Oral administration in horses refers to the delivery of medications, supplements, or nutrients via the mouth. This method is commonly used in equine veterinary medicine for its practicality and ease of use. Oral formulations can include powders, pastes, or liquids, which are designed to be palatable and easily ingested by horses. The effectiveness of oral administration depends on factors such as the horse's digestive physiology, the formulation of the product, and the consistency with which it is administered. This page compiles peer-reviewed research studies and scholarly articles that explore the techniques, efficacy, and considerations of oral administration in equine care.
Matthews NS, Gleed RD, Short CE, Burrows K.Isoxsuprine (0.6 mg/kg) administered IV to 6 standing horses produced substantial, transient decreases in systemic blood pressure, systemic vascular resistance, and stroke volume. It also produced substantial, transient increases in heart rate, cardiac output, and purposeful movement. Plasma concentrations of isoxsuprine peaked soon after the drug was administered IV and then decreased over a 12-hour period in a biexponential manner, with distribution and elimination half-lives of 14 minutes and 2.67 hours, respectively. Total body clearance and steady-state volume of distribution were calcula...
Lees P, Higgins AJ, Mawhinney IC, Reid DS.The absorption pattern of phenylbutazone was studied in five horses during administration of the drug in a paste formulation on days 1, 5, 8 and 12 of a 12-day dosing schedule. Since two or more plasma concentration peaks were usually obtained following each oral dose, it was concluded that phasic absorption was a particular feature of the oil:water formulation of the product. Possible causes of this unusual absorption pattern are discussed and the therapeutic implications of both phasic absorption and the recorded values of Cmax, tmax and AUC024 for phenylbutazone and its active metabolite ox...
Köhler M, Hiepe T.Efficacy of Ivermectin in combating Strongyloides westeri infection of foal. The efficacy of Ivermectin and Mebendazol in combating spontaneous Strongyloides westeri infections in foals has been tested by examining faecal egg output reduction. Ivermectin as a paste formulation was given to sucking foals and pregnant mares in a single dosage of 200 micrograms/kg bodyweight by oral administration. A high efficacy of Ivermectin in combating patent Strongyloides westeri infection could be demonstrated; no side effects have been observed. Mebendazol at a dosage rate of 8 mg/kg did not yield satisfa...
Sweeney RW, Sweeney CR, Soma LR, Woodward CB, Charlton CA.Serum and peritoneal fluid concentrations of metronidazole were determined in 6 healthy adult horses given the drug (25 mg/kg) by IV or oral routes. The disposition of metronidazole in horses given the drug by the IV route conformed to a 2-compartment model with a distribution half-life of 0.16 hours, an elimination half-life of 2.9 hours, and a body clearance of 0.40 +/- 0.05 L/kg/hr. The oral absorption half-life was 0.40 hours, and the bioavailability, 85.0 +/- 18.6%. Peritoneal fluid concentrations were approximately equal to serum concentrations at all times, regardless of the route of ad...
Seibert BP, Newcomb KM, Michael BF.Critical tests were done on 24 naturally parasitized horses to compare the antiparasitic activity of an oral paste preparation of mebendazole and trichlorfon with that of the marketed powder formulation. Each formulation was administered at the recommended dosages of 8.8 mg of mebendazole and 40 mg of trichlorfon/kg of body weight. Efficacy of the paste formulation ranged from 97.7% to 100% against 2nd- and 3rd-stage Gasterophilus spp, adult Strongylus vulgaris, S edentatus, Parascaris equorum, small strongyles; and larval and adult forms of Oxyuris equi. Adverse effects were generally limited...
Pollitt CC, Holdsworth PA, Kelly WR, Meacham CS, Sheahan B.A single oral dose of ivermectin paste was administered to 12 horses with dermatitis and clinical signs typical of onchocerciasis. Two of the horses also had lesions of Queensland itch. Microfilarias of Onchocerca cervicalis were identified in fresh, macerated, skin biopsies from the neck, brisket or umbilical regions of all horses and microfilarias of O. gutturosa from the neck of 2. Eight of the horses developed skin reactions 4 to 24 h after the administration of the ivermectin, notably weals over the neck, shoulders and flanks and pitting oedema of the ventral midline and intermandibular s...
DiPietro JA, Todd KS, Reuter V.Four groups of 10 horses (mares) each were treated with a 1% solution of ivermectin (200 micrograms/kg of body weight) in a propylene glycol-glycerol formal base orally, a 1% solution of ivermectin (200 micrograms/kg) in a propylene glycol-glycerol formal base via nasogastric tube, a 1.87% paste of ivermectin (200 micrograms/kg) orally, or a 22.7% paste of oxibendazole (10 mg/kg) orally. Fecal examinations were done before treatment and on posttreatment days (PTD) 14, 28, 42, 56, and 70. Strongyle egg per gram counts and sugar flotation fecal examinations were performed. Results of fecal exami...
Tobin T, Chay S, Kamerling S, Woods WE, Weckman TJ, Blake JW, Lees P.Phenylbutazone is an acidic, lipophilic, non-steroidal anti-inflammatory drug (NSAID). It is extensively metabolized in the horse. The metabolites so far identified, oxyphenbutazone, gamma-hydroxyoxyphenbutazone, account for some 25-30% of administered dose over 24 h. The plasma half-life of phenylbutazone and termination of its pharmacological action are determined primarily by its rate of hepatic metabolism. Phenylbutazone acts by inhibiting the cyclooxygenase enzyme system, which is responsible for synthesis of prostanoids such as PGE2. It appears to act on prostaglandin-H synthase and pros...
Maitho TE, Lees P, Taylor JB.The disposition of phenylbutazone (4.4 mg/kg), administered intravenously to six Welsh Mountain ponies, was described by a two-compartment open model. Pharmacokinetic parameters were not significantly different after morning dosing in comparison with afternoon dosing. When phenylbutazone (4.4 mg/kg) was administered orally to the same ponies, marked variations in time to peak concentrations were produced with different feeding schedules. When access to hay was permitted before and after dosing, the mean time to peak concentration was 13.2 +/- 1.2 h and double peaks in the plasma concentration-...
Donecker JM, Sams RA, Ashcraft SM.The pharmacokinetics and bioavailability of probenecid given IV and orally at the dosage level of 10 mg/kg of body weight to mares were investigated. Probenecid given IV was characterized by a rapid disposition phase with a mean half-life of 14.0 minutes and a subsequent slower elimination phase with a mean half-life of 87.8 minutes in 5 of 6 mares. In the remaining mare, a rapid disposition phase was not observed, and the half-life of the elimination phase was slower (172 minutes). The mean residence time of probenecid averaged 116 minutes for all 6 mares and 89.2 minutes for the 5 mares with...
Christensen JM, Blythe LL, Craig AM.Phenylbutazone was administered to six Thoroughbred horses in a cross-over study in which the horses received cimetidine pretreatment or no cimetidine pretreatment. Blood samples were collected at various times for 48 h after phenylbutazone administration and the plasma was analysed for phenylbutazone. Cimetidine pretreatment elevated phenylbutazone plasma concentrations during the first 8 h after phenylbutazone administration. The absorption rate, maximum phenylbutazone plasma concentrations and AUC were significantly greater with cimetidine pretreatment. The half-life of phenylbutazone did n...
Errecalde JO, Button C, Mülders MS.A single intravenous administration of theophylline as aminophylline at 10 mg/kg to four mares induced a diuresis in which maximal urine production was more than seven times the control volume. The diuretic effect was maximal within the first hour post-administration, and lasted approximately 6 h. Theophylline resulted in dose-related tachycardia, polypnoea and nervous symptoms (tactile, visual and auditory hypersensitivity, muscle tremor, sweating) in normal mares, but had only minor effects on arterial and central venous blood pressures, intrapleural pressure, red blood cell variables and pl...
Thomas DE, Beadle RE.The pharmacokinetics of 3-methylindole (3MI) given orally in 2 doses (10 mg/kg and 20 mg/kg) to horses were determined. The pharmacokinetic plasma-concentration profiles for 3MI (10- and 20-mg/kg dosages) in horses were represented by a 2-compartment open model with first-order absorption, as determined by nonlinear least-squares regression analysis. Absorption of 3MI at both dosages was rapid. Comparisons of the peak plasma concentrations, the postdistribution half lives, total clearances, and areas under the curve of the plasma-concentration profiles between the 10- and the 20-mg/kg dosages ...
Britt DP, Preston JM.The efficacy of orally administered ivermectin against induced Dictyocaulus arnfieldi infection was evaluated in a controlled study comprising 12 yearling ponies. Treatment with ivermectin paste, at a dose rate of 200 micrograms/kg bodyweight orally once, was 100 per cent effective against both adult and immature or inhibited stages of the horse lungworm. Similar control of second and third instars of Gastrophilus intestinalis was observed and no nematode eggs were present in faeces from seven to 15 days after treatment when the study was terminated.
Lees P, Maitho TE, Taylor JB.A clinical dose rate (4.4 mg/kg bodyweight) of phenylbutazone was administered intravenously and orally to six Welsh mountain ponies to provide data on the pharmacokinetics and bioavailability of the drug. In three, three-year-old ponies, clearance of the drug from plasma after intravenous administration was almost twice as rapid as in three ponies aged eight to 10 years. After oral administration, plasma phenylbutazone levels were greater in the older ponies, the area under the plasma concentration time curve being almost twice as high. This did not result from more efficient absorption but f...
Ingvast-Larsson C, Paalzow G, Paalzow L, Ottosson T, Lindholm A, Appelgren LE.The pharmacokinetics of theophylline were determined in Standardbred trotters after single intravenous and oral administration. A bi-exponential equation was fitted to the intravenous data and a tri-exponential equation to the oral data. The biological half-life of theophylline was found to be 14.8 h, the volume of distribution 1.02 l/kg and the total plasma clearance 0.86 ml/kg/min. The oral absorption of the drug was complete (bioavailability 108%) and rapid (absorption half-life 0.4 h).
Burrows GE, MacAllister CG, Beckstrom DA, Nick JT.The plasma concentrations and pharmacokinetics of rifampin disposition were determined after a single IV, IM, or oral dose of 10 mg/kg of body weight and an oral dose of 25 mg/kg. The overall elimination rate constants per minute were similar for the 10 mg/kg dose (0.0021 +/- 0.0004, IV; 0.0017 +/- 0.0002, IM; and 0.0023 +/- 0.0006, orally). The apparent bioavailability was moderate to low for IM and oral administrations (59.8% +/- 3.2% and 39.5% +/- 5.0%, respectively). The rate of absorption was most rapid for oral administration with an absorption half-life of 249.7 +/- 71.6 minutes as comp...
Guerrero J, Newcomb K, Seibert BP, Michael BF.Two controlled tests were conducted in equine foals and yearlings to determine the optimal oral dosage and the duration of activity of closantel for the prevention of Gasterophilus spp larval infections. Additional data were collected on the activity of closantel against Strongylus vulgaris larval infections. In experiment 1, 12 foals and 12 yearlings were equally allocated to 4 experimental groups, and were given oral treatments with closantel at dosages of 0 (nontreated controls), 2, 5, or 8 mg/kg of body weight every 2 months during bot season. The foals and yearlings were allowed to graze ...
Bogan JA, Galbraith A, Baxter P, Ali NM, Marriner SE.Phenylbutazone, sulphadiazine and trimethoprim were administered to three horses on two occasions, recently fed and unfed, and the effect of feeding on the pharmacokinetics of the three drugs assessed. The mean peak concentrations of phenylbutazone and trimethoprim were reduced by feeding by 34 and 75 per cent, respectively. The pharmacokinetics of sulphadiazine were not significantly affected.
Chay S, Woods WE, Nugent TE, Weckman T, Houston T, Sprinkle F, Blake JW, Tobin T, Soma LR, Yocum J.Experiments to determine the residual plasma concentrations of phenylbutazone and its metabolites found in horses racing on a 'no-race day medication' or 24-h rule were carried out. One dosing schedule (oral-i.v.) consisted of 8.8 mg/kg (4 g/1000 lbs) orally for 3 days, followed by 4.4 mg/kg (2 g/1000 lbs) intravenously on day 4. A second schedule consisted of 4.4 mg/kg i.v. for 4 days. The experiments were carried out in Thoroughbred and Standardbred horses at pasture, half-bred horses at pasture, and in Thoroughbred horses in training. After administering the i.v. schedule for 4 days to Thor...
Slocombe JO, Cote JF.Thirteen Standardbred horses, two to five years of age, were treated with ivermectin paste per os at 200 mug/kg of body weight and 13 were untreated. Two weeks after treatment, previously untreated horses were given the paste. Fecal samples were collected from all horses at the time of treatment and periodically thereafter up to 14 weeks and were examined for nematode eggs using the Cornell-McMaster dilution and the Cornell-Wisconsin double centrifugation procedures.All horses consumed the paste readily and had no signs of toxicosis. Strongyle eggs were found in the feces of all horses before ...
Muylle E, Nuytten J, Van den Hende C, Deprez P, Vlaminck DK, Oyaert W.The concentration of potassium in the red blood cells in 15 horses with severe diarrhoea was determined. The red blood cell potassium content (RBCK+) was low compared with levels obtained in normal horses. The decrease in the RBCK+ was used to evaluate the total body potassium deficit. This calculated amount was administered orally, following each RBCK+ determination. In those horses which recovered, RBCK+ content returned to normal levels. During treatment, refilling of the red blood cells with potassium occurred only gradually as long as the diarrhoea persisted. In each case, oral loading wi...
Brown MP, Gronwall R, Kroll WR, Beal C.Five foals from two to three days old were given a single oral dose of ampicillin trihydrate (20 mg/kg bodyweight [bwt]). Serum ampicillin concentrations were measured serially over a 24 h period. The study was repeated in the same foals at 16 to 21 days old. The mean peak serum ampicillin concentration at two to three days old was 5.0 micrograms/ml at 1 h after treatment; the mean peak serum concentration at 16 to 21 days old was 2.7 micrograms/ml at 2 h. The concentrations steadily declined and ampicillin was not detected in the serum from any of the foals by 24 h. Serum clearance averaged 1...
Presson BL, Hamm D, Yazwinski TA, Pote LM.Critical tests were performed on 6 horses to evaluate the antiparasitic effectiveness of oxfendazole given in combination with trichlorfon in a paste formulation. Treatments were given orally as a single dose. The rates of active ingredient administration were 2.5 and 40 mg/kg of body weight for oxfendazole and trichlorfon, respectively. The combined activities of the 2 antiparasitic compounds proved 100% efficacious in the removal of adult Strongylus vulgaris, S edentatus, Oxyuris equi, and Parascaris equorum. Fourth stage O equi, and 2nd and 3rd instars of Gasterophilus nasalis also were com...
Breeze RG, Brown CM, Turk MA.3-methylindole was administered orally and intravenously to horses and ponies in order to determine the ability of this chemical to provide a model of equine pulmonary disease. Both routes produced a severe and sometimes fatal pulmonary disease, characterised by bronchiolitis. Clinical signs developed 48 to 72 h after dosing and were most severe between Days 4 and 10 post dosing. Intravenous administration of 3-methylindole produced lung injury more rapidly and at a lower dose rate than the oral route. It is suggested that the respiratory condition induced by this chemical could become a metho...
Löscher W, Jaeschke G, Keller H.The pharmacokinetics of ascorbic acid were studied in 29 horses after intravenous (iv), subcutaneous, intramuscular (im) and oral administration. Following iv injection of 5 and 10 g ascorbic acid, respectively, a biphasic decline of ascorbic acid serum levels was found, indicating that the vitamin distributes in the body according to a two-compartment open model. The apparent volume of distribution (average value for Vd(ss) = 0.6 litre/kg) was approximately equivalent to the volume of total body water. The terminal half-life of the biexponential serum level-time curve (t1/2 beta) varied betwe...
Klei TR, Torbert BJ, Chapman MR, Turk MA.A controlled test method was used to evaluate the efficacy of injectable micelle and oral paste formulations of ivermectin (22,23-dihydroavermectin B1) against 8-week-old Strongylus vulgaris larvae in experimentally infected pony foals. The dosage level of the drug in both formulations tested was 0.2 mg/kg. Ponies were euthanatized and necropsied 5 weeks after treatment. Based on the recovery of live vs dead S vulgaris from mesenteric arteries, both formulations were greater than 99% effective. Increased weight gains and marked reductions in the severity of arterial lesions were observed in tr...
Merritt AM, Duelly P.The phloroglucinol microassay technique for measuring plasma concentrations of xylose was compared with the more tedious orcinolferric chloride technique. Sequential blood samples were collected from 5 dogs and 6 horses every 30 minutes after oral administration of 0.5 g of D-xylose/kg of body weight. Comparison of the results by regression analysis shows a highly significant (P less than 0.01) positive linear correlation for both dogs (r = 0.95) and horses (r = 0.77). These results indicate that xylose in canine and equine plasma can be accurately measured by the phloroglucinol technique.
Soma LR, Gallis DE, Davis WL, Cochran TA, Woodward CB.Phenylbutazone (PBZ) was administered (8.8 mg/kg of body weight) every 24 hours for 5 consecutive days, orally for the first 4 days and IV on day 5. The half-life (t 1/2) after this daily administration was 6.2 hours and the volume of distribution was 0.152 +/- 0.014 L/kg; the bioavailability after oral administration was 91.8 +/- 2.5%. The plasma concentration of PBZ at experimental hour (EH) 24 (24 hours after the 1st oral dose) was 1.7 +/- 0.39 micrograms/ml and increased to 4.2 +/- 0.29 micrograms/ml at EH 48 (24 hours after the 2nd oral dose). Values at EH 72, 96, and 120 (24 hours after ...
Arana Valencia N, Thompson DL, Southerland CV.Four experiments assessed factors affecting prolactin responses to sulpiride administration in horses. Experiment 1 compared the efficacy of the (-) enantiomer of sulpiride to that of the commonly used (+/-) racemic mixture. Mares were used in an 8 × 8 Latin square to compare the prolactin responses to four doses of levosulpiride to four corresponding doses of the racemic mixture at twice the dose. Responses at each dose indicated equal and similar (P > .1) responses. Experiment 2 compared the efficacy of 1 gram of orally administered racemic sulpiride to 100 mg of intramuscularly injec...
Villa R, Cagnardi P, Belloli C, Zonca A, Zizzadoro C, Ferro E, Carli S.The selective COX-2-inhibitor nimesulide is used extra-label in equine veterinary practice as an anti-inflammatory agent. However, there are no data on which to base the rational use of the drug in this species. Objective: To determine the effective COX selectivity of nimesulide in the horse, and suggest a suitable dosing schedule. Methods: The pharmacokinetics of nimesulide in the horse after oral administration (1 mg/kg bwt), and oral and i.v. administration (1.5 mg/kg bwt) were investigated, effects of feeding status on bioavailability determined, and plasma protein binding of the drug and ...
Seibert BP, Newcomb KM, Michael BF.Critical tests were done on 24 naturally parasitized horses to compare the antiparasitic activity of an oral paste preparation of mebendazole and trichlorfon with that of the marketed powder formulation. Each formulation was administered at the recommended dosages of 8.8 mg of mebendazole and 40 mg of trichlorfon/kg of body weight. Efficacy of the paste formulation ranged from 97.7% to 100% against 2nd- and 3rd-stage Gasterophilus spp, adult Strongylus vulgaris, S edentatus, Parascaris equorum, small strongyles; and larval and adult forms of Oxyuris equi. Adverse effects were generally limited...
Kranenburg LC, Westermann CM, de Sain-van der Velden MG, de Graaf-Roelfsema E, Buyse J, Janssens GP, van den Broek J, van der Kolk JH.Insulin resistance in horses is an emerging field of interest as it is thought to be a contributing factor in the pathogenesis of many equine conditions. Objective: The objectives of the present study were to determine the effects of long-term oral administration of L-carnitine on insulin sensitivity, glucose disposal, plasma leptin concentrations and acylcarnitine spectrum both in plasma and urine. Methods: Six 3-year-old healthy warmblood geldings were used. In a double blind 2 × 2 Latin square design at a dosage of 100 mg/kg body weight (BW)/day for 28 days the effects of oral supplementat...
Knych HK, Stanley SD, Arthur RM, McKemie DS.Cetirizine is an antihistamine used in performance horses for the treatment of hypersensitivity reactions and as such a withdrawal time is necessary prior to competition. The objective of the current study was to describe the disposition and elimination of cetirizine following oral administration in order to provide additional serum concentration data upon which appropriate regulatory recommendations can be established. Nine exercised thoroughbred horses were administered 0.4 mg/kg of cetirizine orally BID for a total of five doses. Blood samples were collected immediately prior to drug admin...
Wallace GE, McKaba VF, Reinhart JM, Li Z, Austin S, Fries RC.Large vessel and microvascular thrombi are common complications in systemically ill horses contributing to patient morbidity and mortality. Apixaban, an oral factor Xa inhibitor, shows excellent efficacy against stroke and deep vein thrombosis in humans. The purpose of this study was to determine serum apixaban concentrations and anti-factor Xa activity in horses after orally administered apixaban. Five horses received a single dose of intravenous (0.09 mg/kg) and oral (1 mg/kg) apixaban in a cross-over design. Serum apixaban concentrations and anti-Xa activity were measured serially via liq...
Bousquet-Melou A, Bernard S, Schneider M, Toutain PL.Marbofloxacin is a fluoroquinolone antibiotic expected to be effective in the treatment of infections involving gram-negative and some gram-positive bacteria in horses. In order to design a rational dosage regimen for the substance in horses, the pharmacokinetic properties of marbofloxacin were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the termi...
Goetz TE, Ogilvie GK, Keegan KG, Johnson PJ.Cimetidine, an H2 histamine antagonist, was used in the clinical management of progressive, multifocal melanomatosis in 3 adult gray horses. Prior to treatment, the tumors had increased rapidly in size and number in 2 horses (duration of 6 and 27 months, respectively) and slowly in the third horse (duration of 48 months). All 3 horses were treated with cimetidine (2.5 mg/kg of body weight, PO, q 8 h) for 2 months to 1 year. During treatment, the number and size of the melanomas decreased substantially (50 to 90%). The progression of the disease was halted in 2 horses and controlled in the thir...
Pyörälä S, Kotilainen T, Silvennoinen P, Hänninen U, Mero M, Kaartinen L.Serum tinidazole concentrations were monitored in five clinically healthy adult horses after intravenous (i.v.) and oral administration of the drug (15 mg/kg and 25 mg/kg, respectively). After i.v. administration, the mean residence time was 7.0 h, the elimination half-life 5.2 h and the body clearance rate 1.6 ml/min/kg. The distribution volume was found to be 660 ml/kg. After oral administration, the mean residence time was 8.5 h, the absorption half-life 1.1 h and the bioavailability essentially 100%. In view of the in-vitro sensitivities of various anaerobic bacteria, a dosage of 10-15 mg/...
Witte TS, Melkus E, Walter I, Senge B, Schwab S, Aurich C, Heuwieser W.Persistent breeding-induced endometritis is ranked as the third most common medical problem in the adult mare and leads to enormous economic loss in horse breeding. In mares suffering from persistent breeding-induced endometritis, increased amounts of intrauterine (i.u.) fluid or viscous mucus in estrus or after breeding may act as a barrier for sperm and can contribute to low fertility. Current therapies of these mares aim to eliminate i.u. fluid and mucus by uterine lavage and/or administration of ecbolic drugs. Recently, i.u. administration of N-acetylcysteine (NAC) has been shown to suppor...
Recchi L, Alvariza S, Benech A, Ruiz N, José Estradé M, Suarez G, Crosignani N.The purpose of this study was to evaluate the pharmacokinetics of oral amitriptyline in horses. Oral amitriptyline (1 mg/kg) was administered to six horses. Blood samples were collected from jugular and lateral thoracic vein at predetermined times from 0 to 24 hr after administration. Plasma concentrations were determined by high-performance liquid chromatography and analyzed using noncompartmental methods. Pharmacodynamic parameters including heart rate, respiration rate, and intestinal motility were evaluated, and electrocardiographic examinations were performed in all subjects. The mean m...
Paradis MR, Breeze RG, Laegreid WW, Bayly WM, Counts DF.Eight ponies were allotted to 2 groups of 4. Group-1 ponies (1-4) were given 0.2 g of indole/kg of body weight orally and group-2 ponies (5 to 8) were given 0.1 g of indole/kg. Various physical, hematologic, and physiologic measurements were obtained after administration of indole. Intravascular hemolysis and hemoglobinuria were detected in both groups within 24 hours of dosing. Hemolysis was reflected by decreases in PCV, hemoglobin concentration, and RBC count, and an increase in indirect bilirubin. Erythrocyte fragility appeared to increase in both groups at 8 hours after dosing and peaked ...
Hoffmann SL, Seminoff K, McKemie DS, Kass PH, Knych HK.Grapiprant is a prostaglandin E2 receptor antagonist that has been found to be an effective anti-inflammatory in dogs and that is devoid of some of the adverse effects associated with traditional NSAIDs that elicit their effects through inhibition of PGE2 production. Previously published reports have described the pharmacokinetics of this drug in horses when administered at 2 mg/kg; however, pharmacodynamic effects in this species have yet to be described. The objective of the current study was to describe the pharmacokinetics and pharmacodynamics of grapiprant at a higher dose. Eight horses...
Roncada P, Tomasi L, Montesissa C, Grossi G, Stracciari GL, Anfossi P.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...
Vander Werf KA, Davis EG, Kukanich B.The objective of this study was to assess the pharmacokinetic profile and determine whether any adverse effects would occur in seven healthy adult horses following oral meloxicam tablet administration once daily for 14 days at a dose of 0.6 mg/kg·bwt. Horses were evaluated for health using physical examination, complete blood count, serum chemistry, urinalysis, and gastroscopy at the beginning and end of the study. Blood was collected for the quantification of meloxicam concentrations with liquid chromatography and mass spectrometry. The mean terminal half-life was 4.99 ± 1.11 h. There was n...
Van Duijkeren E, Vulto AG, Van Miert AS.The indications for use, side-effects, and pharmacokinetic parameters of trimethoprim, sulfonamides and their combinations in the horse are reviewed. Trimethoprim/sulfonamide (TMPS) combinations are used for the treatment of various diseases caused by gram-positive and gram-negative bacteria, including infections of the respiratory tract, urogenital tract, alimentary tract, skin joints and wounds. TMPS combinations can be administered orally, since absorption from the gastrointestinal tract is relatively good. However, peak serum concentrations can vary significantly between individual horses....
Soma LR, Behrend E, Rudy J, Sweeney RW.The disposition of flunixin meglumine administered IV at a dosage of 1.1 mg/kg was described by a 2-compartment model; the alpha and beta half-lives (t1/2) were 0.61 and 1.5 hours, respectively. When administered IV at a rate of 2.2 mg/kg, the disposition was best described by a 3-compartment model, and the alpha, beta, and lambda t1/2 were 0.16, 1.52, and 6.00 hours, respectively. The zero-time plasma concentrations after flunixin meglumine was administered at 1.1 and 2.2 mg/kg were 9.3 +/- 0.76 and 21.5 +/- 7.4 mg/L, respectively. The bioavailability after oral administration of 1.1 mg/kg wa...
MacAllister CG, Sangiah S, Mauromoustakos A.Using video gastroscopy, the efficacy of a Histamine-H2 type receptor antagonist (WY 45, 727) was investigated in young ponies with spontaneous and experimentally induced gastric ulcers. Oral administration of WY 45, 727 at 2 mg/kg and 10 mg/kg of body weight every 12 hours for 14 days resulted in complete healing of spontaneous gastric ulcers in the non-glandular portion of the stomach in 2/5 (40%) and 3/4 (75%) of the ponies, respectively, compared (P < 0.05) to 0/5 (0%) placebo-treated ponies. After intramuscular administration of flunixin meglumine at 1.5 mg/kg body weight every 8 hours fo...
Yamarik TA, Wilson WD, Wiebe VJ, Pusterla N, Edman J, Papich MG.Using a randomized, cross-over study design, ciprofloxacin was administered i.g. to eight adult mares at a dose of 20 mg/kg, and to seven of the eight horses at a dose of 5 mg/kg by bolus i.v. injection. The mean C(0) was 20.5 μg/mL (±8.8) immediately after i.v. administration. The C(max) was 0.6 μg/mL (±0.36) at T(max) 1.46 (±0.66) h after the administration of oral ciprofloxacin. The mean elimination half-life after i.v. administration was 5.8 (±1.6) h, and after oral administration the terminal half-life was 3.6 (±1.7) h. The overall mean systemic availability of ...
Doucet MY, Vrins AA, Dionne R, Alva R, Ericsson G.The efficacy of a paste formulation of the H+, K+, -ATPase inhibitor omeprazole was evaluated in standardbred racehorses for the treatment and prevention of gastric ulcers. Twenty standardbred racehorses in training, aged 2 to 9 years, were enrolled from 2 training centres in this field trial. Endoscopic examinations confirmed the presence of gastric ulcers in all horses, prior to allocation and treatment and on day 0. Lesions were scored on a scale of 0 to 3 (intact epithelium to extensive ulceration). Replicates were formed, based on training level and location. Within replicates, 1 horse wa...
Gokbulut C, Ozuicli M, Aksit D, Aksoz E, Korkut O, Yalcinkaya M, Cirak VY.The horse milk gains increasing interest as a food product for sensitive consumers, such as children with food allergies or elderly people. We investigated the plasma and milk disposition, faecal excretion and efficacy of per os ivermectin (IVM) and pour-on eprinomectin (EPM) in horses. Ten mares were divided into two groups. The equine paste formulation of IVM and bovine pour-on formulation of EPM were administered orally and topically at dosage of 0.2 and 0.5 mg/kg bodyweight. Blood, milk and faecal samples were analysed using high-performance liquid chromatography. The plasma concentration...
Ewing PJ, Burrows G, MacAllister C, Clarke C.The pharmacokinetic properties of four erythromycin formulations were compared in six adult horses after administration of single and multiple oral doses. Formulations of erythromycin administered were estolate and phosphate given 37.5 mg/kg every 12 h and 25 mg/kg every 8 h, and stearate and ethylsuccinate given 25 mg/kg every 8 h. Areas under the curve (AUC) and maximum plasma erythromycin concentrations (Cmax) were equal or greater (P > or = 0.05) following administration of erythromycin phosphate and stearate compared with those values following administration of erythromycin estolate or e...
Eby G.Arthritis is inflammation in a joint often with joint damage, usually accompanied by pain, swelling and stiffness, resulting from infection, trauma, degenerative changes, metabolic disturbances, autoimmune or other causes. It occurs in various forms, including rheumatoid arthritis, osteoarthritis, bacterial arthritis and gout. Gallium III can inhibit the production of inflammatory cytokines, such as IL-1beta, produced by macrophage-like cells in vitro. A dose-dependent inhibition of IL-1beta and TPA stimulated MMP activity by gallium nitrate at increasing concentrations occurs, demonstrating t...
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, 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...
Andrews FM, Doherty TJ, Blackford JT, Nadeau JA, Saxton AM.To determine the effects of orally administered omeprazole, as enteric-coated capsules, on baseline and stimulated gastric acid secretion in horses. Methods: 5 healthy 8-year-old mixed-breed horses fitted with gastric cannulas. Methods: Enteric-coated granules of omeprazole were mixed with corn syrup and administered orally once daily for 5 consecutive days. On days 1 and 5 beginning 5 hours after omeprazole administration, 4 gastric fluid samples were collected, each for 15 minutes, via the gastric cannula (baseline samples). Pentagastrin was administered IV as a constant infusion for the sub...
Holbrook TC, Simmons RD, Payton ME, MacAllister CG.Electrolyte supplementation is common in horses during endurance competitions, but the effect on the gastric mucosa is unknown. Objective: Repeated oral administration of hypertonic electrolyte solution is associated with exacerbation of gastric ulcers in mature horses. Methods: The study design was a randomised, blinded, crossover trial. Fourteen horses were divided randomly into equal groups and administered either 60 ml water (placebo) or 56.7 g commercial electrolyte supplement mixed with 60 ml water by dose syringe orally once an hour for 8 h. The minimum concentration of individual const...
