Glyburide

Pronunciation

Pronunciation: glie-BYOO-ride
Class: Sulfonylurea

Trade Names

DiaBeta
- Tablets 1.25 mg
- Tablets 2.5 mg
- Tablets 5 mg

Glynase PresTab
- Tablets, micronized 1.5 mg
- Tablets, micronized 3 mg
- Tablets, micronized 6 mg

Apo-Glyburide (Canada)
Gen-Glybe (Canada)
Novo-Glyburide (Canada)
Nu-Glyburide (Canada)
PMS-Glyburide (Canada)
ratio-Glyburide (Canada)
Sandoz Glyburide (Canada)

Pharmacology

Decreases blood glucose by stimulating insulin release from pancreas. May also decrease hepatic glucose production or increased response to insulin.

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Pharmacokinetics

Absorption

Significantly absorbed. T max is about 4 h; about 2 to 3 h (micronized). Mean C max is 104 ng/mL; 106 ng/mL (micronized). Mean AUC is 746 ng•h/mL; 568 ng•h/mL (micronized).

Distribution

Protein binding is extensive.

Metabolism

The major metabolite is the 4-trans-hydroxy derivative (no significant activity). The minor metabolite is the 3-cis-hydroxy derivative (no significant activity).

Elimination

T 1/ 2 is about 10 h, about 4 h (micronized). Excreted as metabolites in the urine and feces equally.

Duration

24 h.

Indications and Usage

Adjunct to diet to lower blood glucose in patients with non-insulin-dependent diabetes mellitus (type 2) whose hyperglycemia cannot be controlled by diet alone; in combination with metformin when diet and glyburide or diet and metformin alone do not result in adequate glycemic control.

Contraindications

Hypersensitivity to sulfonylureas; diabetes complicated by ketoacidosis with or without coma; sole therapy of insulin-dependent diabetes mellitus (type 1); diabetes when complicated by pregnancy.

Dosage and Administration

Nonmicronized Form
Adults

PO 2.5 to 5 mg/day with breakfast or first main meal.

Patients More Sensitive to Hypoglycemic Drugs (eg, elderly or patients with renal or hepatic function impairment)
Adults

PO 1.25 mg/day initially. Maintenance: 1.25 to 20 mg daily in single or divided doses (patients receiving more than 10 mg/day may have better response to twice-daily dosing). Daily doses more than 20 mg are not recommended.

Micronized Form ( Glynase Pres Tab )
Adults

PO 1.5 to 3 mg/day with breakfast or first main meal. Maintenance: 0.75 to 12 mg/day. Patients receiving more than 6 mg/day have more satisfactory response to twice-daily dosing. Daily doses more than 12 mg are not recommended.

Concomitant Metformin
Adults

PO Add micronized glyburide gradually to the dosing regimen of patients who have not responded to the maximum dose of metformin monotherapy after 4 wk.

Storage/Stability

Store in tightly capped container, and keep out of reach of children.

Drug Interactions

Alcohol

Produces disulfiram-like reaction (eg, facial flushing, headache, breathlessness).

Androgens, chloramphenicol, clofibrate, dicumarol, fenfluramine, fluconazole, gemfibrozil, histamine H 2 antagonists, magnesium salts, methyldopa, monoamine oxidase inhibitors, phenylbutazone, probenecid, salicylates, sulfinpyrazone, sulfonamides, tricyclic antidepressants, urinary acidifiers

May increase hypoglycemic effect.

Beta-blockers, cholestyramine, diazoxide, hydantoins, rifampin, thiazide diuretics, urinary alkalinizers

May decrease hypoglycemic effect.

Ciprofloxacin

A possible interaction between glyburide and ciprofloxacin has been reported, resulting in a potentiation of the hypoglycemic action.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Although the issue is controversial, oral sulfonylureas may have increased risk of CV mortality when compared with patients treated with diet alone.

CNS

Dizziness; vertigo.

Dermatologic

Allergic skin reactions; eczema; pruritus; erythema; urticaria; morbilliform or maculopapular eruptions; lichenoid reactions; photosensitivity.

EENT

Tinnitus.

GI

Nausea, epigastric fullness; heartburn.

Genitourinary

Mild diuresis; mild to moderate elevations in BUN and creatinine.

Hematologic

Leukopenia; thrombocytopenia; aplastic anemia; agranulocytosis; hemolytic anemia; pancytopenia; hepatic porphyria.

Hepatic

Cholestatic jaundice; elevated LFT results.

Metabolic

Hypoglycemia.

Miscellaneous

Disulfiram-like reactions; weakness; paresthesia; fatigue; malaise.

Precautions

Monitor

Blood sugar

Check blood sugars frequently and observe for symptoms of hypoglycemia or hyperglycemia and report to health care provider.


Pregnancy

Category B . Insulin is recommended to maintain blood glucose levels during pregnancy. Prolonged severe neonatal hypoglycemia can occur if sulfonylureas are administered at time of delivery.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Elderly and debilitated patients are particularly susceptible to the hypoglycemic action. Hypoglycemia may be difficult to recognize in elderly patients.

Renal Function

Use drug with caution; lower doses may be adequate.

Hepatic Function

Use drug with caution; lower doses may be adequate.

Bioavailability

Micronized glyburide ( Glynase Pres Tab ) and conventional (nonmicronized) glyburide formulations are not equivalent. Dose must be readjusted when switching between micronized and conventional (nonmicronized) formulations.

Overdosage

Symptoms

Hypoglycemia, tingling of lips and tongue, hunger, nausea, lethargy, yawning, confusion, agitation, nervousness, tachycardia, sweating, tremor, convulsions, stupor, coma.

Patient Information

  • Review with patient dietary guidelines for diabetes.
  • Instruct patient to take drug with meals.
  • Teach patient to self-monitor urine or blood glucose.
  • Inform patient that this drug is not substitute for exercise and diet control and that patient should follow prescribed regimens.
  • Instruct patient to inform all health care providers involved in the patient's care that this drug is being taken and to carry medical identification (eg, card, bracelet).
  • Instruct patient to notify health care provider if symptoms of hypoglycemia occur (eg, fatigue, excessive hunger, profuse sweating, numbness of extremities) or if blood glucose is below 60 mg/dL.
  • Tell patient to notify health care provider if symptoms of hyperglycemia occur (eg, excessive thirst or urination, urinary glucose or ketones).
  • Instruct patient to report these symptoms to health care provider: nausea, vomiting, diarrhea, heartburn, sore throat, rash, unusual bruising, or bleeding, other physical complaints.

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