Scholtysik G, Fetkovská N
Preclinical Research, Sandoz Ltd., Basel, Switzerland.
Cor Vasa. 1987;29(4 Suppl 1):11-6.
The pharmacologic data obtained from animal experiments and pharmacokinetics of guanfacine in man are reviewed. Guanfacine exhibits a high selectivity for alpha 2-adrenoceptors with predominantly central action, but peripheral presynaptic alpha 2-adrenoceptor stimulation may also contribute to the antihypertensive effect. Guanfacine has the advantage over other centrally acting antihypertensives of being less sedative and causing no rebound hypertension after discontinuation of treatment. The latter is mainly due to its pharmacokinetic properties. Human pharmacokinetic studies in patients with renal failure indicate that due to an increase in metabolic clearance and increase in non-renal elimination of the drug guanfacine may be administered to elderly patients and patients with renal impairment without dosage adjustment.
本文综述了胍法辛在动物实验中获得的药理学数据及其在人体中的药代动力学。胍法辛对α2-肾上腺素能受体具有高度选择性，主要发挥中枢作用，但外周突触前α2-肾上腺素能受体刺激也可能有助于其降压效果。与其他中枢性抗高血压药物相比，胍法辛具有较少镇静作用且停药后不引起反跳性高血压的优势。后者主要归因于其药代动力学特性。对肾衰竭患者的人体药代动力学研究表明，由于药物代谢清除率增加和非肾清除增加，胍法辛可用于老年患者和肾功能损害患者，无需调整剂量。
