Sulfonylureas, which stimulate insulin secretion from pancreatic β-cells, are widely used to treat both type 2 diabetes and neonatal diabetes. These drugs mediate their effects by binding to the sulfonylurea receptor subunit (SUR) of the ATP-sensitive K(+) (KATP) channel and inducing channel closure. The mechanism of channel inhibition is unusually complex. First, sulfonylureas act as partial a...

OBJECTIVE The hypothesis that pioglitazone treatment is superior to gliclazide treatment in sustaining glycemic control for up to 2 years in patients with type 2 diabetes was tested. RESEARCH DESIGN AND METHODS This was a randomized, multicenter, double-blind, double-dummy, parallel-group, 2-year study. Approximately 600 patients from 98 centers participated. Eligible patients had completed a...

OBJECTIVE To compare effects of different oral hypoglycemic drugs as first-line therapy on lipoprotein subfractions in type 2 diabetes. RESEARCH DESIGN AND METHODS Sixty overweight type 2 diabetic patients not on lipid-lowering therapy were randomized to metformin, pioglitazone, or gliclazide after a 3-month dietary run-in. Drug doses were uptitrated for 3 months to optimize glycemia and were...

BACKGROUND The diagnosis of "factitious hypoglycemia" is essentially based on the disclosure of hypoglycemic agents in blood or urine. The aim of this study was to evaluate the performance of capillary electrophoresis (CE) as a quantitative method for determination of chlorpropamide, tolbutamide, glipizide, gliclazide, and glibenclamide in serum. METHODS Serum samples (1 mL), with internal st...

The prolonged release gliclazide matrix tablets were prepared using polymeric materials, namely, HPMC, Kollidon SR, Carbopol with Xanthan gum, Eudragit RSPO and Eudragit RLPO. HPMC, Kollidon SR and Carbopol with Xanthan gum were able to retard gliclazide release from matrix tablets in a concentration dependent manner, but the rate of retardation differed among the polymers. On the other hand, d...

The objective of the study was to compare pharmacokinetic and pharmacodynamic parameters of gliclazide after administration of immediate (IR) and modified release (MR) tablets. The experiment included rats with both normoglyceamia and streptozocin (STZ)-induced hyperglyceamia. Several MR formulations were designed and in vitro drug release profile was assessed by a dissolution test. For the fur...

BACKGROUND Diabetes is closely linked with coronary artery disease, either by means of direct effects of hyperglycemia, or indirectly by its frequent association with dyslipidemia. Any treatment for diabetes that has beyond the capacity of reduce glycated hemoglobin, the propensity to improve lipid profile and reduce weight will bring many benefits to patients. METHOD We compare the effects o...

The title compound, C(15)H(21)N(3)O(3)S, is known to be an impurity of gliclazide [systematic name: N-(hexa-hydro-1H-cyclopenta[c]pyrrol-2-ylcarbamo-yl)-4-methyl-benzene-sulfonamide], a sul-fonyl-urea anti-diabetic drug. Gliclazide has a p-tolyl group substituting the sulfonamide functionality, while the title mol-ecule contains an o-tolyl group. Both five-membered fused rings adopt envelope co...

OBJECTIVE To investigate the potential effect of gliclazide on serum ICAM-1 (intercellular adhesion molecule-1) and VCAM-1 (vascular cell adhesion molecule-1) levels in poorly controlled type 2 diabetic patients. PATIENTS AND METHODS The study included 104 patients, randomly divided into two groups. Group A comprised 53 patients (26 men) treated with gliclazide with a mean age of 67.5+/-9.9 y...

p-glycoprotein (p-gp) is a trans-membrane drug efflux pump. several drugs are p-gp substrates. some drugs may affect the activity of p-gp by inhibiting its function, resulting in significant drug-drug interactions (ddis). it is critical to understand which drugs are inhibitors of p-gp so that adverse ddis can be minimized or avoided. this study investigated the effects of gliclazide, metformin,...