Journal of Targeted Drug Delivery

Clinical Pharmacology of Ceftriaxone in Infants and Children

Author(s): Gian Maria Pacifici

Ceftriaxone is a versatile and useful third-generation β-lactam-resistant cephalosporin. It is given intravenously or intramuscularly once a day. This antibiotic is active against some important gram-positive and most gram-negative bacteria. Ceftriaxone distributes widely in body tissues and in body fluids and penetrates into the cerebrospinal fluid and it is used to treat bacterial meningitis. In 34 infants and children aged 1 month to 19 years with bacterial meningitis, ceftriaxone cured 88% of subjects and the overall clinical response was 96%. Ceftriaxone may be used to treat nasopharyngeal, gonococcal ophthalmia, and epiglottises. Ceftriaxone is associated with biliary, renal, and haemolytic adverse events in children. Ceftriaxone displays bilirubin from albumin binding sites, thereby increases the amount of unconjugated bilirubin in infants and this drug is not recommended in neonates < 6 weeks old at risk of developing unconjugated hyperbilirubinaemia. Concurred administration of ceftriaxone and calcium is contraindicated. Ceftriaxone extensively binds to plasma proteins. In neonates, the ceftriaxone concentration slowly decays in plasma, after intravenous administration of 50 mg/kg ceftriaxone, the plasma ceftriaxone concentrations (μg/ml) are 155, 147, and 110 at 0.25, 1, and 7 hours, respectively, after administration. The half-life of ceftriaxone is age-depended and is longer in infants than in children. After intravenous administration, the plasma ceftriaxone concentrations are significantly higher than after intramuscular administration 0.25 and 0.5 hours after administration. Some bacteria may become resistant to ceftriaxone. The aim of this study is to review the published data on effects, pharmacokinetics, and bacterial-resistance of ceftriaxone in infants and children.

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