OVERVIEW OF CLINICAL SAFETY AND EFFICACY OF TERTATOLOL

Tertalolol is a noncardioselective beta-blocker, devoid of intrinsic s ympathomimetic activity. Its renal vasodilating properties have been d emonstrated both in animals and in man. The beta-blocking activity of tertatolol was assessed on the reduction of heart rate at submaximal e xercise. The oral dose of 5 mg was optimal, leading to a significant r eduction of diastolic blood pressure throughout 24 h. The efficacy was confirmed in mid- and long-term studies. In mid-term, randomized cont rolled studies, versus beta-blockers, the antihypertensive efficacy of tertatolol 5 mg was comparable to that of acebutolol 400 mg but of ea rlier onset, and comparable to that of atenolol 100 mg. Its efficacy w as confirmed in 3 long-term studies. In the first study, tertatolol 5 mg alone or combined with a diuretic and, if necessary, dihydralazine, controlled 93.6% of patients (supine DBP <90 mm Hg). 72.7% of patient s were controlled with tertatolol alone, 16.4% with tertatolol plus di uretic, and 4.5% with tertatolol plus diuretic and dihydralazine. In a second study, 88.5% of patients were controlled, 56.3% with tertatolo l alone and 32.2% with tertatolol plus diuretic. In the third study, 8 8.8% of patients were controlled after 1 year treatment, 66.1% with te rtatolol alone and 22.7% with tertatolol plus diuretic. The overall cl inical safety was excellent: only 6.6% of the 2,706 patients treated f or 1 year withdrew from the study because of side effects. In patients followed for 1 year, side effects were rare, transient and mostly of mild severity. Biochemical surveillance did not show any adverse metab olic effects of tertatolol. Conversely, in two long-term studies, crea tinine and cholesterol levels decreased significantly. When administer ed to normo- and hyperlipidemic hypertensive patients, tertatolol indu ced a moderate increase in triglyceride levels without any change in H DL-cholesterol levels or in the total cholesterol/HDL-cholesterol rati o. Tertatolol was also studied in hypertensive patients with risk fact ors. In patients with left ventricular hypertrophy, tertatolol 5 mg si gnificantly improved the left ventricular anatomy and function by redu cing the left ventricular mass index and the early-to-late ratio of th e diastolic peak flow velocity across the mitral valve. In patients wi th chronic renal failure, a 3-month treatment with tertatolol 5 mg sig nificantly increased the glomerular filtration rate and the effective renal plasma flow. Meanwhile, renal vascular resistance decreased and the filtration fraction remained unchanged.