Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: KEGG:D05731 (Rimonabant)
 326 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The development of a variety of new substances will considerably expand the therapeutic choices in the treatment of type 2 diabetes. In 2006, the endocannabinoid receptor blocker Rimonabant has been approved for the treatment of type 2 diabetes in Germany. This compound has led to significant reductions of body weight along with improvements of HbA1c levels and lipid profiles, but the lack of health insurance coverage limits its large scale use in germany. In April 2007, the first members of the GLP 1 analogues/incretin mimetics (exenatide, Byetta) and DPP 4 inhbitors (sitagliptin, Januvia) have become available for the treatment of type 2 diabetes in Germany. Both drugs have significantly lowered HbA1c levels in clinical studies. In addition, the incretin mimetics have caused a progressive reduction of body weight, while the DPP 4 inhibitors have been rather weight neutral. Sitagliptin can be administered orally, whereas exenatide has to be injected subcutaneously. Neither the DPP 4 inhibitors, nor the incretin mimetics have led to the development of hypoglycaemia, unless combined with sulfonylureas. Overall, the introduction of these new drug classes will certainly broaden our therapeutic choices in the management of type 2 diabetes. The long-term effects of these drugs on the development of diabetic complications in long-term trials remains to be awaited.
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PMID:[New concepts in the treatment of type 2 diabetes]. 1754 29

Pharmaceutical products reviewed in this paper markedly extend possibilities for the management of DM-2 and create prerequisites for diferential therapy of this disease. Exenatide and DPP-4 inhibitors do not cause hypoglycemia and may be prescribed to subjects in whom this condition may affect the ability to drive or operate machinery (drivers, pilots, etc.). The mechanism of action of DPP-4 inhibitors make them especially suitable for the treatment of early stages of DM-2 when B-cells are still capable of insulin secretion. They can be used at a dose of 100 mg once daily both for monotherapy and in combination with other oral hypoglycemic agents. These drugs are well tolerated by the patients but contraindicated to those with severe renal insuficiency. Exenatid is more eficacious than DPP-4 inhibitors and has advantages over insulin therapy because it does not increase body weight and do not require as frequent blood glucose monitoring. However, it produces side effects. Therefore, the treatment should be started with a low dose of the drug (5 mg subcutaneously twice daily) that can be doubled in 4 weeks. Bearing in mind the mechanism of action of exanatide, it is indicated largely to patients with DM-2 associated with obesity and a moderately elevated HbAlc level. Rimonabant is especially efficient due to its effect on the endocannabioid system of DM-2 patients with obesity, however it has a drawback of frequently producing adverse affects.
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PMID:[New avenues for pharmacotherapy of type 2 diabetes mellitus]. 1904 30

OBJECTIVE To examine the efficacy and safety of rimonabant, a selective cannabinoid receptor type-1 antagonist, in patients with type 2 diabetes receiving insulin monotherapy. RESEARCH DESIGN AND METHODS Patients (n = 368; A1C > or =7%) were randomized to 20 mg/day rimonabant or placebo in this 48-week, double-blind, placebo-controlled multicenter trial. Change in baseline A1C to week 48 (primary outcome) and changes in body weight, waist circumference, and lipid levels (secondary outcomes) were assessed. RESULTS Rimonabant significantly reduced baseline A1C versus placebo (-0.89 vs. -0.24%; P < 0.0001), and significantly greater improvements were observed in cardiometabolic risk factors. More rimonabant patients achieved >10% reduction in mean total daily insulin dose versus placebo (P = 0.0012), and fewer required rescue medication (P < 0.0001). Hypoglycemia, nausea, dizziness, anxiety, and depression were more frequent with rimonabant. CONCLUSIONS Rimonabant improved glycemic control and cardiometabolic risk factors in patients with type 2 diabetes receiving insulin.
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PMID:Effect of rimonabant on glycemic control in insulin-treated type 2 diabetes: the ARPEGGIO trial. 2000 90

Over the past decade, pharmacological manipulation of cannabinoid 1 receptor (CB1R) has become an interesting approach for the management of food ingestion disorders, among other physiological functions. Searching for new substances with similar desirable effects, but fewer side-effects we have synthesized a SR141716A (a cannabinoid receptor inverse agonist also called Rimonabant) analog, 1-(2,4-Difluorophenyl)-4-methyl-N-(1-piperidinyl)-5-[4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide, ENP11, that so far, as we have previously shown, has induced changes in glucose availability, i.e. hypoglycemia, in rats. In this study we tested the effects, if any, of ENP11 (0.5, 1.0, and 3.0mg/kg) in food ingestion, core temperature, pain perception and motor control in adult Wistar rats. Results showed that ENP11 reduced food ingestion during the first hour immediately after administration. Likewise, ENP11 (1.0mg/kg) blocked anandamide (AEA)-induced hyperphagia during the first 4h of the dark phase of the light-dark cycle, and it also blocked AEA-induced hypothermia. However, none of the ENP11 doses used affected pain perception or motor control. We believe that ENP11 is a potential useful CB1R antagonist that reduces food ingestion and regulates core temperature.
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PMID:ENP11, a potential CB1R antagonist, induces anorexia in rats. 2607 92