Description

Simple

A medication used along with diet changes and exercise to lower blood sugar in diabetes.

Clinical

An alpha-glucosidase inhibitor used in conjunction with diet and exercise for management of type II diabetes mellitus.

Overview

An inhibitor of alpha glucosidase that retards the digestion and absorption of carbohydrates in the small intestine and hence reduces the increase in blood-glucose concentrations after a carbohydrate load. It is given orally to non-insulin dependent diabetes mellitus patients where diet modification or oral hypoglycemic agents do not control their condition. (From Martindale The Extra Pharmacopoeia, 31st ed)

Pharmacology

Indication

For treatment and management of diabetes type II (used in combination therapy as a second or third line agent)

Pharmacodynamic

Used to reduce blood gluose in patients with type 2 diabetes. Acarbose is a complex oligosaccharide that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. Acarbose binds to and inhibits alpha amylase and alpha-gluocsid... Read more

Mechanism of action

Acarbose reversibly bind to pancreatic alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolases. These enzymes inhibit hydrolysis of complex starches to oligosaccharides in the lumen of the small intestine and hydrolysis of oligosaccharides, trisaccharides, and disaccharides to glucose... Read more

Absorption

Extremely low bioavailability. Less than 2% of an oral dose of acarbose was absorbed as active drug. Peak plasma concentrations of the active drug were achieved 1 hour after dosing. Drug accumulation does not occur with multiple doses.

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Healthy volunteers = 2 hours

Route of elimination

The fraction of acarbose that is absorbed as intact drug is almost completely excreted by the kidneys. A fraction of the metabolites (approximately 34% of the dose) was absorbed and subsequently excreted in the urine. The active metabolite is excreted into the urine and accounts for less than 2% of... Read more

Toxicity

Gastrointestinal symptoms are the most common reactions to acarbose.

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Flatulence US
  • Kind: experimental
    • Percent: 74%
  • Kind: placebo
    • Percent: 29%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 31%
  • Kind: placebo
    • Percent: 12%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 19%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Thrombocytopenia US
    Post Marketing
    Hepatitis and associated liver damage US
    Post Marketing
    Jaundice US
    Post Marketing
    Subileus US
    Post Marketing
    Ileus US
    Post Marketing
    Edema US
    Post Marketing
    Hypersensitive skin reactions US
    Post Marketing
    Fulminant hepatitis US
    Post Marketing
    Low plasma vitamin B6 levels US
    Clinical Trial
    Low serum calcium levels US
    Clinical Trial
    Elevated serum transaminase levels US
    Clinical Trial
    Pneumatosis Cystoides Intestinalis US
    Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Predisposition to intestinal obstruction
        • Drugbank Id: DBCOND0107555
    • Regions: US
    • Patient Conditions:
        • Name: Chronic intestinal diseases
        • Drugbank Id: DBCOND0107556
        • Modification Of:
          • Base:
            • Name: Intestinal Diseases
            • Drugbank Id: DBCOND0035935
          • Severity:
            • Includes:
              • chronic
    • Regions: US
    • Patient Conditions:
        • Name: Diabetic Ketoacidosis
        • Drugbank Id: DBCOND0000979
    • Regions: US
    • Patient Conditions:
        • Name: Partial intestinal obstruction
        • Drugbank Id: DBCOND0107554
    • Regions: US
    • Patient Conditions:
        • Name: Colonic ulceration
        • Drugbank Id: DBCOND0107553
    • Regions: US
    • Patient Conditions:
        • Name: Inflammatory Bowel Disease
        • Drugbank Id: DBCOND0028153
    • Regions: US
    • Patient Conditions:
        • Name: Cirrhosis
        • Drugbank Id: DBCOND0028910

    Food Interactions

    Take with food. Take at the beginning of a meal.