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Ceftriaxone pharmacokinetics following multiple intramuscular dosing
European Journal of Clinical Pharmacology
|January 1, 1986
Summary
This study investigated ceftriaxone pharmacokinetics and tolerance in healthy volunteers receiving multiple intramuscular doses. Ceftriaxone demonstrated rapid absorption and was well-tolerated, with no serious adverse reactions observed.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Infectious Diseases
Background:
- Ceftriaxone is a widely used third-generation cephalosporin antibiotic.
- Understanding its pharmacokinetic profile after intramuscular administration is crucial for optimizing therapeutic outcomes.
- Assessing tolerance is essential for patient safety and adherence.
Purpose of the Study:
- To evaluate the steady-state pharmacokinetics of ceftriaxone following multiple intramuscular (i.m.) doses.
- To assess the tolerance and safety profile of ceftriaxone in healthy adult volunteers.
Main Methods:
- Twelve healthy adult volunteers received intramuscular ceftriaxone at 0.5 g and 1 g every 12 hours for 3.5 days.
- Plasma concentrations were measured to determine pharmacokinetic parameters like absorption, peak time, and steady-state levels.
- Adverse events were monitored to assess tolerance.
Main Results:
- Ceftriaxone showed rapid absorption after i.m. administration, with peak plasma concentrations reached between 1.3 to 1.9 hours.
- Steady-state plasma concentrations were achieved by the third dose.
- Elimination half-life remained unchanged, while minor, therapeutically insignificant increases in clearance and volume of distribution were noted at the 1-g dose due to non-linear protein binding.
Conclusions:
- Multiple intramuscular doses of ceftriaxone exhibit predictable pharmacokinetics and are well-tolerated in healthy adults.
- The observed pharmacokinetic changes at higher doses are not clinically significant.
- Ceftriaxone is a safe and effective option for intramuscular administration.