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Topic:Phenylbutazone
Phenylbutazone is a non-steroidal anti-inflammatory drug (NSAID) commonly used in horses to manage pain and inflammation associated with musculoskeletal disorders. It functions by inhibiting the cyclooxygenase enzymes (COX-1 and COX-2), which play a role in the inflammatory process. Phenylbutazone is administered in various formulations, including oral and injectable forms, and is often used in the treatment of conditions such as arthritis, laminitis, and soft tissue injuries. The pharmacokinetics, therapeutic effects, and potential side effects, such as gastrointestinal irritation and renal impairment, are subjects of ongoing research. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacology, clinical applications, and safety considerations of phenylbutazone in equine medicine.
Effects of phenylbutazone on thiamylal disposition and anaesthesia in ponies. Phenylbutazone given during the perisurgical period has been reported to increase the intensity and duration of thiamylal anaesthesia in horses. A possible mechanism of competitive plasma protein binding has been suggested. The purpose of the present study was to experimentally reproduce the phenomenon of increased intensity and/or duration of thiamylal anaesthesia and to determine if there is competitive displacement of plasma protein bound thiamylal by phenylbutazone. Six ponies each received one of three treatments, 11 mg/kg intravenous (i.v.) thiamylal; 8.8 mg/kg i.v. phenylbutazone; and 1...
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 ...
Exercise-induced connective tissue turnover and lipid peroxidation in horses. Four unfit thoroughbred horses were exercised on a treadmill twice, 5 weeks apart. Exercise consisted of stepwise increments in treadmill speed up to a maximum of 12 m s-1 and then maintained at this speed until the horses were fatigued. Two of the horses were administered phenylbutazone (4.4 mg kg-1) intravenously immediately before the first exercise period and the other two horses immediately before the second exercise period. Clinical observation revealed stiffness of gait and palpable soreness over the lumbar-sacral region in the horses 24 h after the exercise concluded. Mean plasma aspar...
Pharmacokinetics of phenylbutazone in neonatal foals. Single doses (2.2 mg/kg of body weight) of phenylbutazone (PBZ) were administered IV to 6 neonatal horses (5 to 17 hours old at time of dosing). Plasma concentrations of PBZ and its metabolite oxyphenbutazone were monitored serially for 120 hours after drug administration. Pharmacokinetic variables were calculated, using 1- and 2-compartment open models. Descriptive equations from the best model for each foal were then used to derive model-independent variables describing PBZ disposition. Median volume of distribution at steady-state was 0.274 L/kg (range, 0.190 to 0.401 L/kg). Median terminal...
The intramuscular bioavailability of a phenylbutazone preparation in the horse. The plasma concentrations of phenylbutazone (PBZ) and its major metabolites, oxyphenbutazone (OPBZ) and gamma-OH-phenylbutazone (OHPBZ) were determined for up to 72 h in six horses, following intravenous (i.v.) and intramuscular (i.m.) administration of 4 g phenylbutazone, 20 ml Phenylarthrite Ventoquinol (Vetoquinol Spécialités Pharmaceutiques Vétérinaires, Magny-Vernois, 70200 Lure, France). After i.v. dosing the plasma disposition was best described by a two-compartment open model. The hydroxylated metabolites OPBZ and OHPBZ were present in detectable concentrations for 72 h and 48 h, r...
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...
Modulation of bronchial responsiveness in horses by phenylbutazone and furosemide. Effects of phenylbutazone (PBZ) and furosemide (FUR) on the respiratory tract of horses were evaluated, focusing on bronchial responsiveness. Four healthy Thoroughbreds were used and data were analyzed by use of a Latin square design. Histamine provocation tests (0.5, 1, 2, and 4 micrograms/min, i.v.) were done: (1) without prior treatment with PBZ or FUR, (2) 30 minutes after administration of PBZ (8 mg/kg, i.v.), (3) 1 hour after administration of FUR (1 mg/kg, i.v.), and (4) after administration of PBZ plus FUR. Pulmonary function tests (dynamic compliance, resistance, respiratory frequency...
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...
Computer-assisted three-dimensional gait analysis of amphotericin-induced carpal lameness in horses. Motion of 6 clinically sound horses trotting at a speed of 4 m/s on a treadmill was captured by video cameras before and 9, 16, and 23 days after amphotericin-induced lameness to determine the quantitative variables of three-dimensional computer-assisted image analysis that objectively describe carpal lameness. Amphotericin-B was used to induce lameness, and phenylbutazone (2.2 mg/kg of body weight, PO, once) and butorphanol tartrate (0.1 mg/kg IM, q 6 h, to effect) were used to control discomfort. Four 60-Hz cameras were symmetrically placed around the treadmill to capture 6 seconds of images...
Comparison of adverse effects of phenylbutazone, flunixin meglumine, and ketoprofen in horses. The relative toxicity of phenylbutazone, flunixin meglumine, and ketoprofen was studied in healthy adult horses. Sixteen horses were randomly assigned to receive 10 ml of physiologic saline solution, or ketoprofen (2.2 mg/kg of body weight), flunixin meglumine (1.1 mg/kg), or phenylbutazone (4.4 mg/kg) IV, every 8 hours, for 12 days. Results of CBC, serum biochemical analyses, and fecal occult blood tests were monitored. On day 13, all horses were euthanatized and complete necropsy examinations were performed. Mean CBC values remained within normal limits for all groups. Phenylbutazone-treated...
Serum triiodothyronine, total thyroxine, and free thyroxine concentrations in horses. The objectives of this experiment were to determine serum concentrations of triiodothyronine (T3), thyroxine (T4), and free thyroxine (fT4) at rest, following thyroid-stimulating hormone (TSH) administration, and following phenylbutazone administration in healthy horses. This was done to determine which available laboratory test can best be used for diagnosis of hypothyroid conditions in horses. Serum T3, T4, and fT4 concentrations in serum samples obtained before and after TSH stimulation and following phenylbutazone administration for 7 days were determined. Baseline values ranged from 0.21 ...
Arthroscopic removal of a palmar radial osteochondroma causing carpal canal syndrome in a horse. A 5-year-old Arabian stallion with moderate effusion in the right carpal canal and intermittent lameness in this limb was diagnosed to have an osteochondroma projecting from the distal portion of the radius into the carpal canal. oral phenylbutazone treatment over the next 3 years allowed the stallion to continue its show career. Right forelimb lameness returned at that time, and ultrasonography revealed the osteochondroma impinging on the dorsal surface of the deep digital flexor tendon. The owner elected to have the osteochondroma surgically removed. The horse was anesthetized, and the carpa...
Influence of cyclooxygenase inhibitors on furosemide-induced hemodynamic effects during exercise in horses. Furosemide, which commonly is used as a prophylactic treatment for exercise-induced pulmonary hemorrhage in horses, may mediate hemodynamic changes during exercise by altering prostaglandin metabolism. To determine if furosemide's hemodynamic effects during exercise in horses could be reversed, cyclooxygenase inhibitors were administered with furosemide. Four treatments were administered 4 hours prior to treadmill exercise at 9 and 13 m/s. They included a control treatment (10 ml of 0.9% NaCl solution, IV), furosemide (1 mg/kg of body weight, IV) administered alone, and furosemide in combinati...
A comparison of drug binding sites on mammalian albumins. The fluorescent probes warfarin and dansylsarcosine are known to selectively interact with binding sites I and II, respectively, on human albumin. This paper investigates whether similar binding sites exist on bovine, dog, horse, sheep and rat albumins. Binding sites on albumins were studied by: (1) displacement of warfarin and dansylsarcosine by site I (phenylbutazone) and site II (diazepam) selective ligands; (2) the effects of non-esterified fatty acids (carbon chain lengths: C5-C20) and changes in pH (6-9) on the fluorescence of warfarin and dansylsarcosine; and (3) the ability of site sel...
Arthrotomy versus arthroscopy and partial synovectomy for treatment of experimentally induced infectious arthritis in horses. To evaluate the clinical, laboratory, and histologic effects of 2 methods of treatment for infectious arthritis in horses, Staphylococcus aureus (3.4 to 3.9 x 10(3) colony-forming units) was inoculated into the tarsocrural joints of 8 horses on day 0. Each horse was treated with phenylbutazone (2 g, PO, q 24 h) and gentamicin sulfate (2.2 mg/kg of body weight, IV, q 8 h) for 14 days. On day 2, general anesthesia was induced, and each horse had 1 tarsocrural joint treated by arthrotomy, with removal of accessible fibrin and lavage with 3 L of sterile balanced electrolyte solution. An indwelling...
Effect of probenecid on the pharmacokinetics of flunixin meglumine and phenylbutazone in healthy mares. Pharmacokinetic values for flunixin meglumine (1 mg/kg of body weight) and phenylbutazone (4 mg/kg) dosages were determined after a single IV injection with and without concurrent intragastric administration of probenecid (50 mg/kg) in 6 healthy mares. Significant difference was not apparent in the pharmacokinetic values of flunixin meglumine with and without concurrent probenecid administration. Significant (P less than or equal to 0.05) increase was evident in the 12-hour mean concentration of phenylbutazone (11.45 +/- 1.66 micrograms/ml without probenecid; 14.56 +/- 1.20 micrograms/ml with ...
Nonsurgical treatment of cubital subchondral cyst-like lesions in horses: seven cases (1983-1987). Subchondral cyst-like lesions of the cubital joint were diagnosed in 7 horses at the teaching hospital between 1983 and 1987. Diagnosis of the lesions was made by administration of intra-articular local anesthesia and/or radiographically. Initial treatment for all horses consisted of stall rest for 60 to 90 days. In addition, 2 horses were administered sodium hyaluronate intra-articularly, 1 horse was given injections of polysulfated glycosaminoglycans IM, and 1 horse was given phenylbutazone orally. Follow-up information was compiled 6 weeks to 4 years after initial examination. At the time o...
Evaluation of sodium hyaluronate therapy in induced septic arthritis in the horse. This study was conducted to determine the efficacy of sodium hyaluronate (SH) with antibiotic therapy and joint lavage for reducing acute inflammatory and degenerative changes induced by septic arthritis. Septic arthritis was induced in six adult horses by inoculating the tarsocrural joints with 1 x 10(4) colony-forming units of Staphylococcus aureus. When clinical signs appeared, trimethoprim-sulphamethoxazole (30 mg/kg bodyweight [bwt] daily) and phenylbutazone (4.4 mg/kg bwt sid) were administered and continued until termination of the study (Treatment Day 18). Twenty-four hours post inocul...
Fusion of the distal intertarsal and tarsometatarsal joints in the horse using intraarticular sodium monoiodoacetate. Six normal horses received 3 intra-articular injections of sodium monoiodoacetate (MIA) in the distal intertarsal (DIT) and tarsometatarsal (TMT) joints of one hindlimb. Injections were at three week intervals, and post injection pain was controlled with routine administration of phenylbutazone for five days following each injection. All horses underwent a gradually increasing exercise programme consisting of walking and trotting beginning one week after the first injection and continuing for 24 weeks. All treated joints showed increasingly severe radiographic evidence of degenerative joint di...
Effect of administration of phenylbutazone or progesterone on recovery of embryos from the uterus of mares 5 days after ovulation. Twelve horse mares were used to investigate the effect of phenylbutazone or progesterone administration on uterine tubal motility, as reflected by embryo recovery from the uterus on day 5 after ovulation. Four treatment groups were used: group A (controls), in which uterine flush was performed 7 to 11 days after ovulation; group B (5-day controls), in which uterine flush was performed 5 days after ovulation; group C, in which uterine flush was performed 5 days after ovulation following administration of phenylbutazone (2 g, IV) on day 3; and group D, in which uterine flush was performed 5 days...
Poisoning with equine phenylbutazone in a racetrack worker. Phenylbutazone is a potent nonsteroidal, anti-inflammatory drug often used by veterinarians to treat racetrack animals. Its use in human beings is limited because of significant adverse effects and the availability of newer, safer drugs. We report the case of a 24-year-old man who ingested 17 g of equine phenylbutazone over a 24-hour period to treat the pain of a toothache. He developed grand mal seizures, coma, hypotension, respiratory and renal failure, and hepatic injury. Serum phenylbutazone concentration obtained approximately eight hours after presentation was 900 micrograms/mL. The pati...
Disruption of the caudal component of the reciprocal apparatus in two horses. Two horses became acutely lame following a fall during strenuous exercise and were diagnosed as having disruption of the caudal component of the reciprocal apparatus. Clinical signs consisted of lameness of the right pelvic limb, characterized by flexion of the hock and simultaneous extension of the stifle. Radiography revealed an avulsion fracture from the supracondylar tuberosity and fossa of the distal portion of the femur in one horse. Clinical and radiographic findings indicated avulsion of the lateral origin of the gastrocnemius and superficial digital flexor muscles. Treatment consisted...
Right dorsal colitis. Moderate to severe ulcerative colitis of the right dorsal colon was diagnosed by necropsy or by exploratory celiotomy and biopsy in 13 horses with a primary clinical complaint of either colic, diarrhea, or weight loss. Clinical signs varied from acute fulminating diarrhea (possibly with fever), colic, dehydration, endotoxic shock and death, to a chronic condition manifested by mild intermittent colic up to several months in duration, and weight loss with or without mild diarrhea. In a large percentage of the horses, those affected had been hypovolemic and received nonsteroidal anti-inflammator...
The effects of phenylbutazone on the intestinal mucosa of the horse: a morphological, ultrastructural and biochemical study. Phenylbutazone, a non-steroidal anti-inflammatory drug known to produce intestinal erosions, was administered intravenously (13.46 mg/kg bodyweight) to 12 horses which were killed after 24, 48, 72 and 96 h. Eight untreated horses served as controls. Annular erosions in the duodenum and mucosal necrosis in the colon were seen after 48 h which progressed in severity. The erosions were characterised by sloughing of the surface epithelium, subepithelial cleft and bleb formation, necrosis of the lamina propria, degeneration of the walls of subsurface capillaries and microthrombosis. Large numbers o...
