Summary: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.
- Etcheverry S, Barrio D, Cortizo A, Williams P. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002;88:94-100 pubmed..Ibuprofen (2-(4-isobutylphenyl)propionic acid), Naproxen (6-methoxy-alpha-methyl-2-naphthalene acetic acid) and Tolmetin (1-methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic acid) were studied...
- Pignatello R, Consoli P, Puglisi G. In vitro release kinetics of Tolmetin from tabletted Eudragit microparticles. J Microencapsul. 2000;17:373-83 pubmed..by three different techniques, of microparticles made of Eudragit RS 100 and RL 100 containing a NSAI agent, Tolmetin. Freely flowing microparticles failed to affect significantly the in vitro drug release, which displayed a ..
- Taylor J, Jones M, Williams J, Bull S. Friedel-Crafts acylation of pyrroles and indoles using 1,5-diazabicyclo[4.3.0]non-5-ene (DBN) as a nucleophilic catalyst. Org Lett. 2010;12:5740-3 pubmed publisher..A detailed mechanistic study implies that DBN is acting as a nucleophilic organocatalyst, with the X-ray crystal structure of a key N-acyl-amidine intermediate having been determined for the first time. ..
- Sotgiu M, Biella G, Formaglio F, Marchettini P. Central effect of ketorolac involving NMDA receptors activity. Brain Res. 1998;813:223-6 pubmed..The data suggest that Ketorolac can achieve its central analgesic effect by interfering with the NMDA receptor activity on the spinal neurons. ..
- Coruzzi G, Coppelli G, Spaggiari S, Cavestro G, Okolicsanyi L, Lo Giudice P, et al. Gastroprotective effects of amtolmetin guacyl: a new non-steroidal anti-inflammatory drug that activates inducible gastric nitric oxide synthase. Dig Liver Dis. 2002;34:403-10 pubmed..The anti-inflammatory drug tolmetin and the bacterial lipopolysaccharide from Escherichia coli were studied for comparison...
- Neamtu S, Toşa N, Bogdan M. Spectroscopic investigation of tolmetin interaction with human serum albumin. J Pharm Biomed Anal. 2013;85:277-82 pubmed publisherThe interaction of tolmetin (TOL) with human serum albumin (HSA) in physiological buffer solution (pH 7...
- Borga O, Borgå B. Serum protein binding of nonsteroidal antiinflammatory drugs: a comparative study. J Pharmacokinet Biopharm. 1997;25:63-77 pubmed..21%; fenoprofen 0.25%, flurbiprofen 0.022%, ketoprofen 0.52%, naproxen 0.039%, and tolmetin 0.37%. Thus the least bound NSAID, ketoprofen, had a value 24-fold that of the most highly bound, flurbiprofen...
- Wang M, Gorrell M, Abbott C, Jaggi R, Marguet D, Dickinson R. Hepatic covalent adduct formation with zomepirac in the CD26-deficient mouse. J Gastroenterol Hepatol. 2002;17:66-71 pubmed..These data definitively showed that CD26 was a component of ZP-modified proteins in vivo. In addition, the data suggested that at least one other protein of approximately 110 kDa was modified by covalent adduct formation with ZAG. ..
- Chen F, Chen C, Chen C, Wu A. Quantitation of tolmetin by high-performance liquid chromatography and method validation. J Chromatogr Sci. 2003;41:381-4 pubmedA high-performance liquid chromatographic (HPLC) assay method for assessing the degradation of tolmetin (TLM) is developed and validated under acidic, basic, and photoirradiated conditions...
- Yee R. Analgesic efficacy and safety of nonpreserved ketorolac tromethamine ophthalmic solution following radial keratotomy. Ketorolac Radial Keratotomy Study Group. Am J Ophthalmol. 1998;125:472-80 pubmed..To compare the analgesic efficacy and safety of nonpreserved ketorolac tromethamine 0.5% with those of its vehicle in the treatment of postsurgical ocular pain following radial keratotomy...
- Pannuti F, Robustelli della Cuna G, Ventaffrida V, Strocchi E, Camaggi C. A double-blind evaluation of the analgesic efficacy and toxicity of oral ketorolac and diclofenac in cancer pain. The TD/10 recordati Protocol Study Group. Tumori. 1999;85:96-100 pubmed..Interestingly, a pronounced sequence effect was found: gastric disturbances after ketorolac were observed mainly (10 out of 15 observed events) when the drug was given to patients pretreated with diclofenac. ..
- Genç L, Demirel M, Guler E, Hegazy N. Microencapsulation of ketorolac tromethamine by means of a coacervation-phase separation technique induced by the addition of non-solvent. J Microencapsul. 1998;15:45-53 pubmed..The yield was calculated and the release properties of KT were investigated by USP XXII paddle method and using UV spectrophotometry at 318 and 323 nm. ..
- Brandl M, Conley D, Johnson D. Racemization of ketorolac in aqueous solution. J Pharm Sci. 1995;84:1045-8 pubmed..Alternative buffers, in particular phosphate buffer, provide formulations exhibiting a T90 greater than 2 years. ..
- Krowicki Z. Involvement of hindbrain and peripheral prostanoids in gastric motor and cardiovascular responses to delta-9-tetrahydrocannabinol in the rat. J Physiol Pharmacol. 2012;63:581-8 pubmed..2 mg/kg, i.v.) were administered before and 15-min after the COX inhibitor tolmetin (50 mg/kg, i.v.) or 15 min after topical application of tolmetin to the surface of the dorsal medulla (0...
- Trinchero A, Bonora S, Tinti A, Fini G. Spectroscopic behavior of copper complexes of nonsteroidal anti-inflammatory drugs. Biopolymers. 2004;74:120-4 pubmed..Crystalline complexes, Cu(II)-NSAID (ibuprofen, naproxen, tolmetin, and diclofenac), with a carboxylic function have been studied by means of infrared and Raman spectroscopy...
- Bai G, Cui Y, Yang Y, Ye C, Liu M. A competitive low-affinity binding model for determining the mutual and specific sites of two ligands on protein. J Pharm Biomed Anal. 2005;38:588-93 pubmed..The model was examined by using human serum albumin (HSA) as a receptor and tolmetin (TOL) and salicylic acid (SAL) as ligands...
- Tito A, Jimenez Lopez C, Kowalska A, Wysocki S. A study of the intermolecular interactions of tolmetin/N-acetyl-L-tyrosine ethyl ester complex. Spectrochim Acta A Mol Biomol Spectrosc. 2009;72:1000-6 pubmed publisherThe formation of tolmetin/N-acetyl-l-tyrosine ethyl ester (ATEE) complex has been reported by means of both theoretical and experimental studies, including quantum mechanical calculations as well as UV-vis absorption, fluorescence and ..
- van Leeuwen J, Unlü B, Vermeulen N, Vos J. Differential involvement of mitochondrial dysfunction, cytochrome P450 activity, and active transport in the toxicity of structurally related NSAIDs. Toxicol In Vitro. 2012;26:197-205 pubmed publisher..The class III NSAIDs sulindac, ketorolac and zomepirac were relatively non-toxic in yeast. In conclusion, we demonstrate the use of yeast to investigate the mechanisms underlying the toxicity of structurally related drugs. ..
- Klapper J, Stanton J. Ketorolac versus DHE and metoclopramide in the treatment of migraine headaches. Headache. 1991;31:523-4 pubmed..The average improvement in patients receiving DHE and metoclopramide was greater in pain (p = .031) and disability scores (p = .057), than in those patients given ketorolac. ..
- Harden R, Carter T, Gilman C, Gross A, Peters J. Ketorolac in acute headache management. Headache. 1991;31:463-4 pubmed..This open label trial suggests that Ketorolac Tromethamine may be a useful agent in the treatment of headache crisis, and a controlled study to examine this is warranted. ..
- Abraham J. Regulating the cancer-inducing potential of non-steroidal anti-inflammatory drugs: some lessons from the 1970s and 1980s. Soc Sci Med. 1998;46:39-51 pubmed..This takes the form of awarding the benefit of the many scientific doubts in carcinogenicity testing to manufacturers rather than to patients. ..
- Ripamonti C, Ticozzi C, Zecca E, Rodriguez C, De Conno F. Continuous subcutaneous infusion of ketorolac in cancer neuropathic pain unresponsive to opioid and adjuvant drugs. A case report. Tumori. 1996;82:413-5 pubmed..Furthermore, the analgesia lasted over 75 days of treatment without any significant renal and gastric side effects. ..
- Geisslinger G, Peskar B, Pallapies D, Sittl R, Levy M, Brune K. The effects on platelet aggregation and prostanoid biosynthesis of two parenteral analgesics: ketorolac tromethamine and dipyrone. Thromb Haemost. 1996;76:592-7 pubmed..This is in line with clinical observations and may be an advantage when these drugs are given as postoperative analgesics at the doses tested...
- Varrassi G, Marinangeli F, Agro F, Aloe L, De Cillis P, De Nicola A, et al. A double-blinded evaluation of propacetamol versus ketorolac in combination with patient-controlled analgesia morphine: analgesic efficacy and tolerability after gynecologic surgery. Anesth Analg. 1999;88:611-6 pubmed..Morphine consumption and pain scores were comparable in the two studied groups. Propacetamol is as effective as ketorolac and has an excellent tolerability after gynecologic surgery. ..
- Ely D, Carvajal M. Determination of the scale of segregation of low dose tablets using hyperspectral imaging. Int J Pharm. 2011;414:157-60 pubmed publisher..infrared (NIR) hyperspectral imaging was used to quantify the spatial distribution of drug in tablets containing tolmetin sodium dihydrate...
- Mendel H, Guarnieri K, Sundt L, Torjman M. The effects of ketorolac and fentanyl on postoperative vomiting and analgesic requirements in children undergoing strabismus surgery. Anesth Analg. 1995;80:1129-33 pubmed..Fentanyl should be avoided, as it was associated with a significantly greater incidence of postoperative vomiting compared to ketorolac or placebo. ..
- Jelvehgari M, Valizadeh H, Rezapour M, Nokhodchi A. Control of encapsulation efficiency in polymeric microparticle system of tolmetin. Pharm Dev Technol. 2010;15:71-9 pubmed publisherEthylcellulose microparticles containing tolmetin sodium, an anti-inflammatory drug, were prepared by a solvent diffusion method based on the formation of multiple W/O(1)/O(2)-emulsion...
- Jones D, Bjorksten A. Detection of ketorolac enantiomers in human plasma using enantioselective liquid chromatography. J Chromatogr B Biomed Appl. 1994;661:165-7 pubmed..The detection limit was 5 ng/ml for each enantiomer. The method has been applied to determine the concentration of ketorolac enantiomers during an infusion of the racemic drug and has proven to be rapid and sensitive. ..
- Costa D, Gomes A, Lima J, Fernandes E. Singlet oxygen scavenging activity of non-steroidal anti-inflammatory drugs. Redox Rep. 2008;13:153-60 pubmed publisher..On the other hand, the pyrrole derivatives (tolmetin and ketorolac), the indolacetic acid derivatives (indomethacin, and etodolac), as well as sulindac and its ..
- Francois J, Mulier M. Idiopathic chondrolysis of the hip: a case report. Acta Orthop Belg. 2007;73:653-7 pubmed..Some authors advocate conservative treatment until spontaneous fusion. A case of idiopathic chondrolysis conventionally managed is reported. ..
- Chaudhary R, Gangwal S, Jindal K, Khanna S. Reversed-phase high-performance liquid chromatography of ketorolac and its application to bioequivalence studies in human serum. J Chromatogr. 1993;614:180-4 pubmed..The assay procedure was linear in the range 0.25-1.5 micrograms/ml, with a sensitivity of 0.01 micrograms/ml ketorolac. The recovery of ketorolac from serum ranged from 90 to 95%. ..
- Cordell W, Wright S, Wolfson A, Timerding B, Maneatis T, Lewis R, et al. Comparison of intravenous ketorolac, meperidine, and both (balanced analgesia) for renal colic. Ann Emerg Med. 1996;28:151-8 pubmed..Because many subjects in all three treatment groups received supplemental meperidine and because response to ketorolac alone cannot be predicted, clinicians may choose to initiate treatment with a ketorolac-meperidine combination. ..
- Gupta A, Peck G, Miller R, Morris K. Nondestructive measurements of the compact strength and the particle-size distribution after milling of roller compacted powders by near-infrared spectroscopy. J Pharm Sci. 2004;93:1047-53 pubmed..cellulose powder as well as from a typical direct compression pharmaceutical powder blend containing tolmetin sodium dihydrate, microcrystalline cellulose, and dicalcium phosphate dihydrate...
- López Muñoz F, Ventura R, Diaz I, Fernandez Guasti A, Tost D, Cabre F, et al. Antinociceptive effects of S(+)-ketoprofen and other analgesic drugs in a rat model of pain induced by uric acid. J Clin Pharmacol. 1998;38:11S-21S pubmed..Whereas SFB was an effective antinociceptive, RFB had no antinociceptive effect at the doses tested when given either orally or intracerebroventricularly. ..
- Callanan D, Fellman R, Savage J. Latanoprost-associated cystoid macular edema. Am J Ophthalmol. 1998;126:134-5 pubmed..The macular edema resolved in both eyes. Topical latanoprost may be associated with cystoid macular edema; this may be related to a prostaglandin-like action. ..
- Kauffman R, Lieh Lai M, Uy H, Aravind M. Enantiomer-selective pharmacokinetics and metabolism of ketorolac in children. Clin Pharmacol Ther. 1999;65:382-8 pubmed..Enantiomeric pharmacokinetic differences are best explained by stereoselective plasma protein binding. Selective glucuronidation of the S(-) enantiomer suggests that stereoselective metabolism may also be a contributing factor. ..
- Persico F, Pritchard J, Fisher M, Yorgey K, Wong S, Carson J. Effect of tolmetin glycine amide (McN-4366), a prodrug of tolmetin sodium, on adjuvant arthritis in the rat. J Pharmacol Exp Ther. 1988;247:889-96 pubmedThe glycine amide of tolmetin sodium (TGA) functions as a prodrug and was demonstrated to be more potent than the parent compound as an inhibitor of developing and established adjuvant arthritis in the female Lewis rat...
- Pitarresi G, Cavallaro G, Giammona G, De G, Salemi M, Sortino S. New hydrogel matrices containing an anti-inflammatory agent. Evaluation of in vitro release and photoprotective activity. Biomaterials. 2002;23:537-50 pubmed..PAHy) chemically crosslinked with ethyleneglycol diglycidylether (EGDGE) containing Tolmetin sodium salt, are reported...
- Cannell G, Vesey D, Dickinson R. Inhibition of proliferation of HT-29 colon adenocarcinoma cells by carboxylate NSAIDs and their acyl glucuronides. Life Sci. 2001;70:37-48 pubmed..The anti-epileptic drug valproate had no effect on inhibition of thymidine uptake, though, surprisingly, its acyl glucuronide and isomers were active. The reasons for this are unclear at present. ..
- Obach R. Glycerolysis of acyl glucuronides as an artifact of in vitro drug metabolism incubations. Drug Metab Dispos. 2009;37:1581-6 pubmed publisher..Other drugs that are converted to acyl glucuronides in vitro (diclofenac, mefenamic acid, tolmetin, and naproxen) were also shown to form corresponding glycerol esters when incubated with human liver S-9 fraction ..
- Perez Urizar J, Flores Murrieta F, Castaneda Hernandez G. Effect of experimental hypoalbuminemia on the plasma protein binding of tolmetin. Life Sci. 2002;71:1015-22 pubmedThe purpose of this work was to study tolmetin plasma protein binding in an experimental model of hypoalbuminemia in the rat. Hypoalbuminemia was produced by repetitive plasmapheresis, achieving a 26.2 +/- 4...
- Cruz Vera M, Lucena R, Cárdenas S, Valcarcel M. Ionic liquid-based dynamic liquid-phase microextraction: application to the determination of anti-inflammatory drugs in urine samples. J Chromatogr A. 2008;1202:1-7 pubmed publisher..Limits of detection were in the range from 38 ng mL(-1) (indomethacin) to 70 ng mL(-1) (naproxen). The repeatability of the proposed method expressed as RSD (n=5) varied between 2.1% (flurbiprofen) and 3.8% (tolmetin).
- Hixson L, Alberts D, Krutzsch M, Einsphar J, Brendel K, Gross P, et al. Antiproliferative effect of nonsteroidal antiinflammatory drugs against human colon cancer cells. Cancer Epidemiol Biomarkers Prev. 1994;3:433-8 pubmed..A cytostatic response was demonstrated with sulindac sulfide. These data further support the potential role of these agents for chemoprevention of colorectal neoplasia. ..
- Iyer V. Ketorolac (Toradol) induced lithium toxicity. Headache. 1994;34:442-4 pubmed..A case of lithium neurotoxicity in a patient with cluster headache, resulting from coadministration of ketorolac is reported. While lithium interaction with many other NSAIDs is well-known, ketorolac has not been incriminated. ..
- Kamath B, Shivram K, Shah A. Determination of diclofenac sodium, famotidine and ketorolac tromethamine by flow injection analysis using dichloronitrophenol. J Pharm Biomed Anal. 1994;12:343-6 pubmed..6%). The FIA method was applied to the determination of diclofenac sodium, famotidine and ketorolac tromethamine in pharmaceutical formulations. ..
- Malmberg A, Yaksh T. Pharmacology of the spinal action of ketorolac, morphine, ST-91, U50488H, and L-PIA on the formalin test and an isobolographic analysis of the NSAID interaction. Anesthesiology. 1993;79:270-81 pubmed..These studies also demonstrate that spinal synergy is not a common property of all interactions. Thus, the NSAID synergy appears to occur with agents that exert a concurrent action both pre- and postsynaptic to the primary afferents. ..
- Kirkova M, Alexandova A, Kesiova M, Todorov S. In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems. Comparison with non-selective and COX-2 selective NSAIDs. Auton Autacoid Pharmacol. 2007;27:99-104 pubmed..1. The in vivo effects of the non-steroid anti-inflammatory drug (NSAID) amtolmetin guacyl, a pro-drug of the NSAID tolmetin, on lipid peroxidation, glutathione levels and activity of antioxidant enzymes (superoxide dismutase, catalase, ..
- Nunes C, Brezesinski G, Lopes D, Lima J, Reis S, Lucio M. Lipid-drug interaction: biophysical effects of tolmetin on membrane mimetic systems of different dimensionality. J Phys Chem B. 2011;115:12615-23 pubmed publisherThis work focuses on the application of different biophysical techniques to study the interaction of tolmetin with membrane mimetic models of different dimensionality (liposomes, monolayers, and supported lipid bilayers) composed of 1,2-..
- Glassman S, Rose S, Dimar J, Puno R, Campbell M, Johnson J. The effect of postoperative nonsteroidal anti-inflammatory drug administration on spinal fusion. Spine (Phila Pa 1976). 1998;23:834-8 pubmed..The authors recommend that these drugs be avoided in the early postoperative period. ..
- Flanagan J, Yosaatmadja Y, Teague R, Chai M, Turnbull A, Squire C. Crystal structures of three classes of non-steroidal anti-inflammatory drugs in complex with aldo-keto reductase 1C3. PLoS ONE. 2012;7:e43965 pubmed publisher..This new data from ten crystal structures greatly broadens the base of structures available for future structure-guided drug discovery efforts. ..
- Arsac M, Frileux C. Comparative analgesic efficacy and tolerability of ketorolac tromethamine and glafenine in patients with post-operative pain. Curr Med Res Opin. 1988;11:214-20 pubmed..The most prominent were drowsiness and sleeping, both of which are common in post-surgical patients. ..
- Gillis J, Brogden R. Ketorolac. A reappraisal of its pharmacodynamic and pharmacokinetic properties and therapeutic use in pain management. Drugs. 1997;53:139-88 pubmed..When used in accordance with current dosage guidelines, this drug provides a useful alternative, or adjuvant, to opioids in patients with moderate to severe pain. ..
- Jett M, Ramesha C, Brown C, Chiu S, Emmett C, Voronin T, et al. Characterization of the analgesic and anti-inflammatory activities of ketorolac and its enantiomers in the rat. J Pharmacol Exp Ther. 1999;288:1288-97 pubmed..Therefore, the physicochemical and pharmacokinetics properties of (R,S)-ketorolac may optimize the concentrations of (S)-ketorolac at its biological target(s), resulting in greater efficacy and potency in vivo. ..