Drugs online research references
J Cell Biochem. 1998 Nov 1;71(2):182-8.
Characterization of sulfonylurea receptors in isolated human pancreatic islets.
Giannaccini G, Lupi R, Trincavelli ML, Navalesi R, Betti L, Marchetti P, Lucacchini A, Del Guerra S, Martini C.
Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Pisa, Italy.
Current information on pancreatic islet sulfonylurea receptors has been obtained with laboratory animal pancreatic beta cells or stable beta-cell lines. In the present study, we evaluated the properties of sulfonylurea receptors of human islets of Langherans, prepared by collagenase digestion and density-gradient purification. The binding characteristics of labeled glibenclamide to pancreatic islet membrane preparations were analyzed, displacement studies with several oral hypoglycemic agents were performed, and these latter compounds were tested as for their insulinotropic action on intact human islets. [3H]glibenclamide saturable binding was shown to be linear at < or =0.25 mg/ml protein; it was both temperature and time dependent. Scatchard analysis of the equilibrium binding data at 25 degrees C indicated the presence of a single class of saturable, high-affinity binding sites with a Kd value of 1.0+/-0.07 nM and a Bmax value of 657+/-48 fmol/mg of proteins. The displacement experiments showed the following rank order of potency of the oral hypoglycemic agents we tested: glibenclamide = glimepiride > tolbutamide > chlorpropamide >> metformin. This binding potency order was parallel with the insulinotropic potency of the evaluated compounds.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9779817&dopt=Abstract
Horm Metab Res Suppl. 1985;15:105-11.
Metformin and the sulphonylureas: the comparative risk.
Campbell IW.
A review of the world literature until December 1982 revealed 843 cases of sulphonylurea-induced hypoglycaemia (SIH) with a mortality of 9%. There were 42 cases of metformin-associated lactic acidosis (MALA) with 18 deaths (43%); 40 of the MALA cases had documented contra-indications, especially renal impairment, and the remaining two cases were due to drug overdosage, one being a suicide. A comparative mortality risk was obtained from the Swedish Adverse Drug Reactions Advisory Committee (SADRAC) where there is accurate information regarding MALA and glibenclamide-associated hypoglycaemia. The calculated mortality risk for MALA and glibenclamide-associated hypoglycaemia showed no significant differences with values of 0.0240 and 0.0332 per 1,000 patient years, respectively. The incidence of hypoglycaemia with glibenclamide was greater than that of lactic acidosis associated with metformin (2p = 0.036). Sulphonylureas are not less dangerous than metformin and both groups of drugs should be used with care in non-insulin-dependent diabetics, especially in alderly subjects and those with impaired renal or hepatic function.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3935560&dopt=Abstract
Diabetes Care. 1984 May-Jun;7 Suppl 1:54-8.
Effects of biguanides and sulfonylureas on insulin receptors in cultured cells.
Goldfine ID, Iwamoto Y, Pezzino V, Trischitta V, Purrello F, Vigneri R.
The effects of the two groups of oral agents on insulin receptors were studied in several types of cells in tissue culture: MCF-7 human breast cancer cells, IM-9 human lymphocytes, human fibroblasts, and H-35 rat hepatoma cells. In none of these cells did the four sulfonylureas tested, tolbutamide, glibenclamide (glyburide), gliclazide, and glisolamide, have any significant effects on insulin binding to its receptor. In contrast the two biguanides tested, phenformin and metformin, increased insulin binding in all cell types by 44 to 101%. These studies raise the possibility, therefore, that biguanides may have a direct effect on insulin receptors and this effect may account for the known effects of biguanides to lower elevated blood sugar levels in diabetic patients.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6734405&dopt=Abstract
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