小細胞肺癌、睪丸腫瘤 Small cell lung cancer; Testicular cancer
藥理
Antineoplastic Agent, Topoisomerase II Inhibitor
Etoposide has been shown to delay transit of cells through the S phase and arrest cells in late S or early G2 phase. It may inhibit mitochondrial transport at the NADH dehydrogenase level or inhibit uptake of nucleosides into HeLa cells.
藥動學
Distribution:
1. Average Vd: (Children) 10 L/m2; (Adults) 7 to 17 L/m2; poor penetration across the blood-brain barrier; CSF concentrations <5% of plasma concentrations
2. Protein binding: 94% to 98% Metabolism:
Hepatic, via CYP3A4 and 3A5, to various metabolites; in addition, conversion of etoposide to the O-demethylated metabolites (catechol and quinine) via prostaglandin synthases or myeloperoxidase occurs, as well as glutathione and glucuronide conjugation via GSTT1/GSTP1 and UGT1A1 Half-life elimination:
Children: 6 to 8 hours; Adults: 4 to 11 hours Excretion:
1. Children: Urine (~55% as unchanged drug) in 24 hours
2. Adults: Urine (56%; 45% as unchanged drug) within 120 hours; feces (44%) within 120 hours
禁忌症
1. Hypersensitivity to etoposide or any component of the formulation.
2. Severe leukopenia or thrombocytopenia; severe hepatic impairment; severe renal impairment
懷孕分類
1. Fetal growth restriction and newborn myelosuppression have been observed following maternal use of regimens containing etoposide during pregnancy
2. In general, if chemotherapy is indicated, it should be avoided during in the first trimester, there should be a 3-week time period between the last chemotherapy dose and anticipated delivery, and chemotherapy should not be administered beyond week 33 of gestation
哺乳分類
Due to the potential for serious adverse reactions in the breastfed infant, the manufacturer recommends a decision be made taking into account the importance of treatment to the mother.
Small cell lung cancer:
120 mg/m2 on days 1, 2, and 3 every 3 weeks (in combination with cisplatin and concurrent radiation) for 4 courses or
100 mg/m2 on days 1, 2, and 3 every 4 weeks (in combination with cisplatin and concurrent radiation) for 4 cycles or
100 mg/m2 on days 1, 2, and 3 every 3 weeks (in combination with cisplatin and sequential radiation) for 4 cycles or
100 mg/m2 on days 1, 2, and 3 every 3 weeks (in combination with carboplatin and radiation) up to a maximum of 6 cycles or
100 mg/m2 on days 1, 2, and 3 every 3 to 4 weeks (in combination with cisplatin) for 6 cycles or
100 mg/m2 IV on day 1 (in combination with cisplatin and concurrent radiation), followed by 200 mg/m2 orally on days 2 through 4 every 3 weeks for a maximum of 5 courses Testicular cancer:
1. Good risk: 100 mg/m2 on days 1 to 5 every 3 weeks (in combination with cisplatin) for 4 cycles
2. Intermediate or poor risk: 100 mg/m2 on days 1 to 5 every 3 weeks (in combination with bleomycin and cisplatin) for 4 cycles or 75 mg/m2 on days 1 to 5 every 3 weeks (in combination with cisplatin, ifosfamide, and mesna) for 4 cycles
3. high-dose regimens: 750 mg/m2/day administered 5, 4, and 3 days before peripheral blood stem cell infusion (in combination with carboplatin); repeat for a second cycle after recovery of granulocyte and platelet counts or 400 mg/m2/day (beginning on cycle 3) on days 1, 2, and 3, with peripheral blood stem cell support, administered at 14- to 21-day intervals (in combination with carboplatin) for 3 cycles
小兒調整劑量
腎功能調整劑量
1. CrCl >50 mL/minute: No adjustment required.
2. CrCl 15 to 50 mL/minute: Administer 75% of dose
3. CrCl <15 mL minute: Data not available; consider further dose reductions
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling.
安定性
注射給藥指引
給藥途徑
IV
靜脈輸注液
NS, D5W
每瓶稀釋液體積
注射濃度
0.2-0.4 mg/ml
給藥速率
Administer standard doses over at least 30 to 60 minutes to minimize the risk of hypotension.