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头孢曲松药代动力学的年龄相关变化。

Age-associated changes in ceftriaxone pharmacokinetics.

作者信息

Hayton W L, Stoeckel K

出版信息

Clin Pharmacokinet. 1986 Jan-Feb;11(1):76-86. doi: 10.2165/00003088-198611010-00005.

Abstract

Ceftriaxone pharmacokinetic parameters were compiled from recent publications. The subjects (27 female, 93 male) were from 1 day to 92 years old and appeared to have normal renal and hepatic function. In 1- to 8-day-old neonates, the half-life averaged 19 hours; it declined to 6.3 hours in 1- to 6-year-old subjects and then increased gradually throughout the remainder of the life-span to 14 hours in 75- to 92-year-old subjects. The age-associated changes in half-life appeared to result from changes in systemic clearance. The fraction of the dose eliminated renally averaged 70% in neonates and declined throughout childhood to 40 to 60% in adults, in whom it was age invariant. No clinically significant differences between males and females were detected in ceftriaxone kinetic parameter values. Plasma protein binding of ceftriaxone (100 mg/L) was about 70% in neonates and it increased throughout childhood to the adult value of 90 to 95%. To achieve a given free concentration of ceftriaxone, the same dosage per unit surface area can be used for children and adults, provided glomerular filtration and biliary secretion function are normal for age. Dosage should be reduced by as much as a factor of 5 in neonates less than 1 week of age and perhaps by a factor of 2 in the very old.

摘要

头孢曲松的药代动力学参数取自近期发表的文献。受试者(27名女性,93名男性)年龄从1天至92岁,肾功能和肝功能似乎正常。在1至8日龄的新生儿中,半衰期平均为19小时;在1至6岁的受试者中降至6.3小时,然后在整个剩余寿命期间逐渐增加,在75至92岁的受试者中达到14小时。半衰期与年龄相关的变化似乎是由全身清除率的变化引起的。经肾脏消除的剂量分数在新生儿中平均为70%,在整个儿童期下降,在成年人中为40%至60%,且在成年人中与年龄无关。在头孢曲松动力学参数值方面,未检测到男性和女性之间存在临床显著差异。头孢曲松(100mg/L)的血浆蛋白结合率在新生儿中约为70%,在整个儿童期增加至成年人的90%至95%。为达到给定的头孢曲松游离浓度,只要肾小球滤过和胆汁分泌功能在相应年龄正常,儿童和成年人可使用相同的单位表面积剂量。对于小于1周龄的新生儿,剂量应减少多达5倍,对于高龄者可能减少2倍。

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