The Sound of Evolution
Cilastatin
西司他丁
Mechanism of action:
Cilastatin 是一種腎臟脫氫肽酶-1 抑制劑（renal dehydropeptidase-I inhibitor），主要功能是保護亞胺培南（imipenem）等 β-內醯胺類（β-lactam）抗生素免於腎臟代謝失去活性，因此幾乎只與亞胺培南併用。脫氫肽酶-1 是位於腎臟近曲小管刷狀緣（brush border）的酵素，能水解含 β-內醯胺環的抗生素，尤其是亞胺培南。當單獨給予亞胺培南時，相當一部分會在腎臟被脫氫肽酶-1 分解失去活性。Cilastatin 能可逆性抑制脫氫肽酶-1 酵素活性，讓亞胺培南能發揮療效。
Reference(s):
1. Keynan S et al. (1995). The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterial metallo-beta-lactamase enzyme CphA. Antimicrob Agents Chemother.
2. Buckley MM et al. (1992). Imipenem/cilastatin: A reappraisal of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy. Drugs.
3. Balfour JA et al. (1996). Imipenem/cilastatin: An update of its antibacterial activity, pharmacokinetics and therapeutic efficacy in the treatment of serious infections. Drugs.