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Drug and Therapeutics Bulletin Dec 1980
Topics: Humans; Mezlocillin; Penicillins
PubMed: 6450670
DOI: No ID Found -
Reviews of Infectious Diseases 1984The new acylampicillin derivatives azlocillin, mezlocillin, and piperacillin have an increased activity against many gram-negative bacilli, especially Klebsiella... (Review)
Review
The new acylampicillin derivatives azlocillin, mezlocillin, and piperacillin have an increased activity against many gram-negative bacilli, especially Klebsiella pneumoniae, Serratia marcescens, and Pseudomonas aeruginosa, when compared with the carboxypenicillins carbenicillin and ticarcillin. The new penicillins show synergistic activity in combination with aminoglycosides but, when combined with other beta-lactams, may be synergistic (piperacillin and moxalactam; mezlocillin and cefoperazone), indifferent, or antagonistic (azlocillin, mezlocillin, or piperacillin and cefoxitin or cefamandole). The in vitro activity of these agents, either alone or in combination, appears to correlate with in vivo efficacy in animal models. The new penicillins are clinically effective for a very broad range of infections, including life-threatening nosocomial infections. Adverse effects with these, as with other semisynthetic penicillins, are minimal. Attention must be paid to the potential for infection by naturally resistant, gram-negative bacilli such as beta-lactamase-producing Escherichia coli and for the emergence of resistance during therapy. The granulocytopenic patient should receive these agents only in conjunction with another agent, such as an aminoglycoside; this combination will often result in a synergistic effect when tested in vitro. The carboxypenicillins and the newer penicillins have substantial similarities, and prospective, comparative studies have so far failed to demonstrate significant clinical superiority. However, the increased activity of the acylampicillins may be advantageous for the treatment of infections due to K. pneumoniae and P. aeruginosa.
Topics: Agranulocytosis; Animals; Azlocillin; Bacteria; Bacterial Infections; Cefoxitin; Cystic Fibrosis; Disease Models, Animal; Humans; Kinetics; Mezlocillin; Neoplasms; Penicillins; Piperacillin
PubMed: 6369480
DOI: 10.1093/clinids/6.1.13 -
Annals of Internal Medicine Oct 1993
Topics: Aged; Humans; Male; Mezlocillin; Thrombocytopenia
PubMed: 8379614
DOI: 10.7326/0003-4819-119-8-199310150-00025 -
The Journal of Antimicrobial... Nov 2022
Topics: Infant; Infant, Newborn; Humans; Mezlocillin; Bacterial Infections; Kinetics
PubMed: 36205004
DOI: 10.1093/jac/dkac335 -
The Journal of Antimicrobial... Nov 2022
Topics: Infant; Infant, Newborn; Humans; Mezlocillin; Bacterial Infections; Kinetics
PubMed: 36101504
DOI: 10.1093/jac/dkac305 -
The Journal of Antimicrobial... Jul 2022Mezlocillin is used in the treatment of neonatal infectious diseases. However, due to the absence of population pharmacokinetic studies in neonates and young infants,...
OBJECTIVES
Mezlocillin is used in the treatment of neonatal infectious diseases. However, due to the absence of population pharmacokinetic studies in neonates and young infants, dosing regimens differ considerably in clinical practice. Hence, this study aimed to describe the pharmacokinetic characteristics of mezlocillin in neonates and young infants, and propose the optimal dosing regimen based on the population pharmacokinetic model of mezlocillin.
METHODS
A prospective, open-label pharmacokinetic study of mezlocillin was carried out in newborns. Blood samples were collected using an opportunistic sampling method. HPLC was used to measure the plasma drug concentrations. A population pharmacokinetic model was developed using NONMEM software.
RESULTS
Ninety-five blood samples from 48 neonates and young infants were included. The ranges of postmenstrual age and birth weight were 29-40 weeks and 1200-4000 g, respectively, including term and preterm infants. A two-compartment model with first-order elimination was developed to describe the population pharmacokinetics of mezlocillin. Postmenstrual age, current weight and serum creatinine concentration were the most important covariates. Monte Carlo simulation results indicated that the current dose of 50 mg/kg q12h resulted in 89.2% of patients achieving the therapeutic target, when the MIC of 4 mg/L was used as the breakpoint. When increasing the dosing frequency to q8h, a dose of 20 mg/kg resulted in 74.3% of patients achieving the therapeutic target.
CONCLUSIONS
A population pharmacokinetic model of mezlocillin in neonates and young infants was established. Optimal dosing regimens based on this model were provided for use in neonatal infections.
Topics: Anti-Bacterial Agents; Creatinine; Humans; Infant; Infant, Newborn; Infant, Premature; Mezlocillin; Microbial Sensitivity Tests; Monte Carlo Method; Prospective Studies
PubMed: 35662337
DOI: 10.1093/jac/dkac176 -
Clinical Pharmacology and Therapeutics Oct 1980Mezlocillin kinetics was examined in 28 adult subjects with varying renal function. Mezlocillin 3 gm, was infused over 30 min. Mean peak plasma concentrations ranged...
Mezlocillin kinetics was examined in 28 adult subjects with varying renal function. Mezlocillin 3 gm, was infused over 30 min. Mean peak plasma concentrations ranged from 204 to 253 mg/I. When the area under the curve (AUC) was plotted against creatinine clearance (CCr), the relationship found was expressed by the equation AUC = 656e(-0.01)(CCr). From this relationship a dosage nonogram was derived describing a power function with the following equaton: Dose fraction = 1.32--e(-0.01)(CCr). Therapeutic guidelines are suggested.
Topics: Adult; Aged; Dose-Response Relationship, Drug; Half-Life; Humans; Kidney Diseases; Kinetics; Mezlocillin; Middle Aged; Penicillins; Regression Analysis
PubMed: 6447570
DOI: 10.1038/clpt.1980.197 -
The American Journal of Pediatric... 1992
Topics: Adolescent; Bone Neoplasms; Drug Interactions; Female; Humans; Lung Neoplasms; Metabolic Clearance Rate; Methotrexate; Mezlocillin
PubMed: 1550270
DOI: No ID Found -
Journal of Pharmaceutical and... Feb 2022To effectively control the polymerized impurities in mezlocillin sodium and sulbenicillin sodium, a HPSEC method with TSK-gel G2000SWxl column and a RP-HPLC method with...
To effectively control the polymerized impurities in mezlocillin sodium and sulbenicillin sodium, a HPSEC method with TSK-gel G2000SWxl column and a RP-HPLC method with C18 analytical column were established to replace the classical gel filtration chromatography with Sephadex G-10 gel as stationary phase. By studying the chromatographic behavior of polymerized impurities in both methods with different chromatographic separation mechanisms, the polymerized impurities in mezlocillin sodium and sulbenicillin sodium were separated and detected effectively. The column switching two-dimension liquid chromatography ion trap/time-of-flight mass spectrometry was applied to characterize the structures of polymerized impurities eluted from the HPSEC method and RP-HPLC method for both drugs. The structures of the polymerized impurities in mezlocillin sodium and sulbenicillin sodium were deduced based on the MS data. The results showed that the polymerized impurities detected by HPSEC method and RP-HPLC method were completely different. Therefore, two methods should be used meanwhile to control the polymerized impurities in mezlocillin sodium and sulbenicillin sodium.
Topics: Chromatography, High Pressure Liquid; Drug Contamination; Mezlocillin; Pharmaceutical Preparations; Sodium; Sulbenicillin; Tandem Mass Spectrometry
PubMed: 35026591
DOI: 10.1016/j.jpba.2022.114584 -
The Journal of Antimicrobial... May 1983
Review
Topics: Administration, Oral; Bile; Dose-Response Relationship, Drug; Humans; Injections, Intramuscular; Kidney; Kinetics; Liver; Mezlocillin
PubMed: 6352604
DOI: 10.1093/jac/11.suppl_c.1