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转化酶抑制剂、钙通道阻滞剂和利尿剂的临床药理学。

Clinical pharmacology of converting enzyme inhibitors, calcium channel blockers and diuretics.

作者信息

Sinaiko A R

机构信息

Department of Pediatrics, University of Minnesota Medical School, Minneapolis 55455.

出版信息

J Hum Hypertens. 1994 May;8(5):389-94.

PMID:8064788
Abstract

The predominant trend in pediatric antihypertensive management is towards increasing reliance on angiotensin converting enzyme (ACE) inhibitors and calcium channel blockers because of their general effectiveness, low incidence of adverse reactions and potential specific benefit in patients with renal disease. The common aetiological relationship between renal disease and elevated BP also is the reason that diuretic therapy continues to be included in many treatment regimens. A number of ACE inhibitors are available for clinical use, although only captopril has been subjected to any meaningful degree of investigation in children. Initial doses of captopril are 0.5 mg/kg in children > 6 months of age and 0.01-0.1 mg/kg in neonates, because of an apparent increased antihypertensive effect and duration of action in this age group. Side-effects are few and the major adverse effect is a reduction in glomerular filtration in patients with bilateral renal artery stenosis. The calcium channel blockers reduce cytosolic calcium concentration and are particularly effective in patients with volume dependent forms of hypertension. The pharmacokinetic properties of these drugs are similar with drug clearance by hepatic metabolism. In particular, nifedipine has a rapid onset of action and is widely used to treat hypertensive emergencies. Although it has been used sublingually, the effectiveness of the drug is due to absorption from the gastrointestinal tract. Few side-effects from these drugs have been reported in children. Heart rate and cardiac output increase but return to pretreatment levels within a few weeks. As is the case with the ACE inhibitors, calcium channel blockers appear to have a positive effect on renal function.

摘要

小儿高血压治疗的主要趋势是越来越依赖血管紧张素转换酶(ACE)抑制剂和钙通道阻滞剂,因为它们总体疗效好、不良反应发生率低,且对肾病患者可能有特定益处。肾病与血压升高之间常见的病因关系也是利尿剂疗法仍被纳入许多治疗方案的原因。有多种ACE抑制剂可供临床使用,不过在儿童中仅对卡托普利进行过有一定意义程度的研究。6个月以上儿童卡托普利的初始剂量为0.5mg/kg,新生儿为0.01 - 0.1mg/kg,因为该年龄组的降压效果和作用持续时间明显增加。副作用较少,主要不良反应是双侧肾动脉狭窄患者的肾小球滤过率降低。钙通道阻滞剂可降低胞质钙浓度,对容量依赖性高血压患者特别有效。这些药物的药代动力学特性相似,通过肝脏代谢清除药物。特别是硝苯地平起效迅速,广泛用于治疗高血压急症。虽然它曾被舌下含服,但药物的有效性是由于从胃肠道吸收。儿童中这些药物的副作用报道较少。心率和心输出量增加,但在几周内会恢复到治疗前水平。与ACE抑制剂一样,钙通道阻滞剂似乎对肾功能有积极作用。

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