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Glyburide (DiaBeta®, Micronase®)

By: Dr. Nicholas Dodman

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Overview

  • Diabetes mellitus is a disorder of the pancreas characterized by insufficient production of insulin and high blood sugar. Insulin acts to move blood sugar into cells after eating, thereby lowering the blood glucose. Diabetes in dogs is typically of the type I variety, meaning there is an absolute lack of insulin. In many cats, as in people, diabetes mellitus is often of the type II variety. In type II diabetes, the cells are resistant to the effects of available insulin.
  • Glyburide is an oral drug used to help control type II diabetes mellitus. It has been shown to lower blood sugar in animals. Glyburide can be further described as a potent, second generation sulfonylurea hypoglycemic agent.
  • Glyburide is especially helpful in cats with type II diabetes. It is not effective in insulin dependant diabetics (type I diabetes) or in insulin resistant animals.
  • Glyburide binds to the plasma membrane of beta cells in the pancreatic islets causing transmembrane ionic shifts that lead to the exocytosis of insulin-containing secretory granules and, consequently, lowering of blood glucose concentrations. Glyburide also potentiates ADH causing a mild diuresis.
  • Glyburide has not been shown effective in dogs.
  • Following oral administration, glyburide is well absorbed, though it may be more effective when given 30 minutes prior to a meal.
  • It is transported in plasma highly bound to proteins (primarily albumin) and metabolized in the liver to weakly active metabolites that are excreted in the urine and feces. Glyburide has an onset of action of 2 to 4 hours, a plasma half-life of about 10 hours in humans, and duration of action of about 16 to 24 hours.
  • Glyburide is a prescription drug and can only be obtained from a veterinarian or by prescription from a veterinarian.
  • This drug is not approved for use in animals by the Food and Drug Administration but it is prescribed legally by veterinarians as an extra-label drug.

    Brand Names and Other Names

  • This drug is registered for use in humans only.
  • Human formulations: DiaBeta® (Hoechst Marion Rousell), Micronase® (Pharmacia & Upjohn), Glynase PresTab® (Pharmacia & Upjohn), and generic forms of glyburide.
  • Veterinary formulations: None

    Uses of Glyburide

  • Glyburide is used to regulate type II diabetes mellitus in cats.

    Precautions and Side Effects

  • While generally safe and effective when prescribed by a veterinarian, glyburide can cause side effects in some animals.
  • Glyburide should not be used in animals with known hypersensitivity or allergy to the drug.
  • Glyburide should be avoided in cats with low blood sugar. It will further lower the sugar.
  • Glyburide should not be used in cats with severe burns, infections, diabetic-related coma or ketosis.
  • Glyburide should not be used in animals with known cirrhosis, inflammatory bowel disease, intestinal obstruction, colonic ulceration, and chronic intestinal problems.
  • This drug should be used with caution in patients with adrenal and pituitary insufficiency, hypothyroidism, renal or hepatic impairment, or other debilitating disease.
  • Side effects may include vomiting, increases in ALT, or icterus. CNS side effects, dermatologic side effects, GI disturbance, and various hematologic changes have been reported in humans treated with glyburide.
  • During treatment with glyburide, blood glucose levels should be carefully monitored and periodic monitoring of CBC and hepatic function is warranted.

    Drug Interactions

  • Glyburide may interact with other medications. Consult with your veterinarian to determine if other drugs your pet is receiving could interact with glyburide. The effects may be enhanced or inhibited as will be discussed below.
  • The hypoglycemic effects of sulphonureas may be enhanced by various mechanisms including decreased hepatic metabolism and renal elimination, displacement from protein binding sites, decreased blood glucose, and alteration of carbohydrate metabolism. Drugs that can cause one or more of these effects include androgens, anticoagulants, azole antifungals, chloramphenicol, clofibrate, fenfluramine, gemfibrozil, H2 blockers, Mg salts, methyldopa, MAO inhibitors (e.g. L-deprenyl), probenecid, salicylates, sulfinpyrazone, sulfonamides, tricyclic antidepressants (e.g. amitriptyline, clomipramine), and urinary acidifiers.
  • The hypoglycemic effects of sulfonureas may be inhibited by drugs that increase hepatic clearance, decrease insulin release, or increase renal excretion.
  • Drugs that may cause one or other of these effects include beta blockers, calcium channel blockers, cholestyramine, corticosteroids, diazoxide, estrogens, hydantoins, isoniazid, nicotininc acid, phenothiazines, rifampin, sympathomimetics, thiazide diuretics, thyroid agents, and urinary alkalinizers.
  • In addition, charcoal may inhibit glyburide's absorption, ciprofloxacin may potentiate glyburide's hypoglycemic action, there is some interaction of glyburide with anticoagulants, and it may increase serum digitalis concentrations.

    How Glyburide is Supplied

  • Glyburide is available in 1.25 mg, 2.5 mg, 3 mg, 4.5 mg, 5 mg, and 6 mg tablets. Some tablet forms are micronized.

    Dosing Information

  • Medication should never be administered without first consulting your veterinarian.
  • Dosing of glyburide depends on the needs of the diabetic cat. Typically, cats are given 0.625 mg once daily.
  • The dose of glyburide may need to periodically be altered, based on the cat's response and the severity of diabetes.
  • The duration of administration depends on the condition being treated, response to the medication and the development of any adverse effects. Be certain to complete the prescription unless specifically directed by your veterinarian.




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