Topic:Drug
The topic of drugs and horses encompasses the study of various pharmacological agents used in equine medicine for therapeutic purposes. This includes the administration of medications for pain management, disease treatment, and performance enhancement. The pharmacokinetics and pharmacodynamics of drugs in horses are key areas of research, as they determine the absorption, distribution, metabolism, and excretion of these substances. Additionally, the topic covers the detection and regulation of substances in competitive equestrian sports to ensure fair play and animal welfare. This page compiles peer-reviewed research studies and scholarly articles that explore the effects, safety, and regulatory aspects of drug use in equine health and performance.
A comparison of the actions of platelet activating factor (PAF) antagonists WEB 2170 and WEB 2086 in the horse. The effects of the selective platelet activating factor (PAF) receptor antagonist WEB 2170 on PAF-induced responses in equine cells and tissues have been examined and compared with those of WEB 2086. In initial experiments WEB 2170 was shown to inhibit in vitro platelet aggregation in a dose-dependent, competitive reversible manner (pA2 = 7.21). Co-administration of the antagonists with either PAF or histamine also inhibited PAF, but not histamine, induced wheal formation and PAF-induced neutrophil accumulation in vivo in equine skin. Intravenous (i.v.) administration of both drugs at a dose o...
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...
Regulatory aspects of drug use in performance horses. The control of drug use in performance horses and the policing of rules and regulations to prevent unauthorized drug use are important tasks for agencies overseeing equestrian events. This article describes the roles of the American Horse Shows Association, the Federation Equestre Internationale, and the Association of Racing Commissioners International, Inc, in the policing of drug use in horses competing in events under their control.
Effects of sympathomimetic and sympatholytic drugs on exercise performance. This article has presented information on the importance of the sympathetic nervous system in the response to exercise. The authors have reviewed the very limited information on the effects of sympathomimetic and sympatholytic drugs on exercise performance in the horse. Most of these drugs are specifically prohibited under the rules of racing, and they have significant side effects that either decrease performance or make their use dangerous to both the horse and horse-man. Additionally, all of these drugs or their metabolites are readily detected by current drug testing protocols. Further inf...
Pharmacokinetics of metronidazole after rectal administration in horses. Five healthy adult mares and 1 gelding were given a single dose (15 mg/kg of body weight) of metronidazole per rectum. After manual evacuation of feces from the rectum, a suspension of crushed tablets and water (40 ml) was administered via a 28-F catheter advanced 30 cm into the rectum. Blood samples were obtained by jugular venipuncture, and metronidazole concentration was measured serially for the 14 hours after drug administration. Mean serum concentration of metronidazole peaked at 4.5 micrograms/ml, 0.83 hour after administration, and decreased to 0.38 microgram/ml, 14 hours after adminis...
Cardiopulmonary and behavioral responses to computer-driven infusion of detomidine in standing horses. Cardiopulmonary and behavioral responses to detomidine, a potent alpha 2-adrenergic agonist, were determined at 4 plasma concentrations in standing horses. After instrumentation and baseline measurements in 7 horses (mean +/- SD for age and body weight, 6 +/- 2 years, and 531 +/- 48.5 kg, respectively), detomidine was infused to maintain 4 plasma concentrations: 2.1 +/- 0.5 (infusion 1), 7.2 +/- 3.5 (infusion 2), 19.1 +/- 5.1. (infusion 3), and 42.9 +/- 10 (infusion 4) ng/ml, by use of a computer-controlled infusion system. Detomidine caused concentration-dependent sedation and somnolence. The...
Factors affecting drug withholding time estimates in horses. Although all the factors discussed in this article may have an effect on drug withholding time estimates, the factors that have the potential for the greatest effect or that have been found to cause positive tests in the past are 1. Dosage: Increasing the drug dosage will require a longer withholding time. 2. Dosing interval: Narrowing the dosing interval will require a longer withholding time. 3. Administration route: In general, oral administration results in lower peak plasma concentrations but may result in longer excretion in the urine and therefore longer withholding time. 4. Drug intera...
Effects of single intravenously administered doses of omeprazole and ranitidine on intragastric pH and plasma gastrin concentration in nonfed ponies. We investigated the effects of a range of IV administered doses of omeprazole (0.125 to 2.0 mg/kg of body weight) on gastric pH (monitored by indwelling electrode) and plasma gastrin concentration, compared with those of IV administered ranitidine (1.0 mg/kg) in 4 Welsh mountain-type ponies. Pharmacokinetic variables of IV administered omeprazole also were examined. Episodes of high gastric pH in the basal state obscured the effect of acid suppression on intragastric pH; however, omeprazole induced dose-dependent increase in mean gastric pH (P < 0.01) during the 11 hours after its administr...
Determination of alclofenac in equine plasma and urine by high-performance liquid chromatography. A high-performance liquid chromatographic method to measure plasma and urinary alclofenac levels in equine biofluids is described. Isolation of the drug from plasma is achieved using liquid-liquid extraction with diethyl ether. Reversed-phase C18 solid phase extraction is used for the extraction of free and conjugated alclofenac from urine. The reproducibility and accuracy of the method were well within acceptable limits over the concentration ranges 0-10 and 0-20 micrograms/ml, respectively, for plasma and urine. Starting with 2 ml of plasma, a concentration of 0.1 microgram/ml could easily b...
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...
Species scaling of propafenone disposition and concentration–time relationships among eight mammalian species. Usually, smaller mammals have higher clearances per unit body mass than do larger mammalian species. When clearance and other pharmacokinetic parameters are correlated with internal physiological processes, species tend to dispose of drugs at a similar pace. The first application of this concept is pharmacokinetic time, expressed with different units: Kallynochron, Apolysichron, Dienetichron, and Syndesichron. The present work describes pharmacokinetic time in these units from data obtained with propafenone in eight animal species: mouse, rat, rabbit, dog, sheep, human, cow, and horse. Additio...
Comparison of immunoaffinity chromatography combined with gas chromatography-negative ion chemical ionisation mass spectrometry and radioimmunoassay for screening dexamethasone in equine urine. A comparison of the sensitive analytical methods of radioimmunoassay (RIA) and immunoaffinity chromatography (IAC) combined with gas chromatography-negative ion chemical ionisation mass spectrometry for the specific and reliable screening of dexamethasone in equine post-race urine is presented. Results from analyses of samples collected from a mare during 144 hours post administration of 26 mg of dexamethasone sodium phosphate are described.
Microdilution antimicrobial susceptibilities of selected gram-negative veterinary bacterial isolates. Gram-negative bacterial isolates (635) obtained from routine submissions to the Oklahoma Animal Disease Diagnostic Laboratory during 1983-1987 were tested for antimicrobial susceptibility. Minimal inhibitory concentrations (MICs) were determined for the following antimicrobials using commercially prepared microdilution assay materials: ampicillin, cephalothin, chloramphenicol, erythromycin, gentamicin, kanamycin, oxytetracycline, penicillin G, spectinomycin, sulfachlorpyridazine, sulfadimethoxine, and tylosin. Results for isolates from cattle, dogs, horses, and pigs are presented. In only a fe...
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...
Kanamycin concentrations in synovial fluid after intramuscular administration in the horse. Six adult ponies were injected in the same intramuscular site with kanamycin sulphate (10 mg/kg). Two hours later, arthrocenteses of the right metacarpophalangeal, radio-carpal, intercarpal, tibio-tarsal and metatarsophalangeal joints were performed within 3 minutes. Arthrocenteses of the same joints on the left side were conducted 5 hours later. When expressed as a percentage of plasma drug concentration, differences in synovial fluid drug concentration between the joints sampled at 2 and 5 hours after injection were not detected.
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...
Disposition, bioavailability and clinical efficacy of orally administered acepromazine in the horse. The pharmacokinetics and pharmacological efficacy of orally (p.o.) administered acepromazine were studied and compared with the intravenous (i.v.) route of administration in a cross-over study using six horses. The oral kinetics of acepromazine can be described by a two-compartment open model with first-order absorption. The drug was rapidly absorbed after p.o. administration with a half-life of 0.84 h, tmax of 0.4 h and Cmax of 59 ng/ml. The elimination was slower after p.o. administration (half-life 6.04 h) than after i.v. injection (half-life 2.6 h). The bioavailability of the orally admini...
Hemodialysis for treatment of oxytetracycline-induced acute renal failure in a neonatal foal. Acute renal failure in a 4-day-old foal secondary to oxytetracycline toxicosis was treated by hemodialysis. Oxytetracycline had been administrered as treatment for forelimb flexor tendon contracture. Conservtive treatment with fluids, furosemide, and dopamine partially alleviated serum electrolyte concentration imbalances, but was ineffective in promoting diuresis or decreasing azotemia. Three hemodialysis treatments over 4 days were administered, after which the clinical appearance of the foal improved, and biochemical and electrolyte values returned to within reference ranges. The nephrotoxi...
ELISA screening with GC-MS confirmation of the tranquilizer chlorprothixene administered in subtherapeutic doses to horses. A commercially available generic promazine ELISA kit is available which shows cross-reactivity for the tranquilizer chlorprothixene (CPT). The ELISA test readily detects the presence of CPT or its metabolites in equine urine for up to 24 h after the i.v. and i.m. administration of sub-therapeutic doses (4.5 mg) to three horses. Maximum concentrations (CPT equivalents) are obtained 2 h after i.v. dosing. No distinct concentration peak values are observed after i.m. administration. Following solid-phase extraction, confirmation of CPT and its metabolites by electron impact mass spectrometry afte...
Clinical pharmacokinetics of amikacin in hypoxic premature foals. The pharmacokinetics of amikacin, administered iv at 7 mg/kg, every 8 h, were evaluated over the first 48 h of hospitalisation in 7 critically ill hypoxic premature foals and compared with those in 8 full-term nonhypoxic critically ill neonatal foals. The pharmacokinetic data were used to calculate dosage schedules that would maintain the plasma amikacin concentrations in individual foals within a target range of > or = 15 micrograms/ml but < 30 micrograms/ml for peak values and < or = 3 micrograms/ml for trough values. The results indicated a statistically significant increase in the amikacin...
In-vitro susceptibility to antimicrobial drugs of bacterial isolates from horses in The Netherlands. Minimum inhibitory concentrations (MICs) of 30 antimicrobial agents (including the hitherto unreported antimicrobial agents doxycycline, minocycline, vanomycin, 3 quinolones and 3 combinations of antimicrobial agents) for isolates of Salmonella spp. (20), Escherichia coli (17), Klebsiella spp. (8), Proteus spp. (7), Pseudomonas aeruginosa (7), Actinobacillus equuli (5), Rhodococcus equi (4), Streptococcus zooepidemicus (23), Streptococcus equisimilis (6), Streptococcus equi (4), coagulase-positive Staphylococcus spp. (20) and Taylorella equigenitalis (19) were determined using the agar dilutio...
Pharmacokinetics of digoxin administered to horses with congestive heart failure. Nine horses with (naturally acquired) congestive heart failure were treated with 2.2 micrograms of digoxin/kg of body weight by the IV route, followed by 11 micrograms/kg administered orally every 12 hours thereafter. Furosemide was administered IV concurrently with IV administered digoxin every 12 hours. Serum concentration of digoxin was measured after the first (IV) and seventh (orally administered) dose. After IV administration, digoxin disposition was described by a 2-compartment model, with a rapid distribution phase (t1/2 alpha = 0.17 hour), followed by a slower elimination phase (beta ...
Clinical evaluation of romifidine/ketamine/halothane anaesthesia in horses. Romifidine, 100 micrograms/kg administered by intravenous injection, was evaluated as a premedicant to ketamine/halothane anaesthesia in 60 horses. Sedation developed within one to two minutes. In three cases mild staggering occurred within two minutes. Anaesthesia was induced after five minutes by the intravenous administration of ketamine (2 to 2.2 mg/kg). A mean time of 79 seconds elapsed before lateral recumbency was adopted. Fifty-four of the horses sank smoothly to the floor, with occasional steps sideways. Jaw tone, limb rigidity and mild muscle tremors often persisted for short periods...
Critical tests of thiabendazole, oxibendazole, and oxfendazole for drug resistance of population-B equine small strongyles (1989 and 1990). Critical tests were conducted in horses (n = 11) with naturally acquired infections of benzimidazole (BZ)-resistant population-B small strongyles in 1989 and 1990. Anthelmintics administered were thiabendazole (44 mg/kg of body weight, n = 4), oxibendazole (10 mg/kg, n = 3), and oxfendazole (OFZ, 10 mg/kg; n = 4). All compounds were paste formulations administered orally except for 1 of the OFZ treatments, which was a suspension formulation given by stomach tube. Aggregate mean efficacy was calculated for all species of small strongyles, drug-resistant and non-resistant. The highest efficacy w...
Pharmacokinetics of single intravenous and single and multiple dose oral administration of rifampin in mares. The disposition of rifampin in six healthy mares after single intravenous (i.v.) and oral (p.o.) doses and after seven oral doses of 10 mg/kg administered twice a day was investigated using a high performance liquid chromatographic (HPLC) method. Pharmacokinetic variables for rifampin determined using the HPLC method were comparable to variables reported from earlier studies utilizing a microbiological assay. Desascetylrifampin, a major metabolite of the parent compound, could not be detected in the serum but was detected at low concentrations in urine. Mean trough concentrations of rifampin i...
Pharmacokinetics and metabolism of avermectins in livestock. The kinetics of avermectin disposition and metabolism in ruminant livestock and horses are reviewed with particular emphasis on the influence of route of administration and formulation on persistence of residues in tissues and excretion in faeces. Because information is not publicly available on other compounds in this class currently under development (e.g. moxidectin, doramectin), ivermectin only is considered. The biological half-life of ivermectin in plasma is similar in cattle and sheep but because of a larger volume of distribution, plasma clearance is more rapid in sheep. However, injec...
Effects of clenbuterol hydrochloride on pulmonary gas exchange and hemodynamics in anesthetized horses. We evaluated the effects of clenbuterol HCl (0.8 micrograms/kg, of body weight, IV), a beta 2 agonist, on ventilation-perfusion matching and hemodynamic variables in anesthetized (by IV route), laterally recumbent horses. The multiple inert gas elimination technique was used to assess pulmonary gas exchange. Clenbuterol HCl induced a decrease in arterial oxygen tension (from 57.0 +/- 1.8 to 49.3 +/- 1.2 mm of Hg; mean +/- SEM) as a result of increased shunt fraction (from 6.6 +/- 2.1 to 14.4 +/- 3.1%) and ventilation to regions with high ventilation-perfusion ratios. In contrast, no changes in...