WordNet

snowdrop; narcissus; daffodil; in some classification systems considered a subfamily of the Liliaceae (同)family Amaryllidaceae, amaryllis family
type genus of the Amaryllidaceae; bulbous flowering plants of southern Africa

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/08/28 15:12:20」(JST)

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Glimepiride is a medium- to long-acting sulfonylurea antidiabetic drug. It is marketed as SUGRAL by Pakistani firm Rakaposhi Pharmaceuticals, 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.

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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1. 糖尿病の治療におけるスルホニル尿素およびメグリチニド sulfonylureas and meglitinides in the treatment of diabetes mellitus
2. 2型糖尿病における持続性高血糖のマネージメント management of persistent hyperglycemia in type 2 diabetes mellitus
3. 成人における低血糖：臨床症状、定義、および原因 hypoglycemia in adults clinical manifestations definition and causes
4. 2型糖尿病のGlucagon-like peptide-1をベースとした治療 glucagon like peptide 1 based therapies for the treatment of type 2 diabetes mellitus
5. 小児および思春期における2型糖尿病のマネージメント management of type 2 diabetes mellitus in children and adolescents

English Journal

A toxicology study to evaluate the embryotoxicity of metformin compared with the hypoglycemic drugs, the anticancer drug, the anti-epileptic drug, the antibiotic, and the cyclo-oxygenase (COX)-2 inhibitor.

Li L1,2, Zhang X2,3, Wang L2,3, Chai Z2, Shen X2, Zhang Z2, Liu C1,4.
Journal of diabetes.J Diabetes.2015 Nov;7(6):839-849. doi: 10.1111/1753-0407.12251. Epub 2015 Mar 4.
BACKGROUND: The safe use of medications in pregnant females, their embryos and in offspring is important. The aim of the present study was to evaluate embryotoxicity of metformin (MET) compared with other hypoglycemic drugs (rosiglitazone [RSG] and glimepiride [GLIM]), the anticancer drug 5-fluorour
PMID 25492223

Open-label randomized non-inferiority trial of a fixed-dose combination of glimepiride and atorvastatin for the treatment of people whose Type 2 diabetes is uncontrolled on metformin.

Ambery P1, Stylianou A2, Atkinson G3, Dott C3, Baylor Curtis L3, Haque N3, LaCroix K4, Min KW5; glimepiride/atorvastatin investigational team.
Diabetic medicine : a journal of the British Diabetic Association.Diabet Med.2015 Oct 20. doi: 10.1111/dme.13003. [Epub ahead of print]
AIMS: To evaluate, in a randomized, open-label study, the non-inferiority of a bioequivalent fixed-dose combination of glimepiride and atorvastatin vs. separately co-administered tablets in people with Type 2 diabetes mellitus.METHODS: Participants with HbA1c ≥53 to <80 mmol/mol (≥7.0 to <
PMID 26484794

Teneligliptin: A Review in Type 2 Diabetes.

Scott LJ1.
Clinical drug investigation.Clin Drug Investig.2015 Oct 16. [Epub ahead of print]
Oral teneligliptin [Teneglucon® (Argentina)], a dipeptidyl peptidase-4 inhibitor, is indicated for the treatment of adults with type 2 diabetes (T2DM). This article reviews the pharmacology, therapeutic efficacy and tolerability of teneligliptin in the treatment of adults with T2DM. In 12- or 16-we
PMID 26475720

Japanese Journal

文字形状の類似性に基づく医薬品名の類似度算出手法の提案

鍋田啓太,今井貴広,木村昌臣,大倉典子,土屋文人
日本感性工学会論文誌 10(2), 287-294, 2011
… There are many reports of medical errors mainly caused by the similarity of drug names in Japanese such as '_??__??__??__??__??_' (Amaryl) and '_??__??__??__??__??_' (Almarl). …
NAID 130001362013

スルホニルウレア系経口血糖降下薬グリメピリド (アマリール^<【○ ! R】>) の薬理作用と臨床効果

坂東勝啓,山田宜和
日本薬理学雑誌 118(1), 59-67, 2001-07-01
2型糖尿病は, 膵β細胞からのインスリン分泌不全およびインスリンの標的組織(肝臓, 筋肉, 脂肪組織)におけるインスリン感受性低下が原因で高血糖を呈することが知られている. 現在2型糖尿病の薬物治療の主流をなしている薬剤は, インスリン分泌を促進することで強い血糖降下作用を示すスルホニルウレア系経口血糖降下薬(SU薬)であるが, 強力なインスリン分泌促進作用のため, 体重増加·低血糖·膵β細胞の疲 …
NAID 10007366734

新規スルホニルウレア剤グリメピリド (HOE490, Amaryl) の抗粥状動脈硬化作用

赤藤修司
糖尿合併 15(Suppl 1), 68, 2001
NAID 50000689998

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★リンクテーブル★

リンク元	「グリメピリド」
拡張検索	「Amaryllidaceae alkaloid」

「グリメピリド」

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 cat.	C (US)
Legal status	Rx only
Routes	Oral
Pharmacokinetic data
Bioavailability	100%
Protein binding	>99.5%
Half-life	5 hours
Excretion	Urine, faeces
Identifiers
CAS 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
Mol. 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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