Antineoplastic Agent (Anthracycline; Topoisomerase II Inhibitor)
Daunorubicin inhibits DNA and RNA synthesis by intercalation between DNA base pairs and by steric obstruction. Daunomycin intercalates at points of local uncoiling of the double helix. Although the exact mechanism is unclear, it appears that direct binding to DNA (intercalation) and inhibition of DNA repair (topoisomerase II inhibition) result in blockade of DNA and RNA synthesis and fragmentation of DNA.
藥動學
Distribution:
Distributes widely into tissues, particularly the liver, kidneys, lung, spleen, and heart; does not distribute into the CNS Metabolism:
Primarily hepatic to daunorubicinol (active), then to inactive aglycones, conjugated sulfates, and glucuronides Half-life elimination:
1. Initial: 45 minutes; Terminal: 18.5 hours
2. Daunorubicinol plasma half-life: ~27 hours Excretion:
Feces (40%); urine (~25% as unchanged drug and metabolites)
禁忌症
Hypersensitivity to daunorubicin or any component of the product.
懷孕分類
Based on data from animal reproduction studies, in utero exposure to daunorubicin may cause fetal harm.
哺乳分類
Due to the potential for serious adverse reactions in the breastfed infant, the manufacturer recommends that breastfeeding be discontinued during daunorubicin therapy.
副作用
Alopecia, Nausea and vomiting, Cardiotoxicity, Hyperuricemia, Myelosuppression
劑量和給藥方法
General dose:
1. Initial dose: IV 1mg/ky/day for 4-5 days, monitor closely; then restart treatment after 8-10 days
2. Maintenance dose: IV 1-2mg/kg once to twice every week
小兒調整劑量
腎功能調整劑量
SCr >3 mg/dL: Administer 50% of normal dose
肝功能調整劑量
1. Serum bilirubin 1.2-3 mg/dL: Administer 75% of dose
2. Serum bilirubin >3 mg/dL: Administer 50% of dose