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Pharmacokinetics of tolfenamic acid in pediatric patients after single oral dose
I Niopas1, M Georgarakis, V Sidi-Frangandrea
1Department of Pharmacy, Aristotle University, Thessaloniki, Greece.
Insights
Tolfenamic acid effectively reduced fever in children, showing favorable pharmacokinetics with a short half-life and good tolerability. This non-steroidal anti-inflammatory drug is a promising option for pediatric fever management.
Area of Science:
- Pharmacology
- Pediatrics
- Drug Metabolism
Background:
- Tolfenamic acid is a non-steroidal anti-inflammatory drug (NSAID) used for its analgesic and antipyretic properties.
- Understanding the pharmacokinetics of NSAIDs in children is crucial for safe and effective dosing.
Purpose of the Study:
- To determine the pharmacokinetic profile of tolfenamic acid in febrile children.
- To assess the safety and efficacy of a single oral dose of tolfenamic acid in reducing fever.
Main Methods:
- A single oral dose of 1 mg/kg tolfenamic acid suspension was administered to 6 febrile children (ages 2-14 years).
- Plasma concentrations of tolfenamic acid were measured using reversed-phase High-Performance Liquid Chromatography (HPLC) at timed intervals up to 8 hours post-dose.
- Pharmacokinetic parameters were calculated using model-independent methods.
Main Results:
- Tolfenamic acid significantly reduced body temperature by approximately 2 degrees C.
- The drug was well-tolerated with no adverse effects reported.
- Key pharmacokinetic parameters included a mean peak plasma concentration (Cmax) of 1.09 µg/mL, time to peak concentration (tmax) of 1.4 hours, elimination half-life (t1/2) of 2.82 hours, and apparent total clearance (CL/F) of 3.83 mL/min/kg.
Conclusions:
- Tolfenamic acid demonstrates favorable pharmacokinetics in febrile children following a single oral dose.
- The drug is effective in reducing fever and appears to be well-tolerated in the pediatric population.
- Further studies may be warranted to establish optimal dosing regimens for pediatric use.
Abstract:
The pharmacokinetics of tolfenamic acid, a non-steroidal anti-inflammatory drug, were determined following administration of a 1 mg/kg single oral dose of tolfenamic acid suspension to 6 feverish children. Their ages were from 2-14 years (mean 7.5 years) and their weights were from 12-50 kg (mean 29.2 kg). Tolfenamic acid produced a significant fall in temperature (about 2 degrees C) compared to the initial value before oral intake of the drug and was well tolerated without adverse effects. Blood samples for determination of tolfenamic acid concentrations in plasma were obtained at timed intervals for up to 8 h post-dose. Plasma concentrations of tolfenamic acid were determined using a reversed phase HPLC method and pertinent pharmacokinetic parameters were estimated by model-independent standard methods and were the following: the mean peak plasma concentration (Cmax +/- SEM) was 1.09 +/- 0.44 micrograms/ml (range, 0.65-1.63 micrograms/ml) and the mean time (tmax +/- SEM) to reach peak plasma concentration was 1.4 +/- 0.4 h (range, 0.5-3.0 h). The mean area under the plasma concentration-time curve (AUC0-->infinity +/- SEM) was 4.61 +/- 0.40 micrograms.h/ml (range, 2.74-5.98 micrograms.h/ml), the mean elimination half-life (t1/2 +/- SEM) was 2.82 +/- 0.21 h (range, 2.19-3.40 h) and the mean apparent total clearance (CL/F +/- SEM) was 3.83 +/- 0.41 ml/min/kg (range, 2.79-6.08 ml/min/kg).