Bilumide

Bilumid contains the component bicalutamide, which is an anti-androgenic substance of non-steroid nature; The drug does not have any other effect on the endocrine system. Entering the compound with androgenic endings, and without leading to gene expression, the drug blocks androgenic activity, thereby contributing to the regression of the neoplasm in the prostate.

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

Indications Bilumide

A dosage of 50 mg is used for a common form of prostate carcinoma (in the later stages) in combination with an analogue of the element of the PHGR or with a surgical castration procedure.

A portion of 0.15 g is prescribed for local prostate carcinoma (TK-T4, some N, M0; and in addition T1-T2, N + and M0) in the form of monotherapy or as a supplement to radiation therapy or radical prostatectomy.

Locally used for prostate carcinoma that occurs without metastasis, when surgical castration or other medical procedures are considered impossible or impractical.

[1], [2]

Release form

Drug release is made in tablets - 7 pieces inside a cell package, 4 packs inside a box (50 mg volume), and 28 pieces inside a special container equipped with a SC-lid (volume 0.15 g).

Pharmacokinetics

Bicalutamide has good absorption inside the gastrointestinal tract when ingested. There is no information on the clinically significant effect of food on the bioavailability of drugs. The excretion of the (S) -enantiomer proceeds much faster than the analogous process in the (R) -enantiomer; The term half-life of the latter is approximately 7 days.

In the case of daily administration of the drug, the plasma values of the (R) -enantiomer increase approximately tenfold, due to the prolonged term of 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 inside the blood are active (R) -enantiomers.

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

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

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

Metabolic components are excreted with bile and urine in approximately the same proportions.

Dosing and administration

In case of prostate carcinoma of a common nature: men (also elderly) should use the first tablet of medication (50 mg) 1 time per day. Therapy should be started together with the use of an analogue of KHRLH or by performing surgical castration.

In case of locally progressive carcinoma of the prostate: for men (and the elderly as well) it is required to take 1 tablet of 0.15 g 1 time per day. The dosage form of 0.15 g must be applied continuously for at least 2 years or until the appearance of changes in the course of pathology.

In the case of a severe or moderate degree of hepatic disorder, bicalutamide may accumulate inside the body - therefore, Bilumid is prescribed extremely carefully for such patients.

[3]

Use Bilumide during pregnancy

Bilumid is used in the treatment of the prostate, so it is not prescribed to women.

Contraindications

The main contraindications:

• severe intolerance against bicalutamide or other elements of the drug;
• combination of drugs with astemizole, terfenadine or cisapride.

Side effects Bilumide

Bilumid is often tolerated without the appearance of any complications. Only occasionally with the development of negative signs requires the abolition of the drug. The use of drugs can provoke such violations:

• most often: hot flashes, gynecomastia or pain in the sternum;
• also often enough: nausea, weight gain, diarrhea, cholestasis, a temporary increase in intrahepatic transaminase activity, jaundice, and also asthenia, impotence, itching, weakening of libido and alopecia;
• sometimes: depression, hematuria, abdominal pain, dyspepsia, and interstitial process that affects the lungs. In addition, signs of intolerance are noted, including urticaria and angioedema;
• single: skin dryness, vomiting and insufficiency of hepatic function.

Liver-related disorders are mostly temporary and weakened or disappear completely if therapy is continued or after it is canceled. Only a single failure of the liver was noted, while failing to identify a causal link with the drug. Periodic monitoring of hepatic activity is required.

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

• CAS lesions: development of HF;
• problems with the work of the digestive tract: dyspepsia, anorexia, bloating, dryness, affecting the oral mucous membranes, and constipation;
• dysfunction of the central nervous system: drowsiness, dizziness, weakening of libido and insomnia;
• disorders of the respiratory system: dyspnea;
• lesions of the urogenital tract: nocturia or impotence;
• blood disorders: anemia;
• infection of the subcutaneous tissue and epidermis: hirsutism or alopecia, hyperhidrosis and rash;
• 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

Information regarding intoxication in a person is missing.

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 inside the urine in an unchanged state. It requires the implementation of general support activities and monitoring of the work of the vital organs.

Interactions with other drugs

There is no data regarding drug interactions when combining bicalutamide and LHRH analogues.

It was established that R-bicalutamide inhibits the action of CYP 3A4, as well as, less actively, CYP 2С9 and 2С19 with 2D6. The introduction of the component for 28 days along with the use of midazolam caused an increase in the AUC values of the latter by 80%.

Combining Bilumid with astemizole, terfenadine or cisapride is prohibited.

It is necessary to very carefully combine the drug with substances that block the activity of the Ca channels, or cyclosporines. It may be necessary to reduce the portions of these drugs, especially if you suspect or develop negative symptoms.

Persons using cyclosporine should be carefully monitored, especially at the initial stage of therapy and at its termination.

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

Bicalutamide is able to displace warfarin (coumarin anticoagulant) from the areas of its protein synthesis. Because of this, with the introduction of drugs in people who use coumarin anticoagulants, you need to constantly monitor the performance of PTV.

[4], [5]

Storage conditions

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

Shelf life

Bilumid can be used for a 24-month term from the moment of drug implementation.

Application for children

In pediatrics, the drug is not used.

Analogs

Analogues of drugs are the substances Androblock, Kalumid, Balutar with Bikana, and in addition Bikalutamid, Bikaprost and Bicalutera with Casodex.