N,N-bis(2-chloroethyl)-1,3,2-oxazaphosphinan-2-amine 2-oxide
防治癌症
Absorption
Well absorbed orally. T max is 2 to 3 h for metabolites (IV dose).
Distribution
More than 75% bioavailable after oral administration. More than 60% of metabolites are bound to plasma proteins. Low protein binding for cyclophosphamide.
Metabolism
Converted to active alkylating metabolites in the liver.
Elimination
The t ½ is 3 to 12 h (unchanged drug). Eliminated primarily as metabolites. 5% to 25% is excreted in urine as unchanged drug.
Special Populations
Renal Function Impairment
Metabolites may be elevated but increased toxicity has not been seen.
Anticoagulants
Increased hypoprothrombinemic effect may occur.
Barbiturates, other enzyme inducers
May increase the rate of active cyclophosphamide metabolite formation and possibly increase neutropenic effects.
Chloramphenicol, other enzyme inhibitors
May inhibit cyclophosphamide's antineoplastic activity by decreasing rate of active metabolite formation.
Digoxin
May cause decreased serum levels of digoxin.
Oral quinolone antibiotics
May cause decreased GI absorption of quinolone antibiotics.
Succinylcholine and possibly mivacurium
Prolongation of neuromuscular blockade by cyclophosphamide's inhibition of pseudocholinesterase may occur.
2.骨髓功能嚴重受損者(尤其是曾以cytotoxic agent治療或接受放射性治療的病人)
3.膀胱炎。
4.尿道阻塞。
5.感染症(active infection)。
6.懷孕及授乳期。
1.白血球、血小板減少症。
2.骨髓之腫瘤細胞浸潤。
3.以前用X光治療過。
4.以前用其他的Cytatoxic agent治療過。
5.肝功能損害。
因為Endoxan有抑制免疫機轉之作用，病人如引起細菌、黴菌或病毒之感染應停藥或更改劑量，尤其是與類固醇藥物合併治療，有時會使病人死亡。在這些情況下，水痘-帶狀泡疹之感染尤其危險。
