Vergleichende Untersuchungen von Morphologie und Hormongehalt des Kälberpankreas nach Sulfonylharnstoffen (D 860)

Ef, Pfeiffer; Steigerwald, H; Sandritter, W.; Bänder, Alfred; Mager, Aviv; Becker, U.; Retiene, K.

doi:10.1055/s-0028-1116938

Cited by 42 publications

(7 citation statements)

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“…Tolbutamidet, which is known for its stimulatory action on insulin secretion [8] fails to increase the biosynthesis of insulin as judged by the incorporation of radioactive leucine into the insulin fraction of pancreatic slices or isolated islets [13,11]. Tanese et al [12] even described a dose-related inhibition of the leucine incorporation into proinsulin and insulin, effected by tolbutamide at low glucose concentrations.…”

Section: Introductionmentioning

confidence: 99%

The effect of tolbutamide and glibenclamide on the incorporation of [³H]leucine and on the conversion of proinsulin to insulin in isolated pancreatic islets

et al. 1972

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Section: Introductionmentioning

confidence: 99%

The effect of tolbutamide and glibenclamide on the incorporation of [³H]leucine and on the conversion of proinsulin to insulin in isolated pancreatic islets

et al. 1972

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“…The effectiveness of sulphonylureas is due mainly to their ability to stimulate the secretion of endogenous insulin and to overcome the "secretory block", existing in all type II diabetics as described by Pfeiffer (Pfeiffer et al, 1957). In addition to this well known "primary effect" of suiphonyllureas, a number of extrapancreatic effects have also been described with these compounds, but their therapeutic relevance is still a matter of discussion (Feldman et al, 1977).…”

Section: Endocrinology Anddiabetesmentioning

confidence: 99%

Comparative effects of glimepiride and glibenclamide on blood glucose, C-peptide and insulin concentrations in the fasting and postprandial state in normal man

Raptis

Hatziagelaki²,

Dimitriadis³

et al. 2009

Exp Clin Endocrinol Diabetes

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A single-center, randomised, placebo- controlled, cross-over study was conducted to characterize the new sulfonylurea glimepiride and to compare its profile of action with the second generation sulfonylurea glibenclamide. The total duration of each experiment was 5 hours. At zero time an i.v. injection of 2 and 4 mg glimepiride, 1 mg glibenclamide or placebo was given i.v. to 24 healthy volunteers. Blood samples were collected for three hours after the injection (0-3 hours, preprandial experiment). At 3 hours, a standard mixed meal was given (20%, of a 30 Kcal/Kg Body Weight diet) and blood samples were collected for 2 more hours (postprandial experiment). Pre-prandially (0-3 hrs) blood glucose (expressed as the area under the curve divided by the time) was significantly lower (p < 0.0001) after the administration of 2 and 4 mg glimepiride (3.8 +/- 0.22 and 3.5 +/- 0.3 mM respectively) compared to placebo (4.63 +/- 0.31 mM), but not compared to glibenclamide. Insulin and C-peptide were not different after glimepiride or glibenclamide. Both glimepiride and glibenclamide had similar effects on insulin secretion. Post-prandially (3-5 hrs) blood glucose was significantly higher after glibenclamide (6.54 +/- 0.8 mM) (p < 0.0001) than after 2 mg glimepiride (5.75 +/- 0.5 mM). Despite this C-peptide was significantly higher (p < 0.002) glibenclamide (5.7 +/- 1.5 ng/ml) compared to glimepiride (5.1 +/- 1.3 ng/ml); the trend was the same for insulin but the results were not significantly different (p = 0.06) In conclusion, in the fasting state, glimepiride and glibenclamide had similar effects on the changes in blood glucose levels after i.v. administration. After the meal, less pronounced hyperglycemia and lower insulin and C-peptide levels following glimepiride (2 mg) suggests either that glimepiride induces insulin secretion through a pathway which is different from that of glibenclamide or that glimepiride facilitates insulin action through extrapancreatic effects.

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“…In 1957, Pfeiffer and co-workers demon-strated for the first time that sulfonylureas act on the pancreatic Il-cells restoring their insulin secretion defect, which is characteristic of NIDDM (Pfeiffer, Steigenwald, Sandritter, Baender, Mager, Becker and Retiene 1957). In addition, it was more recently shown that sulfonylureas, besides their pancreatic action (Loubatieres 1944;Pfeiffer et al 1957), also have a peripheral effect, mainly on the insulin receptors (Beck-Nielsen, Pedersen and Lindskov 1976;Prince and Olefsky 1980;Gold-man, Tamayo, Whitehouse and Kahkonen 1984). After the development of glibenclamide (a second generation of sulfonylurea) a new era for the oral treatment of diabetes commenced in Europe and later in America.…”

Section: Introductionmentioning

confidence: 99%

Therapeutic Effect of Glibenclamide in a Fixed Combination with Metformin or Phenformin in NIDDM Patients

Ae¹,

Nb²,

Ag³

et al. 1996

Horm Metab Res

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The combination of a sulfonylurea with a biguanide improves the pancreatic beta-cell insulin secretion and the insulin utilization in peripheral tissues in NIDDM. This open, crossover, randomised and prospective study was designed to compare the effects of the fixed combination glibenclamide-metformin (GL-METF)-2.5 and 400 mg respectively, with the fixed combination glibenclamide-phenformin (GL-PHEN)-2.5 and 25 mg respectively, on NIDDM diabetes control. Thirty NIDDM patients, in ideal metabolic control, who were being treated with GL-PHEN were divided in two groups. One group received GL-PHEN for 12 weeks followed by 12 weeks treatment with GL-METF and the reverse treatment was given to the second group. A statistically significant decrease of post-prandial blood glucose (p = 0.034) and glycosylated haemo-globin (p < 0.02) values was observed under GL-METF treatment compared to those with GL-PHEN. The values of lactic acid were within normal limits during both treatments. The insulin secretion after breakfast was similar with both drug compounds. The BMI of the patients remained the same during a follow-up study of 24 weeks. Lipid metabolism did not change significantly during the trial and the safety parameters (renal and liver function, full blood count) remained unchanged. In conclusion, the administration of GL-METF leads to better diabetes control in NIDDM patients compared to that of GL-PHEN.

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Vergleichende Untersuchungen von Morphologie und Hormongehalt des Kälberpankreas nach Sulfonylharnstoffen (D 860)

Cited by 42 publications

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The effect of tolbutamide and glibenclamide on the incorporation of [³H]leucine and on the conversion of proinsulin to insulin in isolated pancreatic islets

The effect of tolbutamide and glibenclamide on the incorporation of [³H]leucine and on the conversion of proinsulin to insulin in isolated pancreatic islets

Comparative effects of glimepiride and glibenclamide on blood glucose, C-peptide and insulin concentrations in the fasting and postprandial state in normal man

Therapeutic Effect of Glibenclamide in a Fixed Combination with Metformin or Phenformin in NIDDM Patients

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Vergleichende Untersuchungen von Morphologie und Hormongehalt des Kälberpankreas nach Sulfonylharnstoffen (D 860)

Cited by 42 publications

References 0 publications

The effect of tolbutamide and glibenclamide on the incorporation of [3H]leucine and on the conversion of proinsulin to insulin in isolated pancreatic islets

The effect of tolbutamide and glibenclamide on the incorporation of [3H]leucine and on the conversion of proinsulin to insulin in isolated pancreatic islets

Comparative effects of glimepiride and glibenclamide on blood glucose, C-peptide and insulin concentrations in the fasting and postprandial state in normal man

Therapeutic Effect of Glibenclamide in a Fixed Combination with Metformin or Phenformin in NIDDM Patients

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The effect of tolbutamide and glibenclamide on the incorporation of [³H]leucine and on the conversion of proinsulin to insulin in isolated pancreatic islets

The effect of tolbutamide and glibenclamide on the incorporation of [³H]leucine and on the conversion of proinsulin to insulin in isolated pancreatic islets