It is used in the UK as a treatment formigraine.[5][6] It is generally not available in the US.[4] It is available in some Asian, Latin American and European countries as ageneric drug for humans and for animals.[7]
Tolfenamic acid finds utility in the prevention and treatment of conditions associated with pain and inflammation.[8][9] However, despite its efficacy when administered intramuscularly, subcutaneously, or orally,[10] TFA-based drugs have not yet gained approval in the United States and some other countries due to the significant number of reported side effects.[11][12]
Tolfenamic acid, belonging to the pharmacological group of fenamates, possesses a chemical structure typical ofanthranilic acid derivatives. In this structure, one of the hydrogen atoms of the nitro group is substituted by a benzene ring featuring a methyl group and a chlorine atom at the ortho- and meta- positions, respectively.[13]
Nine forms of tolfenamic acid have been identified, some of which are determined by conformational states.[14][15][16] These polymorphic forms exhibit variations in the spatial arrangement within the unit cell and in the values of the C-N(H)-C-C angle.[16] This diversity in solid forms makes TFA an attractive candidate for modification and utilization in medical applications.
^abPentikäinen PJ, Neuvonen PJ, Backman C (1981). "Human pharmacokinetics of tolfenamic acid, a new anti-inflammatory agent".European Journal of Clinical Pharmacology.19 (5):359–365.doi:10.1007/bf00544587.PMID7238564.S2CID9428076.
^abNIH LiverTox DatabaseMefenamic Acid Last updated June 23, 2015. Page accessed July 3, 2015. Quote: "(fenamates generally not available in the United States, such as tolfenamic acid and flufenamic acid)"
^Kajander A, Laine V, Gothoni G (January 1972). "Effect of tolfenamic acid in rheumatoid arthritis".Scandinavian Journal of Rheumatology.1 (2):91–93.doi:10.3109/03009747209103003.PMID4572954.
^Basha R, Baker CH, Sankpal UT, Ahmad S, Safe S, Abbruzzese JL, et al. (January 2011). "Therapeutic applications of NSAIDS in cancer: special emphasis on tolfenamic acid".Frontiers in Bioscience.3 (2):797–805.doi:10.2741/s188.PMID21196413.
^Corum O, Corum DD, Er A, Yildiz R, Uney K (December 2018). "Pharmacokinetics and bioavailability of tolfenamic acid in sheep".Journal of Veterinary Pharmacology and Therapeutics.41 (6):871–877.doi:10.1111/jvp.12702.PMID30084126.S2CID51930602.
^Kjaersgård Rasmussen MJ, Holt Larsen B, Borg L, Soelberg Sørensen P, Hansen PE (June 1994). "Tolfenamic acid versus propranolol in the prophylactic treatment of migraine".Acta Neurologica Scandinavica.89 (6):446–450.doi:10.1111/j.1600-0404.1994.tb02664.x.PMID7976233.S2CID12334561.
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