Pharmaceuticals in equine medicine encompass a wide range of drugs and therapeutic agents used to treat various conditions in horses. These substances include analgesics, anti-inflammatories, antibiotics, sedatives, and anthelmintics, among others. Each class of pharmaceuticals is designed to address specific health issues, such as pain management, infection control, or parasitic infestations. The pharmacokinetics and pharmacodynamics of these drugs can vary significantly between horses and other species, necessitating careful consideration of dosage and administration methods. This page compiles peer-reviewed research studies and scholarly articles that explore the development, efficacy, safety, and regulatory aspects of pharmaceuticals used in equine healthcare.
Hood DM, Stephens KA, Bowen MJ.Phenoxybenzamine, an alpha adrenergic antagonist, was administered IV to 6 clinically normal horses, 5 horses with experimentally induced diarrhea, and 7 horses with naturally-occurring diarrhea. It was established that a total of 2 mg of phenoxybenzamine/kg of body weight given in divided doses resulted in alpha adrenergic blockage of approximately 72 hours' duration, tranquilization, and mild constipation in the normal horse. The 5 experimental cases of diarrhea were involved in a laminitis research protocol in which laminitis was induced by oral carbohydrate overload. In all 5 of those case...
Alexander F.Phenylbutazone administered in therapeutic doses to ponies decreased urinary sodium and chloride excretion. The volume and osmolality of the urine was unaffected as was potassium excretion. Faecal excretion of chloride decreased and that of potassium increased, while faecal sodium excretion was unaffected. Plasma pH, bicarbonate and total carbon dioxide decreased after phenylbutazone administration. Packed cell volume, plasma sodium, potassium, carbon dioxide tension and chloride were unchanged.
Houghton E, Dumasia MC, Wellby JK.Negative ion chemical ionization mass spectra of some corticosteroids have been obtained by direct syringe introduction on to the Finnigan moving belt high-performance liquid chromatography-mass spectrometer interface. Proprietary preparations based upon dexamethasone, betamethasone and prednisolone were administered to horses at therapeutic dose level. Urine samples were extracted, the extracts purified by Sephadex LH-20 chromatography and the presence of the parent steroids in the eluates was confirmed by combined high-performance liquid chromatography negative ion chemical ionization mass s...
Brown MP, Stover SM, Kelly RH, Farver TB.Six healthy adult mares were given a single dose of kanamycin sulfate (200 mg/ml) IM at a dosage rate of 5 mg/kg of body weight. Kanamycin concentrations in serum, synovial fluid, peritoneal fluid, and urine were measured serially over a 48-hour period. The mean peak serum kanamycin concentration was 12.55 microgram/ml at 1 hour. Mean peak kanamycin concentrations in synovial fluid and peritoneal fluid were 7.25 microgram/ml and 9.27 microgram/ml at 2 hours and 3 hours, respectively. These concentrations decreased steadily in parallel with serum concentrations and were still measurable at 48 h...
Nizolek DJ, White KK.Degenerative arthrosis is perhaps the most common debilitating disease of performance horses. Treatment should be based upon a knowledge of the anatomy and physiology of normal joints and upon an understanding of the processes of degeneration and repair. These topics are briefly reviewed. Although rest is probably, the most beneficial therapy, physical and pharmaceutical treatments are often employed in an effort to speed recovery. The effects and relative benefits of intrasynovial injections of corticosteroids, hyaluronica cid, and Arteparon are considered in detail. Although local corticoste...
Gingerich DA, Mia AS.Thirty adult horses were used to compare the toxicity and cholinesterase (ChE) inhibition of various dosages of a combination anthelmintic, trichlorfon + mebendazole. Single oral doses of up to 5 times the effective dosage (39.7 mg of trichlorfon and 8.8 mg of mebendazole/kg of body weight) did not result in deaths. Horses given a placebo and horses treated at the recommended dosage rate showed few or no side effects, whereas horses given higher dosages showed dosage-related increases in the severity of clinical signs of organophosphate toxicosis. Dosage-related inhibition of erythrocyte ChE a...
Pedersoli WM, Ravis WR, Belmonte AA, McCullers RM.Digoxin (elixir, 0.022 mg/kg) was administered via stomach tube to healthy horses of mixed breeding and sexes. Serum digoxin concentrations reached a peak (2.21 +/- 0.6 ng/ml) at approximately 1 hour after dosing and had a half-life of 28.8 +/- 10.7 hours. Digoxin kinetics followed a triexponential curve, indicating that at least a 2 compartmental model is required to characterize the serum concentration-time curve after this route of administration. It was calculated that to achieve average serum concentrations of 1.1 ng/ml, an oral dose of 17.4 microgram of digoxin elixir/kg/day and an IV do...
Dumasia MC, Houghton E.1. Isomers of 3,17-dihydroxyandrostan-16-one, 3,16-dihydroxyandrostan-17-one and androstane-3,16,17-triol have been identified as urinary metabolites of testosterone in the horse. 2. Following XAD-2 extraction of urine samples, Sephadex LH-20 chromatography was used to separate the extract into conjugate groups. Metabolites obtained after hydrolysis of the conjugates have been investigated by g.l.c.-mass spectrometry. 3. Testosterone, 3,17-dihydroxyandrostan-16-one and 3,16-dihydroxyandrostan-17-one were found only in the sulphate fraction. 5 alpha-Androstane-3 beta,17 beta-diol, and two isome...
Pecheur M.A number of good anthelmintic drugs are currently available which eliminate gastrointestinal nematodes of equids with over 90% success. This is shown by comparing results of critical tests conducted with 9 anthelmintic agents on ponies using the following dosages: 19 mg/kg for Pyrantel embonate, 10 mg/kg for Oxfendazole, 10 mg/kg for Mebendazole, 5 mg/kg for Albendazole, 40 mg/kg for Dichlorvos, 44 mg/kg for Thiabendazole, 7.5 mg/kg, for Fenbendazole, 20 mg/kg for Cambendazole and 7 mg/kg for Parbendazole. From 6 to 9 ponies were treated with each of these anthelmintic agents. Based on total a...
Dewey EA, Maylin GA, Ebel JG, Henion JD.Promazine hydrochloride and acetylpromazine maleate were administered intravenously at clinical dose levels to horses. In urine from horses given promazine hydrochloride, the parent drug and four metabolites were detected. The two major metabolites, present as conjugates were identified after hydrolysis by beta-glucuronidase/arylsulfatase as 3-hydroxypromazine and 3-hydroxydesmonomethyl-promazine. Conjugated 3-hydroxypromazine has been previously identified as a major metabolite in the horse. Two minor metabolites isolated in this study were primaizine N-oxide and promazine N-oxide sulfoxide. ...
Frincke JM, Henderson GL.Fentanyl, a potent, synthetic narcotic analgesic, has reportedly been used to "dope" racehorses. Urine was collected from a horse dosed with 70 mg of [3H]fentanyl, and the primary metabolite, a water-soluble, amphoteric compound, was isolated by high-pressure liquid chromatography and identified by spectroscopic analysis. This metabolite was found to be N-[1-(2-phenethyl-4-piperidinyl)] malonanilinic acid.
Jonckheere JA, Thienpont LM, De Leenheer AP, De Backer P, Debackere M, Belpaire FM.A method has been developed for quantification of bromhexine in plasma using gas chromatography mass spectrometry with selected ion monitoring. A deuterium labelled analogue was synthesized and used as the internal standard. To evaluate the gas chromatographic electron capture detection method described earlier, 23 plasma samples have been analysed by both techniques. Although a good correlation was shown, selected ion monitoring was superior to the electron capture detection method for levels below 3 ng ml-1. The mass spectrometric method has also been used to set up a pharmacokinetic study o...
Dodman NH.Drugs and drug combinations currently in use for chemical restraint of the horse are discussed with a view to establishing their likely usefulness to the practising veterinary surgeon. Acepromazine maleate and xylazine hydrochloride are considered to be the most useful tranquillisers in spite of their limitations. A xylazine-methadone sequence is described for more profound chemical restraint and the possible future role of ketamine and glyceryl guaiacolate in combination with other agents to produce recumbency is discussed.
Mirck MH.The use of trichlorfon as an anthelmintic in horses has increased since it was combined with mebendazole and febantel, and became commercially available as Telmin-trichlorfon and Rintal-plus respectively. Field studies showed that these combined preparations frequently gave rise to cases of poisoning. Mild to severe colic was observed up to six hours after treatment, diarrhoea and/or anorexia continuing to be present for one to six days after administration. The 'horse weight measurer' introduced by Janssen Pharmaceutica is not sufficiently accurate to prevent overdosage. It is advisable only ...
Yoxall AT.This paper is an introduction to a series of commissioned articles on therapeutic medicine to be published in Equine Veterinary Journal under differing authorship, during the next 2 years. It presents an account of fundamental concepts common to the use of all drugs and introduces some pharmacokinetic principles to which reference will be made in later articles.
Delbeke FT, Vynckier L, Debackere M.A high performance liquid chromatographic method is described to determine the anti-inflammatory drug suxibuzone (SXB) and its major metabolites phenylbutazone (PBZ) and oxyphenbutazone (OPBZ) in equine plasma and urine. When suxibuzone (6 mg/kg) was administered intravenously (i.v.) or orally (p.o.) no parent drug was detected in plasma or in urine. The disposition of the metabolite PBZ (i.v.) could be described by a 2 compartment model with a beta half-life varying from 7.40 to 8.35 h. Due to severe side effects the use of i.v. suxibuzone should not be encouraged in the horse. PBZ and OPBZ w...
Short CR, Sams RA, Soma LR, Tobin T.The primary reason for developing the ARCI Uniform Classification of Foreign Substances was to give stewards and other racing regulators guidelines to assist them in understanding the relative performance effects and general offensiveness to the Rules of Racing of various drugs and medications. As such, these guidelines have been very useful in the world of racing regulation--officially or unofficially--because this classification system, for the first time, places a relative number on the inappropriateness of any one of more than 750 agents appearing in forensic samples taken from racing hors...
Underwood C, Collins SN, Mills PC, Van Eps AW, Allavena RE, Medina Torres CE, Pollitt CC.Pharmaceutical agents with potential for laminitis prevention have been identified. Many of these, including the MMP inhibitor marimastat, are impractical for systemic administration. This study compared local delivery of marimastat by regional limb perfusion (RLP) to systemic intravenous bolus dosing (SIVB), and established whether RLP results in local lamellar drug delivery. Six adult horses received 0.23 mg/kg of marimastat by RLP followed by 0.23 mg/kg marimastat by SIVB, with a 24-h washout period. Lamellar ultrafiltration probes sampled lamellar interstitial fluid as lamellar ultrafiltra...
Philip M, Karakka Kal AK, Subhahar MB, Karatt TK, Mathew B, Koshy SA.It is important to remember that performance-enhancing agents such as non-peptide growth hormone secretagogues present a significant risk of abuse. Ibutamoren (MK-0677) is a potent, long-acting, selective non-peptide growth hormone secretagogue that can be taken orally. Methods: This study examines ibutamoren and its metabolites in thoroughbred horses after oral administration. Liquid chromatography/high-resolution mass spectrometry was used to determine the probable structures of the detected metabolites. Results: In this study, 22 metabolites of ibutamoren were identified (17 phase I and 5 p...
Doran G, Hughes K, Rendle D, Edwards S.Pergolide is used to treat pituitary pars intermedia dysfunction (equine Cushing's Disease), a neurodegenerative condition associated with loss of dopaminergic inhibition of the pituitary in horses. After oral administration, only low concentrations of the drug are achieved in plasma, making drug detection and quantification difficult. While direct analysis of plasma using sensitive MS/MS techniques is possible, dirty plasma samples and mobile phase buffers can cause instrumentation to become rapidly incapacitated. A method using LC with fluorescence detection was developed for pergolide analy...
Timms M, Botteon A, Manos C, Griffin J, Levina V, Steel R.Gonadotropin-releasing hormone (GnRH) and its synthetic analogues are considered banned substances by the racing industry. GnRH is used as a pharmaceutical to regulate the female oestrous cycle, but the hormone is also thought to increase the production of testosterone in male animals. Using liquid chromatography in conjunction with high-resolution mass spectrometry (LC-HRMS) and data-independent acquisition (DIA), a method is presented for the detection of intact and truncated peptides of GnRH and its analogues down to the low picogram level in equine urine. The study of the catabolism of GnR...