Sulbactam

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Sulbactam
Sulbactam.svg
Sulbactam ball-and-stick.png
Clinical data
AHFS/Drugs.comInternational Drug Names
MedlinePlusa693021
Routes of
administration		Injection
ATC code
Legal status
Legal status
  • UK: POM (Prescription only)
Pharmacokinetic data
Protein binding29%
Elimination half-life0.65–1.20 hrs
ExcretionMainly kidneys (41–66% within 8 hrs)
Identifiers
  • (2S,5R)-3,3-Dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 4,4-dioxide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.063.506 Edit this at Wikidata
Chemical and physical data
FormulaC8H11NO5S
Molar mass233.24 g·mol−1
3D model (JSmol)
Melting point148 to 151 °C (298 to 304 °F)
  • O=S2(=O)C([C@@H](N1C(=O)C[C@H]12)C(=O)O)(C)C
  • 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 checkY
  • Key:FKENQMMABCRJMK-RITPCOANSA-N checkY
  

Sulbactam is a β-lactamase inhibitor. This drug is given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys the antibiotics.[1]

It was patented in 1977 and approved for medical use in 1986.[2]

Medical uses[]

Sulbactam is able to inhibit the most common forms of β-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 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.

The combination cefoperazone/sulbactam (Sulperazon) is available in many countries.[3]

Recently, its use in treating Acinetobacter sepsis is receiving renewed interest.

Mechanism[]

Sulbactam is an irreversible inhibitor of β-lactamase; it binds to the enzyme and does not allow it to degrade the antibiotic.

See also[]

References[]

  1. ^ 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.
  2. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 492. ISBN 9783527607495.
  3. ^ "Sulperazon". drugs.com.

Further reading[]

  • 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.


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