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Clinical pharmacology of mezlocillin
Abstract:
Mezlocillin is a new broad-spectrum semisynthetic penicillin that has shown encouraging in vitro activity against the infecting organisms most likely to cause mortality and morbidity in cancer patients receiving chemotherapy. The serum clearances and urine recoveries of mezlocillin, ampicillin, and carbenicillin were compared after the intravenous administration of single 3-g doses. The peak mean serum concentrations of mezlocillin and carbenicillin were 269 and 278 mug/ml, respectively, whereas the peak ampicillin level was lower at 167 mug/ml. The terminal half-life of mezlocillin, 66 min, was not significantly different from those of ampicillin and carbencillin (63 and 77 min, respectively). Recoveries of mezlocillin, ampicillin, and carbenicillin from urine over 6-h periods after drug dosage were 45, 61, and 80%, respectively. A further study in 11 cancer patients examined serum maintenance levels of mezlocillin when 3-g doses were given intravenously every 4 h for at least 7 consecutive days. After 3 days of therapy, the mean serum concentrations were maintained above 50 mug/ml. Although therapeutic efficacy was not an objective of this study, all of three documented bacterial infections were cured, and no serious toxicity was encountered.
Insights
Mezlocillin, a broad-spectrum penicillin, shows promising in vitro activity against common infections in cancer patients. Pharmacokinetic studies reveal favorable serum concentrations and clearance, with no serious toxicity observed in preliminary cancer patient trials.
Area of Science:
- Pharmacology and Infectious Diseases
Background:
- Cancer patients undergoing chemotherapy are susceptible to life-threatening infections.
- Broad-spectrum antibiotics are crucial for managing infections in immunocompromised individuals.
Purpose of the Study:
- To evaluate the pharmacokinetics of mezlocillin compared to ampicillin and carbenicillin.
- To assess mezlocillin's serum maintenance levels in cancer patients.
Main Methods:
- Intravenous administration of 3-g doses of mezlocillin, ampicillin, and carbenicillin.
- Comparison of serum concentrations, half-life, and urine recovery.
- Monitoring of serum maintenance levels over 7 days in cancer patients.
Main Results:
- Mezlocillin achieved peak serum concentrations comparable to carbenicillin and higher than ampicillin.
- Mezlocillin exhibited a similar terminal half-life to ampicillin and carbenicillin.
- Sustained serum concentrations above 50 mug/ml were maintained in cancer patients receiving mezlocillin every 4 hours.
Conclusions:
- Mezlocillin demonstrates favorable pharmacokinetic properties for treating infections in cancer patients.
- Preliminary data suggest potential therapeutic efficacy and good tolerability in this patient population.