Description
Pharmacological action
Antitumor drug, non-steroidal andandrogenic drug – a competitive endogenous androgen antagonist.
By binding to receptors on the surface of cells of target organs, it makes them inaccessible to androgens, while increasing the concentration of hormones in the plasma. The result is a regression of prostate neoplasms.
Prescribing bicalutamide at a dose of 150 mg / day to patients with localized (T1-T2, N0 or NX, MO) or locally advanced (T3-T4, any N, MO T1-T2, N +, MO) prostate cancer reduces the risk of disease progression by 42% and the relative risk of bone metastasis by 33% during the observation period up to 2 years.
However, the effectiveness of bicalutamide with respect to survival rates is lower than that when performing surgical castration.
In some patients, discontinuation of treatment may lead to the development of antiandrogen withdrawal syndrome (after cancellation, 10-15% of patients have a temporary stabilization of the disease).
Pharmacokinetics
After oral administration, it is rapidly and completely absorbed from the digestive tract (food intake does not affect absorption).
Communication with plasma proteins – 96-99%.
Intensively metabolized in the liver (by oxidation and the formation of conjugates with glucuronic acid) to inactive (S) – and active (R) -enantiomers. TCmax of the (R) -enantiomer – 31.3 hours. The (S) -enantiomer is excreted much faster than the (R) -enantiomer T1 / 2 of the latter – about 7 days. With a daily intake of bicalutamide at a dose of 150 mg / day, the Css (K) -enantiomer in plasma is 22 Ñg / ml. With Css, about 99% of all enantiomers circulating in the blood are the active (R) -enantiomer. With daily use, the concentration of (R) -enantiomer in plasma increases by about 10 times due to prolonged T1 / 2.
It is excreted in the form of metabolites by the kidneys and with bile in equal proportions. The pharmacokinetics of the (R) enantiomer does not depend on age, the state of renal function, and the elimination of the (R) enantiomer from plasma slows down in patients with severe hepatic impairment.
Indications for
prostate cancer (treatment of localized prostate cancer in patients who have not undergone radical prostatectomy or radiotherapy
monotherapy or adjuvant therapy in combination with radical prostatectomy or radiotherapy for locally advanced prostate cancer
treatment of locally advanced, prostate cancer when surgical castration or other drugs are not effective or unacceptable).
Contraindications
concomitant use of terfenadine, astemizole and cisapride
children
hypersensitivity.
The drug is not prescribed for women during pregnancy and lactation.
Caution should be prescribed in case of liver failure.
Composition
1 tab. contains: Active substances: bicalutamide – 50 mg,
Excipients: lactose monohydrate – 88.93 mg, sodium carboxymethyl starch – 5 mg, colloidal silicon dioxide – 0.45 mg, povidone – 4.5 mg, magnesium stearate – 1.12 mg.
Shell composition: white opadray (Y-1-7000) – 3.75 mg (hypromellose 5 cP – 2.344 mg, titanium dioxide – 1.172 mg, macrogol 400 – 0.234 mg).
Dosage and administration of
In case of advanced prostate cancer, by mouth, 50 mg / day, once in combination with a GnRH analog or surgical castration.
With non-metastatic prostate cancer in situ as monotherapy (if there are contraindications to surgical castration or to the appointment of other drugs) – 150 mg / day once.
Bicalutamide should be taken continuously for at least 2 years.
Dose adjustment is required in patients with moderate to severe impaired liver function.
Side effects of
From the cardiovascular system: angina pectoris, development or worsening of heart failure, increased blood pressure.
From the respiratory system: chest pain, cough, pharyngitis, bronchitis, pneumonia, rhinitis.
From the digestive system: rarely – abdominal pain, flatulence, dyspepsia, stomach bleeding, dry mouth, transient increase in liver transaminases, cholestasis, jaundice is very rare – impaired liver function.
From the nervous system: dizziness, insomnia or drowsiness, anxiety, rarely depression.
From the musculoskeletal system: myasthenia gravis, myalgia, cramps, arthritis, joint contractures.
From the endocrine system: often (> 10%) – gynecomastia (may persist after discontinuation of therapy, especially if the drug is taken for a long time), breast tenderness hyperglycemia, diabetes mellitus, polyuria.
From the urinary system: dysuria, urinary retention, edema rarely – hematuria.
Other: often – asthenia, alopecia, decreased or increased body weight, decreased libido, fever, chills, increased sweating, anemia, pelvic pain, dry skin, hirsutism, allergic reactions, flushing of the face.
Overdose
Treatment: symptomatic, specific antidote does not exist. Dialysis is ineffective, since bicalutamide is firmly bound to proteins and is not excreted unchanged in urine. General supportive therapy and monitoring of vital body functions are indicated.
Storage conditions
Keep out of the reach of children at a temperature not exceeding 30 ° C.
Active ingredient
Bicalutamide
Terms and conditions
prescription
lekarstvennaja form
tablets
Prescription
For adults by as prescribed by the doctor
Indications
Onkologicheskie ill