(ay-kar-bose) Precose®
ANTIDIABETIC
May be useful for mild reductions in blood glucose concentrations (250–350 mg/dL range) in dogs and cats with non-insulin-dependent diabetes mellitus and as adjunctive treatment of insulin dependent diabetes mellitus. Acarbose is unlikely to give adequate glucose control when used alone and most recommend dietary therapy and other antihyperglycemic agents (e.g., insulin) instead.
Acarbose competitively inhibits pancreatic alpha-amylase and alphaglucosidases found in the small intestine. This delays the digestion of complex carbohydrates and disaccharides to glucose and other monosaccharides. Glucose is absorbed lower in the GI tract in lesser amounts than is normal thereby reducing insulin requirements during the postprandial hyperglycemic phase. Acarbose has no effect on lactase.
In dogs about 4% of an oral dose is absorbed; in humans only about 2% of an oral dose is absorbed from the gut that is then excreted by the kidneys. Practically all remaining drug in the gut is metabolized in the GI tract by intestinal bacteria. Patients with severe renal dysfunction attain serum levels approximately 5 times those of normal subjects.
Acarbose is contraindicated in patients with known hypersensitivity to the drug, diabetic ketoacidosis, inflammatory bowel disease, colonic ulceration, partial intestinal obstruction or predisposition to obstruction, chronic intestinal disease with marked disorders of digestion or absorption, and when excessive gas formation would be detrimental. Acarbose is not indicated in patients of low body weight (some say normal body weight as well) as it may have deleterious effects on nutrition status. Use caution in patients with renal dysfunction or severe liver disease.
Adverse effects reported in cats include flatulence, soft stools and diarrhea; in dogs, diarrhea and weight loss. Adverse effects are more likely at higher doses.
While acarbose alone does not cause hypoglycemia, it may contribute to it by reducing the rate and amount of glucose absorbed when the patient is receiving other hypoglycemic agents (insulin, oral hypoglycemics).
Safety in pregnancy has not been established; weigh any potential risks versus benefits in pregnant animals. In humans, the FDA categorizes this drug as category B for use during pregnancy (Animal studies have not yet demonstrated risk to the fetus, but there are no adequate studies in pregnant women; or animal studies have shown an adverse effect, but adequate studies in pregnant women have not demonstrated a risk to the fetus in the first trimester of pregnancy, and there is no evidence of risk in later trimesters.)
Acute overdosages are likely to cause only diarrhea and flatulence. No treatment should be necessary. Should acute hypoglycemia occur secondary to other antihypoglycemics, parenteral glucose should be administered. If treating orally, use glucose (do not use sucrose).
The following drug interactions have either been reported or are theoretical in humans or animals receiving acarbose and may be of significance in veterinary patients:
Increased serum aminotransferase levels have been noted in some humans taking high dosages for a long period
a) For dogs poorly controlled with insulin and dietary therapy when another reason for the poor control cannot be identified: Initially 12.5–25 mg total dose per dog PO with each meal. Give only at the time of feeding. May increase dose after two weeks to 50 mg per dog and then to 100 mg per dog (in large dogs, >25 kg) if response has been inadequate. There is a greater chance of diarrhea at the higher dosages. (Nelson 2005)
b) 12.5–20 mg (total dose) per meal PO (Daminet 2003)
a) 12.5–25 mg (total dose) PO with meals. When acarbose is used with a low carbohydrate diet it may improve glycemic control and reduce insulin dependence. (Scherk 2005)
b) 12.5 mg per cat PO twice daily with meals. May be able to reduce insulin dosage and thereby reduce hypoglycemia occurrence. (Greco 2002)
c) 12.5–20 mg (total dose) per meal PO (Daminet 2003)
A complex oligosaccharide antihyperglycemic agent, acarbose occurs as white to off-white powder, is soluble in water and has a pKa of 5.1.
Acarbose may also be known as: Bay-g-5421, Precose®, Asucrose®, Glicobase®, Glucobay®, Glucor®, Glumida®, or Prandase®.
Do not store tablets above 25°C (77°F); protect from moisture.
Tablets may be split or crushed and mixed with food just prior to administration.
VETERINARY-LABELED PRODUCTS: None
HUMAN-LABELED PRODUCTS:
Acarbose Oral Tablets: 25 mg, 50 mg & 100 mg; Precose® (Bayer), generic; (Rx)