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

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.

Interactions

Type in a drug name to check for interaction with Acarbose
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Acarbose is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinoline
The therapeutic efficacy of Acarbose can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Acarbose.
Abacavir
Acarbose may decrease the excretion rate of Abacavir which could result in a higher serum level.
Acebutolol
The therapeutic efficacy of Acarbose can be increased when used in combination with Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Acarbose which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Acarbose which could result in a higher serum level.
Acetaminophen
Acarbose may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
Acetazolamide
The therapeutic efficacy of Acarbose can be increased when used in combination with Acetazolamide.
Acetohexamide
The risk or severity of hypoglycemia can be increased when Acarbose is combined with Acetohexamide.
Acetyl sulfisoxazole
The therapeutic efficacy of Acarbose can be increased when used in combination with Acetyl sulfisoxazole.
Acetyldigoxin
The serum concentration of Acetyldigoxin can be decreased when it is combined with Acarbose.
Acetylsalicylic acid
The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Acarbose.
Aclidinium
Acarbose may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acrivastine
Acarbose may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Acarbose which could result in a higher serum level.
Adefovir
Adefovir may decrease the excretion rate of Acarbose which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Acarbose which could result in a higher serum level.
Agmatine
The risk or severity of hypoglycemia can be increased when Agmatine is combined with Acarbose.
AICA ribonucleotide
The risk or severity of hypoglycemia can be increased when Acarbose is combined with AICA ribonucleotide.
1 References
  1. 1 . Clissold SP, Edwards C: Acarbose. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. Drugs. 1988 Mar;35(3):214-43.PubMed: 3286212