions

Talk to your doctor or pharmacist before taking bicalutamide

  • if the liver is moderately or severely impaired.The drug should only be taken after your doctor has carefully considered possible benefits and risks. If this is the case, your doctor will regularly perform tests of liver function (bilirubin, transaminases, alkaline phosphatase). If severe disturbances to liver function develop, treatment with bicalutamide should be discontinued.
  • If you have diabetes and are already taking an “LHRH analogue”.These include goserelin, buserelin, leuprorelin and triptorelin.

Other medicines and bicalutamide

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines.

Do not take bicalutamide together with any of the following medicines:

  • Terfenadine or astemizole (for hay fever or allergy)
  • Cisapride (for stomach problems)

If you take bicalutamide together with one of the following medicines, the effect of bicalutamide as well as the other medicine may be influenced. Please speak to your doctor before taking any of these medicines together with bicalutamide:

  • Warfarin or any similar medicine to prevent blood clots
  • Ciclosporin (used to suppress the immune system to prevent and treat rejection of a transplanted organ or bone marrow)
  • Cimetidine (to treat stomach ulcers)
  • Ketoconazole (used to treat fungal infections of the skin and nails)
  • Calcium channel blockers (to treat high blood pressure)

Taking bicalutamide with food, drink and alcohol

Take one bicalutamide tablet, preferably at the same time of the day with or without food.

Pregnancy, breast-feeding and fertility

Bicalutamide is contra-indicated in women and must not be given to pregnant women or breast-feeding mothers.

Driving and using machines

There is a possibility that these tablets could make you feel dizzy or drowsy. If you are affected in this way, you should not drive or operate machinery.

This product contains lactose

If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine.

  1. HOW TO TAKE BICALUTAMIDE

Always take this medicine exactly as your doctor or pharmacist has told you. Check with your doctor or pharmacist if you are not sure.

The doctor prescribes an appropriate dosage for you personally. The recommended dosage is one tablet daily.

Tablets are swallowed whole with some liquid. Try to take the product at approximately the same time each day.

If you take more bicalutamide than you should

If you have taken too many tablets, contact your doctor or the nearest hospital as soon as possible. Take the remaining tablets or the pack with you so the doctor can identify what you have taken.

If you forget to take bicalutamide

If you forget to take your daily dose, skip the missed dose and wait until the next administration time. Do not take a double dose to make up for a forgotten dose.

If you stop taking bicalutamide

Do not stop using the drug even if you feel healthy unless advised to do so by your doctor.

If you have any further questions on the use of this medicine, ask your doctor or pharmacist.

  1. POSSIBLE SIDE EFFECTS

Like all medicines, this medicine can cause side effects, although not everybody gets them.

You should contact your doctor straight away if you notice any of the following serious side effects:

Uncommon serious side effects?(may affect up to 1 in 100 people):

Serious allergic reaction which causes:

  • Rash, itching or hives on the skin
  • Swelling of the face, lips, tongue, throat or other parts of the body
  • Shortness of breath, wheezing or trouble breathing

If this happens to you,?see a doctor straight away.

Also tell your doctor straightaway if you notice any of the following side effects:

Very common side effects?(may affect more than 1 in 10 people):

  • Pain in your abdomen
  • Blood in your urine

Common side effects?(may affect up to 1in 10 people):

  • Yellowing of the skin or whites of the eyes (jaundice). These may be signs of liver problems or in rare cases (may affect up to 1 in 1,000 people) liver failure.

Uncommon side effects?(may affect up to 1 in 100 people):

  • Serious shortness of breath or shortness of breath which suddenly gets worse. This may be with a cough or high temperature (fever). These may be signs of an inflammation of the lungs called “interstitial lung disease”

Other possible side effects:

Very common side effects?(may affect more than 1 in 10 people):

  • Low levels of red blood cells (anaemia). This may make you feel tired or look pale.
  • Dizziness
  • Constipation, feeling sick (nausea)
  • Hot flushes
  • Feeling weak, swelling
  • Swelling and tenderness of your breasts.

Common side effects?(may affect up to 1 in 10 people):

  • Weight gain
  • Feeling sleepy
  • Indigestion, wind (flatulence)
  • Hair loss, hair re-growth or growth of extra hair
  • Skin rash, dry skin, itching
  • Decreased appetite
  • Chest pain
  • Being unable to get an erection
  • Reduced sex drive
  • Depression
  • Heart attack, reduced heart function
  • Changes in liver enzymes

Your doctor may do blood tests to check for any changes to your blood.

Reporting of side effects

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.

  1. HOW TO STORE BICALUTAMIDE

This medicinal product does not require any special storage conditions.

Keep this medicine out of the sight and reach of children.

Do not use this medicine after the expiry date which is stated on the carton (EXP). The expiry date refers to the last day of that month.

Do not use if you notice some visible signs of medicine deterioration.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.

  1. CONTENTS OF THE PACK AND OTHER INFORMATION

What Bicalutamide tablets contain:

a) Each film-coated tablet contains:
Bicalutamide USP? ? ? ? ? ? ? ? ? ? ? ? ? ? ??50mg
Excipients? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ?q.s
Colour: Titanium Dioxide USP

b) Each film-coated tablet contains:
Bicalutamide USP? ? ? ? ? ? ? ? ? ? ? ? ? ? ??150mg
Excipients? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ? ?q.s
Colour: Titanium Dioxide USP

Core tablet: Lactose monohydrate, Sodium starch glycolate, Povidone, Magnesium stearate

Coating:Hypromellose,Macrogol, Titanium dioxide.

What are the contents of the pack

Tablets are packed in Bottle/Alu-Alu blisters

Pack Size of: 7, 14, 28, 30, 50, 90, 100 or 200 tablets.

Not all pack sizes may be marketed.

7.Manufactured in India By:
TAJ PHARMACEUTICALS LIMITED
at SURVEY NO.188/1 TO 189/1,190/1 TO 4,
ATHIYAWAD, DABHEL, DAMAN- 396210 (INDIA).

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