Drug information of Glimepiride
Glimepiride is an oral sulfonylurea that contains the active ingredient Glimepiride .
Mechanism of effect
Glimepiride primarily lowers blood glucose by stimulating the release of insulin from pancreatic beta cells. Sulfonylureas bind to the sulfonylurea receptor in the pancreatic beta- cell plasma membrane, leading to closure of the ATP-sensitive potassium channel, thereby stimulating the release of insulin .
Glimepiride, like glyburide and glipizide, is a "second-generation" sulfonylurea agents. Glimepiride is used with diet to lower blood glucose by increasing the secretion of insulin from pancreas and increasing the sensitivity of peripheral tissues to insulin .
In healthy subjects, the time to reach maximal effect (minimum blood glucose concentrations) was approximately 2 to 3 hours after single oral doses of Glimepiride.
Absorption : Studies with single oral doses of Glimepiride in healthy subjects and with multiple oral doses in patients with type 2 diabetes showed peak drug concentrations (C max) 2 to 3 hours post-dose. When Glimepiride was given with meals, the mean C max and AUC (area under the curve) were decreased by 8% and 9%, respectively.
Distribution : After intravenous dosing in healthy subjects, the volume of distribution (Vd) was 8.8 L (113 mL/kg), and the total body clearance (CL) was 47.8 mL/min. Protein binding was greater than 99.5%.
Metabolism : Glimepiride is completely metabolized by oxidative biotransformation after either an intravenous or oral dose .
Excretion : When 14C-Glimepiride was given orally to 3 healthy male subjects, approximately 60% of the total radioactivity was recovered in the urine in 7 days.
* Usual Adult Dose for Diabetes Type 2
Initial dose : 1 to 2 mg orally once a day
Maintenance dose : Increase in 1 or 2 mg increments no more frequently than every 1 to 2 weeks based on glycemic response
Maximum dose : 8 mg respons
* Usual Geriatric Dose for Diabetes Type 2
Initial dose : 1 mg orally once a day; titrate slowly and monitor closely
Usual Pediatric Dose for Diabetes Type 2
Not recommended because of adverse effects on body weight and hypoglycemia.
Drug contraindicationshypersensitivity to this drug
Side effectsnausea , Headache , dizziness , vomiting , Diarrhea , asthenia , aplastic anemia, , Agranulocytosis , Abdominal pains , Leukopenia , thrombocytopenia
InteractionsOlanzapine , insulin , Isoniazid , pentoxifylline , Diazoxide , Ranitidine , Rifampin , Cimetidine , Fluconazole , Clarithromycin , Clonidine , Clozapine , Sitagliptin , Thyrotropin alfa , Peginterferon alfa-2b , Canagliflozin , lumacaftor and Ivacaftor , Grepafloxacin , aminolevulinic acid oral , Aminolevulinic acid topical , Vorinostat , Cannabidiol , Alclometasone , flurandrenolide
All sulfonylureas, including Glimepiride , can cause severe hypoglycemia.Use caution when initiating and increasing Glimepiride doses in patients who may be predisposed to hypoglycemia (e.g., the elderly, patients with renal impairment, patients on other anti- diabetic medications).
There have been postmarketing reports of hypersensitivity reactions in patients treated with Glimepiride, including serious reactions such as anaphylaxis, angioedema, and Stevens- Johnson Syndrome.
If a hypersensitivity reaction is suspected, promptly discontinue Glimepiride , assess for other potential causes for the reaction, and institute alternative treatment for diabetes.Sulfonylureas can cause hemolytic anemia in patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency.
The administration of oral hypoglycemic drugs has been reported to be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin.
Points of recommendation
Some medical conditions may interact with glimepiride . Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you :
• if you are pregnant, planning to become pregnant, or are breast-feeding
• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
• if you have allergies to medicines, foods, or other substances
• if you have had a severe allergic reaction (eg, a severe rash, hives, breathing difficulties, dizziness) to any other sulfonamide medicine, such as acetazolamide, celecoxib, certain diuretics (eg, hydrochlorothiazide), glipizide, probenecid, sulfamethoxazole, valdecoxib, or zonisamide
• if you have a history of stroke or liver, kidney, thyroid, heart, or blood vessel problems
• if you have stomach or bowel problems (eg, stomach or bowel blockage, stomach paralysis), drink alcohol, or have had poor nutrition
• if you have type 1 diabetes, anemia, very poor health, a high fever, a severe infection, severe diarrhea, high blood acid levels, or brain or nervous system problems, or have had a severe injury
• if you have low levels of an enzyme called glucose 6-phosphate dehydrogenase (G6PD)
• if you have a history of certain hormonal problems (eg, adrenal or pituitary problems, syndrome of inappropriate secretion of antidiuretic hormone [SIADH]) or low blood sodium levels
• if you will be having surgery