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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.
Medical management of right dorsal colitis in 5 horses: a retrospective study (1987-1993). Right dorsal colitis in horses has been associated with administration of phenylbutazone. Although reports of right dorsal colitis in this species have described surgical treatment associated with a poor prognosis, we have had success treating this condition medically. This report describes 5 horses with right dorsal colitis confirmed during celiotomy that were initially managed medically. All horses had a history of intermittent abdominal pain; weight loss was noted in only 1 horse. The doses (2.0 to 4.6 mg/kg PO bid) and duration (5 to 30 days) of administration of phenylbutazone were not un...
Pharmacokinetics of ketoprofen in healthy horses and horses with acute synovitis. 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 ...
Retropharyngeal lymph node infection in horses: 46 cases (1977-1992). A retrospective study of 46 horses with retropharyngeal lymph node (RPLN) infection presented to the Rural Veterinary Centre between 1977 and 1992 was undertaken. Horses aged less than one year were most commonly represented (46%). Thirty-nine percent of cases had been exposed to horses with confirmed or suspected strangles (Streptococcus equi subsp equi infection) within the previous 8 weeks. Most frequent signs were unilateral or bilateral swelling of the throat region (65%), respiratory stertor/dyspnoea (35%), purulent nasal discharge (20%), inappetence and signs of depression (15%), and dy...
Pleural effusion associated with acute and chronic pleuropneumonia and pleuritis secondary to thoracic wounds in horses: 43 cases (1982-1992). Case records of 43 horses with pleural effusion associated with acute pleuropneumonia, chronic pleuropneumonia, or pleuritis secondary to a penetrating thoracic wound were reviewed to determine the predisposing factors, diagnosis, and treatment of this condition. Acute pleuropneumonia was diagnosed in 36 horses, the majority of which were Thoroughbreds (89%). Of 22 (61%) horses that were in race training at the onset of illness, 11 (31%) had been recently transported a long distance and 4 (11%) had evidence of exercise-induced pulmonary hemorrhage. Physical examination findings and hematologic...
Screening of non-steroidal anti-inflammatory drugs, barbiturates and methyl xanthines in equine urine by gas chromatography-mass spectrometry. A gas chromatographic-mass spectrometric (GC-MS) screening procedure for 23 acidic drugs in equine urine is described. With the GC-MS method fifteen anti-inflammatory drugs, five barbiturates and three methyl xanthines can be detected with good sensitivity and selectivity. The method consists of alkaline hydrolysis, extraction with organic solvent using salting-out, clean-up extraction, methylation and screening with GC-MS in selected-ion monitoring mode. The limit of detection is 10 micrograms 1(-1) or lower, for most drugs.
Epiglottitis in horses: 20 cases (1988-1993). Epiglottitis was diagnosed and treated in 20 horses (13 Thoroughbreds and 7 Standardbreds) over a 5-year period. Eighteen horses were used for racing, and 2 Standardbreds were broodmares. Primary clinical signs were exercise intolerance, respiratory noise, and coughing. The most common endoscopic diagnosis made by referring veterinarians was epiglottic entrapment (11 horses). In 19 horses, endoscopic evaluation at admission revealed mucosal ulceration and thickening of the lingual surface of the epiglottis. Other endoscopic findings included dorsal displacement of the soft palate (14 horses), ...
Plasma concentrations and therapeutic efficacy of phenylbutazone and flunixin meglumine in the horse: pharmacokinetic/pharmacodynamic modelling. The purpose of the present study was to establish in the horse the relationship between plasma concentration profiles of phenylbutazone (PBZ) and flunixin meglumine (FM) and their pharmacological effects in order to build a predictive pharmacokinetic/pharmacodynamic (PK/PD) model. In five horses, an experimental arthritis was induced by injecting Freund's adjuvant into a carpal joint. PBZ (4 mg/kg) and FM (1 mg/kg) were injected by the intravenous route as a single intravenous dose in two different trials. Five pharmacodynamic end-points were regularly measured after test article injection usi...
Disposition of human drug preparations in the horse. III. Orally administered alclofenac. Concentrations of the non-steroidal anti-inflammatory drug (NSAID) alclofenac were determined by a sensitive high performance liquid chromatographic procedure in plasma and urine of horses following oral administration of a dose of 3 g. In plasma, alclofenac was present in detectable concentrations for 72 h. The plasma disposition in individual horses was best described by a bi-compartmental model with two successive rate constants ka1 = 0.05 +/- 0.06 h-1 and ka2 = 0.06 +/- 0.01 h-1. Alclofenac half-lives t1/2 alpha and t1/2 beta were 1.0 +/- 0.8 h and 6.9 +/- 1.5 h, respectively. Maximal conc...
[Doping problems in horse sports–pharmacokinetics of selected antiphlogistics/analgesics relevant to doping]. Drug treatment of horses which are used in horse-racing is restricted by the regulations of the anti-doping control. Veterinarians and anti-doping control commissions are faced with the problems resulting from the discrepancy between the demand "no drugs in blood/urine of horses at the time of competition" and the need for treatment. The pharmacokinetic data of important antiphlogistics/analgetics (NSAID) for horses given in this article shall facilitate the decision of the veterinarians and commissions whether a horse having been treated with NSAID may participate in a competition or not. Fur...
Pharmacodynamics and pharmacokinetics of carprofen in the horse. The pharmacokinetics and pharmacodynamics of the nonsteroidal anti-inflammatory drug (NSAID) carprofen have been evaluated in 6 horses using a model of acute non-immune inflammation. Following intravenous administration of 0.7 mg racemic carprofen/kg bwt, mean values for pharmacokinetic parameters were 18.1 h (elimination half-life); 0.25 l/kg (volume of distribution, Vd[area]); 58.9 ml/min (clearance); and 57.9 micrograms/ml.h (area under plasma concentration time curve). Mean exudate:plasma concentration ratios exceeded 1.0 at all sampling times between 2 and 48 h. Swelling at the site of ac...
Effect of phenylbutazone on the haemodynamic, acid-base and eicosanoid responses of horses to sustained submaximal exertion. The systemic haemodynamic and acid-base effects of the administration of phenylbutazone (4.4 mg kg-1 intravenously) to standing and running horses were investigated. Phenylbutazone, or a placebo, was administered to each of six mares either 15 minutes before, or after 30 minutes of a 60-minute submaximal exercise test which elicited heart rates approximately 55 per cent of maximal, and to the same horses at rest. The variables examined included the cardiac output, heart rate, systemic and pulmonary arterial pressures, right atrial and right ventricular pressures, and arterial and mixed venous ...
Drug therapy in the neonatal foal. The neonatal period in foals refers to the first 7 days of postnatal life. The effects of drugs (pharmacologic agents) may be different in neonatal foals, particularly during the first 3 days of postnatal life, from those in older foals and adult horses. The changed drug effects decrease as the physiologic processes that affect absorption, distribution, and elimination (metabolism and excretion) of drugs mature. Dosage regimens should take into account the altered pharmacokinetic profiles of drugs, and because of wide individual variation, the response to therapy should be closely monitored fo...
Pharmacokinetic values of drugs frequently used in performance horses. Tables of values of pharmacokinetic variables (volume of distribution, total body clearance, and plasma elimination half-life) of drugs frequently administered to performance horses are accompanied by explanatory notes. Drugs described include the nonsteroidal anti-inflammatory drugs, corticosteroids, anabolic steroids, central nervous system-modifying drugs, respiratory system drugs, diuretics, local anesthetics, and antibacterial drugs.
Pharmacokinetics of and serum thromboxane suppression by flunixin meglumine in healthy foals during the first month of life. Age and species reportedly affect the pharmacokinetic variables of nonsteroidal anti-inflammatory drugs. We determined the effect of age on flunixin pharmacokinetic variables in foals during the first month of life. We also estimated the physiologic activity of the drug in neonatal foals by determining the effect of flunixin on thromboxane production during clotting of blood taken from the foals. Flunixin disposition and clearance were determined after IV administration of 1.1 mg of drug/kg of body weight to 5 healthy foals when they were 24 to 28 hours, 10 to 11 days, and 27 to 28 days old. T...
Effects of concurrent administration of phenylbutazone and flunixin meglumine on pharmacokinetic variables and in vitro generation of thromboxane B2 in mares. Flunixin meglumine and phenylbutazone are nonsteroidal anti-inflammatory drugs commonly used for the management of colic, endotoxemia, and musculoskeletal disorders in equids. Although it is not usually recommended, there appears to be an increasing trend to use nonsteroid anti-inflammatory drugs in combination to enhance or prolong their effects. Therefore, we studied the effect of concurrent administration of flunixin (1.1 mg/kg of body weight, IV) as flunixin meglumine and phenylbutazone (2.2 mg/kg, IV) on the pharmacokinetics of each drug and on in vitro thromboxane B2 production. Pharmaco...
Postoperative analgesia using phenylbutazone, flunixin or carprofen in horses. Horses undergoing surgery were randomly assigned to one of three groups to receive phenylbutazone at 4 mg/kg (n = 72), flunixin at 1 mg/kg (n = 68) or carprofen at 0.7 mg/kg (n = 63) by slow intravenous injection at the end of surgery, just before they were disconnected from halothane. Pain was assessed by either of two resident surgical clinicians (who did not know which non-steroidal anti-inflammatory drug had been given) when the horses first stood up, two and four hours later and the next morning. If repeated doses of analgesic drugs were given the time was recorded and taken as an end poi...
The disposition of suxibuzone in the horse. A high performance liquid chromatographic method is described to determine the anti-inflammatory drug suxibuzone (SXB) and its major metabolites phenylbutazone (PBZ) and oxyphenbutazone (OPBZ) in equine plasma and urine. When suxibuzone (6 mg/kg) was administered intravenously (i.v.) or orally (p.o.) no parent drug was detected in plasma or in urine. The disposition of the metabolite PBZ (i.v.) could be described by a 2 compartment model with a beta half-life varying from 7.40 to 8.35 h. Due to severe side effects the use of i.v. suxibuzone should not be encouraged in the horse. PBZ and OPBZ w...
[Pain prevention and pain treatment in small and large domestic animals]. The aim of this article is to emphasize the need for analgesic medication in animals in possibly painful situations, especially in the postoperative period. The two large groups of compounds used as analgesics--the opiates and the nonsteroidal antiinflammatory drugs (NSAIDs)--are described with special reference to their pharmacokinetics, side-effects and toxicity, their mechanism of action, their indications and contraindications. Recommended doses of the different drugs available are given for the dog, the cat, the horse, the swine and the small and large ruminants.
[Comparative enantioselectivity of the disposition of two non-steroidal anti-inflammatory agents, ketoprofen and carprofen, in man and animals]. 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 ...
Ventricular arrhythmias in horses: 21 cases (1984-1989). Ventricular premature depolarizations (VPD) were identified in 21 horses in which unexplained tachycardia or an arrhythmia was detected on auscultation. Horses were categorized into 3 groups on the basis of ECG findings. Seven horses had uniform isolated VPD (group 1); 7 horses had repetitive uniform VPD at a rate or = 100 VPD/min (group 3). Concurrent systemic disease was identified in 12 horses, 7 of which had gastrointestinal tract disorders. Serum cardiac isoenzyme activities were high in 6 (2 from each group) of 13 horses in which they were measured. Serum electrolyte concentrations were...
Bioavailability of two ibuprofen oral paste formulations in fed or nonfed ponies. The bioavailability and pharmacokinetics of ibuprofen, a nonsteroidal antiinflammatory drug, was studied in healthy Shetland ponies. Ibuprofen was administered IV, as a suspension, and as a solid solution oral paste to ponies from which food was withheld. The suspension paste was also administered to ponies that received hay and water ad libitum. Both formulations had an absolute bioavailability of about 80%. Bioavailability was not influenced by feeding.
Evaluation of some prophylactic therapies for the idiopathic headshaker syndrome. Eighteen horses affected by the idiopathic headshaker syndrome were studied in an owner assessed trial to test the efficacy of some prophylactic therapies. Riding the affected animal with a veil over the nostrils gave varying degrees of temporary relief in three of 10 horses. Local (intra-nasal) corticosteroid therapy was reported to be slightly effective in three of nine horses, but treatment with sodium cromoglycate, systemic corticosteroid, flunixin meglumine and an antihistamine were generally ineffective. Bilateral infraorbital neurectomy provided sustained relief in three of seven horses...
Septic tenosynovitis in horses: 25 cases (1983-1989). The medical records of 25 horses with septic tenosynovitis treated over 7 years (1983 to 1989) were reviewed to determine clinical features of the disease and response to treatment. The median age of horses with septic tenosynovitis was 5 years (range, 1 month to 21 years). Fourteen fore limbs and 11 hind limbs were affected. Sepsis was located in the sheath of the digital flexor tendons of 22 horses. Sepsis was located in the sheath of the extensor carpi radialis tendon (1 horse), sheath of the long digital extensor tendon (1 horse), or sheath of the common digital extensor tendon (1 horse) i...
Pharmacokinetic, biochemical and tolerance studies on carprofen in the horse. Carprofen, a non-steroidal anti-inflammatory drug (NSAID) was administered to three Thoroughbred geldings and three Shetland ponies to determine its plasma disposition and tolerance. The main pharmacokinetic characteristics of carprofen in horses and ponies were a volume of distribution of 0.08 to 0.32 litres/kg (mean +/- se = 0.23 +/- 0.04) a systemic clearance of 26.4 to 78.5 ml/min (mean +/- se = 44.9 +/- 8.0) and a plasma elimination half-life of 14.5 to 31.4 h (mean +/- se = 21.9 +/- 2.3). There was no evidence of any accumulation of carprofen in plasma when the drug was given orally at a...
Pharmacology of furosemide in the horse: a review. Furosemide, a diuretic, is frequently administered to horses for the prophylaxis of exercise-induced pulmonary hemorrhage and the treatment of a number of clinical conditions, including acute renal failure and congestive heart failure. Furosemide increases the rate of urinary sodium, chloride, and hydrogen ion excretion. Plasma potassium concentration decreases after furosemide administration but urinary potassium excretion in horses is minimally affected. Renal blood flow increases after furosemide administration. Systemically, furosemide increases venous compliance and decreases right atrial...
Laminitis in the pony: conservative treatment vs dorsal hoof wall resection. The clinical and radiographic findings in 21 ponies with laminitis and its treatment and results are described. All ponies received non-steroidal anti-inflammatory drugs. All were fed hay and no concentrates. They were box rested for varying periods depending on clinical improvement. Dorsal hoof wall resection was performed in 11 ponies and all regained complete soundness. To shorten the period of non-activity, working ponies were shod and the hoof wall defect was packed with technovit or a combination of glue with cotton cuttings. Ten were treated conservatively; two recovered completely, fou...
Eltenac, a new anti-inflammatory and analgesic drug for horses: clinical aspects. Two controlled studies to determine efficacy in the horse were performed with eltenac, a new injectable, non-steroidal anti-inflammatory drug (NSAID). Clinical trials were carried out with a dose rate of 1 mg/kg body weight in a randomized, placebo-controlled, double-blind design to assess therapeutic efficacy in acute inflammatory disorders and in animals with orthopaedic conditions. In a preliminary pharmacokinetic investigation in six horses mean elimination half-life was 1.7 h after i.v. administration. In the first clinical study, analgesic activity on pain-related lameness was determined...
Pharmacodynamics and pharmacokinetics of miloxicam in the horse. The novel non-steroidal anti-inflammatory drug (NSAID) miloxicam was administered intravenously to six New Forest ponies at a dosage rate of 0.6 mg/kg in a two-part cross-over study. In each part, three horses received miloxicam and three were given a placebo preparation. The actions of miloxicam, compared to placebo, were assessed in a carrageenan-sponge model of acute inflammation. The rise in skin temperature over the site of the acute inflammatory reaction was less in treated ponies, but differences were not statistically significant. Concentrations of the enzymes acid phosphatase (AP) and...
