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Drugs: glyBURIDE

SAFETY ALERT!

glyBURIDE
((glibenclamide))
GLYE-byoor-ide

Diabeta, , Glynase

Therapeutic class: Antidiabetics


Pharmacologic class: Sulfonylureas

Available Forms
Tablets: 1.25 mg; 2.5 mg; 5 mg
Tablets (micronized): 1.5 mg; 3 mg; 6 mg

Indications & Dosages


Adjunct to diet to lower glucose level in patients with type 2 diabetes
Nonmicronized form
Adults: Initially, 2.5 to 5 mg PO once daily with breakfast or first main meal. Adjust to maintenance dose at
no more than 2.5-mg increments at weekly intervals. Usual daily maintenance dose is 1.25 to 20 mg, in
single dose or divided doses. Maximum daily dose is 20 mg PO.
Micronized form
Adults: Initially, 1.5 to 3 mg PO daily with breakfast or first main meal. Adjust to maintenance dose at no
more than 1.5-mg increments at weekly intervals. Usual daily maintenance dose is 0.75 to 12 mg. Dosages
exceeding 6 mg daily may have better response with b.i.d. dosing. Maximum dose is 12 mg PO daily.
Adjust-a-dose: For elderly patients, patients who are more sensitive to antidiabetics, and for those with
renal, hepatic, adrenal, or pituitary insufficiency, start with 1.25 mg (nonmicronized) or 0.75 mg (micronized)
daily.
To replace insulin therapy
Adults: If insulin dose is less than 40 units/day, patient may be switched directly to glyburide when insulin
is stopped. If insulin dose is less than 20 units/day, initial dose is 2.5 to 5 mg (1.5 to 3 mg micronized) PO
daily. If insulin dose is 20 to 40 units/day, initial dose is 5 mg (3 mg micronized) PO daily. If insulin dose is
40 or more units/day, initially, 5 mg (3 mg micronized) PO once daily in addition to 50% of insulin dose.
Gradually taper off insulin as the glyburide dose is increased.

Administration
PO
Give drug with breakfast or first main meal.
Twice-daily dosing may be beneficial if conventional glyburide doses are greater than 10 mg or
micronized glyburide doses are greater than 6 mg.
Patients on nothing-by-mouth status or those requiring decreased caloric intake may need doses
withheld to avoid hypoglycemia.

Action
Unknown. Probably stimulates insulin release from pancreatic beta cells, reduces glucose output by the liver,
and increases peripheral sensitivity to insulin.

Route Onset Peak Duration


PO (micronized) 1 hr 2–3 hr <24 hr
PO (non-micronized) 2–4 hr 2–4 hr <24 hr
Half-life: 4 to 10 hours.

Adverse Reactions
GI: nausea, epigastric fullness, heartburn.
Hematologic: leukopenia, hemolytic anemia, agranulocytosis, thrombocytopenia, aplastic anemia.
Hepatic: cholestatic jaundice, hepatitis.
Metabolic: hypoglycemia, hyponatremia.
Musculoskeletal: arthralgia, myalgia.
Skin: rash, pruritus, other allergic reactions.
Other: angioedema.

Interactions
Many drugs may increase or decrease glucose-lowering effect of glyburide. Consult manufacturer’s product
information for additional information.
Drug-drug
Anabolic steroids, azole antifungals, chloramphenicol, clofibrate, fluoroquinolones, guanethidine, MAO
inhibitors, NSAIDs, probenecid, phenylbutazone, ranitidine, salicylates, sulfonamides: May increase
hypoglycemic activity. Monitor glucose level.
Beta blockers: May prolong hypoglycemic effect and mask symptoms of hypoglycemia. Use together
cautiously.
Bosentan: Increases risk of elevated LFT values. Use together is contraindicated.
Carbamazepine, corticosteroids, glucagon, rifamycins, thiazide diuretics: May decrease hypoglycemic
response. Monitor glucose level.
Colesevelam: May decrease glyburide serum concentration. Give glyburide at least 4 hours before
colesevelam.
Miconazole (oral): May increase serum concentration and enhance hypoglycemic effect of glyburide.
Monitor therapy.
Oral anticoagulants: May increase hypoglycemic activity or enhance anticoagulant effect. Monitor glucose
level, PT, and INR.
Drug-herb
Herbs with hypoglycemic properties: May enhance hypoglycemic effect of glimepiride. Monitor therapy.
Drug-lifestyle
Alcohol use: May alter glycemic control, most commonly causing hypoglycemia. May cause disulfiram-like
reaction. Discourage use together.

Effects on Lab Test Results


May increase alkaline phosphatase, AST, ALT, bilirubin, BUN, and cholesterol levels.
May decrease glucose, sodium, and Hb levels.
May decrease granulocyte, platelet, and WBC counts.

Contraindications & Cautions


Contraindicated in patients hypersensitive to drug and in those with type 1 diabetes or diabetic
ketoacidosis with or without coma.
Use cautiously in patients with hepatic or renal impairment (eGFR less than 60 mL/minute); in
debilitated, malnourished, or elderly patients; and in patients allergic to sulfonamides.
Patients with G6PD deficiency may be at increased risk for sulfonylurea-induced hemolytic anemia. Use
cautiously and consider therapy modification.
Dialyzable drug: Unknown.
Overdose Signs & Symptoms: Hypoglycemia.
Pregnancy-Lactation-Reproduction
Insulin is drug of choice to control diabetes during pregnancy. If used during pregnancy, discontinue at
least 2 weeks before expected delivery date.
Prolonged severe hypoglycemia (4 to 10 days) has been reported in neonates born to mothers receiving
a sulfonylurea at the time of delivery.
Drug may cause hypoglycemia in breastfed infants. Patient should discontinue breastfeeding or
discontinue drug.

Nursing Considerations
Alert: Micronized glyburide (Glynase) contains drug in a smaller particle size and isn’t bioequivalent to
regular glyburide tablets. In patients who have been taking nonmicronized form, adjust dosage.
Although most patients may take drug once daily, those taking more than 10 mg conventional glyburide
or 6 mg micronized glyburide daily may achieve better results with twice-daily dosage.
Drug is a second-generation sulfonylurea. Adverse effects are less common with second-generation
drugs than with first-generation drugs such as chlorpropamide.
Alert: Use of oral antidiabetic drugs may carry a higher risk of CV mortality than use of diet alone or of
diet and insulin therapy.
During periods of increased stress, such as infection, fever, surgery, or trauma, patient may need insulin
therapy. Monitor patient closely for hyperglycemia in these situations.
Patient switching from insulin therapy to an oral antidiabetic should check glucose level at least three
times a day before meals. Patient may need hospitalization during transition.
Look alike-sound alike: Don’t confuse glyburide with glimepiride or glipizide.

Patient Teaching
Teach patient about diabetes and the importance of following therapeutic regimen, adhering to specific
diet, losing weight, getting exercise, following personal hygiene programs, and avoiding infection.
Explain how and when to monitor glucose level, and teach recognition of and intervention for low and
high glucose levels.
Tell patient not to change drug dosage without prescriber’s consent and to report abnormal blood or
urine glucose test results.
Teach patient to carry candy or other simple sugars for mild low glucose level. Patient experiencing
severe episode may need hospital treatment.
Advise patient not to take supplements or other drugs, including OTC drugs, without first checking with
prescriber.
Advise patient to wear or carry medical identification at all times.
Alert: Instruct patient to report episodes of low glucose to prescriber immediately; a severely low
glucose level is sometimes fatal in patients receiving as little as 2.5 to 5 mg daily.
Advise patient to avoid alcohol, which may lower glucose level.

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