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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/06/26 01:50:54」(JST)
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Nateglinide
|
Systematic (IUPAC) name |
(2R)-2-({[trans-4-(1-methylethyl)cyclohexyl]carbonyl}amino)-3-phenylpropanoic acid |
Clinical data |
Trade names |
Starlix |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a699057 |
Licence data |
EMA:Link, US FDA:link |
Legal status
|
- UK: Prescription-only (POM)
- US: ℞-only
|
Routes of
administration
|
Oral |
Pharmacokinetic data |
Protein binding
|
98% |
Biological half-life
|
1.5 hours |
Identifiers |
CAS Registry Number
|
105816-04-4 Y |
ATC code
|
A10BX03 |
PubChem |
CID: 60026 |
IUPHAR/BPS |
6833 |
DrugBank |
DB00731 Y |
ChemSpider |
10482084 Y |
UNII |
41X3PWK4O2 Y |
KEGG |
D01111 N |
ChEBI |
CHEBI:31897 N |
ChEMBL |
CHEMBL286559 N |
Chemical data |
Formula |
C19H27NO3 |
Molecular mass
|
317.423 g/mol |
SMILES
- O=C(N[C@H](Cc1ccccc1)C(O)=O)[C@H]2CC[C@@H](CC2)C(C)C
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InChI
-
InChI=1S/C19H27NO3/c1-13(2)15-8-10-16(11-9-15)18(21)20-17(19(22)23)12-14-6-4-3-5-7-14/h3-7,13,15-17H,8-12H2,1-2H3,(H,20,21)(H,22,23)/t15-,16-,17-/m1/s1 Y
Key:OELFLUMRDSZNSF-BRWVUGGUSA-N Y
|
N (what is this?) (verify) |
Nateglinide (INN, trade name Starlix) is a drug for the treatment of type 2 diabetes. Nateglinide was developed by Ajinomoto, a Japanese company and sold by the Swiss pharmaceutical company Novartis.
Nateglinide belongs to the meglitinide class of blood glucose-lowering drugs.
Contents
- 1 Pharmacology
- 2 Contraindications
- 3 Comparisons with other drugs for type 2 diabetes
- 4 Dosage
- 5 See also
- 6 References
- 7 External links
Pharmacology
Nateglinide lowers blood glucose by stimulating the release of insulin from the pancreas. It achieves this by closing ATP-dependent potassium channels in the membrane of the β cells. This depolarizes the β cells and causes voltage-gated calcium channels to open. The resulting calcium influx induces fusion of insulin-containing vesicles with the cell membrane, and insulin secretion occurs.
Contraindications
Nateglinide is contraindicated in patients who:
- have known hypersensitivity to the compound or any ingredient in the formulation.
- are affected with type 1 (namely insulin-dependent) diabetes mellitus.
- are in diabetic ketoacidosis.
Comparisons with other drugs for type 2 diabetes
A study funded by Novo Nordisk, the U.S. distributor for Repaglinide, compared their product with Nateglinide in "A randomized, parallel-group, open-label, multicenter 16-week clinical trial".[1] They concluded that the two were similar, but "repaglinide monotherapy was significantly more effective than nateglinide monotherapy in reducing HbA1c and FPG values after 16 weeks of therapy."
Dosage
Nateglinide is delivered in 60 mg & 120 mg tablet form.
See also
References
- ^ Rosenstock, Julio Rosenstock; Hassman, David R.; Madder, Robert D.; Brazinsky, Shari A.; Farrell, James; Khutoryansky, Naum; Hale, Paula M. (June 2004), "Repaglinide Versus Nateglinide Monotherapy: A randomized, multicenter study", Diabetes Care (American Diabetes Association) 27 (6): 1265–1270, doi:10.2337/diacare.27.6.1265, retrieved 2014-11-20
External links
- Starlix - website of the manufacturer.
- How Nateglinide Works - website of the manufacturer.
Oral anti-diabetic drugs and Insulin analogs (A10)
|
|
Insulin |
Sensitizers |
Biguanides |
- Metformin#
- Buformin‡
- Phenformin‡
|
|
TZDs/"glitazones" (PPAR) |
- Pioglitazone
- Rivoglitazone†
- Rosiglitazone
- Troglitazone‡
|
|
Dual PPAR agonists |
- Aleglitazar†
- Muraglitazar§
- Saroglitazar
- Tesaglitazar§
|
|
|
Secretagogues |
K+ ATP |
Sulfonylureas |
- 1st generation: Acetohexamide
- Carbutamide
- Chlorpropamide
- Metahexamide
- Tolbutamide
- Tolazamide
- 2nd generation: Glibenclamide (Glyburide)#
- Glibornuride
- Glipizide
- Gliquidone
- Glisoxepide
- Glyclopyramide
- Glimepiride
- Gliclazide
|
|
Meglitinides/"glinides" |
- Nateglinide
- Repaglinide
- Mitiglinide
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|
|
GLP-1 agonists |
- Exenatide
- Liraglutide
- Taspoglutide†
- Albiglutide†
- Lixisenatide
- Dulaglutide
- Semaglutide
|
|
DPP-4 inhibitors |
- Alogliptin
- Anagliptin
- Gemigliptin
- Linagliptin
- Saxagliptin
- Sitagliptin
- Teneligliptin
- Vildagliptin
|
|
GPR40 Free fatty acid receptor 1 |
|
|
|
Analogs/other insulins |
- fast-acting (Insulin lispro
- Insulin aspart
- Insulin glulisine)
- short-acting (Regular insulin)
- long-acting (Insulin glargine
- Insulin detemir
- NPH insulin)
- ultra-long-acting (Insulin degludec†)
- inhalable Exubera
- Afrezza
|
|
|
Other |
Alpha-glucosidase inhibitors |
- Acarbose
- Miglitol
- Voglibose
|
|
Amylin analog |
|
|
Gliflozins |
- Canagliflozin
- Dapagliflozin
- Empagliflozin†
- Remogliflozin§
- Sergliflozin§
- Tofogliflozin†
|
|
Other |
- Bromocriptine
- Benfluorex‡
- Tolrestat‡
|
|
|
-
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
Index of hormones
|
|
Description |
- Glands
- Hormones
- thyroid
- mineralocorticoids
- Physiology
- Development
|
|
Disease |
- Diabetes
- Congenital
- Neoplasms and cancer
- Other
- Symptoms and signs
|
|
Treatment |
- Procedures
- Drugs
- calcium balance
- corticosteroids
- oral hypoglycemics
- pituitary and hypothalamic
- thyroid
|
|
|
UpToDate Contents
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English Journal
- Rapid, sensitive and selective HPLC-MS/MS method for the quantification of topically applied besifloxacin in rabbit plasma and ocular tissues: Application to a pharmacokinetic study.
- Gu XF1, Mao BY2, Xia M3, Yang Y3, Zhang JL3, Yang DS3, Wu WX3, Du YX4, Di B5, Su MX6.
- Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2016 Jan 5;117:37-46. doi: 10.1016/j.jpba.2015.08.023. Epub 2015 Aug 22.
- Besifloxacin is a fourth-generation broad-spectrum fluoroquinolone registered for the topical treatment of bacterial conjunctivitis. In this study, a rapid, sensitive and selective liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed for quantification of besifloxacin in ra
- PMID 26340560
- Effects of nateglinide and rosiglitazone on pancreatic alpha- and beta-cells, GLP-1 secretion and inflammatory markers in patients with type 2 diabetes: randomized crossover clinical study.
- Tostes GC1, Cunha MR1, Fukui RT1, Correia MR1, Rocha DM1, Dos Santos RF1, da Silva ME1.
- Diabetology & metabolic syndrome.Diabetol Metab Syndr.2016 Jan 4;8:1. doi: 10.1186/s13098-015-0120-6. eCollection 2016.
- BACKGROUND: To compare the effects of nateglinide and rosiglitazone on inflammatory markers, GLP-1 levels and metabolic profile in patients with type 2 diabetes (DM2).METHODS: A prospective study was performed in 20 patients with DM2, mean age 51.82 ± 8.05 years, previously treated with dietary
- PMID 26734075
- Preparation of polyclonal antibodies for nateglinide (NTG) and development of a sensitive chemiluminescent immunoassay to detect NTG in tablets and serum.
- Zheng L1, Wang J1, Zhang J2, Song Z1, Dong Y1, Wang Y1, Tong Z2, Deng C3, Yin Y1, Meng M4, Xi R1.
- Talanta.Talanta.2016 Jan 1;146:483-9. doi: 10.1016/j.talanta.2015.09.008. Epub 2015 Sep 9.
- In this study, we prepared polyclonal antibodies against anti-diabetic drug nateglinide (NTG), and established a sensitive chemiluminescent immunoassay (CLIA) to detect NTG in tablets and serum. Two kinds of immunogens were synthesized using ethylcarbodiimide (EDC)/hydroxysuccinimide (NHS) and carbo
- PMID 26695294
Japanese Journal
- 慢性移植片対宿主病による皮膚障害に対してインスリン皮下注射実施に工夫を要したステロイド糖尿病の1例
- Complex Formation with Layered Double Hydroxides for the Remediation of Hygroscopicity
- 多疾患併発の高齢者に対する多剤併用薬物療法中に出現した薬剤性肝障害の一例
Related Links
- The latest Tweets from nateglinide (@nateglinide). 糖尿病専門医。2009年から英語圏でリサーチフェローしてます。. Canada, Japan, UK ... 昨春、若手研究者から「笹井先生には逆らえないし、鳥居さんから直接意見してほしい」と言われた ...
- Sigma-Aldrich offers Sigma-N3538, Nateglinide for your research needs. Find product specific information including CAS, MSDS, protocols and references. ... Biochem/physiol Actions Nateglinide is a Kir6.2/SUR1 channel ...
Related Pictures
★リンクテーブル★
[★]
- 英
- nateglinide
- 商
- スターシス、ファスティック
- 関
- 糖尿病治療薬、薬理学、グリニド系薬
概念
利点
- 食後高血糖を改善する (α-GIより強力)
- インスリンの遅延過剰反応を抑制する
- 一日の血糖変動幅が小さい
- 低血糖を比較的起こしにくい (GOO.1638)
- 軽症糖尿病に使いやすい
- 肥満患者にも使える
作用機序