Identification
- Summary
Miglitol is an oral alpha-glucosidase inhibitor used to improve glycemic control by delaying the digestion of carbohydrates.
- Generic Name
- Miglitol
- DrugBank Accession Number
- DB00491
- Background
Miglitol inhibits the 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 should be taken at the start of a meal for maximal effect and the effect will depend on the amount of poly and oligosaccharides in the diet. Miglitol inhibits alpha-glucosidase, making less sugars available for digestion and reducing postprandial hyperglycemia.
Unlike other drugs of the same class, miglitol is not metabolized and the unmetabolized drug is excreted by the kidneys.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Miglitol (DB00491)
- Weight
- Average: 207.2243
Monoisotopic: 207.110672659 - Chemical Formula
- C8H17NO5
- Synonyms
- Miglitol
- Miglitolum
- External IDs
- Bay m 1099
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.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used as adjunct in combination to manage Type 2 diabetes mellitus Combination Product in combination with: Metformin (DB00331) •••••••••••• ••••• ••••••• •••••••••••• Management of Type 2 diabetes mellitus •••••••••••• - Contraindications & Blackbox Warnings
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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.
Target Actions Organism ALysosomal alpha-glucosidase antagonistHumans ANeutral alpha-glucosidase AB antagonistHumans ANeutral alpha-glucosidase C antagonistHumans AMaltase-glucoamylase, intestinal antagonistinhibitorHumans - 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
- 0.18 L/kg
- 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
- Adverse Effects
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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.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Miglitol. Acebutolol The therapeutic efficacy of Miglitol can be increased when used in combination with Acebutolol. Acetazolamide The therapeutic efficacy of Miglitol can be increased when used in combination with Acetazolamide. Acetohexamide The risk or severity of hypoglycemia can be increased when Miglitol is combined with Acetohexamide. Acetyl sulfisoxazole The therapeutic efficacy of Miglitol can be increased when used in combination with Acetyl sulfisoxazole. - Food Interactions
- Take with food. Take at the beginning of a meal.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- International/Other Brands
- Diaban (Chen Ho) / Diamig (Micro DTF) / Diaset (ACI) / Diastabol (Sanofi-Aventis) / Elitox (Ranbaxy) / Euglitol (Abbott) / Glycet (Pfizer) / Laiping (Xinchang Pharmaceutical) / Migbose (Standard) / Miglit (Biocon) / Mignar (Glenmark) / Migtor (Torrent) / Misobit (Lupin) / Plumarol (Lacer) / Seibule (Sanwa Kagaku)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Glyset Tablet, film coated 50 mg/1 Oral Pharmacia & Upjohn Company LLC 1996-12-18 2021-07-31 US 
Glyset Tablet, film coated 25 mg/1 Oral Pharmacia & Upjohn Company LLC 1996-12-18 2021-07-31 US 
Glyset Tablet, film coated 100 mg/1 Oral Pharmacia & Upjohn Company LLC 1996-12-18 2021-07-31 US Glyset Tablet, film coated 50 mg/1 Oral Physicians Total Care, Inc. 1996-12-18 2010-06-30 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Miglitol Tablet, coated 50 mg/1 Oral Sun Pharmaceutical Industries Inc. 2016-01-04 Not applicable US Miglitol Tablet, coated 100 mg/1 Oral Orient Pharma Co., Ltd. 2015-07-31 Not applicable US Miglitol Tablet, coated 100 mg/1 Oral Proficient Rx LP 2021-01-15 Not applicable US Miglitol Tablet, coated 100 mg/1 Oral Westminster Pharmaceuticals, LLC 2021-01-15 Not applicable US Miglitol Tablet, coated 100 mg/1 Oral Sun Pharmaceutical Industries Inc. 2016-01-04 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image MEGLITIS 100/500MG EFERVESAN TABLET, 100 TABLET Miglitol (100 mg) + Metformin hydrochloride (500 mg) Tablet, effervescent Oral CELTİS İLAÇ SAN. VE TİC. A.Ş. 2013-01-24 Not applicable Turkey 
MEGLITIS 100/850MG EFERVESAN TABLET, 100 TABLET Miglitol (100 mg) + Metformin hydrochloride (850 mg) Tablet, effervescent Oral CELTİS İLAÇ SAN. VE TİC. A.Ş. 2013-01-24 Not applicable Turkey
Categories
- ATC Codes
- A10BF02 — Miglitol
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as piperidines. These are compounds containing a piperidine ring, which is a saturated aliphatic six-member ring with one nitrogen atom and five carbon atoms.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Piperidines
- Sub Class
- Not Available
- Direct Parent
- Piperidines
- Alternative Parents
- Trialkylamines / Secondary alcohols / 1,2-aminoalcohols / Polyols / Azacyclic compounds / Primary alcohols / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- 1,2-aminoalcohol / Alcohol / Aliphatic heteromonocyclic compound / Alkanolamine / Amine / Azacycle / Hydrocarbon derivative / Organic nitrogen compound / Organic oxygen compound / Organonitrogen compound
- Molecular Framework
- Aliphatic heteromonocyclic compounds
- External Descriptors
- piperidines (CHEBI:6935)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 0V5436JAQW
- CAS number
- 72432-03-2
- InChI Key
- IBAQFPQHRJAVAV-ULAWRXDQSA-N
- InChI
- InChI=1S/C8H17NO5/c10-2-1-9-3-6(12)8(14)7(13)5(9)4-11/h5-8,10-14H,1-4H2/t5-,6+,7-,8-/m1/s1
- IUPAC Name
- (2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol
- SMILES
- OCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO
References
- General References
- FDA Approved Drug Products: Glyset (miglitol) tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0014634
- KEGG Drug
- D00625
- KEGG Compound
- C07708
- PubChem Compound
- 441314
- PubChem Substance
- 46504492
- ChemSpider
- 390074
- BindingDB
- 50242271
- 30009
- ChEBI
- 6935
- ChEMBL
- CHEMBL1561
- ZINC
- ZINC000004097426
- Therapeutic Targets Database
- DAP000712
- PharmGKB
- PA164776726
- PDBe Ligand
- MIG
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Miglitol
- PDB Entries
- 3l4w / 5nn6 / 6ca1 / 6ca3
- MSDS
- Download (68.8 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Completed Treatment Type 1 Diabetes Mellitus 1 3 Completed Treatment Type 2 Diabetes Mellitus 6 1 Completed Not Available Healthy Subjects (HS) / Pharmacokinetics of ASP1941 1 Not Available Completed Not Available Type 2 Diabetes Mellitus 3
Pharmacoeconomics
- Manufacturers
- Pharmacia and upjohn co
- Packagers
- Bayer Healthcare
- Kaiser Foundation Hospital
- Pharmacia Inc.
- Physicians Total Care Inc.
- Dosage Forms
Form Route Strength Tablet, effervescent 100 mg Tablet, effervescent 25 mg Tablet, effervescent 50 mg Tablet, film coated Oral 100 mg/1 Tablet, film coated Oral 25 mg/1 Tablet, film coated Oral 50 mg/1 Tablet, effervescent Oral Tablet Oral Tablet, coated Oral 100 mg/1 Tablet, coated Oral 25 mg/1 Tablet, coated Oral 50 mg/1 Tablet Oral 100 mg Tablet Oral 25 mg Tablet Oral 50 mg - Prices
Unit description Cost Unit Glyset 100 mg tablet 1.46USD tablet Glyset 50 mg tablet 1.24USD tablet Glyset 25 mg tablet 1.11USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 114 °C Not Available water solubility Soluble Not Available logP -2.7 Not Available pKa 5.9 Not Available - Predicted Properties
Property Value Source Water Solubility 610.0 mg/mL ALOGPS logP -2.3 ALOGPS logP -3.2 Chemaxon logS 0.47 ALOGPS pKa (Strongest Acidic) 12.9 Chemaxon pKa (Strongest Basic) 7.6 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 5 Chemaxon Polar Surface Area 104.39 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 48.16 m3·mol-1 Chemaxon Polarizability 20.78 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.5422 Blood Brain Barrier - 0.8379 Caco-2 permeable - 0.7375 P-glycoprotein substrate Substrate 0.6354 P-glycoprotein inhibitor I Non-inhibitor 0.7325 P-glycoprotein inhibitor II Non-inhibitor 0.8248 Renal organic cation transporter Non-inhibitor 0.6749 CYP450 2C9 substrate Non-substrate 0.8563 CYP450 2D6 substrate Non-substrate 0.8168 CYP450 3A4 substrate Non-substrate 0.6208 CYP450 1A2 substrate Non-inhibitor 0.927 CYP450 2C9 inhibitor Non-inhibitor 0.9022 CYP450 2D6 inhibitor Non-inhibitor 0.9535 CYP450 2C19 inhibitor Non-inhibitor 0.9676 CYP450 3A4 inhibitor Non-inhibitor 0.9931 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9968 Ames test Non AMES toxic 0.79 Carcinogenicity Non-carcinogens 0.9702 Biodegradation Not ready biodegradable 0.5392 Rat acute toxicity 1.7432 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5797 hERG inhibition (predictor II) Non-inhibitor 0.8756
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-00r5-2900000000-56f32f82ba2fcf0b2f3f Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0a4i-0290000000-be523d426ced7c54327e Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0a59-2960000000-1ef06c9ebe223c58d097 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-052f-1920000000-1e8481b881302fbd86f3 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0f89-9500000000-ab5ebf44cb0c8424e274 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0bt9-9400000000-d0d470803defcd803058 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0a4i-9200000000-35000d72e423f62be8d4 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 150.6386877 predictedDarkChem Lite v0.1.0 [M-H]- 148.3049877 predictedDarkChem Lite v0.1.0 [M-H]- 147.51454 predictedDeepCCS 1.0 (2019) [M+H]+ 150.3344877 predictedDarkChem Lite v0.1.0 [M+H]+ 148.2624877 predictedDarkChem Lite v0.1.0 [M+H]+ 149.91011 predictedDeepCCS 1.0 (2019) [M+Na]+ 150.6092877 predictedDarkChem Lite v0.1.0 [M+Na]+ 147.8993877 predictedDarkChem Lite v0.1.0 [M+Na]+ 155.93768 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Maltose alpha-glucosidase activity
- Specific Function
- Essential for the degradation of glygogen to glucose in lysosomes.
- Gene Name
- GAA
- Uniprot ID
- P10253
- Uniprot Name
- Lysosomal alpha-glucosidase
- Molecular Weight
- 105322.935 Da
References
- Fukaya N, Mochizuki K, Tanaka Y, Kumazawa T, Jiuxin Z, Fuchigami M, Goda T: The alpha-glucosidase inhibitor miglitol delays the development of diabetes and dysfunctional insulin secretion in pancreatic beta-cells in OLETF rats. Eur J Pharmacol. 2009 Dec 10;624(1-3):51-7. doi: 10.1016/j.ejphar.2009.09.048. Epub 2009 Oct 7. [Article]
- Hirata A, Igarashi M, Iwai H, Tominaga M: Effect of miglitol, an alpha-glucosidase inhibitor, on atherogenic outcomes in balloon-injured diabetic rats. Horm Metab Res. 2009 Mar;41(3):213-20. doi: 10.1055/s-0028-1105919. Epub 2008 Dec 15. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Poly(a) rna binding
- Specific Function
- Cleaves sequentially the 2 innermost alpha-1,3-linked glucose residues from the Glc(2)Man(9)GlcNAc(2) oligosaccharide precursor of immature glycoproteins.
- Gene Name
- GANAB
- Uniprot ID
- Q14697
- Uniprot Name
- Neutral alpha-glucosidase AB
- Molecular Weight
- 106873.125 Da
References
- Fukaya N, Mochizuki K, Tanaka Y, Kumazawa T, Jiuxin Z, Fuchigami M, Goda T: The alpha-glucosidase inhibitor miglitol delays the development of diabetes and dysfunctional insulin secretion in pancreatic beta-cells in OLETF rats. Eur J Pharmacol. 2009 Dec 10;624(1-3):51-7. doi: 10.1016/j.ejphar.2009.09.048. Epub 2009 Oct 7. [Article]
- Hirata A, Igarashi M, Iwai H, Tominaga M: Effect of miglitol, an alpha-glucosidase inhibitor, on atherogenic outcomes in balloon-injured diabetic rats. Horm Metab Res. 2009 Mar;41(3):213-20. doi: 10.1055/s-0028-1105919. Epub 2008 Dec 15. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Maltose alpha-glucosidase activity
- Specific Function
- Has alpha-glucosidase activity.
- Gene Name
- GANC
- Uniprot ID
- Q8TET4
- Uniprot Name
- Neutral alpha-glucosidase C
- Molecular Weight
- 104333.445 Da
References
- Fukaya N, Mochizuki K, Tanaka Y, Kumazawa T, Jiuxin Z, Fuchigami M, Goda T: The alpha-glucosidase inhibitor miglitol delays the development of diabetes and dysfunctional insulin secretion in pancreatic beta-cells in OLETF rats. Eur J Pharmacol. 2009 Dec 10;624(1-3):51-7. doi: 10.1016/j.ejphar.2009.09.048. Epub 2009 Oct 7. [Article]
- Hirata A, Igarashi M, Iwai H, Tominaga M: Effect of miglitol, an alpha-glucosidase inhibitor, on atherogenic outcomes in balloon-injured diabetic rats. Horm Metab Res. 2009 Mar;41(3):213-20. doi: 10.1055/s-0028-1105919. Epub 2008 Dec 15. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AntagonistInhibitor
- General Function
- Maltose alpha-glucosidase activity
- Specific Function
- May serve as an alternate pathway for starch digestion when luminal alpha-amylase activity is reduced because of immaturity or malnutrition. May play a unique role in the digestion of malted dietar...
- Gene Name
- MGAM
- Uniprot ID
- O43451
- Uniprot Name
- Maltase-glucoamylase, intestinal
- Molecular Weight
- 209850.8 Da
References
- Mooradian AD, Thurman JE: Drug therapy of postprandial hyperglycaemia. Drugs. 1999 Jan;57(1):19-29. [Article]
- Rossi EJ, Sim L, Kuntz DA, Hahn D, Johnston BD, Ghavami A, Szczepina MG, Kumar NS, Sterchi EE, Nichols BL, Pinto BM, Rose DR: Inhibition of recombinant human maltase glucoamylase by salacinol and derivatives. FEBS J. 2006 Jun;273(12):2673-83. [Article]
- Fukaya N, Mochizuki K, Tanaka Y, Kumazawa T, Jiuxin Z, Fuchigami M, Goda T: The alpha-glucosidase inhibitor miglitol delays the development of diabetes and dysfunctional insulin secretion in pancreatic beta-cells in OLETF rats. Eur J Pharmacol. 2009 Dec 10;624(1-3):51-7. doi: 10.1016/j.ejphar.2009.09.048. Epub 2009 Oct 7. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Chloride ion binding
- Specific Function
- Not Available
- Gene Name
- AMY2A
- Uniprot ID
- P04746
- Uniprot Name
- Pancreatic alpha-amylase
- Molecular Weight
- 57706.51 Da
References
- Mohamed EA, Siddiqui MJ, Ang LF, Sadikun A, Chan SH, Tan SC, Asmawi MZ, Yam MF: Potent alpha-glucosidase and alpha-amylase inhibitory activities of standardized 50% ethanolic extracts and sinensetin from Orthosiphon stamineus Benth as anti-diabetic mechanism. BMC Complement Altern Med. 2012 Oct 8;12:176. doi: 10.1186/1472-6882-12-176. [Article]
Drug created at June 13, 2005 13:24 / Updated at November 03, 2023 23:43