Miglitol

Last updated

Miglitol
Miglitol2.svg
Clinical data
Trade names Glyset
AHFS/Drugs.com Monograph
MedlinePlus a601079
License data
Pregnancy
category
  • AU:B3
Routes of
administration
By mouth (tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability Dose-dependent
Protein binding Negligible (<4.0%)
Metabolism Nil
Elimination half-life 2 hours
Excretion Renal (95%)
Identifiers
  • (2R,3R,4R,5S)-1-(2-Hydroxyethyl)-2-(hydroxymethyl)
    piperidine-3,4,5-triol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.069.670 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C8H17NO5
Molar mass 207.226 g·mol−1
3D model (JSmol)
Density 1.458 g/cm3
Melting point 114 °C (237 °F)
  • OCCN1[C@@H]([C@@H](O)[C@H](O)[C@@H](O)C1)CO
  • 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 Yes check.svgY
  • Key:IBAQFPQHRJAVAV-ULAWRXDQSA-N Yes check.svgY
   (verify)

Miglitol is an oral alpha-glucosidase inhibitor used in the treatment of type 2 diabetes. It works by reversibly inhibiting alpha-glucosidase enzymes in the small intestine, which delays the digestion of complex carbohydrates and subsequently reduces postprandial glucose levels. [1] Approved for clinical use since 1998, miglitol has demonstrated efficacy in improving glycemic control, reducing HbA1c levels, and decreasing both fasting and postprandial plasma glucose concentrations in long-term clinical trials. [1] [2] Additionally, recent studies have suggested that miglitol may have potential as an anti-obesity agent, showing promise in reducing body weight and body mass index in obese or diabetic patients. [3] While generally well-tolerated, the most common side effects associated with miglitol are gastrointestinal disturbances, which are typically mild to moderate and tend to decrease over time. [1]

Contents

It must be taken at the start of main meals to have maximal effect [4]

In contrast to acarbose (another alpha-glucosidase inhibitor), miglitol is systemically absorbed; however, it is not metabolized and is excreted by the kidneys.

Formulation

The benefits of alpha-glucosidase inhibitors on health were shown to be stronger when the powder is consumed orally dissolved in water as a beverage in comparison to its intake as ordinary hard gelatin capsules. [5]

See also

Related Research Articles

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Hypoglycemia, also spelled hypoglycaemia or hypoglycæmia, sometimes called low blood sugar, is a fall in blood sugar to levels below normal, typically below 70 mg/dL (3.9 mmol/L). Whipple's triad is used to properly identify hypoglycemic episodes. It is defined as blood glucose below 70 mg/dL (3.9 mmol/L), symptoms associated with hypoglycemia, and resolution of symptoms when blood sugar returns to normal. Hypoglycemia may result in headache, tiredness, clumsiness, trouble talking, confusion, fast heart rate, sweating, shakiness, nervousness, hunger, loss of consciousness, seizures, or death. Symptoms typically come on quickly.

<span class="mw-page-title-main">Hyperglycemia</span> Too much blood sugar, usually because of diabetes

Hyperglycemia or hyperglycaemia is the situation in which blood glucose level is higher than in a healthy subject. A fasting healthy human shows blood glucose level up to 5.6 mmol/L (100 mg/dL). After a meal (postprandial) containing carbohydrates, healthy subjects show postpandrial euglycemic peaks of less than 140 mg/dL (7.8 mmol/L). Therefore, fasting hyperglycemia are values of blood glucose higher than 5.6 mmol/L (100 mg/dL) whereas postprandial hyperglycemia are values higher than 140 mg/dL (7.8 mmol/L). Postprandial hyperglycemic levels as high as 155 mg/dL (8.6 mmol/L) at 1-h are associated with T2DM-related complications, which worsen as the degree of hyperglycemia increases. Patients with diabetes are oriented to avoid exceeding the recommended postprandial threshold of 160 mg/dL (8.89 mmol/L) for optimal glycemic control. Values of blood glucose higher than 160 mg/dL are classified as ‘very high’ hyperglycemia, a condition in which an excessive amount of glucose (glucotoxicity) circulates in the blood plasma. These values are higher than the renal threshold of 180 mg/dL (10 mmol/L) up to which glucose reabsorption is preserved at physiological rates and insulin therapy is not necessary. Blood glucose values higher than the cutoff level of 200 mg/dL (11.1 mmol/L) are used to diagnose T2DM and strongly associated with metabolic disturbances, although symptoms may not start to become noticeable until even higher values such as 13.9–16.7 mmol/L (~250–300 mg/dL). A subject with a consistent fasting blood glucose range between ~5.6 and ~7 mmol/L is considered slightly hyperglycemic, and above 7 mmol/L is generally held to have diabetes. For diabetics, glucose levels that are considered to be too hyperglycemic can vary from person to person, mainly due to the person's renal threshold of glucose and overall glucose tolerance. On average, however, chronic levels above 10–12 mmol/L (180–216 mg/dL) can produce noticeable organ damage over time.

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α-Amylase Enzyme that hydrolyses α bonds of large α-linked polysaccharides

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References

  1. 1 2 3 Scott LJ, Spencer CM (March 2000). "Miglitol: a review of its therapeutic potential in type 2 diabetes mellitus". Drugs. 59 (3): 521–49. doi:10.2165/00003495-200059030-00012. PMID   10776834.
  2. "Migliotl: MedlinePlus Drug Information". MedlinePlus. National Institutes of Health. 1 September 2010. Retrieved 13 April 2013.
  3. Sugimoto S, Nakajima H, Kosaka K, Hosoi H (2015). "Review: Miglitol has potential as a therapeutic drug against obesity". Nutrition & Metabolism. 12: 51. doi: 10.1186/s12986-015-0048-8 . PMC   4666030 . PMID   26628904.
  4. "Glyset (miglitol) tablets label - Accessdata FDA" (PDF). Drugs@FDA. U.S. Food and Drug Administration. August 2012. Retrieved 13 April 2013.
  5. Moreira FD, Reis CE, Gallassi AD, Moreira DC, Welker AF (2024-10-09). Dardari D (ed.). "Suppression of the postprandial hyperglycemia in patients with type 2 diabetes by a raw medicinal herb powder is weakened when consumed in ordinary hard gelatin capsules: A randomized crossover clinical trial". PLOS ONE. 19 (10): e0311501. Bibcode:2024PLoSO..1911501M. doi: 10.1371/journal.pone.0311501 . PMC   11463819 . PMID   39383145. Creative Commons by small.svg  This article incorporates textfrom this source, which is available under the CC BY 4.0 license.