Vesell E S, Page J G
J Clin Invest. 1968 Dec;47(12):2657-63. doi: 10.1172/JCI105949.
The mean half-life of dicumarol in the plasma of seven sets of identical and seven sets of fraternal twins after a single oral dose of 4 mg/kg was 43.6+/-SD 17.9 hr. Half-lives ranged from 7 to 74 hr in these 28 normal adults not receiving other drugs for 2 wk preceding dicumarol administration. Large differences among unrelated individuals in dicumarol half-life disappeared almost completely in identical twins, but persisted to some extent in most sets of fraternal twins. These results indicate that marked differences among subjects in dicumarol half-life are under genetic rather than environmental control. Reproducibility of values for dicumarol half-life was demonstrated. A direct relationship between the dose and the half-life of dicumarol occurred in unrelated volunteers administered progressively larger doses at 10-day intervals. Dose dependence of the half-life of a drug results in increased variability of half-life and hence in greater risks of toxicity on long-term therapy. Risks of toxicity on the one hand and of failure to anticoagulate adequately on the other can be reduced by determining dicumarol half-life before starting long-term therapy. Half-lives for dicumarol and phenylbutzone tended to be correlated in the 28 twins, but no correlation occurred between dicumarol and antipyrine half-lives.
在单次口服4mg/kg剂量后,7组同卵双胞胎和7组异卵双胞胎血浆中双香豆素的平均半衰期为43.6±标准差17.9小时。在这28名未服用其他药物且在服用双香豆素前2周未服药的正常成年人中,半衰期范围为7至74小时。在不相关个体中双香豆素半衰期的巨大差异在同卵双胞胎中几乎完全消失,但在大多数异卵双胞胎组中仍有一定程度的存在。这些结果表明,双香豆素半衰期在受试者之间的显著差异受遗传而非环境控制。双香豆素半衰期值具有可重复性。在不相关的志愿者中,每隔10天给予逐渐增加的剂量,双香豆素的剂量与半衰期之间存在直接关系。药物半衰期的剂量依赖性导致半衰期变异性增加,因此长期治疗中毒风险更大。通过在开始长期治疗前测定双香豆素半衰期,一方面可以降低中毒风险,另一方面可以降低抗凝不足的风险。在这28对双胞胎中,双香豆素和保泰松的半衰期往往相关,但双香豆素和安替比林的半衰期之间没有相关性。