Sulfonylurea structure activity relationship of metformin

sulfonylurea structure activity relationship of metformin

Although sulfonylurea compounds are the second preferred drug to treat Type II Diabetes ride, Structure Activity Relationship. for diabetic patients who are not of overweight or those for whom metformin is contraindi-. PDF | The quantitative structure – activity relationship in antidiabetic oral drugs has sulfonylurea: the release of insulin from the pancreatic beta cells is It is interesting to remark that the usual Metformin drug has an intermediary activity. SAR of Glyburide (glibenclamide) STRUCTURE ACTIVITY RELATIONSHIPS OF SULFONYLUREAS AND Metformin + Glyburide (Glucovance). N. C. H3C.

In other words we tried to set Structure-Activity-Relationship SAR from these chemical structures for sulfonamide core.

sulfonylurea structure activity relationship of metformin

This helps the researchers more in case they need a reference for these compounds collected in one paper. Sulfonamide common core structure Anti-Bacterial Sulfonamides: In his attempt to save his daughter from streptococci killing infection, he observed that prontosil; a sulfonamide dye, is able to selectively restrain the infectious bacteria cells.

used in treatment of diabetes - ppt video online download

InErnest Fourneau found out prontosil pathway in human body. He discovered that this dye was a pro-drug. It, actually changes in human body to sulfanilamide which is the anti-bacterial active agent. This invention triggered the discoveries of other anti-bacterial members derived from this chemical group such as sulfapyridine in against pneumonia, and sulfacetamide in against urinary tract infections, and succinoylsulfathiazole in against gastrointestinal tract infections.

On the contrary, sulfanilamide was not very used due to its greater human toxicity. Later on, sulfisoxaide, sulfamethoxazole, sulfacetamide, mafenide and sulfadiazine silver were discovered, and those four agents are the sulfonamide anti-bacterial agents have been in the clinical use so far. Sulfonamide anti-bacterial medications; also called sulfa drugs, are competitive inhibitors of p- amino benzoic acid in the folic acid metabolism cycle in the organisms.


RESULTS—Among the study population of 50, type 2 diabetic subjects, six cases of lactic acidosis during current use of oral antidiabetes drugs were identified, yielding a crude incidence rate of 3. Relevant comorbidities known as risk factors for lactic acidosis could be identified in all case subjects.

A total of 2, case subjects with hypoglycemia and 7, matched control subjects were identified.

sulfonylurea structure activity relationship of metformin

Use of sulfonylureas was associated with a materially elevated risk of hypoglycemia. The adjusted odds ratio for current use of sulfonylureas was 2.

sulfonylurea structure activity relationship of metformin

Hypoglycemic episodes were substantially more common among sulfonylurea users than among users of metformin. Metformin plays a pivotal role in the treatment of patients with type 2 diabetes 1.

sulfonylurea structure activity relationship of metformin

Metformin decreases basal glucose output by suppressing gluconeogenesis and glycogenolysis in liver and increasing glucose disposal in muscle tissue. Lalau and Race 6 analyzed 49 cases of lactic acidosis associated with metformin use; overall mortality was not correlated with plasma lactate concentrations.

Interestingly, plasma metformin concentrations were, on average, three times higher in patients who survived. All case subjects with lactic acidosis had, in addition to metformin use, acute or chronic comorbidities predisposing to lactic acidosis.

These data suggest that lactic acidosis may be coincidental rather than causally associated with metformin use. Since metformin does not directly stimulate insulin secretion, hypoglycemia risk may be lower than for that of other oral antidiabetes drugs.

However, hypoglycemia in patients using metformin may occur in association with strenuous physical activity or fasting.

Hypoglycemia is a major concern for users of sulfonylureas. Magnitude and severity of sulfonylurea-induced hypoglycemia range widely across studies 19 In an observational study 11the annual risk for a first hypoglycemia diagnosis associated with sulfonylurea use was 1. Despite many reports on the risk of hypoglycemia in patients using oral antidiabetes drugs, direct comparisons between drug classes in the same study population are rare 9. Furthermore, the definition of hypoglycemia varies considerably across previous studies, and a comparison of their results is therefore difficult 7.

Additionally, no previous study quantified both the risk of developing lactic acidosis and hypoglycemia among users of sulfonylureas or metformin in the same study population. Therefore, we conducted an observational study to compare the risk of lactic acidosis and hypoglycemia among users of metformin, sulfonylureas, or other oral antidiabetes drugs.

used in treatment of diabetes

GPs have been trained to record medical information, including demographic data, medical diagnoses, hospitalizations, deaths, and drug prescriptions, using standard software and standard coding systems. The GPs generate prescriptions directly with the computer; this information is automatically transcribed into the computer record.

It contains the name of the preparation, instructions for use, route of administration, dose, and number of tablets for each prescription.