Lomustin

When ATH:
L01AD02

Characteristic.

Nitrosoureas. Crystalline powder creamy white. The thermally unstable, decomposes upon melting. Practically insoluble in water, Insoluble in 10% and absolute ethyl alcohol, acetone, dimethylsulfoxide and dimethylformamide.

Pharmacological action.
Antitumor, alkylating, cytostatic, immunosuppressive.

Application.

Limfogranulematoz (in combination with other drugs), multiple myeloma, lymphosarcoma, melanoma, undifferentiated lung cancer, ENT, GI, kidneys, Breast, primary and metastatic brain tumors, osteosarcoma.

Contraindications.

Hypersensitivity, severe liver and kidney, kaxeksija, severe myelosuppression (уровень тромбоцитов менее 25·109/l, лейкоцитов менее 2·109/l, anemia).

Restrictions apply.

Assessment of the risk-benefit ratio is needed in the appointment of the following cases: enable vetryanaya, herpes zoster and other systemic infections, impairment of renal function, light (reduced baseline forced vital capacity and diffusion capacity of the lungs below 70%), suppression of bone marrow function, prior cytotoxic or radiation therapy, advanced age.

Pregnancy and breast-feeding.

Contraindicated in pregnancy.

Category actions result in FDA - D. (There is evidence of the risk of adverse effects of drugs on the human fetus, obtained in research or practice, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk, if the drug is needed in life-threatening situations or severe disease, when safer agents should not be used or are ineffective.)

At the time of treatment should stop breastfeeding.

Side effects.

From the digestive tract: gastrointestinal bleeding, anorexia, stomatitis, nausea, vomiting, abnormal liver function, transient and reversible increases in liver function tests.

From the nervous system and sensory organs: confusion, dysarthria, asthenia.

Cardio-vascular system and blood (hematopoiesis, hemostasis): mielodeprescia: leukopenia (число лейкоцитов ниже 5·109/- 65%, ниже 3·109/- 36%), thrombocytopenia, anemia, bleeding and hemorrhage, Acute leukemia, peripheral edema.

From the respiratory system: cough, breathlessness, infiltration of the lung tissue, fibrosis.

With the genitourinary system: painful, strangury, hematuria, impairment of renal function (reducing the size of the kidney, progressive azotemia, renal failure), amenorrhea, azoospermia.

For the skin: alopecia, skin darkening, skin rash, contact dermatitis, itch, necrosis of perivascular spaces, phlebitis, obliteration of the vein at the injection site.

Other: pain syndrome (backache, by), the development of infections, hyperthermia.

Cooperation.

Compatible with other cytotoxic drugs, with carmustine there is some cross-resistance. Weakens the effectiveness of immunization inactivated vaccines; using vaccines, containing live viruses, enhances viral replication and side effects of vaccination. Other myelotoxicity drugs, Radiotherapy enhance bone marrow depression (potentiate the neutropenia, thrombocytopenia).

Overdose.

Symptoms: nausea, vomiting, severe bone marrow depression, gepatotoksichnostь, bleeding.

Treatment: hospitalization, monitoring vital functions; simptomaticheskaya therapy; if necessary - transfusion of blood components, the appointment of broad-spectrum antibiotics.

Dosing and Administration.

Inside, for 1 hour before meals. Dose picked individually, is corrected on the basis of clinical effect, the severity of the toxic effect. Children and adults with monotherapies, the initial dose is 100-130 mg/m2, single, every 6 weeks or 75 mg / m2 every 3 Sun; in combination with other cytotoxic drugs-70-100 mg/m2 every 6 Sun. При уровне тромбоцитов 75–100·109/l and more, лейкоцитов 3–4·109/l and more — the total dose is 100% from the previous dose, при уровне тромбоцитов 25–75·109/l, лейкоцитов 2–3·109/- 70%, при уровне тромбоцитов менее 25·109/l, лейкоцитов менее 2·10 9/- 50%. In patients with oppression of the bone marrow dose is 100 mg / m2.

Precautions.

Use only under medical supervision, with experience chemotherapy. Prior to and during treatment (at short intervals) you must determine the level of hemoglobin, or hematocrit, bilirubin, BUN, creatinine, IS aktivnosti, GOLD, LDH, the number of leukocytes (overall, differential), Platelet, pulmonary function tests. As a result of the cumulative effect of the treatment should be no more 1 times a 6 Sun (the recovery of bone marrow function), an additional course is only possible when the next level of blood cells: число тромбоцитов более 100·109/l , лейкоцитов 4·109/l. The most pronounced leukopenia and thrombocytopenia are observed 4-6 weeks after starting treatment, stored for 1-2 weeks, recovery occurs within 6-7 weeks after treatment (when expressed myelodepression treatment should be discontinued until symptoms resolve gematotoksichnosti). Given the possibility of a late manifestation of thrombocytopenia and other signs of hematopoiesis, other cytotoxic agents should be administered no earlier than 3-6 weeks from the beginning of treatment. Nausea and vomiting develop through 3-6 h after administration and lasts less 24 no (should be the appointment of antiemetics), loss of appetite may persist for 2-3 days after administration. Toxic effect on light observed when applying the cumulative doses of 600-1240 mg or with duration of treatment 6 months or more. If the following symptoms: chills, fever, cough or hoarseness, pain in the lower back or side, painful or difficult urination, bleeding or hemorrhage, black stools, blood in the urine or feces - consult your physician immediately. In the event of thrombocytopenia advised extreme caution when performing invasive procedures, Regular inspection of places on / in the, skin and mucous membranes (for signs of bleeding), limit frequency troublesome and the rejection of the / m injection, control of blood in the urine, vomit, Kale. The patients must be carefully shave, manicure, brush your teeth, dentists use threads and toothpicks, to conduct dental procedures; should be the prevention of constipation, avoid falls and other injuries, as well as the intake of alcohol and acetylsalicylic acid, increase the risk of gastrointestinal bleeding. Should defer vaccination schedule (carried out not earlier than 3 Months before 1 years after completion of the last cycle of chemotherapy) patient and other family members, residing with him (should abandon immunization oral polio vaccine). Avoid contact with infectious patients, or use non-event for the prevention of (face mask, etc.). During treatment should use appropriate contraceptive measures. In case of contact with skin or mucous membranes - rinse thoroughly with water (mucosa) or soap and water (skin).

Cooperation

Active substanceDescription of interaction
BusulfanFMR. Strengthens (mutually) effect, It increases the likelihood of side effects, incl. venookklyuzionnoy liver disease.
DakarʙazinFMR. Strengthens (mutually) effect, incl. the likelihood and severity of side (destruction of bone marrow function, liver and others.).
DoxorubicinFMR. Strengthens (mutually) effect, incl. the likelihood and severity of side.
KarmustinFMR. Strengthens (mutually) effect, incl. the likelihood and severity of side.

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