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°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 μg/ml (range, 0.65–1.63 μg/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→∞ ± SEM) was 4.61 ± 0.40 μg.h/ml (range, 2.74–5.98 μg.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).
This is a preview of subscription content, log in to check access.
Buy single article
Instant access to the full article PDF.
Price includes VAT for USA
Linden i.B., Parantainen J., Vapaatalo H. (1976): Inhibition of prostaglandin biosynthesis by tolfenamic acid in vitro. Scand. J. Rheumatol., 5, 129–132.
Corell T. (1994): Pharmacology of tolfenamic acid. Pharmacol. Toxicol., 75 (Suppl. 2), 14–21.
Moilanen E., Kankaanranta H. (1994): Tolfenamic acid and leukotriene synthesis inhibition. Pharmacol. Toxicol., 75 (Suppl. 2), 60–63.
Vapaatalo H., Parantainen J., Linden I.B., Hakkarainen H. (1977): Prostaglandin and vascular headache. Action of tolfenamic acid, a new anti-inflammatory analgesic, on migraine. In: Sicureti F. (ed.) Headache, new vistas. Biomedical Press, Florence, pp. 287–300.
Kajander A., Martio J., Murtu O., Gothoni G. (1976): Prolonged treatment with tolfenamic acid in inflammatory rheumatic diseases. Scand. J. Rheumatol., 4, 158–160.
Rejholec V., Vapaatalo H., Tokola O., Gothoni G. (1979): A comparative, double-blind study on tolfenamic acid in the treatment of rheumatoid arthritis. Scand. J. Rheumatol., 8 (Suppl. 24), 13–16.
Kauppila A., Ylikorkala O. (1977): Indomethacin and tolfenamic acid in primary dysmenorrhea. Eur. J. Obstet. Gynecol. Reprod. Biol., 7, 59–64.
Hakkarainen H., Vapaatalo H., Gothoni G., Parantainen J. (1979): Tolfenamic acid is as effective as ergotamine during migraine attacks. Lancet, 2, 326–328.
Larsen B.H., Christiansen L.V., Andersen B., Olesen J. (1990): Randomized double-blind comparison of tolfenamic acid and paracetamol in migraine. Acta Neurol. Scand., 81, 464–467.
Vapaatalo H. (1994): Tolfenamic acid and migraine — aspects of prostaglandins and leukotrienes. Pharmacol. Toxicol., 75 (Suppl. 2), 76–80.
Jaussaud P., Guieu D., Courtot D., Barbier B., Bonnaire Y. (1992): Identification of a tolfenamic acid metabolite in the horse by gas chromatography-mass spectrometry. J. Chromatogr., 573, 136–140.
Pentikainen P.J., Neuvonen P.J., Backman C. (1981): Human pharmacokinetics of tolfenamic acid, a new anti-inflammatory agent. Eur. J. Clin. Pharmacol., 19, 359–365.
Pedersen S.B. (1994): Biopharmaceutical aspects of tolfenamic acid. Pharmacol. Toxicol., 75 (Suppl. 2), 22–32.
Pedersen S.B., Alhede B., Buchardt O., Moiler J., Bock K. (1981): Tolfenamic acid detection and structures of urinary metabolites. Arzneimittelforsch., 31, 1944–1948.
Pentikainen P.J., Penttila A., Neuvonen P.J., Khalifah R.G., Hignite C.E. (1982): Human metabolism of tolfenamic acid. 1. Isolation, preliminary characterization and pharmacokinetics of tolfenamic acid and its metabolites. Eur. J. Drug Metab. Pharmacokinet., 7, 259–267.
Hansen S.H., Pedersen S.B. (1986): Assay of tolfenamic acid and its metabolites by liquid chromatography on dynamically modified silica: application in pharmacokinetics. J. Pharm. Biomed. Anal., 4, 69–82.
Niopas I., Georgarakis M. (1995): Determination of tolfenamic acid in human plasma by HPLC. J. Liq. Chromatogr., 18, 2675–2682.
Rowland M., Tozer T.N. (1989): Clinical pharmacokinetics: concepts and applications, 2nd Ed. Lea & Febiger, Philadelphia.
Keinanen S., Simila S., Kouvalainen K. (1978): Oral antipyretic therapy: evaluation of the N-aryl-anthranilic acid derivatives mefenamic acid, tolfenamic acid and flufenamic acid. Eur. J. Clin. Pharmacol., 13, 331–334.
About this article
Cite this article
Niopas, I., Georgarakis, M., Sidi-Frangandrea, V. et al. Pharmacokinetics of tolfenamic acid in pediatric patients after single oral dose. European Journal of Drug Metabolism and Pharmacokinetics 20, 293–296 (1995). https://doi.org/10.1007/BF03190247
- Tolfenamic acid
- antipyretic activity