| Drug ID: | D001 |
| Drug Name: | Acarbose |
| Synonyms: |
--
|
| Type: | Chemical drug |
| DrugBank ID: |
DB00284
|
| DrugBank Description: |
Acarbose is a complex oligosaccharide that acts as an inhibitor of several enzymes responsible for the breakdown of complex carbohydrates in the intestines. It inhibits both pancreatic alpha-amylase and membrane-bound alpha-glucosidases - including intestinal glucoamylase, sucrase, maltase, and isomaltase - which are responsible for the metabolism of complex starches and oligo-, tri-, and disaccharides into absorbable simple sugars. By inhibiting the activity of these enzymes, acarbose limits the absorption of dietary carbohydrates and the subsequent postprandial increase in blood glucose and insulin levels. Acarbose is therefore used in conjunction with diet, exercise, and other pharmacotherapies for the management of blood sugar levels in patients with type 2 diabetes.
Acarbose is one of only two approved alpha-glucosidase inhibitors (the other being ), receiving its first FDA approval in 1995 under the brand name Precose (since discontinued). This class of antidiabetic therapy is not widely used due to their relatively modest impact on A1c, their requirement for thrice-daily dosing, and the potential for significant gastrointestinal adverse effects.
|
| PubChem ID: |
41774
|
| CasNo: |
56180-94-0
|
| Repositioning for NAFLD: |
Yes
|
| SMILES: |
O([C@@H]1[C@@H](CO)O[C@@H]([C@@H]([C@H]1O)O)O[C@@H]([C@@H]([C@H](C=O)O)O)[C@@H](CO)O)[C@@H]1[C@H](O)[C@@H](O)[C@@H]([C@H](O1)C)N[C@H]1C=C(CO)[C@H]([C@@H]([C@H]1O)O)O
|
| Structure: |
|
| InChiKey: |
CEMXHAPUFJOOSV-XGWNLRGSSA-N
|
| Molecular Weight: |
645.608
|
| DrugBank Targets: |
Maltase-glucoamylase, intestinal inhibitor; Sucrase-isomaltase, intestinal inhibitor; Pancreatic alpha-amylase inhibitor; Lysosomal alpha-glucosidase inhibitor
|
| DrugBank MoA: |
Alpha-glucosidase enzymes are located in the brush-border of the intestinal mucosa and serve to metabolize oligo-, tri-, and disaccharides (e.g. sucrose) into smaller monosaccharides (e.g. glucose, fructose) which are more readily absorbed. These work in conjunction with pancreatic alpha-amylase, an enzyme found in the intestinal lumen that hydrolyzes complex starches to oligosaccharides.
Acarbose is a complex oligosaccharide that competitively and reversibly inhibits both pancreatic alpha-amylase and membrane-bound alpha-glucosidases - of the alpha-glucosidases, inhibitory potency appears to follow a rank order of glucoamylase > sucrase > maltase > isomaltase. By preventing the metabolism and subsequent absorption of dietary carbohydrates, acarbose reduces postprandial blood glucose and insulin levels.
|
| DrugBank Pharmacology: |
Acarbose is a complex oligosaccharide that competitively inhibits the ability of brush-border alpha-glucosidase enzymes to break down ingested carbohydrates into absorbable monosaccharides, reducing carbohydrate absorption and subsequent postprandial insulin levels. Acarbose requires the co-administration of carbohydrates in order to exert its therapeutic effect, and as such should be taken with the first bite of a meal three times daily.
Given its mechanism of action, acarbose in isolation poses little risk of contributing to hypoglycemia - this risk is more pronounced, however, when acarbose is used in conjunction with other antidiabetic therapies (e.g. sulfonylureas, insulin). Patients maintained on acarbose in addition to other antidiabetic agents should be aware of the symptoms and risks of hypoglycemia and how to treat hypoglycemic episodes. There have been rare post-marketing reports of the development of pneumatosis cystoides intestinalis following treatment with alpha-glucosidase inhibitors - patients experiencing significant diarrhea/constipation, mucus discharge, and/or rectal bleeding should be investigated and, if pneumatosis cystoides intestinalis is suspected, should discontinue therapy.
|
| DrugBank Indication: |
Acarbose is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
|
| Targets: |
MGAM inhibitor;AMY2A inhibitor; AMY2B inhibitor; GAA inhibitor
|
| Therapeutic Category: |
Improve insulin resistance
|
| Clinical Trial Progress: |
Phase 2 terminated (NCT00677521: Poor recruitment and no student currently interested in working on this project.)
|
| Latest Progress: |
Under clinical trials
|
