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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/04/22 11:11:16」(JST)

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Glimepiride is a medium- to long-acting sulfonylurea antidiabetic drug. It is marketed as GLEAM by Franco Indian Pharmaceuticals,K-GLIM-1 by BLUE CROSS, Glucoryl by Alkem Lab PVT LTD , Amaryl by Sanofi-Aventis, GLIMPID by Ranbaxy Laboratories(Cardiovascular) and GLIMY by Dr.Reddy's Labs.

It is sometimes classified as either the first third-generation sulfonylurea,^[1] or as second-generation.^[2]

Indication / contraindications

Glimepiride is indicated to treat type 2 diabetes mellitus; its mode of action is to increase insulin production by the pancreas. It is not used for type 1 diabetes because in type 1 diabetes the pancreas is not able to produce insulin.^[3]

Its use is contraindicated in patients with hypersensitivity to glimepiride or other sulfonylureas, and during pregnancy.

Adverse effects

Side effects from taking glimepiride include gastrointestinal tract (GI) disturbances, occasional allergic reactions, and rarely blood production disorders including thrombocytopenia, leukopenia, and hemolytic anemia. In the initial weeks of treatment, the risk of hypoglycemia may be increased. Alcohol consumption and exposure to sunlight should be restricted because they can worsen side effects.^[3]

Pharmacokinetics

2-mg oral tablet of glimepiride

Gastrointestinal absorption is complete, with no interference from meals. Significant absorption can occur within one hour, and distribution is throughout the body, 99.5% bound to plasma protein. Metabolism is by oxidative biotransformation. Excretion in the urine is 65%, and the remainder is excreted in the feces.

Mechanism of action

Like all sulfonylureas, glimepiride acts as an insulin secretagogue.^[4] 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 as low as 2% to 4% with glimepiride. Glibenclamide also interferes with the normal homeostatic suppression of insulin secretion in reaction to hypoglycemia, whereas glimepiride does not. Also, glibenclamide diminishes glucagon secretion in reaction to hypoglycemia, whereas glimepiride does not.^[5]

Interactions

Nonsteroidal anti-inflammatory drugs (such as salicylates), sulfonamides, chloramphenicol, coumadin and probenecid) may potentiate the hypoglycemic action of glimepiride. Thiazides, other diuretics, phothiazides, thyroid products, oral contraceptives, and phenytoin tend to produce hyperglycemia.

Synthesis

Glimepiride synthesis: Weyer, R.; Hitzel, V.; Arnzeim.-Forsch. 1988, 8, 1079.

References

^ Hamaguchi T, Hirose T, Asakawa H et al. (December 2004). "Efficacy of glimepiride in type 2 diabetic patients treated with glibenclamide". Diabetes Res. Clin. Pract. 66 Suppl 1: S129–32. doi:10.1016/j.diabres.2003.12.012. PMID 15563963.
^ Davis SN (2004). "The role of glimepiride in the effective management of Type 2 diabetes". J. Diabetes Complicat. 18 (6): 367–76. doi:10.1016/j.jdiacomp.2004.07.001. PMID 15531188.
^ ^a ^b http://www.nlm.nih.gov/medlineplus/druginfo/meds/a696016.html
^ Nissen SE, Nicholls SJ, Wolski K et al. (April 2008). "Comparison of pioglitazone vs glimepiride on progression of coronary atherosclerosis in patients with type 2 diabetes: the PERISCOPE randomized controlled trial". JAMA 299 (13): 1561–73. doi:10.1001/jama.299.13.1561. PMID 18378631.
^ Davis, Stephen N. (2005). "60. Insulin, oral hypoglycemic agents, and the pharmacology of the endocrine pancreas". In Brunton, Laurence L.; Lazo, John S.; Parker, Keith L. (eds.). Goodman & Gilman's The Pharmacological Basis of Therapeutics. New York: McGraw-Hill. p. 1636. ISBN 0-07-142280-3.

External links

http://www.drugdigest.org/DD/DVH/Uses/1,3915,298%7CAmaryl%2BTablets%7C2805,00.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

UpToDate Contents

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4. 高齢患者における2型糖尿病の治療 treatment of type 2 diabetes mellitus in the elderly patient
5. 末期腎不全を併う糖尿病における高血糖のマネージメント management of hyperglycemia in diabetics with end stage renal disease

English Journal

Reno-protection of G004, a novel anti-diabetic sulfonylurea in db/db mice.

Tong X1, Ma H, Amadi SW, Ma L, Wu G.
Naunyn-Schmiedeberg's archives of pharmacology.Naunyn Schmiedebergs Arch Pharmacol.2015 Aug;388(8):831-41. doi: 10.1007/s00210-015-1112-7. Epub 2015 May 6.
1-[4-[2-(4-Bromobenzene-sulfonamino)ethyl]phenylsulfonyl]-3-(trans-4-methylcyclohexyl) urea (G004, CAS865483-06-3) is a synthetic sulfonylurea, incorporating the hypoglycemic active structure of glimepiride (CAS 93479-97-1) and anti-TXA2 receptor (TP) active structure of BM-531(CAS 284464-46-6). In
PMID 25943026

Evaluating the Cost of Bringing People with Type 2 Diabetes Mellitus to Multiple Targets of Treatment in Canada.

Skovgaard R1, Jon Ploug U2, Hunt B3, Valentine WJ3.
Clinical therapeutics.Clin Ther.2015 Jul 14. pii: S0149-2918(15)00829-2. doi: 10.1016/j.clinthera.2015.05.496. [Epub ahead of print]
PURPOSE: Evidence suggests that clinical outcomes for people with type 2 diabetes mellitus can be improved through multifactorial treatment. The key challenges in the successful treatment of type 2 diabetes include maintaining tight glycemic control, minimizing the risk of hypoglycemia, controlling
PMID 26186809

A Pharmacokinetic/Pharmacodynamic Drug-Drug Interaction Study of Tofogliflozin (a New SGLT2 Inhibitor) and Selected Anti-Type 2 Diabetes Mellitus Drugs.

Kasahara N1, Fukase H2, Ohba Y1, Saito T1, Miyata K1, Iida S1, Takano Y1, Ikeda S1, Harigai M3, Terao K1.
Drug research.Drug Res (Stuttg).2015 Jul 9. [Epub ahead of print]
Objective: Tofogliflozin is an oral hypoglycemic agent with a novel mechanism of action that reduces blood glucose levels by promoting glucose excretion in urine, achieved by selectively inhibiting sodium-glucose co-transporter 2 (SGLT2). We evaluated the effects of several selected anti-type 2 diab
PMID 26158794

Japanese Journal

GLP-1受容体作動薬リラグルチド単独療法による包括的な血糖コントロール--LEAD-3試験およびLEAD-3延長試験の意義

吉岡成人
内分泌・糖尿病・代謝内科 32(5), 514-520, 2011-05
NAID 40018905231

症例少量glimepiride投与による急激な血小板減少の1例

中川潤一,川津潤一郎,樹下富貴子 [他]
内科 107(4), 735-738, 2011-04
NAID 40018771209

Related Pictures

★リンクテーブル★

リンク元	「スルホニル尿酸系薬」「グリメピリド」

「スルホニル尿酸系薬」

Glimepiride
Systematic (IUPAC) name
	3-ethyl-4-methyl-N-(4-[N-((1r,4r)-4-methylcyclohexylcarbamoyl)sulfamoyl]phenethyl)-2-oxo-2,5-dihydro-1H-pyrrole-1-carboxamide
Clinical data
Trade names	Amaryl
AHFS/Drugs.com	monograph
MedlinePlus	a696016
Pregnancy; category	US: C (Risk not ruled out);
Legal status	℞ (Prescription only);
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	100%
Protein binding	>99.5%
Half-life	5 hours
Excretion	Urine, faeces
Identifiers
CAS Registry Number	93479-97-1
ATC code	A10BB12
PubChem	CID 3476
DrugBank	DB00222
ChemSpider	16740595
UNII	6KY687524K
KEGG	D00593
ChEBI	CHEBI:5383
ChEMBL	CHEMBL1481
Chemical data
Formula	C24H34N4O5S
Molecular mass	490.617 g/mol
	SMILES O=C3C(/CC)=C(/C)CN3C(=O)NCCc1ccc(cc1)S(=O)(=O)NC(=O)N[C@H]2CC[C@H](C)CC2;
	InChI InChI=1S/C24H34N4O5S/c1-4-21-17(3)15-28(22(21)29)24(31)25-14-13-18-7-11-20(12-8-18)34(32,33)27-23(30)26-19-9-5-16(2)6-10-19/h7-8,11-12,16,19H,4-6,9-10,13-15H2,1-3H3,(H,25,31)(H2,26,27,30)/t16-,19- ; Key:WIGIZIANZCJQQY-RUCARUNLSA-N ;
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