Bikalan

Bicalan is an antiandrogen medication.

Indications Bikalana

It is used in the widespread form of prostate carcinoma (late phases), together with an analogue of the LHRH element or in conjunction with surgical castration.

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Release form

The medicinal element is released in tablet form, in the amount of 10 pieces inside a cellular package. Inside the pack there are 3 such packages.

Pharmacodynamics

Bicalutamide is a non-steroidal antiandrogen with no other hormonal effects.

The drug is a racemic mixture, within which only the (R)-enantiomer has an antiandrogenic effect. This component is synthesized with androgen endings, without causing gene expression - in this way it suppresses androgen activity. Due to this suppression, the tumor in the prostate area begins to regress.

Pharmacokinetics

Bicalutamide has good absorption within the gastrointestinal tract after oral administration. There is no information on the clinically significant effect of food on bioavailability values.

The (S)-enantiomer has a higher rate of excretion from the body than the (R)-enantiomer; the half-life of the latter is approximately 7 days.

Following daily administration of bicalutamide, plasma levels of the (R)-enantiomer increase approximately tenfold due to its long half-life. Therefore, the drug should only be taken once daily.

Following daily administration of 50 mg bicalutamide, plasma levels of the (R)-enantiomer are approximately 9 μg/ml. However, up to 99% of all enantiomers transported in the blood are the active (R)-enantiomer.

The pharmacokinetic characteristics of the (R)-enantiomer are not dependent on the age or degree of liver impairment (moderate or mild) in the patient.

There is information that in people with severe stages of liver disorders, there is a slowdown in plasma elimination of the (R)-enantiomer.

Bicalutamide is synthesized in large quantities with protein (for the racemate the figure is 96%, and for R-bicalutamide – 99.6%), and in addition, it undergoes intensive metabolic processes (oxidation and formation of glucuronic acid with conjugates).

Metabolic products of the substance are excreted in bile and urine in approximately equal parts.

Dosing and administration

Male patients (also elderly) should take 50 mg of the drug per day (1 tablet). Therapy using Bikalan should be started simultaneously with the start of LHRH or the surgical castration procedure. The duration of the therapeutic cycle is prescribed by the doctor.

In people with severe or moderate liver dysfunction, the drug should be administered with great caution to avoid the risk of accumulation of the drug.

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Use Bikalana during pregnancy

Bikalan is not prescribed to women.

Contraindications

Among the contraindications:

• the presence of severe sensitivity to the components of the drug;
• use together with astemizole, terfenadine, and cisapride.

Side effects Bikalana

Bicalutamide is tolerated in most cases without complications. Only rarely, when the following side effects developed, was it necessary to discontinue the drug:

• disorders affecting the mammary glands and reproductive organs: most often observed is gynecomastia ¹ or pain in the mammary glands ¹;
• gastrointestinal tract disorders: nausea or diarrhea are quite common; vomiting is rare;
• problems with the function of the hepatobiliary system: jaundice often develops ² or transaminase values increase. In isolated cases, liver failure occurs ³;
• immune manifestations: occasionally signs of intolerance appear, including urticaria and Quincke's edema;
• lesions of the subcutaneous layers and epidermis: dry skin develops occasionally;
• thoracic, respiratory and mediastinal disorders: interstitial pulmonary pathologies occasionally occur;
• systemic disorders: most often hot flashes (feeling of heat) appear ¹. Itching or asthenia is also often noted.

¹ The severity can be reduced by performing an accompanying castration procedure.

² changes affecting liver function are usually temporary and disappear completely or weaken with continuation of the therapeutic cycle or after its completion.

³ liver failure develops only occasionally, and no connection with the use of Bikalan could be established. It is necessary to periodically monitor liver function indicators.

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Overdose

There is no information on intoxication with Bicalan.

The drug has no antidote, so the patient must be prescribed symptomatic procedures. Dialysis is not performed because bicalutamide has a high degree of protein synthesis and is not detected in the urine in an unchanged state. General supportive measures are also performed and the work of vital systems is monitored.

Interactions with other drugs

There is no information regarding drug interactions between bicalutamide and LHRH analogs.

In vitro tests have demonstrated that R-bicalutamide inhibits CYP 3A4 and, to a lesser extent, CYP 2C9, 2C19, and 2D6.

Although testing with antipyrine, a marker of P450 (CYP) activity, did not demonstrate the likelihood of interactions with bicalutamide, use of the drug for 28 days during treatment with midazolam resulted in an 80% increase in midazolam AUC values. Such an increase in values may be important for drugs with a narrow drug index. For this reason, the drug should not be combined with cisapride, terfenadine, or astemizole.

It is necessary to combine Bikalan with Ca channel blocking drugs or cyclosporine very carefully. It may be necessary to reduce the doses of these drugs, especially if side effects are suspected (or develop). People using cyclosporine need careful monitoring, especially at the initial stage of therapy and when it is stopped.

It is necessary to combine the drug very carefully with substances that inhibit the oxidation processes of drugs (for example, cimetidine or ketoconazole). In theory, such a combination can provoke an increase in bicalutamide values, which will increase the frequency of adverse effects.

In vitro testing has shown that bicalutamide can displace warfarin (a coumarin anticoagulant) from its protein synthesis sites. For this reason, when used in patients who use coumarin anticoagulants, PT values should be constantly monitored.

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Storage conditions

Bikalan should be kept in a place out of reach of small children. Temperature marks – within 25°С.

Shelf life

Bikalan can be used within 5 years from the date of production of the therapeutic agent.

Application for children

The drug cannot be used in pediatrics.

Analogues

Analogues of the drug are Apo-flutamide, Flutan, Frugil, Xtandi with Bicalutamide, and also Flutazin, Bicalutera, Flutamide with Calumid and Flucin with Casodex. Also on the list are Flulem, Flutpharm with Flumid and Flutaplex with Flutamide.