Blenamax (Blenamax)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Active substanceBleomycinBleomycin
Similar drugsTo uncover
  • Blenamax
    lyophilizate for injections 
    Teva Pharmaceutical Enterprises Co., Ltd.     Israel
  • Bleomycetin hydrochloride
    lyophilizate for injections 
    SPbNIIVS FMBA, FSUE     Russia
  • Bleomycin-RONTS®
    lyophilizate for injections 
    RNTS named after N.N. Blokhin RAMS     Russia
  • Bleocin
    lyophilizate for injections 
    Nippon Kayaku Co., Ltd.     Japan
  • Vero-Bleomycin
    lyophilizate for injections 
    LENS-PHARM, LLC     Russia
    • Dosage form: & nbsplyophilizate for solution for injection
    Composition:

    One bottle contains:

    active substance: bleomycin 15 ED (as bleomycin sulfate);

    excipients: no

    Description:

    White or white with a yellowish tint powder or porous mass.

    Pharmacotherapeutic group:Antitumor agent - antibiotic
    ATX: & nbsp

    L.01.D.C.01   Bleomycin

    Pharmacodynamics:

    Bleomycin refers to antitumor antibiotics and is a mixture of structurally related water-soluble salts of glycopeptide antibiotics. The mechanism of the action of bleomycin is based on fragmentation of DNA, destruction of its spiral structure, which leads to inhibition of cell division. Less bleomycin affects RNA and protein synthesis.

    Has a selective effect against tumors of epidermal origin due to its ability to accumulate in skin cells.The selectivity of the action is explained by the low content of bleomycin-hydrolase inactivating enzyme in tumor cells.

    Unlike most other cytotoxic drugs, bleomycin is less toxic to the bone marrow, does not have immunosuppressive action, is not a neurotoxic and cardiotoxic drug.

    With intrapleural administration, it exhibits sclerosing properties.
    Pharmacokinetics:

    After intramuscular injection of the drug at a dose of 15 U / m2 the maximum concentration in the plasma is reached after 30 minutes.

    Bleomycin is rapidly distributed in the tissues of the body with the greatest concentration in the skin, lungs, kidneys, peritoneum and lymph nodes. In intrapureral instillation systemic absorption is 45%. Does not penetrate the blood-brain barrier. Link with blood plasma proteins is insignificant.

    Until now, the mechanism of biotransformation of bleomycin is unknown.

    Inactivation of the drug is carried out with the participation of the enzyme bleomitsin-hydrolase, mainly in blood plasma, liver and other organs, and to a lesser extent, in the skin and lungs.

    The half-life of bleomycin is about 2-3 hours.Approximately 60-70% of the administered amount of bleomycin in normal renal function is excreted unchanged in urine, apparently due to glomerular filtration. The concentration of the drug in plasma sharply increases in the case of the usual dose of bleomycin for patients with impaired renal function. In the case of creatinine clearance <35 ml / min, only 20% of the drug is excreted in the urine.

    Indications:

    Bleomycin is commonly used in combination with other cytostatics and / or radiation therapy to treat squamous cell carcinomas of the head and neck, esophagus, lung, cervix, vulva, skin cancer, penile cancer, germ cell tumors, kidney cancer, Hodgkin's disease and non-Hodgkin's lymphomas including lymphosarcoma and reticulosarcoma), malignant testicular tumors, malignant pleurisy (as a sclerosing agent).

    Contraindications:

    - Pincreased sensitivity to bleomycin;

    - acute pulmonary infections;

    - severe pulmonary dysfunction;

    - severe renal dysfunction;

    - ataxia telangiectatic (Louis-Bar syndrome);

    - pregnancy and lactation.

    Carefully:

    With concomitant or previous radiation therapy, acute infectious or viral diseases, impaired renal function, in childhood.

    Dosing and Administration:

    Blenamax can be administered intramuscularly, intravenously, subcutaneously or intrapleural.

    In each individual case, when choosing a dose and the mode of administration of Blenamax, one should use the literature data. Doses are calculated per unit of total surface area of ​​the body.

    Recommended doses:

    - intramuscularly or subcutaneously (in 1-5 ml of water for injection or 0.9% solution of sodium chloride, alternating injection sites) at a dose of 10-20 units / m2 once or twice a week;

    - intravenously struino (in 5-10 ml of 0.9% solution of sodium chloride or water for injection for 5-10 minutes) at a dose of 10-20 units / m2 once or twice a week;

    - intravenously in the form of a 6-24 hour infusion (in 200-1000 ml of 0.9% solution of sodium chloride) at a dose of 10-20 units / m2 for 4-7 days every 3-4 weeks;

    - Intrapleural (in 50-100 ml of 0.9% solution of sodium chloride after evacuation of the maximum possible amount of exudate) 60 units once.

    Because of the increased risk of developing an anaphylactic reaction in patients with malignant lymphomas, the initial dose may be reduced (for example, up to 2-3 U / m2). In the absence of an acute reaction to the administration of the drug, further therapy can be continued in the usual dose.

    The total total dose of Blenamax should not exceed 400 units and further continuation of the drug administration can be performed only after evaluation of lung function.When the drug is used in combination with other antitumor drugs, pulmonary toxicity may occur with smaller total doses of Blenamax.

    Application in the elderly:

    In elderly patients, the dose of the drug is determined as follows:

    Age (years)

    Total dose

    Weekly dose

    80 and over

    100 units

    15 units

    70-79

    150-200 IU

    30 units

    60-69

    200-300 IU

    30-60 units

    under 60

    400 units

    30-60 units

    Children:

    The introduction of Blenamax to children can be carried out only in special cases. The dose of the drug is determined from the calculation per unit of the total surface area of ​​the body.

    In patients with impaired renal function:

    In patients with impaired renal function, the dose of Blenamax is calculated as follows:

    - with a serum creatinine level of 130-180 μmol / L, the dose of the drug should be reduced by 50%;

    - with a serum creatinine level of more than 180 μmol / L, the drug is delayed until the levels of creatinine are normalized.

    Side effects:

    From the hematopoiesis: bleomycin practically does not depress bone marrow hematopoiesis. Rarely, there is little reversible thrombocytopenia.

    From the immune system: urticaria, anaphylactic reactions (lowering blood pressure, confusion, fever, chills, wheezing).Similar reactions were observed in approximately 1% of patients with malignant lymphomas, usually after the first or second injection of the drug.

    From the nervous system: headache, dizziness, paresthesia and hyperesthesia.

    From the cardiovascular system: episodes of acute dystonia in patients with lymphogranulomatosis, treated with high doses of bleomycin. Reduction of blood pressure (with intravenous administration). Rarely as a result of vascular disorders, cerebral arteritis, thrombotic microangiopathy, myocardial infarction, stroke, Raynaud's syndrome can be observed.

    On the part of the respiratory system: in 2-10% of cases, interstitial pneumonia (dyspnea, cough, wheezing in the lungs), often with outcome in pulmonary fibrosis or even fatal (1%).

    From the skin and skin appendages: dyskeratosis in the region of the elbows or knee joints, palms, fingers, buttocks, scapula; hyperemia, rash, striae, hyperpigmentation, skin itching, deformation and fragility of nails, hyperesthesia of the skin and distal (nail) phalanges, hyperemia of fingertips, alopecia. Skin disorders occur in about 50% of cases, usually after reaching a total dose of bleomycin - 150-200 units.In rare cases, they have a pronounced character and usually disappear after the completion of the course of treatment. There have been individual reports of the development of scleroderma in persons who received bleomycin.

    From the gastrointestinal tract: anorexia, nausea, vomiting, diarrhea, stomatitis, weight loss (with prolonged use).

    Local reactions: local thrombophlebitis, venous occlusions develop, as a rule, with intravenous administration of the drug. When injected into the pleural cavity, pain may occur in the injection site.

    Other: pleuropericarditis, increased fatigue, pain in the area of ​​tumor formations; changes in indicators of functional liver and kidney tests, pain in bones and joints.

    Fever (fever with chills) is observed in 20-60% of patients, usually 2-6 hours after the first injection of bleomycin. The frequency of fever in subsequent bleomycin injections is significantly reduced.

    Overdose:

    Direct reactions in case of an overdose are lowering of arterial pressure, fever, rapid pulse and general symptoms of shock. There is no specific antidote.

    Treatment symptomatic.With complications from the bronchopulmonary system, patients should be treated with glucocorticosteroids and broad-spectrum antibiotics.

    Interaction:

    Bleomycin decreases the bioavailability of digoxin and affects its effectiveness.

    With the combination of bleomycin and vinaalkaloids, Raynaud's syndrome may develop. Bleomycin reduces the level of phenytoin in the blood plasma.

    Combined use of bleomycin with nephrotoxic drugs (cisplatin) leads to a decrease in clearance of bleomycin. The combined use of cisplatin and bleomycin can lead to severe and even fatal pulmonary toxicity.

    With simultaneous administration of bleomycin with carmustine, mitomycin, cyclophosphamide and methotrexate, filgrastim and other cytokines, as well as with prior or currently conducted radiation therapy on the chest area, the risk of pulmonary toxicity increases.

    Patients treated with bleomycin have an increased risk of pulmonary toxicity when using oxygen. the process of anesthesia during surgical interventions. Such patients are recommended to reduce the concentration of oxygen in the process and after a surgical operation.

    Vaccination with live vaccines against bleomycin may lead to an intensification of the replication of the vaccine virus, an increase in its adverse / adverse effects and / or a decrease in the production of antibodies in the patient's body in response to the introduction of the vaccine.

    Special instructions:

    Treatment should be carried out under the supervision of a doctor who has experience of antitumor therapy.

    Patients undergoing bleomycin treatment should regularly perform an external respiratory function, as well as a chest X-ray.

    When coughing, dyspnea, wheezing, or radiographic signs of interstitial pneumonia occur, bleomycin should be discontinued until the toxic effects of the drug are eliminated. If necessary, antibiotics and glucocorticosteroids should be prescribed.

    The toxicity of bleomycin increases when the cumulative dose of 400 U (225 U / m2), however, the toxic dose can be significantly lower in elderly patients, in patients with renal dysfunction, with lung diseases in the history, in the case of previously conducted lung irradiation, as well as smoking.

    Sensitivity to bleomycin is increased in elderly patients.

    To stop fever, you can take antipyretics.

    The concentration of bleomycin in the blood plasma increases sharply when the drug is administered to patients with impaired renal function.

    Due to the potential teratogenic effect of bleomycin against male and female reproductive cells, reliable contraceptive methods should be used during bleomycin treatment and within three months of completion of treatment.

    The usual precautions should be observed during the preparation of the drug solution and its administration. If the product gets on the skin or mucous membrane, these places should be washed with a large amount of water.

    Form release / dosage:Lyophilizate for solution for injection, 15 units.
    Packaging:

    For 15 units of the drug in a bottle of colorless glass USP type I (10 R), with a capacity of 12.5 ml ± 1 ml, with a plug of bottled rubber, an aluminum cap and a colored protective cap-insert made of polypropylene. The glass bottle is covered with a transparent polyethylene film.

    1 bottle with instructions for use in a cardboard box.

    Storage conditions:

    At a temperature of 2 to 8 ° C, in a dark place.

    Keep out of the reach of children.

    After dilution, the drug is stable in a solution of 0.9% sodium chloride for 24 hours at a temperature of 2 to 8 ° C or 12 hours at a temperature of (15-25 ° C), provided that the sterility is maintained.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012754 / 01
    Date of registration:20.05.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp18.02.2017
    Illustrated instructions
      Instructions
      Up