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外観
白色～ほとんど白色粉末～結晶
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解説
スルバクタム，penicillanic acid sulfone．C8H11NO5S(233.24)．化学的に全合成されたβ-ラクタマーゼ阻害剤．白色の結晶．分解点148 ℃．[α]D20"＋251°(pH 5)．水に可溶．一般に，β-ラクタム抗生物質と併用される．肺炎，膀胱炎，腹膜炎治療剤として使用される．また，細菌細胞壁の合成阻害にも用いられる．
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用途
スルバクタム(Sulbactam)は、β-ラクタマーゼ阻害剤である。β-ラクタム系抗生物質とともに投与され、細菌が生産し、抗生物質を分解してしまうβ-ラクタマーゼの働きを阻害する。
スルバクタムは、一般的な形の大部分のβ-ラクタマーゼを阻害できるが、AmpCセファロスポリナーゼとは相互作用できない。そのため、しばしばこの遺伝子を発現させる緑膿菌、シトロバクター属、エンテロバクター属、セラチア属等にはほとんど効果がない。
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効能
抗生物質, 細胞壁合成阻害薬, ベータラクタマーゼ阻害薬, 共力薬 (ペニシリン/セファロスポリン)
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説明
Sulbactam is prepared by partial chemical synthesis from
penicillins. The oxidation of the sulfur atom to a sulfone greatly enhances the potency of sulbactam. The
combination of sulbactam and ampicillin (Unasyn) is now clinically popular.
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使用
Sulbactam sodium is a semi-synthetic penem antibiotic formed by the oxidation of penicillanic acid to its sulfone and was invented by Barth at Pfizer in 1978. Sulbactam sodium is a weak antibiotic but its action as an irreversible inhibitor of β-lactamase is exploited to block the degradation of other penicillin derivatives. Sulbactam acts as a synergist with cephalosporins and penicillins against Gram positive bacteria and is used commercially in combination with ampicillin.
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抗菌性
Sulbactam has very weak antimicrobial activity against most
bacteria. Its only notable activity is against N. gonorrhoeae,
N. meningitidis and Acinetobacter baumannii.
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臨床応用
Sulbactam is penicillanic acid sulfone or 1,1-dioxopenicillanicacid. This synthetic penicillin derivative is a potent inhibitorof S. aureus β-lactamase as well as many β-lactamaseselaborated by Gram-negative bacilli. Sulbactam has weak intrinsicantibacterial activity but potentiates the activity ofampicillin and carbenicillin against β-lactamase–producingS. aureus and members of the Enterobacteriaceae family. Itdoes not, however, synergize with either carbenicillin or ticarcillinagainst P. aeruginosa strains resistant to these agents.Failure of sulbactam to penetrate the cell envelope is a possibleexplanation for the lack of synergy.
Fixed-dose combinations of ampicillin sodium and sulbactamsodium, marketed under the trade name Unasyn assterile powders for injection, have been approved for use inthe United States. These combinations are recommended forthe treatment of skin, tissue, intra-abdominal, and gynecologicalinfections caused by β-lactamase–producing strainsof S. aureus, E. coli, Klebsiella spp., P. mirabilis, B. fragilis,and Enterobacter and Acinetobacter spp.
