Касодекс 50 mg

General characteristics. Structure:

Active ingredient – бикалутамид 50 mg;
Auxiliary ingredients – lactoses monohydrate of 61 mg, carboxymethylstarch of sodium of 7,5 mg, povidone of 5,0 mg, magnesium stearate of 1,5 mg;
structure of a cover – a gipromelloz of 2,5 mg, a macrogoal of 300 0,5 mg, titanium dioxide (E171) of 0,77 mg.
Description
Round, biconvex tablets, film coated white color; with a logo engraving in the form of the rounded-off arrow on one party and Cdx – on another.
50

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.

Pharmacokinetics. After intake it 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 the long period
semi-removal that does possible administration of drug once a day. At daily reception of a bikalutamid in a dose of 50 mg equilibrium concentration (R) - an enantiomer makes about 9 mkg/ml. At reception of 150 mg of a bikalutamid daily equilibrium concentration (R) - an enantiomer 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 on that,
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.

Indications to use:

 Касодекс® in a dose of 50 mg in a combination with GNRG analog (a gonadotrophin - a rileasing hormone) or surgical castration it is shown for treatment of a widespread prostate cancer
- Касодекс® in a dose of 150 mg it is shown for treatment of a locally-spread prostate cancer (T3-T4, any N, M0; T1-T2, N+, M0) as monotherapy or adjuvant therapy in combination with a radical prostatectomy or radiotheraphy
- Касодекс® in a dose of 150 mg it is also shown for treatment of a locally-spread, not metastatic prostate cancer in cases when surgical castration or other medical interventions are unacceptable or do not suit the patient.

Route of administration and doses:

Adult men (including, elderly):
At a widespread prostate cancer in a combination with an analog of GNRG or surgical castration: inside on 50 mg once a day. Treatment by the drug Kasodeks® needs to be begun along with the beginning of reception of an analog of GNRG or surgical castration.
At a locally-spread prostate cancer: inside on 150 mg once a day. Касодекс® it is necessary to accept 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 an average and heavy abnormal liver function the increased drug Kasodeks® cumulation can be observed (see the section "Special Instructions").

Features of use:

Касодекс® it is intensively metabolized in a liver. Considering a possibility of delay of removal of a bikalutamid and cumulation of a bikalutamid at patients with the expressed 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®.
Касодекс® it is necessary to apply with care at patients with an average and heavy abnormal liver function.
Heavy hepatic changes when using the drug Kasodeks® arise seldom (see the section "Side effect"), was reported about cases with a fatal outcome. 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®.
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 (see the section "Contraindications" and "Interaction with Other Medicines and Other Types of Medicinal Interaction").
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.
At the patients accepting GNRG agonists decrease in portability of glucose was observed. This effect can lead to development of a diabetes mellitus or decrease in tolerance to glucose at patients with a diabetes mellitus. In this connection, at the patients accepting Kasodeks® in a combination with GNRG agonists it is necessary to control concentration of glucose in blood.

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:

Касодекс it is well transferred by most of patients, and only in rare instances it should be cancelled because of the side effects caused by it.
 
The following side effects can be caused by Kasodeks's action:
 
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, heat inflows;
 
often (≥1%-<10%): diarrhea, nausea, tranzitorny increase in activity of hepatic transaminases, a cholestasia and jaundice (the described changes of function of a liver seldom were estimated as serious, had tranzitorny character and completely disappeared or decreased, despite continuation of therapy or after its termination), an itch, an adynamy; at use of drug in a daily dose of 150 mg - an alopecia or a growth recovery of hair, decrease in sexual desire, sexual dysfunctions, increase in body weight;
 
seldom (≥0.1%-<1%): hypersensitivity reactions, including a Quincke's disease and a small tortoiseshell, intersticial pulmonary diseases; at use of drug in a dose of 150 mg - an abdominal pain, a depression, dyspepsia, a hamaturia;
 
very seldom (≥ 0.01%-<0.1%): vomiting, a xeroderma (at use of drug in a daily dose of 150 mg it is observed often), a liver failure (relationship of cause and effect is not established with Kasodeks's reception).
 
At simultaneous use of Kasodeks and analogs of GNRG also following side effects with a frequency of 1% can be observed (relationship of cause and effect is not established with administration of drug, some of noted effects often arise at elderly patients without Kasodeks's reception):
 
From cardiovascular system: heart failure.
 
From the alimentary system: anorexia, dryness in a mouth, dyspepsia, a lock, a meteorism.
 
From TsNS: dizziness, headache, sleeplessness, drowsiness.
 
From respiratory system: asthma.
 
From urinogenital system: sexual dysfunction, nocturia.
 
From system of a hemopoiesis: anemia.
 
Dermatological reactions: alopecia, rash, sweating strengthening, hirsutism.
 
From a metabolism: diabetes mellitus, hyperglycemia, hypostases, increase or degrowth of a body.
 
Others: an abdominal pain, a stethalgia, pain in the field of a basin, a fever.

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. In clinical trials with use of phenazone as a marker of activity of P450 (CYP) cytochrome potential ability of the drug Kasodeks® to interaction with other medicines is not revealed, however at use of the drug Kasodeks® within 28 days against the background of midazolam reception, the area under a curve "concentration time" (AUC) of midazolam increased by 80%.
Contraindicated simultaneous use of the drug Kasodeks® with such drugs, as терфенадин, астемизол and цизаприд. It is necessary to be careful at use of the drug Kasodeks® along with cyclosporine or blockers of "slow" calcium channels. Perhaps, the dose decline of these drugs, especially, in case of development of by-effects 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.
To show care at the simultaneous use of the drug Kasodeks® and drugs inhibiting microsomal enzymes of a liver, for example, with Cimetidinum or ketokonazoly. Simultaneous use 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 (the competition for communication with proteins). 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.

Contraindications:

- Hypersensitivity to a bikalutamid or other components
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, a symptomatic treatment. 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 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 of 5 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 50 mg. 14 tablets in the blister from PVC, on 2 blisters in a cardboard pack with the application instruction Is scarlet/.