Bilumide

Bilumid contains the component bicalutamide, which is a non-steroidal antiandrogenic substance; the drug does not have any other effect on the endocrine system. By combining with androgenic endings and not leading to gene expression, the drug blocks androgenic activity, thereby promoting regression of neoplasms in the prostate area.

Bicalutamide is a racemate, but only the R(-)-enantiomer has an antiandrogenic effect.

Indications Bilumide

A dosage of 50 mg is used for widespread prostate carcinoma (at late stages) in combination with an LHRH analogue or with a surgical castration procedure.

A dose of 0.15 g is prescribed for localized prostate carcinoma (T3-T4, any N, M0; and also T1-T2, N+ and M0) as monotherapy or as an adjunct to radiation therapy or radical prostatectomy.

It is also used locally for prostate carcinoma without metastases, when surgical castration or other medical procedures are considered impossible or inappropriate.

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Release form

The drug is produced in tablets - 7 pieces inside a blister pack, 4 packs inside a box (volume 50 mg), and also 28 pieces inside a special container equipped with an SC cap (volume 0.15 g).

Pharmacokinetics

Bicalutamide is well absorbed in the gastrointestinal tract when taken orally. There is no information on the clinically significant effect of food on the bioavailability of the drug. Excretion of the (S)-enantiomer is much faster than that of the (R)-enantiomer; the half-life of the latter is approximately 7 days.

In case of daily administration of the drug, plasma values of the (R)-enantiomer increase approximately tenfold due to the long half-life.

After daily administration of 0.15 g of the drug, the plasma level of the (R)-enantiomer is approximately 22 μg/ml. At the same time, almost 99% of all enantiomers circulating in the blood are active (R)-enantiomers.

The pharmacokinetic parameters of the (R)-enantiomer are independent of age, renal function and degree of liver impairment.

There is information that in individuals with severe liver dysfunction, inhibition of plasma elimination of the (R)-enantiomer occurs.

The drug has a high capacity for protein synthesis (for the racemate it is 96%, and for R-bicalutamide – 99.6%), as well as intensive metabolism (oxidation and formation of glucuronic acid with conjugates).

Metabolic components are excreted in bile and urine in approximately equal proportions.

Dosing and administration

For prostate cancer of a widespread nature: men (also elderly) should take 1 tablet of the drug (50 mg) once a day. Therapy should be started together with the use of an LHRH analogue or surgical castration.

For locally progressive prostate carcinoma: men (including the elderly) are required to take 1 tablet of 0.15 g once a day. The 0.15 g dosage form must be used continuously for at least 2 years or until changes in the course of the pathology occur.

In case of severe or moderate liver dysfunction, accumulation of bicalutamide in the body may occur – therefore, Bilumid is prescribed to such patients with extreme caution.

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Use Bilumide during pregnancy

Bilumid is used to treat the prostate, so it is not prescribed to women.

Contraindications

Main contraindications:

• severe hypersensitivity to bicalutamide or other components of the drug;
• combination of drugs with astemizole, terfenadine or cisapride.

Side effects Bilumide

Bilumid is often tolerated without any complications. Only occasionally, when negative symptoms develop, is it necessary to discontinue the drug. The use of the drug can provoke the following disorders:

• most common: hot flashes, gynecomastia, or chest pain;
• also quite often: nausea, weight gain, diarrhea, cholestasis, temporary increase in the activity of intrahepatic transaminases, jaundice, as well as asthenia, impotence, itching, decreased libido and alopecia;
• sometimes: depression, hematuria, abdominal pain, dyspepsia and interstitial process affecting the lungs. In addition, signs of intolerance are noted, including urticaria and Quincke's edema;
• isolated: dry skin, vomiting and liver failure.

Liver-related disorders are generally temporary and improve or disappear completely with continued therapy or after discontinuation of therapy. Liver failure has been reported only occasionally, and no causal relationship with the drug has been established. Periodic monitoring of liver function is required.

At the same time, when combining the drug with an LHRH analogue, the following side effects may appear:

• CVS lesions: development of heart failure;
• problems with the gastrointestinal tract: dyspepsia, anorexia, bloating, dryness affecting the oral mucosa, and constipation;
• CNS dysfunction: drowsiness, dizziness, decreased libido and insomnia;
• respiratory system disorders: dyspnea;
• urogenital tract lesions: nocturia or impotence;
• blood disorders: anemia;
• infections of subcutaneous tissues and epidermis: hirsutism or alopecia, hyperhidrosis and rashes;
• metabolic disorders: edema, diabetes, weight loss or weight gain and hyperglycemia;
• Systemic manifestations: pain affecting the sternum, abdominal area or pelvis, as well as fever and headaches.

Overdose

There is no information regarding intoxication in humans.

There is no antidote, so the patient is prescribed symptomatic procedures. Dialysis should not be performed because the drug has a high capacity for protein synthesis and is not detected in the urine in an unchanged state. General supportive measures and monitoring of vital organs are required.

Interactions with other drugs

There are no data on drug interactions when combining bicalutamide and LHRH analogues.

It was found that R-bicalutamide inhibits the action of CYP 3A4, and also, less actively, CYP 2C9 and 2C19 with 2D6. The introduction of the component for 28 days together with the use of midazolam caused an increase in the AUC values of the latter by 80%.

Combination of Bilumid with astemizole, terfenadine or cisapride is prohibited.

It is necessary to combine the drug very carefully with substances blocking the activity of Ca channels or cyclosporines. It may be necessary to reduce the doses of the indicated drugs, especially if negative symptoms are suspected or developed.

Patients receiving cyclosporine should be closely monitored, particularly during initiation of therapy and when therapy is discontinued.

Caution is required when combining with drugs that inhibit metabolic processes of drugs (ketoconazole or cimetidine). Potentially, such a combination can cause an increase in Bilumid values, which increases the frequency of side effects.

Bicalutamide is able to displace warfarin (coumarin anticoagulant) from its protein synthesis sites. Because of this, when administering the drug to people using coumarin anticoagulants, it is necessary to constantly monitor the PT indices.

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Storage conditions

Bilumid should be stored in a place inaccessible to small children. Temperature values - no more than 25 ° C.

Shelf life

Bilumid can be used for a period of 24 months from the date of sale of the drug.

Application for children

The drug is not used in pediatrics.

Analogues

The analogs of the drug are Androblok, Kalumid, Balutar with Bicana, and also Bicalutamide, Bicaprost and Bicalutera with Casodex.