1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]anthrachinondihydrochlorid Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R46:Kann vererbbare Schäden verursachen.
R61:Kann das Kind im Mutterleib schädigen.
R26/27/28:Sehr giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
S22:Staub nicht einatmen.
Beschreibung
Mitoxantrone hydrochloride is the first of the synthetic anthracenediones related
to doxorubicin to reach the marketplace. Mitoxantrone is useful in the treatment
of advanced localized and metastatic mammary carcinomas. It is reported to be
less cardiotoxic than doxorubicin.
Chemische Eigenschaften
Dark blue, electrostatic, hygroscopic powder.
Verwenden
analgesic, antipyretic
Allgemeine Beschreibung
Mitoxantrone is supplied as a blue aqueous solution in 10-and 20-mg vials for IV administration in the treatment of acute lymphoid leukemia, acute myeloid leukemia, breastcancer, prostate cancer, non-Hodgkin’s lymphoma, andmultiple sclerosis. The mechanisms of resistance are thesame as those seen for the anthracyclines. The distributionhalf-life is 1.1 to 3.1 hours, and the drug has a large volumeof distribution (11 L/kg). The elimination half-life rangedfrom 23 to 215 hours, and elimination was primarily via thebile. Metabolism of the agent involves oxidation of the sidechainalcohols to give the monocarboxylic and dicarboxylicacids.Other toxicities are those seen for the anthracyclinesand include myelosuppression, nausea, vomiting, mucositis,diarrhea, and alopecia. The intense color of the parent drugand metabolites may turn the urine blue.
Clinical Use
Mitoxantrone is used in combination with other agents during the initial treatment of acute nonlymphocytic leukemia and hormone-refractory prostate cancer. Recent studies have shown that mitoxantrone also decreases the rate of relapse and disease progression in patients with multiple sclerosis. Although too toxic for use in patients with primary progressive disease, it is available for the treatment of chronic progressive, progressive relapsing, or deteriorating relapsing-remitting multiple sclerosis.
Stoffwechsel
Mitoxantrone excretion primarily is biliary. Both the unchanged drug and inactive metabolites resulting from N-dealkylation, deamination, and oxidation of the resultant aldehyde to the carboxylic acid are observed. Both arms of the structure can be metabolized, leading to mono- or dicarboxylic acid metabolites, which are excreted as the glucuronide conjugate. The conjugated metabolites are an intense, dark blue in color and will result in blue-green urine.
1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]anthrachinondihydrochlorid Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
