Classifications: hormone; antidiabetic; sulfonylurea; Therapeutic: antidiabetic; sulfonylurea
Pregnancy Category: C
1 mg, 2 mg, 4 mg tablets
Second-generation sulfonylurea hypoglycemic agent used for once-a-day dosing. Directly stimulates functioning pancreatic beta
cells to secrete insulin, leading to a direct drop in blood glucose. Indirect action leads to increased sensitivity of peripheral
insulin receptors, resulting in increased insulin binding in peripheral tissues.
Lowers blood sugar by increasing secretion of insulin from pancreatic beta cells. Glimepiride improves postprandial glycemic
Adjunct to diet and exercise in patients with type 2 diabetes, may also be used in combination with insulin in type 2 diabetes.
Hypersensitivity to glimepiride, diabetic ketoacidosis, pregnancy (category C), lactation, nondiabetic patients with renal
Previous hypersensitivity to other sulfonylureas, sulfonamides, or thiazide diuretics; hypoglycemia or conditions predisposing
to hypoglycemia (e.g., prolonged nausea and vomiting, alcohol ingestion, renal or hepatic function impairment, severe infections,
surgery). Safe use in children is not established.
Route & Dosage
|Type 2 Diabetes Mellitus
Adult: PO Start with 12 mg once daily with breakfast or first main meal, may increase to usual maintenance dose of 14 mg
once daily (max: 8 mg/d)
- Give with breakfast or first main meal.
- Note: Maximum starting dose is ≤2 mg. With renal or hepatic insufficiency, initial
recommended dose is 1 mg. Increase by ≤2 mg at 1- to 2-wk intervals maximum
of 8 mg/d.
- Store in tightly closed container at 15°30° C (59°86° F).
Adverse Effects (≥1%)CNS:
Dizziness, asthenia, headache, blurred vision, changes in accommodation. GI:
Nausea, vomiting, diarrhea
, abdominal pain. Hematologic: Leukopenia
. Metabolic: Hypoglycemia
Rash, pruritus, erythema
, urticaria, maculopapular eruptions.
Hypoglycemic effects may be potentiated by other highly protein-bound drugs (e.g., adrenergic antagonists
, chloramphenicol, mao inhibitors
, probenecid, salicylates, sulfonamides, warfarin
, phenytoin, isoniazid, nicotinic acid, sympathomimetic amines
, thiazide diuretics
may attenuate effects of glimepiride. Herbal: Ginseng, garlic
may increase hypoglycemic effects.
Completely absorbed from GI tract. Onset:
1 h. Peak:
23 h. Distribution:
>99.5% protein bound; probably secreted into breast milk. Metabolism:
In liver by cytochrome P4502C9 (CYP2C9). Elimination:
60% in urine, 40% in feces. Half-Life:
Assessment & Drug Effects
- Lab tests: monitor fasting and postprandial blood glucose and urinary glucose frequently. Monitor glycosylated hemoglobin
every 36 mo. Monitor periodically during long-term therapy: Liver function tests, serum osmolarity, serum sodium, and
CBC with differential.
- Monitor for hypoglycemia especially with concurrent drugs which enhance hypoglycemic effects.
Patient & Family Education
- Take a missed dose as soon as possible unless it is almost time for next dose; NEVER take two doses at the same time.
- Avoid drinking alcohol or using OTC drugs without informing physician.
- Use sunscreen and avoid sunlamps.
- Learn about adverse reactions and drug interactions.