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Bikalan
Last reviewed: 23.04.2024
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Bicalan is an antiandrogenic medicine.
Indications Bikalana
It is used for the common form of prostate carcinoma (late phase), together with an analogue of the element LHRH or with concomitant surgical castration.
[1]
Release form
The release of the medicinal element is made in pill form, in an amount of 10 pieces inside a cellular packaging. Inside the pack - 3 such packages.
Pharmacodynamics
Bicalutamide is a non-steroidal anti-androgen and has no other hormonal influence.
The drug is a racemic mixture, in which only the (R) -enantiomer has antiandrogenic effects. This component is synthesized with androgenic endings, without causing gene expression - in this way it inhibits the activity of androgens. Due to this suppression, the tumor in the prostate begins to regress.
Pharmacokinetics
Bicalutamide has good absorption inside the gastrointestinal tract after the use of drugs inside. Information on the clinically significant effect of food on bioavailability values is not available.
Element (S) -enantiomer has a higher than (R) -enantiomer, the rate of excretion from the body; the half-life of the latter is approximately 7 days.
After daily use of bicalutamide, the plasma level of the (R) -enantiomer increases approximately tenfold, due to the long half-life. In this regard, the drug should be taken only 1-fold per day.
After the daily administration of bicalutamide in a 50 mg dose, the plasma values of the (R) -enantiomer are approximately 9 μg / ml. At the same time, up to 99% of all enantiomers moving inside the blood fall on the (R) -enantiomer having activity.
The pharmacokinetic characteristics of the (R) -enantiomer do not depend on the patient's age or degree of liver disorder (moderate or mild).
There is information that in people with severe stages of hepatic disorders, plasma elimination of the (R) -enantiomer slows down.
Bicalutamide is synthesized in large quantities with protein (for the racemate, the indicator 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 are excreted with 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 with the use of Bicalan is required to begin in conjunction with the initiation of LHRH or a surgical castration procedure. The duration of the therapeutic cycle is prescribed by the doctor.
People with severe or moderate disorders of the liver, to avoid the risk of accumulation of the drug, it must be prescribed very carefully.
[3]
Use Bikalana during pregnancy
Bicalan is not prescribed to women.
Contraindications
Among the contraindications:
- the presence of strong sensitivity to the elements of the drug;
- use together with astemizol, terfenadine, and cisapride.
Side effects Bikalana
Bicalutamide is tolerated in most cases without complications. Only occasionally, during the development of the following side symptoms, the abolition of the use of drugs was required:
- disorders affecting the mammary glands and reproductive organs: gynecomastia 1 or pain in the area of the mammary glands 1;
- disorders of the digestive tract: nausea or diarrhea is common; single - vomiting;
- problems with the function of the hepatobiliary system: jaundice often develops 2 or transaminase values increase. There is a single deficiency of hepatic activity 3;
- immune manifestations: occasionally signs of intolerance appear, including urticaria and angioedema;
- lesions of the subcutaneous layers and the epidermis: skin dryness is rarely developed;
- thoracic, respiratory and mediastinal disorders: rarely there are pulmonary interstitial pathologies;
- systemic disorders: hot flashes occur most frequently (feeling hot) 1. The occurrence of itching or asthenia is often noted.
1, the severity can be reduced by performing an accompanying castration procedure.
2 changes affecting the hepatic activity are usually temporary and disappear completely or are weakened with the continuation of the therapeutic cycle or after it ends.
3 insufficiency of the hepatic function develops only once, and it was not possible to establish any connection with the use of Bicalan. Required to periodically monitor the performance of the liver.
[2]
Overdose
There is no information on intoxication Bikalanom.
The drug does not have an antidote, so the patient needs to prescribe symptomatic procedures. Dialysis is not performed, because bicaloutamide has a high degree of protein synthesis and it is not detected inside the urine in an unchanged state. General support activities are also performed and the work of life-critical systems is monitored.
Interactions with other drugs
There is no information regarding the drug interaction of bicalutamide with analogues of LHRH.
In vitro tests have demonstrated that R-bikalutamid inhibits CYP 3A4 element, and in addition, components CYP 2C9 with 2C19, as well as 2D6, are less pronounced.
Although testing with antipyrine, which marks the activity of the P450 element (CYP), did not prove the likelihood of the substance interacting with bicalutamide, the use of the drug for 28 days during the use of midazolam caused the AUC values of the latter to increase by 80%. Such an increase in indicators may be important for drugs with a narrow drug index. Because of this, the drug can not be combined with cisapride, terfenadine or astemizole.
It is required to very carefully combine Bicalan with drugs that block the Ca channels, or with cyclosporine. It may be necessary to reduce the portions of these funds, especially if there are suspicions of adverse symptoms (or they will develop). Persons using cyclosporine require careful monitoring, especially at the initial stage of therapy and at its termination.
It is necessary to very carefully combine the drug with substances that inhibit the oxidation of drugs (for example, cimetidine or ketoconazole). In theory, such a combination can provoke an increase in the values of bicalutamide, which will increase the incidence of negative symptoms.
In vitro testing revealed that bicalutamide is able to displace warfarin (coumarin anticoagulant) from the areas of its protein synthesis. Because of this, when it is used in those patients who use coumarin anticoagulants, it is necessary to constantly monitor the performance of PTV.
Storage conditions
Bicalan must be kept in a place closed to prevent access by small children. Temperature marks - within 25 ° С.
Shelf life
Bicalan can be used within 5 years from the date of manufacture of a therapeutic agent.
Application for children
You can not use the drug in pediatrics.
Analogs
Analogues of drugs are the drugs Apo-flutamide, Fluutan, Frugil, Xtandi with Bicalutamide, and in addition Flutazine, Bicalutera, Flutamide with Calumid and Flucin with Casodex. Also on the list are Flülem, Flutpharm with Flumid and Flutaplex with Flutamide.
Attention!
To simplify the perception of information, this instruction for use of the drug "Bikalan" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.