Casodex tablets 150 mg, 28 pcs. (Bykalutamyd)

Latin name srdlp

Release form

Coated tablets.

Packing

28 pcs

Pharmacological action

Pharmacodynamics

Antiandrogenic non-steroidal drug. It is a racemic mixture, moreover, the anti-androgenic activity is predominantly of the (R) -enantiomer. The drug does not have other types of endocrine activity. Casodex® binds to androgen receptors and, while not activating gene expression, inhibits the stimulating effect of androgens. As a result of this, there is a regression of neoplasms of the prostate gland.

In some patients, discontinuation of Casodex may lead to the development of a clinical withdrawal syndrome of antiandrogens.

When using Casodex in a daily dose of 150 mg daily for the treatment of patients with locally advanced (T3-T4, any N, M0 or any T, N +, M0) prostate cancer, as an immediate hormone therapy or as an adjuvant therapy, significantly the risk of disease progression and bone metastases is reduced.

With locally advanced prostate cancer, there has been a tendency to improved life expectancy with no signs of disease progression in groups of patients taking Casodex® 150 mg as immediate or adjuvant therapy compared to standard therapy (surgical treatment, radiation therapy).

Life expectancy has been shown in patients with locally advanced prostate cancer who received Casodex® 150 mg as an immediate monotherapy and as an adjuvant in combination with radiation therapy.

The use of Casodex at a dose of 150 mg compared with surgical castration in patients with locally advanced non-metastatic prostate cancer did not reveal a statistically significant difference in life expectancy and time to progression with a statistically significant advantage of sexual function and physical condition.

Pharmacokinetics

Absorption

After oral administration, it is rapidly and completely absorbed from the digestive tract. Simultaneous food intake does not affect absorption.

Distribution of

With daily administration of Casodex at a dose of 150 mg of the Css (R) enantiomer in plasma, it is about 22 μg / ml. At equilibrium, about 99% of all enantiomers circulating in the blood are the active (R) -enantiomer.

With daily use of Casodex, the concentration of (R) -enantiomer in plasma increases by approximately 10 times due to prolonged T1 / 2, which allows you to take Casodex 1 time / day.

Communication with plasma proteins is high (for the racemic mixture 96%, for the (R) enantiomer 99.6%).

The average concentration of the (R) -enantiomer in the semen of men who received Casodex 150 mg is 4.9 mcg / ml. The amount of bicalutamide that can potentially be detected in women after sexual intercourse is low and is approximately 0.3 μg / kg (the value of this indicator is lower than that required for changes in the development of the fetus in laboratory animals).

Metabolism

Intensively metabolized in the liver by oxidation and the formation of conjugates with glucuronic acid.

Excretion

Metabolites are excreted in the urine and bile in approximately equal proportions. The (S) -enantiomer is excreted much faster than the (R) -enantiomer, T1 / 2 of the last about 7 days.

Pharmacokinetics in special clinical cases

The pharmacokinetics of the (R) enantiomer are not affected by age, impaired renal function, mild to moderate impaired liver function.

There is evidence that in patients with severely impaired hepatic function, the elimination of the (R) enantiomer from plasma slows down.

In patients with moderate to severe impaired liver function, cumulation of bicalutamide in the body may be observed.

Indications

Locally advanced prostate cancer as an immediate monotherapy or as adjuvant therapy in combination with radical prostatectomy or

radiation therapy locally advanced non-metastatic prostate cancer as monotherapy in cases where surgical castration or other medical interventions not applicable.

Contraindications

Concomitant use with terfenadine, astemizole, cisapride

Hypersensitivity to bicalutamide and other components of

Casodex® is not prescribed for women and children.

Caution: Casodex® is used in patients with impaired liver function, with lactose intolerance, lactase deficiency and glucose / galactose malabsorption syndrome.

Use during pregnancy and lactation

CasodexВ® is contraindicated in women and should not be prescribed to pregnant women or during lactation.

Composition

1 tablet contains:

Active ingredient: bicalutamide 150 mg.

Excipients: lactose monohydrate - 183 mg, sodium carboxymethyl starch - 22.5 mg, povidone - 15 mg, magnesium stearate - 4.5 mg.

Shell composition: hypromellose - 7.5 mg, macrogol 300 - 1.5 mg, titanium dioxide (E171) - 2.3 mg.

Dosage and administration of

Casodex® is prescribed to adults and older men at a dose of 150 mg 1 time / day. Casodex® should be taken for a long time, for at least 2 years. If signs of disease progression appear, the drug should be discontinued.

Patients with impaired renal function and mild impaired liver function do not require dose adjustment.

Patients with moderate to severe impaired liver function may experience increased cumulation of the drug.

Side effects of

Except where otherwise indicated, the incidence of side effects is calculated from monotherapy studies with Casodex® early prostate cancer.

Very often ( 10%): gynecomastia (may persist even after discontinuation of therapy, especially if the drug is taken for a long time), tenderness of the mammary glands, skin rash, asthenia.

Often ( 1% - <10%): depression, anorexia, dizziness, drowsiness, hot flashes, itching, abdominal pain, constipation, dyspepsia, flatulence, alopecia or restoration of hair growth, hirsutism, dry skin, hematuria, nausea, decreased sex drive, erectile dysfunction, chest pain, swelling, weight gain, increased activity of hepatic transaminases, hepatotoxicity, jaundice, anemia, decreased appetite.

Infrequently ( 0.1% - <1%): hypersensitivity reactions, angioedema, urticaria, interstitial pulmonary disease (fatal cases reported) *.

Rarely ( 0.01% - <0.1%): liver failure (fatal cases reported). *

Increased activity of hepatic transaminases, cholestasis and jaundice were rarely evaluated as serious, were transient, completely disappeared or decreased with continued therapy or after discontinuation of the drug. Very rarely, liver failure developed with bicalutamide, but a causal relationship between the development of liver failure and treatment with Casodex has not been reliably established.

* - according to the post-marketing use of the drug.

Drug Interaction

No pharmacodynamic or pharmacokinetic interaction has been reported between Casodex and GnRH analogues.

In vitro studies have shown that the Casodex (R) -enantiomer is an inhibitor of CYP3A4, and to a lesser extent CYP2C9, CYP2C19, CYP2D6. The potential ability of Casodex to interact with other medicines has not been identified. However, when using Casodex for 28 days on the background of midazolam AUC of midazolam increased by 80%.

Contraindicated use of Casodex with such drugs as terfenadine, astemizole and cisapride.

Caution should be exercised when prescribing Casodex at the same time as cyclosporine or calcium channel blockers. The dose of these drugs may need to be reduced, especially in case of potentiation or development of undesirable reactions. After initiation of use or withdrawal of Casodex it is recommended to carefully monitor the concentration of cyclosporine in the blood plasma and the clinical condition of the patient.

Concurrent administration of Casodex and drugs that inhibit microsomal oxidation of drugs (cimetidine, ketoconazole) may lead to an increase in plasma bicalutamide concentration and possibly to an increase in the incidence of adverse reactions.

Casodex® enhances the action of the indirect anticoagulants of coumarin (warfarin), since can displace these drugs from the sites of their binding to proteins.

Overdose

There have been no cases of overdose in humans. There is no specific antidote, so symptomatic therapy is carried out if necessary. Dialysis is ineffective because bicalutamide binds strongly to proteins and is not excreted in the urine unchanged. General supportive therapy and monitoring of vital functions of the body are shown.

Storage conditions

Keep out of the reach of children at a temperature not exceeding 30 ° C.

Expiration

4 years.

Deystvuyuschee substances

Bykalutamyd

Dosage form

dosage form

tablets

AstraZeneca, Russia



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