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Inhibition of intestinal cholesterol absorption might explain cholesterol‐lowering effect of telmisartan
Author(s) -
Inoue T.,
Taguchi I.,
Abe S.,
Toyoda S.,
Sakuma M.,
Node K.
Publication year - 2011
Publication title -
journal of clinical pharmacy and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.622
H-Index - 73
eISSN - 1365-2710
pISSN - 0269-4727
DOI - 10.1111/j.1365-2710.2010.01161.x
Subject(s) - telmisartan , lathosterol , medicine , cholesterol , endocrinology , fluvastatin , cholestanol , chemistry , simvastatin , sterol , blood pressure , campesterol
Summary What is known and objective: 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. Methods: 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. Results: 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. What is new and conclusions: 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.