Inhibition of intestinal cholesterol absorption might explain cholesterol-lowering effect of telmisartan.

Telmisartan, an angiotensin II type 1 receptor blocker (ARB), acts as a partial agonist for peroxisome proliferator-activated receptor-γ, and thus improves abnormalities of glucose metabolism and hypertriglyceridaemia in addition to its documented blood pressure-lowering effects. Recently, it has been demonstrated that telmisartan also lowers the levels of total cholesterol and low-density lipoprotein (LDL) cholesterol levels. This study was designed to investigate the mechanism of cholesterol reduction. We measured serum levels of cholestanol, a cholesterol absorption marker, and lathosterol, a cholesterol synthesis marker, in 20 patients with both hypercholesterolaemia and hypertension. Ten patients were treated with telmisartan and the remaining 10 with fluvastatin. After 3 months of treatment, total and LDL cholesterol levels decreased in the telmisartan group ( P < 0·01 for both total and LDL cholesterol levels) and the fluvastatin group ( P < 0·001 for both total and LDL cholesterol levels). The change in cholestanol level after 3 months of treatment was positively correlated with the levels of total ( R = 0·72, P < 0·05) and LDL cholesterol ( R = 0·81, P < 0·01) in the telmisartan group. The change in lathosterol level was positively correlated with the levels of total ( R = 0·88, P = 0·001) and LDL cholesterol ( R = 0·89, P = 0·001) in the fluvastatin group. Our results suggest that the cholesterol-lowering effect of telmisartan might be caused by inhibition of cholesterol absorption, whereas that of statins is by inhibition of cholesterol synthesis. If confirmed, co-treatment with the two agents may be useful for synergistically lowering cholesterol in hypertensive patients. [ABSTRACT FROM AUTHOR]