Bikalutamid Kabi

General characteristics. Structure:

Active ingredient: 50 mg of a bikalutamid.

Excipients: lactoses monohydrate, carboxymethylstarch of sodium, silicon dioxide colloid, povidone, magnesium stearate.

Structure of a cover: опадрай white (Y-1-7000) (gipromelloza of 5 cP, titanium dioxide, macrogoal 400).

Pharmacological properties:

Pharmacodynamics. Antineoplastic means, nonsteroid anti-androgenic drug - the competitive antagonist of endogenous androgens.

Contacting receptors on a surface of cells of target organs, does them unavailable to androgens, increasing at the same time concentration of hormones in plasma. Regression of new growths of a prostate is result of it.

Purpose of a bikalutamid in a dose of 150 mg/days sick with localized (T1-T2, N0 or NX, MO) or locally-spread (T3-T4, any N, MO; T1-T2, N+, MO) a prostate cancer reduces risk of progressing of a disease by 42% and relative risk of innidiation in a bone for 33% during observation up to 2 years.

At the same time efficiency of a bikalutamid concerning indicators of survival is lower that when performing surgical castration.

At some patients the termination of reception can lead to development of a syndrome of "cancellation" of anti-androgens (after cancellation at 10-15% of patients there occurs temporary stabilization of a disease).

Pharmacokinetics. After intake it is quickly and completely soaked up from a GIT (meal does not influence absorption).

Communication with proteins of plasma - 96-99%. It is intensively metabolized in a liver (by oxidation and formation of conjugates with glucuronic acid) to inactive (S) - and active (R) - enantiomer. TCmax (R) - an enantiomer - 31.3 h (S) - an enantiomer is brought out of an organism much quicker (R) - an enantiomer; T1/2 of the last - about 7 days. At daily reception of a bikalutamid in a dose of 150 mg/days of Css (K) - an enantiomer in plasma - 22 mkg/ml. At Css about 99% of all enantiomer circulating in blood make active (R) - an enantiomer. At daily reception concentration (R) - an enantiomer in plasma increases approximately by 10 times owing to long T1/2.

It is removed in the form of metabolites by kidneys and with bile in equal ratios. The pharmacokinetics (R) - an enantiomer does not depend on age, a condition of function of kidneys, against the background of a moderate abnormal liver function; at patients with heavy abnormal liver functions elimination (R) - an enantiomer from plasma is slowed down.

Indications to use:

— a prostate cancer (treatment of the localized prostate cancer of the patients who did not undergo a radical prostatectomy or radiotheraphy; monotherapy or adjuvant therapy in combination with a radical prostatectomy or radiotheraphy of a locally-spread prostate cancer; treatment of a locally-spread, not metastatic prostate cancer in cases when surgical castration or other medicines are not effective or unacceptable).

Route of administration and doses:

At a widespread prostate cancer - inside, 50 mg/days once in combination with an analog of GNRG or surgical castration.

At not metastatic prostate cancer of in situ as monotherapy (in the presence of contraindications to surgical castration or to purpose of other medicines) - po150 mg/days once.

Bikalutamid it is necessary to accept for a long time, at least within 2 years.

Dose adjustment is required from patients with average and heavy abnormal liver functions.

Features of use:

Use at pregnancy and feeding by a breast. Drug is contraindicated at pregnancy and in the period of a lactation.

Use at abnormal liver functions. With care it is necessary to appoint at a liver failure. Dose adjustment is required from patients with average and heavy abnormal liver functions.

Use for children. It is contraindicated to children.

Special instructions. At joint reception with cyclosporine, after the beginning of use or cancellation of a bikalutamid, it is recommended to carry out careful control of concentration of cyclosporine in plasma and conditions of the patient.

The researches in vitro showed what бикалутамид can force out warfarin from binding sites with protein (it is regularly necessary to control a prothrombin time).

Elimination of a bikalutamid from an organism can be slowed down at patients with heavy abnormal liver functions that can lead to its cumulation. It is reasonable to estimate periodically function of a liver (the majority of changes of function of a liver meet within the first 6 months of treatment). To stop treatment at emergence of clinical symptoms and/or increase in functional trials more, than twice. In case of development of severe damages of a liver it is necessary to stop reception.

At patients with progressing of a disease against the background of increase in level of prostatspetsifichesky antigen it is necessary to consider a question of the treatment termination.

Influence on ability to driving of motor transport and to control of mechanisms. 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.

Side effects:

From cardiovascular system: stenocardia, development or aggravation of heart failure, increase in the ABP.

From respiratory system: stethalgia, cough, pharyngitis, bronchitis, pneumonia, rhinitis.

From the alimentary system: seldom - an abdominal pain, a meteorism, dyspepsia, gastric bleeding, dryness in a mouth, tranzitorny increase in activity of "hepatic" transaminases, a cholestasia, jaundice; very seldom - an abnormal liver function.

From a nervous system: dizziness, sleeplessness or drowsiness, uneasiness, is rare - a depression.

From a musculoskeletal system: myasthenia, mialgiya, spasms, arthritis, contractures of joints.

From endocrine system: often (> 10%) - a gynecomastia (can remain after the therapy termination, especially in case of administration of drug for a long time), morbidity of mammary glands; hyperglycemia, diabetes mellitus, polyuria.

From an urinary system: dysuria, ischuria, hypostases; seldom - a hamaturia.

Others: often - an adynamy, an alopecia, decrease or increase in body weight, decrease in a libido; fever, a fever, the increased sweating, anemia, pain in pelvic area, a xeroderma, a hirsutism, allergic reactions, "inflows" of blood to the person.

Interaction with other medicines:

Strengthens effects of anticoagulants of indirect action.

Increases AUC midazolam by 80%.

It is incompatible with terfenadiny, astemizoly, tsizapridy.

Increases risk of emergence of adverse effects at co-administration with the cyclosporine, blockers of slow calcium channels, medicines oppressing a microsomal oxidation (in
т.ч. Cimetidinum, ketokonazoly).

Contraindications:

— concomitant use of a terfenadin, astemizol and tsizaprid;

— children's age;

— hypersensitivity.

Drug is not appointed to women during pregnancy and a lactation.

With care it is necessary to appoint at a liver failure.

Overdose:

Treatment: symptomatic, the specific antidote does not exist. Carrying out dialysis is inefficient as бикалутамид strongly contacts proteins and is not removed with urine in not changed look.

The general maintenance therapy and control of the vital functions of an organism is shown.

Storage conditions:

To store in the place, unavailable to children, at a temperature not above 30 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

10 pieces - blisters (2) - packs cardboard.
10 pieces - blisters (3) - packs cardboard.
10 pieces - blisters (4) - packs cardboard.
10 pieces - blisters (5) - packs cardboard.
10 pieces - blisters (6) - packs cardboard.
14 pieces - blisters (2) - packs cardboard.
14 pieces - blisters (4) - packs cardboard.