Касодекс 150 mg

General characteristics. Structure:

One tablet, film coated, contains:
active agent: бикалутамид 150 mg
excipients: lactoses monohydrate of 183,0 mg, carboxymethylstarch of sodium of 22,5 mg, povidone of 15,0 mg, magnesium stearate of 4,5 mg
structure of a cover: gipromelloza of 7,5 mg, macrogoal of 300 1,5 mg, titanium dioxide (E171) of 2,3 mg
Description
Round, biconvex tablets of white color, film coated; with a logo engraving in the form of the rounded-off arrow on one party and Casodex 150 – on another.

Pharmacological properties:

Pharmacodynamics. Касодекс® represents racemic mix with nonsteroid anti-androgenic activity preferential (R) - an enantiomer, has no other endocrine activity. Касодекс® contacts androgenic receptors and, without activating an expression of genes, suppresses the stimulating influence of androgens. Regression of malignant new growths of a prostate is result of it.
At some patients the termination of administration of drug of Kasodeks® can lead to development of a clinical syndrome of "cancellation" of anti-androgens.
At use of the drug Kasodeks® in a daily dose of 150 mg daily for treatment of patients with locally-spread (T3-T4, any N, M0 or any T, N+, M0) a prostate cancer, as immediate hormonal therapy or as adjuvant therapy, the risk of progressing of a disease and metastasises in a bone considerably decreases.
At a locally-spread prostate cancer the tendency to improvement of indicators of life expectancy without signs of progressing of a disease in groups of the patients accepting Касодекс® 150 mg as immediate therapy or adjuvant therapy on comparison with standard therapy (surgical treatment, radiation therapy) is noted.
Increase in life expectancy among the patients with a locally-spread prostate cancer receiving Kasodeks® in a dose of 150 mg as immediate monotherapy and as adjuvant treatment in a combination with radiation therapy is shown.
Use of the drug Kasodeks® in a dose of 150 mg in comparison with surgical castration at patients with a locally-spread not metastatic prostate cancer did not reveal statistically reliable distinction in life expectancy and time before progressing at statistically reliable advantage of sexual function and a physical state.

The pharmacokinetics After intake is quickly and completely soaked up from digestive tract. Meal does not influence absorption.
(S) - the enantiomer is brought out of an organism much quicker (R) - an enantiomer, an elimination half-life of the last - about 7 days.
At daily reception of a bikalutamid concentration (R) - an enantiomer in plasma increases approximately by 10 times owing to a long elimination half-life that does possible administration of drug once a day. At daily reception of a bikalutamid in a dose of 150 mg equilibrium concentration (R) - an enantiomer in plasma makes about 22 mkg/ml. At an equilibrium state about 99% of all enantiomer circulating in blood make active (R) - an enantiomer.
The pharmacokinetics (R) - an enantiomer is not influenced by age, a renal failure, an easy and moderate abnormal liver function. There are data that at patients with a heavy abnormal liver function elimination (R) - an enantiomer from plasma is slowed down.
Communication with proteins of plasma high (for racemic mix of 96%, for (R) - an enantiomer of 99,6%). It is intensively metabolized in a liver (by oxidation and formation of conjugates with glucuronic acid). Metabolites are removed with urine and bile approximately in equal ratios.
Average concentration (R) - an enantiomer in sperm of the men receiving Касодекс® 150 mg makes 4,9 mkg/ml. The quantity of a bikalutamid which can potentially be found in women after sexual relations low and makes about 0,3 mkg/kg (value of this indicator lower, than is required for changes of fetation from laboratory animals).

Indications to use:

• as immediate monotherapy or as adjuvant therapy in combination with a radical prostatectomy or radiation therapy to patients with a locally-spread prostate cancer.
• as monotherapy for treatment of patients with a locally-spread not metastatic prostate cancer when other medical interventions are not acceptable or are not applicable.

Route of administration and doses:

Adult men (including, elderly): inside on 150 mg once a day.
Èáß«ñѬ߮ 150 mg should be accepted it is long, at least within 2 years.
At emergence of signs of progressing of a disease administration of drug should be stopped.
Renal failures: dose adjustment is not required.
Abnormal liver functions: at an easy abnormal liver function dose adjustment is not required. At patients with average and heavy abnormal liver functions the increased drug Kasodeks® cumulation can be observed.

Features of use:

Considering a possibility of delay of removal of a bikalutamid and cumulation of a bikalutamid at patients with an abnormal liver function, it is reasonable to estimate function of a liver periodically. The majority of changes of function of a liver meet within the first six months of treatment by the drug Kasodeks®.
In case of development of the expressed changes of function of a liver administration of drug of Kasodeks® needs to be stopped.
At patients with progressing of a disease against the background of increase in concentration of prostatspetsifichesky antigen (DOG) it is necessary to consider a question of the treatment termination by the drug Kasodeks®.
At purpose of the drug Kasodeks® the patients receiving anticoagulants of a coumarinic row are recommended to control a prothrombin time regularly.
Considering a possibility of inhibition the drug Kasodeks® of activity of P450 cytochrome (CYP 3A4 isoenzyme), it is necessary to show care at simultaneous use of the drug Kasodeks® with the drugs which are preferential metabolized with participation of an isoenzyme of CYP 3A4.
Patients with a lactose intolerance need to be informed that each tablet of the drug Касодекс® 150 of mg contains 183 mg of monohydrate of lactose.
It is regularly recommended to control a prothrombin time at purpose of the drug Kasodeks® to the patients receiving indirect anticoagulants of a coumarinic row.
Influence on ability to drive the car and other mechanisms
At use of the drug Kasodeks® drowsiness and dizziness can be observed. In this connection it is necessary to be careful at control of motor transport or other moving mechanisms.

Side effects:

Except for especially stipulated cases the frequency of side effects is calculated according to monotherapy researches by the drug Касодекс® 150 of mg of an early prostate cancer.
- very often (> 10%): a gynecomastia (can remain even after the therapy termination, especially in case of administration of drug for a long time), morbidity of chest glands, skin rash, an adynamy.
- often (≥1% and <10%): depression, anorexia, dizziness, drowsiness, heat "inflows", itch, abdominal pain, lock, dyspepsia, meteorism, alopecia or growth recovery hair / hirsutism, xeroderma, hamaturia, nausea, decrease in sexual desire, erectile dysfunction, stethalgia, oedema, increase in body weight, increase in level of transaminases, hepatotoxic, jaundice, anemia, loss of appetite.
- infrequently (≥0,1% - <1%): hypersensitivity reactions, including a Quincke's disease and a small tortoiseshell, intersticial pulmonary diseases (it was reported about cases with a fatal outcome) *.
- seldom (≥0,01 - <0,1%): a liver failure (it was reported about cases with a fatal outcome) *.
Tranzitorny increase in activity of "hepatic" transaminases, cholestasia and jaundice were seldom estimated as serious, had tranzitorny character, completely disappeared or decreased at continuation of therapy or after drug withdrawal. Very seldom against the background of treatment bikalutamidy the liver failure, however relationship of cause and effect between development of a liver failure and treatment by the drug Kasodeks® authentically developed it is not established.
* According to post-marketing use of drug.

Interaction with other medicines:

Proofs of pharmacokinetic or pharmakodinamichesky interaction between the drug Kasodeks® and analogs of GNRG are not received.
In the researches in vitro it is shown that (R) - the enantiomer of a bikalutamid is CYP 3A4 isoenzyme inhibitor, to a lesser extent influencing activity of isoenzymes of CYP 2C9, 2C19 and 2D6. Potential ability of the drug Kasodeks® to interaction with other medicines is not revealed, however when using the drug Kasodeks® within 28 days against the background of midazolam reception, the area under a curve "concentration time" (AUC) of midazolam increases by 80%. It is incompatible with terfenadiny, astemizoly, tsizapridy.
It is necessary to be careful at use of the drug Kasodeks® along with cyclosporine or blockers of calcium channels. Perhaps, the dose decline of these drugs, especially in case of a potentsiirovaniye or development of side reactions will be required. After the beginning of use or drug withdrawal of Kasodeks® it is recommended to carry out careful monitoring of concentration of cyclosporine in plasma and a clinical condition of the patient.
Simultaneous use of the drug Kasodeks® and the drugs inhibiting microsomal enzymes of a liver, for example, with Cimetidinum or ketokonazoly, can lead to increase in concentration of a bikalutamid in plasma and, perhaps, to increase in frequency of emergence of side effects. Strengthens effect of indirect anticoagulants of a coumarinic row, including, warfarin.

Contraindications:

- Hypersensitivity to a bikalutamid or other components of drug.
- A concomitant use with terfenadiny, astemizoly and tsizapridy.
- Касодекс® it should not be appointed to children and women.

With care: abnormal liver function, lactose intolerance, deficit of lactase and glyukozo-galaktozny malabsorption.
Pregnancy and lactation
Касодекс® it is contraindicated to women and it should not be appointed pregnant or in the period of a lactation.

Overdose:

Overdose cases at the person are not described. The specific antidote does not exist. Symptomatic treatment. Carrying out dialysis is not effective as бикалутамид strongly contacts proteins and is not removed with urine in not changed look. The general maintenance therapy and monitoring of the vital functions of an organism is shown.

Storage conditions:

At a temperature below 30 °C, in the place, unavailable to children. Period of validity 4 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 150 mg. On 14 tablets in the blister from PVC Is scarlet/. On 2 blisters in a cardboard pack with the application instruction.