A Clinical Study on Cicletanine Monotherapy in Patients with Mild to Moderate Essential Hypertension

ABSTRACT

BACKGROUND: Cicletanine is a new antihypertensive agent, derived from the furopyridine family. It acts directly on vascular smooth muscle by increasing prostacyclin synthesis and decreasing intracytosolic calcium. In order to investigate the efficacy and safety of cicletanine, a clinical study was performed in the patients with mild to moderate essential hypertension. METHOD: The study subject consisted of 30 patients with diastolic blood pressure of 95mmHg~114mmHg(mean age 55.1+/-7.9 years, 13 males and 17 females). Cicletanine was administrated orally in a daily dose of 100mg Q.D. for 12 weeks after the administration of a placebo for 2 weeks. During cicletanine medication, antihypertensive efficacy, clinical side effects and laboratory changes were monitored. RESULT: Cicletanine decreased mean blood pressure from the baseline value of 123.6+/-3.4mmHg to 108.6+/-7.5mmHg(p<0.001) after 2 weeks, 105.0+/-7.4mmHg after 4 weeks, 103.9+/-6.6mmHg after 6 weeks, 102.5+/-8.9mmHg after 8 weeks, 101.4+/-6.8mmHg after 10 weeks and 99.6+/-6.6mmHg after 12 weeks of medication. There was a highly significant decrease in blood pressure at each of the assessments after 2,4,6,8,10 and 12 weeks of medication when compared to the baseline value(p<0.001). Mean blood pressure after 4 weeks of medication showed a significant decrease when compared to the value after 2 weeks of medication, and the value after 12 weeks of medication showed a significantly decrease when compared to the value after 8 weeks of medication. Heart rate did not change significantly with cicletanine monotherapy for 12 weeks. There was no significant changes in blood chemistry, glucose, lipid and electrolytes. The side effect was pruritus(1 case, 3.3%). CONCLUSION: Cicletanine monotherapy with 100mg once a day regimen was effective and well tolerated in the patients with mild to moderate essential hypertension.