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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.
The effects of cyclo-oxygenase inhibitors on bile-injured and normal equine colon. A potential adverse effect of cyclo-oxygenase (COX) inhibitors (nonsteroidal anti-inflammatory drugs [NSAIDs]) in horses is colitis. In addition, we have previously shown an important role for COX-produced prostanoids in recovery of ischaemic-injured equine jejunum. It was hypothesised that the nonselective COX inhibitor flunixin would retard repair of bile-injured colon by preventing production of reparative prostaglandins, whereas the selective COX-2 inhibitor, etodolac would not inhibit repair as a result of continued COX-1 activity. Segments of the pelvic flexure were exposed to 1.5 mmol/l...
Effects of anti-arthritic drugs on proteoglycan synthesis by equine cartilage. The concentration-effect relationships of phenylbutazone, indomethacin, betamethasone, pentosan polysulphate (PPS) and polysulphated glycosaminoglycan (PSGAG), on proteoglycan synthesis by equine cultured chondrocytes grown in monolayers, and articular cartilage explants were measured. The effect of PSGAG on interleukin-1beta induced suppression of proteogycan synthesis was also investigated. Proteoglycan synthesis was measured by scintillation assay of radiolabelled sulphate (35SO4) incorporation. Polysulphated glycosaminoglycan and PPS stimulated proteoglycan synthesis in chondrocyte monolay...
In vitro anion transport alterations and apoptosis induced by phenylbutazone in the right dorsal colon of ponies. To study the functional and structural responses of the right dorsal colon (RDC) of ponies to phenylbutazone (PBZ) in vitro at a concentration that could be achieved in vivo. Methods: 8 adult ponies. Methods: Short circuit current and conductance were measured in mucosa from the RDC. Tissues incubated with and without HCO3- were exposed to PBZ, bumetanide, or indomethacin. Bidirectional Cl- fluxes were determined. After a baseline flux period, prostaglandin E2 (PGE2) was added to the serosal surfaces and a second flux period followed. Light and transmission electron microscopy were performed. ...
Retrospective study of primary intention healing and sequestrum formation in horses compared to ponies under clinical circumstances. In accidental wounds, trauma and infection can result in dehiscence of primarily closed wounds and in sequestrum formation when cortical bone is exposed. In experimental studies, it has been shown that second intention healing is faster and occurs with less complications in ponies than in horses. Also, a greater initial inflammatory response was seen in ponies. Based on these experimental data, it was hypothesised that accidental wounds in ponies would heal with a lower incidence of wound dehiscence and/or sequestrum formation compared to horses. A retrospective study of 89 ponies and 422 hors...
Management of equine orthopedic pain. Pain management is an extremely vital part of equine orthopedic surgery. Providing optimum analgesia for the patient will decrease recovery time, decrease physiologic stress on the animal, and provide maximum comfort during the post-operative period. The major analgesic drug categories and routes covered are nonsteroidal anti-inflammatory drugs, local anesthetics, intra-articular drugs, and epidurals.
Effects of oral administration of phenylbutazone to horses on in vitro articular cartilage metabolism. To evaluate the effects of orally administered phenylbutazone on proteoglycan synthesis and chondrocyte inhibition by IL-1beta in articular cartilage explants of horses. Methods: 11 healthy 1- to 2-year-old horses. Methods: Horses were randomly assigned to the control (n = 5) or treated group (4.4 mg of phenylbutazone/kg of body weight, p.o., q 12 h; n = 6). Articular cartilage specimens were collected before treatment was initiated (day 0), after 14 days of treatment, and 2 weeks after cessation of treatment (day 30). Proteoglycan synthesis and stromelysin concentration in cartilage extracts ...
In vitro effects of cyclooxygenase inhibitors in whole blood of horses, dogs, and cats. 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...
Measurement of ketoprofen in horse urine using gas chromatography-mass spectrometry. A gas chromatographic-mass spectrometric (GC-MS) method for the determination of ketoprofen, a non-steroidal anti-inflammatory drug (NSAID), in horse urine by selected ion monitoring (SIM) mode is described. Urine samples (2 mL) were extracted by liquid-liquid extraction with diethyl ether. The residues were then evaporated, derivatized and injected into the GC-MS system. Validation of the GC-MS method in the SIM mode using flurbiprofen as the internal standard (IS) included linearity studies (10-10 000 ng/mL), recovery (95%) and limit of quantitation (LOQ) (10 ng/mL). The response was linear,...
Effects of intra-articular injections of bufexamac suspension in healthy horses. To evaluate the effects of intra-articular (IA) injections of bufexamac in horses, focusing particularly on the effects of bufexamac on articular cartilage. Methods: 20 Standardbreds. Methods: Horses were randomly allocated into 4 groups consisting of 5 horses each, and 20, 60, or 100 mg of bufexamac or 1 ml of sterile saline (0.9% NaCl) solution (control) was injected into 1 intercarpal joint at weekly intervals for 6 treatments (days 0, 7, 14, 21, 28, and 35). Clinical signs and results of hematologic, serum biochemical, and synovial fluid (SF) analyses and radiography were used to evaluate ...
The role of nutritional therapy in the treatment of equine Cushing’s syndrome and laminitis. Equine Cushing's syndrome, a relatively common and complex condition, is difficult to treat with conventional medicine. Cushing's syndrome involves a hyperplasia or adenoma of the anterior pituitary gland. Biochemical alterations include increased endogenous cortisol, insulin resistance, elevated adrenocorticotrophic hormone, and decreased thyroid hormone levels. Symptoms include hirsutism with no loss of the winter coat in summer, refractory laminitis, weight problems (over- or underweight), polyuria/polydipsia (Pu/Pd), frequent infections, lowered immunity to intestinal parasites, decreased ...
Owner survey of headshaking in horses. To determine signalment, history, clinical signs, duration, seasonality, and response to various treatments reported by owners for headshaking in horses. Methods: Owner survey. Methods: 109 horses with headshaking. Methods: Owners of affected horses completed a survey questionnaire. Results: 78 affected horses were geldings, 29 were mares, and 2 were stallions. Mean age of onset was 9 years. Headshaking in 64 horses had a seasonal component, and for most horses, headshaking began in spring and ceased in late summer or fall. The most common clinical signs were shaking the head in a vertical pla...
A study of ten cases of focal peritarsal infection as a cause of severe lameness in the thoroughbred racehorse: clinical signs, differential diagnosis, treatment and outcome. The differential diagnoses of tarsal joint infection, fracture and peritarsal focal infection are of particular importance in practice. The objective of the present report is to provide additional clinical data to assist in the understanding of one of these conditions. The haematological parameters, clinical signs, treatment and outcome of 10 cases of severe lameness associated with peritarsal infection are reviewed. All horses had a significant rise in rectal temperature. The majority of cases (6/10) had haematological changes consistent with acute bacterial infection on the day of first exam...
Enantiospecific pharmacokinetics of ketoprofen in plasma and synovial fluid of horses with acute synovitis. Pharmacokinetic parameters were established for enantiomers of the nonsteroidal anti-inflammatory drug (NSAID) ketoprofen (KTP) administered as the racemic mixture at a dose of 2.2 mg/kg and as separate enantiomers, each at a dose of 1.1 mg/kg to a group of six horses (five mares and one gelding). A four-period cross-over study in a LPS-induced model of acute synovitis was used. After administration of the racemic mixture S(+)KTP was the predominant enantiomer in plasma as well as in synovial fluid. Unidirectional inversion of R(-) to S(+)KTP was demonstrated but the inversion was less marked ...
Pharmacokinetics of phenylbutazone and its metabolite oxyphenbutazone in miniature donkeys. To describe the pharmacokinetics of phenylbutazone and oxyphenbutazone after IV administration in miniature donkeys. Methods: 6 clinically normal miniature donkeys. Methods: Blood samples were collected before and 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300, 360, and 480 minutes after IV administration of phenylbutazone (4.4 mg/kg of body weight). Serum was analyzed in triplicate by use of high-performance liquid chromatography for determination of phenylbutazone and oxyphenbutazone concentrations. The serum concentration-time curve for each donkey was analyzed separately to estimate model-i...
Scapulohumeral osteoarthritis in 20 Shetland ponies, miniature horses and falabella ponies. This paper describes the clinical and diagnostic features of 20 cases of scapulohumeral osteoarthritis in Shetland ponies, miniature horses and falabella ponies. The history and clinical signs were similar in all the cases Radiographically they all had consistent changes which consisted predominantly of articular osteophytes and periarticular enthesiophytes. Six of the cases had radiographic evidence of dysplasia of the scapulohumeral joint, although it was uncertain whether this was a primary or a secondary finding. No specific treatment appeared to be advantageous. At follow up, six of the p...
Acute thrombosis of limb arteries in horses with sepsis: five cases (1988-1998). A hypercoagulable condition and poor perfusion to distal extremities might occur during equine endotoxaemic or septic shock, which could cause thrombosis of limb arteries. In our review, thrombosis occurred in neonatal foals in association with gram-negative bacteraemia. In 3 older foals and adults, thrombosis was associated with inflammatory bowel disease, diarrhoea and toxaemia. All patients had been treated with broad-spectrum antibiotics, nonsteroidal antiinflammatory drugs and i.v. crystalloid solutions. Two horses received i.v. hyperimmune plasma. A generalised coagulopathy was not suspe...
Effects of anti-inflammatory drugs on lipopolysaccharide-challenged and -unchallenged equine synovial explants. To evaluate the effects of anti-inflammatory drugs on lipopolysaccharide (LPS)-challenged and -unchallenged equine synovial membrane in terms of production of prostaglandin E2 (PGE2) and hyaluronan, viability, and histomorphologic characteristics. Methods: Synovial membranes were collected from the carpal, tarsocrural, and femoropatellar joints of 6 adult horses. Methods: Synovial membranes from each horse were minced and pooled and explants were treated with one of the following: no drug (control), drug, LPS alone, or LPS and drug. Treatment drugs were phenylbutazone (PBZ), flunixin meglumine...
The role of cyclooxygenase inhibitors in repair of ischaemic-injured jejunal mucosa in the horse. Cyclooxygenase inhibitors are administered to horses to prevent endotoxin-induced elaboration of prostaglandins. However, PGE2 and PGI2 stimulate repair of injured intestine. There are 2 isoforms of cyclooxygenase: COX-1, which constitutively produces prostaglandins and COX-2, which is induced by inflammation. We hypothesised that the nonspecific cyclooxygenase inhibitor flunixin meglumine would retard repair of ischaemic intestinal injury by preventing production of reparative prostaglandins, whereas the selective COX-2 inhibitor, etodolac, would permit repair as a result of continued COX-1 p...
In vitro investigation of the effect of prostaglandins and nonsteroidal anti-inflammatory drugs on contractile activity of the equine smooth muscle of the dorsal colon, ventral colon, and pelvic flexure. To determine the in vitro effect of prostaglandin E2 (PGE2), PGF2alpha, PGI2; and nonsteroidal anti-inflammatory drugs (NSAID; ie, flunixin meglumine, ketoprofen, carprofen, and phenylbutazone) on contractile activity of the equine dorsal colon, ventral colon, and pelvic flexure circular and longitudinal smooth muscle. Methods: 26 healthy horses. Methods: Tissue collected from the ventral colon, dorsal colon, and pelvic flexure was cut into strips and mounted in a tissue bath system where contractile strength was determined. Incremental doses of PGE2, PGF2alpha,, PGI2, flunixin meglumine, carp...
Effects of phenylbutazone on bone activity and formation in horses. To determine the effects of phenylbutazone (PBZ) on bone activity and bone formation in horses. Methods: 12 healthy 1- to 2-year-old horses. Methods: Biopsy was performed to obtain unicortical bone specimens from 1 tibia on day 0 and from the contralateral tibia on day 14. Fluorochromic markers were administered IV 2 days prior to and on days 0, 10, 15, and 25 after biopsy was performed. Six horses received PBZ (4.4 mg/kg of body weight, PO, q 12 h) and 6 horses were used as controls. All horses were euthanatized on day 30 and tissues from biopsy sites, with adjacent cortical bone, were collec...
Ulceration and stricture of the right dorsal colon after phenylbutazone administration in four horses. Four cases of ulceration and stricture of the right dorsal colon were encountered. Ulceration of the right dorsal colon is generally associated with nonsteroidal anti-inflammatory drug (NSAID) toxicosis but there are few reports of stricture following ulceration. All four horses had recent phenylbutazone use: three had been given doses well in excess of the recommended dose and in one the dose was marginally above those recommended but was combined with administration of other NSAIDs. All four horses presented with intermittent low-grade colic, weight loss and ventral oedema. Diarrhoea was als...
Effects of flunixin on movement and performance of standardbred trotters on the track. An often discussed and controversial issue is the effect of nonsteroidal anti-inflammatory drugs (NSAIDs) on performance. The purpose of this study was to investigate the effect of the NSAID flunixin on the movement pattern and performance capacity of Standardbred trotters using a standardised track model. Five adult Standardbred horses in training trotted at 2 occasions with a 2 week interval on the same oval dirt track. Before each occasion the horses were either injected with flunixin meglumine (Finadyne) or normal saline solution i.m. 4 h before the performance test (double blind crossover...
Analgesia. Critical to reducing patient morbidity as well as heightened ethical awareness, alleviation of pain in animals has become integral to medical case management and surgical procedures. Pharmacotherapy is directed at peripheral nociceptors, primary and secondary spinal neurons, and pain-processing areas in the CNS. Accordingly, three primary pharmacologic strategies have evolved: drugs that bind to and activate opioid receptors, drugs that bind to and activate alpha 2 receptors, and drugs that reduce de novo prostaglandin synthesis. In horses, the two predominant types of pain encountered are mus...
Modes of local drug delivery to the musculoskeletal system. A number of methods for the local delivery of drugs to musculoskeletal tissues in the horse are now available. Further research is required to document the disposition of drugs delivered by such methods and to correlate this information with efficacy. Perhaps the greatest potential area for the methods discussed is the treatment of synovial and bone infections. To be able to provide high and sustained therapeutic concentrations of antimicrobials to the site of infection should increase the chances of success in such cases. These methods of drug delivery need to be used in conjunction with othe...
Equine infectious keratitis. Corneal ulcers are one of the most common ocular disease presentations in the horse. With the use of correct diagnostic techniques and selection of an appropriate treatment regimen, most cases result in a satisfactory outcome. The eye does not respond well to inflammation, and in complicated ulcers, this should be managed aggressively using systemic NSAIDs with a high priority assigned to removing the infectious agent. Care needs to be taken to avoid topical or systemic corticosteroid use for the treatment of equine ocular disease, however, unless the clinician is completely sure that the corn...
Disposition and tolerance of suxibuzone in horses. Suxibuzone (SBZ), a nonsteroidal anti-inflammatory drug, was administered to 6 horses at a dose rate of 7.5 mg/kg bwt by intravenous (i.v.) route. Plasma and synovial fluid concentrations of suxibuzone and its main active metabolites, phenylbutazone (PBZ) and oxyphenbutazone (OPBZ), were measured simultaneously by a sensitive and specific high-performance liquid chromatographic method. The pharmacokinetic parameters were determined by noncompartmental analysis. Plasma SBZ concentrations rapidly decreased and were not detectable beyond 20 min after treatment. The parent drug was not detected in...
Bioavailability of racemic ketoprofen in healthy horses following rectal administration. 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...
Pharmacokinetics and bioequivalence of two suxibuzone oral dosage forms in horses. A disposition and bioequivalence study with a suxibuzone granulated and a suxibuzone paste oral formulation was performed in horses. Suxibuzone (SBZ) is a nonsteroidal anti-inflammatory drug, which was administered to horses (n = 6) at a dosage of 19 mg/kg bwt by the oral route (p.o.) in a two period cross-over design. Suxibuzone is very rapidly transformed into its main active metabolites, phenylbutazone (PBZ) and oxyphenbutazone (OPBZ). Therefore plasma and synovial fluid concentrations of SBZ, PBZ and OPBZ were simultaneously measured by a sensitive and specific high-performance liquid chro...
Detection and identification of flunixin after multiple intravenous and intramuscular doses to horses. The objectives of the study were to compare various methods to determine flunixin in test samples collected periodically from horses after intramuscular (IM) and intravenous (IV) dosing at the maximum recommended dosage and to document detection times for this drug in test samples. Flunixin, a nonsteroidal anti-inflammatory drug approved for use in horses, was administered to eight mares in five consecutive daily doses of 1.1 mg per kilogram of body weight by the IM or IV route. Flunixin was detected in urine samples collected at various times after drug administration by flunixin enzyme-linke...
