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glyburide (glibenclamide (UK))
Pharmacologic class: Sulfonylurea
Therapeutic class: Hypoglycemic
Pregnancy risk category B
Increases insulin binding and sensitivity at receptor sites, stimulating insulin release from beta cells in pancreas and reducing blood glucose level. Also decreases production of basal glucose in liver, enhances sensitivity of peripheral tissue to insulin, inhibits platelet aggregation, and causes mild diuresis.
Tablets: 1.25 mg, 2.5 mg, 5 mg
Tablets (micronized): 1.5 mg, 3 mg, 6 mg
Indications and dosages
➣ To control blood glucose in type 2 (non-insulin-dependent) diabetes mellitus in patients who have some pancreatic function and don't respond to diet therapy
Adults: Initially, 2.5 to 5 mg (regular tablets) P.O. daily; range is 1.25 to 20 mg/day as a single dose or in divided doses. Or initially, 1.5 to 3 mg (micronized tablets) P.O. daily, with range of 0.75 to 12 mg/day; give dosages above 6 mg in two divided doses.
➣ Conversion from insulin therapy
Adults: If patient takes less than 20 units of insulin daily, give 2.5 to 5 mg glyburide daily; with insulin dosage of 20 to 40 units/day, give 5 mg glyburide; with insulin dosage above 40 units/day, give 5 mg glyburide daily or 3 mg (micronized tablets) P.O. daily and reduce insulin dosage by 50%.
• Hepatic or renal failure
• Elderly patients
• Hypersensitivity to drug
• Type 1 (insulin-dependent) diabetes
• Severe renal, hepatic, thyroid or other endocrine disease
• Pregnancy or breastfeeding
Use cautiously in:
• mild to moderate hepatic, renal, or cardiovascular disease; impaired thyroid, pituitary, or adrenal function
• infection, stress, or dietary changes
• elderly patients.
☞ Know that micronized glyburide is not bioequivalent to regular glyburide.
• Check baseline creatinine level for normal renal function before giving first dose.
• Give daily dose at breakfast; for patient receiving drug b.i.d., give second dose at dinner.
• Adjust dosage slowly if patient is taking metformin.
CNS: dizziness, drowsiness, headache, weakness
CV: increased CV mortality risk
EENT: visual accommodation changes, blurred vision
GI: nausea, vomiting, diarrhea, constipation, cramps, heartburn, epigastric distress, anorexia
Hematologic: aplastic anemia, leukopenia, thrombocytopenia, agranulocytosis, pancytopenia
Hepatic: cholestatic jaundice, hepatitis
Metabolic: hyponatremia, hypoglycemia
Skin: rash, pruritus, urticaria, eczema, erythema, photosensitivity, angioedema
Other: increased appetite
Drug-drug. Androgens (such as testosterone), chloramphenicol, clofibrate, guanethidine, MAO inhibitors, nonsteroidal anti-inflammatory drugs (except diclofenac), salicylates, sulfonamides, tricyclic antidepressants: increased risk of hypoglycemia
Beta-adrenergic blockers: altered response to glyburide, requiring increased or decreased dosage; prolonged hypoglycemia (with nonselective agents)
Calcium channel blockers, corticosteroids, estrogens, hydantoins, hormonal contraceptives, isoniazid, nicotinic acid, phenothiazines, phenytoin, rifampin, sympathomimetics, thiazide diuretics, thyroid preparations: decreased hypoglycemic effect of glyburide
Warfarin: initially increased, then decreased, effects of both drugs
Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, blood urea nitrogen, cholesterol: increased values
Glucose, granulocytes, hemoglobin, platelets, white blood cells: decreased values
Drug-herbs. Agoral marshmallow, aloe (oral), bitter melon, burdock, chromium, coenzyme Q10, dandelion, eucalyptus, fenugreek: increased hypoglycemic effect
Glucosamine: impaired glycemic control
Drug-behaviors. Alcohol use: disulfiram-like reaction
• Monitor blood glucose level, especially during periods of increased stress.
• Monitor CBC and renal function test results.
• If patient is ill or has abnormal laboratory findings, monitor electrolyte, ketone, glucose, pH, lactate dehydrogenase, and pyruvate levels.
• Evaluate cardiovascular status.
• Advise patient to take daily dose with breakfast (and second dose, if prescribed, with dinner).
• Teach patient how to self-monitor his glucose level as prescribed; tell him to report significant changes.
• Inform patient that he may need supplemental insulin during times of stress or when he can't maintain adequate oral intake.
• Teach patient how to recognize signs and symptoms of hypoglycemia and hyperglycemia.
• Instruct patient to keep sugar source available at all times.
• Encourage patient to drink plenty of fluids.
• Stress importance of diet and exercise in helping to control diabetes.
• Advise patient to wear or carry medical identification stating he has diabetes.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Tell patient he'll undergo regular blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.
AcetohexamideA first-generation oral sulfonylurea used to reduce glucose in type 2 diabetics whose diabetes can’t be controlled by diet.
Mechanism of action Triggers release of insulin from the pancreas.
Pharmacokinetics Metabolised in liver to an active analogue; excreted via kidneys.
Adverse effects Hypoglycaemic reactions—e.g., coma, nausea, vomiting, dizziness, cholestatic jaundice, agranulocytosis, aplastic and haemolytic anaemia, hypersensitivity, skin reactions including photosensitivity, rash and itching.
Precautions Hypertension, liver and kidney disease, allergies