シラスタチン
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/05/30 22:48:38」(JST)
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Cilastatin
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Systematic (IUPAC) name |
(Z)-7-[(2R)-2-Amino-3-hydroxy-3-oxopropyl]sulfanyl-2-{[(1S)-2,2-dimethylcyclopropanecarbonyl]amino}hept-2-enoic acid
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Clinical data |
AHFS/Drugs.com |
International Drug Names |
MedlinePlus |
a686013 |
Routes of
administration |
IV |
Identifiers |
CAS Number |
82009-34-5 Y |
ATC code |
J01DH51 (WHO) (combination with imipenem) |
PubChem |
CID 5280454 |
IUPHAR/BPS |
5166 |
DrugBank |
DB01597 Y |
ChemSpider |
4940183 Y |
UNII |
141A6AMN38 Y |
KEGG |
D07698 Y |
ChEBI |
CHEBI:3697 Y |
ChEMBL |
CHEMBL766 Y |
Chemical data |
Formula |
C16H26N2O5S |
Molar mass |
358.454 g/mol |
SMILES
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O=C(N\C(=C/CCCCSC[C@@H](C(=O)O)N)C(=O)O)[C@H]1CC1(C)C
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InChI
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InChI=1S/C16H26N2O5S/c1-16(2)8-10(16)13(19)18-12(15(22)23)6-4-3-5-7-24-9-11(17)14(20)21/h6,10-11H,3-5,7-9,17H2,1-2H3,(H,18,19)(H,20,21)(H,22,23)/b12-6-/t10-,11+/m1/s1 Y
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Key:DHSUYTOATWAVLW-WFVMDLQDSA-N Y
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(verify) |
Cilastatin is a chemical compound which inhibits the human enzyme dehydropeptidase.[1]
Dehydropeptidase is an enzyme found in the kidney and is responsible for degrading the antibiotic imipenem. Cilastatin can therefore be combined intravenously with imipenem in order to protect it from dehydropeptidase and prolong its antibacterial effect. Imipenem alone is an effective antibiotic and can be given without the cilastatin. Cilastatin itself does not have antibiotic activity although it has been proved to be active against a zinc-dependent beta-lactamase that usually confer antibiotic resistance to certain bacteria; more precisely the carbapenem family of antibiotics. This property is due to the phisico-chemical similarities between membrane dipeptidase (MDP), the compound it is usually set to target, and the bacterial metallo-beta-lactamase carried by the CphA gene[1] Therefore, Cilastatin is considered a beta-lactamase inhibitor, not an antibiotic per se.
See also
References
- ^ a b Keynan S, Hooper NM, Felici A, Amicosante G, Turner AJ (1995). "The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterial metallo-beta-lactamase enzyme CphA". Antimicrob. Agents Chemother. 39 (7): 1629–31. doi:10.1128/aac.39.7.1629. PMC 162797. PMID 7492120.
Leukotriene signaling
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Receptor
(ligands) |
BLT |
BLT1
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- Agonists: 12-HETE
- 20-Hydroxy-LTB4
- Leukotriene B4
- LY-255283
- Antagonists: 20-Carboxy-LTB4
- Amelubant
- CGS-23131 (LY-223982)
- CGS-25019C
- CP-105696
- CP-195543
- Etalocib
- LY-293111
- Moxilubant
- ONO-4057
- RG-14893
- RP-69698
- SB-209247
- SC-53228
- Ticolubant
- U-75302
- ZK-158252
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BLT2
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- Agonists: 12-HETE
- 12-HHT
- 12-HpETE
- 15-HETE
- 15-HpETE
- 20-Hydroxy-LTB4
- Leukotriene B4
- Antagonists: CP-195543
- LY-255283
- ZK-158252
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CysLT |
CysLT1
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- Agonists: Leukotriene C4
- Leukotriene D4
- Leukotriene E4
- Antagonists: Ablukast
- BAYu9773
- BAYu9916
- BAYx7195
- Cinalukast
- FPL-55712
- ICI-198615
- Iralukast
- LY-170680
- Masilukast
- MK-571
- Montelukast
- ONO-1078
- Pobilukast
- Pranlukast
- Ritolukast
- SKF-104353
- SR-2640
- Sulukast
- Tipelukast
- Tomelukast
- Verlukast
- Zafirlukast
- ZD-3523
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CysLT2
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- Agonists: Leukotriene C4
- Leukotriene D4
- Leukotriene E4
- Antagonists: BAYu9773
- BAYu9916
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CysLTE
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Enzyme
(inhibitors) |
5-Lipoxygenase |
- 2-TEDC
- Baicalein
- BW-A4C
- BW-B70C
- Caffeic acid
- CDC
- CJ-13610
- Curcumin
- Hyperforin
- Hypericum perforatum (St. John's Wort)
- Meclofenamic acid (meclofenamate)
- Minocycline
- N-Stearoyldopamine
- Timegadine
- Zileuton
- FLAP inhibitors: AM-103
- AM-679
- BAYx1005
- MK-591
- MK-886
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12-Lipoxygenase |
- 2-TEDC
- 3-Methoxytropolone
- Baicalein
- CDC
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15-Lipoxygenase |
- 2-TEDC
- CDC
- Luteolin
- PD-146176
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LTA4 hydrolase |
- Acebilustat
- Captopril
- DG-051
- Fosinoprilat
- JNJ-26993135
- SA-6541
- SC-57461A
- Ubenimex (bestatin)
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LTB4 ω-hydroxylase |
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LTC4 synthase |
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LTC4 hydrolase |
- Acivicin
- Serine-borate complex
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LTD4 hydrolase |
- Cilastatin
- Ubenimex (bestatin)
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Others |
- Precursors: Linoleic acid
- γ-Linolenic acid (gamolenic acid)
- Dihomo-γ-linolenic acid
- Diacylglycerol
- Arachidonic acid
- 5-HPETE (arachidonic acid 5-hydroperoxide)
- Leukotriene A4
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See also: Prostanoids
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UpToDate Contents
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English Journal
- Colistin-tigecycline versus colistin-imipenem-cilastatin combinations for the treatment of Acinetobacter baumannii ventilator-acquired pneumonia: a prognosis study.
- Chaari A1, Pham T2,3,4, Mnif B5, Chtara K6, Medhioub F6, Baccouche N6, Bahloul M6, Hammami A5, Bouaziz M6.
- Intensive care medicine.Intensive Care Med.2015 Nov;41(11):2018-9. doi: 10.1007/s00134-015-4010-z. Epub 2015 Aug 12.
- PMID 26264246
- Comparison of the Carba NP, Modified Carba NP, and Updated Rosco Neo-Rapid Carb Kit Tests for Carbapenemase Detection.
- AbdelGhani S1, Thomson GK2, Snyder JW3, Thomson KS4.
- Journal of clinical microbiology.J Clin Microbiol.2015 Nov;53(11):3539-42. doi: 10.1128/JCM.01631-15. Epub 2015 Aug 26.
- The accurate detection of carbapenemase-producing organisms is a major challenge for clinical laboratories. The Carba NP test is highly accurate but inconvenient, as it requires frequent preparation of fresh imipenem solution. The current study was designed to compare the Carba NP test to two altern
- PMID 26311862
- Epidemiology and risk factors of multidrug-resistant bacteria in respiratory samples after lung transplantation.
- Tebano G1, Geneve C1, Tanaka S2, Grall N3, Atchade E1, Augustin P1, Thabut G4,5, Castier Y5,6, Montravers P1,5, Desmard M1,7.
- Transplant infectious disease : an official journal of the Transplantation Society.Transpl Infect Dis.2015 Oct 11. doi: 10.1111/tid.12471. [Epub ahead of print]
- BACKGROUND: Multidrug-resistant (MDR) bacteria are a growing concern worldwide. The aim of this study was to describe the epidemiology and risk factors of MDR bacteria detected in respiratory invasive samples during hospitalization in the intensive care unit (ICU) after lung transplantation (LT).MET
- PMID 26455730
Japanese Journal
- 糖尿病性壊疽による四肢切断症例での患部検出菌と抗菌薬の感受性
- 山口 勇人,福岡 清二,中村 正則,荏原 徹,木村 聡
- 昭和学士会雑誌 74(5), 543-547, 2014
- … みると7割(17名)の症例が経過良好で退院,3割(7名)が再手術となり8%(2名)が手術以外の原因で死亡した.使用された抗菌薬はCEZ(Cefazolin)が8名と最も多く,次いでPIPC(Piperacillin)5名,IPM/CS(Imipenem/cilastatin)4名,VCM(Vancomycin)4名,MEPM(Meropenem)2名などが使われていた.術後経過不良例では当初CEZを使用した例が多く認められた.複数菌が検出された15名のうち再手術となった症例は5名であり,菌種が多いほ …
- NAID 130005056878
- 慢性的な肩関節の夜間痛に対する経動脈的微小血管塞栓療法の有効性
- 奥野 祐次
- PAIN RESEARCH 29(4), 233-241, 2014
- … We hypothesized that abnormal neovessels also play an important role in nighttime shoulder pain with other conditions as well as adhesive capsulitis and that TAME can relieve pain. Material and Methods: TAME using imipenem ⁄ cilastatin sodium as an embolic agent proceeded to seventeen shoulders in sixteen patients, including adhesive capsulitis (n=6), subacromial impingement syndrome (n=7), rotator cuff tear without surgical indication (n=2), stiff shoulder (n=1), and chronic pain post scapula fracture (n=1). …
- NAID 130004839647
- Lung Nocardia elegans Infection Diagnosed on Matrix-assisted Laser Desorption Ionization-time of Flight Mass Spectrometry (MALDI-TOF MS)
- , , , , , , ,
- Internal Medicine 53(18), 2111-2113, 2014
- … The patient recovered following treatment with imipenem/cilastatin and amikacin. …
- NAID 130004687653
Related Pictures
★リンクテーブル★
[★]
- 英
- cilastatin
- 化
- シラスタチンナトリウム cilastatin sodium
- 商
- イミスタン、イミペナーム、インダスト、チエクール、チエナム、チエペネム
- ジヒドロペプチダーゼ1阻害薬、イミペネム作用増強の合剤成分
[★]
シラスタチンナトリウム
- 関
- cilastatin