Acarbose Tablets

Mechanism

Acarbose inhibits enzymes (glycoside hydrolases) needed to digest carbohydrates ,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.

Pharmacokinetics

• Absorption: An oral dose of acarbose was absorbed as active drug, while approximately 35% of total radioactivity from a 14C-labeled oral dose was absorbed. An average of 51% of an oral dose was excreted in the feces as unabsorbed drug-related radioactivity within 96 hours of ingestion. The delayed absorption of acarbose-related radioactivity reflects the absorption of metabolites that may be formed by either intestinal bacteria or intestinal enzymatic hydrolysis.
• Distribution: Primarily confined to intestinal lumen.
• Metabolism: Acarbose is metabolized within the gastrointestinal tract , by intestinal bacteria, and also by digestive enzymes. A fraction of these metabolites was absorbed and excreted in the urine. The fraction of acarbose that is absorbed as intact drug is almost completely excreted by the kidneys. This is consistent with the low bioavailability of the parent drug. The mean steady-state area under the curve (AUC) and maximum concentrations of acarbose were approximately 1.5 times higher in elderly compared to young volunteers these differences were not statistically significant.
• Elimination: Excreted mainly in feces; small amount via urine.

Side Effects

• Flatulence
• Diarrhea
• Abdominal pain
• Bloating

Contraindication

• Hypersensitivity to Acarbose
• Inflammatory bowel disease
• Intestinal obstruction

Interaction

• Insulin & sulfonylureas (risk of hypoglycemia)
• Corticosteroids (increase blood glucose)
• Diuretics (reduce efficacy)

Warning and Precautions

This has been prescribed for the patient's specific condition. It may be dangerous to any other person.

• Take with first bite of meal
• Monitor blood glucose regularly
• Avoid alcohol
• Use cautiously in liver disorders

Dosage

As directed by the Physician.