Levin V A, Kabra P M, Freeman-Dove M A
J Neurosurg. 1978 Apr;48(4):587-93. doi: 10.3171/jns.1978.48.4.0587.
A comparison of intravenous to intracarotid artery (ICA) administration of 14C-BCNU (1,3-bis(2-chloroethyl)-1-nitrosourea) was made in squirrel monkeys. Radioactivity was measured as soluble drug products and as RNA-, DNA-, and protein-bound radioactivity. The ICA administration of BCNU achieved 190% to 280% higher brain nucleic acid-bound drug levels than use of the intravenous route in the infused hemisphere and 130% to 280% higher levels than in the noninfused hemisphere. In addition, some brain regions directly subserved by the middle cerebral artery had bound drug levels four- to fivefold greater than those found in regions of noninfused brain. The data suggest that a need for BCNU dose reduction due to myelotoxicity may be an indication for ICA therapy in selected brain-tumour cases.
在松鼠猴身上对14C-卡莫司汀（1,3-双(2-氯乙基)-1-亚硝基脲）进行了静脉注射与颈内动脉给药的比较。放射性以可溶性药物产物以及与RNA、DNA和蛋白质结合的放射性来测量。卡莫司汀经颈内动脉给药后，在注入侧半球的脑核酸结合药物水平比静脉给药途径高190%至280%，在未注入侧半球比静脉给药途径高130%至280%。此外，大脑中动脉直接供血的一些脑区的结合药物水平比未注入脑区高四至五倍。数据表明，在某些脑肿瘤病例中，由于骨髓毒性而需要降低卡莫司汀剂量可能是颈内动脉治疗的一个指征。
