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Query: UMLS:C0011849 (diabetes)
 277,896 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Glyburide is an effective hypoglycemic agent in patients with type II diabetes even after the loss of its ability to increase insulin secretion. The exact mechanism is unknown. In an attempt to describe the direct effect of glyburide on glucose metabolism, a very low dose of glyburide (20 micrograms/kg body weight) was given orally to 12 healthy volunteers in an attempt to increase blood concentrations of the drug without causing a marked increase in insulin secretion. Fasting hepatic glucose production (HGP), carbohydrate oxidation (CO), leucine appearance, leucine oxidation, and fat oxidation were determined between hours 3 and 4 and hours 7 and 8. The changes seen in the glyburide-treated volunteers were compared with the changes seen in 5 non-treated, healthy volunteers during the same 8-hour period. Mean blood glucose decreased greater in the glyburide-treated volunteers (20 +/- 2% vs 5 +/- 2%, P < 0.01). Insulin and C-peptide concentrations after glyburide administration (hour 7 to 8) did not differ significantly from baseline (hour 3 to 4) values (insulin: 53 +/- 9 pmol/L vs 52 +/- 9 pmol/L; C-peptide: 0.34 +/- 0.06 ng/mL vs 0.39 +/- 0.07 ng/mL). This low dose of glyburide resulted in a significantly greater decrease in HGP (16 +/- 2%; P < 0.001) than seen with fasting alone (8 +/- 4%; P < 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Low-dose oral glyburide reduces fasting blood glucose by decreasing hepatic glucose production in healthy volunteers without increasing carbohydrate oxidation. 787 17

1. Decreased beta-adrenergic responses have been reported in gastro-intestinal tract of rats with diabetes mellitus. Effects of glyburide and insulin on the decreased beta-adrenergic responsiveness of the gastro-intestinal tract due to non-insulin-dependent diabetes were investigated using duodenum, jejunum and ileum from rats which were injected with alloxan in their neonatal periods. 2. Insulin treatment of non-insulin-dependent diabetic rats for 10 days corrected the decreased beta-adrenergic responses of the isolated duodenum, jejunum and ileum confirming the previous results obtained from insulin-dependent diabetic rats. 3. Glyburide treatment alone for 3 weeks also reversed the changes in the gastro-intestinal beta-adrenergic responses of non-insulin-dependent diabetic rats. Combination of glyburide with insulin, however, did not cause an additive or supra-additive interaction in terms of beta-adrenergic sensitivities of the diabetic tissues. 4. The results obtained in the present study strongly suggested that non-insulin-dependent diabetes may cause a decrease in the number of gastro-intestinal beta-adrenoceptors, while glyburide and insulin treatments correct the changes related to beta-adrenoceptors. The effect of insulin on the beta-adrenergic sensitivity of diabetic rat duodenum, jejunum and ileum may occur via a direct mechanism, whereas glyburide seems to be effective on the beta-adrenergic responses through the increases in the insulin secretion and/or in the number of gastro-intestinal insulin receptors.
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PMID:The effects of glyburide and insulin on the decreased beta-adrenergic responsiveness of the gastrointestinal tract in rats with non-insulin-dependent diabetes. 789 68

In the present study we administrated glyburide (glibenclamide) to type 2 (NIDDM) diabetic rats and determined the effect of such treatment on liver superoxide dismutase (SOD) activity. Hepatic SOD activity was significantly reduced in diabetic animals. Glyburide treatment of diabetic rats for 4 weeks corrected the changes observed in diabetic liver. In addition, blood glucose levels of untreated diabetic rats decreased following glyburide treatment. Administration of glyburide to diabetic rats reversed the diabetes-induced changes, suggesting that glyburide may directly increase liver SOD enzyme activity.
Diabetes Res Clin Pract 1994 Jan
PMID:Effect of the sulfonylurea glyburide on superoxide dismutase activity in alloxan-induced diabetic rat hepatocytes. 820 Mar 1

Oral antidiabetic agents continue to play an important role in the treatment of type 2 diabetes. Of decisive importance is the timing of their use, together with a knowledge of their specific properties. Acarbose, which needs to be initiated at a low, slowly increasing dose, is noted for the fact that it has virtually no systemic side effects. Metformin reduces plasma glucose levels without inducing hyperinsulinemia, and carries virtually no risk of lactic acidosis. Glibenclamide can be used either alone to treat type 2 diabetes or in combination with other oral antidiabetics or insulin. Today, intensified insulin therapy represents the optimal standard of insulin replacement. It permits meal-oriented injection of normal insulin and the use of longer-acting insulin overnight. This form of treatment is now facilitated by the possibilities of plasma glucose selfmonitoring and the use of injection aids (pen). Intensified treatment should be initiated at the time type I diabetes is diagnosed. In the case of a particularly instable metabolic situation or neuropathy, it may become necessary to use insulin pumps.
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PMID:[Management of diabetes in general practice--current requirements. 2: Oral antidiabetics and insulin therapy]. 820 Jun 2

The subjects were 206 patients (123 men, 83 women) with non-insulin-dependent diabetes mellitus, aged 33 to 80 years. For at least 4 weeks prior to the study each subject had been taking 5-mg tablets of original, nonmicronized glyburide (Micronase tablets) in doses of 5, 10, 15, or 20 mg daily. In a double-blind 12-week study, the subjects were randomly assigned to continue receiving 5-mg tablets of original glyburide or to substitute 3-mg tablets of reformulated, micronized glyburide (Glynase PresTab tablets) for the original tablets. Glyburide tablets had been reformulated to improve their bioavailability. Baseline mean fasting serum glucose levels in the groups taking reformulated and original glyburide were 169.3 and 168.3 mg/dl, respectively; at study end point, their respective serum glucose levels were 186.0 and 177.0 mg/dl. The differences between groups were not significant; in both groups, however, end point glucose levels were significantly higher than baseline levels. Baseline hemoglobin A1C levels in the groups taking reformulated and original glyburide were both 7.6%; at study end point, hemoglobin A1C levels had improved slightly in each group to 7.4% and 7.5%, respectively. The differences between and within groups at end point were not significant. No between-group differences at baseline or at end point were found in mean levels of postprandial serum glucose, fasting C-peptide, or postprandial C-peptide. Medical events experienced by the subjects in the two groups were similar in nature and number. Changes in other laboratory test results, vital signs, and weight were not clinically meaningful.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Efficacy and safety of reformulated, micronized glyburide tablets in patients with non-insulin-dependent diabetes mellitus: a multicenter, double-blind, randomized trial. 826 45

1. The effects of glyburide were studied on the myocardial contractile force and heart rate in the atria isolated from non-diabetic and non-insulin-dependent diabetic rats (diabetic). 2. In order to examine the myocardial changes in the alloxan model of non-insulin-dependent diabetes, atrial functions of 11-week old diabetic rats were evaluated by comparing with the atria from their age-matched controls. 3. Diabetic atria were found to possess an increased contractile force and reduced inotropic responses to isoprenaline as a consequence of non-insulin-dependent diabetes induced by neonatal alloxan injection. 4. However, no significant change was observed in the heart rate of diabetic atria in response to isoprenaline when compared with controls. 5. Since apparent affinity constant (pD2 value) calculated for the inotropic response of diabetic atria to isoprenaline was also reduced, it might be suggested that non-insulin-dependent-diabetes causes a decrease in the beta-adrenoceptor affinity of the rat atria. 6. Glyburide treatment (5 mg/kg/day per os) for 3 weeks was able to improve the reduced responsiveness of rat atria due to non-insulin-dependent diabetes as well. The results obtained in this study indicated that glyburide possesses an improving effect on the decreased beta-adrenergic responses of rat atria with non-insulin-dependent diabetes mellitus.
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PMID:The effects of glyburide and insulin on the cardiac performance in rats with non-insulin-dependent diabetes mellitus. 848 92

In vitro and in vivo studies suggest that opening of ATP-sensitive potassium channels following ischaemia enhances recovery of myocardial contraction, dilates blood vessels and has an antiarrhythmic effect. Different sulphonylurea compounds that block the ATP-sensitive potassium channels exert different effects on cardiac functions. Glibenclamide decrease, arrhythmogenesis during acute myocardial infarction in rats and reduces strophanthin cardiotoxicity in rabbits. Other sulphonylurea compounds, but not glibenclamide, increase arterial blood pressure and myocardial contractility. These effects may be partly secondary to blockade of ATP-sensitive potassium channels and partly due to independent cardiac and extracardiac actions. Glimepiride may have a more advantageous cardiovascular effect than glibenclamide. The studies suggest the hypothesis that deleterious cardiovascular effects of some hypoglycaemic sulphonylurea drugs may contribute to the high cardiovascular mortality rate in diabetes mellitus. An observational study suggested glibenclamide decreased the incidence of fatal myocardial infarction and development of ventricular fibrillation in patients suffering from acute myocardial infarction. Glibenclamide may also decrease the incidence of ventricular ectopic beats in digitalized patients compared with other sulphonylurea compounds. The studies suggested the survival of subjects treated with glibenclamide, insulin, or diet alone after the first attack of angina pectoris or after first acute myocardial infarction may be longer compared with those on other sulphonylurea therapies. Further large scale prospective, randomised studies are needed to determine whether the reported effects can be verified and are sufficiently large to affect clinical prescribing.
Diabetes Res Clin Pract 1995 Aug
PMID:Potassium channels in the cardiovascular system. 852 23

Antidiabetic drug-induced hypoglycemia as a cause of acute medical admissions is more common in Hong Kong (1.7%) than in other countries (0.1-0.5%). To determine if this higher incidence may be related to the frequent use of some sulphonylureas, we have studied the overall prescribing patterns in the public sector in 1994 by reviewing the utilization of antidiabetic drugs in the general out-patient/general practice clinics (GOPD) and Hospital Authority public hospitals and affiliated specialist clinics (HA). The vast majority of patients (90.5%) receiving antidiabetic treatment were taking sulphonylureas and/or metformin, confirming that diabetes mellitus in Hong Kong is predominantly of the noninsulin-dependent type. The GOPD and the HA each accounted for approximately half of the sulphonylureas (55% vs 45%) and metformin (43% vs 57%) prescribed. Glibenclamide (84.9% vs 79.1%, 83.7% overall) and gliclazide (12.8% vs 16.6%, 14.5% overall) were the 2 most frequently used sulphonylureas. Only 9.5% of patients on antidiabetic drugs were receiving insulin and 92% of this was prescribed by the HA. For comparison, Singapore has a similar prevalence of diabetes mellitus but a much lower incidence of antidiabetic drug-induced hypoglycemia amongst acute medical admissions (0.5%). Tolbutamide was the most frequently used there sulphonylurea (66.6-72.2%) with glibenclamide only contributing 20.8-28.6%. Thus, the predominant use of glibenclamide in Hong Kong may contribute to the high incidence of antidiabetic drug-induced hypoglycemia amongst acute medical admissions.
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PMID:Utilization of antidiabetic drugs in Hong Kong: relation to the common occurrence of antidiabetic drug-induced hypoglycemia amongst acute medical admissions and the relative prevalence of NIDDM. 868 96

Since the first publication of the University Group Diabetes Programme in 1970 the possible deleterious cardiovascular effects of certain hypoglycaemic sulphonylurea products has been well known. In contrast, international knowledge of the advantageous cardiovascular effects of certain sulphonylurea compounds became available recently. Glibenclamide decreases the incidence of fatal myocardial infarction and the development of ventricular fibrillation in patients suffering from acute myocardial infarction. It also lowers the incidence of ventricular ectopic beats in digitalized patients compared with patients treated with other investigated sulphonylurea compounds. The survival of patients treated with glibenclamide, insulin or diet alone is longer after the first attack of angina pectoris or after first acute myocardial infarction compared with those on other investigated sulphonylurea therapy. Glibenclamide decreases arrhythmogenesis during acute myocardial infarction in rats and strophanthin cardiotoxicity in rabbits. Arterial blood pressure and myocardial contractile force are not influenced by glibenclamide whereas these parameters are increased by other investigated sulphonylurea compounds. Consequently, deleterious cardiovascular effects of certain hypoglycaemic sulphonylurea drugs may contribute to the high cardiovascular mortality rate in diabetes mellitus, partly due to the effect on membrane channels and partly due to independent cardiac and extracardiac actions. Finally, recent observations suggest that glimepiride has a more advantageous cardiovascular effect than glibenclamide.
Diabetes Res Clin Pract 1996 Jul
PMID:What kind of cardiovascular alterations could be influenced positively by oral antidiabetic agents? 886 38

Both glibenclamide and metformin have been used alone or in association for many years. In the treatment of type 2 or non-insulin-dependent diabetes (NIDDM). Glibenclamide stimulates insulin release by pancreatic beta cells (pancreatic attachment point), while metformin acts at a peripheral level by increasing glucose absorption in muscular, fatty and hepatic tissues, thus considerably reducing insulin resistance (extra-pancreatic attachment point). The aim of this study was to evaluate the therapeutic efficacy of the pre-formed association of glibenclamide 2.5 mg+metformin 400 mg (treatment group 1) compared to treatment with glibenclamide 5 mg alone (treatment group 2) at almost double therapeutic doses compared to those contained in the association. A total of 40 NIDDM patients were examined (24 females and 16 males) with a mean age of 55.86 years, a mean duration of disease of 9.37 years, generally obese or overweight. From the final results of the study it was found that the associative therapy of glibenclamide 2.5 mg+metformin 400 mg was very advantageous, leading to a significant improvement in the glycometabolic control (HbA1c and fasting plasma glucose) compared to patients treated using single drug therapy who maintained almost stable control of the disease.
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PMID:[Comparison of two treatment models in type-II diabetic patients with poor metabolic control: Preformed combination of glibenclamide 2,5 mg + metformin 400 mg or mono-therapy with sulfonylurea at maximal doses? An evaluation at six months]. 907 66


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