BICALUTAMIDE PILLS 50MG

Indications

- common prostate cancer in combination with a gonadotropin-releasing hormone analogue (GnRH) or surgical castration;

- locally advanced prostate cancer (T3-T4, any N, M0; T1-T2, N +, M0) as monotherapy or adjuvant therapy in combination with radical prostatectomy or radiotherapy;

- locally advanced non-metastatic prostate cancer in cases where surgical castration or other medical interventions are not applicable or unacceptable.

Dosage and administration

Inside

Adult men (incl. Elderly):

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

For locally advanced prostate cancer: on 150 mg once a day.

Bicalutamide should be taken for a long time, at least for 2 years.

If there is evidence of disease progression, the drug should be discontinued.

Renal impairment: dose adjustment is not required.

Liver dysfunction: with a slight violation of liver function dose adjustment is not required.In patients with moderate to severely impaired liver function, an increased cumulation of bicalutamide may be observed.

Adverse effects

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

- very often (> 10%): gynecomastia (it may persist even after stopping therapy, especially when taking the drug for a long time), pain in the chest glands, flushing of the blood to the face;

- often (≥1% and <10%): diarrhea, nausea, transient increase in the activity of “liver” transaminases, cholestasis and jaundice (the described changes in liver function were rarely evaluated as serious, were transient, completely disappeared or decreased with continued therapy drug withdrawal), itching, asthenia; with the use of the drug in a daily dose of 150 mg - alopecia or restoration of hair growth, decreased sexual desire, sexual dysfunction, weight gain.

- rarely (≥0.1% - <1%): hypersensitivity reactions, including angioedema and urticaria, interstitial lung diseases; angina pectoris, prolongation of the QT interval, cardiac arrhythmias; with the use of the drug in a daily dose of 150 mg - abdominal pain, depression, dyspepsia, hematuria.

- very rarely (≥0.01% - <0.1%): vomiting, dry skin (when using the drug in a daily dose of 150 mg, dry skin is often observed), liver failure (causal relationship with bicalutamide is not reliably established), thrombocytopenia.

With the simultaneous use of bicalutamide and GnRH analogues, the following side effects can also occur with a frequency of ≥1% (a causal relationship with the drug intake has not been established, some of the noted side effects have occurred in elderly patients):

Cardiovascular: heart failure.

Gastrointestinal: anorexia, dry mouth, dyspepsia, dysphagia, constipation, flatulence.

Nervous system: dizziness, headache, insomnia, increased sleepiness.

Respiratory: dyspnea.

Urogenital: nocturia, urinary tract infection, dysuria, urinary retention, frequent urination, polyuria, hydronephrosis.

Hemic and lymphatic: anemia, leukopenia.

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

From the laboratory indicators: hyperglycemia, increased activity of liver transaminases.

Other: abdominal pain, chest pain, pain in the pelvic region, back pain, weight loss or increase, edema, diabetes mellitus, fever.

Contraindications

Hypersensitivity to any component of the drug, simultaneous reception with terfenadine, astemizole, cisapride; lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the product contains lactose); childhood. Should not be prescribed to female patients.

Carefully. Liver dysfunction.

Use during pregnancy and lactation

Should not be prescribed to female patients.

Application for violations of the liver

With care: abnormal liver function. Given the possibility of slowing the excretion of bicalutamide in patients with impaired liver function, it is advisable to periodically assess liver function. Most changes in liver function occur during the first six months of treatment with bicalutamide. In the case of the development of pronounced changes in liver function, the drug should be stopped.

Application for violations of kidney function

The use is possible according to the dosing regimen.

Use in children

Contraindicated in children.

Use in elderly patients

The use is possible according to the dosing regimen.

Special notes

Given the possibility of slowing the excretion of bicalutamide in patients with impaired liver function, it is advisable to periodically assess liver function. Most changes in liver function occur during the first six months of treatment with bicalutamide.

In the case of the development of pronounced changes in liver function, the drug should be stopped.

In patients with progression of the disease while increasing the level of prostate-specific antigen (PSA), consideration should be given to discontinuing treatment with bicalutamide.

When prescribing bicalutamide to patients receiving coumarin anticoagulants, it is recommended that prothrombin time be regularly monitored.

Considering the possibility of inhibition of cytochrome P450 (CYPZA4) activity by bicalutamide, caution should be exercised with the simultaneous administration of bicalutamide with drugs mainly metabolized with CYPZA4.

Influence on ability to drive motor transport and control mechanisms. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.

Overdosage

Cases of overdose in humans are not described. There is no specific antidote. Symptomatic treatment. Dialysis is not effective because bicalutamide binds strongly to proteins and is not excreted by the kidneys unchanged. General supportive therapy and monitoring of vital body functions is shown.

Drug interaction

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

In vitro studies have shown that (R) -enantiomer of bicalutamide inhibits CYPZA4, to a lesser extent, affecting the activity of CYP2C9, 2C19 and 2D6. The potential ability of bicalutamide to interact with other drugs was not found, but when using bicalutamide for 28 days while taking midazolam, the AUC of midazolam is increased by 80%.

Incompatible with terfenadine, astemizole, cisapride.

Care should be taken when prescribing bicalutamide simultaneously with cyclosporine or Calcium channel blockers. It may be necessary to reduce the dose of these drugs, especially in the case of potentiation or the development of side effects. After the use or discontinuation of bicalutamide has begun, careful monitoring of plasma cyclosporine concentration and the patient’s clinical status is recommended.

The simultaneous use of bicalutamide and drugs that inhibit microsomal oxidation of drugs, for example, cimetidine or Ketoconazole, can lead to an increase in plasma plasma concentration of bicalutamide and, possibly, to an increase in the incidence of side effects. Enhances the effect of coumarin anticoagulants, incl. Warfarin (competition for communication with proteins).

Terms and conditions of storage

In a dry, dark place at a temperature not higher than 25 ° C. Keep out of the reach of children.