Vero-Bleomycin (Vero-Bleomycin)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceBleomycinBleomycin
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  • Vero-Bleomycin
    lyophilizate for injections 
    LENS-PHARM, LLC     Russia
    • Dosage form: & nbsplyophilizate for solution for injection
    Composition:

    1 bottle contains:

    active substance: bleomycetin hydrochloride (in terms of bleomycin) 5 mg or 15 mg;

    Excipients: mannitol (mannitol).

    Description:

    A porous mass of white or yellowish color. Hygroscopic.

    Pharmacotherapeutic group:Antitumor agent - antibiotic
    ATX: & nbsp

    L.01.D.C.01   Bleomycin

    Pharmacodynamics:

    Antitumor antibiotic obtained from culture Streptovertifromillium griseocameum var. Bleomycini. It is a mixture of structurally related water-soluble salts of glycopeptide antibiotics, the main component of which is pure bleomycin A5. The mechanism of action of bleomycin is based on the fragmentation of DNA molecules in G1 phase and at the beginning S-phase of the cell cycle, 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. With intrapleural administration, it exhibits sclerosing properties.

    Unlike most other cytotoxic drugs, bleomycin is low in toxicity to the bone marrow, does not have a significant immunosuppressive effect, is not a neurotoxic and cardiotoxic drug.

    Pharmacokinetics:

    After parenteral administration, it accumulates in the tumor cells of the skin and lungs, to a lesser extent - the kidneys, peritoneum, lymph nodes, and little - in the hemopoietic tissue.

    The mechanism of metabolism is unknown, probably it is carried out by cleavage in tissues with the participation of the bleomycin-hydrolase enzyme. The intensity of metabolism in tissues is variable, which can determine the toxic effect and antitumor effect of bleomycin. The activity of enzymes is high in the liver, kidneys, in the bone marrow and lymph nodes, but low in the skin and lungs. The dynamics of concentration in the blood is described by a bi-exponential curve. Half-life (T1/2) alpha - 25 min, T1/2 Beta - 4 hours.

    With intrapleural or intraperitoneal injection, systemic absorption is 45%. The connection with plasma proteins is negligible. With the clearance of creatinine (CC) more than 35 ml / min T1/2 is 115 min, with a QC of less than 35 ml / min T1/2 increases exponentially as the QC decreases. It is excreted by the kidneys, 60-70% unchanged (in patients with normal renal function); with moderate chronic renal failure - 20%. Total clearance - 50 ml / min / m2. When dialysis is probably not output.

    Indications:

    Bleomycin is used either as monotherapy or in combination with other cytostatics and / or radiation therapy to treat squamous cell forms of skin, head and neck cancer, esophagus; thyroid cancer; lymphogranulomatosis, non-Hodgkin's lymphomas; reticulosarcoma, Kaloshi's sarcoma in AIDS, osteogenic sarcoma; melanoma; germinogenous testicular and ovarian tumors; penile cancer, vulvar cancer, cervical cancer; metastatic pleurisy, ascites against a background of malignant tumors (treatment and prevention as a sclerosing agent).

    Contraindications:

    Hypersensitivity to the components of the drug, severe renal failure,respiratory failure (pulmonary fibrosis, chronic interstitial pneumonia), decompensated heart failure, pregnancy, the period of breastfeeding.

    Carefully:

    Inhibition of bone marrow hematopoiesis, renal and / or hepatic insufficiency, previous or concomitant radiotherapy to the thoracic region, varicocele, elderly age, childhood, acute infectious diseases of viral, fungal or bacterial nature (including chicken pox, shingles) .

    Dosing and Administration:

    Intravenous, intramuscular, in the cavity.

    In each individual case, when choosing a dose and mode of administration, you should use the literature data.

    Usually the drug is administered:

    - intramuscularly (in 3-5 ml of a 0.9% solution of sodium chloride or water for injections, alternating injection sites) or intravenously slowly (in 15-20 ml 0.9% solution of sodium chloride or water for injection for 5-10 minutes) at a dose of B-10 mg (4-5 mg / m2) three times a week or 15-20 mg (8-10 mg / m2) two times a week;

    - in the form of intravenous infusion (in 200-1000 ml of 0.9% solution of sodium chloride) for 6-24 hours at a dose of 10-15 mg / m2 daily for 4-7 days with a repetition of the course every 3-4 weeks;

    - intrapleural or abdominal cavity 50-60 mg in 40 ml of 0.9% sodium chloride solution after evacuation of the maximum possible amount of exudate.

    Because of the risk of developing an anaphylactic reaction, the initial dose, especially for patients with lymphoma, can be reduced (for example, to 2-3 mg / m2). If the acute reaction does not develop, then the drug can be applied in the usual dose.

    The total total dose should not exceed 250-300 mg. Further introduction of the drug can be carried out with great care and only after determining the function of the lungs.

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

    Age (years)

    Total dose

    Weekly dose

    80 and over

    65 mg

    10 mg

    70-79

    100-140 mg

    20 mg

    60-69

    140-200 mg

    30-40 mg

    less than 60

    250-300 mg

    30-40 mg

    The introduction of bleomycin to children can be carried out only in special cases, the determination of the dose of the drug should be made from the calculation of the surface of the body.

    When carrying out radiation therapy, the dose of bleomycin should be reduced, since irradiated tissues are more sensitive to the drug. Correction of the dose of the drug should be carried out and if it is used in combination with other chemotherapeutic drugs.

    In patients with impaired renal function the dose of bleomycin varies as follows: at 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 respiratory system: interstitial pneumonia, pulmonary fibrosis, pleurisy with pain syndrome, cough, dyspnea.

    From the nervous system: headache, dizziness.

    From the digestive system: decreased appetite, nausea, vomiting, diarrhea, weight loss (with prolonged use); abnormal liver function.

    From the urinary system: impaired renal function.

    From the skin and skin appendages: hyperkeratosis, peeling, hyperemia, hyperpigmentation and itching of the skin, striae, deformation and fragility of nails, hyperesthesia of the skin and distal (nail) phalanges, skin hyperemia of the fingertips, sclerodermal-like skin changes, stomatitis, alopecia.

    Allergic reactions: urticaria, anaphylactoid reactions, idiosyncrasy (lowering of arterial pressure, confusion, fainting, fever, chills, stridorous breathing).

    On the part of the reproductive system: azoospermia, amenorrhea.

    Local reactions: phlebitis and thrombosis (when the speed of intravenous injection is exceeded); intrapleural injection - local pain.

    Other: hyperthermia (2 hours after administration, with a maximum after 4-8 hours); bleeding due to rapid disintegration of the tumor; cardiovascular disorders (including cerebral arteritis, stroke, myocardial infarction, thrombotic microangiopathy, Raynaud's syndrome); pain in the area of ​​tumor lesions; a feeling of general malaise; rarely leukopenia; conjunctivitis, vulvitis and other manifestations from the mucous membranes (usually 2-5 weeks after the start of therapy after reaching total doses of 150-200 mg).

    Overdose:

    Symptoms: lowering blood pressure, fever, rapid heart rate and general shock symptoms.

    Treatment: symptomatic. With complications from the bronchopulmonary system, glucocorticosteroids and broad-spectrum antibiotics are prescribed.

    Interaction:

    With the simultaneous administration of bleomycin with carmustine, mitomycin, cyclophosphamide and methotrexate, as well as with the use of oxygen (especially in surgical interventions) and other agents that have a toxic effect on the lungs (smoking), the risk of pulmonary toxicity increases.

    With the combined use of bleomycin and vinaalkaloids, the risk of vascular disorders increases.

    Myelotoxic drugs and radiation therapy increase the incidence of side effects.

    Special instructions:

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

    For early detection of side effects during the treatment period, it is necessary to conduct: measurement of body temperature every 3 hours after drug administration, examination of the skin and visible mucous membranes at least 2 times a week, auscultation of the lungs, lung radiography once a month, a blood test and urine at least once a week.

    Newborns, premature babies and young children can be appointed only for life indications, under constant supervision.

    Sensitivity to bleomycin is increased in elderly patients.

    Great care requires the use of the drug after radiotherapy (especially in the chest, head and neck).

    With ulcerative stomatitis and allergic rash treatment is stopped; when suspected of pneumonia, treatment is immediately stopped and glucocorticosteroids administered under the cover of antibiotics.

    When surgical interventions are used with caution, oxygen; in the operating room, the oxygen content in the air is not more than 25%.

    Women of reproductive age and men during bleomycin treatment and within three months after it should use reliable methods of contraception.

    Avoid the introduction of a solution when the color changes and large particles are present. For the introduction use freshly prepared solutions.

    Care should be taken when preparing the solution and when it is injected; If the product gets on the skin or mucous membranes, they should be washed with plenty of water.

    Form release / dosage:Liofilizate for the preparation of solution for injection, 5 mg and 15 mg.
    Packaging:

    5 mg and 15 mg in vials.

    For 1, 5 or 10 bottles together with the instructions for use in a pack of cardboard with partitions or special cardboard sockets.

    For 25, 35 or 50 bottles with instructions for use, based on one instruction for ten bottles, in a box of cardboard (for hospitals).

    Storage conditions:

    In a dry, dark place at a temperature of no higher than 10 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-008999/09
    Date of registration:09.11.2009 / 29.07.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:LENS-PHARM, LLC LENS-PHARM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp30.01.2017
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