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Treating the metabolic syndrome: telmisartan as a peroxisome proliferator-activated receptor-gamma activator.
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- Author(s): Kurtz TW;Kurtz TW
- Source:
Acta diabetologica [Acta Diabetol] 2005 Apr; Vol. 42 Suppl 1, pp. S9-16.- Publication Type:
Journal Article; Review- Language:
English - Source:
- Additional Information
- Source: Publisher: Springer Verlag Country of Publication: Germany NLM ID: 9200299 Publication Model: Print Cited Medium: Print ISSN: 0940-5429 (Print) Linking ISSN: 09405429 NLM ISO Abbreviation: Acta Diabetol Subsets: MEDLINE
- Publication Information: Publication: Berlin : Springer Verlag
Original Publication: Berlin : Springer International, c1991- - Subject Terms: Benzimidazoles/*pharmacology ; Benzoates/*pharmacology ; Metabolic Syndrome/*drug therapy ; PPAR gamma/*agonists; Angiotensin-Converting Enzyme Inhibitors/pharmacology ; Angiotensin-Converting Enzyme Inhibitors/therapeutic use ; Benzimidazoles/therapeutic use ; Benzoates/therapeutic use ; Cardiovascular Diseases/prevention & control ; Clinical Trials as Topic ; Diabetes Mellitus, Type 2/drug therapy ; Humans ; Hypertension/drug therapy ; Telmisartan
- Abstract: Hypertension commonly occurs as part of a genetically complex disorder of carbohydrate and lipid metabolism known as the metabolic syndrome. Most current antihypertensive drugs appear ineffective against the metabolic syndrome, which is a strong predictor of cardiovascular disease and death in affected patients. Angiotensin II can influence the activity of certain genes and cellular and biochemical pathways that may contribute to the pathogenesis of the metabolic syndrome. However, as a class, angiotensin II receptor blockers (ARBs) have proven only minimally to modestly effective in ameliorating the disturbances in carbohydrate and lipid metabolism that characterise the metabolic syndrome. Recent preclinical studies indicate that the ARB telmisartan acts as a selective peroxisome proliferators-activated receptor-gamma (PPARgamma) modulator when tested at concentrations that might be achievable with oral doses recommended for treatment of hypertension; this property does not appear to be shared by other ARBs. PPARgamma is a nuclear receptor that influences the expression of multiple genes involved in carbohydrate and lipid metabolism and is an attractive therapeutic target for the prevention and control of insulin resistance, type 2 diabetes and atherosclerosis. In cellular transactivation assays, telmisartan functioned as a partial agonist of PPARgamma and achieved 25-30% of maximal receptor activation attained with conventional PPARgamma ligands. Preclinical and clinical studies indicate that administration of telmisartan can improve carbohydrate and lipid metabolism without causing the side effects that accompany full PPARgamma activators. If the preliminary data are supported by the results of ongoing large-scale clinical studies, telmisartan could have a central role in the prevention and treatment of metabolic syndrome, diabetes and atherosclerosis.
- Number of References: 60
- Accession Number: 0 (Angiotensin-Converting Enzyme Inhibitors)
0 (Benzimidazoles)
0 (Benzoates)
0 (PPAR gamma)
U5SYW473RQ (Telmisartan) - Publication Date: Date Created: 20050504 Date Completed: 20050524 Latest Revision: 20220409
- Publication Date: 20221213
- Accession Number: 10.1007/s00592-005-0176-0
- Accession Number: 15868121
- Source:
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