Microbiology,Pharmacology, and Clinical Use of Mezlocillin Sodium |
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| Authors: | Dr. Richard V. McCloskey M.D. Dr. Jack L. LeFrock M.D. Dr. Bruce R. Smith Pharm.D. Dr. George R. Aronoff M.D. |
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| Affiliation: | 1. Department of Medicine, Albert Einstein Medical Center (Daroff Division), Thomas Jefferson University, Philadelphia;2. Division of Infectious Diseases and Clinical Microbiology, Hahnemann Medical College and Hospital, Philadelphia;3. Division of Nephrology and Clinical Pharmacology, Indiana University Medical Center, Indianapolis. |
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| Abstract: | ![]()
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. |
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