Glimepiride
Encyclopedia
Glimepiride is a medium-to-long acting sulfonylurea
anti-diabetic drug
. It is marketed as Amaryl by Sanofi-Aventis
and GLIMY by Dr.Reddy's Labs. Glimepiride is the first third-generation sulfonylurea, and is very potent.
It is sometimes classified as third-generation, and sometimes classified as second-generation.
disturbance, rarely thrombocytopenia , leukopenia, hemolytic anemia, occasionally allergic reactions occur. In the initial weeks of treatment, the risk of hypoglycemia may be increased.
. It lowers blood sugar by stimulating the release of insulin by pancreatic beta cells and by inducing increased activity of intracellular insulin receptors.
Not all secondary sufonylureas have the same risks of hypoglycemia. Glibenclamide (glyburide) is associated with an incidence of hypoglycemia of up to 20–30%, compared to 2% to 4% with glimepiride. Glibenclamide also interferes with the normal homeostatic suppression of insulin secretion in reaction to hypoglycemia, whereas glimepiride does not have this property. Furthermore, glibenclamide diminishes the glucagon secretion in reaction to hypoglycemia, whereas glimepiride does not suppress this counter-regulatory reaction.
, coumadin
and probenecid
may potentiate the hypoglycemic action of glimepiride. Thiazide
s, other diuretic
, phothiazides, thyroid products, oral contraceptives, phenytoin
tend to produce hyperglycemia
.
Sulfonylurea
Sulfonylurea derivatives are a class of antidiabetic drugs that are used in the management of diabetes mellitus type 2. They act by increasing insulin release from the beta cells in the pancreas.-First generation:* Carbutamide...
anti-diabetic drug
Anti-diabetic drug
Anti-diabetic medications treat diabetes mellitus by lowering glucose levels in the blood. With the exceptions of insulin, exenatide, and pramlintide, all are administered orally and are thus also called oral hypoglycemic agents or oral antihyperglycemic agents...
. It is marketed as Amaryl by Sanofi-Aventis
Sanofi-Aventis
Sanofi S.A. is a multinational pharmaceutical company headquartered in Paris, France, the world's fourth-largest by prescription sales. Sanofi engages in the research and development, manufacturing and marketing of pharmaceutical products for sale principally in the prescription market, but the...
and GLIMY by Dr.Reddy's Labs. Glimepiride is the first third-generation sulfonylurea, and is very potent.
It is sometimes classified as third-generation, and sometimes classified as second-generation.
Adverse effects
GIGastrointestinal tract
The human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....
disturbance, rarely thrombocytopenia , leukopenia, hemolytic anemia, occasionally allergic reactions occur. In the initial weeks of treatment, the risk of hypoglycemia may be increased.
Pharmacokinetics
With glimepiride GI absorption is complete, with no interference of meals. Significant absorption of glimepiride was seen within 1 hour, and distributed throughout the body, bound to the plasma protein to an extent of 99.5% and it is metabolized by oxidative biotransformation and 60% is excreted in the urine, the remaining being excreted in the feces.Mechanism of action
Like all sulfonylureas, glimepiride acts as a secretagogueSecretagogue
A secretagogue is a substance that causes another substance to be secreted. One example is gastrin,, which stimulates the H/K ATPase in the parietal cells...
. It lowers blood sugar by stimulating the release of insulin by pancreatic beta cells and by inducing increased activity of intracellular insulin receptors.
Not all secondary sufonylureas have the same risks of hypoglycemia. Glibenclamide (glyburide) is associated with an incidence of hypoglycemia of up to 20–30%, compared to 2% to 4% with glimepiride. Glibenclamide also interferes with the normal homeostatic suppression of insulin secretion in reaction to hypoglycemia, whereas glimepiride does not have this property. Furthermore, glibenclamide diminishes the glucagon secretion in reaction to hypoglycemia, whereas glimepiride does not suppress this counter-regulatory reaction.
Interactions
With NSAIDs like Salicylates, Sulphonamides, ChloramphenicolChloramphenicol
Chloramphenicol is a bacteriostatic antimicrobial that became available in 1949. It is considered a prototypical broad-spectrum antibiotic, alongside the tetracyclines, and as it is both cheap and easy to manufacture it is frequently found as a drug of choice in the third world.Chloramphenicol is...
, coumadin
Coumadin
*For the rodenticide class of anticoagulant poisons sometimes loosely referred to as coumadins or coumarins, see 4-hydroxycoumarins.*For the pharmaceutical with the trade name Coumadin, see warfarin....
and probenecid
Probenecid
Probenecid is a uricosuric drug that increases uric acid excretion in the urine. It is primarily used in treating gout and hyperuricemia.Probenecid was developed as an alternative to caronamide...
may potentiate the hypoglycemic action of glimepiride. Thiazide
Thiazide
Thiazide is a term used to describe a type of molecule and a class of diuretics often used to treat hypertension and edema ....
s, other diuretic
Diuretic
A diuretic provides a means of forced diuresis which elevates the rate of urination. There are several categories of diuretics. All diuretics increase the excretion of water from bodies, although each class does so in a distinct way.- Medical uses :...
, phothiazides, thyroid products, oral contraceptives, phenytoin
Phenytoin
Phenytoin sodium is a commonly used antiepileptic. Phenytoin acts to suppress the abnormal brain activity seen in seizure by reducing electrical conductance among brain cells by stabilizing the inactive state of voltage-gated sodium channels...
tend to produce hyperglycemia
Hyperglycemia
Hyperglycemia or Hyperglycæmia, or high blood sugar, is a condition in which an excessive amount of glucose circulates in the blood plasma. This is generally a glucose level higher than 13.5mmol/l , but symptoms may not start to become noticeable until even higher values such as 15-20 mmol/l...
.
External links
- http://www.drugdigest.org/DD/DVH/Uses/1,3915,298|Amaryl%2BTablets|2805,00.html*
- http://www.theodora.com/drugs/amaryl_tablets_sanofi_aventis.html
- http://www.rxlist.com/cgi/generic/glimepiride.htm
- http://www.pharmgkb.org/do/serve?objId=213&objCls=DrugProperties