Sulfonylureas efficacy

Warren, L.S., T.W. Gannon, and F.H. Yelverton (2005). Efficacy of recently registered sulfonylurea herbicides for broadleaf weed control in warm season turf. Proc. South. Weed Sci. Soc., 58 115. 

Troglitazone, the first clinically available thiazolidinedione, was approved for use in patients who have failed diet therapy and, in combination with insulin and/or sulfonylureas, in patients inadequately controlled with these agents alone (117). Although studies have documented the hypoglycemic efficacy of troglitazone in patients with type 2 diabetes, its use was associated with elevated liver enzymes, liver damage, and death... 

Efficacy of 4- and 8-mg/day Doses of Rosiglitazone Combined with Sulfonylureas (108, 124)... 

This study was designed as a proof-of-con-cept Phase 11 study to determine the safety and efficacy of Orahn in place of glybur-ide (a sulfonylurea) or insulin secretagogues on a long-term basis (90 days or more) in subjects with type 2 diabetes. The primary hypothesis was that Oralin could be used safely in combination with metformin to help maintain or improve the eight-point glucose profiles and the baseUne HbAlc levels at 90 days or more after treatment. 

Disulfiram (tetraethylthiuram disulfied Antabuse) was taken in the course of an investigation of its potential anthelminthic efficacy by two Danish physicians, who became ill at a cocktail party and were quick to realize that the compound had altered their responses to alcohol. They initiated a series of pharmacological and clinical studies that provided the basis for the use of disulfiram as an adjunct in the treatment of chronic alcoholism. Similar responses to alcohol ingestion are produced by various congeners of disulfiram, namely, cyanamide, the fungus Copri-nus atramentarius, the hypoglycemic sulfonylureas, metronidazole, certain cephalosporins, and animal charcoal. 

THERAPEUTIC USES Sulfonylureas are used to control hyperglycemia in type 2 DM patients who cannot achieve appropriate control with diet alone. In all patients, continued dietary restrictions are essential to maximize the efficacy of the sulfonylureas. Contraindications to the use of these drugs include type 1 DM, pregnancy, lactation, and for the first-generation agents, significant hepatic or renal insufficiency. 

Nauck MA, Meininger G, Sheng D, Terranella L, Stein P. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, compared to the sulfonylurea, glipizide, in patients with type 2 diabetes inadequately controlled on metformin alone A randomized, double-blind, non-inferiority trial. Diabetes Obesity Metab 2007 9 194-205. 

Francillard M. Efficacy of benfluorex in combination with sulfonylurea in type 2 diabetic patients an 18-week, randomized, double-blind study. Diabetes Care 2006 29(3) 515-20. 

Francillard M. Efficacy of benfluorex in combination with sulfonylurea in type 2... 

Foley JE, Sreenan S. Efficacy and safety comparison between the DPP-4 inhibitor vildagliptin and the sulfonylurea gliclazide after two years of monotherapy in drug-naive patients with type 2 diabetes. Horm Metab Res 2009 41(12) 905-9. 

Numerous substituted p pmidine and tiiazine amines have found utility as precursors to highly active and crop selective sulfonylurea herbicides. In the process of optimizing herbicidal efficacy and crop safety within this class, a variety of structurally diverse heterocyclic amines have been synthesized and evaluated. This paper reviews the methods of preparation that have been developed for some of the different structural types used as intermediates to active sulfonylurea herbicides. These methods include cyclizations, rearrangements, and side-chain metalations that have led to furo[2,3-d]pyriiindines, pyrazinones, and selectively functionalized pyrimitoes, triazines, triazoles, and pyridines. 

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