Lysomustine (Lisomustine)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbsplyophilizate for solution for infusion
Composition:

Per 1 bottle:

active substance: Lysomustine-100 mg;

Excipients: dextran M.M. 60 000 ± 10 000 - 100 mg, acid citric monohydrate - 5 mg.
Description:

A porous mass of white with a yellowish tinge.

Pharmacotherapeutic group:An antitumour agent, an alkylating compound
ATX: & nbsp
  • Analogs of pyrimidine
    • Pharmacodynamics:

    Being an antimetabolite of amino acid - lysine, inhibits the synthesis of DNA in tumor cells. In experimental studies, it is effective against tumors with drug resistance to such drugs of this class as nimustine and carmustine.

    Pharmacokinetics:

    The concentration of Lysomustine in the blood depends on the dose administered, the half-life period is an average of 30 minutes. It is quickly distributed in tissues and body fluids (the volume of distribution is 0.35 l / kg), penetrates the blood-brain barrier. About 3% unchanged drug is excreted in the first 2 hours with urine. With repeated administration, there was a slowdown in the elimination of the drug from the blood. A drug undergoes a rapid metabolic transformation in the liver with an amide bond break and formation of lysine- and urea-containing parts of the molecule. The unmodified molecule of Lysomustine has a weakly expressed ability to bind to proteins, in distinctione from the metabolites formed in the plasma, mainly in the form of complexes.

    Indications:

    Melanoma of the skin, lung cancer.

    Contraindications:

    - The general severe condition of the patient, leukopenia below 3000 and thrombocytopenia below 120,000 / μL and severe anemia;

    - an increase in bilirubin and / or transaminase activity is 2 times higher than normal;

    - Stomach ulcer and duodenal ulcer in the stage of exacerbation.

    - severe cardiovascular and neurological diseases;

    - severe violations of the liver and kidneys;

    - period of pregnancy and lactation;

    - Hypersensitivity to the drug.

    The drug is not used in persons younger than 18 years.

    Carefully:

    The presence in the patient's history of an indication of allergic reactions, intolerance to drugs, serums, vaccines, as well as intravenous infusions of protein preparations, plasma substitutes, including dextran preparations.

    Use of the drug in weakened and depleted patients.

    Dosing and Administration:

    The drug is used only as a monotherapy in a dose of 500-550 mg / m2 once intravenously drip for 30-40 minutes.

    A single dose of the drug should not exceed 1 g.

    Repeated courses are carried out with an interval of 4-6 weeks in the absence of any manifestations of toxicity.

    Dose-limiting toxicity - thrombocytopenia.

    The solution is prepared immediately before the administration of the drug by preliminary dissolving the contents of each vial (100 mg of the preparation) in 20 ml of a 5% dextrose solution, followed by the addition of 5% dextrose to 200 ml (to a concentration of 5 mg / ml).

    When administered, the drug should be protected from exposure to light.

    To prevent a hypersensitivity reaction (vascular collapse) 30 minutes prior to the administration of Lisomustine, a premedication should be performed: dexamethasone 20 mg intramuscularly, diphenhydramine 1 mg intramuscularly.

    Side effects:

    From the hematopoiesis: leukopenia, thrombocytopenia, erythrocytopenia, reduction of hemoglobin.

    From the digestive system: nausea, vomiting, stomatitis, anorexia.

    From the nervous system: headache, inhibition, lethargy, weakness, drowsiness.

    From the skin and skin appendages: alopecia.

    Laboratory indicators: an increase in the activity of "hepatic" samples, proteinuria.

    Other: hemorrhagic syndrome, allergic reactions.

    Side effects of Lysomustine treatment are reversible and do not limit the conduct of chemotherapy.

    Overdose:

    Symptoms: repeated or unceasing vomiting and / or diarrhea, marked inhibition of hematopoiesis.

    If the first signs of an overdose occur, Lisomustine should be discontinued until the symptoms disappear.

    Treatment: symptomatic. The antidote is not known.
    Interaction:The drug in combination with other cytostatics has not been studied.
    Special instructions:

    It is used strictly according to the prescription of a doctor who has experience of antitumor chemotherapy, in a hospital.

    Treatment should be carried out under the control of the content of leukocytes, platelets, erythrocytes in peripheral blood. It should be borne in mind that hematological toxicity may occur 1-3 weeks after the end of treatment.

    During treatment Lizomustinom necessary to carry out systematic monitoring of peripheral blood picture 1 once a week and consider the possibility of delayed thrombocytopenia.

    At the end of the administration of the drug, liver and kidney function control is necessary.

    Lysomustine solution should be administered immediately after its preparation and not mixed with other solutions and medications.

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

    Given that when using Lysomustine, patients may experience drowsiness, drowsiness, lethargy and weakness, it is better to abstain for the time of taking the drug from the management of vehicles and mechanisms and the performance of other works that require concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Lyophilizate for solution for infusion, 100 mg.
    Packaging:

    For 100 mg of active substance in neutral glass bottles with a capacity of 20 ml, corked with rubber stopper under running in aluminum caps.

    10 bottles of the drug with instructions for use are placed in a cardboard box.
    Storage conditions:At a temperature of no higher than minus 10 ° C (freezer compartment conditions), in a dry, protected from light place.

    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:LS-002311
    Date of registration:21.05.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:GLEAS FIRM, LLC GLEAS FIRM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp24.02.2018
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