Drugs online research references
Res Vet Sci. 1992 Mar;52(2):177-81.
Effect of glipizide on serum insulin and glucose concentrations in healthy cats.
Miller AB, Nelson RW, Kirk CA, Neal L, Feldman EC.
Veterinary Medical Teaching Hospital, Department of Medicine, University of California, Davis 95616.
With the recent identification of non-insulin-dependent diabetes mellitus (NIDDM) in cats, new possibilities arise for the use of oral hypoglycaemic agents in the treatment of feline NIDDM, similar to their use in humans. To identify the future applicability of the oral hypoglycaemic agent, glipizide, in the treatment of feline NIDDM, its effects on serum insulin and glucose concentrations in healthy cats was examined. In addition, adverse effects seen clinically or on bloodwork following short-term use of the drug were looked for. Serum insulin and glucose concentrations were evaluated after the oral administration of 2.5, 5.0 and 10.0 mg glipizide and placebo in 10 healthy cats. For each drug trial, blood was obtained five minutes before, immediately before, and 7.5, 15, 30, 45, 60, 90 and 120 minutes after glipizide or placebo administration. Mean serum insulin concentration increased after glipizide administration, with peak mean serum insulin concentration occurring 15 minutes after administration and declining to baseline by 60 minutes. There was no significant difference in peak mean serum insulin concentration, mean serum insulin concentration at 60 minutes after glipizide administration, or mean total insulin secretion between the three glipizide dosages. Mean serum glucose concentration decreased within 15 minutes of glipizide administration, with the glucose nadir occurring 60 minutes after glipizide administration. Placebo trials showed no significant change in mean serum insulin or glucose concentrations from baseline concentrations.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1585076&dopt=Abstract
Ann Med Interne (Paris). 1992;143(1):11-7.
[Hypoglycemia induced by oral hypoglycemic agents. Records of the French Regional Pharmacovigilance Centers 1985-1990]
[Article in French]
Girardin E, Vial T, Pham E, Evreux JC.
Service d'Endocrinologie, Hopital Edouard-Herriot, Lyon.
All 98 cases of sulfonylurea-induced hypoglycemia reported by the 30 regional drug-monitoring centers between 1985 and 1990 were analyzed: 46 with gliclazide, 40 with glibenclamide, 5 with glipizide, 1 with glibornuride and 6 with first-generation sulfonylureas. These cases of hypoglycemia were often serious. The patients were 61% female and their mean age was 78.9 years. The average number of medications being taken was 3.4, but ranged up to 14. The risk factors were: reduced food intake (4.2%), renal failure (4.2%), prescription error (3.2%), voluntary or accidental overdose (5.2%), alcohol (1.1%), suspected drug interactions (50%), unknown (32.6%). The most frequent drug interactions involved miconazole (8 cases), angiotensin-converting enzyme inhibitors (9 cases), lipid-regulating agents (fibrates) (7 cases), co-trimoxazole (trimethoprim-sulfamethoxazole; 5 cases), metformin (4 cases), histamine H2-receptor antagonists (4 cases). The mechanisms of these interactions are discussed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1605454&dopt=Abstract
J Biol Chem. 1992 Jul 25;267(21):14928-33.
Specificity of photolabeling of beta-cell membrane proteins with an 125I-labeled glyburide analog.
Nelson DA, Aguilar-Bryan L, Bryan J.
Department of Medicine, Baylor College of Medicine, Houston, Texas 77030.
The interaction between sulfonylureas and membrane proteins from a hamster insulin-secreting tumor (HIT) cell line has been examined. Four HIT cell membrane proteins were covalently linked to an 125I-labeled glyburide analog by photolabeling. Three photolabeled polypeptides of M(r) 65,000, 55,000, and 30,000 were identified as low affinity "glyburide receptors." These proteins appear to be of similar abundance, when quantitated by photolabeling, with half-maximal displacements (Ki values) by glyburide, glipizide, and tolbutamide in the low micromolar range. The glyburide analog is more tightly bound to a M(r) 140,000 protein with dissociation constants, determined by filtration binding assays and by photolabeling, of 7 and 9.0 nM, respectively. The labeled analog was displaced from the M(r) 140,000 protein by glyburide, glipizide and tolbutamide with Ki values of 3.3 nM, 103 nM, and 25 microM, respectively, as estimated by photolabeling. Optimal conditions established for visualizing the M(r) 140,000 band on autoradiograms prepared after UV cross-linking and sodium dodecyl sulfate-polyacrylamide gel electrophoresis include irradiating the radioligand-receptor complex at 1.5 J/cm2 at 312 nm, followed by heating samples in pH 9.0 sodium dodecyl sulfate-gel sample buffer. With receptor sites partially occupied (5 nM radioligand), approximately 0.75% of the protein is photocoupled to the radioligand and visualized by autoradiography. Our results confirm that the M(r) 140,000 polypeptide contains the beta-cell high affinity glyburide binding site and show that the second generation sulfonylurea antidiabetic drugs have a selective increase in affinity for this receptor.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1634533&dopt=Abstract
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