Efficacy and safety of amlodipine in hypertensive patients with renal dysfunction.

Amlodipine, a dihydropyridine calcium antagonist, was administered at 2.5-5.0 mg/day for 8 weeks to 35 hypertensive patients with renal dysfunction, and its efficacy and safety were evaluated. The target reduction in blood pressure was achieved in 28 of the 35 patients (80%), while blood pressure was decreased in 4 patients (11.4%) and unchanged in 3 patients (8.6%). A side effect of mild headache was reported by one patient (2.9%). In addition, abnormal changes in laboratory values were observed in five patients, but all of the changes were mild. Blood urea nitrogen and serum creatinine levels both increased in two of these five patients, and serum creatinine levels increased in another two patients. Serum amlodipine concentration was 4.86 +/- 2.57 ng/ml (n = 8) and 3.01 +/- 1.02 ng/ml (n = 8) in patients receiving a daily dose of 2.5 mg for 2-5 weeks and 8-10 weeks, respectively. Serum concentration in patients receiving 5 mg from Weeks 2-6 was 9.72 +/- 6.89 ng/ml (n = 6) after 7-9 weeks, suggesting no tendency for the accumulation of this drug. The drug was rated as of clinical benefit in 27 of the 35 patients (77.1%), and as slightly beneficial in another 5 patients (14.3%). Thus, amlodipine significantly decreased the blood pressure while causing little or no aggravation of renal dysfunction in hypertensive patients with renal impairment.

Clinical efficacy of carvedilol in severe hypertension.

In an open clinical study, the efficacy and safety of carvedilol was investigated in 26 severely hypertensive patients controlled inadequately on a diuretic [diastolic blood pressure (DBP) greater than 120 mm Hg at first visit and greater than 110 mm Hg following more than 1 week administration of a diuretic]. Following diuretic treatment all patients were initially administered 5 mg of carvedilol once daily. The dose was gradually increased to 10 mg and 20 mg until DBP was reduced below 100 mm Hg or until it was reduced by at least 10 mm Hg. Antihypertensive activity of carvedilol (5 mg) was sufficient in only three cases, but after 4 weeks (inpatients) or 8 weeks (outpatients) administration of carvedilol (10 mg or 20 mg), DBP/systolic blood pressure was significantly reduced from 176 +/- 6/117 +/- 3 to 145 +/- 3/94 +/- 2 mm Hg (p less than 0.001) in all patients. Overall, a sufficient antihypertensive effect was observed in 80% of the patients. Heart rate was significantly decreased from 76 +/- 2 to 67 +/- 2 beats/min, but no patient experienced bradycardia. Carvedilol was generally well tolerated. These findings suggest that 10-20 mg of carvedilol once daily, in combination with a diuretic, is an effective and safe treatment for patients with severe hypertension.