Drug Guide
Glimepiride
Classification
Therapeutic: Antidiabetic agent, oral—Antidiabetic (sulfonylurea)
Pharmacological: Sulfonylurea, insulin secretagogue
FDA Approved Indications
- Monotherapy or combination therapy for type 2 diabetes mellitus to improve glycemic control.
Mechanism of Action
Stimulates release of insulin from pancreatic beta cells by binding to sulfonylurea receptors, leading to closure of ATP-sensitive potassium channels, which causes cell depolarization and insulin secretion.
Dosage and Administration
Adult: Initial dose is generally 1-2 mg once daily, titrated based on blood glucose response up to a maximum of 8 mg once daily.
Pediatric: Not approved for pediatric use.
Geriatric: Start at lower end of dosing range; monitor closely due to increased risk of hypoglycemia.
Renal Impairment: Use with caution; dosage adjustments may be necessary.
Hepatic Impairment: Use with caution; monitor closely due to decreased metabolism risk.
Pharmacokinetics
Absorption: Well absorbed from gastrointestinal tract.
Distribution: Widely distributed; protein-bound (~99%).
Metabolism: Primarily hepatic via CYP2C9 and CYP3A4 enzymes.
Excretion: Excreted mainly in urine as metabolites; minimal unchanged drug.
Half Life: Approximately 1.5-3 hours, but hypoglycemic effect lasts longer due to active metabolites.
Contraindications
- Type 1 diabetes mellitus
- Diabetic ketoacidosis
- Hypersensitivity to sulfonylureas or meglitinides
Precautions
- Use with caution in renal or hepatic impairment; risk of hypoglycemia; in elderly patients, risk of hypoglycemia is increased.
Adverse Reactions - Common
- Hypoglycemia (Common)
- Weight gain (Common)
- Gastrointestinal disturbances (nausea, epigastric pain) (Less common)
Adverse Reactions - Serious
- Severe hypoglycemia (Rare)
- Allergic reactions (rash, pruritus, swelling) (Rare)
Drug-Drug Interactions
- Other sulfonylureas, insulin, meglitinides (risk of hypoglycemia)
- CYP2C9 inhibitors (e.g., fluconazole, warfarin) may increase glimepiride levels.
Drug-Food Interactions
- Excessive alcohol intake can potentiate hypoglycemia.
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor blood glucose levels regularly; observe for signs of hypoglycemia; check hepatic and renal function periodically.
Diagnoses:
- Risk for hypoglycemia
- Impaired tissue perfusion related to hypoglycemia
Implementation: Administer with breakfast or first meal of the day; educate patient on recognition and management of hypoglycemia.
Evaluation: Assess blood glucose levels and clinical response to therapy; adjust dose accordingly.
Patient/Family Teaching
- Take medication with food to reduce gastrointestinal upset.
- Report symptoms of hypoglycemia (sweating, trembling, confusion).
- Maintain consistent diet and monitor blood glucose as instructed.
- Carry quick-acting carbohydrate source in case of hypoglycemia.
Special Considerations
Black Box Warnings:
- Potential for hypoglycemia; not for use in type 1 diabetes or diabetic ketoacidosis.
Genetic Factors: CYP2C9 genetic polymorphisms can affect drug metabolism and response.
Lab Test Interference: None significant.
Overdose Management
Signs/Symptoms: Severe hypoglycemia—confusion, seizures, unconsciousness.
Treatment: Administer glucose orally or intravenously; use of glucagon may be necessary if the patient is unconscious.
Storage and Handling
Storage: Store at room temperature, 20-25°C (68-77°F), away from moisture and light.
Stability: Stable for the duration of the labeled expiration date when stored properly.