Indications:
Acarbose is used with a proper diet and exercise to control high blood sugar in people with type 2 diabetes. Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems.
Mechanism of Action:
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 Properties:
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.
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.
Side Effects:
● Yellow colored eyes or skin
● Abdominal pain
● Diarrhea
● Flatulence
● Nausea or Vomiting
● Stomach pain, swelling
● Swelling of your skin
● Mucus discharge
● Rectal bleeding
Contraindications:
● ALLERGY: Acarbose tablet is not recommended in the patients with known allergy.
● Gastrointestinal Disease: Acarbose tablet is not recommended in the patients with history of gastrointestinal disease like inflammatory bowel disease, colonic ulceration or any intestinal obstruction.