Vinblastine (Vinblastinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

Antineoplastic agents

Included in the formulation
  • Vinblastine-LENS®
    lyophilizate in / in 
    LENS-PHARM, LLC     Russia
  • Vinblastine Richter
    lyophilizate in / in 
    GEDEON RICHTER, OJSC     Hungary
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    L.01.C.A.01   Vinblastine

    L.01.C.A   Vinca alkaloids and its analogues

    Pharmacodynamics:

    Antitumor agent. The mechanism of action is associated with the blockade of tubulin and the arrest of cell division in the metaphase.

    Pharmacokinetics:

    It penetrates to an insignificant degree through blood-brain barrier. Binding to plasma proteins is 75%. Biotransformiruetsya in the liver with the formation of active metabolites. It is mainly excreted with bile, in part - kidneys. After intravenous The introduction is quickly distributed into tissues. Binding to proteins is high (75%). Does not penetrate blood-brain barrier. Metabolised in the liver. It is excreted from the body in three phases with half-lives (average values) of 5 minutes, 2 hours and 30 hours, respectively.

    Indications:

    Hodgkin's disease, lymphocytic lymphoma, lymphosarcoma, reticulosarcoma, non-Hodgkin's lymphoma, histiocytic lymphoma, chronic leukemia, mycosis fungoides, germ cell tumor testicular, germ cell tumor of the ovary, testicular tumor, multiple myeloma, horionepitelioma, Kaposi's sarcoma, Letterer-Siva disease, neuroblastoma, kidney cancer, cancer of the bladder, lung cancer.

    ICD-10

    II.C64-C68.C67   Malignant neoplasm of bladder

    II.C60-C63.C62   Malignant neoplasm of testis

    II.C50.C50   Malignant neoplasm of breast

    II.C30-C39.C34   Malignant neoplasm of bronchi and lungs

    II.C51-C58.C58   Malignant neoplasm of placenta

    II.C64-C68.C64   Malignant neoplasm of kidney, except for renal pelvis

    II.C45-C49.C46   Kaposi's Sarcoma

    II.C81-C96.C81   Hodgkin's disease [lymphogranulomatosis]

    II.C81-C96.C82.9   Follicular non-Hodgkin's lymphoma, unspecified

    II.C81-C96.C83   Diffuse non-Hodgkin's lymphoma

    II.C81-C96.C84.0   Mushroom mycosis

    II.C81-C96.C96.0   Disease Letterter-Sieve (non-lipid reticuloendotheliosis, reticulosis)

    Contraindications:

    Severe leukopenia, pregnancy, hypersensitivity to vinblastine.

    Carefully:

    Use with caution vinblastine in patients with chickenpox (including the recently transferred or after contact with the diseased), herpes zoster, other acute infectious diseases, gout, nephrolithiasis (including in the anamnesis). In patients with impaired liver function, the risk of toxic effects of vinblastine is increased.

    With caution apply to the background of treatment with drugs that depress the activity of the isoenzyme CYP3A.

    Pregnancy and lactation:

    FDA Action Category - D.

    Vinblastine is contraindicated in pregnancy. If necessary, use during lactation should stop breastfeeding.

    When used in women of childbearing age, it is recommended to use reliable methods of contraception.

    AT experimental research established teratogenic effect of vinblastine.

    Dosing and Administration:

    Intravenously, spray or drip, once a week. Apply a freshly prepared solution. The dose is determined individually, taking into account the clinical picture, the patient's condition and the number of leukocytes in the peripheral blood. The initial dose for adults is 0.025-0.1 mg / kg (3.7 mg / m2), daily monitor the number of leukocytes in the peripheral blood: if their number does not fall below 2000-3000 cells / μl within a week, re-inject 0.15 mg / kg. In the future (with insufficient therapeutic effect and lack of leukopenia), the dose can be increased to 0.2 mg / kg. After achieving a visible regression of tumor growth, they pass to a maintenance dose of 0.15 mg / kg every 7-14 days.

    Another treatment regimen is possible: the initial dose is 0.025-0.1 mg / kg,Further (with daily control of the number of leukocytes in peripheral blood) is administered every day at a dose of 2.5 mg and gradually increases the dose to 5 mg (not more). The therapeutic effect with this scheme of administration is achieved within 2-3 days. After normalizing the number of white blood cells, treatment can be continued using a smaller dose.

    Children are prescribed in an initial dose of 0, 075 mg / kg (2.5 mg / m2) Once a week, re-injected after the normalization of the number of leukocytes in peripheral blood (usually on the 3-7th day); if after the first injection the number of leukocytes did not decrease, the dose is increased.

    Side effects:

    From the side of the central nervous system and the peripheral nervous system: neuropathy, neuritis of the peripheral nerves, headache, depression, convulsions.

    On the part of the hematopoiesis system: leukopenia, granulocytopenia, thrombocytopenia, anemia.

    From the digestive system: anorexia, nausea, vomiting, abdominal pain, paralytic intestinal obstruction, constipation, diarrhea, ulcerative stomatitis, hemorrhagic enterocolitis.

    From the side of the cardiovascular system: increased blood pressure, the development of myocardial infarction, cerebral circulatory disorders, increased symptoms of Raynaud's disease.

    From the respiratory system: acute respiratory failure, bronchospasm.

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

    Other: alopecia, pain in the bones.

    Overdose:

    Symptoms: leukopenia, peripheral nerve damage, convulsions, coma.

    Treatment: symptomatic therapy, monitoring of vital functions, careful monitoring of the picture of peripheral blood, if necessary - blood transfusion. There is no specific antidote. Hemodialysis is ineffective.

    Interaction:

    When used simultaneously with inhibitors of the activity of the isoenzyme CYP3A, an earlier appearance and / or aggravation of the severity of the side effects of vinblastine is possible.

    With simultaneous use with vinblastine, a decrease in the concentration of phenytoin in the blood plasma and a decrease in its anticonvulsant activity, apparently due to a decrease in absorption, an increase in the metabolic rate and elimination of phenytoin.

    With the simultaneous use of vinblastine in high doses with interferon alpha-n1, severe myelodepression is possible.

    Special instructions:

    The maximum depression of hematopoiesis (primarily the reduction in the number of leukocytes in the peripheral blood) is achieved 5-10 days after the termination of vinblastine.Normalization of the number of leukocytes in peripheral blood is observed after 7-14 days. The development of thrombocytopenia (less than 200 000 per μL) is most likely in patients who received previous antitumor or radiation therapy. Normalization of the number of platelets is noted, as a rule, a few days after the abolition of vinblastine.

    The risk of developing leukopenia with vinblastine is increased in patients with cachexia and ulcerative lesions of the skin, so patients with the above conditions do not recommend it. In patients with metastases in the bone marrow, a marked decrease in the number of leukocytes and platelets was observed after the administration of vinblastine in medium doses. In these cases, further use of vinblastine is not indicated.

    In the process of therapy, it is necessary to monitor the activity of liver transaminases and lactate dehydrogenase, the level of bilirubin and the concentration of uric acid in the blood plasma.

    During the period of treatment, vaccination of patients and their families is not recommended.

    Intraoblositive administration of vinblastine can lead to death. In case of accidental ingestion, severe inflammation may occur.

    Instructions
    Up