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庆大霉素、新霉素和土霉素在新生犊牛体内的比较药代动力学

Comparative pharmacokinetics of gentamicin, neomycin and oxytetracycline in newborn calves.

作者信息

Burrows G E, Barto P B, Martin B

出版信息

J Vet Pharmacol Ther. 1987 Mar;10(1):54-63. doi: 10.1111/j.1365-2885.1987.tb00077.x.

Abstract

The pharmacokinetics of three antibiotics--gentamicin, neomycin and oxytetracycline were determined in newborn calves. The kinetic determinations, using two-compartment open models, were made at increasing ages from 1 day to 42 days and compared with those made from older calves (250+ days). Although all three antibiotics are eliminated unchanged primarily by glomerular filtration, there were marked differences in the development of elimination processes for individual drugs. The pharmacokinetics of neomycin were not influenced by age. Although the elimination half-life of gentamicin appeared to decrease with age, the changes were not significant and were due to an increased elimination rate in only one calf. There was no change with age in the remaining three calves. Oxytetracycline elimination was significantly reduced in newborn calves. This was exemplified by a decrease in the half-life of elimination t1/2 (beta) from 672.5 +/- 99.4 in the newborn to 385.6 +/- 76.8 at 6 weeks of age, and 377.3 +/- 40.8 min in the 250-day-old calf. These changes were consistent in all four calves. The rate of elimination remained low for the first 4 weeks of life. The volume of distribution Vd, area was not changed after the first week of life. Based on pharmacokinetic changes, an adjustment of dosage is indicated for oxytetracycline in the newborn calf as compared to the older calf or adult.

摘要

在新生犊牛中测定了三种抗生素——庆大霉素、新霉素和土霉素的药代动力学。采用二室开放模型,在1日龄至42日龄的犊牛中随着年龄增长进行动力学测定,并与年龄较大的犊牛(250日龄以上)的测定结果进行比较。尽管所有三种抗生素主要通过肾小球滤过以原形排出,但个别药物的排泄过程发展存在显著差异。新霉素的药代动力学不受年龄影响。虽然庆大霉素的消除半衰期似乎随年龄降低,但变化不显著,且仅在一头犊牛中是由于消除速率增加所致。其余三头犊牛的消除半衰期未随年龄变化。新生犊牛中土霉素的消除显著减少。这表现为消除半衰期t1/2(β)从新生犊牛的672.5±99.4分钟降至6周龄时的385.6±76.8分钟,以及250日龄犊牛的377.3±40.8分钟。所有四头犊牛的这些变化都是一致的。在出生后的前4周内消除速率一直较低。分布容积Vd、面积在出生后第一周后没有变化。基于药代动力学变化,与年龄较大的犊牛或成年牛相比,新生犊牛中土霉素的剂量需要调整。

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