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Acarbose



Acarbose
Systematic (IUPAC) name
(2R,3R,4S,5R,6R)-5-[(2R,3R,4S,5R,6R)-5-
[(2R,3R,4S,5R,6R)-3,4-dihydroxy-6-methyl-
5-[[(1S,4S,5S,6S)-4,5,6-trihydroxy-3-(hydroxy
methyl)-1-cyclohex-2-enyl]amino]oxan-2-yl]
oxy-3,4-dihydroxy-6-(hydroxymethyl)oxan-
2-yl]oxy-6-(hydroxymethyl)oxane-2,3,4-triol
Identifiers
CAS number 56180-94-0
ATC code A10BF01
PubChem 441184
DrugBank APRD00656
Chemical data
Formula C25H45N3O16 
Mol. mass 643.635 g/mol
Pharmacokinetic data
Bioavailability Extremely low
Metabolism Gastrointestinal tract
Half life 2 hours
Excretion Renal (less than 2%)
Therapeutic considerations
Licence data

US

Pregnancy cat.

B3(AU) B(US)

Legal status

POM(UK) -only(US)

Routes Oral

Acarbose is an anti-diabetic drug used to treat type 2 diabetes mellitus and, in some countries, prediabetes. It is sold in Europe under the brand name Glucobay® (Bayer AG), in North America as Precose® (Bayer AG), and in Canada as Prandase® (Bayer AG). It is an inhibitor of alpha glucosidase, an enteric enzyme that releases glucose from larger carbohydrates.

Additional recommended knowledge

Contents

Mechanism of action

Acarbose inhibits enzymes (glycoside hydrolases) needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines and pancreatic alpha-amylase. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, whereas the membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. Inhibition of these enzyme systems reduces the rate of digestion of complex carbohydrates. Less glucose is absorbed because the carbohydrates are not broken down into glucose molecules. In diabetic patients, the short-term effect of these drugs therapies is to decrease current blood glucose levels: the long term effect is a small reduction in HbA1c level.[1]

Dosing

Since acarbose prevents the digestion of complex carbohydrates, the drug should be taken at the start of main meals. (Taken with first bite of meal.) Moreover, the amount of complex carbohydrates in the meal will determine the effectiveness of acarbose in decreasing postprandial hyperglycemia. Adults are to take doses of 25mg 3 times daily.

Side effects

Since acarbose prevents the degradation of complex carbohydrates into glucose, the carbohydrates will remain in the intestine. In the colon, bacteria will digest the complex carbohydrates, thereby causing gastrointestinal side effects such as flatulence (78% of patients) and diarrhea (14% of patients).

Since these effects are dose-related, it is generally advised to start with a low dose and gradually increase the dose to the desired amount.

If a patient using acarbose suffers from a bout of hypoglycemia, the patient should eat something containing monosaccharides, such as glucose tablets. Since acarbose will prevent the digestion of complex carbohydrates, starchy foods will not effectively reverse a hypoglycemic episode in a patient taking acarbose.

References

  1. ^ Drug Therapy in Nursing, 2nd Edition.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Acarbose". A list of authors is available in Wikipedia.
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