glyburide

Contraindicated in:

Hypersensitivity;
Hypersensitivity to sulfonamides (cross-sensitivity may occur);
Type 1 diabetes;
Diabetic coma or ketoacidosis;
Lactation: Lactation.

Use Cautiously in:

Severe cardiovascular or hepatic disease;
Glucose 6-phosphate dehydrogenase deficiency (↑ risk of hemolytic anemia);
Severe renal impairment (↑ risk of hypoglycemia);
Infection, stress, or changes in diet may alter requirements for control of blood sugar;
Impaired thyroid, pituitary, or adrenal function;
Malnutrition, high fever, prolonged nausea, or vomiting;
OB: Safety not established during pregnancy; insulin recommended during pregnancy;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. ↑ risk of prolonged hypoglycemia in older adults. Avoid use as first- or second-line monotherapy or as add-on treatment in older adults unless there are significant barriers to the use of safer and more effective agents. If a sulfonylurea must be used, glipizide is preferred.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: photosensitivity, ERYTHEMA MULTIFORME, exfoliative dermatitis, rash

Endo: hypoglycemia

F and E: hyponatremia

GI: constipation, cramps, diarrhea, dyspepsia, hepatitis, nausea, vomiting

Hemat: agranulocytosis, APLASTIC ANEMIA, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia

Metab: ↑appetite, ↑weight

Neuro: dizziness, drowsiness, headache, weakness

Interactions ⬆ ⬇

Drug-drug:

↑risk of elevated liver enzymes when used with bosentan; avoid concurrent use.
Ingestion of alcohol may result in disulfiram-like reaction.
Effectiveness may be ↓ by concurrent use of diuretics,corticosteroids, phenothiazines,oral contraceptives, estrogens, thyroid preparations, phenytoin, nicotinic acid, sympathomimetics, rifampin, and isoniazid.
Alcohol, androgens (testosterone), chloramphenicol, ACE inhibitors, disopyramide, fluoxetine, clarithromycin, fluoroquinolones,MAO inhibitors, NSAIDs (except diclofenac), salicylates , and warfarin may ↑ the risk of hypoglycemia.
Concurrent use with warfarin may alter the response to both agents (↑ effects of both initially, then ↓ activity); close monitoring recommended during any changes in dose.
Beta-adrenergic blockers may mask the signs and symptoms of hypoglycemia.
May ↑cyclosporine levels.
Colesevelam may ↓ effects; administer glyburide ≥4 hr before colesevelam
Topiramate may ↓ levels and ↓ effects

Availability ⬆ ⬇

(Generic available)

Nonmicronized tablets: 1.25 mg; 2.5 mg ; 5 mg
Micronized tablets (Glynase): 1.5 mg; 3 mg; 6 mg
In combination with:
metformin.

Route/Dosage ⬆ ⬇

The nonmicronized formulation cannot be used interchangeably with the micronized formulation.
PO (Adults ): Non-micronized: 2.5–5 mg once daily initially (range 1.25–20 mg/day). Micronized: 1.5–3 mg/day initially (range 0.75–12 mg/day; doses >6 mg/day should be given as divided doses). Increments should not exceed 1.5 mg/wk.
PO Geriatric Patients ): Nonmicronized: 1.25–2.5 mg/day initially; may be ↑ by 2.5 mg/day weekly. Micronized: 0.75–3 mg/day; may be ↑ by 1.5 mg/day weekly.

US Brand Names ⬆ ⬇

~~DiaBeta,~~ Glynase

Action ⬆ ⬇

Lowers blood sugar by stimulating the release of insulin from the pancreas and increasing the sensitivity to insulin at receptor sites.
May also decrease hepatic glucose production.

Therapeutic effects:

Reduction in blood glucose.

Classifications ⬆ ⬇

Therapeutic Classification: antidiabetics

Pharmacologic Classification: sulfonylureas

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration; micronized forms have better absorption.

Distribution: Reaches high concentrations in bile and crosses the placenta.

Metabolism/Excretion: Mostly metabolized by the liver, primarily by the CYP2C9 isoenzyme.

Half-Life: 10 hr.

Time/Action Profile ⬆ ⬇

(hypoglycemic activity)

ROUTE	ONSET	PEAK	DURATION
PO	45–60 min	1.5–3 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication at same time each day. Take missed doses as soon as remembered unless almost time for next dose. Do not take if unable to eat.
Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.
Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to drink a glass of orange juice or ingest 2–3 tsp of sugar, honey, or corn syrup dissolved in water or an appropriate number of glucose tablets and notify health care professional.
Concurrent use of alcohol may cause a disulfiram-like reaction (abdominal cramps, nausea, flushing, headaches, and hypoglycemia).
Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
Instruct patient in proper testing of serum glucose and ketones. Monitor closely during periods of stress or illness and health care professional notified if significant changes occur.
May occasionally cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Caution patient to avoid other medications, especially aspirin and alcohol, while on this therapy without consulting health care professional.
Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Advise patient to inform health care professional of medication regimen prior to treatment or surgery.
Advise patient to notify health care professional promptly if unusual weight gain, swelling of ankles, drowsiness, shortness of breath, muscle cramps, weakness, sore throat, rash, or unusual bleeding or bruising occurs.
Rep: Insulin is the recommended method of controlling blood sugar during pregnancy. Counsel female patients to use a form of contraception other than oral contraceptives and to notify health care professional promptly if pregnancy is planned or suspected and to avoid breastfeeding. Discontinue glyburide at least 2 wk before expected delivery. Neonates of women with gestational diabetes who are treated with sulfonylureas during pregnancy may be at increased risk for respiratory distress and hypoglycemia (jitters, cyanosis, apnea, hypothermia, excessive sleepiness, poor feeding, seizures).
Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
Emphasize the importance of routine follow-up exams.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇