Active substanceDacarbazineDacarbazine
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  • Dosage form: & nbsp

    lyophilizate for the preparation of a solution for intravenous administration

    Composition:
    1 bottle contains:
    Active substance:
    Dacarbazine 100mg 200mg
    Excipients:

    citric acidbush

    100 mg

    200 mg

    mannitol

    50 mg

    100 mg

    Description:The porous mass is from white to white with a yellowish or pinkish hue of color.
    Pharmacotherapeutic group:An antitumour agent, an alkylating compound
    ATX: & nbsp

    L.01.A.X   Other alkylating preparations

    L.01.A.X.04   Dacarbazine

    Pharmacodynamics:

    Dakarbazine is an antitumor agent of the chemical composition of the chemical composition that is 5- (3,3-dimethyl-1-triazeno) -imidazole-4-carboxamide.

    The drug becomes active after metabolism in the liver. It is assumed that there are three ways of the mechanism of action of dacarbazine: alkylation due to carbonium ions, oppression of purine bases and interaction with SH groups. The preparation is phase-specific.
    Pharmacokinetics:

    The maximum concentration in the plasma is usually achieved immediately immediately after intravenous administration of the drug.The connection with plasma proteins is very low (about 5%). Penetrates through the blood-brain barrier in small amounts. There is no evidence of its penetration into the placenta and breast milk.

    The drug is withdrawn from the body biphasic with an initial half-life of about 20 minutes and the final - about 5 hours, with violations of the liver or kidneys, these indicators are approximately 55 minutes and 7 hours respectively. The drug is subjected to dimethylation with hepatic microsomal enzymes with the formation of carbon dioxide, which is excreted with exhaled air and aminoimidazolecarboxamide, which is excreted in the urine. 40% of the drug is excreted by the kidneys unchanged, mainly due to glomerular filtration.
    Indications:

    - Melanoma

    - Lymphogranulomatosis

    - Soft tissue sarcoma (excluding the Kalosha sarcoma)

    There have been reports of the effectiveness of dacarbazine in combination with other cytostatics in the treatment of osteogenic sarcoma, uterine sarcoma, pleural and peritoneal mesothelioma, small cell lung cancer, thyroid cancer, carcinoid, pheochromocytoma, insulinoma, neuroblastoma and gliomas.
    Contraindications:

    - Hypersensitivity to dacarbazine or any of the auxiliary components of the drug;

    - severe oppression of bone marrow hematopoiesis;

    - severe hepatic or renal insufficiency;

    - pregnancy and the period of breastfeeding.

    Carefully:With myelodispression (including on the background of concomitant radiation and chemotherapy), acute infectious diseases of the viral (including chicken pox, shingles), fungal or bacterial nature (risk of serious complications and generalization of the process), concomitant radiation therapy .
    Pregnancy and lactation:The use of dacarbazine during pregnancy and during breastfeeding is contraindicated.
    Dosing and Administration:

    When choosing the doses and the mode of administration of the drug in each individual case, one should use the data of the specialized literature.

    The drug is administered strictly intravenously. Doses up to 200 mg / m2 injected slowly for 1-2 minutes. Higher doses should be administered in the form of intravenous infusions for 15-30 minutes.

    Usually as a monotherapy dacarbazine used in a dose of 200-250 mg / m2 daily for 5 days.Repeated courses are held at intervals of 3 weeks.

    When combined with other cytostatics dacarbazine is administered in a dose of 100-150 mg / m2 4-5 consecutive days with an interval of 4 weeks or 375 mg / m2 every 15 days.

    Before administration, the drug is diluted with water for injection to reach a concentration of 10 mg / 1 ml. To obtain a solution for infusion, a freshly prepared solution is diluted in 200-300 ml with 0.9% sodium chloride solution or 5% dextrose solution.

    A solution of dacarbazine should be protected from light.

    Side effects:

    From the hematopoiesis: anemia, leukopenia, granulocytopenia, thrombocytopenia. Oppression of myelopoiesis is a limiting dose, a side effect. Leukocytopenia is usually observed on day 14, thrombocytopenia - on day 18 after the end of therapy and lasts an average of 1 week. Recovery of blood counts occurs by the 4th week.

    From the digestive system: nausea, vomiting, decreased appetite, stomatitis; rarely - diarrhea, increased activity of "liver" enzymes. Very rarely, a hepatonecrosis caused by occlusion of the intrahepatic veins, possibly with a lethal outcome (as a rule, this syndrome appeared during the 2nd course of treatment).Among his symptoms include fever, eosinophilia, abdominal pain, enlargement of the liver and shock, the severity of which rapidly builds up over several hours or days. From the nervous system: headache, visual impairment, confusion, marked drowsiness, convulsions, asthenic syndrome, paresthesia, facial hypodeses.

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

    Allergic reactions: skin rash, hyperemia of the facial skin, febrile syndrome, anaphylactic reactions.

    From the skin and skin appendages: rarely - alopecia, hyperpigmentation and skin photosensitization.

    Local reactions: soreness in the place of injection and along the vein. If the product gets under the skin - severe pain, necrosis of surrounding tissues.

    Other: influenza-like syndrome, attachment of secondary infections, thrombosis of hepatic veins, myalgia. With prolonged use, the risk of developing neoplasms increases.

    Overdose:

    Symptoms: increased oppression of bone marrow hematopoiesis and severity of dyspepsia.

    Treatment: a symptomatic, specific antidote is unknown.

    Interaction:

    Enhances the effect (incl.toxic) phenobarbital, azathioprine, 6-mercaptopurine, allopurinol.

    Inducers of microsomal liver enzymes (barbiturates, rifampicin, phenytoin) increase the toxic effect of dacarbazine.

    Dacarbazine can enhance the photosensitizing effect of methoxypsoralen. A solution of dacarbazine is chemically incompatible with heparin, hydrocortisone, Lcysteine ​​and sodium bicarbonate.

    Special instructions:

    Dakarbazine should be used under the supervision of a doctor who has experience with antitumor drugs.

    During the period of treatment and after it, careful monitoring of the picture of peripheral blood, liver function and its size is necessary.

    If there are violations of the function of the liver or kidneys, symptoms of hypersensitivity to the drug or thrombosis of hepatic veins, dacarbazine treatment should be stopped immediately.

    When the first signs of extravasation of dacarbazine (burning or soreness at the injection site), the introduction should be immediately stopped. The remaining dose should be injected into another vein.

    During treatment and within 6 months after it is necessary to apply reliable methods of contraception.

    During the treatment with dacarbazine, vaccination with vaccines containing live pathogens can not be performed.

    Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Lyophilizate for the preparation of a solution for intravenous administration 100 mg, 200 mg.
    Packaging:

    Lyophilizate for the preparation of a solution for intravenous administration in vials of colorless and light-protective glass by 100 mg or 200 mg. For 1 bottle with instructions for use in a cardboard bundle.

    By 5,10, 20 bottles with instructions for use in a pack with partitions or special cardboard sockets.

    For 25, 30, 36, 50 or 72 bottles with instructions for use, at the rate of 1 instruction for 10 bottles in a cardboard box (for hospitals).

    Storage conditions:

    List B. At a temperature of 2 to 8 ° C in a dry, protected from light and out of reach of children.

    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:P N000389 / 01
    Date of registration:28.02.2012 / 29.07.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp17.03.2017
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