Bikalutamid Grindeks

General characteristics. Structure:

Active ingredient: 50 mg of a bikalutamid.

Vspomogatelyy substances: lactoses monohydrate, K-30 povidone, sodium of starch glikolit, magnesium stearate.

Cover: опадрай white Y-1-7000 which part are: gipromelloza, titanium dioxide (Е 171), macrogoal 400.

Anti-androgenic nonsteroid means.

Pharmacological properties:

Pharmacodynamics. Bikalutamid represents nonsteroid anti-androgenic drug – the competitive antagonist of endogenous androgens, without other endocrine activity. Bikalutamid Grindeks is the racemic mix having anti-androgenic activity preferential at the expense of (R) - an enantiomer. Contacting androgenic receptors without activation of a gene expression, on a surface of cells of target organs, does them unavailable to androgens, increasing at the same time concentration of hormones in plasma. This braking is resulted by regression of tumors of a prostate. Treatment cancellation bikalutamidy can cause a syndrome of "cancellation" of anti-androgens in some patients. Bikalutamid possesses low degree of affinity with GSPG (the globulin connecting sex hormones), but it has no clinical value.

Pharmacokinetics. After intake it is quickly and completely soaked up from a GIT (meal does not influence absorption). Bikalutamid has high ability to contact proteins (racemic mix of 96%, (R) - бикалутамид 99,6%) and is intensively metabolized in a liver by oxidation and formation of conjugates with glucuronic acid to inactive (S) - and active (R) - enantiomer. Metabolites are removed by kidneys and with bile approximately in equal proportions.

TCmax (R) - an enantiomer – 31,3 h (S) - an enantiomer is brought out of an organism much quicker, an elimination half-life – (S) - an enantiomer about 7 days. At long reception the maximum concentration (R) - an enantiomer of a bikalutamid in plasma increase approximately by 10 times in comparison with indicators after reception of a single dose of a bikalutamid of 50 mg. At daily reception of 50 mg of a bikalutamid equilibrium concentration (R) - an enantiomer makes about 9 mkg/ml, and owing to a long elimination half-life the equilibrium state is reached approximately in 1 month of treatment.

The pharmacokinetics (R) - an enantiomer not зависитот age, a renal failure or a weak and moderate liver failure, at patients with heavy abnormal liver functions is slowed down elimination (R) - an enantiomer from a blood plasma.

Indications to use:

Locally widespread prostate cancer (in combination with use of analog LGRG-lyuteiniziruyushchego of hormone a rileasing of hormone or surgical castration).

Route of administration and doses:

Adult men, including elderly: on one tablet of 50 mg inside once a day. Treatment bikalutamidy needs to be begun along with treatment by an analog of LGRG or surgical castration.

Duration of a course of treatment of a combination therapy depends on individual clinical reaction of the patient. Assessment of efficiency of treatment requires periodic control of a specific antigen of a prostate (DOG) in syvorotkekrov.

Individual dose adjustment for patients with a renal failure and for patients with an easy form of a liver failure is not required.

Features of use:

Do not appoint to female patients and children up to 18 years.

With care to apply at patients with moderately expressed and heavy abnormal liver functions since cumulation of a bikalutamid in an organism is possible.

During treatment regular control of function of a liver is required. In case of development of heavy changes it is necessary to stop reception of a bikalutamid.

Considering side effects, during treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Use of drug is contraindicated to patients with a rare vrozhdennoyneperenosimost of a galactose, deficit of Lapp of lactase or a malyabsorbtsiyeyglyukozy-galactose.

Side effects:

Stenocardia attack, hypertensia, heart failure, cough, pharyngitis, bronchitis, pneumonia, rhinitis, dispeptic phenomena, xerostomia, gastric bleedings, melena, alarm, depression, decrease libido, drowsiness, nervousness, myasthenia, mialgiya, arthritis, convulsive twitchings of muscles of extremities, contractures, stethalgia, diabetes mellitus, polyuria, dysuria, ischuria, hypostases, fever, perspiration, allergic reactions.

Interaction with other medicines:

At use of a bikalutamid within 28 days against the background of reception of midazolam, AUC of midazolam increased by 80%.

At simultaneous use of a bikalutamid with cyclosporine or blockers of calcium channels potentiation or development of undesirable reactions is possible.

Increase in concentration of a bikalutamid in a blood plasma at its simultaneous use with inhibitors of microsomal enzymes of a liver is theoretically possible that can be followed by increase in frequency of emergence of undesirable reactions.

The researches in vitro showed what бикалутамид can force out anticoagulant of a coumarinic row warfarin from binding sites with proteins of plasma.

Contraindications:

- гиперчувствительностьк to a bikalutamid, other components of drug;

- odnovremennyypriy terfenadina, astemizola and tsizaprida;

- female;

- children's age up to 18 years.

Overdose:

Cases of overdose were not observed. Strengthening of side effects is possible. The specific antidote is not available. Treatment has to be symptomatic. Dialysis is ineffective as it бикалутамид has high ability of linkng with proteins and it is not found in urine in an invariable look. The usual supporting treatment with frequent monitoring of the vital functions of an organism is appointed.

Storage conditions:

At a temperature not above 25 °C. (in tight packaging) in places, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil or in a blister strip packaging from a film polyvinyl chloride with a polyvinylidene chloride covering and aluminum foil.

On 3 blister strip packagings together with the application instruction in the state and Russian languages place in a pack from a cardboard.