Topic:Pharmaceuticals
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.
Adverse drug reactions in the horse. Adverse drug reactions occasionally occur in the horse. The majority can be anticipated and avoided. The practicing veterinarian should understand the various types of adverse reactions as well as their mechanisms so that should such a reaction occur, the practitioner can promptly recognize the problem and institute corrective measures.
Pharmacologic considerations in drug therapy in foals. Rational drug therapy in the foal requires a sound knowledge of the pharmacodynamics and pharmacokinetics of various drugs as well as a thorough understanding of the physiologic differences that exist between the neonate and the adult and that may serve to alter drug disposition and, therefore, drug response. A summary of these physiologic factors with emphasis on the foal is presented and is followed by recommendations regarding the applied therapeutics of various antimicrobial agents.
Drug therapy of respiratory disorders. The emphasis of this article is on the clinical application of drugs in therapy for treatment of disorders of the lower respiratory tract. Medications discussed include those used to enhance clearance of secretions and those employed to prevent and/or alleviate bronchoconstriction. Antimicrobial agents and respiratory stimulants are briefly mentioned.
Metabolism, excretion, pharmacokinetics and tissue residues of phenylbutazone in the horse. The pharmacokinetics, metabolism, excretion and tissue residues of phenylbutazone (PBZ) in the horse were studied following both intravenous and oral administration of the drug at a dose rate of 4.4 mg/kg. A 72-hour blood sampling schedule failed to demonstrate a third exponential phase; the plasma disposition following intravenous injection being described by a two compartment open model, with the following elimination phase parameters: beta = 0.13h-1, t1/2 beta = 5.46h, Vdarea = 0.141 1/kg and C1B = 17.9 ml/kg/h. The hydroxylated metabolites oxyphenbutazone (OPBZ) and gamma-hydroxyphenylbuta...
Detection and identification of ketamine and its metabolites in horse urine. The possibility exists that ketamine, or ketamine in combination with xylazine, is being used illicitly to affect the performance of racehorses. This study was undertaken to identify the metabolites of ketamine in the urine of adult horses and to evaluate methods for detecting and confirming ketamine administration. Detection of ketamine and two ketamine metabolites is described using thin-layer chromatography (TLC) and their identities are confirmed by comparing their mass spectra and gas chromatographic retention times with those of authentic standards.
Pharmacokinetics and renal clearance of sulfamethazine, sulfamerazine, and sulfadiazine and their N4-acetyl and hydroxy metabolites in horses. Plasma disposition, protein binding, urinary recovery, and renal clearance of sulfamethazine (SMZ), sulfamerazine (SMR), and sulfadiazine (SDZ) and their N4-acetyl and hydroxy derivatives were studied in 4 horses in a crossover trial. The plasma concentration-time curves of the metabolites paralleled those of the parent drug in the elimination phase. Sulfamethazine and SMR were extensively metabolized. In plasma and urine, the main metabolite of the 3 sulfonamides tested was the 5-hydroxypyrimidine derivative, which was highly glucuronidated. Difference in elimination half-life of SMZ, SMR, an...
The biotransformation and urinary excretion of dexamethasone in equine male castrates. The pro-drugs of dexamethasone, a potent glucocorticoid, are frequently used as anti-inflammatory steroids in equine veterinary practice. In the present study the biotransformation and urinary excretion of tritium labelled dexamethasone were investigated in cross-bred castrated male horses after therapeutic doses. Between 40-50% of the administered radioactivity was excreted in the urine within 24 h; a further 10% being excreted over the next 3 days. The urinary radioactivity was largely excreted in the unconjugated steroid fraction. In the first 24 h urine sample, 26-36% of the total dose was...
Detomidine: a new sedative for horses. Detomidine, given intravenously at doses of 5 to 30 (mean 13) micrograms/kg bodyweight (bwt), provided adequate sedation for a variety of clinical procedures in 93 per cent of administrations, and improved the ease of handling in the remaining animals. Side effects of ataxia and bradycardia were minimal at the lower dose rates. Higher doses were required for intramuscular use. In experimental trials 10 and 20 micrograms/kg bwt resulted in deep sedation and also significant hypertension and bradycardia of over 15 mins duration. Current literature on the use of detomidine in horses is reviewed.
Pharmacokinetics and diuretic effect of bumetanide following intravenous and intramuscular administration to horses. Concentrations of the potent diuretic bumetanide were determined by a sensitive high performance liquid chromatographic procedure in plasma and urine from horses following intravenous and intramuscular administration of a dose rate of 15 micrograms/kg. The elimination half-life was found to be 6.3 min, the volume of distribution at steady state 68 ml/kg and the total plasma clearance 10.9 ml/min/kg. The onset of diuresis occurred within 15 min and diuresis was no longer apparent 1 h after i.v. administration. Given by the intramuscular (i.m.) route, bumetanide was rapidly absorbed; bioavailabi...
Pharmacokinetic disposition of dimethyl sulfoxide administered intravenously to horses. Dimethyl sulfoxide (DMSO) was administered IV to 6 Thoroughbred horses at 2 dosages: 1.0 g/kg and 0.1 g/kg. The pharmacokinetics seemed linear, with biological half-lives of 8.6 +/- 0.3 hours and 9.8 +/- 2.2 hours for the 1.0 g/kg and 0.1 g/kg dosages, respectively. This was further substantiated by mean residence times of 9.8 +/- 0.44 hours and 13.8 +/- 4.25 hours, areas under the curve of 12.55 +/- 1.42 mg/ml/hr and 1.63 +/- 0.49 mg/ml/hr, and the clearances of 0.081 +/- 0.009 L/kg/hr and 0.066 +/- 0.022 L/kg/hr for the large and small dosages, respectively. At 12 hours after 1.0 g/kg was ad...
Determination of nefopam in equine plasma by gas chromatography-mass spectrometry with chemical ionization. This study demonstrates the development of a method using gas chromatography-mass spectrometry for determining nefopam, a non-narcotic pain reliever that is sometimes abused in horse doping, in equine plasma. Background […]
Phenylbutazone in the horse: a review. 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...
Effects of xylazine on renal function and plasma glucose in ponies. The intravenous administration of xylazine (1.1 mg/kg bodyweight) in six ponies resulted in a significant increase in urine output over two hours, with maximum flow occurring between 30 and 60 minutes after injection. Urine specific gravity, osmolality and glucose concentration decreased. Renal clearance of endogenous creatinine was unchanged. Significant increases in the excretion of potassium and chloride occurred. Plasma glucose concentration was increased 30 minutes after the administration of xylazine by a mean value of 37 per cent. Serum osmolality and sodium, potassium and chloride conc...
Isolation of meclofenamic acid and two metabolites from equine urine–a comparison between horse and man. Two metabolites of meclofenamic acid have been isolated from equine urine. Both metabolites are found to be monohydroxylated forms of meclofenamic acid by gas chromatography-mass spectrometry after extractive alkylation. The parent drug and the metabolites are separated by reversed-phase liquid chromatography on a Spherisorb ODS column, using methanol-phosphate buffer eluents and UV detection at 280 nm. The structure of the metabolites is discussed on the basis of LC, TLC and GC-MS data.
Renal toxicity of non-steroidal anti-inflammatory drugs. Non-steroidal anti-inflammatory drugs represent the most heavily prescribed and used class of drugs in human medicine. Most are derivatives of either salicylates, propionic acid, indoleacetic acid, anthranilic acid, pyrazolone, or oxicams. They depress the synthesis of prostaglandins from arachidonic acid by reversible inhibition of the enzyme cyclooxygenase. In the kidney, prostaglandins PGE2 and PGI2 modulate the vasoconstrictor effects of angiotensin II, norepinephrine, and vasopressin. In the presence of volume contraction, anesthesia, or disease states associated with high levels of these...
Identification of betamethasone and a major metabolite in equine urine. Betamethasone and its major unconjugated metabolite, 6-beta-hydroxybetamethasone, were detected in equine urine by thin-layer chromatography and characterized by micro-liquid chromatography/mass spectrometry (micro-LC/MS). Their structures were confirmed by a combination of infrared spectroscopy and nuclear magnetic resonance spectroscopy.
Analysis of pharmaceutical dosage forms for oxfendazole: II. Simultaneous liquid chromatographic determination of oxfendazole and trichlorfon in equine paste. A reverse phase liquid chromatographic procedure is described for the simultaneous determination of oxfendazole [2-(methoxycarbonylamino)-5-phenylsulfinylbenzimidazole] and trichlorfon [(2,2,2-trichloro-1-hydroxyethyl)phosphonic acid dimethyl ester] in equine paste. The sample is extracted by sonication in methanol. Insoluble excipients are removed by centrifugation and an aliquot plus internal standard are diluted with dilution solvent (water-acetonitrile-phosphoric acid, 80 + 20 + 1). The samples are filtered and injected onto a Partisil-5 ODS-3 column with acetonitrile-0.01 M phosphate buff...