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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.
Attenuation by phenylbutazone of the renal effects and excretion of frusemide in horses. The objectives of this study were to determine the effect of phenylbutazone premedication on the pharmacokinetics and urinary excretion of frusemide in horses; and on frusemide-induced changes in urinary electrolyte excretion. Six Standardbred mares were used in a 3-way crossover design. The pharmacokinetics and renal effects of frusemide (1 mg/kg bwt i.v.) were studied with and without phenylbutazone premedication (8.8 mg/kg bwt per os 24 h before, followed by 4.4 mg/kg bwt i.v. 30 min before frusemide administration). A control (saline) treatment was also studied. Administration of frusemide...
In vitro effects of nonsteroidal anti-inflammatory agents and prostaglandins I2, E2, and F2alpha on contractility of taenia of the large colon of horses. 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...
Hemothorax in 2 horses. This report documents the successful conservative medical management of hemothorax in 2 horses. Hemothorax occurred after a lung biopsy procedure (horse 1) and strenuous exercise on a treadmill (horse 2). The horses had tachypnea, tachycardia, nostril flaring, hemoptysis, and pawing. Hemothorax was suspected based upon absence of auscultable ventral lung sounds; development of cool extremities and pale, tacky mucous membranes; the ultrasonographic appearance of moderate to severe amounts of pleural fluid; and a concurrent decrease in hematocrit and total plasma protein. Both horses were treate...
Pharmacokinetics of carprofen enantiomers in equine plasma and synovial fluid – a comparison with ketoprofen. Carprofen is a Non Steroidal Anti-Inflammatory Drug (NSAID) which is widely used for the treatment of musculoskeletal disorders in horses. The commercial preparation is a racemic mixture of two enantiomers (R and S carprofen). We used HPLC to measure plasma and synovial fluid R and S carprofen concentrations following a single intravenous (i.v.) dose, and computer modelling to determine the pharmacokinetic parameters of the enantiomers in these two body fluids. A comparison was made with results from an identical experiment using ketoprofen. The plasma elimination half lives of R and S carprof...
The elimination profiles of oxaprozin in equine urine and serum after a 4.8-g dose. A method for the extraction of oxaprozin from equine urine and serum and its quantitation by high-performance liquid chromatography-ultraviolet detection is presented. Confirmation of oxaprozin in postadministration extracts was accomplished by gas chromatographic- mass spectrometric analysis of methylated extracts or liquid chromatography with tandem mass spectrometry daughter ion mass spectra of underivatized extracts. Daypro, a formulation of oxaprozin, was administered orally at a dose of 4.8 g to four standardbred mares. Urine and serum samples were collected to 120 h postadministration. ...
Renal medullary rim sign in 2 adult quarter horses. This report describes a renal ultrasonographic abnormality (medullary rim sign), which was identified in 2 separate cases of spontaneously occurring disease associated with chronic and acute overdosage of phenylbutazone therapy. In horses, medullary rim sign has only been documented in neonatal foals experimentally administered large doses of phenylbutazone.
Post traumatic keratouveitis in horses. Traumatic keratouveitis in horses is characterised by a unilateral, aseptic, vascularising keratitis accompanied by moderate to severe anterior uveitis. In a series of 9 cases of post traumatic keratouveitis, topical and systemic nonsteroidal drugs and atropine were used to control the anterior uveitis while allowing spontaneous corneal healing. Among the 9 cases reported, 6 affected eyes previously treated with local corticosteroids took significantly longer to resolve when compared to 3 eyes in which corticosteroids had not been administered. It was concluded that, in cases of equine post tr...
Phenylbutazone prevents the endotoxin-induced delay in gastric emptying in horses. The effect of phenylbutazone on gastric emptying in horses was determined by measuring serum concentrations of acetaminophen. Gastric emptying was determined in normal fasted horses (n = 6), horses given endotoxin intravenously (n = 6), horses given intravenous phenylbutazone (n = 6), and horses given intravenous phenylbutazone plus endotoxin (n = 6). The mean time to reach maximum serum acetaminophen concentration (Tmax), the maximum serum concentration (Cmax), and the area under the serum acetaminophen concentration versus time curve (AUC) were compared among treatment groups. Phenylbutazone...
Review of furosemide in horse racing: its effects and regulation. Furosemide has been used empirically and has been legally approved for many years by the US racing industry for the control of exercise-induced pulmonary haemorrhage (EIPH) or bleeding. Its use in horses for this purpose is highly controversial and has been criticized by organizations outside and inside of the racing industry. This review concentrates on its renal and extra-renal actions and the possible relationship of these actions to the modification of EIPH and changes in performance of horses. The existing literature references suggest that furosemide has the potential of increasing perfo...
Use of metronidazole in equine acute idiopathic toxaemic colitis. Sixteen cases of acute idiopathic toxaemic colitis developed in a veterinary hospital over a period of three years. Before the onset of colitis, 15 horses had received antibiotics, 11 had undergone general anaesthesia and various surgical procedures, and 10 had been treated with non-steroidal anti-inflammatory drugs. The horses had acute onset, profuse watery diarrhoea, profound depression, mild to moderate abdominal pain, reduced intestinal borborygmi, tachycardia, dehydration and endotoxic shock. Leucopenia, neutropenia and pyrexia were common early indicators of impending colitis. Metronida...
HPLC on Chiralcel OJ-R for enantiomer separation and analysis of ketoprofen, from horse plasma, as the 9-aminophenanthrene derivative. Racemic ketoprofen is a non-steroidal anti-inflammatory drug used to treat musculoskeletal and colic conditions in horses. The enantioselective chiral inversion of ketoprofen administered to horses has been studied by use of cellulose tris(4-methylbenzoate), also known as Chiralcel OJ-R, as chiral stationary phase; acetonitrile - 0.02 M perchlorate buffer (pH 2.0)-methanol, 60:15:25 (v/v/v) was used as mobile phase. Before chromatography, to effect adequate chiral interaction with the chiral stationary phase ketoprofen was derivatized with 9-aminophenanthrene, under acid conditions, after soli...
Disposition of human drug preparations in the horse. VI. Tiaprofenic acid. 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. 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. 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...
[Effect of flunixin meglumine on plasma prostanoid concentrations in horses with colic in the perioperative period]. 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. 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...
Effects of flunixin meglumine on short circuit current in equine colonic mucosa in vitro. 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...
Current concepts in management of abdominal adhesions. 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.
A unique metabolite of nimesulide. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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,...
