English alias: Seibule;BAY 1099; BAY-m-1099; GLYSET; Plumarol;
CAS No.: 72432-03-2
Molecular formula: CeightHseventeenNOfive
Molecular weight: 207.22400
Precision quality: 207.11100
PSA：104.39000
Physicochemical properties
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Appearance and property: white to yellowish crystalline powder
Density: 1.458 g/cmthree
Melting point: 114 º C
Boiling point: 453.7 º C at 760 mmHg
Flash point: 284.3 º C
Refractive index: 1.597
Storage condition: Store in original container in a cool dark place[1]
Related drug information
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Classification name
Class I classification: endocrine system drugs Class II classification: drugs for diabetes and pancreatic islet diseases Class III classification:
English name of drug
Miglitol
Drug alias
Desaytian, Mignesol, Glyset
Drug dosage form
Miglitol tablets: 25mg/tablet;50mg/tablet;100mg/tablet.Store at 15~30 ℃.
pharmacological action
This product is the second generation glucosidase inhibitor.This product is a small molecule compound, and its structure is similar to glucose.During food digestion, α - glucosidase (including maltase, isomaltase, sucrase, glucoamylase, etc.) can hydrolyze polysaccharides and oligosaccharides in food into monosaccharides (including glucose).α - glucosidase inhibitors can delay the production and absorption of glucose, thus alleviating the postprandial hyperglycemia and its rapid changes in blood glucose in diabetic patients.This product mainly acts on the small intestine and has little effect on the hydrolysis of carbohydrates in the colon. The gastrointestinal adverse reactions secondary to the fermentation of unabsorbed sugars are less common than acarbose.
Pharmacokinetics
This product is more easily absorbed in the small intestine than acarbose, and the absorption degree of oral administration decreases with the increase of dosage.The bioavailability of 25 mg orally is 100%, and that of 100 mg orally is about 50%~70%. At higher doses, the absorption can reach saturation.Its protein binding rate is lower than 4%, and its distribution volume is 0.18L/kg.It is less metabolized in the body, and more than 95% of the drug is excreted from urine in its original form. When the dose exceeds 25mg, a small amount of drug can be reabsorbed through urine due to incomplete absorption.The half-life of this product is 2h.
Indications
It is used to treat adult type 2 diabetes.
Contraindication
The following patients are forbidden.1. People who are allergic to this product.2. Diabetic ketoacidosis.3. Patients with chronic intestinal diseases with indigestion or malabsorption.4. Inflammatory bowel disease or other diseases that increase intestinal gas production.5. Intestinal obstruction.6. This product is not suitable for children.
matters needing attention
1. This product should be taken at the beginning of each meal.2. In case of hypoglycemia, it is better to take glucose orally rather than sucrose, because this product can delay the absorption of sucrose.3. In the case of trauma, fever, infection, surgery, etc., this product may not be effective in reducing blood sugar, and insulin should be used when necessary.4. The pregnancy safety of this product is classified as Grade B.5. The concentration of this product excreted to the milk is very low, which has almost no effect on the newborn, but it is still recommended that lactating women stop taking the drug.6. Monitor blood glucose regularly during medication, and monitor blood glucose level 1h after meal at the beginning of treatment.HbAlc is monitored regularly.7. Caution: Patients with serum creatinine concentration higher than 2mg/dl should be cautious.
Adverse reactions
1. Metabolic/endocrine system: This product can affect glycogen metabolism, may inhibit glycogen decomposition in the liver, and may cause hypoglycemia if overdosed on an empty stomach.According to the mechanism of action of this product, hypoglycemia should not be caused when it is used alone on an empty stomach or after meals, but combined with sulfonylurea drugs or insulin, it may lead to further reduction of blood glucose concentration, increasing the possibility of hypoglycemia.2. Digestive system: common gastrointestinal reactions. The incidence of abdominal pain, diarrhea, and flatulence may be positively related to the dose. When continuing treatment, abdominal pain and diarrhea can be alleviated.3. Blood: There are reports of decreased serum iron concentration and anemia.4. Skin: Most rashes are transient.
Usage and dosage
Oral administration, used for type 2 diabetes, can be used alone or in combination with sulfonylurea hypoglycemic drugs.The initial dose is 25mg per time, 3 times per day, and individual patients need to gradually increase from 1 time per day to 3 times per day at the beginning.After 4-8 weeks, it can be increased to 50mg each time, three times a day, for three months.During this period, the glycosylated hemoglobin (HbAlc) should be measured to determine whether it is necessary to add it to 100mg every time, three times a day (the maximum recommended amount).Some studies believe that in the range of 25-200mg, the efficacy increases with the dose, but the gastrointestinal adverse reactions also increase accordingly.The optimal dosage range of the product used alone is 50-100mg each time, three times a day.
Drug interaction
1. When used together with intestinal adsorbents such as activated carbon, the efficacy of this product will be reduced, and the combination of the two should be avoided.2. When used together with digestive enzyme agents containing amylase, pancreatin and other sugar decomposing enzymes, the efficacy of this product is reduced, so it should be avoided.3. This product may reduce the blood concentration of digoxin. When the two drugs are used together, the blood concentration of digoxin should be monitored.4. This product can slightly reduce the peak blood concentration and the area under the drug time curve of glibenclamide, but this change has no significant clinical significance.In addition, when this product is used in combination with sulfonylurea hypoglycemic drugs, the risk of hypoglycemia increases, which should be noted.5. This product can reduce the bioavailability of ranitidine by about 60%. When the two are used together, attention should be paid to the efficacy of ranitidine.6. There is no obvious interaction between this product and antacid, warfarin, nifedipine.[2]
clinical application
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Clinical research shows that for patients with type II diabetes mellitus, 50mg is administered three times a day, and blood samples are collected to 3 hours every 30 minutes before (0 hours) and after administration, and the average is plottedblood sugarConcentration time curve.Compared with the control group, the blood glucose decreased most significantly 60~90 minutes after taking the medicine, and there was no adverse reaction.The study showed that oral administration of 50mg miglitol and oral administration of 300mgAcarboseLower after mealhyperglycemiaAnd mean blood glucose concentration.The drug is not metabolized in the body and is quickly excreted in the urine after oral administration.AndSulfonylureaandBiguanidesCompared with the drugs, the side effects were significantly reduced.Since the drug only delays the absorption of monosaccharide in the intestinal tract and does not inhibit α - amylase, it will not leave unabsorbed oligosaccharides in the intestinal tract, eliminating the serious intestinal side effects of acarbose.Although sometimes mild gastrointestinal side effects may occur, the method of gradually increasing the dose can be used to alleviate them.In addition, clinical studies have shown that long-term oral administration of this drug canurinary system、cardiovascular system, respiratory system and blood parameters have no significant impact, therefore, elderly patients, patients with liver function or mild renal function injury do not need to adjust the dosage when taking this product.
Other information
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Miglitol is a new type of drug developed by Bayer Pharmaceutical Company in the early 1990sHypoglycemic drugsIs a new kind of small intestineα - glucosidase inhibitor。Miglitol is similar to glucose in structure and can reversiblyCompetitive inhibitionPseudomonosaccharide alpha glucosidase, paraVillus of small intestineα - of brush edgeGlycosidaseasSucraseGlucoamylaseMaltase、IsomaltoseEnzymesTrehalaseAnd lactase, which are highly effective inhibitors of sucrase and do not inhibit the activity of α - amylase.Because the mechanism of action is reversible competitive inhibition, the compound does not completely inhibit the absorption of glucose, but retards the absorption process of glucose, making the absorption of glucose in various regions of the digestive tract more average, thus smoothing the sharp points produced by the digestion and absorption of carbohydrates after mealsblood sugarpeak value.
