药品详细
Miglitol (米格列醇 )
化学结构式图
中文名
米格列醇
英文名
Miglitol
分子式
Not Available
化学名
(2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol
分子量
Average: 207.2243
Monoisotopic: 207.110672659
Monoisotopic: 207.110672659
CAS号
72432-03-2
ATC分类
A10B Oral Blood Glucose Lowering Drugs, Excl. Insulins
药物类型
small molecule
阶段
商品名
Glyset;
同义名
基本介绍
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.
生产厂家
- Pharmacia and upjohn co
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Glyset 100 mg tablet | 1.46 USD | tablet |
| Glyset 50 mg tablet | 1.24 USD | tablet |
| Glyset 25 mg tablet | 1.11 USD | tablet |
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
Diabetes 糖尿病;
药理
| 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. |
| Pharmacodynamics | Miglitol, an oral alpha-glucosidase inhibitor, is a desoxynojirimycin derivative that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. As a consequence of plasma glucose reduction, miglitol reduce levels of glycosylated hemoglobin in patients with Type II (non-insulin-dependent) diabetes mellitus. Systemic nonenzymatic protein glycosylation, as reflected by levels of glycosylated hemoglobin, is a function of average blood glucose concentration over time. Because its mechanism of action is different, the effect of miglitol to enhance glycemic control is additive to that of sulfonylureas when used in combination. In addition, miglitol diminishes the insulinotropic and weight-increasing effects of sulfonylureas. Miglitol has minor inhibitory activity against lactase and consequently, at the recommended doses, would not be expected to induce lactose intolerance. |
| 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. |
| Volume of distribution |
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| Protein binding | The protein binding of miglitol is negligible (<4.0%). |
| Metabolism |
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. |
| Half life | The elimination half-life of miglitol from plasma is approximately 2 hours. |
| Clearance | Not Available |
| 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. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 114 oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Glucosamine | Possible hyperglycemia |
| Somatropin recombinant | Somatropin may antagonize the hypoglycemic effect of miglitol. Monitor for changes in fasting and postprandial blood sugars. |
食物相互作用
- Take with food, at beginning of each meal. Iron needs increased.
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