(glye' byoor ide)
Albert Glyburide (CAN), DiaBeta, Euglucon (CAN), Gen-Glybe (CAN), Glibenclamide, Glynase PresTab, Micronase
Pregnancy Category B
Stimulates insulin release from functioning beta cells in the pancreas; may improve binding between insulin and insulin receptors or increase the number of insulin receptors; more potent in effect than first-generation sulfonylureas.
· Adjunct to diet to lower blood glucose with type 2 (non–insulin-dependent) diabetes mellitus
· Adjunct to metformin when adequate results are not achieved with either drug alone
· Adjunct to insulin therapy in the stabilization of certain cases of type 2 diabetes, reducing the insulin requirement, and decreasing the chance of hypoglycemic reactions
Contraindications and cautions
· Contraindicated with allergy to sulfonylureas; diabetes with ketoacidosis, sole therapy of type 1 (insulin-dependent) diabetes or diabetes complicated by pregnancy, serious hepatic or renal impairment, uremia; diabetes complicated by fever, severe infections, severe trauma, major surgery, ketosis, acidosis, coma (insulin is contraindicated).
· Use cautiously with pregnancy, lactation, thyroid or endocrine impairment, glycosuria, hyperglycemia associated with primary renal disease; labor and delivery (if glyburide is used during pregnancy, discontinue drug at least 1 mo before delivery).
Tablets—1.25, 1.5, 2.5, 3, 4.5, 5, 6 mg
· Initial therapy: 2.5–5 mg PO with breakfast (DiaBeta, Micronase); 1.5–3 mg/day PO (Glynase).
· Maintenance therapy: 1.25–20 mg/day PO given as a single dose or in divided doses. Increase in increments of no more than 2.5 mg at weekly intervals based on patient's blood glucose response (DiaBeta, Micronase); 0.75–12 mg/day PO (Glynase).
Safety and efficacy not established.
Geriatric patients tend to be more sensitive to the drug; start with initial dose of 1.25 mg/day PO (DiaBeta, Micronase) 0.75 mg/day PO (Glynase). Monitor for 24 hr, and gradually increase dose after at least 1 wk as needed.
Metabolism: Hepatic; T1/2: 4 hr
Distribution: Crosses placenta; enters breast milk
Excretion: Bile and urine
· CNS: Drowsiness, tinnitus, fatigue, asthenia, nervousness, tremor, insomnia
· CV: Increased risk of CV mortality
· Endocrine: Hypoglycemia
· GI: Anorexia, nausea, vomiting, epigastric discomfort, heartburn, diarrhea
· Hematologic: Leukopenia, thrombocytopenia, anemia
· Hypersensitivity: Allergic skin reactions, eczema, pruritus, erythema, urticaria, photosensitivity, fever, eosinophilia, jaundice
· Increased risk of hypoglycemia with sulfonamides, chloramphenicol, oxyphenbutazone, phenylbutazone, salicylates, clofibrate
· Decreased effectiveness of glyburide and diazoxide if taken concurrently
· Increased risk of hyperglycemia with rifampin, thiazides
· Risk of hypoglycemia and hyperglycemia with ethanol; "disulfiram reaction" has been reported
· Increased risk of hypoglycemia if taken with juniper berries, ginseng, garlic, fenugreek, coriander, dandelion root, celery
Name confusion has occurred between DiaBeta (glyburide) and Zebeta (bisoprolol); use caution.
· History: Allergy to sulfonylureas; diabetes with complications; type 1 diabetes, serious hepatic or renal impairment, uremia, thyroid or endocrine impairment, glycosuria, hyperglycemia associated with primary renal disease, pregnancy
· Physical: Skin color, lesions; T; orientation, reflexes, peripheral sensation; R, adventitious sounds; liver evaluation, bowel sounds; urinalysis, BUN, serum creatinine, liver function tests, blood glucose, CBC
· Give drug before breakfast. If severe GI upset occurs, dose may be divided and given before meals.
· Monitor urine or serum glucose levels frequently to determine drug effectiveness and dosage.
· Monitor dosage carefully if switching to or from Glynase.
· WARNING: Transfer to insulin therapy during periods of high stress (eg, infections, surgery, trauma).
· WARNING: Use IV glucose if severe hypoglycemia occurs as a result of overdose.
· Do not discontinue this medication without consulting your health care provider.
· Monitor urine or blood for glucose and ketones.
· Do not use this drug during pregnancy; consult health care provider.
· Avoid alcohol while using this drug.
· Report fever, sore throat, unusual bleeding or bruising, rash, dark urine, light-colored stools, hypoglycemic or hyperglycemic reactions.
Adverse effects in Italic are most common; those in Bold are life-threatening.