Treatment and control of benign prostatic hyperplasia (BPH) in patients with enlarged prostate for:
reducing the size (regression) of the enlarged gland, improving the outflow of urine, and reducing the symptoms associated with BPH;
reducing the risk of acute urinary retention and the need for surgery, including transurethroresection of the prostate and prostatectomy.
Adenosterid PHARMACOLOGICAL PROPERTIES
Casodex® is a racemic mixture with non-steroidal antiandrogenic activity, predominantly (R) -enantiomer; does not have any other endocrine activity. Casodex® binds to androgen receptors and, without activating gene expression, suppresses the stimulating effect of androgens. The result is a regression of prostate malignant neoplasms.
In some patients, discontinuation of Casodex® may lead to the development of a clinical antiandrogen withdrawal syndrome. Pharmacokinetics
After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect absorption.
The (S) -enantiomer is excreted from the body much faster than the (R) -enantiomer, the half-life of the latter is about 7 days.
With daily intake of bicalutamide, the concentration of the (R) -enantiomer in plasma increases by about 10 times due to the long half-life, which makes it possible to take the drug once a day.
With a daily intake of bicalutamide at a dose of 50 mg, the equilibrium concentration of the (R) -enantiomer is about 9 μg / ml. When taking 150 mg of bicalutamide daily, the equilibrium concentration of the (R) -enantiomer is approximately 22 μg / ml. At equilibrium, about 99% of all enantiomers circulating in the blood are the active (R) -enantiomer.
The pharmacokinetics of the (R) -enantiomer is not affected by age, impaired renal function, mild to moderate impairment of liver function. There is evidence that in patients with severe liver dysfunction, the elimination of the (R) -enantiomer from plasma slows down.
The connection with plasma proteins is high (for the racemic mixture 96%, for (R) – the enantiomer 99.6%). It is extensively metabolized in the liver (by oxidation and the formation of conjugates with glucuronic acid). Metabolites are excreted in urine and bile in approximately equal proportions.
Adenosterid INDICATIONS FOR USE
Casodex® 50 mg in combination with a GnRH analogue (gonadotropin-releasing hormone) or surgical castration is indicated for the treatment of advanced prostate cancer
Casodex® 150 mg is indicated for the treatment of 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
Casodex® 150 mg is also indicated for the treatment of locally advanced, non-metastatic prostate cancer in cases where surgical castration or other medical interventions are unacceptable or inappropriate for the patient
– Hypersensitivity to bicalutamide or other components of the drug.
– Simultaneous reception with terfenadine, astemizole and cisapride.
– Casodex® should not be administered to children and women.
With care: in case of liver dysfunction of moderate and severe severity; in patients with known risk factors for lengthening the QT interval or taking drugs that prolong the QT interval; with simultaneous use with cyclosporine or blockers of “slow” calcium channels, with drugs that inhibit microsomal oxidation of drugs (cimetidine and ketoconazole), with drugs, mainly metabolized with the participation of the isoenzyme CYP 3A4; with lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
PREGNANCY AND LACTATION
Casodex® is contraindicated in women and should not be administered to pregnant or lactating women.