Seedat Y K
S Afr Med J. 1985 Apr 6;67(14):557-9.
The pharmacology of central alpha-adrenoceptor-stimulating agents is discussed, with particular reference to clonidine (Catapres; Boehringer Ingelheim) and guanfacine (Estulic; Sandoz), and their haemodynamic effects are compared and contrasted. The main differences between the effects of clonidine and guanfacine on hypertension are: guanfacine activates presynaptic alpha-adrenoceptors 10 times more selectively than clonidine; guanfacine has an alpha 2/alpha 1-selectivity ration 25 times higher than clonidine; clonidine decreases cardiac output and guanfacine decreases peripheral resistance, clonidine has no effect on stroke volume but guanfacine increases it; and when the clonidine withdrawal syndrome in the spontaneously hypertensive rat is compared with cessation of guanfacine treatment at an equipotent antihypertensive dose, the withdrawal syndrome after guanfacine appears later and is much less severe. Guanfacine may be preferable to clonidine as a central alpha-adrenoceptor stimulant in the treatment of hypertension.
本文讨论了中枢性α-肾上腺素能受体激动剂的药理学,特别提及可乐定(凯他乐;勃林格殷格翰公司)和胍法辛(宜思力;山德士公司),并对它们的血流动力学效应进行了比较和对比。可乐定和胍法辛对高血压的影响的主要差异在于:胍法辛对突触前α-肾上腺素能受体的激活选择性比可乐定高10倍;胍法辛的α2/α1选择性比可乐定高25倍;可乐定降低心输出量,胍法辛降低外周阻力,可乐定对每搏量无影响,而胍法辛可增加每搏量;当将自发性高血压大鼠的可乐定撤药综合征与等量降压剂量的胍法辛治疗停止后的情况进行比较时,胍法辛后的撤药综合征出现较晚且严重程度轻得多。在高血压治疗中,胍法辛作为中枢性α-肾上腺素能受体激动剂可能比可乐定更可取。