药理学和临床使用moxonidine,一个新的集中作用阻滞交感神经的抗高血压药。
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普里查德BN,欧文斯CW,格雷厄姆BR
药理学和临床使用moxonidine,一个新的集中作用阻滞交感神经的抗高血压药。
J哼Hypertens。1997年8月,11增刊1:S29-45。
- PubMed ID
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9321737 (在PubMed]
- 文摘
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Moxonidine集中作用抗高血压。它的动作是由咪唑啉I1受体位于延髓吻ventro-lateral (RVLM)。动物实验显示多少量需要降低血压(BP)时由于脑池内的,或者直接注入RVLM,而静脉注射剂量。显微镜下注射的抗高血压作用的moxonidine到RVLM自发性高血压鼠(月)被预处理与咪唑啉I1 efaroxan封锁,但α(2)从86466年SKF封锁少得多的效果。同样的BP月从静脉moxonidine逆转的显微镜下注射efaroxan RVLM。受体结合的研究表明moxonidine结合I1咪唑啉受体的亲和力三十三倍更有效比α(2)受体结合,而对于可乐定的区别仅仅是四倍。Moxonidine降低肾上腺素、去甲肾上腺素和肾素水平的人,找到符合中央抑制同情的语气。急性血液动力学的研究表明,moxonidine导致BP秋天由于全身血管阻力下降,而心率、心输出量、中风体积和肺动脉压力不受影响。左心室收缩末期和舒张期量减少。左心室肥大被发现与moxonidine 6个月治疗后回归。 After oral administration Tmax is about 1 h, bioavailability approaches 90%. Moxonidine is mostly excreted unchanged, biotransformation is unimportant. The T1/2 is 2.5 h, which is prolonged by renal insufficiency. However, suggesting possible retention in the central nervous system (CNS), the antihypertensive effect lasts longer than would be expected from the half-life, as moxonidine is suitable for once daily administration. Moxonidine is an effective antihypertensive agent. It has been compared with representatives from each important class of antihypertensive drugs, with clonidine, diuretics, both alpha- and beta-blocking drugs, calcium antagonists and ACE inhibitors. BP control has been similar with moxonidine and these other agents. The side effect profile of moxonidine is favourable, its lack of effect on central alpha(2) receptors is important in this regard.
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