Bicalutamide pills 150mg, 30pcs

Composition

Active ingredients:

bicalutamide 150 mg.

Auxiliary substances:

Lactose monohydrate (milk sugar) 183.0 mg,

Potato starch – 81.0 mg,

Povidone K 25 (polyvinylpyrrolidone K 25) – 21.0 mg,

Sodium Carboxymethyl starch – 9.0 mg,

Magnesium stearate – 3.0 mg,

Colloidal silicon dioxide – 3.0 mg.

Composition of the film shell:

Aquarius Prime VAR 218010 White [hypromellose-65% – 13.5 mg

. titanium dioxide-25%, macrogol (polyethylene glycol) – 10%]

Pharmacological action

Pharmacotherapy group

Antitumor agent-antiandrogen

ATX code

L02BB03

Pharmacodynamics :

Bicalutamide is a racemic mixture with non-steroidal antiandrogenic activity mainly of the (R) – enantiomer and has no other endocrine activity. Bicalutamide binds to androgen receptors and suppresses the stimulating effect of androgens without activating gene expression. The result is a regression of malignant neoplasms of the prostate gland.

In some patients, discontinuation of bicalutamide may lead to the development of a clinical “antiandrogen withdrawal syndrome”.

Pharmacokinetics:

After oral use, it is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect absorption.

The (S)-enantiomer is eliminated from the body much faster than the (R) – enantiomer. The half-life of the latter is about 7 days.

With daily use of bicalutamide, the concentration of the (R)-enantiomer in plasma increases approximately 10 times due to a long half-life, which makes it possible to take the drug once a day.

When bicalutamide is taken daily at a dose of 50 mg, the steady-state concentration of the (R)- enantiomer in plasma is about 9 micrograms/ml. When taking 150 mg of bicalutamide daily, the steady-state concentration of the (R) – enantiomer is approximately 22 micrograms / ml. At steady state, about 99% of all enantiomers circulating in the blood are the active (R)-enantiomer.

The pharmacokinetics of the (R)-enantiomer are not affected by age renal impairment mild to moderate hepatic impairment. There is evidence that the elimination of the (R)-enantiomer from plasma slows down in patients with severe hepatic impairment.

Plasma protein binding is high (96% for the racemic mixture and 996% for the (R) – enaptiomer). It is intensively metabolized in the liver (by oxidation and formation of conjugates with glucuronic acid). Metabolites are excreted in the urine and bile in approximately equal proportions.

Indications

– Common prostate cancer in combination with an analogue of GnRH (gonadotropin-releasing hormone) or surgical castration;

– locally advanced prostate cancer (T 3-T 4, any N M 0 T 1-T 2 N+ M 0) as monotherapy or adjuvant therapy in combination with radical prostatectomy or radiotherapy;

– nemetallicheskie locally advanced prostate cancer in the cases where surgical castration or other medical intervention inapplicable or inappropriate.

Use during pregnancy and lactation

Bicalutamide is contraindicated in women and should not be given to pregnant or nursing mothers

Contraindications

-Hypersensitivity to bicalutamide and auxiliary components of the drug;

– simultaneous use with terfenadine astemizole and cisapride;

– bicalutamide should not be prescribed to children and women.

Due to the presence of lactose in the composition: lactase deficiency lactose intolerance glucose-galactose malabsorption.

With caution:

Impaired liver function.

Side effects

The pharmacological action of bicalutamide may cause the following side effects:

– very common (>10%): gynecomastia (may persist even after discontinuation of therapy, especially if the drug is taken for a long time) soreness of the mammary glands” hot flashes”;>

– often (≥1% and

– rare (≥01% – :  hypersensitivity reactions including angioedema and urticaria interstitial lung diseases; when using the drug in a daily dose of 150 mg – abdominal pain depression dyspepsia hematuria;

– very rarely (≥001% – hepatic insufficiency (a causal relationship with bicalutamide intake has not been reliably established).

When bicalutamide and GnRH analogues are co-administered, the following side effects may also occur with a frequency of ≥ 1% (no causal relationship with the drug has been established Some of the reported side effects occurred in elderly patients):

From the cardiovascular system:  heart failure.

From the gastrointestinal tract:  anorexia dry mouth dyspepsia constipation flatulence.

From the central nervous system:  dizziness headache insomnia increased drowsiness.

Respiratory system disorders:  shortness of breath.

From the genitourinary system:  sexual dysfunction nocturia polyuria.

From the hematopoietic system: anemia.

From the skin and its appendages: alopecia skin rash increased sweating hirsutism.

Other services:  diabetes mellitus hyperglycemia increased or decreased body weight abdominal pain chest pain pelvic pain chills.

Interaction

There are no data on pharmacokinetic or pharmacodynamic interactions between bicalutamide and GnRH analogues.

In vitro studies have shown that the (R)-enantiomer of bicalutamide inhibits the CYP3A4 isoenzyme to a lesser extent affecting the activity of the CYP2C9 2C19 and 2D6 isoenzymes. Bicalutamide has not been shown to interact with other medicinal products, but when used for 28 days while taking midazolam, the area under the concentration-time curve (AUC) of midazolam increases by 80%.

Incompatible with terfenadine astemizole cisapride.

Caution should be exercised when prescribing bicalutamide concomitantly with cyclosporine or slow calcium channel blockers. It may be necessary to reduce the dose of these drugs, especially in the case of potentiation or development of side effects. After starting or discontinuing bicalutamide, careful monitoring of cyclosporine plasma concentrations and the patient’s clinical condition is recommended.

Concomitant use of bicalutamide and drugs that inhibit microsomal oxidation of drugs such as cimetidine or ketoconazole may lead to an increase in the concentration of bicalutamide in plasma and possibly to an increase in the frequency of side effects.

Increases the effect of indirect anticoagulants (coumarin derivatives), including warfarin (competition for binding to plasma proteins).

How to take, course of use and dosage

Adults and older men:

For advanced prostate cancer in combination with an analog of GnRH or surgical castration: inside 50 mg once a day. Treatment with Bicalutamide om should be started simultaneously with the start of taking the GnRH analog or surgical castration.

For locally advanced prostate cancer: inside 150 mg once a day. Bicalutamide should be taken continuously for at least 2 years. If there are signs of disease progression, the drug should be discontinued.

Renal impairment: no dose adjustment is required.

Liver function disorders:  no dose adjustment is required for mild to moderate hepatic insufficiency. In severe hepatic insufficiency, despite the fact that T 1/2 of the active enantiomer of bicalutamide increases by 76%, however, no dose adjustment is required.

Overdose

Cases of overdose in humans are not described. There is no specific antidote.

Treatment is symptomatic. Dialysis is not effective because bicalutamide binds strongly to plasma proteins and is not excreted unchanged in the urine. General maintenance therapy and monitoring of vital body functions are indicated.

Special instructions

Given the possibility of slowing the elimination of bicalutamide and its accumulation in patients with impaired liver function, it is advisable to periodically evaluate liver function. Most changes in liver function occur during the first six months of bicalutamide treatment.

In case of severe changes in liver function, bicalutamide should be discontinued.

Discontinuation of bicalutamide treatment should be considered in patients with progressive disease with elevated prostate-specific antigen (PSA) concentrations.

When prescribing bicalutamide to patients receiving indirect anticoagulants (coumarin derivatives), including warfarin, it is recommended to regularly monitor prothrombin time.

Each tablet of Bicalutamide 50 mg contains 61 mg of lactose monohydrate. Each Bicalutamide 150 mg tablet contains 183 mg of lactose monohydrate.

Given the possibility that bicalutamide may inhibit the activity of cytochrome P450 (the CYP3A4 isoenzyme), caution should be exercised when prescribing bicalutamide concomitantly with drugs primarily metabolized with the participation of the CYP3A4 isoenzyme.

Influence on the ability to drive vehicles and mechanisms:

Bicalutamide may affect the ability of patients to drive vehicles or engage in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions due to the development of dizziness and drowsiness with the combined use of bicalutamide and GnRH analogues.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25°C.

Keep out of reach of children.

Shelf

life is 2 years.

Do not use the product after the expiration date indicated on the package.

Active ingredient

Bicalutamide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets