Casodex, pills 50mg, 28pcs

Composition

1 tablet contains:

Active ingredient:

bicalutamide 50 mg;

Auxiliary substances:

lactose monohydrate,

sodium carboxymethyl starch,

povidone,

magnesium stearate,

purified water (evaporated during production);

Shell composition:

hypromellose, macrogol 300, titanium dioxide, purified water.

Pharmacological action

Casodex – antitumor, antiandrogenic.

Pharmacodynamics

Antiandrogenic nonsteroidal drug. It is a racemic mixture, and the antiandrogenic activity is mainly due to the (R) – enantiomer. The drug does not have other types of endocrine activity. Casodex® binds to androgen receptors and, without activating gene expression, suppresses the stimulating effect of androgens. As a result, there is a regression of prostate neoplasms.

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

Pharmacokinetics

Suction

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

Distribution

When Casodex is taken daily at a dose of 50 mg, the C_ss (R) – enantiomer in plasma is about 9 micrograms/ml. At steady state, about 99% of all enantiomers circulating in the blood are the active (R)-enantiomer. With daily intake of Casodex, the concentration of the (R)-enantiomer in plasma increases approximately 10 times due to a long T_1/2, which allows you to take Casodex 1 time/day. Plasma protein binding is high (96% for the racemic mixture,99.6% for the (R) – enantiomer).

Metabolism

It is intensively metabolized in the liver by oxidation and formation of conjugates with glucuronic acid.

Deduction

Metabolites are excreted in the urine and bile in approximately equal proportions. The (S) – enantiomer is eliminated from the body much faster than the (R) – enantiomer, T_1/2 of the latter is about 7 days.

Pharmacokinetics in special clinical cases

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

Indications

Advanced prostate cancer (in combination with a GnRH analog or with surgical castration).

Use during pregnancy and lactation

Casodex® is contraindicated in women and should not be administered to pregnant women or during lactation.

Contraindications

• Concomitant use with terfenadine, astemizole, cisapride;
• hypersensitivity to bicalutamide and other components of the drug;
• Casodex is not prescribed for women and children.

With caution: use Casodex® in patients with impaired liver function, lactose intolerance, lactase deficiency and glucose / galactose malabsorption syndrome.

Side effects

Casodex® is well tolerated by most patients, and only in rare cases it has to be discontinued due to the side effects it causes.

The pharmacological action of Casodex 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), breast tenderness, hot flashes.

Frequently (≥1%-

Rarely (≥ 0.1%-

Very rare (≥ 0.01%-

* – concomitant use of Casodex and GnRH analogues has been associated with frequent side effects.

Interaction

There are no data on the pharmacodynamic or pharmacokinetic interaction between Casodex and GnRH analogues.

In vitro studies have shown that the (R)-enantiomer of Casodex is an inhibitor of CYP3A4, to a lesser extent-of CYP2C9, CYP2C19, and CYP2D6. In clinical studies using phenazone as a marker of cytochrome P 450 activity, the potential ability of Casodex to interact with other drugs was not found. However, when using Casodex for 28 days while taking midazolam, the AUC of midazolam increased by 80%.

Concomitant use of Casodex with drugs such as terfenadine, astemizole and cisapride is contraindicated.

Caution should be exercised when prescribing Casodex simultaneously with cyclosporine or slow calcium channel blockers. It may be necessary to reduce the dose of these drugs, especially in case of potentiation or development of adverse reactions. After starting to use or discontinuing Casodex, it is recommended to carefully monitor the concentration of cyclosporine in blood plasma and the patient’s clinical condition.

Caution should be exercised when using Casodex® concomitantly with drugs that inhibit microsomal liver enzymes (for example, cimetidine, ketoconazole). The use of these combinations may lead to an increase in the concentration of bicalutamide in plasma and, possibly, to an increase in the frequency of adverse reactions.

Casodex ® enhances the effect of indirect coumarin anticoagulants (including warfarin), as it can displace these drugs from the sites of their binding to proteins. It is recommended to regularly monitor prothrombin time when prescribing Casodex to patients receiving coumarin-type indirect anticoagulants.

How to take, course of use and dosage

Casodex® is prescribed to adult men (including the elderly) with advanced prostate cancer in combination with a GnRH analog or with surgical castration at a dose of 50 mg 1 time / day. Treatment should be started simultaneously with the start of taking a GnRH analog or surgical castration.

In patients with impaired renal function and mild hepatic impairment, no dose adjustment is required.

Patients with moderate to severe hepatic impairment may experience increased accumulation of the drug.

Overdose

Cases of overdose in humans are not described.

There is no specific antidote, so if necessary, symptomatic therapy is performed.

Dialysis is ineffective because bicalutamide binds strongly to proteins and is not excreted unchanged in the urine.

General maintenance therapy and monitoring of vital body functions are indicated.

Special instructions

The drug is metabolized in the liver. Given the possibility of slowing the elimination of bicalutamide and accumulation of bicalutamide in patients with severe hepatic impairment, it is advisable to periodically evaluate liver function. Most changes in liver function occur during the first 6 months of treatment with Casodex.

Casodex® should be used with caution in patients with moderate to severe hepatic impairment.

Severe hepatic impairment with Casodex is rare (fatal cases have been reported).

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

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

Given the possibility of Casodex inhibiting the activity of cytochrome P450 (CYP3A4), caution should be exercised when concomitantly prescribing Casodex with drugs that are mainly metabolized with the participation of CYP3A4.

Patients taking GnRH agonists experienced a decrease in glucose tolerance. This effect can lead to the development of diabetes mellitus or a decrease in glucose tolerance in patients with diabetes mellitus. Therefore, blood glucose concentrations should be monitored in patients taking Casodex® and GnRH agonists.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

When using Casodex, drowsiness and dizziness may occur, and therefore caution should be exercised when driving vehicles or other moving mechanisms.

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

5 years

Active ingredient

Bicalutamide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets