スルバクタム, SBT
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/06/10 12:59:32」(JST)
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Sulbactam
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Systematic (IUPAC) name |
(2S,5R)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 4,4-dioxide |
Clinical data |
AHFS/Drugs.com |
International Drug Names |
MedlinePlus |
a693021 |
Pregnancy cat. |
? |
Legal status |
POM (UK) |
Routes |
Injection |
Pharmacokinetic data |
Bioavailability |
1 |
Excretion |
Kidneys? |
Identifiers |
CAS number |
68373-14-8 Y |
ATC code |
J01CG01 |
PubChem |
CID 130313 |
ChemSpider |
115306 Y |
UNII |
S4TF6I2330 Y |
KEGG |
D08533 Y |
ChEBI |
CHEBI:9321 Y |
ChEMBL |
CHEMBL403 Y |
Chemical data |
Formula |
C8H11NO5S |
Mol. mass |
233.243 g/mol |
SMILES
- O=S2(=O)C([C@@H](N1C(=O)C[C@H]12)C(=O)O)(C)C
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InChI
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InChI=1S/C8H11NO5S/c1-8(2)6(7(11)12)9-4(10)3-5(9)15(8,13)14/h5-6H,3H2,1-2H3,(H,11,12)/t5-,6+/m1/s1 Y
Key:FKENQMMABCRJMK-RITPCOANSA-N Y
|
Y (what is this?) (verify)
|
Sulbactam is a beta-lactamase inhibitor. This molecule is given in combination with beta-lactam antibiotics to inhibit beta-lactamase, an enzyme produced by bacteria that destroys the antibiotics. [1]
Contents
- 1 Mechanism
- 2 Uses
- 3 See also
- 4 References
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Mechanism[edit]
Sulbactam is an irreversible inhibitor of beta-lactamase; it binds the enzyme and does not allow it to interact with the antibiotic.
Uses[edit]
Sulbactam is able to inhibit the most common forms of beta-lactamase but is not able to interact with the ampC cephalosporinase. Thus, it confers little protection against bacteria such as Pseudomonas aeruginosa, Citrobacter, Enterobacter, and Serratia, which often express this gene.
In the United States, sulbactam is combined to form cefoperazone/sulbactam and ampicillin/sulbactam. It does possess some antibacterial activity when administered alone, but it is too weak to have any clinical importance. Its use in the UK is restricted to hospitals.
Recently its use in treating Acinetebacter septicemia is receiving renewed interest,
See also[edit]
Tazobactam
References[edit]
- ^ Totir MA, Helfand MS, Carey MP, et al. (August 2007). "Sulbactam forms only minimal amounts of irreversible acrylate-enzyme with SHV-1 beta-lactamase". Biochemistry 46 (31): 8980–7. doi:10.1021/bi7006146. PMC 2596720. PMID 17630699.
- Singh GS (January 2004). "Beta-lactams in the new millennium. Part-II: cephems, oxacephems, penams and sulbactam". Mini Rev Med Chem 4 (1): 93–109. doi:10.2174/1389557043487547. PMID 14754446.
Antibacterials: cell envelope antibiotics (J01C-J01D)
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Intracellular |
- inhibit peptidoglycan subunit synthesis and transport: NAM synthesis inhibition (Fosfomycin)
- DADAL/AR inhibitors (Cycloserine)
- bactoprenol inhibitors (Bacitracin)
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Glycopeptide |
- inhibit PG chain elongation: Vancomycin# (Oritavancin
- Telavancin)
- Teicoplanin (Dalbavancin)
- Ramoplanin
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β-lactams/
(inhibit PBP
cross-links) |
Penicillins
(penams)
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Extended sp.
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- aminopenicillins: Amoxicillin#
- Ampicillin# (Pivampicillin
- Hetacillin
- Bacampicillin
- Metampicillin
- Talampicillin)
- Epicillin
- carboxypenicillins: Carbenicillin (Carindacillin)
- Ticarcillin
- Temocillin
- ureidopenicillins: Azlocillin
- Piperacillin
- Mezlocillin
- other: Mecillinam (Pivmecillinam)
- Sulbenicillin
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Narrow sp.
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β-lactamase sensitive
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- Benzylpenicillin (G)#: Clometocillin
- Benzathine benzylpenicillin#
- Procaine benzylpenicillin#
- Azidocillin
- Penamecillin
- Phenoxymethylpenicillin (V)#: Propicillin
- Benzathine phenoxymethylpenicillin
- Pheneticillin
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β-lactamase resistant
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- Cloxacillin# (Dicloxacillin
- Flucloxacillin)
- Oxacillin
- Meticillin
- Nafcillin
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Penems
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Carbapenems
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- Biapenem
- Ertapenem
- antipseudomonal (Doripenem
- Imipenem
- Meropenem)
- Panipenem
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Cephalosporins/Cephamycins
(cephems)
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1st (PEcK)
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- Cefazolin#
- Cefacetrile
- Cefadroxil
- Cefalexin
- Cefaloglycin
- Cefalonium
- Cefaloridine
- Cefalotin
- Cefapirin
- Cefatrizine
- Cefazedone
- Cefazaflur
- Cefradine
- Cefroxadine
- Ceftezole
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2nd (HEN)
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- Cefaclor
- Cefamandole
- Cefminox
- Cefonicid
- Ceforanide
- Cefotiam
- Cefprozil
- Cefbuperazone
- Cefuroxime
- Cefuzonam
- cephamycin (Cefoxitin
- Cefotetan
- Cefmetazole)
- carbacephem (Loracarbef)
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3rd
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- Cefixime#
- Ceftriaxone#
- antipseudomonal (Ceftazidime#
- Cefoperazone)
- Cefcapene
- Cefdaloxime
- Cefdinir
- Cefditoren
- Cefetamet
- Cefmenoxime
- Cefodizime
- Cefotaxime
- Cefpimizole
- Cefpiramide
- Cefpodoxime
- Cefsulodin
- Cefteram
- Ceftibuten
- Ceftiolene
- Ceftizoxime
- oxacephem (Flomoxef
- Latamoxef ‡)
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4th (antips-)
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- Cefepime
- Cefozopran
- Cefpirome
- Cefquinome
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5th
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- Ceftobiprole
- Ceftaroline fosamil
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Veterinary
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- Ceftiofur
- Cefquinome
- Cefovecin
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Monobactams
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- Aztreonam
- Tigemonam
- Carumonam
- Nocardicin A
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β-lactamase inh.
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- penam (Sulbactam
- Tazobactam)
- clavam (Clavulanic acid)
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Combinations
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- Amoxicillin/clavulanic acid#
- Imipenem/cilastatin#
- Ampicillin/flucloxacillin
- Ampicillin/sulbactam (Sultamicillin)
- Piperacillin/tazobactam
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Other |
- polymyxins/detergent (Colistin
- Polymyxin B)
- depolarizing (Daptomycin)
- hydrolyze NAM-NAG (Lysozyme)
- Gramicidin
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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gr+f/gr+a (t)/gr-p (c)/gr-o
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drug (J1p, w, n, m, vacc)
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UpToDate Contents
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English Journal
- In Vitro Synergistic Effects of Antimicrobial Combinations on Extensively Drug-Resistant Pseudomonas aeruginosa and Acinetobacter baumannii Isolates.
- Lee H1, Roh KH2, Hong SG3, Shin HB4, Jeong SH5, Song W6, Uh Y7, Yong D8, Lee K9.
- Annals of laboratory medicine.Ann Lab Med.2016 Mar;36(2):138-44. doi: 10.3343/alm.2016.36.2.138.
- BACKGROUND: Extensively drug-resistant (XDR) Pseudomonas aeruginosa and Acinetobacter baumannii are a threat to hospitalized patients. We evaluated the effects of antimicrobial combinations on XDR P. aeruginosa and A. baumannii isolates.METHODS: P. aeruginosa and A. baumannii isolates, which were re
- PMID 26709261
- Spectrum and treatment of anaerobic infections.
- Brook I1.
- Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy.J Infect Chemother.2016 Jan;22(1):1-13. doi: 10.1016/j.jiac.2015.10.010. Epub 2015 Nov 24.
- Anaerobes are the most predominant components of the normal human skin and mucous membranes bacterial flora, and are a frequent cause of endogenous bacterial infections. Anaerobic infections can occur in all body locations: the central nervous system, oral cavity, head and neck, chest, abdomen, pelv
- PMID 26620376
- "Study of Common Bacterial and Fungal Pathogens in Children with Hematological Malignancies during Febrile Neutropenia: Single Center Egyptian Study".
- Hagag AA1.
- Infectious disorders drug targets.Infect Disord Drug Targets.2015 Dec 30. [Epub ahead of print]
- BACKGROUND: Infection 'is a common complication in children with hematological malignancies' during febrile neutropenia.AIM OF THE WORK: The aim of this study was to' evaluate common bacterial and fungal pathogens in children with hematological malignancies during febrile neutropenia in single cente
- PMID 26715443
Japanese Journal
- クリンダマイシン, 穿刺排膿による扁桃周囲膿瘍治療 : 広域抗菌剤や多剤併用は必要なのか?
- 竹中 幸則,武田 和也,喜井 正士,橋本 典子,猪原 秀典
- 耳鼻咽喉科臨床 104(1), 67-73, 2011-01-01
- … Antibiotics used were clindamycin, sulbactam/cefoperazon, cefepime, and carbapenems. …
- NAID 10027626338
- Antimicrobial Susceptibility of Bordetella bronchiseptica Isolates from Pigs with Respiratory Diseases on Farms in China
- ZHAO Zhanqin,XUE Yun,WANG Chen,DING Ke,WU Bin,HE Qigai,CHENG Xiangchao,CHEN Huanchun
- Journal of Veterinary Medical Science 73(1), 103-106, 2011
- … bronchiseptica isolates were sensitive to polymyxin B and cefoperazone/sulbactam; … 81.0%), ampicillin/sulbactam (127/163; …
- NAID 40018701690
Related Links
- Sulbactam / Ampicillin [SBT/ABPC] スルバクタム/アンピシリン, ペニシリン系 β-ラクタマーゼ阻害剤配合 1. 商品名 先発品 ユナシン-S静注用0.75g/ユナシン-S静注用1.5g 【ファイザー】 ユナシン-Sキット静注用1.5g/ユナシン-Sキット静 ...
- Sulbactam / Cefoperazone [SBT/CPZ] スルバクタム/セフォペラゾン, セフェム系(ureid型 MTT基 β-ラクタマーゼ阻害剤配合) 1. 商品名 先発品 スルペラゾン静注用0.5g/スルペラゾン静注用1g/スルペラゾンキット静注用1g 【ファイザー】 ...
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スルバクタム, sulbactam
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