Acarbose 1128859 223651845 2008-07-05T02:30:35Z AkhtaBot 6756213 robot Adding: [[ar:أيكاربوس]] {{drugbox | IUPAC_name = (2''R'',3''R'',4''S'',5''R'',6''R'')-5-[(2''R'',3''R'',4''S'',5''R'',6''R'')-5-<br>[(2''R'',3''R'',4''S'',5''R'',6''R'')-3,4-dihydroxy-6-methyl-<br>5-<nowiki>[[</nowiki>(1''S'',4''S'',5''S'',6''S'')-4,5,6-trihydroxy-3-(hydroxy<br>methyl)-1-cyclohex-2-enyl]amino]oxan-2-yl]<br>oxy-3,4-dihydroxy-6-(hydroxymethyl)oxan-<br>2-yl]oxy-6-(hydroxymethyl)oxane-2,3,4-triol | image = Acarbose.svg | CAS_number = 56180-94-0 | ATC_prefix = A10 | ATC_suffix = BF01 | ATC_supplemental = | PubChem = 441184 | DrugBank = APRD00656 | C = 25 |H = 43 |N = 1 |O = 18 | molecular_weight = 645.604 [[Gram|g]]/[[Mole (unit)|mol]] | bioavailability = Extremely low | protein_bound = | metabolism = [[Gastrointestinal tract]] | elimination_half-life = 2 [[hour]]s | excretion = [[Kidney|Renal]] (less than 2%) | licence_US = Precose | pregnancy_AU = B3 | pregnancy_US = B | legal_UK = POM | legal_US = Rx-only | routes_of_administration = 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|Bayer AG]]), in North America as '''Precose''' ([[Bayer|Bayer Pharmaceuticals]]), and in Canada as '''Prandase''' ([[Bayer|Bayer AG]]). It is an inhibitor of ''alpha glucosidase'', an enteric enzyme that releases [[glucose]] from larger [[carbohydrate]]s. ==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 [[oligosaccharide]]s, [[trisaccharide]]s, and [[disaccharide]]s to [[glucose]] and other [[monosaccharide]]s 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 [[glycosylated hemoglobin|Hb<sub>A1c</sub>]] level.<ref>''Drug Therapy in Nursing'', 2nd Edition.</ref> ==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 (anatomy)|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 [[monosaccharide]]s, 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== {{Reflist}} == External links == * [http://dailymed.nlm.nih.gov/dailymed/fdaDrugXsl.cfm?id=2451&type=display Precose (acarbose) Tablet - NIH Information] [Bayer Pharmaceuticals Corporation] * [http://www.cfsan.fda.gov/~dms/fdpancre.html "Probing the Pancreas" - by Craig D. Reid, Ph.D.] (US FDA Consumer Article) {{Oral_hypoglycemics}} {{Carbohydrates}} [[Category:Alpha-glucosidase inhibitors]] [[Category:Oligosaccharides]] [[Category:Amino sugars]] [[ar:أيكاربوس]] [[de:Acarbose]] [[eo:Acarboso]] [[fr:Acarbose]] [[it:Acarbosio]] [[pl:Akarboza]]