2010/06/09

Dacarbazine

Trade name:
Dacarbazine Medak

International name:
Dacarbazine (Dacarbazine)

Group Affiliation:
Antitumor agents, alkylating

Description of the active substance (INN):
Dacarbazine

Dosage form:
lyophilisates for solution for intravenous

Mode of action:
Antitumor agents, alkylating agents, becomes active after metabolism in the liver releases diazomethane, covalently bind to SH-groups of biomolecules. As an analog of purine bases, also has the properties of antimetabolites. It blocks the synthesis of RNA and DNA (due to the formation of complexes with carbonium ions) leads to the cessation of mitosis of cells. Fazonespetsifichen.

Indications:
Melanoma, venereal disease, soft tissue sarcoma (excluding Kaposi's sarcoma). In the composition of multicomponent chemotherapy: osteogenic sarcoma, uterine sarcoma, lymphosarcoma, embryonal rhabdomyosarcoma, mesothelioma of the pleura and peritoneum, carcinoid tumor (including bronchogenic carcinoma, small cell lung cancer, thyroid cancer), pheochromocytoma, insulinoma, neuroblastoma, CNS tumors (gliomas).

Contraindications:
Hypersensitivity, severe suppression of bone marrow hematopoiesis, severe hepatic and / or renal failure, pregnancy, laktatsii.C caution. Mielodepressiya (including on a background of concomitant radiotherapy and chemotherapy), acute infectious viral disease (including chickenpox, herpes zoster), fungal or bacterial origin (the risk of severe complications and the generalization of the process), concomitant radiotherapy

Side effects:
On the part of the digestive tract: decreased appetite, stomatitis, nausea, vomiting rarely - increased activity of "liver" enzymes, diarrhea, and in rare cases - gepatonekroz caused by occlusion of the intrahepatic veins, possibly with fatal consequences (usually the syndrome arose during the 2 treatment) - fever, eosinophilia, abdominal pain, liver enlargement and shock, the severity of which increases rapidly for several hours or days. From the side of blood: anemia, granulocytopenia, thrombocytopenia, leukopenia. the nervous system: headache, blurred vision, confusion, marked drowsiness, seizures, asthenia, paresthesia, hypoesthesia skin. On the part of the endocrine system: alopecia, amenorrhea, azoospermia. Allergic reactions: skin rash, flushing skin, a feverish syndrome, anaphylactic reaction. Local reactions: pain in the injection site and along the veins when the product enters the skin - a sharp pain at the injection site and necrosis of surrounding tissues. Other: increased bleeding, hemorrhage, superinfection, thrombosis of hepatic veins, myalgia, flu-like syndrome. With long-term use increases the risk of novoobrazovaniy.Peredozirovka. Symptoms: increased suppression of bone marrow hematopoiesis and severity of dyspeptic disorders. Treatment: symptomatic, specific antidote known.

Dosage and administration:
When choosing the dose and the drug treatment in each individual case should use the data of literature. The drug is introduced strictly in / in. Doses up to 200 mg / m entered the jet slowly over 1-2 minutes. Higher doses should be administered in the form of intravenous infusion over 15-30 min. Usually used as monotherapy dacarbazine at a dose of 200-250 mg / m daily for 5 days. Repeated courses are held at intervals of 3 weeks. In combination with other cytostatic agents dacarbazine is introduced at a dose of 100-150 mg / m 4-5 consecutive days with an interval of 4 weeks or 375 mg / m² every 15 days. Before the introduction of product diluted with water for injection to achieve a concentration of 10 mg / ml. For freshly prepared solution for infusion solution is diluted in 200-300 ml 0.9% NaCl solution or 5% dextrose solution (a solution of dacarbazine should be protected from light).

Cautions:
The drug should be administered under the supervision of a physician who has considerable experience in conducting anti-tumor therapy. During and after treatment is necessary to monitor patterns of peripheral blood, liver function and its size. In the event of violations by the liver or kidneys, symptoms of hypersensitivity to the drug or thrombosis hepatic veins dacarbazine treatment should be stopped immediately. When the first signs of extravasation dacarbazine (burning or pain at the injection site), the introduction should be stopped immediately. The remaining dose should be introduced in other vein. At the period of treatment should be abandoned immunization (including all family members residing with the patient), oral polio vaccine, as well as to avoid contact with people who receive it, or wear a protective mask, Cover your mouth and nose. If you suspect depression blood should avoid contact with patients with bacterial infections. During the treatment sessions to avoid contact sports and other situations which are likely to hemorrhage and trauma. Given that the different sensitivity of dacarbazine, the solutions of the drug should be stored protected from light. Women and men during treatment and for 6 months after should use reliable methods of contraception.

Interaction:
Compatible with bleomycin, cisplatin, 5-fluorouracil, vincristine, prednisone. Strengthens effect (including toxicity), phenobarbital, azathioprine, 6-mercaptopurine. Inductors microsomal liver enzymes (barbiturates, rifampicin, phenytoin) increase the toxic effect of dacarbazine. Intensifies effects arthrifuge drugs, as well as bone marrow depression on the background of myelotoxicity of drugs. dacarbazine may increase the photosensitizing action metoksipsoralena. dacarbazine solution are chemically incompatible with heparin, hydrocortisone, L-cysteine and sodium bicarbonate.