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Microbiology, Pharmacology, and Clinical Use of Mezlocillin Sodium
Author(s) -
McCloskey Richard V.,
LeFrock Jack L.,
Smith Bruce R.,
Aronoff George R.
Publication year - 1982
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1002/j.1875-9114.1982.tb03204.x
Subject(s) - mezlocillin , clinical pharmacology , pharmacology , microbiology and biotechnology , medicine , computational biology , biology , bacteria , pseudomonas aeruginosa , genetics , piperacillin
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.