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Chemical Compound Review

acarbose     (2S,3R,4R,5S,6R)-5- [(2S,3R,4R,5S,6R)-5...

Synonyms: AC1L9HYX, 1gah, 1lf9, 1k1y, ACR
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Disease relevance of acarbose


Psychiatry related information on acarbose

  • However, even if these subjects are excluded, patients having acarbose treatment still saw a significant risk reduction in the development of diabetes (p=0.0027) [5].
  • Adjunctive treatment with acarbose (possibLy together with sulphonylurea or insulin treatment) can be effectively utilised to achieve blood glucose control if postprandial hyperglycaemia is a problem and cannot be sufficiently controlled by dietary modifications [6].
  • 3. Acarbose at both dosages was associated with phenotype-specific alterations in food intake amount and feeding pattern, resulting in an attenuation of age-associated increases in food intake [7].

High impact information on acarbose

  • 13 days after the start of treatment with acarbose, generalised erythema multiforme developed with blood eosinophilia [2].
  • A challenge test for acarbose confirmed allergic reaction clinically and histologically [2].
  • The aim of the present experiments was to investigate the fate and effects of acarbose along the small intestine using a slow-marker perfusion technique [8].
  • Recovery of acarbose during 4 h was 65% +/- 9% (mean +/- SEM) of ingested dose in the ileum but 94% +/- 9% in the jejunum, indicating that the compound was neither degraded nor absorbed by the intestine to a major degree [8].
  • Acarbose reduces the absorption of monosaccharides derived from dietary carbohydrates, which play an important role in the metabolism and toxicity of some chemical compounds [9].

Chemical compound and disease context of acarbose


Biological context of acarbose


Anatomical context of acarbose


Associations of acarbose with other chemical compounds


Gene context of acarbose

  • The results demonstrate that acarbose delays gastric emptying of solid meals and augments release of CCK, GLP-1, and PYY mainly by retarding/inhibiting carbohydrate absorption [27].
  • Inhibition of gastric emptying by acarbose is correlated with GLP-1 response and accompanied by CCK release [27].
  • Glucagon levels were higher with acarbose in the last 3 h of the 6 h observation period (p = 0.02) [28].
  • To probe the interactions of acarbose with other carbohydrate recognition enzymes, the crystal structure of E. coli maltodextrin phosphorylase (MalP) complexed with acarbose has been determined at 2.95 A resolution and refined to crystallographic R-values of R (Rfree) = 0.241 (0.293), respectively [29].
  • GIP plasma concentrations (increasing with placebo from approximately 10 to approximately 85 pmol/l and with acarbose to approximately 55 pmol/l (P < 0.0001) and their integrated responses were significantly lowered (by 43%) by acarbose (P = 0.021) [30].

Analytical, diagnostic and therapeutic context of acarbose

  • Fate and effects of the alpha-glucosidase inhibitor acarbose in humans. An intestinal slow-marker perfusion study [8].
  • We performed peptide mapping analysis to identify the protected Trp residues, and Trp321, Trp337, Trp433, and Trp569 were identified as candidates to be protected by acarbose [31].
  • Titration of placebo/acarbose is well described in the protocol and in the study design paper [5].
  • PATIENTS AND METHODS: Ninety-six patients with NIDDM (35-70 years of age, body mass index (BMI) < or = 35 kg/m2, insufficiently treated with diet alone, glycated hemoglobin (HbA1c; 7% to 11%) were randomized into 3 groups and treated for 24 weeks with acarbose, 3 x 100 mg/day, or metformin, 2 x 850 mg/day, or placebo [12].
  • This multicenter double-blind study compared the efficacy and safety of acarbose with placebo in the treatment of obese subjects with non-insulin-dependent diabetes mellitus (NIDDM) managed by diet [32].


  1. Acarbose for prevention of type 2 diabetes mellitus: the STOP-NIDDM randomised trial. Chiasson, J.L., Josse, R.G., Gomis, R., Hanefeld, M., Karasik, A., Laakso, M. Lancet (2002) [Pubmed]
  2. Acarbose-induced generalised erythema multiforme. Kono, T., Hayami, M., Kobayashi, H., Ishii, M., Taniguchi, S. Lancet (1999) [Pubmed]
  3. Low dose acarbose without symptoms of malabsorption in the dumping syndrome. Jenkins, D.J., Barker, H.M., Taylor, R.H., Fielden, H. Lancet (1982) [Pubmed]
  4. Acarbose and lymphocytic colitis. Piche, T., Raimondi, V., Schneider, S., Hébuterne, X., Rampal, P. Lancet (2000) [Pubmed]
  5. Acarbose for the prevention of Type 2 diabetes, hypertension and cardiovascular disease in subjects with impaired glucose tolerance: facts and interpretations concerning the critical analysis of the STOP-NIDDM Trial data. Chiasson, J.L., Josse, R.G., Gomis, R., Hanefeld, M., Karasik, A., Laakso, M. Diabetologia (2004) [Pubmed]
  6. Nutritional recommendations for diabetic patients and treatment with alpha-glucosidase inhibitors. Toeller, M. Drugs (1992) [Pubmed]
  7. The effect of acarbose on the food intake, weight gain, and adiposity of LA/N-cp rats. Vedula, U., Schnitzer-Polokoff, R., Tulp, O.L. Comparative biochemistry and physiology. A, Comparative physiology. (1991) [Pubmed]
  8. Fate and effects of the alpha-glucosidase inhibitor acarbose in humans. An intestinal slow-marker perfusion study. Ruppin, H., Hagel, J., Feuerbach, W., Schutt, H., Pichl, J., Hillebrand, I., Bloom, S., Domschke, W. Gastroenterology (1988) [Pubmed]
  9. Acarbose alone or in combination with ethanol potentiates the hepatotoxicity of carbon tetrachloride and acetaminophen in rats. Wang, P.Y., Kaneko, T., Wang, Y., Sato, A. Hepatology (1999) [Pubmed]
  10. Effect of starch malabsorption on fecal bile acids and neutral sterols in humans: possible implications for colonic carcinogenesis. Bartram, H.P., Scheppach, W., Heid, C., Fabian, C., Kasper, H. Cancer Res. (1991) [Pubmed]
  11. Effect of an alpha-glycosidase inhibitor on experimentally-induced obesity in mice. Le Marchand-Brustel, Y., Rochet, N., Grémeaux, T., Marot, I., Van Obberghen, E. Diabetologia (1990) [Pubmed]
  12. Efficacy of 24-week monotherapy with acarbose, metformin, or placebo in dietary-treated NIDDM patients: the Essen-II Study. Hoffmann, J., Spengler, M. Am. J. Med. (1997) [Pubmed]
  13. Pathophysiology of type 2 diabetes and modes of action of therapeutic interventions. Dagogo-Jack, S., Santiago, J.V. Arch. Intern. Med. (1997) [Pubmed]
  14. Multicenter, placebo-controlled trial comparing acarbose (BAY g 5421) with placebo, tolbutamide, and tolbutamide-plus-acarbose in non-insulin-dependent diabetes mellitus. Coniff, R.F., Shapiro, J.A., Seaton, T.B., Bray, G.A. Am. J. Med. (1995) [Pubmed]
  15. The effect of chronic alpha-glycosidase inhibition on diabetic nephropathy in the db/db mouse. Lee, S.M. Diabetes (1982) [Pubmed]
  16. Site-directed mutagenesis of histidine 93, aspartic acid 180, glutamic acid 205, histidine 290, and aspartic acid 291 at the active site and tryptophan 279 at the raw starch binding site in barley alpha-amylase 1. Søgaard, M., Kadziola, A., Haser, R., Svensson, B. J. Biol. Chem. (1993) [Pubmed]
  17. Crystal structures of 4-alpha-glucanotransferase from Thermococcus litoralis and its complex with an inhibitor. Imamura, H., Fushinobu, S., Yamamoto, M., Kumasaka, T., Jeon, B.S., Wakagi, T., Matsuzawa, H. J. Biol. Chem. (2003) [Pubmed]
  18. Single Nucleotide Polymorphisms of the Peroxisome Proliferator-Activated Receptor-{alpha} Gene (PPARA) Influence the Conversion From Impaired Glucose Tolerance to Type 2 Diabetes: The STOP-NIDDM Trial. Andrulionyte, L., Kuulasmaa, T., Chiasson, J.L., Laakso, M. Diabetes (2007) [Pubmed]
  19. The AcbC protein from Actinoplanes species is a C7-cyclitol synthase related to 3-dehydroquinate synthases and is involved in the biosynthesis of the alpha-glucosidase inhibitor acarbose. Stratmann, A., Mahmud, T., Lee, S., Distler, J., Floss, H.G., Piepersberg, W. J. Biol. Chem. (1999) [Pubmed]
  20. The pseudotetrasaccharide acarbose inhibits pancreatic islet glucan-1,4-alpha-glucosidase activity in parallel with a suppressive action on glucose-induced insulin release. Salehi, A., Panagiotidis, G., Borg, L.A., Lundquist, I. Diabetes (1995) [Pubmed]
  21. Improvement of metabolic control in insulin dependent diabetics treated with the alpha-glucosidase inhibitor acarbose for two months. Gérard, J., Luyckx, A.S., Lefebvre, P.J. Diabetologia (1981) [Pubmed]
  22. Effect of acarbose on glucose homeostasis, lipogenesis and lipogenic enzyme gene expression in adipose tissue of weaned rats. Maury, J., Issad, T., Perdereau, D., Gouhot, B., Ferré, P., Girard, J. Diabetologia (1993) [Pubmed]
  23. Effect of acarbose on exocrine and endocrine pancreatic function in the rat. Otsuki, M., Sakamoto, C., Ohki, A., Okabayashi, Y., Suehiro, I., Baba, S. Diabetologia (1983) [Pubmed]
  24. Combining insulin and oral agents. Buse, J. Am. J. Med. (2000) [Pubmed]
  25. Hyperglycemia as a cardiovascular risk factor. Haffner, S.J., Cassells, H. Am. J. Med. (2003) [Pubmed]
  26. Glibenclamide, but not acarbose, increases leptin concentrations parallel to changes in insulin in subjects with NIDDM. Haffner, S.M., Hanefeld, M., Fischer, S., Fuçker, K., Leonhardt, W. Diabetes Care (1997) [Pubmed]
  27. Inhibition of gastric emptying by acarbose is correlated with GLP-1 response and accompanied by CCK release. Enç, F.Y., Imeryüz, N., Akin, L., Turoğlu, T., Dede, F., Haklar, G., Tekeşin, N., Bekiroğlu, N., Yeğen, B.C., Rehfeld, J.F., Holst, J.J., Ulusoy, N.B. Am. J. Physiol. Gastrointest. Liver Physiol. (2001) [Pubmed]
  28. Prolonged and enhanced secretion of glucagon-like peptide 1 (7-36 amide) after oral sucrose due to alpha-glucosidase inhibition (acarbose) in Type 2 diabetic patients. Seifarth, C., Bergmann, J., Holst, J.J., Ritzel, R., Schmiegel, W., Nauck, M.A. Diabet. Med. (1998) [Pubmed]
  29. The crystal structure of the Escherichia coli maltodextrin phosphorylase-acarbose complex. O'Reilly, M., Watson, K.A., Johnson, L.N. Biochemistry (1999) [Pubmed]
  30. alpha-Glucosidase inhibition (acarbose) fails to enhance secretion of glucagon-like peptide 1 (7-36 amide) and to delay gastric emptying in Type 2 diabetic patients. Hücking, K., Kostic, Z., Pox, C., Ritzel, R., Holst, J.J., Schmiegel, W., Nauck, M.A. Diabet. Med. (2005) [Pubmed]
  31. Functional roles of Trp337 and Glu632 in Clostridium glucoamylase, as determined by chemical modification, mutagenesis, and the stopped-flow method. Ohnishi, H., Matsumoto, H., Sakai, H., Ohta, T. J. Biol. Chem. (1994) [Pubmed]
  32. Long-term efficacy and safety of acarbose in the treatment of obese subjects with non-insulin-dependent diabetes mellitus. Coniff, R.F., Shapiro, J.A., Seaton, T.B. Arch. Intern. Med. (1994) [Pubmed]
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