Pharmacokinetics of intra-arterial chemotherapy.
Pharmacokinetics of intra-arterial chemotherapy.
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动脉内化疗的药代动力学。
DOI：
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发表时间：
1983
期刊：
影响因子：
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通讯作者：
F. Stephens
中科院分区：
文献类型：
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作者：
F. Stephens
晚期或侵袭性但局限性的恶性肿瘤通常可以通过使用“基础化疗”减少到更可治愈的比例，即在确定性放疗和/或手术切除之前使用化疗作为第一治疗模式。在使用抗癌剂时，采用利用癌细胞与正常组织和细胞之间的差异的药物组合、给药时机和方法。一个经常被忽视的可利用的差异是局部肿瘤通常由一条动脉供血的事实;这可以被插管，使得所使用的药剂可以以高浓度选择性地递送到包含肿瘤的区域。通过动脉内输注局部递送药物的优点取决于输注的动脉的大小、所用药剂的排泄或解毒速率、输注进入组织的药剂的量（特别是从第一循环）、以及特别是进入组织的对肿瘤细胞具有生物活性的药剂的量。考虑到所有这些因素，数学计算表明，在最坏的可能情况下，动脉内输注抗癌剂的区域有效性应至少是静脉内给药的1.8倍。在大多数情况下，使用大多数代理时，优势将明显大于此。这些计算得到了文献中的证据以及动脉内给药药物的更大区域效应（尽管具有毒性）的观察结果的支持。这些影响包括输注动脉分布区域的毛发脱落更明显，输注动脉分布区域的皮肤和粘膜溃疡增加。使用动脉内输注递送的缺点是需要住院治疗。因此，应进行适当对照的随机临床试验，以比较动脉内和静脉内化疗给药的临床结果。
Advanced or aggressive, but localised, malignancies can often be reduced to more curable proportions by the use of "basal chemotherapy", that is, using chemotherapy as the first mode of treatment, prior to definitive radiotherapy and/or surgical excision. In using anticancer agents, drug combinations, timing and methods of administration are employed which exploit differences between cancer cells and normal tissues and cells. One exploitable difference which is often overlooked is the fact that localised tumour is often supplied with blood by one artery; this can be cannulated so that the agents used can be delivered selectively in high concentration to the region containing the tumour. The advantage in delivering drugs regionally by intra-arterial infusion depends upon the size of the artery infused, the rate of excretion or detoxification of the agents used, the amount of the agent infused entering the tissues - especially from the first circulation, and especially the amount of agent entering the tissues which is biologically active against tumour cells. Taking all these factors into account, mathematical calculations indicated that under the worst possible circumstances infusion of anticancer agents intra-arterially should be at least 1.8 times more effective regionally than intravenous administration. In most situations and with most agents used the advantage would be significantly greater than this. These calculations are supported by evidence in the literature and by observations of a greater regional effect, albeit toxic, of intra-arterial administration of the agents. These effects include more pronounced loss of hair in the region of distribution of the artery infused, and increased skin and mucosal ulceration in the distribution of the artery infused. The disadvantage of using intra-arterial infusion delivery is the need for hospitalisation. Therefore, properly controlled, randomised clinical trials should be conducted to compare clinical results of intra-arterial and intravenous chemotherapy administration.