Clinical and pharmacological group: & nbsp

Alkylating agents

Included in the formulation
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  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

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    ONLS

    АТХ:

    L.01.A.B.01   Busulfan

    Pharmacodynamics:The exact mechanism of action is unknown, alkylation and chain binding deoxyribonucleic acid. Has a more selective cytostatic effect on myeloid cells than derivatives of nitrogenous mustard gas and folic acid antagonists. In relatively low doses selectively inhibits granulocytopoiesis.
    Pharmacokinetics:Completely absorbed from the gastrointestinal tract. It is found in the blood after 0.5-2 hours after ingestion. The distribution is uniform (including in the cerebrospinal fluid). Five minutes after intravenous administration, 95% of the drug comes from the bloodstream. The connection with plasma proteins is 32% (low), irreversible, mainly with albumin. Biotransformation in the liver by conjugation with glutathione (spontaneous and catalyzed by glutathione-S-transferase) and subsequent oxidation. Half-life - 2,5 hours. Elimination by the kidneys (30% within 48 hours, mainly in the form of metabolites); sulfur-containing decomposition products (mainly methanesulfonic acid) are excreted more intensively by the kidneys than the degradation products of the alkylating part of the molecule.With repeated administration, it accumulates in the plasma. Hemodialysis is ineffective due to the low solubility of busulfan in water and the prolonged circulation of metabolites in the body.
    Indications:Chronic myelogenous leukemia, erythremia, true polycythemia, essential thrombocythemia, myelofibrosis, preparation for bone marrow transplantation.

    II.C81-C96.C92.1   Chronic myeloid leukemia

    II.C81-C96.C94.0   Acute erythremia and erythroleukemia

    II.C81-C96.C94.1   Chronic erythremia

    II.C81-C96.C94.5   Acute myelofibrosis

    II.D37-D48.D45   Polycythemia true

    II.D37-D48.D47.3   Essential (hemorrhagic) thrombocythemia

    XXI.Z40-Z54.Z51.4   Preparatory procedures for subsequent treatment, not elsewhere classified

    Contraindications:Hypersensitivitythrombocytopenia, pancytopenia, condition after radio or chemotherapy of tumors, blast crisis, pregnancy, lactation period, children's age (excluding application for vital signs).
    Carefully:Assessment of the risk / benefit ratio is necessary for the appointment in the following cases: chicken pox, shingles, gout, urolithiasis, craniocerebral trauma (incl.in the anamnesis), a convulsive syndrome (including in the anamnesis).
    Pregnancy and lactation:

    Recommendations Food and Drug Administration (US Food and Drug Administration) category D. Controlled studies on humans have not been conducted. Possible development of fetal side effects observed in adults. Cases of normal pregnancy outcomes and one case of fetal development anomalies, whose mother received busulfan in combination with radiotherapy and other antitumor drugs.

    In view of the potential threat to the fetus for women of childbearing age during the treatment with busulfan, contraceptives are recommended.

    There is no information on the penetration into breast milk. Due to the excretion of other antitumor drugs with milk and the potential risk of unwanted effects on the child (side effects, carcinogenicity, mutagenicity) during the treatment with busulfan, breastfeeding is recommended to be discontinued.

    Dosing and Administration:

    Inside, once, at the same time of day. The dose is selected individually, adjusted based on the clinical effect and the degree of oppression of bone marrow function.

    In chronic myelogenous leukemia: adults at a rate of 0.06 mg / kg per day (before the decrease in the level of leukocytes below 15 × 109/ l), with sharply expressed splenomegaly and a large number of leukocytes - 8-10 mg, with a decrease in the number of leukocytes to 40 × 109/ l-50 × 109/ l dose should not exceed 4 mg. The maximum daily dose is 10 mg; usually maintaining a dose of 0.5-2 mg per day, treatment is continued with a remission period of less than 3 months. Treatment is resumed at the remission stage, if the number of white blood cells is 50 × 109/ l.

    In myelofibrosis and essential thrombocythemia: 2-4 mg per day (under the control of platelets - not less than 500 × 109/ l or leukocytes 5 × 109/ l).

    With true polycythemia: 4-6 mg per day for 4-6 weeks.

    For children with chronic myelogenous leukosis, the initial dose is 0.06-0.12 mg / kg per day or 1.8-4.6 mg / m2 per day. The dose is selected in such a way as to reduce the number of leukocytes and maintain their level of about 20 × 109/ l.

    Side effects:

    On the part of the organs of the gastrointestinal tract: anorexia, gastrointestinal bleeding, stomatitis, dryness of the oral mucosa, diarrhea, nausea, vomiting, cholestatic jaundice, weight loss, impaired liver function, dysplastic changes in the cells of the pancreas, liver.

    From the nervous system and sensory organs: dizziness, weakness, fatigue, cataract.

    Cardio-vascular system and the blood: lower limb edema, hypotension, cardiac tamponade, endocardial fibrosis, mielodeprescia (leucopenia, thrombocytopenia, anemia), bleeding and hemorrhage.

    On the part of the respiratory organs: bronchopulmonary dysplasia with the development of pneumosclerosis (cough, dyspnea).

    With the genitourinary system: a painful, difficult urination, hematuria, nephropathy, dysplastic changes in bladder cells, amenorrhea, cervical dysplasia cells, suppression of ovarian function, azoospermia, testicular atrophy, sterility.

    Skin and soft tissue: skin hyperpigmentation (5-10%), erythema multiforme, alopecia, urticaria, "allopurinolovaya rash", dry skin (up to full agidroza), at high doses - fibrosis with atrophy and skin necrosis.

    Metabolism: hyperuricemia, hyperuricosuria, reducing excretion gidroksikortikosteroidov 17, resembling adrenal insufficiency syndrome.

    Pain syndrome (pain in the back, side,joints); development of infections; fever, chills; gynecomastia; myasthenia gravis; dysplastic changes in cells of the breast, lymph nodes, thyroid gland.

    Overdose:

    Symptoms: nausea, vomiting, dizziness, severe bone marrow depression, fever, bleeding.

    Treatment: induction of vomiting, gastric lavage followed by the use of activated charcoal; hospitalization, monitoring of vital functions; symptomatic therapy; if necessary - transfusion of blood components, the appointment of broad-spectrum antibiotics.

    Interaction:

    Anti-gouty drugs (allopurinol, colchicine, probenecid, sulfinpyrazone): an increase in the concentration of uric acid in the blood plasma, correction of the dose of the antifungal drug. In view of the risk of developing urinary acid nephropathy with the use of antidotal agents for the prevention and treatment of busulfan-mediated hyperuricemia, the use of allopurinol is preferable.

    Thioguanine - increased risk of liver function abnormalities, development of nodal regenerative liver hyperplasia, portal hypertension, varicose veins of the esophagus with parallel application.

    Itraconazole - a decrease in busulfan clearance by 25% (not more); toxicity monitoring in parallel application is required.

    Paracetamol - it is possible to reduce the clearance of busulfan when taking the drug less than 72 hours before or simultaneously with busulfan.

    Phenytoin - it is possible to reduce the clearance of busulfan by 15% with parallel application.

    Inactivated vaccines: weakening the effectiveness of immunization;

    Vaccines containing live viruses: increased viral replication and side effects of vaccination.

    Special instructions:

    Before intravenous administration, the contents of the vial are diluted with 0.9% sodium chloride solution or 5% dextrose solution in a volume 10 times the volume of the vial to a final concentration of at least 0.5 mg / ml. To do this, the required amount of busulfan is taken with a syringe with a needle and a filter with a pore size of 5 microns (supplied with the drug), after which the needle is changed and the contents of the syringe are introduced into the container with a pre-prepared solution of 0.9% sodium chloride or 5% dextrose solution. In all cases, you should enter busulfan in the solvent, and not vice versa. The resulting solution is mixed by inverting.

    It is not recommended fast infusions of busulfan. Use infusion pumps. Before and after each infusion, the catheter should be rinsed with 5 ml of 0.9% sodium chloride or 5% dextrose solution.

    Patients with hyperuricemia and / or hyperuricosuria need correction of these conditions before treatment with busulfan.

    With the possible development of delayed myelotoxicity, it is recommended to stop busulfan treatment or reduce its dose at the first sign of a sudden decrease in the number of leukocytes (in particular, granulocytes) in order to prevent irreversible myelosuppression.

    Some patients may be more susceptible to busulfan and demonstrate rapid myelosuppression. Frequent and careful monitoring of peripheral blood parameters is necessary. Reducing the number of leukocytes has an exponential character and the construction of a semilogarithmic dependence of the weekly decrease in the number of leukocytes allows one to predict the time of reaching their number to 15 × 109/ l and cancellation of the drug.

    Cytological studies of the lungs, bladder, breast, cervix, lymph nodes, pancreas and thyroid gland, adrenal glands,bone marrow - the dysplasia of cells, induced by busulfan, can be expressed and make it difficult to interpret cytological preparations.

    Busulfan causes myelosuppression, which increases the incidence of microbial infections, slows the healing of wounds and increases bleeding gums. It is necessary, if possible, to complete all dental work before chemotherapy begins and to resume them only after the resolution of myelosuppression.

    Dimethylacetamide (a solvent included in the formulation of busulfan) can cause an increase in the activity of transaminases and the appearance of neurologic symptoms.

    The diluted busulfan solution is stable for less than 8 hours at room temperature (25 ° C) and less than 12 hours - when stored in a refrigerator. It is necessary to complete the infusion by this time.

    The tablet form of the preparation is stored in a tightly-closed container at a temperature below 40 ° C (preferably 15-25 ° C) unless otherwise directed by the manufacturer.

    The solution for intravenous administration is stored at a temperature of 2-8 ° C.

    The application is possible only under the supervision of a physician with experience in chemotherapy.

    Before and during the treatment (at short intervals) it is necessary to determine the level of hemoglobin or hematocrit, the number of leukocytes (total, differential), platelets, activity of alanine aminotransferase, alkaline phosphatase, bilirubin level, uric acid concentration, constant monitoring of kidney and lung function.

    If the following symptoms occur: chills, fever, cough or hoarseness, pain in the lower back or in the side, painful or difficult urination, bleeding or hemorrhage, black stools, blood in the urine or feces, consult a doctor immediately.

    Leukopenia develops from 10-15 days after the start of therapy (before a short-term increase in the number of leukocytes is observed), the lowest level is observed on the 11th-30th day of treatment (it may decrease within 1 month after drug discontinuation), the level of leukocytes is restored during the next 12- 20 weeks (with severe myelodepression, treatment should be discontinued until symptoms of hematotoxicity are eliminated). With mielodepression (pancytopenia) after busulfan withdrawal, the restoration of the number of uniform elements to the normal level occurs within 1 month - 2 years.

    In case of nausea and vomiting, busulfan should be continued, at the first signs of interstitial pneumosclerosis, treatment should be discontinued. Bronchopulmonary dysplasia with the development of pneumosclerosis, accompanied by a decrease in the vital function of the lungs and elasticity of the lung tissue, can develop in 8 months - 10 years (on average 4 years) after the start of treatment, within 6 months after diagnosis is possible fatal outcome.

    When thrombocytopenia occurs, extreme caution is recommended when performing invasive procedures, regular examination of the sites of intravenous injections, skin and mucous membranes (to detect signs of bleeding), limiting the frequency of venous punctures and refusing intramuscular injections, monitoring blood in urine, vomit, feces. Such patients need to shave with care, do a manicure, brush their teeth, use dental floss and toothpicks, and perform dental procedures; should prevent constipation, avoid falls and other injuries, as well as taking alcohol and acetylsalicylic acid, increasing the risk of gastrointestinal bleeding.

    In order to prevent nephropathy due to increased uric acid formation (occurs most often in the initial stage of treatment), it is necessary to consume enough fluids, increase diuresis, prescribe allopurinol (in some cases), and use drugs that cause alkalinization of urine.

    In patients with increased seizure activity, treatment should be performed under the cover of anticonvulsants (preferably benzodiazepines, since enzyme inducers, for example phenytoin, can increase the clearance of busulfan and reduce its effectiveness).

    If the reception was missed, the dose is not replenished, and the subsequent dose is not doubled.

    It is necessary to delay the vaccination schedule (not earlier than 3 months or even 1 year after the end of the last course of chemotherapy) to the patient and other family members living with him (oral immunization against poliomyelitis should be discarded). Avoid contact with infectious patients or use non-specific measures for prevention (protective mask, etc.).

    It should be refrained from using in pediatric practice, since safety and effectiveness of its use in children are not defined.Adequate contraceptive measures should be used during treatment.

    In case of contact with the skin or mucous membranes, thorough rinsing with water (mucous membranes) or with soap and water (skin) is necessary.

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