Sulbaktam

Sulbaktam
Nama sistematis (IUPAC)
(2S,5R)-3,3-Dimetil-7-okso-4-tia-1-azabisiklo[3.2.0]heptana-2-asam karboksilat 4,4-dioksida
Data klinis
AHFS/Drugs.com International Drug Names
MedlinePlus a693021
Kat. kehamilan ?
Status hukum POM (UK)
Rute Intravena, intramuskular
Data farmakokinetik
Ikatan protein 29%
Waktu paruh 0,65–1,20 jam
Ekskresi Terutama ginjal (41–66% dalam 8 jam)
Pengenal
Nomor CAS 68373-14-8 YaY
Kode ATC J01CG01
PubChem CID 130313
ChemSpider 115306 YaY
UNII S4TF6I2330 YaY
KEGG D08533 YaY
ChEBI CHEBI:9321 YaY
ChEMBL CHEMBL403 YaY
Data kimia
Rumus C8H11NO5S 
SMILES eMolecules & PubChem
  • 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 YaY
    Key:FKENQMMABCRJMK-RITPCOANSA-N YaY

Data fisik
Titik lebur 148–151 °C (298–304 °F)

Sulbaktam adalah inhibitor beta-laktamase. Obat ini diberikan dalam kombinasi dengan antibiotik beta-laktam untuk menghambat β-laktamase, enzim yang diproduksi oleh bakteri yang menghancurkan antibiotik.[1] Obat ini dipatenkan pada tahun 1977 dan disetujui untuk penggunaan medis pada tahun 1986.[2]

Mekanisme kerja

Sulbaktam terutama digunakan sebagai penghambat bunuh diri β-laktamase, melindungi beta-laktam yang lebih kuat seperti ampisilin.[3] Sulbaktam sendiri mengandung cincin beta-laktam, dan memiliki aktivitas antibakteri yang lemah dengan menghambat protein pengikat penisilin (PBP) 1 dan 3, tetapi tidak menghambat 2.[4]

Kombinasi

Kombinasi ampisilin/sulbaktam tersedia di Amerika Serikat.[5]

Kombinasi sefoperazon/sulbaktam (Sulperazon) tersedia di banyak negara.[6]

Kombinasi sulbaktam/durlobaktam yang dikemas bersama telah disetujui untuk penggunaan medis di Amerika Serikat pada Mei 2023.[7]

Referensi

  1. ^ Totir MA, Helfand MS, Carey MP, Sheri A, Buynak JD, Bonomo RA, Carey PR (August 2007). "Sulbactam forms only minimal amounts of irreversible acrylate-enzyme with SHV-1 beta-lactamase". Biochemistry. 46 (31): 8980–8987. doi:10.1021/bi7006146. PMC 2596720alt=Dapat diakses gratis. PMID 17630699. 
  2. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery (dalam bahasa Inggris). John Wiley & Sons. hlm. 492. ISBN 9783527607495. 
  3. ^ Crass RL, Pai MP (February 2019). "Pharmacokinetics and Pharmacodynamics of β-Lactamase Inhibitors". Pharmacotherapy. 39 (2): 182–195. doi:10.1002/phar.2210. PMID 30589457. 
  4. ^ Penwell WF, Shapiro AB, Giacobbe RA, Gu RF, Gao N, Thresher J, et al. (March 2015). "Molecular mechanisms of sulbactam antibacterial activity and resistance determinants in Acinetobacter baumannii". Antimicrobial Agents and Chemotherapy. 59 (3): 1680–1689. doi:10.1128/AAC.04808-14. PMC 4325763alt=Dapat diakses gratis. PMID 25561334. 
  5. ^ "Unasyn- ampicillin sodium and sulbactam sodium injection, powder, for solution". DailyMed. U.S. National Library of Medicine. 29 March 2023. Diakses tanggal 25 May 2023. 
  6. ^ "Sulperazon". drugs.com. 
  7. ^ "FDA Approves New Treatment for Pneumonia Caused by Certain Difficult-to-Treat Bacteria". U.S. Food and Drug Administration (Siaran pers). 24 May 2023. Diakses tanggal 24 May 2023. 

Bacaan lebih lanjut

  • Singh GS (January 2004). "Beta-lactams in the new millennium. Part-II: cephems, oxacephems, penams and sulbactam". Mini Reviews in Medicinal Chemistry. 4 (1): 93–109. doi:10.2174/1389557043487547. PMID 14754446. 

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