GLIMEPIRIDE

GLIMEPIRIDE
(gli-me'pi-ride)
Amaryl
Classifications: hormone; antidiabetic; sulfonylurea;
Therapeutic: antidiabetic
; sulfonylurea
Prototype: Glyburide
Pregnancy Category: C

Availability

1 mg, 2 mg, 4 mg tablets

Action

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.

Therapeutic Effect

Lowers blood sugar by increasing secretion of insulin from pancreatic beta cells. Glimepiride improves postprandial glycemic control.

Uses

Adjunct to diet and exercise in patients with type 2 diabetes, may also be used in combination with insulin in type 2 diabetes.

Contraindications

Hypersensitivity to glimepiride, diabetic ketoacidosis, pregnancy (category C), lactation, nondiabetic patients with renal glycosuria.

Cautious Use

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 1–2 mg once daily with breakfast or first main meal, may increase to usual maintenance dose of 1–4 mg once daily (max: 8 mg/d)

Administration

Oral
  • 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, agranulocytosis (rare), thrombocytopenia. Metabolic: Hypoglycemia. Skin: Rash, pruritus, erythema, urticaria, maculopapular eruptions.

Interactions

Drug: Hypoglycemic effects may be potentiated by other highly protein-bound drugs (e.g., adrenergic antagonists, chloramphenicol, mao inhibitors, nsaids, probenecid, salicylates, sulfonamides, warfarin). corticosteroids, phenytoin, isoniazid, nicotinic acid, sympathomimetic amines, thiazide diuretics may attenuate effects of glimepiride. Herbal: Ginseng, garlic may increase hypoglycemic effects.

Pharmacokinetics

Absorption: Completely absorbed from GI tract. Onset: 1 h. Peak: 2–3 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: 5–9 h.

Nursing Implications

Assessment & Drug Effects

  • Lab tests: monitor fasting and postprandial blood glucose and urinary glucose frequently. Monitor glycosylated hemoglobin every 3–6 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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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