Elimination half-life of drugs: value and limitations.
Elimination half-life of drugs: value and limitations.
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DOI：
10.1146/annurev.me.36.020185.002225
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发表时间：
1985
影响因子：
10.5
通讯作者：
D. Greenblatt
中科院分区：
文献类型：
--
作者：
D. Greenblatt
药物从血浆或血清中消除的半衰期长期以来被认为是一个熟悉的和重要的药理学性质。事实上，消除半衰期具有局限性，其价值被高估。消除半衰期是一个因变量，与分布容积直接相关，与清除率成正比。药物分布和清除率的变化可改变消除半衰期。半衰期作为单次给药后药物药理作用持续时间的预测指标也有局限性，这与分布的关系比与消除或清除的关系更大。在多次给药期间，消除半衰期在预测药物蓄积的速率和相对程度以及治疗终止后的洗脱速率方面确实具有价值。临床医生在评价药物的药代动力学特性时，除消除半衰期外，还应考虑分布容积和清除率。
A drug's half-life of elimination from plasma or serum has long been considered a familiar and important pharmacologic property. In fact, elimination half-life has limitations, and its value has been overestimated. Elimination half-life is a dependent variable, related directly to volume of distribution and inversely to clearance. Changes in drug distribution as well as in rate of clearance can alter elimination half-life. Half-life also has limitations as a predictor of a drug's duration of pharmacologic action after single doses, which is related more to distribution than to elimination or clearance. During multiple dosage, elimination half-life does have value in predicting the rate and relative extent of drug accumulation, as well as the rate of washout after termination of treatment. Clinicians should consider volume of distribution and clearance, in addition to elimination half-life, when evaluating the pharmacokinetic properties of drugs.