Introduction
Acarbose is an oral antihyperglycemic drug used in the management of diabetes mellitus. Acarbose binds to and inhibits the action of alpha glucosidase, an enzyme found in the gastrointestinal tract and involved in the hydrolysis of saccharides into glucose and other monosaccharides. This mechanism will prevent the breakdown of large carbohydrates into glucose thereby lowering postprandial glucose levels.
Hyperglycemia is a medical condition in which blood glucose levels are higher than normal. Hyperglycemia is a characteristic of several diseases, especially type 2 diabetes mellitus.
The chemical formula of acarbose is C25H43NO18. Use in pregnant women is allowed.
Indication
The main indication for acarbose is as an oral antihyperglycemic drug in patients with diabetes mellitus. To reduce the risk of side effects, the dose should be titrated. Acarbose can also be used for prediabetes conditions.
Acarbose can be used as a first-line drug in type 2 diabetes mellitus patients with poor postprandial blood sugar control compared to fasting blood sugar. This situation often occurs in patients with a high-carbohydrate diet.
Acarbose Contraindications And Warnings
Acarbose is contraindicated if there is hypersensitivity to acarbose, patients with liver cirrhosis, and patients with diabetic ketoacidosis. Acarbose warnings are given regarding the risk of hypoglycemia and elevated serum transaminase levels.[5]
Contraindications
Acarbose is contraindicated in patients with hypersensitivity to this drug or its components. Acarbose should also not be used in patients with diabetic ketoacidosis, gastrointestinal disorders such as inflammatory bowel disease, duodenal ulcers, partial intestinal obstruction, patients with malabsorption, and liver cirrhosis.
Acarbose Pharmacology
Pharmacologically acarbose is an oral antidiabetic drug that works by inhibiting the alpha glucosidase enzyme.
Pharmacodynamics
Acarbose binds to and inhibits the action of alpha glucosidase enzymes on the intestinal brush border. Alpha glycosidase is an enzyme that catalyzes the conversion of complex carbohydrates, oligosaccharides, and disaccharides into monosaccharides and glucose to then enter the intestinal lumen and bloodstream.
By inhibiting the action of the alpha glucosidase enzyme, acarbose is able to lower postprandial blood sugar levels. In a clinical trial, alpha glucosidase inhibitors were able to reduce HbA1c levels by 0.5-0.8%. Due to this effect, acarbose is effectively used in the treatment of type 2 diabetes mellitus [2-4].
Pharmacokinetics
Acarbose is minimally absorbed. Within 14-24 hours, almost all of the absorbed drug is excreted in the kidneys.
Absorption
Acarbose is minimally absorbed, ie <2% as the active drug and about 35% as metabolites.
Distribution
The half-life of acarbose is 2 hours. Acarbose has an onset of action of 1 hour, and peaks within 1 hour.
Metabolism
Acarbose is metabolized in the gastrointestinal tract by bacteria and digestive enzymes.
Elimination
Acarbose is eliminated through urine and feces. 34% of metabolites in urine are inactive metabolites, while 51% in feces are unabsorbed drugs. Due to low absorption, almost all of the absorbed drug is excreted in the urine.
Side Effects And Drug Interactions of Acarbose
The most common side effect of acarbose is gastrointestinal disturbances and a potentially fatal side effect is hypoglycemia. Acarbose interacts with a variety of drugs, including thiazide diuretics, corticosteroids, phenothiazines, thyroid medications, estrogens, phenytoin, nicotinic acid, and calcium channel blockers.
Side effects
Acarbose side effects that often occur are gastrointestinal disorders such as malabsorption, flatus, diarrhea, and flatulence. This side effect occurs due to increased fermentation of carbohydrates that are not absorbed by bacteria.
Acarbose Clinical Supervision
Clinical supervision on the use of acarbose includes monitoring of blood glucose level regulation and monitoring of drug side effects. The targets for controlling diabetes mellitus were HbA1c <7% and blood glucose 2 hours post prandial <180 mg/dl. To evaluate side effects, serum transaminase tests can be performed every 3 months in the first year of therapy. After that, inspections can be carried out regularly as needed.
Acarbose Formula
The acarbose formulation is in an oral dosage form.
Preparation Form
Acarbose is available in oral dosage forms, in the form of tablets in strengths of 50 and 100 mg. Acarbose is used as an antihyperglycemic drug in type 2 diabetes mellitus.
How to Consume
Acarbose should be taken just before a meal, or at the same time as the first bite.
Storage Method
Acarbose preparations should be stored at temperatures close to room temperature, which is < 25 C. Avoid storage in humid conditions.
Use In Pregnancy And Breastfeeding Acarbose
The use of acarbose in pregnant women is classified as category B by the FDA and category B3 by the TGA. Data regarding the safety of acarbose in nursing mothers are not yet available. The FDA includes acarbose in category B. This means that animal studies have not shown any risk to the fetus, but there have been no controlled studies in pregnant women.