Omneity® Pellets
All-In-One Vitamin & Mineral Pellet
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.
Development of an ELISA using a universal method of enzyme-labelling drug-specific antibodies. Part I: Detection of dexamethasone in equine urine. The development, validation, and application of an ELISA for dexamethasone in equine urine is described. The drug-protein conjugate was immobilised in microtitre plate wells and antiserum raised against the same drug-protein conjugate was allowed to compete with sample or standard drug and the immobilised drug-protein conjugate. The proportion of antiserum binding to the immobilised drug-protein conjugate was detected using a biotinylated protein G/extravidin-alkaline phosphatase complex in situ and measurement of the substrate product. The method was used to detect the presence of drug-derive...
Pharmacokinetics of ketoprofen after multiple intravenous doses to mares. The pharmacokinetics and urinary excretion of ketoprofen in six healthy mares after the first and last of five daily intravenous doses of 2.2 mg of ketoprofen per kg body weight were investigated using a high-performance liquid chromatographic (HPLC) method for determining plasma and urinary ketoprofen concentrations. Plasma ketoprofen concentrations declined triexponentially after each dose with no significant differences in plasma concentrations or pharmacokinetic parameter values between the first and last doses. The harmonic mean of the terminal elimination half-life of ketoprofen after th...
Sedative and analgesic effects of detomidine and romifidine in horses. In a double blind study, eight horses were treated intravenously at seven-day intervals with detomidine at doses of 10, 20 and 40 micrograms/kg, or with romifidine at doses of 40, 80 and 120 micrograms/kg, or with a placebo solution. Their sedative and analgesic effects were evaluated by objective measurements and by a clinician at 15-minute intervals for three hours and the horses' instability in stocks, locomotor ataxia and heart rate were recorded simultaneously. The administration of both drugs at all doses resulted in sedation. The sedation achieved with romifidine was significantly shall...
Enantioselective glucuronidation and subsequent biliary excretion of carprofen in horses. Carprofen (CPF) enantiomers and their glucuronide conjugates (GLUC) were measured in plasma and bile of horses after IV administration of the racemic compound (0.7 mg/kg of body weight). The CPF was detectable in plasma for up to 72 hours after dosing, whereas GLUC appeared early (time for maximal plasma concentration, 1 hour) and was measurable transiently at low concentration (maximal plasma concentration, 0.5 microgram/ml). The enantiospecific plasma profiles indicated a clear predominance of R-CPF, whereas the stereoselectivity of the glucuronides favored S-GLUC. At 1, 2, and 12 hours afte...
Evaluation of propofol as a general anesthetic for horses. This study provides baseline information on the potential use of propofol as a general anesthetic for horses. Using a Latin square design, propofol (2, 4, and 8 mg/kg) was administered intravenously on three separate occasions to six mature horses. Information about anesthetic induction, duration, and recovery was recorded along with results of rectal temperature, heart rate, respiratory rate, pHa, PaCO2 and PaO2. Statistical analysis included a mixed model analysis of variance, a general linear model analysis and least square means test for post hoc comparisons. A P < .05 was considered si...
[Intravenous administration of Ivomec in horses]. Now and then cases have been reported where horses died suddenly after intravenous application of Ivomec. Lethal anaphylactic reactions in horses are known to occur incidentially after intravenous application of drug dissolved in propyleneglycol or glycerolformol. Since Ivomec is registered for use in cattle, sheep and pig, its use in horses has to be regarded as 'off label use'. It is concluded that in the treatment of inhibited stages of cyathostomes ivermectin has no effect whether or not it is applied intravenously or orally. Since lethal anaphylactic reactions can occur, intravenous appli...
Pharmacokinetics of trimethoprim/sulphachlorpyridazine in horses after oral, nasogastric and intravenous administration. In the present study, the pharmacokinetic parameters of a trimethoprim/sulphachlorpyridazine preparation following intravenous administration, administration by nasogastric tube and administration with concentrate were determined in the horse. Eight adult horses were dosed at 1 week intervals in a sequentially designed study at a dose of 5 mg/kg trimethoprim (TMP) and 25 mg/kg sulphachlorpyridazine (SCP) on all occasions. Plasma concentrations of both drugs were measured serially for 48 h. Pharmacokinetic parameters of clinical importance (distribution and elimination half-lives, clearance, bi...
Efficacy of moxidectin oral gel against Onchocerca cervicalis microfilariae. During a series of dose-titration experiments designed to evaluate the efficacy of moxidectin oral gel against equine gastrointestinal parasites, infection with Onchocerca cervicalis was diagnosed in 25 of 82 ponies prior to treatment. Microfilariae were identified in full-thickness skin biopsies taken from the ventral midline. Treatment with moxidectin in single doses of 300, 400, or 500 micrograms/kg of body weight was 100% effective in eliminating microfilariae from 20 skin biopsies taken 14 days posttreatment, whereas 5 microfilaria-positive ponies in 2 control groups remained positive fol...
Pharmacokinetics of ciprofloxacin in ponies. The pharmacokinetics of ciprofloxacin was investigated in healthy, mature ponies. Ciprofloxacin was administered intravenously to six ponies at a dose of 5 mg per kg body weight. Seven days later, ciprofloxacin was administered orally to each pony at the same dose. Intravenous ciprofloxacin concentration vs. time data best fit a two-compartment open model with first-order elimination from the central compartment. Mean plasma half-life, based on the terminal phase, was 157.89 min (harmonic mean). Total body clearance of ciprofloxacin was 18.12 +/- 3.99 mL/min/kg. Volume of distribution at stead...
Haemodynamic effects of hyoscine-N-butylbromide in ponies. The haemodynamic effects of hyoscine-N-butylbromide (0.30 mg/kg, intravenously) were studied in eight adult ponies in a blinded two-period crossover experiment with repeated measures. Values for heart rate were 63%, 48% and 13% greater than control values at 1, 16 and 46 min, respectively, after administration of hyoscine-N-butylbromide. Cardiac output increased by 16% at 16 min after drug injection. Mean right atrial pressure was decreased by 79%, 63%, 45% and 52% at 1, 16, 46 and 61 min, respectively, after drug administration. Stroke volume was decreased by 32% at 1 min and pulmonary arteri...
[Demonstration of two trimethoprim/sulfonamide combinations in bronchoalveolar lavage fluid of horses and determination of blood levels]. Five healthy horses were given a sulfadoxine/trimethoprim combination (Borgal, Hoechst AG) i.v. on day 1. The next ten days the horses got once a day a sulfadimethoxine/trimethoprim combination orally (Trafigal, Hoechst AG). The doses were given as recommended. One horse received no medicaments for control. On each horse six bronchoalveolar lavages were performed. Blood samples were taken to calculate blood levels and elimination half lives. To determine the amount of substances in lavage fluid and plasma the high performance liquid chromatography (HPLC) was used. Regularly low quantities of s...
Activity of praziquantel (0.5 mg kg-1) against Anoplocephala perfoliata (Cestoda) in equids. Praziquantel injectable formulation was administered at 0.5 mg k-1 per os to 24 equids naturally infected with 1-183 (average 40) Anoplocephala perfoliata. Drug activity was evaluated by a modified critical test method with necropsy 24 h after treatment. There was variable efficacy of 0-100% (aggregate average 85%); for 18 equids, 93-100%, for three equids, 70-85%, and for three equids, 0-20%.
Allometry of pharmacokinetics and pharmacodynamics of the muscle relaxant metocurine in mammals. We investigated the effects of body size on the pharmacokinetics and pharmacodynamics of the renally cleared muscle relaxant metocurine. We hypothesized that pharmacokinetics of the drug would change allometrically in proportion to physiological time [infinity Mb0.25, where Mb is body mass] and that pharmacodynamics would be independent of size because of the highly conserved structure of the acetylcholine receptor. Metocurine effects during general anesthesia were examined in 17 rats, 8 cats, 6 dogs, 5 pigs, 7 sheep, and 12 horses. Allometric analysis demonstrated size dependence for pharmaco...
Absorption and dosage of theophylline in the horse after single and repeated administration of a microencapsulated preparation. The kinetics of 2 formulations of theophylline were studied in horses. In an initial cross-over study (Phase I) serum concentration-time curves were determined for granulated and microencapsulated theophylline after a single oral administration (5 mg/kg bwt). In Phase II microencapsulated theophylline was administered at 5 mg/kg bwt/12 h for 10 days at feeding time, as in normal clinical practice. Although no significant differences between the 2 preparations were found with respect to the main kinetic parameters, the microencapsulated form was more evenly and completely absorbed from the dige...
Determination of succinonitrile in horse urine by gas chromatography-nitrogen-phosphorus detector and gas chromatography-mass spectrometry. A chromatographic method was developed to detect and confirm the presence of succinonitrile (SDN) in horse urine samples, for antidoping control. The urine samples (5 ml) were extracted with diethyl ether and screened by gas chromatography-nitrogen-phosphorus detector and the confirmation of the drug's presence was accomplished by using gas chromatography-mass selective detection. The recovery of extraction was 78 and 81% for 1.0 and 2.0 micrograms ml-1 (relative standard deviation, < 10%), respectively. Urine samples collected after the administration of Energisan were positive for SDN (1-30 ...
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.
Experimental treatment of equine sarcoid using a xanthate compound and recombinant human tumour necrosis factor alpha. A xanthate compound with antiviral and antitumoural activities, tricyclodecan-9-yl-xanthogenate (D609) in combination with the potassium salt of the lauric acid (KC12) and, in a further investigation, the above-mentioned substances together with recombinant human TNF alpha (rh-TNF alpha), were tested on equine sarcoid tumours for therapeutic efficacy. A pilot investigation on 5 healthy horses showed that the compounds were well-tolerated; apart from a local, temporary oedema at the injection site, no other clinical symptoms were observed after subcutaneous administration of volumes from 0.1 to...
A comparative study of the pharmacokinetics of intravenous and oral trimethoprim/sulfadiazine formulations in the horse. The biopharmaceutical properties of four fixed trimethoprim/sulfonamide combinations were investigated in the horse. Eight fasted horses were dosed at 1 week intervals in a sequentially designed study with one intravenous (i.v.) and three oral trimethoprim/sulfadiazine (TMP/SDZ) formulations (1, 2 and 3) administered at a dose of 5 mg/kg trimethoprim (TMP) and 25 mg/kg sulfadiazine (SDZ). Plasma concentrations of each compound were monitored for 48 h. Pharmacokinetic parameters (volume of distribution, bioavailability and total body clearance) for TMP and SDZ were calculated and compared. Afte...
Models for assessing the relationship between drug concentration and drug effect in performance horses. The actions of most drugs are dependent upon achieving adequate plasma concentrations. Plasma concentrations are influenced by the degree to which a drug is absorbed, distributed, metabolized and excreted. Pharmacokinetic assessment reflects changes in these variables as a function of time. Pharmacodynamics refers to specific drug effects or mechanisms of drug action. Individual drug pharmacokinetics provides information on which to base a therapeutic dose, route of administration and dosing interval. However, not all drug actions temporally correlate with plasma kinetics. To resolve this disc...
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...
Pharmacokinetics of thiopentone in the horse. The pharmacokinetics of thiopentone sodium administered intravenously as a single dose (11 mg/kg) were studied in acepromazine pre-medicated horses and ponies in which anaesthesia was maintained with either halothane (Group 1) or isoflurane (Group 2). The results showed that the disposition kinetics of thiopentone in horses and ponies were best described by a three-compartment open model. In plasma, a very short initial distribution phase in both horses and ponies, half-life 1.4 +/- 1.2 min (mean +/- SD) and 1.3 +/- 0.7 min, respectively, was obtained, which was followed by a second comparativ...
In vitro susceptibility of equine Salmonella strains to trimethoprim and sulfonamide alone or in combination. The in vitro activity of trimethoprim (TMP) and 9 sulfonamides and their combinations in 6 concentration ratios was tested against 62 Salmonella strains isolated from horses over a 3-year period in the Netherlands, using the agar-dilution method. Most of the isolates were S typhimurium strains (n = 52); the others were S heidelberg (n = 3), S hadar (n = 2), S thompson (n = 2), S enteritidis (n = 1), S infantis (n = 1), and S derby (n = 1). The minimal TMP concentration at which 50% of the Salmonella strains were inhibited (MIC50) was 0.12 micrograms/ml. Sulfachlorpyridazine (SCP; MIC50, 16 mic...
Pharmacokinetics and pharmacodynamics of acepromazine in horses. A specific, sensitive, reverse-phase high-performance liquid chromatographic assay for acepromazine, with analytic sensitivity as low as 5 ng/ml of plasma, and electrochemical detection with an oxidation potential of 0.7 V, was used to study the pharmacokinetics of acepromazine given at a dosage of 0.15 mg/kg of body weight in horses. The relation between effect and pharmacokinetics of the drug was examined. The effects studied included those on blood pressure, pulse, PCV, measures of respiration function, and sedation. Intravenously administered doses led to a biphasic concentration decay pat...
Effect of route of administration and age on the pharmacokinetics of amikacin administered by the intravenous and intraosseous routes to 3 and 5-day-old foals. The suitability of the intraosseous (i.o.) route for drug administration to equine neonates was evaluated in a study comparing the pharmacokinetics of amikacin administered by the i.o. and intravenous (i.v.) routes. Using a cross-over study design amikacin sulphate (7 mg/kg bwt) was administered i.o. or i.v. to 6 healthy foals at 3 and 5 days of age. Amikacin was instantaneously and completely absorbed after i.o. administration, achieving a mean +/- sd peak concentration (34.17 +/- 3.54 micrograms/ml) in the first sample collected 3 min after administration which was not significantly differen...
Effects of alpha 2-agonists on intrauterine pressure and sedation in horses: comparison between detomidine, romifidine and xylazine. The effect of three alpha 2-agonistic sedatives, Detomidine (0.04 mg/kg), Romifidine (0.08 mg/kg) Xylazine (1.1 mg/kg) and placebo (NaCl), on intrauterine pressure was investigated with an intrauterine balloon model in four non-pregnant warmblood mares. Within 6.0 (+/- 2.2) min mean pressure increases of 9.80 (+/- 3.74), 6.88 (+/- 3.95) and 13.95 (+/- 5.19) mmHg were recorded for Detomidine, Romifidine and Xylazine, respectively. Placebo had no significant effect. The mean duration of pressure increase was 30.0 (+/- 5.10), 17.67 (+/- 9.87) and 19.50 (+/- 13.78) min for Detomidine, Romifidine a...
Effect of drug formulation and feeding on the pharmacokinetics of orally administered quinidine in the horse. Quinidine is the drug of choice for the treatment of cardiac arrhythmias in horses. The plasma concentrations vs. time profiles following oral administration of two formulations of quinidine sulphate, an oral solution and an oral suspension paste, were evaluated in nine horses. They received multiple administrations of the oral solution under fed and non-fed conditions and of the paste under non-fed conditions. A loading dose of 20 mg.kg-1 and a maintenance dose of 10 mg.kg-1 quinidine with dosing interval of 6 h were used. The relative bioavailability of the oral solution under fed conditions...
The pharmacokinetics and pharmacodynamics of procainamide in horses after intravenous administration. Six horses were administered either 15 or 20 mg/kg body weight (b.w.) procainamide (PA) as an intravenous (i.v.) dose over 10 min. The plasma concentrations of PA and N-acetylprocainamide (NAPA) as well as the pharmacodynamic effect (prolongation of the QT interval) were monitored. The PA plasma concentrations could be described by a one-compartment model with a t1/2 of 3.49 +/- 0.61 h. The total body clearance of PA was 0.395 +/- 0.090 l/hr/kg and the volume of distribution was 1.93 +/- 0.27 l/kg. As observed after PA administration, NAPA (an active metabolite) had a t1/2 longer than PA of 6....
[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...
Kinetics of inhibition of replication of vesicular stomatitis virus in blood mononuclear cells of horses after in vitro and in vivo treatment with recombinant equine interferon-beta 1. Recombinant equine interferon-beta 1 (reqIFN-beta 1) induces an antiviral state in blood mononuclear cells (BMC) of horses. Maximal protection against replication of vesicular stomatitis virus is achieved 6 hours after treatment with IFN in vitro and in vivo. Duration of the protective effect depends on the dose of IFN in vitro and in vivo. Availability of reqIFN-beta 1 in cultures of BMC for up to 48 hours does not prolong the antiviral state. The protective effect on BMC after treatment with IFN has similar duration in vivo and in vitro. Monitoring of the effect of IFN in vivo is, thus, simp...
