- Tablets 1 mg
- Tablets 2 mg
- Tablets 4 mg
Decreases blood glucose by stimulating insulin release from pancreas. May also decrease hepatic glucose production as well as increase sensitivity to insulin.
Bioavailability is 100%. C max is about 103 to 591 ng/mL (dose dependent). T max is about 2 to 3 h.Food
T max increased, and C max and AUC are slightly decreased.
Vd is 8.8 L. Protein binding is more than 99.5%.
Completely metabolized by oxidation via CYP-450 2C9. Major metabolites are cyclohexylhydroxymethyl (M1) (about one-third of the activity of the parent) and carboxyl (M2) derivatives.
About 60% is excreted in urine and about 40% in feces as metabolites. The half-life is about 5 to 9.2 h.
2 to 3 h.
Special PopulationsRenal Function Impairment
Serum levels decrease, M1 and M2 levels increase, and half-lives for M1 and M2 increase.Elderly
Mean AUC was about 13% lower. Mean weight-adjusted Cl was about 11% higher.Children
Mean AUC, C max , and half-life are comparable with adults.Gender
No differences in pharmacokinetics when adjustment was made for differences in body weight.Race
Does not appear to affect the pharmacokinetics.
Indications and Usage
Adjunct to diet and exercise in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone.
Hypersensitivity to sulfonylureas; diabetic ketoacidosis with or without coma.
Dosage and AdministrationAdults
PO 1 to 2 mg daily (max, 2 mg/day initial dose) with breakfast or the first main meal of the day. Increase by 1 to 2 mg/dose. Titrate at 1- to 2-wk intervals based on blood glucose response.Maintenance
1 and 4 mg daily (max, 8 mg/day). Combination therapy with insulin is appropriate for secondary failure to oral sulfonylureas. The same dosing recommendations apply.In Combination With Metformin
PO Obtain desired control of blood glucose by adjusting the dose of each drug; however, make attempts to determine the minimum effective dose of each drug.In Combination With Insulin
PO The fasting glucose level for instituting combination therapy is greater than 150 mg/dL. The recommended glimepiride dosage is 8 mg once daily with the first main meal. Start with low-dose insulin and adjust the insulin dose weekly, as guided by fasting blood glucose. Once stabilized, monitor capillary blood glucose daily. Periodic adjustments in insulin may be necessary, as determined by glucose and glycosylated hemoglobin levels.Renal Impairment, Hepatic Impairment, Debilitated or Malnourished Patients, or Patients With Adrenal or Pituitary Insufficiency
PO Start at 1 mg once daily and titrate carefully to avoid hypoglycemic reactions.
Store between 59° and 86°F.
Drug InteractionsACE inhibitors, beta-blockers, chloramphenicol, clofibrate, diazoxide, fenfluramine, histamine H 2 antagonists, MAOIs, miconazole, NSAIDs, probenecid, quinolones (eg, ciprofloxacin), salicylates, sulfinpyrazone, sulfonamides, tricyclic antidepressants, urinary acidifiers
May increase hypoglycemic effect.Alcohol
Produces disulfiram-like reaction (eg, breathlessness, facial flushing, headache).Corticosteroids, estrogens, isoniazid, nicotinic acid, oral contraceptives, phenothiazines, phenytoin, sympathomimetics, thiazide and other diuretics, thyroid products
These agents may produce hyperglycemia, leading to loss of glycemic control.Fluconazole, fluvastatin, fluvoxamine, gemfibrozil, ketoconazole
May elevate glimepiride blood levels, increasing the risk of hypoglycemia.Rifamycins
Glimepiride blood levels may be decreased, increasing the risk of hyperglycemia.
Laboratory Test Interactions
None well documented.
Asthenia, dizziness, headache (2%).
Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia.
Hepatic porphyria reactions and disulfiram-like reactions, hyponatremia.
Monitor fasting blood glucose to determine therapeutic response, monitor glycosylated hemoglobin every 3 to 6 mo.
Category C . Insulin is recommended to maintain blood glucose levels during pregnancy. Prolonged severe neonatal hypoglycemia can occur if sulfonylureas are administered at the time of delivery.
Data are insufficient to recommend the use of glimepiride in children.
Increased risk for development of hypoglycemia. Hypoglycemia may be difficult to detect in elderly patients.
Use with caution; lower doses may be adequate.
Use with caution; lower doses may be adequate.
Oral hypoglycemic agents have been associated with an increase in CV mortality compared with diet alone or diet plus insulin.
Use with caution. May cause hemolytic anemia. Consider a nonsulfonylurea alternative.
Treatment of patients with G6PD deficiency with sulfonylurias can lead to hemolytic anemia.
All sulfonylurea drugs may cause severe hypoglycemia. Debilitated or malnourished patients; elderly patients; and patients with adrenal, pituitary, or hepatic insufficiency are particularly susceptible to these effects. Combined use of glimepiride with insulin or metformin may increase the potential for hypoglycemia.
Loss of control of blood glucose
Consider combined therapy with metformin or with insulin if diminished responsiveness from secondary failure occurs.
No clinical studies establishing conclusive evidence of macrovascular risk reduction.
Coma, confusion, convulsions, hunger, hypoglycemia, lethargy, nausea, stupor, sweating, tachycardia, tingling of lips and tongue, tremor.
- Instruct patient in signs, symptoms, and treatment of hypoglycemic reaction.
- Review dietary and exercise guidelines for diabetes with patient.
- Instruct patient to take dose with breakfast.
- Teach patient to self-monitor urine or blood glucose.
- Instruct patients to inform all health care providers that they are taking this medicine and to carry medical identification (eg, card, bracelet).
- Instruct patient to notify health care provider if symptoms of hypoglycemia occur (eg, excessive hunger, fatigue, numbness of extremities, profuse sweating) or if blood glucose is below 60 mg/dL.
- Tell patient to notify health care provider if symptoms of hyperglycemia occur (eg, excessive thirst or urination, urinary glucose or ketones).
- Instruct patient to report the following symptoms to health care provider: diarrhea, heartburn, nausea, rash, sore throat, unusual bleeding or bruising, vomiting, or any other adverse reactions.
- Advise patient to avoid exposure to sunlight or sunlamps, and to use sunscreen or wear protective clothing to avoid photosensitivity reaction.
- Advise patient to check with health care provider before drinking alcohol.
Copyright © 2009 Wolters Kluwer Health.
More about glimepiride
- Other brands: Amaryl