DB00491 - Miglitol
| Identification | |||||||
|---|---|---|---|---|---|---|---|
| Name | Miglitol | ||||||
| Accession Number | DB00491 (APRD01117) | ||||||
| Type | small molecule | ||||||
| Description | Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body. Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. Since miglitol works by preventing digestion of carbohydrates, it lowers the degree of postprandial hyperglycemia. It must be taken at the start of main meals to have maximal effect. Its effect will depend on the amount of non-monosaccharide carbohydrates in a person's diet. In contrast to acarbose (another alpha-glucosidase inhibitor), miglitol is systemically absorbed; however, it is not metabolized and is excreted by the kidneys. | ||||||
| Structure |
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| Categories (*) | |||||||
| Molecular Weight | 207.2243 | ||||||
| Groups | approved | ||||||
| Monoisotopic Weight | 207.110672659 | ||||||
| Pharmacology | |||||||
| Indication | For use as an adjunct to diet to improve glycemic control in patients with non-insulin-dependent diabetes mellitus (NIDDM) whose hyperglycemia cannot be managed with diet alone. | ||||||
| Mechanism of action | In contrast to sulfonylureas, miglitol does not enhance insulin secretion. The antihyperglycemic action of miglitol results from a reversible inhibition of membrane-bound intestinal a-glucoside hydrolase enzymes. Membrane-bound intestinal a-glucosidases hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia. | ||||||
| Absorption | Absorption of miglitol is saturable at high doses with 25 mg being completely absorbed while a 100-mg dose is only 50-70% absorbed. No evidence exists to show that systemic absorption of miglitol adds to its therapeutic effect. | ||||||
| Protein binding | The protein binding of miglitol is negligible (<4.0%). | ||||||
| Biotransformation | Miglitol is not metabolized in man or in any animal species studied. | ||||||
| Route of elimination | Miglitol is not metabolized in man or in any animal species studied. It is eliminated by renal excretion as an unchanged drug. | ||||||
| Toxicity | Unlike sulfonylureas or insulin, an overdose will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdomi-nal discomfort. Because of the lack of extra-intestinal effects seen with miglitol, no serious systemic reactions are expected in the event of an overdose. | ||||||
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Targets
| Maltase-glucoamylase, intestinal | |
|---|---|
| Name | Maltase-glucoamylase, intestinal |
| Gene Name | MGAM |
| Pharmacological action | yes |
| Actions | antagonist,inhibitor |
| References |
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| DTHybrid score | 1.3023 |
| Lysosomal alpha-glucosidase | |
| Name | Lysosomal alpha-glucosidase |
| Gene Name | GAA |
| Pharmacological action | yes |
| Actions | antagonist |
| References |
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| DTHybrid score | 0.8558 |
| Neutral alpha-glucosidase AB | |
| Name | Neutral alpha-glucosidase AB |
| Gene Name | Not Available |
| Pharmacological action | yes |
| Actions | antagonist |
| References |
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| DTHybrid score | Not Available |
| Neutral alpha-glucosidase C | |
| Name | Neutral alpha-glucosidase C |
| Gene Name | Not Available |
| Pharmacological action | yes |
| Actions | antagonist |
| References |
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| DTHybrid score | Not Available |
Enzymes
| Pancreatic alpha-amylase | |
|---|---|
| Name | Pancreatic alpha-amylase |
| Gene Name | AMY2A |
| Actions | Not Available |
| References | Not Available |
| DTHybrid score | 1.586 |