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Pharmacokinetics of tiaprofenic acid in children after a single oral dose
1Département de Pharmacologie Clinique Périnatale et Pédiatrique, Hôpital Saint-Vincent de Paul, Paris, France.
Insights
Tiaprofenic acid (TA) pharmacokinetics in children aged 3-11 years showed no age-related differences. Despite higher plasma clearance than adults, current dosing regimens are recommended due to lack of established efficacy or toxicity correlations.
Area of Science:
- Pharmacology
- Pediatric Medicine
- Drug Metabolism
Background:
- Tiaprofenic acid (TA) is a non-steroidal anti-inflammatory drug (NSAID).
- Understanding TA pharmacokinetics in children is crucial for safe and effective use.
- Limited data exists on TA's absorption, distribution, metabolism, and excretion (ADME) in pediatric populations.
Purpose of the Study:
- To investigate the pharmacokinetic profile of tiaprofenic acid in healthy children.
- To compare TA pharmacokinetics in different pediatric age groups.
- To compare pediatric TA pharmacokinetics with those reported in adults.
Main Methods:
- A single oral dose of tiaprofenic acid (3 mg/kg) was administered to 12 healthy children (three age groups).
- Blood and urine samples were collected at specified intervals for TA concentration analysis.
- High-performance liquid chromatography (HPLC) was used to measure TA concentrations in plasma and urine.
Main Results:
- No significant differences in TA pharmacokinetic parameters (Cmax, tmax, AUC, t1/2, Vd, CL) were observed between pediatric age groups.
- Apparent plasma clearance of TA was 56% higher in children compared to adults.
- 33% of the TA dose was recovered in 24-hour urine, with a higher proportion of unconjugated TA in children than adults.
Conclusions:
- Tiaprofenic acid exhibits predictable pharmacokinetics in children aged 3-11 years, irrespective of age.
- The higher plasma clearance in children compared to adults warrants consideration, although direct correlation to efficacy/toxicity is not established.
- Current adult dosing recommendations for tiaprofenic acid are considered appropriate for children aged 3-11 years in the absence of established dose-response relationships.
Abstract:
Twelve healthy children in three age groups anaesthetized for minor surgery were given a single oral dose of tiaprofenic acid (3 mg.kg-1) (TA). Seven blood samples and zero to 8 and 8 to 24 h urines were collected. TA concentrations in plasma and urine were measured by HPLC. No significant difference was found between the age groups in the kinetic parameters of TA and no correlation was found between these parameters and age: tmax = 2.12 h, Cmax = 8.78 mg.l-1, AUC(0----8 h) 33.9 mg.h.l-1, AUC = 39.3 mg.h.l-1, t1/2 = 2.35 h, Vt = 0.319 l.kg-1, CL = 0.094 l.h-1.kg-1. Renal clearance was 14 ml.h-1.kg-1.33% of the TA dose was recovered in the 24 h urine, 48% of which was conjugated, whereas in adults, TA is only found in urine as conjugates. The apparent plasma clearance was significantly higher (56%) than in 12 healthy adults given 1.5 mg.kg-1 TA. Volume of distribution and t1/2 did not significantly differ between children and adults. Since no relationship has been established between plasma TA and either efficacy or toxicity, a different dose regimen cannot be recommended in 3-11 year-old children from that in adults.