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

Abstract

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.

• Authors: T Inoue, I Taguchi, S Abe, S Toyoda, M Sakuma, K Node
• Journal: Journal of clinical pharmacy and therapeutics (J Clin Pharm Ther) Vol. 36 Issue 1 Pg. 103-10 (Feb 2011) ISSN: 1365-2710 [Electronic] England
• PMID: 21198725 (Publication Type: Comparative Study, Controlled Clinical Trial, Journal Article)
• Copyright: © 2010 Blackwell Publishing Ltd.

Chemical References

• Angiotensin II Type 1 Receptor Blockers
• Anticholesteremic Agents
• Benzimidazoles
• Benzoates
• Biomarkers
• Cholesterol, LDL
• Fatty Acids, Monounsaturated
• Gastrointestinal Agents
• Indoles
• PPAR gamma
• Fluvastatin
• lathosterol
• Cholestanol
• Cholesterol
• Telmisartan

Topics

• Aged
• Aged, 80 and over
• Angiotensin II Type 1 Receptor Blockers (pharmacology)
• Anticholesteremic Agents (pharmacology, therapeutic use)
• Benzimidazoles (pharmacology, therapeutic use)
• Benzoates (pharmacology, therapeutic use)
• Biomarkers (blood)
• Cholestanol (blood)
• Cholesterol (blood, metabolism)
• Cholesterol, LDL (blood)
• Fatty Acids, Monounsaturated (pharmacology, therapeutic use)
• Female
• Fluvastatin
• Gastrointestinal Agents (pharmacology, therapeutic use)
• Humans
• Hypercholesterolemia (blood, complications, drug therapy)
• Hypertension (blood, complications, drug therapy)
• Indoles (pharmacology, therapeutic use)
• Intestinal Absorption (drug effects)
• Male
• Middle Aged
• PPAR gamma (agonists)
• Telmisartan