Tolfenamic Acid (tolfenamic + acid)

Distribution by Scientific Domains


Selected Abstracts


Anti-Inflammatory, Antiproliferative, and Radical-Scavenging Activities of Tolfenamic Acid and Its Metal Complexes

CHEMISTRY & BIODIVERSITY, Issue 6 2009
Dimitra Kovala-Demertzi
Abstract Some new complexes of tolfenamic acid (=2-[(2-methyl-3-chlorophenyl)amino]benzoic acid; Htolf) with potentially interesting biological activities are described. The complexes [Mn(tolf)2(H2O)2], [Co(tolf)2(H2O)2], [Ni(tolf2(H2O)2], [Cu(tolf)2(H2O)]2, and [Zn(tolf)2(H2O)] were prepared by the reaction of tolfenamic acid, a potent anti-inflammatory drug, with metal salts. The radical-scavenging activities of the complexes were evaluated using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical-scavenging assay. Their ability to inhibit soybean lipoxygenase, , -glucuronidase, and trypsin-induced proteolysis was studied. Their inhibitory effects on rat paw edema induced by carrageenin was studied and compared with those of tolfenamic acid. The complex [Zn(tolf)2(H2O)] exhibited the strongest in vivo inhibitory effect at 0.1,mm/kg Body Weight (BW; 93.0±0.9%), superior than the inhibition induced by tolfenamic acid at the same molar dose (76.0±0.9%). Tolfenamic acid and its metal complexes have been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines, MCF-7 (breast cancer cell line), T24 (bladder cancer cell line), and A-549 (non-small cell lung carcinoma), and a mouse fibroblast L-929 cell line. The complexes [Mn(tolf)2(H2O)2] and [Cu(tolf)2(H2O)]2 have shown selectivity against T24 cell line. The IC50 values of these two complexes against T24 cancer cell lines are in a micromolar range similar or better to that of the antitumor drug cisplatin. [source]


Postoperative analgesic efficacy of meloxicam compared to tolfenamic acid in cats undergoing orthopaedic surgery

JOURNAL OF SMALL ANIMAL PRACTICE, Issue 10 2010
P. J. Murison
Objectives: To investigate the efficacy of meloxicam or tolfenamic acid administered preoperatively and postoperatively (five days in total) to cats undergoing surgical fracture repair. Methods: Eighty-eight otherwise healthy cats were matched according to fracture site and then randomly allocated to one of two groups, receiving 0·2 mg/kg meloxicam by subcutaneous injection (group M) or 1·5 to 3 mg/kg tolfenamic acid orally (group T) before anaesthesia. Analgesia was continued with 0.05 mg/kg oral meloxicam once daily or 1·5 to 3 mg/kg oral tolfenamic acid twice daily for four days postoperatively. Pain was assessed by a blinded observer using visual analogue scales and a functional limb score. The drug administrator assessed feed intake and palatability of the treatment. Results: Data from 66 cats were analysed. Visual analogue scale pain scores and functional limb scores decreased over time in both groups but were not significantly different between treatments. Feed intake was similar in both groups. Meloxicam was significantly more palatable than tolfenamic acid on all treatment days. Clinical Significance: Meloxicam and tolfenamic acid demonstrated comparable analgesia, without clinically observable side effects. Meloxicam may be associated with superior compliance in clinical practice due to the higher palatability and once daily treatment resulting in better ease of administration. [source]


Field evaluation of the efficacy of tolfenamic acid administered in one single preoperative injection for the prevention of postoperative pain in the dog

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 6 2007
E. GRANDEMANGE
In this randomized, placebo-controlled, blinded field trial, 62 dogs (of which four were excluded) taken to a veterinary practice for orthopaedic surgery with a postoperative painful component were enrolled to assess the efficacy of a preoperative intramuscular injection of tolfenamic acid (TA) at a dose of 4 mg/kg in preventing postoperative pain. The animals were clinically examined at T1 + 1H, T1 + 4H, T1 + 24H (T1 = extubation). The efficacy results showed a statistical effect of TA in preventing postoperative pain with the evolution in the pain statistically in favour of TA treatment (Visual Analogue Scale). This was confirmed by the sum of the scores calculated at T1 + 24H that was statistically higher in the placebo group, and by the evolution in the respiratory rate, which was statistically lower in the TA-treated animals after surgery. TA treatment was very well tolerated as no clinical sign (except one isolated case of vomiting and diarrhoea, i.e. 3.5%) or change in biochemical and haematological values was observed and as no interaction with the anaesthetic drugs and with marbofloxacin was reported. [source]


Anti-Inflammatory, Antiproliferative, and Radical-Scavenging Activities of Tolfenamic Acid and Its Metal Complexes

CHEMISTRY & BIODIVERSITY, Issue 6 2009
Dimitra Kovala-Demertzi
Abstract Some new complexes of tolfenamic acid (=2-[(2-methyl-3-chlorophenyl)amino]benzoic acid; Htolf) with potentially interesting biological activities are described. The complexes [Mn(tolf)2(H2O)2], [Co(tolf)2(H2O)2], [Ni(tolf2(H2O)2], [Cu(tolf)2(H2O)]2, and [Zn(tolf)2(H2O)] were prepared by the reaction of tolfenamic acid, a potent anti-inflammatory drug, with metal salts. The radical-scavenging activities of the complexes were evaluated using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical-scavenging assay. Their ability to inhibit soybean lipoxygenase, , -glucuronidase, and trypsin-induced proteolysis was studied. Their inhibitory effects on rat paw edema induced by carrageenin was studied and compared with those of tolfenamic acid. The complex [Zn(tolf)2(H2O)] exhibited the strongest in vivo inhibitory effect at 0.1,mm/kg Body Weight (BW; 93.0±0.9%), superior than the inhibition induced by tolfenamic acid at the same molar dose (76.0±0.9%). Tolfenamic acid and its metal complexes have been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines, MCF-7 (breast cancer cell line), T24 (bladder cancer cell line), and A-549 (non-small cell lung carcinoma), and a mouse fibroblast L-929 cell line. The complexes [Mn(tolf)2(H2O)2] and [Cu(tolf)2(H2O)]2 have shown selectivity against T24 cell line. The IC50 values of these two complexes against T24 cancer cell lines are in a micromolar range similar or better to that of the antitumor drug cisplatin. [source]