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[Bone concentrations of imipenem after a dose of imipenem/cilastatin]
Abstract:
The concentration of imipenem in organic bone, determined in 16 patients by bioassay after short infusion (15 min) of 1 g imipenem/cilastatin was 4.3 +/- 2.06 mg/kg (geometric mean +/- standard deviation, n = 13) after 45 minutes, and 2.8 +/- 1.86 mg/kg (n = 26) after 88 minutes. Imipenem penetrates into inorganic hydroxylapatite (imbution), however, its antimicrobial activity is lost. The mean serum concentration in 12 patients (mean age 77 years) with normal renal and hepatic function 15 minutes after the beginning of the infusion was 93.1 mg/l imipenem. The mean serum half life t (1/2 beta) was 1.32 hours, the total body clearance 108.6 1/h, and the volume of distribution during the beta phase V(beta) 12.4 1.
Insights
Imipenem penetrates bone tissue, reaching concentrations of 4.3 mg/kg at 45 minutes post-infusion. While imipenem enters hydroxylapatite, its antimicrobial activity is lost in this inorganic bone component.
Area of Science:
- Pharmacology
- Infectious Diseases
- Orthopedics
Background:
- Imipenem is a broad-spectrum antibiotic used for severe infections.
- Understanding its penetration into bone tissue is crucial for treating bone infections.
Purpose of the Study:
- To quantify imipenem concentration in human bone after intravenous infusion.
- To assess imipenem's antimicrobial activity within bone tissue and hydroxylapatite.
Main Methods:
- Bioassay used to determine imipenem levels in organic bone samples from patients.
- Imipenem penetration into inorganic hydroxylapatite was investigated.
- Serum concentrations, half-life, clearance, and volume of distribution were measured.
Main Results:
- Mean imipenem bone concentrations were 4.3 mg/kg at 45 minutes and 2.8 mg/kg at 88 minutes post-infusion.
- Imipenem penetrated inorganic hydroxylapatite but lost its antimicrobial activity.
- Mean serum concentration was 93.1 mg/l, with a half-life of 1.32 hours.
Conclusions:
- Imipenem achieves measurable concentrations in bone tissue.
- Antimicrobial activity of imipenem is compromised within inorganic bone components like hydroxylapatite.