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Microbiology, Pharmacology, and Clinical Use of Mezlocillin Sodium

1982; Wiley; Volume: 2; Issue: 6 Linguagem: Inglês

10.1002/j.1875-9114.1982.tb03204.x

1875-9114

Richard V. McCloskey, Jack L. LeFrock, Bruce R. Smith, George R. Aronoff,

Plant chemical constituents analysis

The acylureido penicillin mezlocillin is active against gram‐positive, gram‐negative, and anaerobic bacteria. It easily penetrates the outer membrane of gram‐negative bacteria, and it has a strong affinity for penicillin binding protein 3. Its stability to 3‐lactamases is weak. Mezlocillin is synergistic when given in combination with aminoglycoside antibiotics. In pharmacokinetic studies mezlocillin conforms to a two compartment open model; its pharmacokinetic properties are dose‐dependent. The half‐life of the drug is about 1 hour after intravenous injection and 1.5 hours after intramuscular injection. Protein binding ranges from 16 to 42%, and 55% of a dose is excreted in the urine. Biliary excretion ranges from 0.5 to 25%. Clinical trial cure rates were as follows: bacteremia (78%), respiratory tract (62%), urinary tract (81%), gynecological (86%), bone and joint (55%), intraabdominal (67%) and skin and soft tissue (59%). The frequency of adverse reactions was 7.7%. Interstitial nephritis, CNS toxicity, and bleeding have not been reported.