Drugs online research references
J Pharm Sci. 1984 Feb;73(2):253-6.
Adsorption of sulfonylureas onto activated charcoal in vitro.
Kannisto H, Neuvonen PJ.
Adsorption of carbutamide, chlorpropamide, tolazamide, tolbutamide, glibenclamide (glyburide), and glipizide onto activated charcoal was compared in vitro using different charcoal-to-drug ratios. Maximal binding capacities of different sulfonylureas were 0.45-0.52 g/g of charcoal at pH 7.5. The affinity of the second generation derivatives, glibenclamide and glipizide, was considerably higher than that of the first generation derivatives. The affinity of sulfonylureas to charcoal was higher at pH 4.9 than at pH 7.5. Poor water solubility of sulfonylureas at pH 1 prevents the adequate testing in these conditions. Contrary to what has appeared previously, activated charcoal effectively adsorbs different sulfonylureas and can be used to possibly prevent their gastrointestinal absorption.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6707896&dopt=Abstract
Diabetologia. 1982 Jul;23(1):54-60.
Efflux of radioactive nucleotides from mouse pancreatic islets prelabelled with 2-3H-adenosine.
Welsh M.
Cultured mouse pancreatic islets were prelabelled with 2-3H-adenosine in order to monitor the efflux pattern of radioactivity and insulin. The outflow of radioactivity decreased continuously when the islets were perifused with glucose (1.67 mmol/l). When raising the glucose concentration to 16.7 mmol/l, there was a prompt inhibition of the radioactive efflux concomitant with an increased rate of insulin release. These effects were reversed when the high glucose challenge was withdrawn. Similar radioactive efflux patterns were obtained after addition of alpha-ketoisocaproic acid, leucine or pyruvate to the perifusion medium, and also when the islets were challenged with high glucose concentrations in the absence of calcium. Both antimycin A and glipizide stimulated the efflux of radioactivity, although only the addition of glipizide was accompanied by a stimulation of the insulin release. Nucleotides constituted approximately 90% of the total effluent radioactivity. Decrease in the radioactive AMP and ADP efflux due to high glucose was furthermore found to be the cause of the observed inhibition of the total radioactive efflux. The changes in radioactive efflux induced by glucose probably reflect changes in the intracellular concentrations of AMP and ADP. It is concluded that no simple correlation exists between radioactive efflux and insulin release and that changes in the intracellular concentrations of nucleotides may be an early event in the stimulus-secretion coupling of glucose-induced insulin release.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6749585&dopt=Abstract
Int J Clin Pharmacol Ther Toxicol. 1982 Sep;20(9):417-22.
Glipizide pharmacokinetics and response in diabetics.
Huupponen R, Seppala P, Iisalo E.
The pharmacokinetics of and response to glipizide were studied in six insulin-independent diabetics by radioimmunoassay for glipizide and insulin. Blood glucose was also monitored. Beside control (off glipizide) the patients were studied when given 10 mg glipizide either as a single daily dose or divided into two doses. The peak drug concentration was reached on an average within 1.8-2.3 h. The AUCs did not differ between the two dosage regimens. The mean elimination half-life was 4.7 +/- 0.4 h, Vd 17.0 +/- 2.6 l, and the calculated total clearance 41.6 +/- 4.3 ml/min (mean +/- s.e.m.). In one patient a more than two-compartment pharmacokinetic model was obvious. The once or twice daily dosage regimens did not differ significantly in their ability to reduce blood glucose, but the overall efficacy of the therapy was poor in these patients. The maximal efficacy of a single 10-mg dose of glipizide to reduce blood glucose was maintained at the same level between 1.5 and 8 h despite the continued rapid falling of serum glipizide concentration over this period.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6754633&dopt=Abstract
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