Acarbose (acarbose)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Acarbose is an alpha-glucosidase inhibitor antidiabetic agent.
Acarbose is an alpha-glucosidase inhibitor antidiabetic agent. The drug is a complex oligosaccharide produced by fermentation of Actinoplanes utahensis. Acarbose is a reversible, competitive inhibitor of alpha-glucosidase enzymes (e.g., glucoamylase, sucrase, maltase, isomaltase) that hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the intestinal brush-border.
Acarbose also has a small inhibitory effect on pancreatic alpha-amylase, which hydrolyzes starch into maltose, maltotriose, and dextrins in the lumen of the small intestine. In patients with diabetes, inhibition of these enzymes results in delayed carbohydrate breakdown and glucose absorption and in a resultant reduction in postprandial hyperglycemia. Acarbose has no inhibitory effect on lactase and would not be expected to produce lactose intolerance.
The systemic bioavailability of acarbose is low, with less than 2% absorbed as the active parent drug. Peak plasma concentrations of the active drug are attained at approximately 1 hour. Acarbose is metabolized in the GI tract, principally by intestinal bacteria but also by digestive enzymes to multiple metabolites, one of which is active.
Acarbose is excreted principally in the feces (51%) as unabsorbed drug and in the urine as metabolites (34% of the dose). The plasma half-life of acarbose is approximately 2 hours; accumulation does not occur with the recommended multiple daily dosing frequency (i.e., three times daily). Mean steady-state AUC and peak plasma concentrations of acarbose were approximately 1.5-times higher in geriatric patients compared to younger adults; however, these differences were not statistically significant.
The plasma concentration of acarbose increases proportionally relative to the degree of renal dysfunction. In patients with severe renal impairment (creatinine clearance <25 mL/minute per 1.73 m2), peak plasma concentrations and AUC of acarbose were 5- and 6-times higher, respectively, than those with normal renal function.
USES: Acarbose is used with a proper diet and exercise program 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. Proper control of diabetes may also lessen your risk of a heart attack or stroke.
Acarbose works in your intestines to slow the breakdown and absorption of carbohydrates from foods that you eat. This effect helps lessen your blood sugar rise after a meal.
Generic name: acarbose
Pronunciation: (AY-kar-bose)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Acarbose
Indications
The following indications are listed for Acarbose:
- Type 2 Diabetes Mellitus
Also known as: Adult Onset Diabetes, Adult Onset Diabetes Mellitus, Adult Onset Dm, Diabetes Mellitus Type 2, Diabetes Mellitus Type Ii, Ketosis-Resistant Diabetes Mellitus, Ketosis-Resistant Dm, Maturity Onset Diabetes, Maturity Onset Diabetes Mellitus, Non-Insulin Dependent Diabetes Mellitus, Non-Insulin-Dependent Diabetes Mellitus, Type Ii Diabetes Mellitus.
Dosing
No dosing information is available for this tab.
Acarbose is administered orally 3 times daily. The drug should be administered at the beginning (with the first bite) of each main meal. If the prescribed diet designed to minimize adverse GI effects is not observed, adverse GI effects may be intensified. Common adverse GI effects (e.g., flatulence, diarrhea, abdominal discomfort) usually develop during the first few weeks of therapy and generally diminish in frequency and intensity with time, although flatulence usually is only abated rather than returned to pretreatment levels. If adverse GI effects are strongly distressing despite adherence to the prescribed diabetic diet, a clinician should be consulted and the dosage of acarbose temporarily or permanently reduced.
Store acarbose tablets at 20--25degreesC in a tightly closed container protected from moisture.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Hypersensitivity to acarbose.
*Diabetic ketoacidosis.
*Cirrhosis.
*Inflammatory bowel disease, colonic ulceration, existing partial intestinal obstruction or predisposition to this condition.
*Chronic intestinal diseases associated with marked disorders of digestion or absorption.
*Co-existing conditions that may deteriorate as a result of increased intestinal gas formation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects of acarbose are GI symptoms, including flatulence, diarrhea, and abdominal pain.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of acarbose have not been established in pediatric patients younger than 18 years of age.
There are no adequate and well-controlled studies of acarbose in pregnancy. In animal reproduction studies conducted in rats, acarbose doses up to 480 mg/kg (corresponding to 9 times the exposure in humans based on plasma levels) revealed no evidence of impaired fertility or harm to the fetus. In rabbits, acarbose doses up to 160 mg/kg (corresponding to 10 times the human dose based on body surface area) showed no evidence of embryotoxicity and there was no evidence of teratogenicity at a dose 32 times the human dose (based on body surface area). However, in rabbits, reduced maternal body weight gain, likely the result of the pharmacodynamic activity of high doses of acarbose in the intestines, may have been responsible for a slight increase in embryonic losses.
Abnormal glucose levels during pregnancy are associated with a higher incidence of congenital anomalies as well as increased neonatal morbidity and mortality; acarbose should be used during pregnancy only if clearly needed as safety in pregnant women has not been established.
There is no information regarding the presence of acarbose in human milk. Acarbose is distributed into milk in rats. Acarbose is not recommended for use while breast-feeding.
The manufacturer makes no specific dosage recommendations for geriatric patients.
No overall differences in safety or efficacy of acarbose have been observed between patients >=65 years of age and younger patients. In clinical studies of acarbose, 27% of patients were >=65 years of age and 4% of patients were >=75 years of age. The mean steady-state AUC and maximum concentration of acarbose are approximately 1.5-times higher in geriatric patients compared to younger patients; these differences are not considered significant.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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