関: mitiglinide calcium、mitiglinide calcium hydrate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/11 04:56:52」(JST)

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Mitiglinide (INN, trade name Glufast) is a drug for the treatment of type 2 diabetes.^[1]

Mitiglinide belongs to the meglitinide class of blood glucose-lowering drugs and is currently co-marketed in Japan by Kissei and Takeda. The North America rights to mitiglinide are held by Elixir Pharmaceuticals. Mitiglinide has not yet gained FDA approval.

Pharmacology

Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) K(ATP) channels in pancreatic beta-cells.

Dosage

Mitiglinide is delivered in tablet form.

References

^ Malaisse WJ (October 2008). "Mitiglinide: a rapid- and short-acting non-sulfonylurea insulinotropic agent for the treatment of type 2 diabetic patients". Expert Opin Pharmacother 9 (15): 2691–8. doi:10.1517/14656566.9.15.2691. PMID 18803455.

External links

Elixir Pharmaceuticals - website of the U.S. rights holder for mitiglinide.

English Journal

The glycemic/metabolic responses to meal tolerance tests at breakfast, lunch and dinner, and effects of the mitiglinide/voglibose fixed-dose combination on postprandial profiles in Japanese patients with type 2 diabetes mellitus.

Ono Y, Nakamura A, Yong Cho K, Nomoto H.Author information Yuri Ono Clinic, Diabetes, Internal Medicine , Sapporo Kita-1 Ekimaedori Building 7F, 3-27, Nishi-3, Kita-1, Chuo-Ku, Sapporo 060-0001 , Japan +81 11 223 5152 ; +81 11 223 5153 ; yuriono@ja2.so-net.ne.jp.AbstractBackground: Meal tolerance tests (MTTs) are usually conducted at breakfast after overnight fasting in type 2 diabetes mellitus (T2DM) patients, but differences in postprandial glycemic responses between meals have been reported. Objective: We conducted MTTs at breakfast, lunch, and dinner to examine the effects of a fixed combination of 10 mg mitiglinide/0.2 mg voglibose (the combination) on glycemic/metabolic responses to meals during the day in T2DM patients. MTTs with unified meals were conducted in 11 T2DM patients before and after 4 weeks of treatment with the combination administered thrice daily before meals. Glycemic/metabolic profiles measured before and at 30, 60, and 120 min after each meal were compared between each meal and between the baseline and treatment periods. Results and conclusion: The combination significantly reduced postprandial hyperglycemia after each meal. Postprandial AUC0 - 120 min for insulin significantly decreased after lunch and dinner compared with after breakfast, while insulin levels significantly increased at only 30 min after breakfast and dinner. The combination also significantly increased postprandial C-peptide and active glucagon-like peptide-1 levels, and reduced free fatty acid and triglyceride levels, but did not significantly affect glucagon levels compared with baseline, confirming that treatment with the combination improves postprandial responses in Japanese T2DM patients.
Expert opinion on pharmacotherapy.Expert Opin Pharmacother.2014 Feb;15(3):311-24. doi: 10.1517/14656566.2014.868437. Epub 2013 Dec 13.
Background: Meal tolerance tests (MTTs) are usually conducted at breakfast after overnight fasting in type 2 diabetes mellitus (T2DM) patients, but differences in postprandial glycemic responses between meals have been reported. Objective: We conducted MTTs at breakfast, lunch, and dinner to examine
PMID 24328511

Perturbation of mitiglinide metabolism by chronic unpredicted mild stress in rats.

Zeng Y1, Xie X2, Duan J2, Zhou T2, Zhang Y2, Yang M1, Xu F2.Author information 1Guangdong General Hospital, Guangdong Academy of Medical Sciences, Guangzhou, 510080, China.2Sixth People's Hospital South Campus, Shanghai Jiaotong University, Shanghai, 201400, China.AbstractMany diabetic patients complicated with wild to severe depression. It is unclear in diabetic medication whether depression perturbs the drug metabolic process of the hypoglycemic agents or not. The present study was designed to investigate the impact of chronic unpredicted mild stress (CUMS) -induced depression on mitiglinide (MGN) pharmacokinetics in rats. Adult female Sprague-Dawley rats in CUMS group were subjected to different types of stressors and the stress procedures lasted for 8 weeks. Control group without receiving stress had free access to food and water. Open-field test and 5-HT levels were assayed to evaluate the depression. After CUMS all rats were given 2.5 mg/kg of mitiglinide per os. The blood samples were collected at different time and mitiglinide plasma concentration was measured by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). Non-compartmental statistical moment analysis was processed with DAS software. In CMUS-induced depression group, peak concentration (Cmax), peak time (Tmax), area under curve (AUC0 → ∞), mean residence time (MRT0 → ∞), and half-life (T1/2z) were reduced while total plasma clearance (CLz/F) was increased compared to control group. These preliminary results indicated that CUMS-induced depression alter the drug metabolic process of mitiglinide in rats. This finding will be significant in clinic.
Scientific reports.Sci Rep.2014 Jan 21;4:3794. doi: 10.1038/srep03794.
Many diabetic patients complicated with wild to severe depression. It is unclear in diabetic medication whether depression perturbs the drug metabolic process of the hypoglycemic agents or not. The present study was designed to investigate the impact of chronic unpredicted mild stress (CUMS) -induce
PMID 24445843

Erratum to: Additive Postprandial Glucose-Lowering Effects of Mitiglinide and Sitagliptin in Patients with Type 2 Diabetes Mellitus.

Jung JA, Kaku K, Kim JH, Kim JR, Ko JW, Lee SY, Huh W.
Advances in therapy.Adv Ther.2013 Dec 19. [Epub ahead of print]
PMID 24353067

Japanese Journal

Nateglinide Stimulates Glucagon-Like Peptide-1 Release by Human Intestinal L Cells via a KATP Channel-Independent Mechanism

Kitahara Yoshiro,Miura Kyoko,Yasuda Reiko,Kawanabe Haruka,Ogawa Shimpei,Eto Yuzuru
Biological & Pharmaceutical Bulletin 34(5), 671-676, 2011
… In addition, the major metabolite of nateglinide, tolbutamide, and mitiglinide, all of which augment insulin secretion by the pancreatic islets, had no effect on GLP-1 release by this cell line. …
NAID 130000657778

O2-14 胃内pH上昇によるmitiglinideの吸収遅延に関する検討(一般演題口頭発表,薬物動態・TDM・投与設計,臨床から学び臨床へと還元する医療薬学)

浦嶋庸子,有本諭司,茅野英司,加藤隆児,井尻好雄,田中一彦
日本医療薬学会年会講演要旨集 20, 259, 2010-10-25
NAID 110008108229

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「ミチグリニド」

Mitiglinide
Systematic (IUPAC) name
	(2S)-2-benzyl-4-[(3aR,7aS)-octahydro-2H-isoindol- 2-yl]-4-oxobutanoic acid
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	oral
Identifiers
CAS Registry Number	145375-43-5
ATC code	A10BX08
PubChem	CID: 121891
DrugBank	DB01252
ChemSpider	108739
UNII	D86I0XLB13
KEGG	D01854
ChEMBL	CHEMBL471498
Chemical data
Formula	C19H25NO3
Molecular mass	315.41 g/mol
	SMILES O=C(O)[C@@H](Cc1ccccc1)CC(=O)N3C[C@H]2CCCC[C@H]2C3 ;
	InChI InChI=1S/C19H25NO3/c21-18(20-12-15-8-4-5-9-16(15)13-20)11-17(19(22)23)10-14-6-2-1-3-7-14/h1-3,6-7,15-17H,4-5,8-13H2,(H,22,23)/t15-,16+,17-/m0/s1 ; Key:WPGGHFDDFPHPOB-BBWFWOEESA-N ;
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