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年龄对单独使用左旋多巴以及在卡比多巴存在情况下左旋多巴药代动力学的影响。

The effect of age on the pharmacokinetics of levodopa administered alone and in the presence of carbidopa.

作者信息

Robertson D R, Wood N D, Everest H, Monks K, Waller D G, Renwick A G, George C F

机构信息

Clinical Pharmacology Group, University of Southampton, Southampton General Hospital.

出版信息

Br J Clin Pharmacol. 1989 Jul;28(1):61-9. doi: 10.1111/j.1365-2125.1989.tb03506.x.

Abstract
  1. The effect of age on the pharmacokinetics of levodopa administered alone and in the presence of carbidopa was investigated in young and elderly healthy volunteers. 2. The plasma clearance of levodopa following intravenous administration of 50 mg was 14.2 +/- 2.8 (s.d.) ml min-1 kg-1 in the elderly compared with 23.4 +/- 4.1 ml min-1 kg-1 in the young (P less than 0.01) which resulted in a 49% greater area under the plasma concentration-time curve (AUC) in the older subjects (P less than 0.01). The volume of distribution (Vss) was lower in the elderly (1.01 +/- 0.29 l kg-1) than in the young (1.65 +/- 0.39 l kg-1) (P less than 0.002). 3. Following oral administration of 250 mg of levodopa the AUC was 2512 +/- 588 ng ml-1h in the elderly compared with 1056 +/- 282 ng ml-1h in the young (P less than 0.002). Cmax was also significantly greater in the elderly (P less than 0.05). The bioavailability of levodopa was significantly greater in the elderly (0.63 +/- 0.12 compared with 0.41 +/- 0.16, P less than 0.01). 4. In the presence of carbidopa, the plasma clearance of intravenous levodopa (50 mg) was reduced in both age groups but remained lower in the elderly (5.8 +/- 0.9 ml min-1 kg-1 compared with 9.3 +/- 1.0 ml min-1 kg-1; P less than 0.01). This resulted in a 54% greater AUC in the older subjects (P less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)
摘要
  1. 在年轻和老年健康志愿者中,研究了年龄对单独使用左旋多巴以及在卡比多巴存在情况下左旋多巴药代动力学的影响。2. 静脉注射50毫克左旋多巴后,老年人的血浆清除率为14.2±2.8(标准差)毫升/分钟/千克,而年轻人为23.4±4.1毫升/分钟/千克(P<0.01),这导致老年受试者血浆浓度-时间曲线下面积(AUC)比年轻人高49%(P<0.01)。老年人体内分布容积(Vss)(1.01±0.29升/千克)低于年轻人(1.65±0.39升/千克)(P<0.002)。3. 口服250毫克左旋多巴后,老年人的AUC为2512±588纳克/毫升/小时,而年轻人为1056±282纳克/毫升/小时(P<0.002)。老年人的Cmax也显著更高(P<0.05)。左旋多巴在老年人中的生物利用度显著更高(分别为0.63±0.12和0.41±0.16,P<0.01)。4. 在卡比多巴存在的情况下,两个年龄组静脉注射左旋多巴(50毫克)后的血浆清除率均降低,但老年人仍然更低(分别为5.8±0.9毫升/分钟/千克和9.3±1.0毫升/分钟/千克;P<0.01)。这使得老年受试者的AUC高54%(P<0.01)。(摘要截断于250字)

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