可乐定在患者体内的药代动力学及其与降压效果的关系。
Pharmacokinetics of clonidine and its relation to the hypotensive effect in patients.
作者信息
Frisk-Holmberg M, Edlund P O, Paalzow L
出版信息
Br J Clin Pharmacol. 1978 Sep;6(3):227-32. doi: 10.1111/j.1365-2125.1978.tb04589.x.
Abstract
1 The kinetics of clonidine and its relation to the blood pressure response after single intravenous doses of 75 micrograms--275 micrograms in hypertensive patients were determined. 2 Clonidine disposition could be described by a two compartment open model and pharmacokinetic parameters show a rapid distribution phase of 20--30 min and a mean plasma clearance of 4.6 ml min-1 kg-1 (75--200 microgram). The half-life of the beta-phase was found to be in the range of 7.4--11.4 h. Indications of dose dependent kinetics were obtained. 3 A dose-dependent decrease in blood pressure was obtained. 4 The maximal reduction in MAP (mean arterial blood pressure) was significantly (P less than 0.01) related to plasma concentrations of clonidine. 5 The reduction in MAP was always related to plasma concentrations of clonidine (r = 0.88, P less than 0.01) when pseudoequilibrium of distribution of the drug was achieved.
摘要
- 测定了高血压患者单次静脉注射75微克至275微克可乐定后的动力学及其与血压反应的关系。2. 可乐定的处置可用二室开放模型描述，药代动力学参数显示快速分布相为20至30分钟，平均血浆清除率为4.6毫升/分钟/千克（75至200微克）。发现β相半衰期在7.4至11.4小时范围内。获得了剂量依赖性动力学的指征。3. 获得了剂量依赖性的血压下降。4. 平均动脉血压（MAP）的最大降幅与可乐定的血浆浓度显著相关（P<0.01）。5. 当药物分布达到假平衡时，MAP的降低始终与可乐定的血浆浓度相关（r = 0.88，P<0.01）。
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