Bicalutamide Kabi - instructions for use, dose, side effects, contraindications

Active substance:
Bicalutamide	50.00 mg
Excipients:
Lactose Monohydrate	88.93 mg
Sodium carboxymethyl starch	5.00 mg
Silica colloidal dioxide	0.45 mg
Povidone	4.50 mg
Magnesium stearate	1.12 mg
Sheath:
Drop off white (Y-1-7000):	3.75 mg
- hypromellose 5 cP	2.344 mg
- titanium dioxide	1.172 mg
- macrogol-400	0.234 mg

Description:

Round, biconvex tablets covered with a film shell, white or almost white with engraving DB01 on one side and smooth on the other side. On the cross section, the core of the tablet is white.

Pharmacotherapeutic group:Antitumor agent - antiandrogen

ATX: & nbsp

L.02.B.B.03 Bicalutamide

Pharmacodynamics:

An antitumor agent, a nonsteroidal antiandrogenic drug is a competitive antagonist of endogenous androgens.By binding to receptors on the surface of the cells of target organs, they make them inaccessible to androgens, thereby increasing the concentration of hormones in the plasma. The result of this is the regression of prostate tumors.

The administration of bicalutamide at a dose of 150 mg / day to patients with localized (T1-T2, N0 or NX, M0) or locally advanced (T3-T4, any N, M0, T1-T2, N +, M0) prostate cancer reduces the risk of disease progression 42% and the relative risk of metastasis in the bone by 33% during the observation period to 2 years.

At the same time, the effectiveness of bicalutamide in relation to survival rates is lower than that for surgical castration.

In some patients, discontinuation may lead to the development of the syndrome of "cancellation" of antiandrogens (after the abolition of 10-15% of patients there is a temporary stabilization disease).

Pharmacokinetics:

After intake, quickly and completely absorbed from the digestive tract (eating does not affect the suction). The connection with plasma proteins is 96-99%. Intensively metabolized in the liver (by oxidation and the formation of conjugates with glucuronic acid) to inactive (S) - and active (R) -enantiomers. TS_mOh (R) -enantiomer-31.3 hours, (R) -enantiomer is excreted from the body much faster (R) -enantiomer, T_1/2the last - about 7 days.

With a daily intake of bicalutamide in a dose of 150 mg / day Css (R) enantiomer in plasma was 22 μg / ml. At Css, about 99% of all enantiomers circulating in the blood are active (R) -enantiomer. With daily intake of concentration (R) -enantiomer in plasma increases approximately 10-fold due to prolonged T_1/2. It is excreted as metabolites by the kidneys and with bile in equal proportions. The pharmacokinetics of the (R) -enantiomer does not depend on the age, the state of the kidney function, against a background of moderate impaired hepatic function; In patients with severe impairment of liver function, elimination is slowed (R) -enantiomer from the plasma.

Indications:

Prostate cancer (treatment of localized prostate cancer in patients who have not undergone radical prostatectomy or radiotherapy, monotherapy or adjuvant therapy in combination with radical prostatectomy or radiotherapy of locally advanced prostate cancer, treatment of locally advanced, non-metastatic prostate cancer in cases where surgical castration or other. Drugs are ineffective or unacceptable).

Contraindications:

Hypersensitivity, simultaneous reception of terfenadine, astemizole and cisapride, children's age, women, pregnancy, lactation.

Carefully:

Liver failure.

Dosing and Administration:

With advanced prostate cancer - Inside, 50 mg / day once in combination with an analogue of LHRF or surgical castration.

In nonmetastatic prostate cancer in situ as a monotherapy (in the presence of contraindications to surgical castration or to the appointment of other drugs) - 150 mg / day once.

Bicalutamide should be taken continuously for at least 2 years.

Correction of dose is required in patients with moderate and severe impairment of liver function.

Side effects:

From the CAS side: angina pectoris, development or exacerbation of heart failure, increased blood pressure.

From the respiratory system: pain in the chest, cough, pharyngitis, bronchitis, pneumonia, rhinitis.

From the digestive system: rarely - abdominal pain, flatulence, indigestion, gastric bleeding, dry mouth, transient increase in the activity of "liver" transaminases, cholestasis, jaundice; very rarely - a violation of the liver.

From the nervous system: dizziness, insomnia or drowsiness, anxiety; rarely - depression.

From the musculoskeletal system: myasthenia gravis, myalgia, convulsions, arthritis, joint contractures.

From the endocrine system: often (> 10%) - gynecomastia (may persist after cessation of therapy, especially if taken for a long time), tenderness of the mammary glands; Hyperglycemia, diabetes, polyuria.

From the urinary system: dysuria, urinary retention, edema, rarely - hematuria.

Other: often - asthenia, alopecia, body weight decrease or increase, decrease, libido; fever, chills, increased sweating, anemia, pelvic pain, dry skin, hirsutism, allergic reactions, "flushes" of blood to the face.

Overdose:

Treatment: symptomatic, there is no specific antidote. Dialysis is ineffective, because bicalutamide strongly binds to proteins and is not excreted in the urine unchanged. The general supportive therapy and control over the vital functions of the body are shown.

Interaction:

Enhances the effects of anticoagulants of indirect action.

Increases AUC of midazolam by 80%.

Incompatible with terfenadine, astemizole, cisapride.

Increases the risk of adverse effects with concomitant administration with cyclosporine, BCCC, drugs that depress microsomal oxidation of drugs (including cimetidine, ketoconazole).

Special instructions:

When co-administered with cyclosporine after starting the use or the elimination of bicalutamide, careful monitoring of the plasma cyclosporin concentration and the patient's condition is recommended.

Research in vitro showed that bicalutamide can displace warfarin from binding sites with protein (regular prothrombin time monitoring).

Elimination of bicalutamide from the body can be slowed down in patients with severe impairment of liver function, which can lead to its cumulation. It is advisable to periodically evaluate liver function (most liver function changes occur during the first 6 months of treatment). Stop treatment if there are clinical symptoms and / or increase functional tests by more than 2 times. In case of development of severe liver damage, it is necessary to stop taking.

In patients with progression of the disease against a background of increased levels prostate specific antigen should consider the termination of treatment.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 50 mg.

Packaging:

For 10 or 14 tablets in a PVC / aluminum foil blister.

By 2, 3, 4, 5 or 6 blisters of 10 tablets and 2 or 4 blisters of 14 tablets are placed in cardboard pack together with instructions for use.

Storage conditions:

At a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

The drug should not be used after the expiry date indicated on the packaging.

Terms of leave from pharmacies:On prescription

Registration number:LP-000625

Date of registration:21.09.2011

Date of cancellation:2016-09-21

The owner of the registration certificate:Fresenius Kabi Deutschland GmbHFresenius Kabi Deutschland GmbH Germany

Manufacturer: & nbsp

FRESENIUS KABI ONCOLOGY, Limited India

Representation: & nbspFRESENIUS KABI DEYCHLAND GmbH FRESENIUS KABI DEYCHLAND GmbH Germany

Information update date: & nbsp21.11.2015

Illustrated instructions

Instructions

Bicalutamide Cabi (Bicalutamid-Kabi)