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an oral antidiabetic drug (trade name Glucotrol) that stimulates the release of insulin from the pancreas (同)Glucotrol

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/05 00:34:09」(JST)

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Glipizide is an oral rapid- and short-acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. Second-generation sulfonylureas are both more potent and have shorter half-lives than the first-generation sulfonylureas.

Originally available in 1984, it is marketed by Pfizer under the brand name Glucotrol in the USA, where Pfizer sells Glucotrol in doses of 5 and 10 milligrams and Glucotrol XL (an extended release form of glipizide) in doses of 2.5, 5, and 10 milligrams. Other companies also market glipizide, most commonly extended release tablets of 5 and 10 milligrams.

Mechanism of Action

Glipizide acts by partially blocking potassium channels among beta cells of pancreatic islets of Langerhans. By blocking potassium channels, the cell depolarizes which results in the opening of voltage-gated calcium channels. The resulting calcium influx encourages insulin release from beta cells.

Sulfonylureas may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues.^{[citation needed]} The mouse model of MODY diabetes suggested that the reduced glipizide clearance stands behind their therapeutic success in human MODY patients, but Urbanova et al. found that human MODY patients respond differently to the mouse model and that there was no consistent decrease in glipizide clearance in randomly selected HNF1A-MODY and HNF4A-MODY patients.^[1]

References

^ Urbanova, J.; et al. (2015). "Half-Life of Sulfonylureas in HNF1A and HNF4A Human MODY Patients is not Prolonged as Suggested by the Mouse Hnf1a-/- Model". Current Pharmaceutical Design 21: 5736–5748. doi:10.2174/1381612821666151008124036.

External links

Glucotrol XL Full U.S. Prescribing Information. Accessed on July 26, 2005.

UpToDate Contents

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1. 2型糖尿病の治療のためのジペプチジルペプチダーゼ4（DPP-4）阻害剤 dipeptidyl peptidase 4 dpp 4 inhibitors for the treatment of type 2 diabetes mellitus
2. 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
3. 透析前慢性腎臓病または末期腎不全を伴う2型糖尿病患者における高血糖のマネージメント management of hyperglycemia in patients with type 2 diabetes and pre dialysis chronic kidney disease or end stage renal disease
4. 成人の2型糖尿病における血糖の初期マネージメント initial management of blood glucose in adults with type 2 diabetes mellitus
5. 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

English Journal

Durability of glycaemic efficacy over 2 years with dapagliflozin versus glipizide as add-on therapies in patients whose type 2 diabetes mellitus was inadequately controlled with metformin.

Nauck MA1, Del Prato S, Durán-García S, Rohwedder K, Langkilde AM, Sugg J, Parikh SJ.
Diabetes, obesity & metabolism.Diabetes Obes Metab.2014 Jun 12. doi: 10.1111/dom.12327. [Epub ahead of print]
AIMS: To assess long-term glycaemic durability, safety and tolerability of dapagliflozin versus glipizide as add-on therapies in patients with type 2 diabetes inadequately controlled on metformin. Research Design And Methods This was a 52-week, randomized, double-blind study of dapagliflozin (n =�
PMID 24919526

Coadministration of Co-trimoxazole With Sulfonylureas: Hypoglycemia Events and Pattern of Use.

Tan A1, Holmes HM2, Kuo YF3, Raji MA4, Goodwin JS5.
The journals of gerontology. Series A, Biological sciences and medical sciences.J Gerontol A Biol Sci Med Sci.2014 May 24. pii: glu072. [Epub ahead of print]
BACKGROUND: Coadministration of co-trimoxazole with sulfonylureas is reported to increase the risk of hypoglycemia.METHODS: We identified a cohort of Medicare beneficiaries aged 66 years or older who took glyburide or glipizide for diabetes from a 5% national sample of Medicare Part D claims data in
PMID 24858839

Diabetes mellitus and kidney disease in the elderly.

Iglesias P, Heras M, Díez JJ.
Nefrologia : publicacion oficial de la Sociedad Espanola Nefrologia.Nefrologia.2014 May 21;34(3):285-292. doi: 10.3265/Nefrologia.pre2014.Feb.12319. Epub 2014 Apr 10.
Management of diabetic elderly patients with chronic kidney disease involves specific characteristics that affect both metabolic control and therapeutic measures. Blood glucose control targets should be individualised based on life expectancy, renal function, hypoglycaemia risk and comorbidity. Metf
PMID 24798557

Japanese Journal

Sulfonylurea receptor as a target for molecular imaging of pancreas beta cells with ^<99m>Tc-DTPA-glipizide

OH Chang-Sok,KOHANIM Saady,KONG Fan-Lin,SONG Ho-Chun,HUYNH Nathan,MENDEZ Richard,CHANDA Mithu,KIM E. Edmund,YANG David J.
Annals of nuclear medicine 26(3), 253-261, 2012-04-01
NAID 10030623886

Extended Release Dosage Form of Glipizide : Development and Validation of a Level A in Vitro-in Vivo Correlation(Biopharmacy)

GHOSH Animesh,BHAUMIK Uttam Kumar,BOSE Anirbandeep,MANDAL Uttam,GOWDA Veeran,CHATTERJEE Bappaditya,CHAKRABARTY Uday Sankar,PAL Tapan Kumar
Biological & pharmaceutical bulletin 31(10), 1946-1951, 2008-10-01
… During the development of once daily extended-release (ER) tablet of glipizide, a predictive in vitro drug release method was designed and statistically evaluated using three formulations with varying release rates. … In order to establish internally and externally validated level A in vitro-in vivo correlation (IVIVC), a total of three different ER formulations of glipizide were used to evaluate a linear IVIVC model based on the in vitro test method. …
NAID 110006936339

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「グリピジド」

Glipizide
Systematic (IUPAC) name
	N-(4-[N-(cyclohexylcarbamoyl)sulfamoyl]phenethyl)-5-methylpyrazine-2-carboxamide
Clinical data
Trade names	Glucotrol
AHFS/Drugs.com	monograph
MedlinePlus	a684060
Pregnancy; category	C (Au, U.S.);
Legal status	POM (UK), ℞-only (U.S.);
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	100% (regular formulation); 90% (extended release)
Protein binding	98 to 99%
Metabolism	Hepatic hydroxylation
Biological half-life	2 to 5 hours
Excretion	Renal and fecal
Identifiers
CAS Number	29094-61-9
ATC code	A10BB07
PubChem	CID: 3478
IUPHAR/BPS	6821
DrugBank	DB01067
ChemSpider	3359
UNII	X7WDT95N5C
KEGG	D00335
ChEBI	CHEBI:5384
ChEMBL	CHEMBL1073
Chemical data
Formula	C21H27N5O4S
Molecular mass	445.536 g/mol
	SMILES O=C(c1ncc(nc1)C)NCCc2ccc(cc2)S(=O)(=O)NC(=O)NC3CCCCC3 ;
	InChI InChI=1S/C21H27N5O4S/c1-15-13-24-19(14-23-15)20(27)22-12-11-16-7-9-18(10-8-16)31(29,30)26-21(28)25-17-5-3-2-4-6-17/h7-10,13-14,17H,2-6,11-12H2,1H3,(H,22,27)(H2,25,26,28) ; Key:ZJJXGWJIGJFDTL-UHFFFAOYSA-N ;
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英: glipizide

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グリピジド : 約 7,180 件
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米国における糖尿病治療薬。日本での発売はないらしい。
スルフォニル尿酸系薬

[Urbanova_et_al._2015-1] Urbanova, J.; et al. (2015). "Half-Life of Sulfonylureas in HNF1A and HNF4A Human MODY Patients is not Prolonged as Suggested by the Mouse Hnf1a-/- Model". Current Pharmaceutical Design 21: 5736–5748. doi:10.2174/1381612821666151008124036.

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glipizide