Glimepiride: Dose, Frequency, Indications, Interactions & more

Dose and Dosage #

• Initial Dose: Typically starts at 1 to 2 mg once daily.
• Maintenance Dose: May be increased gradually based on blood glucose levels, generally up to a maximum of 8 mg once daily.
• Dosage adjustments should be made cautiously and under medical supervision to avoid hypoglycemia.

Frequency #

• Typically taken once daily, usually with breakfast or the first main meal of the day.

Route of Administration (ROA) #

• Oral administration, usually in the form of tablets.

Mechanism of Action (MOA) #

• Stimulates insulin release from pancreatic beta cells by binding to sulfonylurea receptors on the pancreatic beta cell plasma membrane.
• Enhances peripheral glucose utilization.

Pharmacokinetics (PK) #

• Well-absorbed after oral administration.
• Peak plasma concentrations reached within 2 to 3 hours.
• Extensively metabolized in the liver, primarily via CYP2C9.
• Excreted mainly in the urine, with a half-life of about 5 to 8 hours.

Pharmacodynamics (PD) #

• Lowers blood glucose levels by increasing insulin release from pancreatic beta cells.
• Enhances peripheral glucose utilization.

Pathophysiology #

• Glimepiride works by increasing insulin secretion from the pancreas, thereby lowering blood sugar levels.
• It primarily acts on pancreatic beta cells to enhance insulin release in response to glucose.

Indications #

• Type 2 Diabetes Mellitus: Used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Contraindications #

• Type 1 Diabetes Mellitus: Not indicated for use in patients with type 1 diabetes.
• Diabetic Ketoacidosis: Contraindicated in patients with diabetic ketoacidosis.
• Hypersensitivity: Contraindicated in individuals with a known hypersensitivity to glimepiride or other sulfonylureas.

Drug Interactions #

• Hypoglycemia Risk: Concurrent use with other antidiabetic agents or medications that potentiate hypoglycemia (e.g., insulin, sulfonylureas) may increase the risk of hypoglycemia.
• CYP2C9 Inhibitors and Inducers: Drugs that inhibit or induce CYP2C9 enzymes may affect the metabolism of glimepiride, potentially altering its efficacy or risk of hypoglycemia.

Precautions #

• Hypoglycemia: Monitor blood glucose levels regularly to reduce the risk of hypoglycemia.
• Renal Impairment: Use with caution in patients with renal impairment, as glimepiride is primarily excreted by the kidneys.
• Hepatic Impairment: Use with caution in patients with hepatic impairment, as glimepiride metabolism may be altered.

Monitoring and Laboratory Tests #

• Blood Glucose Levels: Regular monitoring of blood glucose levels is essential to assess glycemic control and adjust dosage as needed.
• Liver and Renal Function Tests: Periodic monitoring of liver and renal function may be warranted, especially in patients with pre-existing liver or renal impairment.

Storage and Disposal #

• Store at room temperature, away from moisture and heat.
• Keep out of reach of children.
• Dispose of unused or expired medication properly according to local regulations.

Emergency Situations #

• Hypoglycemia: In the event of hypoglycemia, consume glucose or a sugar-containing beverage immediately. If severe, seek medical assistance promptly.
• Overdose: Contact a healthcare professional or emergency services immediately if an overdose is suspected.
• Symptomatic Management: Treatment of overdose may include symptomatic and supportive measures, including close monitoring of vital signs and glucose levels. Administration of glucose or intravenous dextrose may be necessary in severe cases.

Medication Information and Guidelines