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Topic:Ketoprofen

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) commonly used in equine medicine to manage pain and inflammation. It is often administered to horses dealing with conditions such as musculoskeletal disorders, post-surgical pain, and laminitis. Ketoprofen functions by inhibiting the cyclooxygenase (COX) enzymes, which play a role in the inflammatory process. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacokinetics, efficacy, safety, and clinical applications of ketoprofen in horses.
Single-dose nonsteroidal anti-inflammatory drugs in horses have no impact on concentrations of cytokines or growth factors in autologous protein solution and platelet-rich plasma.
American journal of veterinary research    February 15, 2024   Volume 85, Issue 4 doi: 10.2460/ajvr.23.11.0258
Brown KA, Gregorio EN, Barot D, Usimaki A, Linardi RL, Missanelli JR, You Y, Robinson MA, Ortved KF.To determine the effects of a single dose of the NSAIDs phenylbutazone, firocoxib, flunixin meglumine, and ketoprofen on concentrations of growth factors and cytokines in autologous protein solution (APS) and platelet-rich plasma (PRP). Methods: 6 adult university-owned horses. Methods: For the first phase, 6 horses were randomized to receive ketoprofen (1,000 mg) or flunixin meglumine (500 mg) IV. Blood was obtained and processed for APS (Pro-Stride) and PRP (Restigen) before and 6 hours after administration of NSAIDs. Horses underwent a 2-week washout period, after which the protocol was rep...
Analgesic Efficacy of Non-Steroidal Anti-Inflammatory Drug Therapy in Horses with Abdominal Pain: A Systematic Review.
Animals : an open access journal from MDPI    November 8, 2023   Volume 13, Issue 22 doi: 10.3390/ani13223447
Citarella G, Heitzmann V, Ranninger E, Bettschart-Wolfensberger R.This systematic review aimed to identify the evidence concerning the analgesic efficacy of non-steroidal anti-inflammatory drugs to treat abdominal pain in horses, and to establish whether one non-steroidal anti-inflammatory drug could provide better analgesia compared to others. This systematic review was conducted following the "Systematic Review Protocol for Animal Intervention Studies". Research published between 1985 and the end of May 2023 was searched, using three databases, namely, PubMed, Embase, and Scopus, using the words equine OR horse AND colic OR abdominal pain AND non-steroidal...
Ketoprofen in horses: Metabolism, pharmacokinetics, and effects on inflammatory biomarkers.
Drug testing and analysis    July 13, 2023   doi: 10.1002/dta.3543
Knych HK, McKemie DS, Kass PH, Stanley SD, Blea J.Ketoprofen is an anti-inflammatory drug that is commonly administered to racehorses for the alleviation of musculoskeletal pain and inflammation. This study represents a comprehensive examination of the metabolism (in vivo and in vitro), pharmacokinetics and ex vivo pharmacodynamics, of ketoprofen in horses. The in vitro metabolism as well as specific enzymes responsible for metabolism was determined by incubating liver microsomes and recombinant CYP450 and UGT enzymes with ketoprofen. For the in vivo portion, 15 horses were administered a single intravenous dose of 2.2-mg/kg ketoprofen. Blood...
Comparison of Flunixin Meglumine, Meloxicam and Ketoprofen on Mild Visceral Post-Operative Pain in Horses.
Animals : an open access journal from MDPI    February 21, 2022   Volume 12, Issue 4 doi: 10.3390/ani12040526
Lemonnier LC, Thorin C, Meurice A, Dubus A, Touzot-Jourde G, Couroucé A, Leroux AA.The analgesic efficacy of meloxicam and ketoprofen against equine visceral pain is unclear. The aim of this study was to compare the analgesic efficacy of meloxicam (M) and ketoprofen (K) to flunixin meglumine (F) following inguinal castration. Horses undergoing inguinal castration under general anesthesia were randomly assigned F (1.1 mg/kg), M (0.6 mg/kg) or K (2.2 mg/kg) intravenously two hours pre-operatively and 24 h later. A pain score (out of 31) was recorded blindly by a senior clinician and veterinary student before NSAIDs administration (T0), and after the first (T1) and second (T2) ...
Pharmacokinetics of ketoprofen enantiomers following intravenous and oral administration to exercised Thoroughbred horses.
Veterinary journal (London, England : 1997)    May 7, 2016   Volume 207 196-198 doi: 10.1016/j.tvjl.2015.09.018
Knych HK, Arthur RM, Steinmetz S, McKemie DS.Ketoprofen (KTP) is currently only available as an injectable formulation for intravenous administration to horses. The primary goal of the study reported here was to characterize the pharmacokinetics of KTP, including determination of bioavailability following oral administration of the currently available injectable formulation as well as a paste formulation. KTP was administered intravenously and orally, and blood and urine samples were collected at various time points up to 96 h. KTP enantiomer concentrations were determined using LC–MS/MS, and pharmacokinetic analyses were performed. Me...
Modulatory effects of non-steroidal anti-inflammatory drugs on the luminol and lucigenin amplified chemiluminescence of equine neutrophils.
Veterinary research communications    October 21, 2011   Volume 36, Issue 1 29-33 doi: 10.1007/s11259-011-9507-5
Benbarek H, Ayad A, Deby-Dupont G, Boukraa L, Serteyn D.The purpose of this study was to explore the potential modulation of equine neutrophil oxidative burst by a series of classical NSAIDs which was subsequently monitored by the luminol or lucigenin-enhanced chemiluminescence (CL) technique. A significant dose-dependent inhibition of the luminol CL was observed with the majority of investigated drugs. This inhibition was very significant for phenylbutazone and Indomethacin; while for aspirin, a higher concentration is required. The action of Ketoprofen was significant during the first 5 min and only when the concentration was above 1 mM. Indometh...
Cathodic iontophoresis of ketoprofen over the equine middle carpal joint.
Equine veterinary journal    November 27, 2001   Volume 33, Issue 6 614-616 doi: 10.2746/042516401776563427
Eastman T, Panus PC, Honnas CM, Ferslew KE, Blackford J, Doherty TJ.No abstract available
In vitro effects of cyclooxygenase inhibitors in whole blood of horses, dogs, and cats.
American journal of veterinary research    November 13, 2001   Volume 62, Issue 11 1755-1760 doi: 10.2460/ajvr.2001.62.1755
Brideau C, Van Staden C, Chan CC.To determine potency and selectivity of nonsteroidal anti-inflammatory drugs (NSAID) and cyclooxygenase- (COX-) specific inhibitors in whole blood from horses, dogs, and cats. Methods: Blood samples from 30 healthy horses, 48 healthy dogs, and 9 healthy cats. Methods: Activities of COX-1 and COX-2 were determined by measuring coagulation-induced thromboxane and lipopolysaccharide-induced prostaglandin E2 concentrations, respectively, in whole blood with and without the addition of various concentrations of phenylbutazone, flunixin meglumine, ketoprofen, diclofenac, indomethacin, meloxicam, car...
Application of the restricted-access precolumn packing material alkyl-diol silica in a column-switching system for the determination of ketoprofen enantiomers in horse plasma.
Journal of chromatography. A    March 29, 2000   Volume 871, Issue 1-2 153-161 doi: 10.1016/s0021-9673(99)01089-4
Baeyens WR, Van der Weken G, Haustraete J, Aboul-Enein HY, Corveleyn S, Remon JP, García-Campaña AM, Deprez P.The group of LiChrospher ADS (alkyl-diol silica) sorbents that make part of a unique family of restricted-access materials, have been developed as special packings for precolumns used in the LC-integrated sample processing of biofluids. The advantage of these sorbents lies in the direct injection of untreated biological fluids, that is without sample clean-up, the elimination of the protein matrix with a quantitative recovery together with an on-column enrichment. The present method is based on previous work applying UV detection at 260 nm for ketoprofen determinations. Plasma samples introduc...
Bioavailability of racemic ketoprofen in healthy horses following rectal administration.
Research in veterinary science    September 30, 1999   Volume 67, Issue 2 203-204 doi: 10.1053/rvsc.1999.0303
Corveleyn S, Henrist D, Remon JP, Van Der Weken G, Baeyens W, Haustraete J, Aboul-Enein HY, Sustronck B, Deprez P.Ketoprofen (KTP) is a chiral non-steroidal anti-inflammatory drug (NSAID) of the propionic acid class, approved by the FDA for the allevation of pain associated with musculoskeletal disorders in horses. The present study was designed to examine the bioavailability of ketoprofen enantiomers after rectal administration of the racemate to healthy horses. One gram of racemic ketoprofen was injected intravenously and administered rectally as a fat based suppository in a cross-over design study (n = 4). Blood samples were analysed for KTP enantiomers using HPLC. After IV administration, the S(+) ena...
In vitro effects of nonsteroidal anti-inflammatory agents and prostaglandins I2, E2, and F2alpha on contractility of taenia of the large colon of horses.
American journal of veterinary research    August 18, 1999   Volume 60, Issue 8 1004-1009 
Van Hoogmoed L, Rakestraw PC, Snyder JR, Harmon FA.To determine the in vitro effect of various prostaglandins (PG) and nonsteroidal anti-inflammatory drugs (NSAID) on contractile activity of the large-colon taenia of horses. Methods: 14 healthy horses. Methods: The taenia was collected from the ventral colon, cut into strips (2 X 10 mm), and mounted in a tissue bath system (20-ml capacity) that contained oxygenated Krebs buffer solution warmed to 37.5+/-0.5 C. After equilibration, incremental doses of PGE2, PGF2alpha, PGl2, flunixin meglumine, carprofen, ketoprofen, and phenylbutazone were added to the baths, and contractile activity was recor...
Effect of a conjugate of polymyxin B-dextran 70 in horses with experimentally induced endotoxemia.
American journal of veterinary research    January 26, 1999   Volume 60, Issue 1 68-75 
MacKay RJ, Clark CK, Logdberg L, Lake P.To determine the efficacy of polymyxin B-dextran 70 (PBD) for treatment of endotoxemic horses. Methods: 15 horses during study 1 and 6 horses during study 2. Methods: 3 groups were used in study 1. Horses in groups 1 and 2 were given 30 ng of lipopolysaccharide (LPS)/kg of body weight, IV, over 60 minutes. Horses in group 3 were given saline (0.9% NaCl) solution. Beginning 15 minutes before LPS infusion and continuing for 75 minutes, horses in groups 1 and 3 were given PBD, IV. Horses in group 2 were given dextran 70. Blood samples were obtained for hemograms and determination of cytokine, lac...
Comparative narrow-bore high-performance liquid chromatographic determination of ketoprofen in horse plasma.
Biomedical chromatography : BMC    July 1, 1998   Volume 12, Issue 3 167-169 doi: 10.1002/(SICI)1099-0801(199805/06)12:3<167::AID-BMC798>3.0.CO;2-5
Baeyens WR, Van der Weken G, Van Overbeke A, Corveleyn S, Remon JP, Deprez P.No abstract available
Stereospecific pharmacokinetics of free and protein-bound ketoprofen in serum and synovial fluid of horses after intravenous and intramuscular administration.
American journal of veterinary research    June 12, 1998   Volume 59, Issue 6 739-743 
Brink P, DeGraves F, Ravis WR, Johansen D, Campbell JD, Duran SH.To determine intravascular and intrasynovial pharmacokinetics of the R and S enantiomers of ketoprofen after i.v. and i.m. administration to horses. Methods: 6 healthy adult mares. Methods: Horses were weighed and ketoprofen (2.2 mg/kg of body weight) was administered i.v. Blood and synovial fluid samples were obtained and analyzed for concentrations of the R and S enantiomers by means of a modified reverse-phase stereospecific high-pressure liquid chromatographic method. Three weeks later, the procedure was repeated, except that ketoprofen was given IM. Protein binding of ketoprofen enantiome...
Pharmacokinetics of ketoprofen in healthy foals less than twenty-four hours old.
American journal of veterinary research    April 2, 1998   Volume 59, Issue 3 290-292 
Wilcke JR, Crisman MV, Scarratt WK, Sams RA.To determine pharmacokinetic variables that describe disposition of ketoprofen after its i.v. administration to foals < 24 hours old. Methods: 6 healthy foals (1 male and 5 females); mean age, 12.5 (range, 8.5 to 17) hours at time of dose administration. Methods: Ketoprofen was administered i.v. to foals at a dosage of 2.2 mg/kg of body weight. Ketoprofen concentration in plasma samples was analyzed, using high-performance liquid chromatography. Concentration versus time profiles were analyzed according to standard pharmacokinetic techniques. Blood samples were obtained from foals by jugula...
Intramuscular bioavailability of ketoprofen lysine salt in horses.
The veterinary quarterly    June 1, 1997   Volume 19, Issue 2 65-68 doi: 10.1080/01652176.1997.9694743
Anfossi P, Villa R, Montesissa C, Carli S.Lysine salts are often used in human pharmaceuticals to increase the solubility and absorption of acidic drugs when these are administered parenterally. In this study the intramuscular bioavailability of ketoprofen administered as the lysine salt was evaluated in horses (n = 5) treated intravenously and intramuscularly (2.2 mg/kg active substance) in a cross-over study. The absorption rate of ketoprofen administered as the lysine salt was rather low: the mean residence time increased from 31.7 min after IV injection to 128.9 min (after IM injection), and the bioavailability was high (mean 92.4...
Pharmacokinetics and pharmacodynamics of ketoprofen enantiomers in the horse.
Journal of veterinary pharmacology and therapeutics    December 1, 1996   Volume 19, Issue 6 466-474 doi: 10.1111/j.1365-2885.1996.tb00084.x
Landoni MF, Lees P.Pharmacokinetic and pharmacodynamic parameters were established for enantiomers of the non-steroidal anti-inflammatory drug (NSAID) ketoprofen (KTP), each administered separately at a dose level of 1.1 mg/kg to a group of six New Forest geldings, in a three-period cross-over study using a tissue cage model of inflammation. For both S(+)-and R(-)-KTP, penetration into tissue cage fluid (transudate) and inflamed tissue cage fluid (exudate) was rapid, and clearances from exudate and transudate were much slower than from plasma. AUC values were, therefore, higher for exudate and, to a lesser degre...
Bioavailability of ketoprofen in horses after rectal administration.
Journal of veterinary pharmacology and therapeutics    October 1, 1996   Volume 19, Issue 5 359-363 doi: 10.1111/j.1365-2885.1996.tb00064.x
Corveleyn S, Deprez P, Van der Weken G, Baeyens W, Remon JP.Six healthy mares ranging in age from 6 to 12 years and weighing from 415 to 540 kg were used to determine the rectal bioavailability of ketoprofen. For the rectal administration, three different formulations, each containing 1 g of ketoprofen, were administered in a fatty and a hydrophilic suppository base and as a liquid suspension. An average elimination half-life of 1.3 h (+/-1.2) was found. The average value for the total plasma clearance (ClT) was 131.9mL/ min.kg (range 95-183.5). The volume of distribution Vd(area) was 255 mL/kg and the mean residence time (MRT) value was 0.47 h. After ...
Pharmacokinetics of ketoprofen in the donkey (Equus asinus).
Zentralblatt fur Veterinarmedizin. Reihe A    September 1, 1996   Volume 43, Issue 7 423-426 doi: 10.1111/j.1439-0442.1996.tb00470.x
Oukessou M, Bouljihad M, Van Gool F, Alvinerie M.The pharmacokinetic parameters of ketoprofen were determined in four donkeys after a single intravenous injection of a dose of 2.2 mg/kg body weight. The total body clearance (ClB) was 414.0 +/- 98.70 ml/h/kg (mean +/- SD), the volume of distribution at steady state (Vss) 263.10 +/- 55.43 ml/kg and the elimination half-life 1.30 +/- 0.75 h. These values were compared to those obtained in horses.
Effects of ketoprofen and phenylbutazone on chronic hoof pain and lameness in the horse.
Equine veterinary journal    July 1, 1995   Volume 27, Issue 4 296-300 doi: 10.1111/j.2042-3306.1995.tb03080.x
Owens JG, Kamerling SG, Stanton SR, Keowen ML.The analgesic effects of the nonsteroidal anti-inflammatory drugs, ketoprofen (2.2 and 3.63 mg/kg bwt) and phenylbutazone (4.4 mg/kg bwt) were compared in 7 horses with chronic laminitis. Hoof pain was quantified objectively by means of an electronic hoof tester and lameness was subjectively graded on a modified Obel scale. Ketoprofen at a dose of 3.63 mg/kg bwt (phenylbutazone equimolar dose) reduced hoof pain and lameness to a greater extent than the 2.2 mg/kg dose and phenylbutazone. These effects were still present at 24 h in 3 of the 4 pain tests, including lameness grade. These data sugg...
Pharmacokinetics of ketoprofen in healthy horses and horses with acute synovitis.
Journal of veterinary pharmacology and therapeutics    June 1, 1995   Volume 18, Issue 3 187-195 doi: 10.1111/j.1365-2885.1995.tb00577.x
Owens JG, Kamerling SG, Barker SA.The pharmacokinetic properties of a single intravenous dose of ketoprofen (2.2 mg/kg) in plasma and synovial fluid were compared in four healthy animals and four horses with experimentally induced acute synovitis. Synovitis was induced by the injection of a 1% solution of sterile carrageenan into the left intercarpal joint. Ketoprofen was administered at the same time as carrageenan infection. The plasma disposition followed a biexponential equation or a two-compartment model in most horses. The plasma harmonic mean half-life in healthy horses (0.88 h) was longer than in horses with synovitis ...
Comparison of the effects of ketoprofen and flunixin meglumine on the in vitro response of equine peripheral blood monocytes to bacterial endotoxin. Jackman BR, Moore JN, Barton MH, Morris DD.The purpose of this study was to investigate the in vitro effects of flunixin meglumine, a cyclo-oxygenase inhibitor, and ketoprofen, a reported cyclo-oxygenase and lipoxygenase inhibitor, on the synthesis of cyclo-oxygenase end-products thromboxane B2 and prostaglandin E2, lipoxygenase derived 12-hydroxyeicosatetraenoic acid, tumor necrosis factor and tissue factor. Six adult horses were each randomly administered flunixin meglumine (1.1 mg/kg) or ketoprofen (2.2 mg/kg) intravenously every 12 hours with the drug treatments separated by two weeks. Blood samples were obtained prior to initiatin...
Enantioselective pharmacokinetics of ketoprofen in horses.
Journal of veterinary pharmacology and therapeutics    September 1, 1993   Volume 16, Issue 3 373-376 doi: 10.1111/j.1365-2885.1993.tb00185.x
Jaussaud P, Bellon C, Besse S, Courtot D, Delatour P.No abstract available
[Comparative enantioselectivity of the disposition of two non-steroidal anti-inflammatory agents, ketoprofen and carprofen, in man and animals].
Bulletin de l\'Academie nationale de medecine    March 1, 1993   Volume 177, Issue 3 515-527 
Delatour P, Benoit E, Bourdin M, Gobron M, Moysan F.After the administration of racemic ketoprofen and carprofen to man, both enantiomers of each compound exhibit similar plasma profiles. This contrasts with the rat where the active S(+) enantiomer is predominant. For carprofen, regardless of the route of administration, the R(-) enantiomer is predominant in the plasma of all investigated animal species. The S(+)/R(-) ratio of the "areas under the curves" during the time course of the kinetics, is: 0.60 in dogs, 0.53 in Yucatan micro-pigs, 0.48 in mini-goats, 0.67 in calves and 0.19 in horses. For ketoprofen, the S(+) enantiomer is predominant ...
Identification of a benzhydrolic metabolite of ketoprofen in horses by gas chromatography-mass spectrometry and high-performance liquid chromatography.
Journal of chromatography    December 2, 1992   Volume 583, Issue 2 167-173 doi: 10.1016/0378-4347(92)80549-6
Benoit E, Jaussaud P, Besse S, Videmann B, Courtot D, Delatour P, Bonnaire Y.A benzhydrolic metabolite of ketoprofen, formed by reduction of the keto group of the drug, has been identified by gas chromatography-mass spectrometry in equine plasma and urine. After partial synthesis, its structure has been confirmed by UV, IR and 1H NMR spectroscopy. The kinetics of ketoprofen and this metabolite have been monitored in plasma by high-performance liquid chromatography. The two products were quantified in plasma up to 4 and 3 h, respectively, and were detected in urine up to 72 and 24 h, respectively, after a single intravenous administration to horses at the dose of 2.2 mg...