Pharmacokinetics in horses involves the study of how drugs are absorbed, distributed, metabolized, and excreted in equine species. This field of study provides insights into the time course of drug concentrations within the horse's body and helps in understanding the effects of various pharmaceuticals. Key parameters in equine pharmacokinetics include absorption rates, bioavailability, half-life, and clearance. These parameters can vary significantly due to factors such as age, breed, and health status of the horse. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacokinetic profiles of different drugs in horses, aiming to optimize dosing regimens and improve therapeutic outcomes in equine medicine.
Miller JR, Blake JW, Tobin T.An electron capturing derivative of apomorphine was prepared by incubating the drug with heptafluorobutyric anhydride (HFBA), triethylamine and heat. Mass spectral analysis suggests that HFBA reacts with both phenolic hydroxyl groups on apomorphine to give a derivative detectable at low picogram levels. This method is sufficiently sensitive for pharmacokinetic studies in the horse and is likely applicable to other dopaminergic analogues of apomorphine.
Eales FA.Saffan was injected intravenously on 41 occasions in 11 horses and ponies to investigate its possible use in clinical equine anaesthesia. The optimum dose for induction was 1-90 mg per kg. This dose was divided into two halves, the first half given in five seconds and the second half, containing suxamethonium chloride 0.1 mg per kg, in the next 10 seconds. Induction was associated with excitement for up to 30 secs after the assumption of recumbency. At this dose rate anaesthesia lasted five to eight minutes. Muscle relaxation was poor. Recovery was associated with marked tactile and audible hy...
Delbeke FT, Debackere M.It is well known that nikethamide (N,N-diethylnicotinamide, CoramineR) is metabolized very rapidly to nicotinamide. Hence, there is difficulty in proving that nikethamide has been used as a doping substance because nicotinamide is a normal physiological metabolite in the organism as well as a vitamin preparation. However, an intermediate metabolite (N-ethylnicotinamide) was found by us in the urine of horses treated with CoramineR. This was characterized by gas chromatography/mass spectrometry, and synthesized and identified as being N-ethylnicotinamide. The excretion and metabolism of niketha...
Roberts BL, Blake JW, Tobin T.Horses pretreated with 6.6 mg/kg of phenylbutazone were injected with 1 mg/kg of furosemide intravenously. Furosemide had no clinically significant effect on either plasma levels or plasma half-life of phenylbutazone. Furosemide reduced urinary levels of phenylbutazone 18-fold to concentrations which may result in inconsistent drug detection in routine screening tests. The results show that it is not possible to monitor compliance with phenylbutazone medication rules by means of urinalysis alone if the use of furosemide is permitted. Furosemide treatment, however, does not interfere with monit...
Hillidge CJ.The effects of the analeptic agent, Dopram (doxapram hydrochloride) were investigated in 2 ponies during Immobilon - induced neuroleptanalgesia. Although Dopram was demonstrated to exert a degree of respiratory stimulation, this was concluded to provide no overall advantage. The etorphine-induced hypoxic hypoxia was only partially reversed, and there was additional cardiovascular stimulation, in contrast to the previously reported tendency for arterial blood pressure to return towards conscious control values during the course of action of Immobilon.
Brown RF, Houpt KA, Schryver HF.In two adult horses doses of 0.02-0.03 mg/kg diazepam, intravenously, increased 1 hr intake 54-75% above control levels. Intake was stimulated when the diet was a high grain, calorically dense one and also when the diet was a high fiber, calorically dilute one. Two young rapidly growing weanling horses showed an even more pronounced stimulation of intake. Following diazepam 1 hr intake was increased 105-240% above control lelvels. Promazine at a dose of 0.5 mg/kg also stimulated intake in adult horses, but not as markedly as did diazepam. A transquilizer and a neuroleptic appear to have a stim...
Evans JA, Lambert MB, Miller J.The anti-inflammatory drug Ibuprofen [(+/-)-2-(p-isobutylphenyl) propionic acid] was estimated in the blood and urine of a horse using gas-liquid chromatography of the silylated derivative. Levels of the drug in the two body fluids were measured over a period of about 24 hours after administering a 12 gm dose of Ibuprofen. Plasma peak levels were observed within 30 to 60 min, and the drug was no longer detectable in the plasma by 8 hr. Urinary peak levels were observed 200 to 300 min after dosing, and the drug was no longer detectable in the urine by about 28 hr. It was observed that only 2% t...
Tobin T, Blake JW, Sturma L, Arnett S.Procaine added to whole equine blood or diluted plasma was hydrolyzed with half times of approximately 9 and 12 minutes, respectively, at 37 C. This hydrolytic activity was sensitive to heating and physostigmine, but did not affect procainamide. At pharmacologic concentrations of procaine, the rate of the hydrolytic reaction depended directly on the concentrations of plasma or procaine in the system and was less in whole blood than in plasma. These properties are consistent with hydrolysis being due to plasma esterases operating at less than saturating procaine concentrations. These esterases ...
Tobin T, Swerczek TW, Blake JW.This report concerns the detection and acute toxicity of pine oil (a commercially available disinfectant) after intravenous administration in horses. alpha Terpineol was identified as a major constituent of pine oil. alpha Terpineol was recovered from equine tissues by extraction into heptane and detected by gas chromatography, using either flame ionization detection or pentafluoropropionic anhydride derivatization and electron capture detection. After intravenous injection of 0.1 ml/kg, death due to massive pulmonary edema occurred within minutes. In this animal blood and tissue levels of alp...
Tobin T, Blake JW.Since procaine has both local anaesthetic and central stimulant actions its presence in the blood or urine of racing horses is forbidden. After rapid intravenous injection of procaine HC1 (2.5 mg/Kg) in thoroughbred mares plasma levels of this drug fell rapidly (t 1/2 alpha = 5 min) and then more slowly (t 1/2 beta = 50.2 min). These kinetics were well fitted by a two compartment open model (Model I). This model gave an apparent Vdbeta for procaine in the horse of about 3,500 litres. Since procaine was about 45% bound to equine plasma protein this gives a true Vdbeta for procaine of about 6,50...
Blake JW, Tobin T.Three gas-liquid chromatographic (G.L.C.) procedures discussed have been designed around the four "esses" of detection tests--speed, sensitivity, simplicity, and specificity. These techniques are admirably applicable to the very low plasma drug levels encountered in blood testing under pre-race conditions. The methods are equally applicable to post-race testing procedures, where both blood and urine samples are tested. Drugs can only rarely be detected by the electron capture detector (E.C.D.) without a prior derivatization step, which conveys to the drug(s) high electron affinity. Because of ...
Courtot D.At the request of the Service des Haras, our laboratory works on the toxicological problems of the sport-horse. These studies have resulted in the setting up of an anti-doping control for equestrian competitions of various types, not only flat racing. During events, horses, must be calm and docile to the riders' order. Frequently, the latter use tranquillizers to try and win events. The analytical method for the research and identification of these compounds is described. The technique involves successively: 1. alkalinisation of the sample - saliva, blood or urine after enzymatic hydrolysis. 2...
Tobin T, Blake JW, Tai CY, Arnett S.Rapid intravenous injection of 1 g of procaine hydrochloride in Thoroughbred mares produced variable signs of central nervous system excitation for as long as 4 minutes. Plasma concentrations of procaine were similarly variable and transient, decreasing with a half-life of approximately 25 minutes. In vitro, plasma from freshly collected equine blood hydrolyzed procaine with a half-life of approximately 7.5 minutes. This hydrolysis was apparently due to plasma esterases. Penicillin, when added free or complexed as procaine-penicillin, did not protect procaine against hydrolysis by these plasma...
Sanford J.The usefulness of an antibiotic depends not only upon its antibacterial potency and spectrum but also on the prevalence of resistant organisms and the extent and severity of the adverse reactions to which it may give rise. Variations in formulation of the same compound are reflected in differences in bioavailability. These may be intentional, as in the development of long-acting preparations, but may also be unexpected following differences in drug purity, content and gastro-intestinal absorption. Individual and species differences in treated animals also result in variations in bioavailabilit...
Gopinath G, Ford EJ.The hepatotoxic effect of oral halothane in the horse is increased by pretreatment with phenobarbitone or DDT but not by chlorpromazine. Phenobarbitone and DDT increase the activity of hepatic amidopyrine N-demethylase but chlorpromazine does not. Carbon disulphide protects the liver of the horse against halothane.
Lyons ET, Drudge JH, Tolliver SC.Critical tests of the activity on large strongyles, ascarids, mature pinworms, and bots were carried out in 11 horses intraorally treated with a paste formulation of thiabendazole. The dose level of 44 mg/kg was administered to 3 horses, and the dose level of 88 mg/kg to 8 horses. Removals of Strongylus vulgaris and mature Oxyuris equi were 100% at the 2 dose levels, and efficacy against Strongylus edentatus varied from 95 to 99% and 89 to 100% for the 44- and the 88-mg/kg dose levels, respectively. Strongylus equinus was completely removed from the 1 infected horse treated at the dose level o...
Bland SA, Blake JW, Ray RS.Mefenamic acid is extracted from biological fluids and is acylated with pentafluoropropionic anhydride to form a derivative possessing high electron affinity. The derivative is analyzed by gas-liquid chromatography with an electron capture detector. The method is particularly valuable for determining drug levels in blood where small sample and/or drug concentrations are available.
Hillidge CJ, Lees P.The neuroleptanalgesic drug combination of
etorphine and acepromazine (Large Animal
Immobilon; Reckitt & Colman Ltd.) was
administered i.v. at the recommended dose rate
(24 ,ug/kg etorphine and 100 pg/kg acepromazine)
to twelve Welsh Mountain ponies of 185 to 336 kg
bodyweight. Cardiovascular measurements were
made before and at pre-determined times up to
30 min after the injection. The etorphine
antagonist, diprenorphine (Revivon; Reckitt &
Colman Ltd.), was then injected i.v. (30,ug/kg)
and further measurements were obtained.
Pronounced increases in heart rate, moderate
increase...
Drudge JH, Lyons ET, Taylor EL.Three series of critical tests were completed on a combined total of 46 horses to determine the efficacy of single doses of trichlorfon against bots, ascarids, pinworms, and large strongyles. Different formulations of trichlorfon were administered by tubing intragastrically, mixing with the daily grain ration, injecting intramuscularly, or pouring on the back at dose rates between 20 and 100 mg/kg. Administration by feeding tended to be more efficacious for removal of bots and less toxic to the horese than administration by stomach tube. In many of the tests, trichlorfon was given in the grain...
Dürr A.The affinity and the binding capacity of horse serum proteins for ampicillin and penicillin G were measured by equilibrium dialysis or ultrafiltration technique. From the figures thus obtained it may be concluded that in the range of therapeutic concentrations the protein-bound fraction accounts for 6 X 8-8 per cent of the total ampicillin concentration and for 52-54 per cent of the total penicillin G concentration in serum. The rate of elimination of ampicillin and penicillin G in horses was assessed by following serum concentrations after a single intravenous injection. The biological half l...
Bauer C, Bürger HJ.A paste formulation containing 14.3 per cent of oxibendazole and 44 per cent of trichlorfon was administered to 33 ponies and horses. The dose rate used was equivalent to 10 mg and 30 mg/kg bodyweight, of oxibendazole and trichlorfon respectively. After treatment 25 animals passed between one and 82 third stage larvae of Gasterophilus intestinalis in their faeces. Dosing with 0.2 mg ivermectin/kg bodyweight three weeks later resulted in six animals expelling between one and four bots. The efficacy of the oxibendazole-trichlorfon paste was on average 96.2 per cent. This drug combination given t...
Stahl J, Braun M, Siebert J, Kietzmann M.A water based combination of 0.1% octenidine dihydrochloride and 2% 2 - phenoxyethanol is registered in many European countries as an antiseptic solution (octenisept®) for topical treatment with high antimicrobial activity for human use, but octenidine based products have not been registered for veterinary use yet. The aim of the present study was to investigate whether octenidine dihydrochloride or 2 -phenoxyethanol, the two main components of this disinfectant, permeate through animal skin in vitro. Therefore, permeation studies were conducted using Franz-type diffusion cells. 2 ml of the t...
van der Kolk JH, Wisse H, van Dijk S.A 20-year-old Arab crossbred gelding was examined because it had apparently suffered an overstimulation of the parasympathetic nervous system for three hours. The clinical signs consisted of hypersalivation, profuse sweating, maximal miosis, fasciculation of the muscles and lateral recumbency in combination with continuous convulsions without diarrhoea. The horse's plasma pseudocholinesterase activity was approximately 10 per cent of normal. It responded well to 10 mg atropine and 50 mg diazepam administered intravenously.
Colahan PT, Bailey JE, Chou CC, Johnson M, Rice BL, Jones GL, Cheeks JP.Twelve clinically sound, healthy, athletically conditioned Thoroughbred horses were subjected to an incremental exercise stress test to determine the effects and period of detection of a single dose of flunixin meglumine (1.1 mg/kg by intravenous injection) in serum and urine by ELISA. Flunixin concentrations, performance, and hematologic and clinical chemical parameters were measured. All horses were rotated through four treatment groups of a Latin-square design providing for each horse to serve as its own control. Flunixin meglumine reduced prostaglandin F(1alpha) and thromboxane concentrati...
Ramsay EC, Geiser D, Carter W, Tobin T.To compare the effect of orally delivered detomidine on head posture when administered alone or in combination with two different food items, and to determine the serum concentrations of detomidine after oral delivery. Methods: Prospective randomized experimental study. Methods: Fifteen adult grade mares weighing 328-537 kg. Methods: The horses were randomly assigned to one of the three treatment groups (five horses each). The groups were given detomidine (0.06 mg kg): alone; mixed with 3 mL of an apple sauce and gum mixture; or mixed with 3 mL molasses. Head droop, measured before treatment a...
Martin EM, Schirmer JM, Jones SL, Davis JL.Misoprostol is an E prostanoid (EP) 2, 3 and 4 receptor agonist that is anecdotally used to treat and prevent NSAID-induced GI injury in horses. Misoprostol elicits anti-inflammatory effects in vivo in men and rodents, and inhibits TNFα production in equine leucocytes in vitro. Objective: Define the pharmacokinetic parameters of oral misoprostol in horses, and determine the inhibitory effect of oral misoprostol administration on equine leucocyte TNFα production in an ex vivo inflammation model. Methods: Pharmacokinetic study, ex vivo experimental study. Methods: Six healthy adult horses ...
Brumbaugh GW, Thomas WP, Hodge TG.A 4-year-old Quarter Horse gelding with atrial fibrillation, mitral regurgitation, and signs of bilateral congestive heart failure was initially treated IV with digoxin and furosemide. After parenteral digitalization, a daily maintenance dose of digoxin was administered orally at a rate of 21.7 micrograms/kg of body weight. At this dosage, a steady-state serum digoxin concentration of 2.3 ng/ml was achieved without clinical signs of toxicosis. The furosemide dosage was decreased and eventually discontinued as clinical improvement occurred. Clinical signs of congestive heart failure were contro...
Brumbaugh GW, Thomas WP, Enos LR, Kaneko JJ.Digoxin was administered orally and intravenously to seven healthy adult mares and geldings in two separate trials. At a dose of 44 microgram digoxin/kg body weight, the oral study was characterized by an absorption phase with a mean (+/- 1 standard deviation) peak serum digoxin concentration of 2.21 ng/ml (+/- 0.45) at a mean of 2.29 h (+/- 1.52) after administration. A second rise in serum digoxin concentration started about 6-8 h after administration and extended to about 20 h after administration. The mean bioavailability (F) was 23.38% (+/- 5.96). At a dose of 22 microgram digoxin/kg body...
Berlin S, Kirschbaum A, Spieckermann L, Oswald S, Keiser M, Grube M, Venner M, Siegmund W.The treatment of equine lung infections by Rhodococcus equi with rifampicin is empirically based because pharmacokinetic/pharmacodynamic (PK/PD) indices and pivotal clinical outcome data are not available. Objective: To evaluate the pharmacokinetics and pulmonary distribution of rifampicin into epithelial lining fluid (ELF) and bronchoalveolar lavage cells (BALC) to predict antimicrobial activity in the lung using PK/PD indices. Methods: Controlled, randomised, two-period, crossover, repeated-dose study with an initial arm to measure disposition after i.v. administration of rifampicin. Methods...
Nagy A, Bodo G, Dyson SJ, Szabo F, Barr AR.Proximal diffusion of local anaesthetic solution after perineural anaesthesia may lead to the desensitisation of structures other than those intended. However, there is no evidence-based study demonstrating the potential distribution and diffusion of local anaesthetic solution after perineural analgesia in the distal limb. Objective: To document the potential diffusion of local anaesthetic solution using a radiopaque contrast model and to evaluate the influence of walking compared with confinement in a stable after injection. Methods: Radiopaque contrast medium was injected subcutaneously over...
Manohar M, Goetz TE, Sullivan E, Griffin R.The present study was carried out to examine the effects of phenylbutazone treatment on the pulmonary haemodynamic effects of frusemide in strenuously exercising horses. Using catheter mounted manometers, whose in vivo signals were referenced at the point of the shoulder, heart rate, right atrial, right ventricular and pulmonary vascular pressures were measured in 3 different sets of experiments. Seven Thoroughbreds were subjected to 1) control (no medications), 2) frusemide control and 3) phenylbutazone + frusemide. The experiments were carried out in random order and were separated by 7 days...
Garcia P, Paris AC, Leufroy A, Popot MA, Bonnaire Y.A quantitative method, using LC/ESI-MS(n) with a quadrupole linear ion trap mass analyzer, has been developed for the analysis of ipratropium cation in horse plasma and urine. The method applies solid-phase extraction with WCX cartridges for plasma and MM2 cartridges for urine, prior to analysis by LC/ESI-MS(n). The efficiency of extraction combined with the sensitivity and the selectivity of MS(n) allows for the quantification of ipratropium cation at picogram per milliliter levels. The analytical capabilities of the method have been successfully checked by the quantitative analysis of ipratr...
Hanson RR.Suitable use of prophylactic antimicrobial drugs for wounds depends on the accurate selection of appropriate antibiotics, dosing regimen, and duration of use. Regional intravenous delivery and intraosseous infusion of antibiotics are pivotal to a successful outcome for deep-rooted infections, inadequately perfused tissue, and infected wounds containing biofilm. Antibiotic-impregnated polymethylmethacrylate beads are predominantly helpful for wounds that have a poor blood supply and for those containing surgical implants that must remain in place.
Younkin JT, Santschi EM, Kukanich B, Lubbers BV, Warner M.Penicillin is administered intravenously (IV) or intramuscularly (IM) to horses for the prevention and treatment of infections, and both routes have disadvantages. To minimize these shortcomings, a 24-hr hybrid administration protocol (HPP) was developed. Our objective was to determine penicillin plasma concentrations in horses administered via HPP. Venous blood was collected from seven healthy horses administered IV potassium penicillin G at 0 and 6 hr and IM procaine penicillin G at 12 hr. Blood was collected at 2-hr intervals from 0 to 20 hr and at 24 hr. Plasma penicillin concentration...
Dirikolu L, Lehner AF, Hughes C, Karpiesiuk W, Camargo FC, Harkins JD, Woods WE, Bosken JM, Boyles J, Troppmann A, Fisher M, Tobin T.Furosemide is a potent loop diuretic used for the prevention of exercise-induced pulmonary hemorrhage in horses. This drug may interfere with the detection of other substances by reducing urinary concentrations, so its use is strictly regulated. The regulation of furosemide in many racing jurisdictions is based on paired limits of urinary SG (100 ng/ml). To validate this regulatory mechanism, a liquid chromatography/mass spectrometry/mass spectrometry method employing a solid-phase extraction procedure and furosemide-d5 as an internal standard was developed. The method was used to determine th...
Cunningham FM, Andrews M, Landoni MF, Lees P.Calcium ionophore A23187 induced time and concentration dependent production of immunoreactive leukotriene (LT) B4 by equine heparinized whole blood in vitro. Time dependent production of immunoreactive LTB4 by equine neutrophils and immunoreactive LTC4 by equine eosinophils in vitro was also demonstrated. The 5-lipoxygenase activating protein (FLAP) inhibitors, BAY X 1005 and BAY Y 1015, produced concentration dependent inhibition of ionophore-induced LTB4 synthesis by equine whole blood (mean +/- SEM IC50s n = 5; 6.14 +/- 0.28 microM vs. 12.30 +/- 0.75 microM for BAY Y 1015 and BAY X 1005, r...
Werners A, Karasek I, Butler C, Yeatts J, Enomoto H, Baynes R.Several different tick species are known to infest horses. Aside from causing serious health and welfare issues, including anaemia, ill thrift, and immunosuppression, ticks can transmit a variety of important, sometimes zoonotic, pathogens. The successful prevention and treatment of tick infestations have been described, but the information is scarce and, in many instances, anecdotal. Here we describe a practical and affordable prevention of tick infestation by using abamectin-impregnated cattle ear tags affixed to a safety collar. We have assessed the radial distribution of abamectin by analy...
Hagedorn HW, Meiser H, Zankl H, Schulz R.The misuse of opiates in racehorses relates to their effect of increasing locomotor activity. Because methadone, a narcotic analgesic, has been suspected of use as a doping compound in the past, it was added to the list of banned drugs and should be considered in doping control. Because the literature fails to provide information on detection of methadone in blood or urine of horses, an enzyme-linked immunosorbent assay was developed to monitor this narcotic in equine body fluids. Combined with high-performance liquid chromatography, the immunoassay also served to confirm positives indicated b...
Prichard RK, Geary TG.Macrocyclic lactone (ML) anthelmintics are the most important class of anthelmintics because of our high dependence on them for the control of nematode parasites and some ectoparasites in livestock, companion animals and in humans. However, resistance to MLs is of increasing concern. Resistance is commonplace throughout the world in nematode parasites of small ruminants and is of increasing concern in horses, cattle, dogs and other animals. It is suspected in Onchocerca volvulus in humans. In most animals, resistance first arose to the avermectins, such as ivermectin (IVM), and subsequently to...
Söylemez Z, Ozer I.The inhibition of horse plasma cholinesterase by propranolol showed characteristics which depended upon the identity of the substrate used. With butyrylthiocholine as substrate, the inhibition showed a first-order dependence on inhibitor concentration, and was characterized by a Ki of 8 microM (pH 7.4, 20 degrees C). With p-nitrophenylbutyrate as substrate, a biphasic v-1 versus [I] relationship was obtained. The biphasic curve could be resolved into two components, with apparent Ki's of 9 microM and 1.3 mM. Use of butyrylthiocholine as alternative substrate resulted in partial inhibition of p...
Hayami A, Darwish WS, Ikenaka Y, Nakayama SM, Ishizuka M.There is little information about drug metabolism and pharmacokinetics in horses. Therefore, it is necessary to characterize the profiles of drug metabolites for the safe use of drugs. In this study, we focused on cytochrome P450 enzymes (CYPs), which represent an important enzyme group to determine pharmacological effects of drugs. We chose diazepam as the drug of choice for this study. The aim of this study was to elucidate the metabolic pathway of diazepam in horses in comparison with rats, and to clarify CYP subfamilies responsible for diazepam metabolism in horses. Our results showed tema...
Easter JL, Hague BA, Brumbaugh GW, Nguyen J, Chaffin MK, Honnas CM, Kemper DL.To evaluate the effect of peritoneal lavage on pharmacokinetics of gentamicin sulfate in healthy horses after experimental celiotomy. Methods: 13 clinically normal horses. Methods: Horses were randomly assigned to control or experimental groups. All horses received gentamicin (6.6 mg/kg of body weight, IV, q 24 h) before surgery, underwent experimental abdominal surgery, and had abdominal drains placed percutaneously. Horses of the experimental group received postoperative peritoneal lavage; horses of the control group did not receive peritoneal lavage. The day after surgery, 24 hours after th...
Lavy E, Ziv G, Glickman A.An aqueous solution of norfloxacin nicotinate (NFN) was administered to donkeys (Aquus asinus) intravenously (once at 10 mg/kg), intramuscularly and orally (both routes once at 10 and 20 mg/kg, and for 5 days at 20 mg/kg/day). Blood samples were collected at predetermined times after each treatment and urine was sampled after intravenous drug administration. Serum NFN concentrations were determined by microbiological assay. Intravenous injection of NFN over 45-60 s resulted in seizures, profuse sweating and tachycardia. The intravenous half-life (t1/2 beta) was 209 +/- 36 min, the apparent vol...
Ferrante PL, Freeman DE, Ramberg CF, Kronfeld DS.Multicompartmental analysis was applied to study the kinetics of D-xylose distribution after IV administration to healthy mares deprived of food for 12 and 96 hours. Urinary excretion of D-xylose was measured over a 15-hour period after administration. The plasma D-xylose concentrations in this study were in the range found after oral tolerance testing. The disposition of D-xylose was described by a two-compartment model with linear kinetic characteristics. Total volume of distribution decreased significantly (P < 0.025) from 0.270 L/kg of body weight after the 12-hour period of food depriv...
Sisodia CS, Kramer LL, Gupta VS, Lerner DJ, Taksas L.Pharmacological disposition of chloramphenicol was studied in horses. Minimum levels of the antibiotic (greater than or equal to 5 mu g/ml) in blood or plasma recommended to combat infections could not be achieved by 4.4 and 8.8 mg/kg I.V. or 30 and 50 mg/kg I.M. or 30 mg/kg oral (as palmitate salt) doses of chloramphenicol. Increasing the dose to 19.8 and 26.4 mg/kg I.V. provided such levels for about two and three hours respectively. A combination of 20 mg/kg I.V. and 30 mg/kg I.M. administered simultaneously did not provide more prolonged levels than 26.4 mg/kg I.V. alone. Chloramphenicol s...
Ducharme NG, Dill SG, Shin SJ, Schwark WS, Ducharme GR, Beilman WW.This preliminary study evaluated phenoxymethyl penicillin (Penicillin V) as an alternative to parenteral administration of penicillin in horses. Penicillin V was administered orally to five horses at two different doses and plasma levels of the drug were determined at timed intervals. The results were evaluated by regression analysis. Following the administration of penicillin V at a dose of 66,000 IU/kg or 110,000 IU/kg, the mean peak plasma levels obtained were 1.55 micrograms/mL and 2.34 micrograms/mL respectively. A plasma level two to four times above the minimal inhibitory concentration ...
Landuyt J, Delbeke FT, Debackere M.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...
Harðardóttir H, Murison PJ, Blissitt K, Olason S, Clutton RE.Ketamine at 2.2 mg/kg given i.v. is often used to induce anaesthesia for surgical procedures in horses under field conditions. Commonly, additional doses are needed to complete the surgery. We hypothesised that surgical conditions would be improved when 5 mg/kg of ketamine was used to induce anaesthesia, while induction and recovery qualities would not differ from those when 2.2 mg/kg ketamine was used. Objective: To compare the anaesthetic effects of two ketamine doses (5 and 2.2 mg/kg) during field anaesthesia for castration of horses. Methods: Prospective, randomised, blinded, clinical stud...
Dobler D, Gerber M, Schmidts TM, Runkel F, Schlupp P.Human nail diseases, mostly caused by fungal infections, are common and difficult to treat. The development and testing of new drugs and drug delivery systems for the treatment of nail diseases is often limited by the lack of human nail material for permeation studies. Animal material is frequently used, but there are only few comparative data on the human nail plate, and there is neither a standardized test design nor a nail bed analogue to study drug uptake into the nail. In this study, a new permeation device was developed for permeation studies, and the permeation behavior of three model s...
Roberts MC, Seawright AA.Colic was induced in horses and ponies following topical or intravenous (iv) administration of amitraz, a formamidine acaricide. The condition was characterised by rapid cessation of intestinal sounds, stasis, extensive impaction and tympany throughout the large colon. Three animals that were necropsied had a faecalith obstructing the proximal small colon aboral to marked colonic impaction. A reproducible and reversible impaction colic syndrome could be induced by an iv injection of 1 mg amitraz/kg body weight in solvent. There were immediate central nervous system and intestinal signs. Large ...
