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.
McKinney AR, Suann CJ, Stenhouse AM.A method has been developed for the detection of modafinil and its major metabolite, modafinil acid, in equine urine by solid-phase extraction and positive ion electrospray ionisation liquid chromatography/mass spectrometry. The method has been applied to the analysis of equine urine samples obtained after the oral administration of modafinil. Modafinil acid was the major component in the urine, and was detected up to 4 days post-administration. Unchanged modafinil was present at substantially lower concentrations, and was detected for only 24 hours.
Vervuert I, Coenen M, Watermülder E.This study was conducted to evaluate the effects of oral tryptophan (Trp) supplementation on exercise capacity and metabolic responses in horses. Three horses had to perform an exercise test: a 15-min warm-up followed by a 60-min walk (1.7 m/s, W1), a 10-min trot (3.1 m/s, T1), a second 60-min walk (1.7 m/s, W2), a second 10-min trot (3.1 m/s, T2) and a final 30-min walk (1.7 m/s, W3) until the horses were unwilling to continue. The horses exercised on a treadmill at a 6% incline and with a constant draught load of 40 kg (0.44 kN). Two hours before exercise horses were given 50 g Trp (9.8-10.7...
Jongbloets AM, Sloet van Oldruitenborgh-Oosterbaan MM, Meeus PJ, Back W.Equine canker is a chronic, hyperplastic, exudative pododermatitis affecting one or more feet. Although many causes and treatments have been suggested, the cause of the disease is still unknown and most probably multifactorial. Local treatments include radical surgical debridement of the diseased hoof tissue and application of caustic substances, antibiotics, and pressure bandaging. Nevertheless, the number of recurrences is high (45%). This article presents a 3-year-old New Forest pony-cross mare in which all horny structures (frogs, coronets, spurs, chestnuts) of all feet were affected. Bact...
Carrillo NA, Giguère S, Gronwall RR, Brown MP, Merritt KA, O'Kelley JJ.To determine the disposition of orally administered cefpodoxime proxetil in foals and adult horses and measure the minimum inhibitory concentrations (MICs) of the drug against common bacterial pathogens of horses. Methods: 6 healthy adult horses and 6 healthy foals at 7 to 14 days of age and again at 3 to 4 months of age. Methods: A single dose of cefpodoxime proxetil oral suspension was administered (10 mg/kg) to each horse by use of a nasogastric tube. In 7- to 14-day-old foals, 5 additional doses were administered intragastrically at 12-hour intervals. The MIC of cefpodoxime for each of 173...
Hodgson D, Howe S, Jeffcott L, Reid S, Mellor D, Higgins A.Oral administration of altrenogest for oestrus suppression in competition horses is believed to be widespread in some equestrian disciplines, and can be administered continuously for several months during a competition season. To examine whether altrenogest has any anabolic or other potential performance enhancing properties that may give a horse an unfair advantage, we examined the effect of oral altrenogest (0.044 mg/kg), given daily for a period of eight weeks, on social hierarchy, activity budget, body-mass and body condition score of 12 sedentary mares. We concluded that prolonged oral ad...
Laverty S, Sandy JD, Celeste C, Vachon P, Marier JF, Plaas AH.To examine the concentration of glucosamine in the synovial fluid and its pharmacokinetics in serum in a large animal model following dosing with glucosamine HCl at clinically relevant levels. Methods: Eight adult female horses were studied. After an overnight fast, glucosamine HCl (20 mg/kg of body weight) was administered by either nasogastric (NG) intubation or intravenous (IV) injection. Blood samples were collected before dosing and at 5, 15, 30, 60, 120, 180, 240, 360, 480, and 720 minutes after dosing. Synovial fluid samples were collected from the radiocarpal joints 48 hours before dos...
Lees P, Landoni MF, Giraudel J, Toutain PL.This review summarises selected aspects of the pharmacokinetics (PK) and pharmacodynamics (PD) of nonsteroidal anti-inflammatory drugs (NSAIDs). It is not intended to be comprehensive, in that it covers neither minor species nor several important aspects of NSAID PD. The limited objective of the review is to summarise those aspects of NSAID PK and PD, which are important to an understanding of PK-PD integration and PK-PD modelling (the subject of the next review in this issue). The general features of NSAID PK are: usually good bioavailability from oral, intramuscular and subcutaneous administ...
Toutain PL, Reymond N, Laroute V, Garcia P, Popot MA, Bonnaire Y, Hirsch A, Narbe R.To determine pharmacokinetic parameters for meloxicam, a nonsteroidal anti-inflammatory drug, in horses. Methods: 8 healthy horses. Methods: In the first phase of the study, horses were administered meloxicam once in accordance with a 2 x 2 crossover design (IV or PO drug administration; horses fed or not fed). The second phase used a multiple-dose regimen (daily oral administration of meloxicam for 14 days), with meloxicam administered at the recommended dosage (0.6 mg/kg). Plasma and urine concentrations of meloxicam were measured by use of validated methods with a limit of quantification of...
Johansson AM, Gardner SY, Levine JF, Papich MG, Lafevers DH, Goldman RB, Sheets MK, Atkins CE.Furosemide is the most common diuretic drug used in horses. Furosemide is routinely administered as IV or IM bolus doses 3-4 times a day. Administration PO is often suggested as an alternative, even though documentation of absorption and efficacy in horses is lacking. This study was carried out in a randomized, crossover design and compared 8-hour urine volume among control horses that received placebo, horses that received furosemide at 1 mg/kg PO, and horses that received furosemide at 1 mg/kg IV. Blood samples for analysis of plasma furosemide concentrations, PCV, and total solids were obta...
Rothschild CM, Sellon DC, Bryan GM, Gay JM, Hines MT.The objectives of this study were to observe the effects of trimethoprim-sulfadiazine on equine tear production and to determine normal fluctuations in Schirmer tear test (STT) values in horses. A randomized, placebo-controlled, blinded clinical trial measuring STT values in 15 horses over an 8-week period was performed. The treatment group (eight horses) received 30 mg/kg trimethoprim-sulfadiazine orally once a day and the control group (seven horses) received placebo (flour) at the same time. All horses were housed outdoors throughout the study. Schirmer tear test values were measured at 0, ...
Laan TT, Westermann CM, Dijkstra AV, van Nieuwstadt RA, Fink-Gremmels J.Healthy horses received aerosolised, intranasal or oral doses of 3 mg of fluticasone propionate evenly divided over morning and evening treatments for seven days. The bioavailability of the drug was determined in terms of the suppression of the endogenous cortisol concentrations in the horses during the period of treatment. The horses which received the aerosolised drug had significantly lower concentrations of endogenous cortisol on days 5 and 8 than the horses which received aerosolised placebo. The horses which received nasal and oral doses of fluticasone propionate showed no significant ch...
Epstein K, Cohen N, Boothe D, Nieuwoudt C, Chandler J.In many cases of equine infectious disease, long-term administration of antimicrobial drugs is required. Oral agents are preferred because of the relative ease of administration compared with other routes. Enrofloxacin has been shown to be effective against a variety of equine pathogens, but oral administration of this drug has proved difficult in horses. An oral gel formulation made from the injectable cattle product produces blood levels sufficient to resolve infections caused by a variety of common equine pathogens.
McKinney AR, Suann CJ, Stenhouse AM.An investigation has been conducted into the metabolism and urinary excretion of orally administered piroxicam and tenoxicam in the horse. The major component detected in urine after the administration of piroxicam was 5'-hydroxypiroxicam, which was detectable up to 24 h post-administration. Unchanged piroxicam was present only as a minor component. In contrast, unchanged tenoxicam was the major component observed after the administration of tenoxicam, being detectable for 72 h post-administration, while 5'-hydroxytenoxicam was a minor component. Phase II beta-glucuronide conjugation in each c...
Sanchez LC, Murray MJ, Merritt AM.To evaluate the efficacy of omeprazole paste, a commonly used antiulcer drug, on intragastric pH in clinically normal neonatal foals. Methods: 6 clinically normal foals between 5 and 14 days of age. Methods: Intragastric pH was recorded in each foal by use of a disposable antimony pH electrode with internal reference. Values for intragastric pH were recorded every 4 seconds by use of an ambulatory pH monitor. There were two 24-hour recordings of intragastric pH for each foal, with 24 hours between recordings. Foals were not administered any drugs during the first recording. Foals were administ...
Moore I, Horney B, Day K, Lofstedt J, Cribb AE.The effect of oral treatment with natural or recombinant human interferon alpha (HIA) on inflammatory airway disease in young standardbreds was assessed in a double-blind, randomized clinical trial. A total of 34 horses with nasal discharge, excess mucus in the trachea, and a persistent cough of at least 2 weeks' duration that interfered with training completed the trial. Horses were rested for 1 week and received oral treatment with either a saline placebo, recombinant human interferon alpha (rHIA; 90 U/horse/day), or natural human interferon alpha (nHIA: 50 U/horse/day) for 5 days. There was...
Cornelisse CJ, Robinson NE, Berney CE, Kobe CA, Boruta DT, Derksen FJ.Although the efficacy of dexamethasone for the treatment of recurrent airway obstruction (RAO) has been documented, the speed of onset of effect and duration of action are unknown, as is the efficacy of orally administered dexamethasone with or without fasting. Objective: To document the time of onset of effect and duration of action of a dexamethasone solution i.v. or orally with and without fasting. Methods: Protocol 1 used 8 RAO-affected horses with airway obstruction in a crossover design experiment that compared the effect of i.v. saline and dexamethasone (0.1 mg/kg bwt) on pulmonary func...
Stradaioli G, Sylla L, Zelli R, Chiodi P, Monaci M.The effect of orally administered l-carnitine on the quality of semen obtained from stallions with different semen qualities was investigated. Four stallions with proven fertility (high motility group, HM) and with normal seminal characteristics (>50% progressive motility and > 80 x 10(6) spermatozoa/ml), and four questionable breeders (low motility group, LM) with <50% of sperm progressive motility and < 80 x 10(6) spermatozoa/ml, received p.o. 20 g of l-carnitine for 60 days. Blood and semen samples were collected before treatment (T0) and after 30 (T1) and 60 days (T2). Semen ev...
Dunnett M, Richardson DW, Lees P.Hair analysis to detect drug administration has not been studied extensively in horses. This study aimed to (a) develop an analytical method for enrofloxacin and its metabolite ciprofloxacin in mane and tail hair, (b) relate measured values to doses, routes of administration, hair colour, and (c) demonstrate long-term detectability. Samples were extracted in trifluoroacetic acid at 70 degrees C. Extracts were cleaned-up by solid-phase extraction and analysed by high-performance liquid chromatography with UV-diode array detection. Analyte recoveries were > 87%. Horses were sampled after therape...
Rothschild CM, Hines MT, Breuhaus B, Gay J, Sellon DC.Trimethoprim-sulfadiazine was administered to horses in a randomized, placebo controlled study to determine the effects of potentiated sulfonamides on thyroid function in normal horses. The treatment group included eight horses that received trimethoprim-sulfadiazine mixed with molasses orally at 30 mg/kg once daily for eight weeks. The control group included 8 horses that received an oral placebo (flour mixed with molasses) once daily for the same period. Thyroid function was evaluated prior to initiation of treatment and after 8 weeks of treatment. Serum concentrations of total and free trii...
Pellegrini-Masini A, Poppenga RH, Sweeney RW.An injectable preparation of flunixin meglumine was administered orally and intravenously at a dose of 1.1 mg/kg to six healthy adult horses in a cross-over design. Flunixin meglumine was detected in plasma within 15 min of administration and peak plasma concentrations were observed 45-60 min after oral administration. Mean bioavailability of the oral drug was 71.9 +/- 26.0%, with an absorption half-life of 0.76 h. The apparent elimination half-life after oral administration was 2.4 h. The injectable preparation of flunixin meglumine is suitable for oral administration to horses.
Lopes MA, White NA, Donaldson L, Crisman MV, Ward DL.To assess changes in systemic hydration, concentrations of electrolytes in plasma, hydration of colonic contents and feces, and gastrointestinal transit in horses treated with IV fluid therapy or enteral administration of magnesium sulfate (MgSO4), sodium sulfate (NaSO4), water, or a balanced electrolyte solution. Methods: 7 horses with fistulas in the right dorsal colon (RDC). Methods: In a crossover design, horses alternately received 1 of 6 treatments: no treatment (control); IV fluid therapy with lactated Ringer's solution; or enteral administration of MgSO4, Na2SO4, water, or a balanced e...
Grubbs ST, Amodie D, Rulli D, Wulster-Radcliffe M, Reinemeyer C, Yazwinski T, Tucker C, Hutchens D, Smith L, Patterson D.The safety and efficacy of 2% moxidectin/12.5% praziquantel oral gel administered at a rate of 0.4 mg moxidectin and 2.5 mg praziquantel/kg was studied in client-owned horses under field use conditions. Four hundred horses (300 treated with moxidectin/praziquantel oral gel and 100 treated with vehicle) were enrolled, feces were collected, and eggs were counted. Investigators as well as horse owners were masked to treatment assignment. No adverse reactions to treatment were observed in any horses. Moxidectin/praziquantel gel reduced Anoplocephala spp by more than 99% and provided a significant ...
Rehbein S, Holste JE, Doucet MY, Fenger C, Paul AJ, Reinemeyer CR, Smith LL, Yoon S, Marley SE.The efficacy of an oral formulation of ivermectin plus praziquantel in the reduction of nematode and cestode egg counts in horses was assessed in 273 horses under field conditions at 15 sites in North America (n = 6) and Europe (n = 9). Horses were confirmed by fecal examination to have natural infections of strongyles (100%) and tapeworms (76%). Replicates of four horses were formed at each site, and in each replicate three animals received ivermectin (0.2 mg/kg body weight) plus praziquantel (1 mg/kg body weight) oral paste and one animal remained untreated or received vehicle paste. Fecal s...
Dirikolu L, Lehner AF, Karpiesiuk W, Hughes C, Woods WE, Boyles J, Harkins JD, Troppmann A, Tobin T.Selegiline ([R]-[-]N,alpha-dimethyl-N-2- propynylphenethylamine or l-deprenyl), an irreversible inhibitor of monoamine oxidase, is a classic antidyskinetic and antiparkinsonian agent widely used in human medicine both as monotherapy and as an adjunct to levodopa therapy. Selegiline is classified by the Association of Racing Commissioners International (ARCI) as a class 2 agent, and is considered to have high abuse potential in racing horses. A highly sensitive LC/MS/MS quantitative analytical method has been developed for selegiline and its potential metabolites amphetamine and methamphetamine...
Soma LR, Uboh CE, Guan F, Luo Y, Teleis D, Runbo L, Birks EK, Tsang DS, Habecker P.Plasma and tissue concentrations of clenbuterol (CLB) were determined following oral (p.o.) administration of 1.6 microg/kg twice daily (b.i.d.) for 2 weeks. Horses were administered the last dose on morning of day 15, killed at 0.25, 24, 48, and 72 h post-administration. At 0.25 h, the highest tissue concentrations of CLB were found in the liver (16.21 ng/g), lung (6.48 ng/g), left ventricle (4.99 ng/g), kidney (3.35 ng/g), bronchi (2.56 ng/g), right ventricle (2.08 ng/g), and eye fluids (1.09 ng/g) all of which were higher than that of plasma (1.10 ng/mL). The elimination half-lives (t(1/2k)...
Soma LR, Uboh CE, Guan F, Moate P, Luo Y, Teleis D, Li R, Birks EK, Rudy JA, Tsang DS.The pharmacokinetics of clenbuterol (CLB) following a single intravenous (i.v.) and oral (p.o.) administration twice daily for 7 days were investigated in thoroughbred horses. The plasma concentrations of CLB following i.v. administration declined mono-exponentially with a median elimination half-life (t(1/2k)) of 9.2 h, area under the time-concentration curve (AUC) of 12.4 ng.h/mL, and a zero-time concentration of 1.04 ng/mL. Volume of distribution (V(d)) was 1616.0 mL/kg and plasma clearance (Cl) was 120.0 mL/h/kg. The terminal portion of the plasma curve following multiple p.o. administrati...
Du J, White N, Eddington ND.The purpose of this study was to determine if glucosamine (GL) hydrochloride (FCHG49) and low molecular weight (LMW) chondroitin sulfate (CS) (TRH122) are absorbed after oral administration to horses. The bioavailability of LMWCS was evaluated by quantifying the total disaccharides found in the plasma following chondroitinase ABC digestion. Methods: Two separate studies were conducted. In study 1, ten adult horses received the following four treatments in a randomized crossover fashion: (1) i.v. LMWCS (3 g of 8 kDa), (2) p.o. LMWCS (3 g of 8 kDa), (3) i.v. LMWCS (3 g of 16.9 kDa) and (4) p.o. ...
Gardner SY, Atkins CE, Sams RA, Schwabenton AB, Papich MG.The pharmacokinetics of enalapril (0.5 mg/kg i.v.) and the pharmacodynamics of enalapril (0.5 mg/kg PO) in 5 mares were investigated. After single i.v. dosing, concentrations of enalapril and enalaprilat, its active metabolite, were measured. Two weeks later, enalapril was administered by nasogastric tube. Potassium, creatinine, blood urea nitrogen (BUN), enalapril, and enalaprilat concentrations and angiotensin converting enzyme (ACE) activity were measured in serum. In addition, heart rate, blood pressure, digital venous blood gases, and lactate were measured. Two weeks later, enalapril was ...
McKenzie EC, Valberg SJ, Godden SM, Finno CJ, Murphy MJ.To determine the effect of oral administration of dantrolene sodium on serum creatine kinase (CK) activity after exercise in horses with recurrent exertional rhabdomyolysis (RER). Methods: 2 healthy horses and 5 Thoroughbreds with RER. Methods: 3 horses received 2 doses of dantrolene (4, 6, or 8 mg/kg, p.o., with and without withdrawal of food) 2 days apart; 90 minutes after dosing, plasma dantrolene concentration was measured spectrofluorometrically. On the basis of these results, 5 Thoroughbreds with RER from which food was withheld received dantrolene (4 mg/kg) or an inert treatment (water ...
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.
Norris JW, Watson JL, Tablin F, Kozikowski TA, Knych HK.To determine pharmacokinetics and pharmacodynamics after oral administration of a single dose of clopidogrel to horses. Methods: 6 healthy adult horses. Methods: Blood samples were collected before and at various times up to 24 hours after oral administration of clopidogrel (2 mg/kg). Reactivity of platelets from each blood sample was determined by optical aggregometry and phosphorylation of vasodilator-stimulated phosphoprotein (VASP). Concentrations of clopidogrel and the clopidogrel active metabolite derivative (CAMD) were measured in each blood sample by use of liquid chromatography-tandem...
Thomson P, Toro J, Lara F, Hernández D, Aros K, Valenzuela-Lopez N.We present the first case of rhinopharyngitis due to Aspergillus fumigatus in a purebred Chilean horse. Clinically, manifested mucopurulent discharge from both nostrils, inflammation of the nasal, ocular, and ear mucosa; associated with decay and hyporexia. Based on the clinical signs and analysis of the mycological and molecular transtracheal aspirate sample, the present case was diagnosed as Aspergillus fumigatus rhinopharyngitis. After the antifungal susceptibility test, oral itraconazole treatment was maintained for 45 days, showing no clinical sign.
Ziemer EL, Parker HR, Carlson GP, Smith BP.Two horses were admitted separately for evaluation and treatment of profound hyperchloremic metabolic acidosis without azotemia. One, an 11-year-old Quarter Horse mare, had been depressed and ataxic for 2 days. The other, a 2-year-old Quarter Horse colt, had a 6-week history of depression, anorexia, and weight loss. Both horses responded to fluid and electrolyte therapy, but required daily oral administration of sodium bicarbonate for maintenance. In each case, the diagnosis was renal tubular acidosis.
Gordon ME, McKeever KH.This study tested the hypothesis that grain and intravenous dextrose challenges would alter plasma concentrations of active ghrelin, adiponectin, leptin, glucose, insulin, and cortisol in Standardbred mares. To deliver 0.5 g of glucose (dextrose solution for the intravenous test)/kg of BW, mares received intravenous dextrose (50% solution) or oral grain administration in 2 trials. In response to the oral grain challenge, plasma glucose and insulin concentrations increased (P < 0.001) by 56 and 802%, respectively. Plasma ghrelin concentration initially decreased (P < 0.001) by 40%, then s...
Rose RJ, Kohnke JR, Baggot JD.Plasma phenylbutazone concentrations were determined for up to 12 h in 6 horses following intravenous and oral phenylbutazone administration. To evaluate the bioavailability of different oral preparations, phenylbutazone was administered in a paste as well as the traditional powder form. The effect of the state of stomach contents on the absorption of phenylbutazone was investigated by administering the paste before and after feeding; the powder was given in a small bran mash and a full feed of lucerne chaff, wheaten chaff and bran. Despite great variability among individual horses both the pa...
Olsén L, Bondesson U, Broström H, Tjälve H, Ingvast-Larsson C.The pharmacokinetics of the histamine H(1)-antagonist cetirizine and its effect on histamine-induced cutaneous wheal formation were studied in six healthy horses following repeated oral administration. After three consecutive administrations of cetirizine (0.2 mg/kg body weight, bw) every 12h, the trough plasma concentration of cetirizine was 16+/-4 ng/mL (mean+/-SD) and the wheal formation was inhibited by 45+/-23%. After four additional administrations of cetirizine (0.4 mg/kg bw) every 12 h, the trough plasma concentration was 48+/-15 ng/mL and the wheal formation was inhibited by 68+/-11%....
Sigel CW, Byars TD, Divers TJ, Murch O, DeAngelis D.Two fasted and 2 fed horses were dosed orally with a combined trimethoprim and sulfadiazine paste formulation at a dose of 35 mg (1:5 combined active ingredients)/kg. Serum concentrations of each drug were determined periodically for 3 consecutive days for the 4 horses. The extent and rate of absorption for trimethoprim were variable, but peak serum concentrations occurred generally within 3 hours; sulfadiazine absorption was slower, reaching peak concentrations by 6 hours. Fasting did not have a consistent effect on the serum concentration profiles for either drug. Both drugs achieved serum c...
Foster CV, Harris RC, Snow DH.1. L-carnitine was administered orally to thoroughbred horses for 58 days. 2. Acceptability and effects on plasma, muscle and urine concentration were studied. 3. Ten-60 g/day (as 2-3 doses) was acceptable with no deleterious effects. 4. One x 10 g L-carnitine significantly raised the plasma-free carnitine concentration (7 hr post) from 21.2 to 31.8 mumol/l; 2 x 30 g increased the mean to 36.5 mumol/l. 5. Plasma acetylcarnitine increased from approximately 1 to 5.5 mumol/l (7 hr post) on 2 x 30 g/day. 6. Muscle total carnitine was unchanged over 58 days. 7. Urinary output accounted for 3.5-7.5...
Clarke CR, Burrows GE, MacAllister CG, Spillers DK, Ewing P, Lauer AK.Single-dose pharmacokinetic variables of pyrimethamine were studied in horses. Pyrimethamine (1 mg/kg of body weight) was administered IV and orally to 6 adult horses, and plasma samples were obtained at frequent intervals thereafter. Plasma pyrimethamine concentration was assayed by gas chromatography, and concentration-time data were analyzed, using a pharmacokinetic computer program. The IV and oral administration data were best described by 3-compartment and 1-compartment models, respectively. The median volume of distribution at steady state after IV administration was 1,521 ml/kg and the...
Knych HK, Stanley SD, Arthur RM, McKemie DS.The use of anti-ulcer medications, such as cimetidine, ranitidine, and omeprazole, is common in performance horses. The use of these drugs is regulated in performance horses, and as such a withdrawal time is necessary prior to competition to avoid a medication violation. To the authors' knowledge, there are no reports in the literature describing repeated oral administrations of these drugs in the horse to determine a regulatory threshold and related withdrawal time recommendations. Therefore, the objective of the current study was to describe the disposition and elimination pharmacokinetics o...
Yi R, Zhao S, Lam G, Sandhu J, Loganathan D, Morrissey B.Cathinone is the principal psychostimulant present in the leaves of khat shrub, which are widely used in East Africa and the Arab peninsula as an amphetamine-like stimulant. Cathinone readily undergoes metabolism in vivo to form less potent cathine and norephedrine as the metabolites. However, the presence of cathine and norephedrine in biological fluids cannot be used as an indicator of cathinone administration. The metabolism of pseudoephedrine and ephedrine, commonly used in cold and allergy medications, also produces cathine and norephedrine, respectively, as the metabolites. Besides, cath...
Taylor EA, Beard WL, Douthit T, Pohlman L.Caecal acidosis is a central event in the metabolic cascade that occurs following grain overload. Buffering the caecal acidosis by enterally administered sodium bicarbonate (NaHCO3 ) may be beneficial to affected horses. Objective: To determine the effect and duration of enterally administered NaHCO3 on caecal pH in healthy horses. Methods: Experimental study using horses with caecal cannulas. Methods: Nine horses had been previously fitted with a caecal cannula. Six horses received 1.0 g/kg bwt NaHCO3 and 3 control horses were given 3 l of water via nasogastric tube. Clinical parameters, ...
Kollias-Baker C, Sams R.The objective of this study was to determine if the administration of poppy seeds to horses would result in detectable concentrations of morphine in urine and blood samples, as has been shown to occur in humans. In this study blood and urine samples were collected following administration of poppy seeds and morphine sulfate orally to four horses. Urine samples were subjected to enzyme-linked immunosorbent assay (ELISA) for the presence of morphine. All urine samples testing positive by ELISA, as well as plasma samples collected after administration of the 10-g doses of poppy seeds, were analyz...
Afonso T, Giguère S, Brown SA, Barton MH, Rapoport G, Barba M, Dembek KA, Toribio RE, Coleman AE.Despite the paucity of data available, orally administered angiotensin-converting enzyme (ACE) inhibitors are empirically used in horses with valvular regurgitation. Objective: Evaluate the echocardiographic and hormonal changes in response to oral benazepril in horses with left-sided valvular regurgitation. Methods: Prospective, randomised double-blind, placebo-controlled trial. Methods: Horses with mitral valve (MR) and/or aortic valve regurgitation (AR) received oral benazepril (n = 6) at a dosage of 1 mg/kg q 12 h or a placebo (n = 5) for 28 days. Echocardiography was performed before drug...
Toribio RE, Bain FT, Mrad DR, Messer NT, Sellers RS, Hinchcliff KW.Three weak, recumbent neonatal foals with skin lesions, including a thin wooly coat, were born to mares being treated for equine protozoal myeloencephalitis. Mares received sulfadiazine or sulfamethoxazole-trimethoprim, pyrimethamine, folic acid, and vitamin E orally. Foals were anemic, leukopenic, azotemic, hyponatremic, and hyperkalemic. Serum folate concentrations in the 3 foals and 2 mares were lower than those reported in the literature for clinically normal brood mares. Treatment was unsuccessful. For each foal, necropsy revealed lobulated kidneys with thin cortices and a pale medulla, a...
Karatt TK, Sathiq MA, Laya S, Kal AKK, Subhahar MB, Muhammed Ajeebsanu MP, Philip M, Caveney MR, Graiban FM.Nonsteroidal selective androgen receptor modulators (SARMs) are a novel class of compounds that have not yet been clinically approved; however, they appear to have a better anabolic/androgenic ratio than steroids and cause slighter side effects. Sports drug testing laboratories are required to maintain continuously updated doping control analytical methods in light of the widespread misuse of SARMs in elite and amateur sports. This paper describes the metabolic conversion of SARM GSK2881078 in thoroughbred horses following oral administration and in vitro with equine liver microsomes. A liquid...
Bertone AL, Jones RL, McIlwraith CW.The tarsocrural joints of 11 horses were inoculated with 1.2 to 2.16 x 10(6) viable Staphylococcus aureus organisms susceptible to a trimethoprim-sulfadiazine (TMP-SDZ) combination with minimal inhibitory concentration (MIC) of 0.25 micrograms of TMP/ml and 4.75 micrograms of SDZ/ml. Antimicrobial treatment consisted of oral administration of a TMP-SDZ combination--30 mg/kg of body weight given once daily (group-1 horses) or 60 mg/kg given as 30 mg/kg every 12 hours (group-2 horses). Paired serum and synovial fluid samples were obtained before intra-articular inoculation with the S aureus, aft...
Agne GF, Jung SW, Wooldridge AA, Duran SH, Ravis W, Toribio R.Diuretic treatment is the mainstay for management of congestive heart failure in horses, and its use has been restricted to injectable medications because no currently data supports the use of PO administered loop diuretics. Objective: To determine the pharmacokinetic and pharmacodynamic properties of PO administered torsemide and, determine if PO administered torsemide, could be used as an alternative to injectable diuretics in the horse. Methods: Six healthy adult mares. Methods: A 2-phase, prospective study, that consisted of pharmacokinetic profiling of a single dose (6 mg/kg PO) and pharm...
Waraksa E, Owczarek K, Kubica P, Kłodzińska E, Ozimek M, Wrzesień R, Bobrowska-Korczak B, Namieśnik J.Bromhexine (BH), expectorant used in the treatment of respiratory disorders associated with viscid or excessive mucus, is not permitted for use in the competing horse by many authorities in horseracing and Olympic disciplines. Metabolic studies are of the great importance in anti-doping field because they allow for updating the selection of the most appropriate markers for prohibited substances, such as metabolites present at higher concentration levels and/or lasted for a longer period of time in biological samples than a parent drug. This study describes LC-MS/MS-based method for simultaneou...
de Backer P, Vandecasteele-Thienpont LM, Jonckheere JA, Belpaire FM, Debackere M, de Leenheer AP.Bromhexine was administered orally (2 mg./kg.) and intravenously (i. v.) (1 mg./kg.) in 3 horses. Plasma levels were measured and the pharmacokinetic behaviour and bioavailability were estimated. The half-life of elimination after i. v. administration ranged from 3.1 to 4.4 hours. The mean values of the apparent volume of distribution and the volume of distribution of the central compartment amounted to 16.2 and 3.3 1./kg., respectively. A very high plasma clearance, ranging from 49.8 to 59 ml./kg./min., was found.
One hour after oral administration, a mean peak plasma level of about 14 ng....
McGuirk SM, Muir WW, Sams RA.A pharmacokinetic study was made, using 7 healthy adult horses (weighing between 400 and 560 kg) given quinidine gluconate IV and quinidine sulfate orally. The apparent volume of distribution of quinidine base was 3.10 +/- 0.79 L/kg, total body clearance was 5.49 +/- 2.40 ml/minute/kg, and plasma half-life was 6.65 +/- 3.00 hours. The systemic availability of quinidine sulfate after oral administration of a 10 mg/kg dose was 48.5 +/- 20.4%. Oral administrations of quinidine sulfate in doses of 10 mg/kg and 10 g produced peak plasma concentrations of 0.79 microgram/ml at 146 minutes and 1.47 mi...
Castro JR, Adair HS, Radecki SV, Kiefer VR, Elliot SB, Longhofer SL.To determine effects of domperidone and acepromazine maleate on microvascular blood flow in digital laminae of clinically normal adult horses. Methods: 8 clinically normal adult horses (4 mares and 4 geldings). Methods: In a 4-period crossover study, domperidone was administered PO at 1.1 mg/ kg and 5.5 mg/kg and IV at 0.2 mg/kg; acepromazine was administered IV at 0.04 mg/kg. The washout period between treatments was 1 week. A 3-minute measurement of laminar microvascular blood flow (LMBF) was obtained with laser Doppler flowmetry. Baseline measurements were obtained at -2, -1, and 0 hours pr...
Xue C, Davis J, Berghaus LJ, Hanafi A, Vaughn SA, Hart KA.Donkeys with clinical signs of pituitary pars intermedia dysfunction are treated with oral pergolide mesylate despite the lack of species-specific pharmacokinetic data. Objective: To evaluate the pharmacokinetics of intragastric and oral pergolide mesylate in healthy donkeys (Equus asinus). Methods: Pharmacokinetic study. Methods: Six healthy donkeys were administered pergolide mesylate (Prascend®) at 2 μg/kg bodyweight (bwt) intragastrically once, then once daily per os (PO) for 5 days. Blood samples were collected at 0, 10, 20, 30 and 45 min and 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 and ...
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...
Specht TE, Brown MP, Gronwall RR, Rib WJ, Houston AE.Serum concentrations of metronidazole were determined in 6 healthy adult mares after a single IV injection of metronidazole (15 mg/kg of body weight). The mean elimination rate (K) was 0.23 h-1, and the mean elimination half-life (t1/2) was 3.1 hours. The apparent volume of distribution at steady state was 0.69 L/kg, and the clearance was 168 ml/h/kg. Each mare was then given a loading dose (15 mg/kg) of metronidazole at time 0, followed by 4 maintenance doses (7.5 mg/kg, q 6 h) by nasogastric tube. Metronidazole concentrations were measured in serial samples of serum, synovia, peritoneal flui...
Reinemeyer CR, Scholl PJ, Andrews FM, Rock DW.A 3 m, video gastroscope was used to screen 47 horses suspected of being naturally infected with equine bot larvae. 17 of 47 (36.2%) candidate horses harbored Gasterophilus nasalis larvae in the proximal duodenum and 46 of 47 (97.9%) had G. intestinalis larvae in the stomach. All horses infected with G. nasalis had concurrent infections with G. intestinalis. 14 horses with dual infections were allocated randomly to two treatment groups. Seven horses in Group 1 received 2% moxidectin oral gel once at a dosage of 0.4 mg/kg bodyweight (BW), and seven horses in Group 2 were untreated controls. 14 ...
Camargo FC, Robinson NE, Berney C, Eberhart S, Baker S, Detolve P, Derksen FJ, Lehner AF, Hughes C, Tobin T.The bronchodilator effects of trimetoquinol (TMQ) have been studied when administered i.v. or intratracheally, but not in an aerosolised form. Objective: To define the relationship between the therapeutic and adverse responses (therapeutic index) of TMQ when administered as an aerosol or by the oral route. Methods: Increasing doses of TMQ were administered to horses with heaves as an aerosol and by the oral route. Dose ranged 100-1000 microg/horse for aerosolised TMQ and from 6-60 microg/kg bwt for the oral route. Airway and cardiac effects were assessed by measurement of maximal change in ple...
Gómez-Díez M, Muñoz A, Caballero JM, Riber C, Castejón F, Serrano-Rodríguez JM.Pharmacokinetic and pharmacodynamic of IV enalapril at 0.50 mg/kg, PO placebo and PO enalapril at three different doses (0.50, 1.00 and 2.00 mg/kg) were analyzed in 7 healthy horses. Serum concentrations of enalapril and enalaprilat were determined for pharmacokinetic analysis. Angiotensin-converting enzyme (ACE) activity, serum ureic nitrogen (SUN), creatinine and electrolytes were measured, and blood pressure was monitored for pharmacodynamic analysis. The elimination half-lives of enalapril and enalaprilat were 0.67 and 2.76 h respectively after IV enalapril. Enalapril concentrations ...
Vatistas NJ, Snyder JR, Nieto J, Thompson D, Pollmeier M, Holste J.Gastric ulceration has been found to occur in 80-90% of Thoroughbreds in active race training. Previously, variable success has been reported using mucosal surface protectants and H2 receptor antagonist. Omeprazole, a substituted benzimidazole, has been shown to inhibit gastric acid secretion in both man and animals. Fourteen horses, in active race training and with endoscopic evidence of moderated to severe gastric ulceration were divided into 2 groups: Group 1 (7 horses) were given placebo paste orally once daily for 28 days; Group 2 (7 horses) received 1.54 g active omeprazole in the placeb...
