Vinblastin Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
An alkaloid derived
from the periwinkle, Catharanthus roseus (formerly Vinca
rosea) used as an antitumor drug in the treatment of Hodgkins
lymphoma and other cancers. It binds to the microtubule subunit, tubulin, at a site distinct from that of colchicine and
podophyllotoxin. This binding is reversible, temperature
dependent and rapid, and results in large tubulin aggregates of
highly ordered structure (vinblastine paracrystals).
Physikalische Eigenschaften
Appearance: needlelike crystals were produced when recrystallized by methanol.
Solubility: soluble in chloroform, acetone, and ethanol. Melting point: 211–
216?°C.?Sulfate melting point of vinblastine is 284–285?°C; hydrochloric acid melting point of vinblastine is 244–246?°C (decomposes). Specific optical rotation:
+42°.
Verwenden
Vinblastine is used for severe lymphoblastic leukemia, Hodgkin’s disease, nonHodgkin’s lymphoma, neuroblastoma, sarcoma, and other cancerous diseases.
Indications
It was recorded in the Pharmacopoeia of the People’s Republic of China (2015), the
British Pharmacopoeia (2017), the United States Pharmacopeia (40), the Japanese
Pharmacopoeia (17th ed.), the European Pharmacopoeia (9th ed.), and The
International Pharmacopoeia (5th ed.).
Vinblastine sulfate injection is used as the first-line therapy to treat Hodgkin
lymphoma, lymphocytic leukemia, testis tumor, and choriocarcinoma intravenously
in clinical practice generally according to ABVD methods (Adriamycin, bleomycin,
vinblastine, and dacarbazine).
Mechanism of action
Vinblastine suppresses cell growth during metaphase, affects amino acid metabolism, in
particular at the level of including glutamine acid into the citric acid cycle and preventing
it from transformation into urea, and it also inhibits protein and nucleic acid synthesis.
Pharmakokinetik
Leukopenia is the dose-limiting side
effect, and dose reductions are warranted in patients with serum bilirubin levels greater than 3 mg/dL. The
drug-related impact on erythrocyte and thrombocyte levels usually is insignificant. Like vincristine, it is
administered as an IV bolus or infusion. The initial elimination half-life of 3.7 minutes is similar to vincristine,
but the 24.8-hour terminal half-life is significantly shorter.
Clinical Use
In addition to the hematologic indications that it shares with vincristine, vinblastine sulfate has
found utility in the treatment of advanced testicular carcinoma (often in combination with bleomycin),
advanced mycosis fungoides, Kaposi's sarcoma, and histiocytosis X.
Vinblastin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
