THE EFFECTS OF TERTATOLOL ON LIPID PROFILE

Tertatolol is a noncardioselective beta-blocker without intrinsic symp athomimetic activity. In a preliminary 3-month open study, it was show n that T was devoid of any atherogenic effect since HDL-cholesterol (H DL-C) and apoprotein levels did not change for 3 months of therapy. To investigate the long-term effects of tertatolol on the lipid profile and its safety in hypertensive patients with peripheral arterial disea se (PAD), a 9-month, randomized, double-blind, parallel group study wa s carried out in 40 patients. Tertatolol 5 mg once daily was compared with metoprolol 200 mg once daily. If BP was not controlled after 2 mo nths, a vasodilatator agent, dihydralazine, was added at the lowest do se required to control BP (diastolic BP < 90 mm Hg). Lipoprotein fract ions and apoproteins were assayed before (MO) and after 2, 6 and 9 mon ths of therapy. At the same occasions, peripheral arterial disease (PA D) was evaluated on exercise tests carried out on a treadmill and on t he regional blood flow measured in the ankle arteries by the Doppler t echnique. Four patients were not eligible for analysis. In the tertato lol group, 1 patient with a normal BP, and 2 patients who dropped out, 1 because of persistent nausea and 1 because of personal reasons. In the metoprolol group, 1 patient refused to take dihydralazine. In the 35 fully documented patients, BP control was achieved in both groups. The mean reductions in supine systolic/diastolic BP were 31.4/14.6 and 34.7/17.1 mm Hg in the tertatolol and metoprolol groups, respectively . Throughout the 9 months, no significant difference between groups wa s observed in the change of lipid parameters, except for the apoprotei n A2 level which increased significantly with tertatolol (+24 vs. +3% with metoprolol, p = 0.043). Changes in lipid profile were less marked with tertatolol than with metoprolol: triglycerides increased by 2 an d by 13% with tertatolol and metoprolol, respectively. HDL-cholesterol decreased by 11% with metoprolol and increased by 2% with tertatolol. Total and LDL-cholesterol remained stable with both drugs. The apo A1 /apo B ratio, which inversely correlates with the atherogenic risk, de creased by 7 and 25% with tertatolol and metoprolol, respectively. Per ipheral arterial disease improved with both drugs: pain-free walking d istance increased by 33.0 and 51.6 m with metoprolol and tertatolol, r espectively. Residual pressure index remained unchanged with both drug s since the calf BP measured in the ankle arteries decreased in propor tion to the decrease in brachial BP. Thus, both drugs were effective a nd well-tolerated since they controlled BP and improved the intermitte nt claudication. Considering its beneficial effects on the lipid param eters, tertatolol could be a better choice than metoprolol in the trea tment of hypertensive patients with severe PAD.