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News About Acarbose

16-September-2008 16:15:13 - Acarbose Acarbose Systematic IUPAC name 2R,3R,4S,5R,6R-5-2R,3R,4S,5R,6R-5- 2R,3R,4S,5R,6R-3,4-dihydroxy-6-methyl- 5-1S,4S,5S,6S-4,5,6-trihydroxy-3-hydroxy methyl-1-cyclohex-2-enylaminooxan-2-yl oxy-3,4-dihydroxy-6-hydroxymethyloxan- 2-yloxy-6-hydroxymethyloxane-2,3,4-triol Identifiers CAS number 56180-94-0 ATC code A10BF01 PubChem 441184 DrugBank APRD00656 Chemical data Formula C25H43NO18 Mol. mass 645.604 g/mol Pharmacokinetic data Bioavailability Extremely low Metabolism Gastrointestinal tract Half life 2 hours Excretion Renal less than 2% Therapeutic considerations Licence data US Pregnancy cat. B3AU BUS Legal status POMUK ℞-onlyUS Routes Oral Acarbose is an anti-diabetic drug used to treat type 2 diabetes mellitus and, in some countries, prediabetes. It is sold in Europe under the brand name Glucobay Bayer AG, in North America as Precose Bayer Pharmaceuticals, and in Canada as Prandase Bayer AG. It is an inhibitor of alpha glucosidase, an enteric enzyme that releases glucose from larger carbohydrates. Contents 1 Mechanism of action 2 Dosing 3 Side effects 4 References 5 External links Mechanism of action Acarbose inhibits enzymes glycoside hydrolases needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines and pancreatic alpha-amylase. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, whereas the membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. Inhibition of these enzyme systems reduces the rate of digestion of complex carbohydrates. Less glucose is absorbed because the carbohydrates are not broken down into glucose molecules. In diabetic patients, the short-term effect of these drugs therapies is to decrease current blood glucose levels: the long term effect is a small reduction in HbA1c level.1 Dosing Since acarbose prevents the digestion of complex carbohydrates, the drug should be taken at the start of main meals. Taken with first bite of meal. Moreover, the amount of complex carbohydrates in the meal will determine the effectiveness of acarbose in decreasing postprandial hyperglycemia. Adults are to take doses of 25mg 3 times daily. Side effects Since acarbose prevents the degradation of complex carbohydrates into glucose, the carbohydrates will remain in the intestine. In the colon, bacteria will digest the complex carbohydrates, thereby causing gastrointestinal side effects such as flatulence 78% of patients and diarrhea 14% of patients. Since these effects are dose-related, it is generally advised to start with a low dose and gradually increase the dose to the desired amount. If a patient using acarbose suffers from a bout of hypoglycemia, the patient should eat something containing monosaccharides, such as glucose tablets. Since acarbose will prevent the digestion of complex carbohydrates, starchy foods will not effectively reverse a hypoglycemic episode in a patient taking acarbose. References ^ Drug Therapy in Nursing, 2nd ion. External links Precose acarbose Tablet - NIH Information Bayer Pharmaceuticals Corporation Probing the Pancreas - by Craig D. Reid, Ph.D. US FDA Consumer Article v d e Oral antidiabetic drugs and Insulin analogs A10 Insulin sensitizers Biguanides Metformin, Buformin‡, Phenformin‡ TZDs PPAR Pioglitazone, Rivoglitazone†, Rosiglitazone, Troglitazone‡ Secretagogues Sulfonylureas 1st generation: Carbutamide, Chlorpropamide, Gliclazide, Tolbutamide, Tolazamide 2nd generation: Glipizide, Glibenclamide Glyburide, Gliquidone, Glyclopyramide 3rd generation: Glimepiride Meglitinides Nateglinide, Repaglinide, Mitiglinide Glucagon-like peptide-1 analog Exenatide, Liraglutide†, Albiglutide†, Taspoglutide† DPP-4 inhibitors Alogliptin†, Linagliptin†, Saxagliptin†, Sitagliptin, Vildagliptin Alpha-glucosidase inhibitors Acarbose, Miglitol, Voglibose Amylin analog Pramlintide Experimental Dual PPAR agonists Aleglitazar†, Muraglitazar§, Tesaglitazar§ SGLT2 inhibitor Dapagliflozin†, Remogliflozin†, Sergliflozin† Insulin analogs fast acting Insulin lispro, Insulin aspart, Insulin glulisine, long acting Insulin glargine, Insulin detemir, Inhalable insulin Exubera †Undergoing clinical trials. ‡ Withdrawn from market. §Development halted. v d e Types of Carbohydrates General: Aldose | Ketose | Pyranose | Furanose Geometry Cyclohexane conformation | Anomer | Mutarotation Monosaccharides Trioses Ketotriose Dihydroxyacetone | Aldotriose Glyceraldehyde Tetroses Ketotetrose Erythrulose | Aldotetroses Erythrose, Threose Pentoses Ketopentose Ribulose, Xylulose Aldopentose Ribose, Arabinose, Xylose, Lyxose Deoxy sugar Deoxyribose Hexoses Ketohexose Psicose, Fructose, Sorbose, Tagatose Aldohexose Allose, Altrose, Glucose, Mannose, Gulose, Idose, Galactose, Talose Deoxy sugar Fucose, Fuculose, Rhamnose Heptose Sedoheptulose Multiple Disaccharides Sucrose | Lactose | Trehalose | Maltose Trisaccharides Raffinose | Melezitose | Maltotriose Tetrasaccharides Acarbose | Stachyose Other oligosaccharides Fructooligosaccharide FOS | Galacto-oligosaccharide GOS | Mannan-oligosaccharides MOS Polysaccharide Glycogen | Starch Amylose | Amylopectin | Cellulose | Chitin | Inulin | Dextrin | Glucan Beta-glucan Glycosaminoglycans Heparin | Chondroitin sulfate | Hyaluronan | Heparan sulfate | Dermatan sulfate | Keratan sulfate Aminoglycosides Kanamycin | Streptomycin | Tobramycin | Neomycin | Paromomycin | Apramycin | Gentamicin | Netilmicin | Amikacin Major families of biochemicals Saccharides | Carbohydrates | Glycosides | | Amino acids | Peptides | Proteins | Glycoproteins | | Lipids | Terpenes | Steroids | Carotenoids Alkaloids | Nucleobases | Nucleic acids | | Enzyme cofactors | Flavonoids | Polyketides | Tetrapyrroles Retrieved from http://en..org/wiki/Acarbose Categories: Alpha-glucosidase inhibitors | Oligosaccharides | Amino sugars Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages العربية Deutsch Esperanto Français Italiano Polski This page was last modified on 5 July 2008, at 02:30

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