Schaller M D, Nussberger J, Waeber B, Porchet M, Brunner H R
JAMA. 1985 Jan 11;253(2):233-5.
The antihypertensive effect of clonidine hydrochloride delivered at a constant rate for seven days by transdermal disks was evaluated in seven patients with essential hypertension. Blood pressure values measured at the physician's office were not significantly decreased by one month of treatment with one (n = 2) or two (n = 5) once-weekly applied clonidine transdermal disks. In contrast, blood pressure values recorded during patients' customary daily activities by means of a portable blood pressure recorder were considerably reduced, from 159/97 +/- 2/2 to 136/76 +/- 7/5 mm Hg. Plasma drug concentration at the end of the fourth week averaged 1.22 +/- 0.24 ng/mL. Plasma renin, vasopressin, and epinephrine levels were not modified by clonidine, whereas plasma norepinephrine level was significantly reduced. Local skin erythema developed in three patients and dry mouth in six. These findings suggest that clonidine transdermal disks lower blood pressure in hypertensive patients, but produce local skin lesions and general side effects.
通过透皮贴剂持续七天给予盐酸可乐定,对七名原发性高血压患者的降压效果进行了评估。使用每周一次的可乐定透皮贴剂治疗一个月后,在医生办公室测量的血压值,使用一片(n = 2)或两片(n = 5)时均未显著降低。相比之下,通过便携式血压记录仪记录的患者日常活动期间的血压值则显著降低,从159/97 +/- 2/2降至136/76 +/- 7/5 mmHg。第四周结束时血浆药物浓度平均为1.22 +/- 0.24 ng/mL。可乐定未改变血浆肾素、血管加压素和肾上腺素水平,而血浆去甲肾上腺素水平显著降低。三名患者出现局部皮肤红斑,六名患者出现口干。这些发现表明,可乐定透皮贴剂可降低高血压患者的血压,但会产生局部皮肤病变和全身副作用。