Efficacy of Amosulalol HCI on Mild to Moderate Essential Hypertension

Ha, Jong Won; Chung, Namsik; Kwan, June; Lee, Moon Hyoung; Lee, Young Joon; Shim, Won Heum; Cho, Seung Yun; Kim, Sung Soon

Abstract

BACKGROUND
The most important hemodynamic disturbance in patients with hypertension is an increase in peripheral vascular resistance due to arteriolar constriction. The most desirable way to lower blood pressure is to decrease peripheral vascular resistance without any adverse effects to cardiovascular function. Accordingly, both alpha and beta-adrenoceptor antagonists are effective drugs for the treatment of hypertension. Amosulalol, a new drug which blocks both sympathetic nerve alpha and beta-receptors, has been developed.
METHODS
In order to investigate the efficacy and safety of oral amosulalol on essectial hypertension, a daily dodse of 20mg to 60mg amosulalol was administered in 31 hypertensive patients(male : 14, female : 17, mean age : 52.7+/-7.9) with diastolic blood pressure in the range of 95mmHg-120mmHg while off all other anti-hypertensive agents. Blood pressure and heart rate were measured every 2 weeks. The complete blood count, blood chemistry by SMA-12 and derum electrolytes and urinalysis were performed at entry, 1st and 8th week of therapy.
RESULTS
1) Baseline blood pressure after 2 weeks of placebo at sitting positing were 167.5+/-12.0/107.8+/-6.6mmHg. There was statistically significant reduction of blood pressure after 2 weeks treatment of amosulalol which was maintained up to 8 weeks(167.5+/-12.0/107.8+/-6.6mmHg vs 157.9+/-12.4/103.7+/-9.5mmHg, P<0.05). There was a significant reduction of systolic and diastolic pressures after the treatment when comparing the average value of two observation periods with that of treatment period(161.1+/-31.6/104.8+/-20.3mmHg vs 145.1+/-13.5/94.7+/-8.8mmHG, P<0.05). 2) The proportion of the patient who had a tendency to decline of bloop pressure after treatment with amosulalol was 94%. When considering the safety and efficacy, 94% of patients demonstrated to be safe and efficacious. 3) There was a significant decrease of heart rate after amosulalol without severe bradycardia(72.7+/-8.3/min vs 67.5+/-7.2/min, p<0.05). 4) There were no significant changes in blood chemistry, serum electrolytes. hematologic findings except two patients who showed slight bilirubin elevation over the treatment period. 5) One patient experienced dizziness that requires to discontinue the medication.
CONCLUSION
In patients with mild to moderate hypertension, twice daily amosulalol(20mg, 40mg and 60mg) provided significant anti-hypertensive effects without serious side effects.