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地高辛用于充血性心力衰竭马匹的药代动力学

Pharmacokinetics of digoxin administered to horses with congestive heart failure.

作者信息

Sweeney R W, Reef V B, Reimer J M

机构信息

Department of Clinical Studies, New Bolton Center, University of Pennsylvania School of Veterinary Medicine, Kennett Square 19348.

出版信息

Am J Vet Res. 1993 Jul;54(7):1108-11.

PMID:8368606
Abstract

Nine horses with (naturally acquired) congestive heart failure were treated with 2.2 micrograms of digoxin/kg of body weight by the IV route, followed by 11 micrograms/kg administered orally every 12 hours thereafter. Furosemide was administered IV concurrently with IV administered digoxin every 12 hours. Serum concentration of digoxin was measured after the first (IV) and seventh (orally administered) dose. After IV administration, digoxin disposition was described by a 2-compartment model, with a rapid distribution phase (t1/2 alpha = 0.17 hour), followed by a slower elimination phase (beta = 0.096 +/- 0.055 h-1, t1/2 beta = 7.2 hours, where beta is the exponential term from the elimination phase of the concentration vs time curve). Bioavailability after oral administration was 21.2 +/- 10.8%. After the seventh orally administered dose, serum concentration of digoxin peaked 1 to 2 hours later, and was 1.9 +/- 0.7 ng/ml (mean +/- SD). In 4 horses, a second increase in serum digoxin concentration was observed 4 to 8 hours after the initial peak, which possibly was evidence of enterohepatic recycling of the drug. Response to treatment included reduction in heart rate, peripheral edema, and pulmonary edema, but these could not be attributed to the digoxin alone because the horses were treated concurrently with furosemide.

摘要

对9匹(自然发生)充血性心力衰竭的马匹,通过静脉途径给予2.2微克/千克体重的地高辛,随后每12小时口服给予11微克/千克。每12小时静脉注射速尿,与静脉注射的地高辛同时给药。在首次(静脉)和第七次(口服)给药后测量地高辛的血清浓度。静脉给药后,地高辛的处置可用二室模型描述,有一个快速分布相(t1/2α = 0.17小时),随后是一个较慢的消除相(β = 0.096 +/- 0.055 h-1,t1/2β = 7.2小时,其中β是浓度-时间曲线消除相的指数项)。口服给药后的生物利用度为21.2 +/- 10.8%。在第七次口服给药后,地高辛的血清浓度在1至2小时后达到峰值,为1.9 +/- 0.7纳克/毫升(平均值 +/- 标准差)。在4匹马中,在初始峰值后4至8小时观察到血清地高辛浓度再次升高,这可能是药物肝肠循环的证据。治疗反应包括心率降低、外周水肿和肺水肿减轻,但这些不能仅归因于地高辛,因为这些马匹同时接受了速尿治疗。

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