Bicalutamide - Instructions For Use, 50 Mg, 150 Mg, Price, Analogues

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

Bicalutamide

Bicalutamide: 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. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Bicalutamide

ATX code: L02BB03

Active ingredient: bicalutamide (bicalutamide)

Manufacturer: Ozone LLC (Russia); Pharmasintez-Nord JSC (Russia); Drug Technology (Russia); Biocad CJSC (Russia); Biosynthesis Laboratories Private Limited (India); Beijing Ilin Bioengineering & Technology Co., Ltd. (Peking ilin BioEngineering and Technology Co. Ltd) (China); Jiangxi Tasli Dii Pharmaceutical Co., Ltd. (Jiangsu Tasly Diyi Pharmaceutical, Co., Ltd.) (China), etc.

Description and photo updated: 2019-27-08

Prices in pharmacies: from 400 rubles.

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Bicalutamide is an antineoplastic hormonal drug that suppresses the stimulating effect of androgens.

Release form and composition

Dosage form of release - film-coated tablets: biconvex, round, white, engraved on one side (depending on the dosage) "50" or "150"; cross-sectional color - white (in blisters of 7 pcs., in a cardboard bundle of 3 or 4 packs; in blister packs of 10 or 30 pcs., in a carton of 1-6, 10 packs; in blister packs of 14 pcs., In a cardboard box 2 or 20 packs; in plastic or glass dark jars of 10, 20, 21, 28, 30, 40, 50, 60 or 100 pcs., In a cardboard box 1 can; each pack also contains instructions for the use of Bicalutamide).

Composition of 1 tablet:

• active substance: bicalutamide - 50 or 150 mg;
• auxiliary components (50/150 mg): lactose monohydrate - 61/183 mg; sodium carboxymethyl starch - 7.5 / 22.5 mg; povidone - 5/15 mg; magnesium stearate - 1.5 / 4.5 mg;
• shell (50/150 mg): film coating (titanium dioxide, macrogol, hypromellose) - 3.8 / 11.3 mg.

Pharmacological properties

Pharmacodynamics

Bicalutamide is a racemic mixture that exhibits a non-steroidal antiandrogenic effect, mainly of the (R) -enantiomer, and has no other endocrine activity. By binding to androgen receptors, Bicalutamide suppresses the stimulating effect of androgens without activating gene expression. As a result, regression of prostate neoplasms occurs.

Discontinuation of Bicalutamide in some patients can cause clinical antiandrogen withdrawal syndrome.

In the case of daily use of a daily dose of 150 mg Bicalutamide for the treatment of locally advanced prostate cancer [T (tumor) size and spread of the primary tumor - T3-T4; N (nodus) absence / presence of metastases in regional lymph nodes - any; M (metastases) - M0 (no signs of distant metastases), or at any value of T and N +, and M0] as monotherapy or adjuvant therapy, the risk of disease progression and bone metastases is clinically significantly reduced.

In the treatment of locally advanced prostate cancer in the groups of patients who used Bicalutamide as mono- or adjuvant therapy at a dose of 150 mg, there was a tendency for an increase in life expectancy indicators without signs of disease progression, compared with standard treatment (surgery, radiation therapy).

An increase in life expectancy has been clinically proven among patients with locally advanced prostate cancer who received Bicalutamide as mono- and adjuvant therapy at a dose of 150 mg in combination with radiotherapy.

Pharmacokinetics

Bicalutamide after oral administration is absorbed in the gastrointestinal tract (GIT) quickly and completely, the bioavailability of the drug does not depend on food intake.

The elimination of the (S) -enantiomer from the body occurs much faster than the (R) -enantiomer. T _1/2 (half-life) of the latter is about 7 days.

Daily intake of Bicalutamide increases the concentration of its (R) -enantiomer in blood plasma by about 10 times, due to a long T _1/2. This allows you to take the drug once a day.

Due to the daily intake of a dose of Bicalutamide 50 mg, the equilibrium plasma concentration of the (Css) (R) -enantiomer is established within 9 μg / ml, with a daily intake of 150 mg, this figure is about 22 μg / ml. In the equilibrium state, up to 99% of all enantiomers circulating in the blood are the active (R) -enantiomer. The indicator of its average concentration in the semen of patients receiving Bicalutamide at a dose of 150 mg is 4.9 μg / ml.

Up to 96% of the racemic mixture binds to plasma proteins, for the (R) -enantiomer this figure is 99.6%. Intensive metabolism of the substance occurs in the liver through oxidation with the formation of conjugates with glucuronic acid. Metabolites are excreted through the genitourinary system and the gastrointestinal tract in approximately equal amounts.

Patient age, impaired renal function, mild and moderate impairment of hepatic function do not affect the pharmacokinetic characteristics of the (R) -enantiomer. There is evidence of a slowdown in the elimination of the (R) -enantiomer from plasma in severe liver dysfunction.

Indications for use

Bicalutamide 50 mg

The drug is prescribed for the treatment of advanced prostate cancer in combination with an analogue of GnRH (gonadotropin-releasing hormone) or surgical castration.

Bicalutamide 150 mg

• locally advanced prostate cancer (T3 – T4, any N, M0; N +, T1 – T2, M0) - alone or as adjuvant therapy in combination with radiation therapy or radical prostatectomy;
• locally advanced non-metastatic prostate cancer in cases where surgical castration or other medical interventions are not suitable for the patient or are unacceptable.

Contraindications

Absolute:

• combined use with terfenadine, cisapride and astemizole;
• individual intolerance to the components of the drug.

In addition, Bicalutamide is not prescribed for women and children.

Relative (Bicalutamide is prescribed with caution in the presence of the following diseases / conditions):

• functional disorders of the liver;
• lactose intolerance, glucose-galactose malabsorption and lactase deficiency.

Bicalutamide, instructions for use: method and dosage

Bicalutamide tablets are taken orally once a day.

For adult men, including elderly patients, the drug is prescribed in the following daily doses:

• advanced prostate cancer: 50 mg (in combination with a GnRH analog or surgical castration, combination therapy begins at the same time);
• locally advanced prostate cancer: 150 mg. Treatment is long-term, for at least two years. The drug is canceled in cases of signs of disease progression.

In case of moderate / severe functional disorders of the liver, an increase in the accumulation of the drug may be observed.

Side effects

In general, Bicalutamide therapy is well tolerated by patients. Due to the development of adverse reactions, the drug is canceled only in rare cases.

Possible violations (very often - ≥ 10%; often - ≥ 1% and <10%; infrequently - ≥ 0.1% and <1%; rarely - ≥ 0.01% and <0.1%; very rarely - < 0.01%, with an unknown frequency - if it is impossible to estimate the frequency of side effects on the basis of available data):

• cardiovascular system: very often - hot flashes; often - arterial hypertension, myocardial infarction (there is evidence of fatal cases); infrequently - heart failure;
• nervous system: very often - dizziness; often - insomnia, drowsiness, anxiety, paresthesia, headache;
• respiratory system, mediastinal and chest organs: very often - shortness of breath; often - bronchitis, rhinitis, pharyngitis, increased cough, pneumonia; infrequently - interstitial lung disease (there is evidence of fatal cases);
• digestive system: very often - constipation, diarrhea, nausea, abdominal pain; often - flatulence, dyspepsia, vomiting;
• immune system: infrequently - hypersensitivity reactions (including urticaria and angioedema);
• blood and lymphatic system: often - anemia;
• endocrine system: often - hyperglycemia; with an unknown frequency - decreased glucose tolerance;
• musculoskeletal system: often - arthritis, arthralgia, myasthenia gravis, pathological fractures, back and bone pain;
• psyche: often - depression, decreased libido;
• liver and biliary tract: often - transient changes in the liver (hepatotoxicity), including jaundice, increased activity of hepatic transaminases and alkaline phosphatase (these disorders were rarely assessed as serious, in most cases they were transient, after discontinuation of Bicalutamide they decreased or completely disappeared); rarely - liver failure (a reliably causal relationship with taking the drug has not been established);
• skin and subcutaneous tissue: very often - rash; often - itchy skin, dry skin, alopecia, hirsutism / hair regrowth, excessive sweating;
• urinary tract and kidneys: very often - hematuria, nocturnal urge to urinate; often - urinary disorders, urinary tract infections, frequent urination, urinary incontinence / retention;
• metabolism and nutrition: very often - asthenia; often - anorexia, weight loss / loss;
• genitals and mammary gland: very often - gynecomastia (the violation can persist even after stopping therapy, especially in cases of prolonged use of Bicalutamide) and breast tenderness; often - erectile dysfunction / impotence;
• general disorders: very often - peripheral edema, infections, chest and pelvic pain; often - flu-like syndrome.

Overdose

There is no data on overdose of Bicalutamide in humans.

The specific antidote for the drug is unknown. Since Bicalutamide strongly binds to plasma proteins and is not excreted unchanged by the kidneys, dialysis is ineffective. A set of measures for general supportive therapy and monitoring of vital body functions are recommended.

special instructions

With the progression of the disease against the background of an increase in the concentration of prostate-specific antigen (PSA), it is necessary to consider the issue of stopping the intake of Bicalutamide.

During the use of GnRH agonists, it is possible to develop a decrease in glucose tolerance, which can lead to the appearance of diabetes mellitus or a decrease in glucose tolerance in patients with diabetes mellitus (during the period of combination therapy with GnRH agonists, it is necessary to control the concentration of glucose in the blood).

With functional disorders of the liver, it is advisable to periodically assess liver function. As a rule, changes in liver function develop during the first half of the year of using Bicalutamide. With the development of pronounced changes, therapy is canceled.

Influence on the ability to drive vehicles and complex mechanisms

During the treatment period, drowsiness and dizziness may develop. In these cases, it is recommended to refuse from driving and other activities that require increased attention.

Application during pregnancy and lactation

Bicalutamide is not used to treat female patients.

Pediatric use

The drug is not used in pediatrics.

With impaired renal function

Patients with renal insufficiency (impaired renal function) do not require dose adjustment.

For violations of liver function

Patients with mild hepatic impairment (impaired liver function) do not require dose adjustment of Bicalutamide.

With hepatic failure of moderate and severe degree, its increased cumulation is possible. But despite the fact that in patients with severe hepatic insufficiency, T _{1/2 of the} active enantiomer of Bicalutamide increases by 76%, dose adjustment is not required.

Drug interactions

There is no evidence of a pharmacodynamic or pharmacokinetic interaction between GnRH analogs and Bicalutamide.

When carrying out therapy for 28 days while taking midazolam, the AUC (area under the concentration-time curve) of the latter increased significantly.

The simultaneous use of terfenadine, astemizole and cisapride is contraindicated.

Caution must be observed when combined use with the following drugs / substances:

• cyclosporine or slow calcium channel blockers: their dose may need to be reduced, especially in cases of adverse reactions; after the start of the course of using bicalutamide or its cancellation, it is recommended to conduct careful monitoring of the plasma concentration of cyclosporine in the blood and the clinical condition of the patient;
• drugs that inhibit liver microsomal enzymes, including cimetidine, ketoconazole: an increase in the plasma concentration of bicalutamide in the blood and an increase in the incidence of side effects is possible;
• indirect coumarin anticoagulants, including warfarin: bicalutamide enhances their effect (it is recommended to regularly monitor the prothrombin time).

Analogs

Bicalutamide analogues are Bicaluthera, Androblock, Bicalutamide Kabi, Bicalutamide-Sigardis, Bicalutamide Canon, Bicalutamide-Teva, Balutar, Bikaprost, Bilumid, Bikana, Casodex, Kalumid, etc.

Terms and conditions of storage

Store in a dark, dry place at temperatures up to 30 ° C. Keep out of the reach of children.

Shelf life is 4 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Bicalutamide

According to reviews, Bicalutamide is an effective drug for the treatment of prostate cancer. Patients recommend strictly adhering to the doctor's prescriptions, which will prolong the period of remission. It is advised to beware of counterfeits and to purchase the drug only in reliable pharmacies. It is noted that the effect may decrease over time, since addiction to Bicalutamide is possible. Some patients complain of side reactions in the form of abdominal pain and jaundice.

Price for Bicalutamide in pharmacies

The approximate price for Bicalutamide 150 mg (for 30 tablets per package) is 1,364 rubles.

Bicalutamide: prices in online pharmacies

Drug name Price Pharmacy

Bicalutamide 50 mg film-coated tablets 30 pcs. RUB 400 Buy

Bicalutamide Canon 50 mg film-coated tablets 30 pcs. RUB 545 Buy

Bicalutamide Canon 150 mg film-coated tablets 30 pcs. 987 r Buy

Bicalutamide Kabi 50 mg film-coated tablets 28 pcs. 1025 RUB Buy

Bicalutamide 150 mg film-coated tablets 30 pcs. 1360 RUB Buy

Bicalutamide 150 mg film-coated tablets 28 pcs. RUB 1575 Buy

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!