2010/06/23

Dacarbazine

Composition, structure and packing

1 flakon preparata contains:

Active ingredient: dakarbazin 100 mg or 200 mg respectively. Vspomogatelnye veschestva: limonnaya kislota, mannitol.

Farmakologicheskie svoystva

Dakarbazin - this means alkiliruyuschego antitumor action of the Chemical sostavu predstavlyayuschee a 5 - (3,3-dimethyl-1-triazeno)-imidazol-4-karboksamid. Preparat stanovitsya Active after metabolizma in the liver.

Predpolagayut that there are three ways of mehanizma dakarbazina: alkilirovanie za by ion karboniya, inhibition of purine and osnovany vzaimodeystvie with SH gruppami. Preparat fazonespetsifichen.

Farmakokinetika

Peak concentration, usually in plazme dostigaetsya srazu immediately after intravenous preparata. Svyazyvanie belkami with very low (around 5%). Dakarbazin pronikaet through gematoentsefalichesky barer in very small kolichestvah. No dannyh of its penetration through platsentu and expose the breast milk. Is derived from the preparat organizma dvuhfaznym way to nachalnym half-life of about 20 minutes and end - about 5 chasov, Irregularities in the liver or kidneys are pokazateli prevalent made approximately 55 minutes and 7 chasov respectively.

Preparat podvergaetsya dimetilirovaniyu pochenochnymi mikrosomalnymi fermentami obrazovaniem with CO2, which is derived from the air and vydyhaemym aminoimidazolkarboksamida, are excreted in the urine. 40% preparata displayed pochkami unchanged mainly by glomerular za filtratsii. Pokazaniya melanoma, limfogranulematoz, sarkomy soft tkaney. In spetsializirovannoy literature there are reports on the effectiveness of dakarbazina in sochetanii with other tsitostatikami in the treatment of osteogenic sarkom, sarkomy Kaposhi, sarkomy matki, testicular tumors, tumors of the gastrointestinal tract and neyroblastomy.

Protivopokazaniya
povyshennaya sensitivity preparatu,
pregnancy and lactation.

Dosage regimen

Preparat introduced strictly intravenously jet within 1-2 minutes. As a possible monoterapii dakarbazin used in doses of 200-250 mg/m2 daily for 5 days. Repeated courses of conduct with intervalom in SW weeks. When sochetanii with other tsitostatikami dakarbazin introduced at a dose of 100-150 mg/m2 days 4-5, courses of treatment with the conduct of intervalom in 4 weeks. Before the introduction of preparat razvodyat water for injection to achieve concentration, 10 mg / 1 ml.

Side effect
From the hematopoietic system: Oppression mielopoeza yavyaletsya ogranichivayuschim dose of side effects and can be Expressed harakter.

Leykotsitopeniya usually nablyudaetsya nA day 14, thrombocytopenia - nA 18 days after After playing terapii and lasts an average of up to 1 week. Have been reported a case of oppression rannih priznakov hematopoiesis (10-12 days) a takzhe late (nA 30 day treatment). Vosstanovlenie pokazateley blood going to the 4 th week. Inogda nablyudalas discharge, anemia.
On the part of the gastrointestinal trakta: the most cost chastymi complications are vyrazhennaya toshnota and rvota normally voznikayut during the first 2 days of treatment and well-cropped antiemetic preparatami. Some patients in this period nablyudaetsya diarrhea.

In a case of isolated otmechayutsya stomatity.

Reaktsii Local: Pain at the injection site and along the veins. If you expose the preparata under the skin - vyrazhennaya pain, necrosis okruzhayuschih tkaney.

Other: In a case of 3-5% nablyudayutsya flu-like syndrome (increase temperatury to 39 ° C, and total vyrazhennaya mialgiya nedomoganie) obratimoe increase in liver enzymes in blood serum, golovnaya pain parestezii. In some patients nablyudayutsya kozhnaya rash, alopetsiya, phlebitis, pokrasnenie litsa.

Cautions

Preparat should be entered under nablyudeniem vracha having dostatochny experience in anti-terapii. Special vnimanie should be given control sistematicheskomu za pokazatelyami blood.

Drug Interactions

Preparaty inducing mikrosomalnye liver enzymes (barbituraty, rimfampitsin, phenytoin), while the application may potentsirovat toxic effect dakarbazina. Application dakarbazina in sochetanii with merkaptopurinom, azatioprinom and allopurinolom can potentsirovat action of the latter and uvelichivat their toxicity.

Peredozirovka

In case of overdose ozhidat increased suppression of bone marrow hematopoiesis and gastrointestinalnoy toxicity. The specific antidot is not known. Treatment simptomaticheskoe.

Terms and Conditions of storage

Hranit the reach of small children at temperature not above 25 ° C, zaschischat from sveta. Shelf life 2 years. Razvedenny preparat can hranitsya in a dark place no more than 6 chasov. Preparat should not be used later sroka life, Indications nA upakovke.