I1咪唑啉受体激动剂。一般临床药理学的咪唑啉受体:对老年人的治疗。
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普里查德BN,格雷厄姆BR
I1咪唑啉受体激动剂。一般临床药理学的咪唑啉受体:对老年人的治疗。
衰老药物。2000年8月,17 (2):133 - 59。
- PubMed ID
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10984201 (在PubMed]
- 文摘
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近年来存在的证据积累了中央咪唑啉(I1)受体影响血压。虽然有一些争议,有人建议,可乐定对其降血压效果主要是通过激活咪唑啉I1延髓腹外侧的髓质受体,而其镇静效应是由中央alpha2-receptors激活。Moxonidine和rilmenidine 2咪唑啉化合物30倍比alpha2-receptors I1更大的特异性受体。相比之下,可乐定显示4倍为I1受体与alpha2受体特异性。Moxonidine rilmenidine降低血压,降低外周阻力。据报道他们降低循环儿茶酚胺水平和moxonidine降低高血压患者的交感神经活动。Moxonidine和rilmenidine适度降低血糖水平升高和Moxonidine一直在报道减少胰岛素抵抗高血压患者胰岛素抵抗。小减少血浆总胆固醇、低密度脂蛋白胆固醇和甘油三酯与rilmenidine已报告。moxonidine和rilmenidine口服后吸收和消除不变的肾脏。消除半衰期(t (1/2)) rilmenidine moxonidine是8和2小时,分别,但槽/血浆浓度峰值比率表明moxonidine可以每日服用一次,暗示可能的中枢神经系统保留。 As would be expected, t(1/2) values are increased in patients with reduced renal function, and in elderly individuals. Both drugs have been compared with established antihypertensive drugs from all the major groups. Studies, almost all of which were of a double-blind, parallel-group design, indicate that blood pressure control with moxonidine or rilmenidine is similar to that with established drugs, i.e. alpha-blocking drugs, calcium antagonists, ACE inhibitors, beta-blocking drugs and diuretic agents. There have been few studies conducted solely in elderly patients. However, evidence clearly suggests that the antihypertensive effect of the imidazoline compounds is not reduced in elderly patients. The overall adverse effect profile of moxonidine and rilmenidine compares reasonably with established agents. In accord with the receptor-binding studies, drowsiness and dry mouth are observed less often with these drugs than with other centrally acting drugs, although the symptoms occur more often than with placebo. An overshoot of blood pressure was seen when treatment with clonidine, but not moxonidine, was abruptly discontinued in conscious, spontaneously hypertensive rats. Clinical evidence of withdrawal reaction with moxonidine or rilmenidine is scant but caution should be observed pending more formal studies.
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