Acute myeloblastic leukemia, acute and chronic lymphatic leukemia, meningeal leukemia
藥理
Antineoplastic Agent, Antimetabolite
Cytarabine is a pyrimidine analog and is incorporated into DNA; however, the primary action is inhibition of DNA polymerase resulting in decreased DNA synthesis and repair. Cytarabine is specific for the S phase of the cell cycle (blocks progression from the G1 to the S phase).
藥動學
Distribution:
1. Vd: 3 ± 11.9 L/kg; crosses blood-brain barrier with CSF levels of 40% to 50% of plasma level
2. Bioavailability: SubQ: 89% to 100%; Protein binding: 13% Metabolism:
1. Primarily hepatic; metabolized by deoxycytidine kinase and other nucleotide kinases to aracytidine triphosphate (active)
2. About 86% to 96% of dose is metabolized to inactive uracil arabinoside (ARA-U)
3. Half-life elimination: (Initial) 7 to 20 minutes; (Terminal) 1 to 3 hours; (Intrathecal) 2 to 6 hours Excretion:
Urine (~80%; 90% as metabolite ARA-U) within 24 hours
禁忌症
1. Hypersensitivity to cytarabine or any component of the formulation
2. Patients with bone marrow depression
3. Pregnancy women
懷孕分類
D.
哺乳分類
Avoided
副作用
Nausea, vomiting, bone marrow depression, ulceration of mouth, conjunctivitis, keratitis, lethargy
劑量和給藥方法
Acute lymphoblastic leukemia: Induction regimen:
(IV) 3,000 mg/m2 over 3 hours daily for 5 days (in combination with idarubicin [day 3]) Dose-intensive regimen:
(IV) 3,000 mg/m2 over 2 hours every 12 hours days 2 and 3 (4 doses/cycle) of even numbered cycles (in combination with methotrexate; alternates with Hyper-CVAD) CALGB 8811 regimen:
1. Early-intensification phase: (SUBQ) 75 mg/m2/dose days 1 to 4 and 8 to 11 (4-week cycle; repeat once)
2. Late-intensification phase: (SUBQ) 75 mg/m2/dose days 29 to 32 and 36 to 39 Acute myeloid leukemia:
100 mg/m2/day continuous infusion for 7 days or 200 mg/m2/day continuous infusion (as 100 mg/m2 over 12 hours every 12 hours) for 7 days Chronic lymphocytic leukemia:
(IV) 1,000 mg/m2/dose over 2 hours days 2 and 3 every 4 weeks for up to 6 cycles (in combination with oxaliplatin, fludarabine, and rituximab)
小兒調整劑量
腎功能調整劑量
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling
安定性
Cytarabine with D5W or NS is compatible for 6 hours (room temperature) and 12 hours (2-8 degree celcius) in glass or polyolefin containers; Maximum concentrartion 100mg/mL
注射給藥指引
給藥途徑
IV, IT, SC
靜脈輸注液
NS
每瓶稀釋液體積
注射濃度
給藥速率
Infuse standard dose therapy for AML (100 to 200 mg/m2/day) as a continuous infusion. Infuse high-dose therapy (off-label) over 1 to 3 hours (usually). Other rates have been used, refer to specific reference.
安定性
Cytarabine with D5W or NS is compatible for 6 hours (room temperature) and 12 hours (2-8 degree celcius) in glass or polyolefin containers; Maximum concentrartion 100mg/mL