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Cannabinoid-1 receptor antagonists in type-2 diabetes.
Best Pract Res Clin Endocrinol Metab. 2007 Dec; 21(4):535-53.BP

Abstract

Type-2 diabetes is closely related to abdominal obesity and is generally associated with other cardiometabolic risk factors, resulting in a risk of major cardiovascular disease. Several animal and human observations suggest that the endocannabinoid system is over-active in the presence of abdominal obesity and/or diabetes. Both central and peripheral endocannabinoid actions, via the activation of CB1 receptors, promote weight gain and associated metabolic changes. Rimonabant, the first selective CB(1) receptor blocker in clinical use, has been shown to reduce body weight, waist circumference, triglycerides, blood pressure, insulin resistance index and C-reactive protein levels, and to increase high-density lipoprotein (HDL) cholesterol and adiponectin concentrations in both non-diabetic and diabetic overweight/obese patients. In addition, a 0.5-0.7% reduction in HbA1c levels was observed in metformin- or sulphonylurea-treated patients with type-2 diabetes and in drug-naïve diabetic patients. Almost half of the metabolic changes, including HbA1c reduction, could not be explained by weight loss, suggesting that there are direct peripheral effects. Rimonabant was generally well-tolerated, and the safety profile was similar in diabetic and non-diabetic patients, with a higher incidence of depressed mood disorders, nausea and dizziness. In conclusion, the potential role of rimonabant in overweight/obese patients with type-2 diabetes and at high risk of cardiovascular disease deserves much consideration.

Authors+Show Affiliations

Division of Diabetes, Nutrition and Metabolic Disorders, CHU Sart Tilman (B35), University of Liege, B 4000 Liege, Belgium. andre.scheen@chu.ulg.be

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

18054734

Citation

Scheen, André J.. "Cannabinoid-1 Receptor Antagonists in Type-2 Diabetes." Best Practice & Research. Clinical Endocrinology & Metabolism, vol. 21, no. 4, 2007, pp. 535-53.
Scheen AJ. Cannabinoid-1 receptor antagonists in type-2 diabetes. Best Pract Res Clin Endocrinol Metab. 2007;21(4):535-53.
Scheen, A. J. (2007). Cannabinoid-1 receptor antagonists in type-2 diabetes. Best Practice & Research. Clinical Endocrinology & Metabolism, 21(4), 535-53.
Scheen AJ. Cannabinoid-1 Receptor Antagonists in Type-2 Diabetes. Best Pract Res Clin Endocrinol Metab. 2007;21(4):535-53. PubMed PMID: 18054734.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Cannabinoid-1 receptor antagonists in type-2 diabetes. A1 - Scheen,André J, PY - 2007/12/7/pubmed PY - 2008/2/27/medline PY - 2007/12/7/entrez SP - 535 EP - 53 JF - Best practice & research. Clinical endocrinology & metabolism JO - Best Pract. Res. Clin. Endocrinol. Metab. VL - 21 IS - 4 N2 - Type-2 diabetes is closely related to abdominal obesity and is generally associated with other cardiometabolic risk factors, resulting in a risk of major cardiovascular disease. Several animal and human observations suggest that the endocannabinoid system is over-active in the presence of abdominal obesity and/or diabetes. Both central and peripheral endocannabinoid actions, via the activation of CB1 receptors, promote weight gain and associated metabolic changes. Rimonabant, the first selective CB(1) receptor blocker in clinical use, has been shown to reduce body weight, waist circumference, triglycerides, blood pressure, insulin resistance index and C-reactive protein levels, and to increase high-density lipoprotein (HDL) cholesterol and adiponectin concentrations in both non-diabetic and diabetic overweight/obese patients. In addition, a 0.5-0.7% reduction in HbA1c levels was observed in metformin- or sulphonylurea-treated patients with type-2 diabetes and in drug-naïve diabetic patients. Almost half of the metabolic changes, including HbA1c reduction, could not be explained by weight loss, suggesting that there are direct peripheral effects. Rimonabant was generally well-tolerated, and the safety profile was similar in diabetic and non-diabetic patients, with a higher incidence of depressed mood disorders, nausea and dizziness. In conclusion, the potential role of rimonabant in overweight/obese patients with type-2 diabetes and at high risk of cardiovascular disease deserves much consideration. SN - 1521-690X UR - https://www.unboundmedicine.com/medline/citation/18054734/Cannabinoid_1_receptor_antagonists_in_type_2_diabetes_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S1521-690X(07)00082-6 DB - PRIME DP - Unbound Medicine ER -