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Topic:NSAID

Non-steroidal anti-inflammatory drugs (NSAIDs) are a class of medications commonly used in horses to manage pain and inflammation. These drugs work by inhibiting enzymes involved in the inflammatory process, specifically cyclooxygenase (COX) enzymes, which play a role in the production of prostaglandins. NSAIDs are frequently administered for conditions such as musculoskeletal disorders, colic, and post-surgical pain. Common NSAIDs used in equine medicine include phenylbutazone, flunixin meglumine, and ketoprofen. While effective, the use of NSAIDs in horses requires careful management due to potential side effects, such as gastrointestinal ulceration and renal impairment. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacology, therapeutic applications, and safety considerations of NSAIDs in equine practice.
Disposition of human drug preparations in the horse. VI. Tiaprofenic acid.
Journal of chromatography. B, Biomedical sciences and applications    March 28, 1998   Volume 704, Issue 1-2 207-214 doi: 10.1016/s0378-4347(97)00461-1
Delbeke FT, Baert K, De Backer P.Urinary and plasma concentrations of the nonsteroidal anti-inflammatory drug tiaprofenic acid were determined following oral and intramuscular administration of a dose of 1 g to five fasted horses. Quantitation was performed by high-performance liquid chromatography (HPLC). The limit of quantitation (LOQ) was 0.1 microg/ml and 0.5 microg/ml in 2 ml plasma and 1 ml urine, respectively. Assay precision and extraction recovery were between acceptable values. Tiaprofenic acid pharmacokinetics were described by non-compartment analysis of the data. Absorption was faster after oral administration as...
A toxicity study of eltenac, a nonsteroidal anti-inflammatory drug, in horses.
Journal of veterinary pharmacology and therapeutics    March 21, 1998   Volume 21, Issue 1 24-33 doi: 10.1046/j.1365-2885.1998.00813.x
Goodrich LR, Furr MO, Robertson JL, Warnick LD.A double-blind study was performed, in horses, to determine the potential toxic effects of the nonsteroidal anti-inflammatory drug, eltenac(4-[(2,6-dichlorophenyl) amino]-3-thiopheneacetic acid). Four treatment groups of six horses were formed. The drug was injected intravenously, once daily, at a dose level of 0.5 mg/kg, 1.5 mg/kg or 2.5 mg/kg for 15 days. A control group was injected with sterile saline solution. Horses were monitored for changes in appetite, physical examinations, biochemical evaluations and gastroscopic examinations. Complete post-mortem examinations were also performed. A...
Enostosis-like lesions in the long bones of 10 horses: scintigraphic and radiographic features.
Equine veterinary journal    February 12, 1998   Volume 30, Issue 1 35-42 doi: 10.1111/j.2042-3306.1998.tb04086.x
Bassage LH, Ross MW.Ten horses admitted for lameness evaluation including bone scintigraphy had enostosis-like lesions, described scintigraphically as focal or multifocal areas of intense increased radioisotope uptake within the medullary cavity of one or more long bones, and radiographically as one or multiple round to irregularly shaped radiopacities within the medullary cavity, often in close proximity to the nutrient foramen. There were 6 Thoroughbreds, one male, one female and 4 geldings, 3 Standardbreds, all geldings and one Appaloosa gelding; age 3-10 years. Enostosis-like lesions were seen in the tibia (5...
Treatment of horses with phenylbutazone.
The Veterinary record    January 10, 1998   Volume 141, Issue 22 584 
Dyson S.No abstract available
[Effect of flunixin meglumine on plasma prostanoid concentrations in horses with colic in the perioperative period].
DTW. Deutsche tierarztliche Wochenschrift    December 31, 1997   Volume 104, Issue 9 365-368 
Gerdemann R, Deegen E, Kietzmann M, Venner M.In the present study the significance of eicosanoids in the development of shock in horses on the basis of ileus has been investigated using the prostanoids thromboxane B2 (TXB2) and prostaglandine E2 (PGE2) as indicators. The prostanoid synthesis inhibitor flunixin meglumine was to be examined regarding its efficacy in the effective blockade of the synthesis of these mediators within the peri-operative timeframe as well as its effects on clinical signs and laboratory parameters. 21 horses suffering from ileus and ready for surgical intervention received an intravenous flunixin dosis of 1.1 mg...
Survey of diplomates of the American College of Veterinary Surgeons regarding postoperative intra-abdominal adhesion formation in horses undergoing abdominal surgery.
Journal of the American Veterinary Medical Association    December 31, 1997   Volume 211, Issue 12 1573-1576 
Southwood LL, Baxter GM, Hutchison JM, Shuster R.To obtain information from specialists in equine surgery as to prevalence of, predisposing factors for, and methods to prevent postoperative adhesion formation in horses undergoing abdominal surgery. Methods: Survey. Methods: Surveys were mailed to 196 diplomates of the American College of Veterinary Surgeons involved in equine practice. Results: 60 (31%) surveys were returned. Most respondents (55/60) routinely informed clients of the risk of postoperative adhesion formation in horses with small intestinal lesions. When asked after which procedures they routinely used measures to prevent adhe...
Use of carprofen in racehorses.
The Veterinary record    November 19, 1997   Volume 141, Issue 15 400 
Balmer T, Curwen A.No abstract available
Current concepts in management of abdominal adhesions.
The Veterinary clinics of North America. Equine practice    August 1, 1997   Volume 13, Issue 2 415-435 doi: 10.1016/s0749-0739(17)30248-1
Southwood LL, Baxter GM.Adhesions are an important complication after abdominal surgery in horses and foals, especially after small intestinal resection and anastomosis. Prevention therapies used in horses have included nonsteroidal anti-inflammatory drugs, antibiotics, heparin, dimethyl sulfoxide, carboxymethylcellulose, and meticulous surgical technique; however, the ideal surgical technique and prevention therapy has not been determined. Further, treatment of abdominal adhesions has a poor prognosis, emphasizing the need for improvements in prevention methods.
Effects of flunixin meglumine on short circuit current in equine colonic mucosa in vitro.
American journal of veterinary research    August 1, 1997   Volume 58, Issue 8 915-919 
Freeman DE, Inoue OJ, Eurell TE.To study the effect of flunixin meglumine on short circuit current (Isc) in equine right ventral colon in vitro. Methods: Intestinal mucosa from healthy horses and ponies. Methods: Isc was measured in mucosa from the right ventral colon mounted in Ussing chambers. In experiment 1, collection and incubation solutions were: control (no additions); flunixin meglumine, 4 micrograms/ml; indomethacin, 10(-6) M; and flunixin meglumine (4 micrograms/ml) with 10(-6) M prostaglandin E2. In experiment 2, incubation conditions were: control [plain Krebs-Ringer bicarbonate [KRB] solution]; flunixin meglumi...
A unique metabolite of nimesulide.
Journal of analytical toxicology    May 1, 1997   Volume 21, Issue 3 197-202 doi: 10.1093/jat/21.3.197
Sarkar P, McIntosh JM, Leavitt R, Gouthro H.Nimesulide is a nonsteroidal anti-inflammatory drug recently detected in equine blood and urine samples taken at the race track. The detection of the drug in a blood sample led to the identification of an unknown thin-layer chromatographic (TLC) spot in track urine samples as a metabolite of nimesulide. Characterization of the unknown TLC spot and comparison with the synthesized compound shows that the unknown TLC spot is a previously unreported equine metabolite of nimesulide. The metabolite was identified as resulting from the reduction of the nitro group on nimesulide to an amino group. Thi...
Adverse reactions to veterinary drugs reported in Sweden during 1991-1995.
Journal of veterinary pharmacology and therapeutics    April 1, 1997   Volume 20, Issue 2 105-110 doi: 10.1046/j.1365-2885.1997.00050.x
Tjälve H.The present article gives a summary of suspected adverse reactions reported by Swedish veterinarians during the period 1991-1995. The summary shows that severe adverse drug-reactions sometimes occur in Swedish veterinary practice. In horses, several cases of acute reactions in animals treated with procaine benzylpenicillin were reported and seven horses died within a few minutes after intramuscular injections of the drug. In cattle and swine most reports referred to the use of antimicrobial agents. In dogs reactions to vaccines were the most frequently reported adverse effects. The reactions w...
Determination of an effective dose of eltenac and its comparison with that of flunixin meglumine in horses after experimentally induced carpitis.
American journal of veterinary research    March 1, 1997   Volume 58, Issue 3 298-302 
Hamm D, Turchi P, Johnson JC, Lockwood PW, Thompson KC, Katz T.To titrate a clinically effective eltenac dosage (0.1, 0.5, and 1.0 mg/kg of body weight), compared with vehicle only, and to compare efficacy of the most effective eltenac dosage with that of 1.1 mg of flunixin meglumine/kg. Methods: 40 healthy horses, ranked after model induction on the basis of lameness severity, were randomly assigned to 5 treatment groups, with 4 replicates of 10 horses each. Methods: On day -5, after surgical preparation of the left carpal region, 0.7 ml of Freund's complete adjuvant was injected into the intercarpal space. Horses were observed daily, from the day of car...
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...
Effects of flunixin, tolfenamic acid, R(-) and S(+) ketoprofen on the response of equine synoviocytes to lipopolysaccharide stimulation.
Equine veterinary journal    November 1, 1996   Volume 28, Issue 6 468-475 doi: 10.1111/j.2042-3306.1996.tb01619.x
Landoni MF, Foot R, Frean S, Lees P.The objective of this study was to analyse the effects of 4 nonsteroidal anti-inflammatory drugs (NSAIDs) on the production of beta-glucuronidase (beta-glu), tumour necrosis factor alpha (TNF alpha), interleukin-6 (IL-6), interleukin-1 (IL-1) and prostaglandin E2 (PGE2) by lipopolysaccharide (LPS)-stimulated equine synoviocytes. The agents studied were flunixin, tolfenamic acid, S(+)ketoprofen (KTP) and R(-)ketoprofen. LPS-induced release of beta-glu from synoviocytes was inhibited in a concentration dependent manner by all 4 compounds, tolfenamic acid being the most potent. Of the 2 KTP enant...
Factors associated with gastric lesions in thoroughbred racehorses.
Equine veterinary journal    September 1, 1996   Volume 28, Issue 5 368-374 doi: 10.1111/j.2042-3306.1996.tb03107.x
Murray MJ, Schusser GF, Pipers FS, Gross SJ.Gastroscopic examinations were performed on 67 Thoroughbred horses in training at a race track and repeat examinations performed in 35 horses, 2 to 3 months later. Horses were age 2-9 years and included 16 two-year-olds, 32 three-year-olds and 19 horses > or = 4-years-old. Forty-two of the 67 horses had raced within the 2 months before the initial examination and the remaining 25 horses were in training. Sixty-two of the 67 horses (93%) had one or more lesions present in the gastric mucosa and lesions were present in all of the 42 horses that had raced. Thirty-two of the 35 horses, examined...
Pulmonary vascular pressures of strenuously exercising thoroughbreds after administration of phenylbutazone.
American journal of veterinary research    September 1, 1996   Volume 57, Issue 9 1354-1358 
Manohar M, Goetz TE, Griffin R, Sullivan E.To determine the effects of phenylbutazone administration on heart rate and right atrial and pulmonary vascular pressures in Thoroughbreds during rest and during exercise performed at maximal heart rate. Methods: 7 healthy, exercise-conditioned Thoroughbreds. Methods: Horses were studied on 3 occasions: without medication [control], after i.v. administration of phenylbutazone (4.4 mg/kg of body weight) at 12-hour intervals for 2 days and a final dose given 1 hour before exercise, and after i.v. administration of phenylbutazone for 2 days in the same manner, but with the final dose given 24 hou...
Phenylbutazone increases right atrial pressure and heart rate of running horses.
Journal of applied physiology (Bethesda, Md. : 1985)    July 1, 1996   Volume 81, Issue 1 312-317 doi: 10.1152/jappl.1996.81.1.312
Mitten LA, Hinchcliff KW, Pate JL.The effect of inhibition of cyclooxygenase activity on the hemodynamic response to exertion was examined in 6 horses. Rates of O2 consumption and CO2 production and carotid, pulmonary arterial, and right atrial pressures were measured while the horses performed a standardized exercise test on a treadmill after treatment with phenylbutazone or a placebo. Phenylbutazone (8.8 mg/kg p.o. for 2 days and 4.4 mg/kg i.v. 60 min before exertion) abolished the exertion-induced increases in plasma 6-ketoprostaglandin F1 alpha and thromboxane B2 concentrations, confirming inhibition of cyclooxygenase acti...
Protein binding and in vitro serum thromboxane B2 inhibition by flunixin meglumine and meclofenamic acid in dog, goat and horse blood.
Research in veterinary science    July 1, 1996   Volume 61, Issue 1 78-81 doi: 10.1016/s0034-5288(96)90115-0
Galbraith EA, McKellar QA.Flunixin was highly protein bound in the serum of dogs (92.2 per cent), goats (84.8 per cent) and horses (86.9 per cent). Meclofenamic acid was also highly protein bound, although there were larger differences between the extent of the binding in dogs (90.3 per cent), goats (84.7 per cent) and horses (99.8 per cent). Both flunixin and meclofenamic acid were potent inhibitors of the in vitro generation of thromboxane (Tx) B2 in blood. Flunixin inhibited the generation of TxB2 by 50 per cent of the maximum response (IC50) in dog, goat and horse blood at concentrations of 0.10, 0.02 and 0.04 micr...
Effects of pretreatment with ketoprofen and phenylbutazone on experimentally induced synovitis in horses.
American journal of veterinary research    June 1, 1996   Volume 57, Issue 6 866-874 
Owens JG, Kamerling SG, Stanton SR, Keowen ML, Prescott-Mathews JS.To compare the analgesic and anti-inflammatory effects of the nonsteroidal anti-inflammatory drugs (NSAID), ketoprofen (2.20 and 3.63 mg/kg of body weight) and phenylbutazone (4.40 mg/kg), in an acute equine synovitis model. Methods: 4 groups of 6 horses received NSAID or saline solution in a randomized design. Methods: 24 clinically normal mares and geldings. Methods: Left intercarpal joints were injected with sterile carrageenan to induce synovitis at the same time as IV administration of NSAID or saline solution. Clinical assessments were made and synovial fluid was withdrawn at 0, 1, 3, 6,...
Rattlesnake venom poisoning in horses: 32 cases (1973-1993).
Journal of the American Veterinary Medical Association    June 1, 1996   Volume 208, Issue 11 1866-1871 
Dickinson CE, Traub-Dargatz JL, Dargatz DA, Bennett DG, Knight AP.To determine the clinical manifestations, morbidity, mortality, and treatment methods for rattlesnake venom poisoning in horses. Methods: Retrospective analysis of medical records. Methods: 27 horses with acute venom poisoning attributable to prairie rattlesnakes, and 5 with chronic problems subsequent to a rattlesnake bite. Results: Most horses were bitten on or near the muzzle while on pasture, resulting in head swelling, dyspnea, and epistaxis. Additional manifestations of acute poisoning included fever, tachycardia, tachypnea, cardiac arrhythmia, hemolytic anemia, thrombocytopenia, hemorrh...
Metacarpophalangeal joint synovial pad fibrotic proliferation in 63 horses.
Veterinary surgery : VS    May 1, 1996   Volume 25, Issue 3 199-206 doi: 10.1111/j.1532-950x.1996.tb01399.x
Dabareiner RM, White NA, Sullins KE.Medical records, radiographs, and sonograms of 63 horses with metacarpophalangeal joint synovial pad proliferation were examined retrospectively. All horses had lameness, joint effusion, or both signs associated with one or both metacarpophalangeal joints. Bony remodeling and concavity of the distodorsal aspect of the third metacarpal bone (Mc3) just proximal to the metacarpal condyles was identified by radiography in 71 joints (93%); 24 joints (32%) had radiographic evidence of a chip fracture located at the proximal dorsal aspect of the proximal phalanx. Fifty-four joints (71%) were examined...
Ultrasonographic renal changes associated with phenylbutazone administration in three foals.
The Canadian veterinary journal = La revue veterinaire canadienne    April 1, 1996   Volume 37, Issue 4 235-236 
Léveillé R, Miyabayashi T, Weisbrode SE, Biller DS, Takiguchi M, Williams JF.No abstract available
Surgical treatment of navicular syndrome in the horse using navicular suspensory desmotomy.
New Zealand veterinary journal    February 1, 1996   Volume 44, Issue 1 26-30 doi: 10.1080/00480169.1996.35927
Bell BT, Bridge IS, Sullivan ST.Seventeen horses diagnosed as having navicular syndrome on the basis of history, clinical findings, regional local anaesthesia and radiography were subjected to bilateral navicular suspensory desmotomy. Before surgery, the duration of navicular lameness ranged from 6 weeks to 4 years. Previous unsuccessful treatments prior to surgery included nonsteroidal anti-inflammatories, corrective shoeing, rest and isoxsuprine. For the seventeen horses subject to surgery, twelve horses were sound, one horse was improved and four horses were lame at a minimum of 6 months after surgery.
Detection of non-steroidal anti-inflammatory drugs in equine plasma and urine by gas chromatography-mass spectrometry.
Journal of chromatography. A    January 5, 1996   Volume 719, Issue 1 251-264 doi: 10.1016/0021-9673(95)00370-3
González G, Ventura R, Smith AK, de la Torre R, Segura J.A gas chromatographic-mass spectrometric (GC-MS) procedure for the detection of seventeen non-steroidal anti-inflammatory drugs (NSAIDs) in equine plasma and urine samples is described. The extraction of the compounds from the biological matrix was performed at acidic pH (2-3) with diethyl ether. Ethereal extracts were washed with a saturated solution of sodium hydrogencarbonate (urine) or treated with a solid mixture of sodium carbonate and sodium hydrogencarbonate (plasma). The ethereal extracts were dried and derivatized by incubation at 60 degrees C with methyl iodide in acetone in the pre...
Chiral inversion of fenoprofen in horses and dogs: an in vivo-in vitro study.
Veterinary research    January 1, 1996   Volume 27, Issue 1 13-22 
Soraci A, Jaussaud P, Benoit E, Delatour P.Fenoprofen (FPF) is a chiral non-steroid antiinflammatory drug, marketed as a racemic mixture of its R(-) and S(+) enantiomers. Its stereoselective disposition in humans and animals is due to a chiral inversion converting R(-)FPF into S(+)FPF. The first step of this reaction, which produces an acyl-CoA thioester, is catalysed by an acyl-CoA ligase. A stereospecific high performance liquid chromatography assay was used to study the disposition of FPF enantiomers in four geldings and three male beagle dogs, following intravenous doses of racemic FPF (1 mg/kg in horses), R(-)FPF (0.5 mg/kg in hor...
A partially automated pretreatment module for routine analyses for seventeen non-steroid antiinflammatory drugs in race horses using gas chromatography/mass spectrometry.
Analytical chemistry    January 1, 1996   Volume 68, Issue 1 118-123 doi: 10.1021/ac950566j
Cárdenas S, Gallego M, Valcárcel M, Ventura R, Segura J.A partially automated module for the routine determination of illicit non-steroid antiinflammatory drugs (NSAIDs) in biological fluids from race horses was built, tested, refined, and shown to work. This pretreatment module retains 17 NSAIDs on an Amberlite XAD-2 column before back-elution derivatization with methyl iodide in acetonitrile. Methylated derivatives are manually injected into a gas chromatograph connected to a mass spectrometer. The quantification limits thus achieved are 50-100 ng/mL in 1 mL of urine or plasma. The proposed method is more expeditious than its manual liquid-liquid...
The dose-related effects of phenylbutazone and a methylprednisolone acetate formulation (Depo-Medrol) on cultured explants of equine carpal articular cartilage.
Journal of veterinary pharmacology and therapeutics    December 1, 1995   Volume 18, Issue 6 429-437 doi: 10.1111/j.1365-2885.1995.tb00621.x
Jolly WT, Whittem T, Jolly AC, Firth EC.The dose-related effects of phenylbutazone and Depo-Medrol on chondrocyte viability and chondrocyte-mediated synthesis and depletion of proteoglycans were investigated using cultured explants of equine middle carpal joint articular cartilage. Explants from 12 horses (941 x 3 mm diameter) were cultured for a total of 5 days, which included 3 days' exposure to either phenylbutazone (0, 2, 20, 200 or 2000 micrograms/mL) or Depo-Medrol (0, 20, 200 or 2000 micrograms/mL). For each explant, amino sugar content was used as a measure of proteoglycan content, 35S incorporation as a measure of the rate ...
Plasma and synovial fluid kinetics, disposition, and urinary excretion of naproxen in horses.
American journal of veterinary research    August 1, 1995   Volume 56, Issue 8 1075-1080 
Soma LR, Uboh CE, Rudy JA, Perkowski SZ.Naproxen (+6-methoxy-[alpha-methyl]-2-naphthalene acetic acid) is a nonsteroidal anti-inflammatory drug that is used for the treatment of inflammatory conditions in horses. We developed a model that describes the drug's disposition and renal excretion, including synovial fluid disposition and elimination after IV administration in horses. The plasma disposition, after IV administration of 5 mg/kg of body weight, was described by a two-compartment model; mean +/- SD distribution and elimination half-lives were 1.42 +/- 0.42 and 8.26 +/- 2.56 hours, respectively. Plasma concentration of naproxen...
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...
Comparison of the anti-inflammatory actions of flunixin and ketoprofen in horses applying PK/PD modelling.
Equine veterinary journal    July 1, 1995   Volume 27, Issue 4 247-256 doi: 10.1111/j.2042-3306.1995.tb03073.x
Landoni MF, Lees P.A comparative study in horses of the pharmacokinetics (PK) and pharmacodynamics (PD) of 2 extensively used nonsteroidal anti-inflammatory drugs (NSAIDs), flunixin (FXN) and ketoprofen (KTP), was carried out applying PK/PD modelling. To evaluate the anti-inflammatory properties of these drugs a model of acute inflammation, comprising surgically implanted subcutaneous tissue cages stimulated by intracaveal injection of carrageenan, was used. FXN elimination half-life (T1/2 beta) in plasma was 3.37 +/- 1.09 h. However, in exudate a much longer T1/2 beta was obtained (15.99 +/- 3.80 h). Apparent v...
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