A safe method for rapidly achieving plasma concentration plateaus
A safe method for rapidly achieving plasma concentration plateaus
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快速达到血浆浓度平台的安全方法
DOI：
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发表时间：
1974
期刊：
影响因子：
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通讯作者：
J. Wagner
中科院分区：
文献类型：
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作者：
J. Wagner
经典的做法是静脉注射负荷量，同时以恒定的速度开始输液，这可能是危险的，或者会导致某些药物的毒性。在这种情况下，初始血浆浓度(CO1)与稳态血浆浓度(CEQ1)的比值往往很大。组织中药物/血浆中药物的比例越高(即药物越“二室”)，CO_1/CEQ_1的比率就越高。提出了一种方法，在该方法中，最初以Q1的速率进行恒速输液，持续时间为T小时(0.25至3小时)；然后突然将速率改变为较低的Q2，只要需要稳定状态就保持该速率。给出了一个简单的关系式，说明了当停止较高输注速率时，Q1Q2的比值必须是什么，才能最快地达到稳态，并使CMAX1C/CEQ的比值最小化，其中CMAX1是在时间T时达到的最大血浆浓度。给出了一个简单的线性图，它允许快速确定给定药物所需的比率Q1Q2。使用该方法所需的变量是血浆清除度和血浆半衰期。
The classical procedure of administering a loading dose as a bolus intravenous iniection and at the same time starting an infusion at a constant rate could be dangerous or lead to toxicity with certain drugs. Under such conditions the ratio of the initial plasma concentration (Co1) to the steady‐state plasma concentration (Ceq1) is often large. The higher the ratio of drug in tissues/drug in plasma (i.e., the more "two compartment" the drug is) the higher will be the Co1/Ceq1ratio. A method is proposed in which initially a constant‐rate infuSion at the rate of Q1 is given over T hours (0.25 to 3 hr); then the rate is abruptly changed to a lower rate Q 2 which is maintained as long as steady state is desired. A simple relationship is given that shows what the ratio of Q1Q2 must be to attain steady state most rapidly and to minimize the ratio CMAX1C/Ceq where CMAX1 is the maximum plasma concentration attained at time T, iust as the infusion at the higher rate ceases. A simple linear graph is given that allows rapid determination of the needed ratio Q 1Q 2 Variables needed for a given drug to use the method are plasma clearance and plasma half‐life.