Burris J F, Mroczek W J
Pharmacotherapy. 1986 Jan-Feb;6(1):30-4. doi: 10.1002/j.1875-9114.1986.tb03447.x.
This study assessed the antihypertensive efficacy and side effects of clonidine administered transdermally. Twenty-five patients with mild to moderate essential hypertension (seated diastolic blood pressure 95-120 mm Hg with diuretic therapy alone) controlled with oral diuretic plus oral clonidine were enrolled. Transdermal clonidine was substituted for oral clonidine and titrated until adequate blood pressure control (seated diastolic blood pressure less than 90 mm Hg) was attained. At the end of titration, seated morning blood pressure averaged 129/90 +/- 15/5 mm Hg (mean +/- standard deviation) compared to 136/96 +/- 13/7 mm Hg (p less than 0.01/0.001) during oral clonidine administration. Standing morning blood pressure was also lower during transdermal than oral therapy (131/94 +/- 16/5 vs 136/99 +/- 14/7, p less than 0.05/0.001). Afternoon blood pressures (at peak effect of oral dose) were virtually identical during oral and transdermal therapy in both seated and standing positions. Typical side effects of oral clonidine, including dry mouth, drowsiness, and sexual dysfunction, were reduced during transdermal therapy. There was less morning-to-afternoon variability of blood pressure control and plasma clonidine concentrations during transdermal than during oral therapy. One patient left the study because of drowsiness and two because of skin reactions to the transdermal skin patch. Mild transient local skin irritation occurred frequently. Transdermal clonidine plus a diuretic is an effective treatment for mild to moderate essential hypertension, improves compliance and reduces side effects of therapy.
本研究评估了经皮给予可乐定的降压疗效及副作用。入选了25例轻度至中度原发性高血压患者(仅接受利尿剂治疗时坐位舒张压为95 - 120 mmHg),这些患者通过口服利尿剂加口服可乐定进行控制。将经皮可乐定替代口服可乐定并进行滴定,直至达到充分的血压控制(坐位舒张压低于90 mmHg)。滴定结束时,坐位晨起血压平均为129/90±15/5 mmHg(均值±标准差),而口服可乐定治疗期间为136/96±13/7 mmHg(p<0.01/0.001)。经皮治疗时站立位晨起血压也低于口服治疗(131/94±16/5 vs 136/99±14/7,p<0.05/0.001)。口服和经皮治疗期间,坐位和站立位的下午血压(口服剂量达到峰值效应时)实际上相同。经皮治疗期间,口服可乐定的典型副作用,包括口干、嗜睡和性功能障碍有所减轻。与口服治疗相比,经皮治疗期间血压控制和血浆可乐定浓度的晨起至下午变异性较小。1例患者因嗜睡退出研究,2例因对经皮贴片有皮肤反应退出。轻度短暂的局部皮肤刺激频繁发生。经皮可乐定加利尿剂是治疗轻度至中度原发性高血压的有效方法,可提高依从性并减少治疗的副作用。