Bilumid - Instructions For Use, Price, Reviews, Analogs Of Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Bilumid

Bilumid: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Bilumide

ATX code: L02BB03

Active ingredient: bicalutamide (Bicalutamide)

Manufacturer: OJSC "Veropharm" (Russia)

Description and photo update: 2020-16-06

Bilumid is a non-steroidal antiandrogenic drug for hormone therapy of malignant neoplasms of the prostate gland in men.

Release form and composition

Dosage form - film-coated tablets: round, biconvex, two layers stand out in the cross-section - yellow film shell and a white to almost white core (in a blister strip of 7, 10 or 14 pcs.; in a cardboard box 4 packs of 7 pcs., 3 packs of 10 pcs. Or 2 packs of 14 pcs. And instructions for use of the drug; in a can of polymeric materials, 28 pcs., In a cardboard box, 1 can and instructions for use of Bilumid).

Composition for 1 tablet (50/150 mg):

• active substance: bicalutamide - 50 or 150 mg;
• excipients: potato starch - 30.8 / 92.4 mg; milk sugar (lactose monohydrate) - 55.7 / 167.1 mg; MCC (microcrystalline cellulose) - 8/24 mg; polyvinylpyrrolidone (povidone) - 8/24 mg; sodium carboxymethyl starch (primogel) - 4.8 / 14.4 mg; magnesium stearate - 1.6 / 4.8 mg; aerosil (colloidal silicon dioxide) - 1.1 / 3.3 mg;
• film shell: polyvinylpyrrolidone (povidone) - 1.35 / 4.05 mg; hydroxypropyl methylcellulose (hypromellose) - 2.15 / 6.45 mg; polysorbate 80 (tween 80) - 0.45 / 1.35 mg; titanium dioxide - 0.4 / 1.2 mg; talc - 0.6 / 1.8 mg; dye quinoline yellow (E104) - 0.05 / 0.15 mg.

Pharmacological properties

Pharmacodynamics

The active ingredient of Bilumid - bicalutamide, is a racemic mixture in which its (R) -enantiomer predominantly possesses non-steroidal antiandrogenic activity. The substance does not show any other endocrine effect.

By binding to androgen receptors, but not activating gene expression, bicalutamide inhibits the stimulating effect of androgens, resulting in the regression of prostate malignant tumors.

Discontinuation of bicalutamide in some patients may lead to the development of clinical antiandrogen withdrawal syndrome.

Pharmacokinetics

Bicalutamide is rapidly and completely absorbed from the digestive tract after oral administration. Food intake does not affect its absorption. Daily use of Bilumid at a dose of 50 mg ensures the equilibrium concentration of the (R) -enantiomer in plasma at a level of ~ 9 μg / ml, at a dose of 150 mg - at a level of ~ 22 μg / ml. The proportion of the active (R) -enantiomer, subject to the equilibrium concentration of the substance in the plasma, is up to 99% of all enantiomers circulating in the blood.

Plasma protein binding is high: racemic mixture - at 96%, (R) - enantiomer - 99.6%.

Bicalutamide undergoes intensive hepatic metabolism through oxidation to form conjugates with glucuronic acid. Metabolites are excreted in approximately equal proportions by the kidneys and intestines.

Since the half-life of the (R) -enantiomer is about 7 days, the (S) -enantiomer is eliminated from the body much faster. Daily intake of bicalutamide approximately 10 times increases the equilibrium concentration of the (R) -enantiomer in blood plasma due to the long half-life. This pharmacokinetic feature of the substance allows you to take Bilumid 1 time per day.

The pharmacokinetic characteristics of the (R) -enantiomer are not influenced by the age of the patient, the state of renal function and mild / moderate hepatic dysfunction.

There is evidence that in severe liver dysfunction, the elimination of the (R) -enantiomer from plasma slows down.

Indications for use

• advanced prostate cancer (prostate cancer) - in combination with an analogue of gonadotropin-releasing hormone (GnRH) or surgical castration;
• locally advanced prostate cancer (stages T3 – T4, any N, M0; stages T1 – T2, N +, M0) - as a drug for monotherapy or adjuvant treatment in addition to radical prostatectomy or radiotherapy;
• locally advanced non-metastatic prostate cancer - when surgical castration and / or other medical interventions are inapplicable or unacceptable.

Contraindications

Absolute:

• hypolactasia, lactase deficiency, glucose-galactose malabsorption;
• simultaneous use with astemizole, terfenadine, cisapride;
• children and adolescents up to 18 years old;
• hypersensitivity to bicalutamide or auxiliary components of the drug.

Bilumid is not prescribed for female patients.

The drug is used with caution in the following cases:

• violations of hepatic function of moderate / severe severity;
• the presence of risk factors for lengthening the QT interval, the simultaneous use of drugs that lengthen the QT interval;
• concomitant use of cyclosporine; BMCC (slow calcium channel blockers); medicines that inhibit microsomal oxidation (cimetidine, ketoconazole); drugs metabolized mainly with the participation of the isoenzyme CYP3A4.

Bilumid, instructions for use: method and dosage

Bilumid tablets are intended for oral administration.

Recommended dosing regimen for adults and older men:

• common prostate cancer (in combination with the use of a GnRH analog or surgical castration): 50 mg (1 tablet) once a day. Therapy begins at the same time as the start of the GnRH analogue or immediately after surgical castration;
• locally advanced prostate cancer: 150 mg (1 tablet of 150 mg or 3 tablets of 50 mg) 1 time per day. The course of therapy is long, the drug is taken for at least 2 years. If symptoms of disease progression appear, the course should be completed.

Side effect

Side effects that develop when taking Bilumid tablets at a dosage of 50 mg:

• very often (10% or more): asthenia, anemia, breast tenderness, gynecomastia (it can persist even after the end of therapy, especially with prolonged use of bicalutamide), rash;
• often (at least 1%, but less than 10%): anemia *, hot flashes *, dizziness *, nausea *, abdominal pain *, constipation *, hematuria *, edema *, hepatotoxicity, transient increase in the activity of hepatic transaminases, jaundice (these changes in hepatic function in rare cases were assessed as serious, more often they were transient, disappeared completely or weakened with the continuation of the course or after discontinuation of therapy), decreased libido, decreased appetite, depression, drowsiness, flatulence, dyspepsia, alopecia or hirsutism (restoration of hair growth), pruritus, dry skin, erectile dysfunction, weight gain, chest pain, prolongation of the QT interval, heart failure **, myocardial infarction (there have been reports of fatal cases) **;
• rarely (not less than 0.01%, but less than 0.1%): hypersensitivity reactions, urticaria, angioedema, interstitial lung diseases (there have been reports of fatal cases), photosensitivity reactions **;
• very rare (less than 0.01%): liver failure (there have been reports of fatal cases).

Notes

* Very often, adverse reactions were observed in cases of combined administration of bicalutamide and GnRH analogues.

** Adverse reactions were observed with bicalutamide monotherapy.

Side effects that develop when taking Bilumid tablets at a dosage of 150 mg:

• very often (10% or more): asthenia, breast tenderness, gynecomastia (it can persist even after the end of therapy, especially with prolonged use of bicalutamide), skin rash;
• often (at least 1%, but less than 10%): anorexia, depression, dizziness, drowsiness, itching, hot flashes, constipation, abdominal pain, dyspepsia, flatulence, alopecia or hirsutism (restoration of hair growth), decreased libido, erectile dysfunction, swelling, chest pain, weight gain, hepatotoxicity, increased liver transaminase activity, jaundice, poor appetite, anemia;
• infrequently (not less than 0.1%, but less than 1%): hypersensitivity reactions, including angioedema and urticaria, interstitial lung disease (there have been reports of fatal cases) *;
• rarely (not less than 0.01%, but less than 0.1%): photosensitization reactions, liver failure (there have been reports of fatal cases) *.

Note

* Based on post-registration research data.

Adverse reactions such as cholestasis, increased activity of hepatic transaminases and jaundice, in rare cases, were assessed as serious. More often they were transient and with the continuation of the course or after the cancellation of Bilumid completely disappeared or their severity decreased. In extremely rare cases, against the background of bicalutamide therapy, liver function failure developed, however, the causal relationship between its development and the drug intake has not been reliably established.

Overdose

Cases of overdose of bicalutamide in humans have not been described.

In case of suspected intoxication with Bilumid, it is recommended to carry out symptomatic and general supportive treatment, while simultaneously monitoring the vital functions of the body.

Dialysis is ineffective because bicalutamide is almost completely bound to plasma proteins and is not excreted unchanged in the urine. The specific antidote for the drug is unknown.

special instructions

Taking into account the likelihood of a decrease in the rate of excretion of bicalutamide and its possible accumulation in the body of patients with hepatic insufficiency, it is recommended to periodically assess liver function in this category of patients. Most disorders of the hepatobiliary system are observed within the first six months after starting treatment with bicalutamide.

In case of progression of the disease against the background of an increase in PSA (prostate-specific antigen) levels, discontinuation of therapy should be considered.

Regular monitoring of prothrombin time is necessary when prescribing Bilumid to patients taking coumarin anticoagulants.

The simultaneous use of Bilumid with drugs metabolized mainly with the participation of CYP3A4 requires caution, since bicalutamide is able to inhibit the activity of this cytochrome P ₄₅₀ isoenzyme.

Antiandrogen therapy may increase the risk of QT prolongation. Before prescribing Bilumid, a thorough assessment of the relationship between the benefits of treatment and the risk of ventricular tachycardia of the "pirouette" type is carried out in predisposed patients with known risk factors for prolonging the QT interval or using drugs that prolong the QT interval.

Influence on the ability to drive vehicles and complex mechanisms

Bilumid does not affect the speed of psychomotor reactions and the ability of patients to increase concentration of attention, which are necessary for driving vehicles or engaging in other activities that pose a potential danger.

Application during pregnancy and lactation

Bilumid is not prescribed for female patients.

Pediatric use

The use of Bilumid in pediatrics is contraindicated.

With impaired renal function

Patients with impaired renal function do not need Bilumid dose adjustment.

For violations of liver function

Bicalutamide dose adjustment is not required in patients with mild hepatic impairment.

In case of moderate / severe liver dysfunction, an increase in the accumulation of bicalutamide is likely, the drug should be taken with caution.

In case of development of pronounced changes in hepatic function, taking Bilumid tablets should be discontinued.

Use in the elderly

There are no special indications for the use of Bilumid in elderly patients.

Drug interactions

There are no data on pharmacodynamic or pharmacokinetic interactions between GnRH analogs and bicalutamide.

In vitro, it was found that the (R) -enantiomer of bicalutamide inhibits the cytochrome P ₄₅₀ 3A4 enzyme; to a lesser extent, it affects the activity of the cytochrome P ₄₅₀ enzymes 2C9, 2C19, and 2D6.

The potential ability of bicalutamide to interact with other drugs has not been found. But it was found that when taking bicalutamide for 4 weeks simultaneously with midazolam, the area under the AUC curve of the latter increases by 80%.

Bilumid is incompatible with astemizole, terfenadine, cisapride.

If necessary, the simultaneous administration of bicalutamide and cyclosporine or BMCC, caution should be exercised. It may be necessary to reduce the doses of these drugs, mainly with the development or intensification of unwanted side effects. At the beginning of the use or after the cancellation of bicalutamide, patients need to control the level of cyclosporine in the blood plasma and careful monitoring of the clinical condition.

The use of bicalutamide in combination with inhibitors of microsomal oxidation, such as cimetidine or ketoconazole, can increase its plasma content, and also, probably, lead to an increase in the incidence of negative adverse reactions.

Showing competition for the connection with proteins, bicalutamide, when used simultaneously with coumarin anticoagulants, for example, warfarin, enhances their effect.

When carrying out antiandrogenic therapy, the risk of prolongation of the QT interval increases, and therefore, care must be taken when using Bilumid simultaneously with drugs that cause prolongation of the QT interval, or drugs that promote the development of ventricular tachycardia of the "pirouette" type. These include class IA antiarrhythmics (quinidine, disopyramide), class III (amiodarone, dofetilide, ibutilide, sotalol), moxifloxacin, methadone, antipsychotics, etc.

Analogs

Bilumid's analogues are Androblock, Balutar, Bikalutera, Bicalutamide, Bikalutamid-Sigardis, Bikalutamid-Teva, Bikaprost, Bikana, Casodex, Kalumid, etc.

Terms and conditions of storage

Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Bilumid

The few reviews about Bilumid are positive. Men who took the drug note its effectiveness both in monotherapy and in the complex treatment of prostate cancer. At the same time, they emphasize the importance of referring to specialists and starting treatment in the early stages of the disease.

Price for Bilumid in pharmacies

Estimated price for Bilumid, film-coated tablets:

• dosage 50 mg: 30 pcs. in the package - 1550-2111 rubles;
• dosage 150 mg: 28 pcs. in the package - 2785–3798 rubles.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!