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Topic:Pharmacokinetics
Pharmacokinetics in horses involves the study of how drugs are absorbed, distributed, metabolized, and excreted in equine species. This field of study provides insights into the time course of drug concentrations within the horse's body and helps in understanding the effects of various pharmaceuticals. Key parameters in equine pharmacokinetics include absorption rates, bioavailability, half-life, and clearance. These parameters can vary significantly due to factors such as age, breed, and health status of the horse. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacokinetic profiles of different drugs in horses, aiming to optimize dosing regimens and improve therapeutic outcomes in equine medicine.
Pharmacokinetics of phenolsulfonphthalein in horse and pony mares. Pharmacokinetics of phenolsulfonphthalein (PSP) in horse and pony mares was determined after injection of 1 mg/kg of body weight, IV. A plasma PSP concentration vs time curve was described adequately in horses and ponies by an open, 2-compartment model. There were significant differences in the elimination phase parameters, apparent volume of distribution at steady state, and apparent volume of distribution of horses and ponies. The harmonic mean elimination half-life of PSP in horses was significantly longer (P less than 0.001) than that in the ponies (16.4 and 10.0 minutes, respectively). Th...
Rapid reversible immobilization of feral stallions using etorphine hydrochloride, xylazine hydrochloride and atropine sulfate. Forty-eight newly captured free-ranging feral stallions (Equus caballus) from two different locations and six captive stallions were immobilized using combinations of etorphine hydrochloride, xylazine hydrochloride and atropine sulfate with or without acepromazine. Six animals were immobilized twice, 1 mo apart. The drugs were administered either intramuscularly (n = 13) or intravenously (n = 44). Mean immobilization time (+/- SE) after intravenous (i.v.) injection of etorphine, xylazine and atropine was 55 +/- 4 sec (range 20 to 185 sec) compared to 708 +/- 131 sec (range 390 to 1,140 sec) fo...
Plasma lidocaine concentrations in conscious horses after cervicothoracic (stellate) ganglion block with 1% lidocaine HCl solution. Arterial and/or central venous plasma concentrations of lidocaine were determined in 12 nonmedicated adult horses (422 +/- 59 kg of body weight, mean +/- SD) after injecting a 1% lidocaine HCl solution into the cervicothoracic ganglion (CTG). A mean dosage of 2.9 +/- 0.5 mg of lidocaine/kg of body weight was used to induce unilateral CTG blockade in 8 horses and 4.8 +/- 0.8 mg was used to induce bilateral CTG blockade in 4 horses. Blood samples were collected before and at 5, 15, 30, 45, 60, 75, 90, 105, and 120 minutes after injection. The plasma lidocaine concentrations were determined by us...
Measurement of flunixin in equine inflammatory exudate and plasma by high performance liquid chromatography. An accurate and reliable method for the separation of flunixin from, and measurement in, equine inflammatory exudate and plasma by high performance liquid chromatography has been developed. Flunixin can be detected in concentrations as low as 0.05 micrograms/ml using an ultraviolet spectrophotometric detector at 285 nm. Samples were acidified with 2M hydrochloric acid and extracted with dichloromethane. The extract was evaporated and reconstituted in acetonitrile. Iminodibenzyl was used as internal standard. The mean recovery of flunixin from plasma was 97.6 +/- 3.9 per cent. Particular advant...
HPLC determination and pharmacokinetics of thiabendazole and its major metabolite 5-OH thiabendazole in equine plasma. Separate high performance liquid chromatographic methods were developed for thiabendazole (TBZ) and 5-hydroxy thiabendazole (5-OH-TBZ) determination in horse plasma using 1-methyl-2-phenyl benzimidazole (MPBZ) as an internal standard. In both methods TBZ and 5-OH-TBZ were extracted from plasma using organic solvents, injected on to a C-18 column, and eluents monitored by a fluorescence detector. However, mobile phase composition, extraction solvent as well as detector wavelength differed in the two methods. The linear range for TBZ was 0.02 to 0.77 microgram ml-1 while that for 5-OH-TBZ was 0....
Atrial fibrillation in a pregnant mare: treatment with quinidine sulfate. Atrial fibrillation in a pregnant, lactating, 15-year-old mare nursing a 70-day-old foal was converted to normal sinus rhythm, using quinidine sulfate. The maximum concentration of quinidine was 4.3 mg/L in the mare's milk and was 2.6 mg/L in the mare's serum. Treatment with quinidine did not interrupt the pregnancy. Six months after treatment, the mare developed acute volvulus of the large colon and died. At necropsy, the mare did not have macroscopic or microscopic cardiac lesions. The fetus was macroscopically and histologically normal.
Actions of non-steroidal anti-inflammatory drugs on equine leucocyte movement in vitro. The direct effects of four non-steroidal anti-inflammatory drugs (NSAIDs) on equine polymorphonuclear (PMN) and mononuclear (MN) leucocyte movement were investigated using two in vitro assay systems. The Boyden chamber microfilter technique measures both chemokinetic and chemotactic locomotion, and the agarose microdroplet assay measures solely chemokinesis. Zymosan-activated plasma (ZAP) and the synthetic peptide N-formyl-methionyl-leucyl-phenylalanine (FMLP) were used as standard chemoattractants for PMN and MN leucocytes, respectively. The actions of six concentrations of each NSAID, indome...
Pharmacokinetics and serum concentrations of cephapirin in neonatal foals. Six healthy foals, from 4 to 6 days of age, were given a single IM injection of sodium cephapirin (250 mg/ml) at a rate of 20 mg/kg of body weight. Serum concentrations of cephapirin were measured serially over an 8-hour period. The mean peak serum concentration was 21.2 micrograms/ml at 10 minutes. The overall elimination rate constant was 1.06/hr and the elimination half-life was 0.70 hour. The apparent volume of distribution at steady state was 1.06 L/kg and plasma clearance was 1,105 ml/hr/kg.
Pharmacokinetics of phenobarbital in the horse. Pharmacokinetics of phenobarbital was examined in 6 mature horses after 12 mg of phenobarbital/kg of body weight was infused over 20 minutes. Biexponential decrease in serum phenobarbital concentrations was observed with a distribution-phase half-life of 0.101 +/- 0.086 hour (mean +/- SD) and a terminal-phase elimination half-life of 18.3 +/- 3.65 hours. The volume of distribution at steady state was 0.803 +/- 0.070 L/kg. Total body clearance of phenobarbital was 30.8 +/- 6.2 ml/h/kg. The high clearance in the horse seems to explain the markedly shorter half-life of phenobarbital in this speci...
Imipramine-induced erection, masturbation, and ejaculation in male horses. Imipramine hydrochloride was administered to five male horses (400-500 kg b.wt.): one experienced young stallion, two mature normal breeding stallions, one 5-year-old stallion with erection and ejaculatory dysfunction, and one long-term castrated male horse. Oral imipramine treatment (100 to 600 mg, twice daily) led to frequent erection and masturbation while at rest in the stall in a nonsexual context. Intravenous imipramine treatment over a range of doses (50 to 1000 mg) similarly induced erection and masturbation in all animals. Erection typically occurred within 10 minutes after injection,...
Absorption of neomycin from the equine uterus: effect of stage of oestrous cycle and volume of vehicle. Plasma concentrations of neomycin were measured following intrauterine infusion of 3.3 mg/kg bodyweight neomycin sulphate. Mares in oestrus absorbed approximately 6 per cent of neomycin infused whereas mares in a luteal phase absorbed 56 per cent. The volume of infusate also affected absorption as increased volume resulted in decreased absorption. The decreased absorption both during oestrus and when large volumes were used was probably due to reflux of antibiotic through the cervix.
Responses of horses to acepromazine maleate administered orally in a paste. The effects of acepromazine maleate (ACP), given orally in a paste form, were examined in six standard-bred geldings over a 12 hour period. Three dose rates, zero (placebo paste), 0.13 mg kg-1 and 0.26 mg kg-1, given before or after feeding, were investigated. The data were divided into two sampling periods for analysis, one from zero to 120 minutes and the other from four to 12 hours. Sedation was assessed by a score (TS score) based on general appearance, anal sphincter relaxation and penile protrusion. This TS score was significantly elevated 40 minutes after dosing with ACP, irrespective o...
Presence of salicylic acid in standardbred horse urine and plasma after various feed and drug administrations. Plasma and urinary levels of salicylic acid were examined in Standardbred mares after administration of various feeds, containing different compositions of hay. In addition, horses were administered acetylsalicylic acid orally and methyl salicylate topically. Elevated salicylic acid levels were observed in horse urine and plasma in animals fed lucerne hay. The plasma and urinary elimination of salicylic acid exhibited a diurnal pattern which was related to the type of feed and the feeding schedule. Within 24 h after oral administration of acetylsalicylic acid, plasma and urine salicylic acid l...
Low dose flunixin meglumine: effects on eicosanoid production and clinical signs induced by experimental endotoxaemia in horses. The efficacy of low doses of flunixin meglumine in reducing eicosanoid generation and clinical signs in response to experimentally induced endotoxaemia was investigated. Thromboxane B2 and 6-keto-prostaglandin F1 alpha were measured in serum and plasma by radioimmunoassay. Plasma flunixin concentrations were determined by high performance liquid chromatography and pharmacokinetic parameters derived non-compartmentally. In horses administered flunixin meglumine before endotoxin challenge, a significant suppression in plasma thromboxane B2 and 6-keto-prostaglandin F1 alpha generation was observe...
Development of an enzyme-linked immunosorbent assay for the detection of phenothiazine tranquillisers in horses. An acepromazine (ACP) hapten was synthesised, coupled to bovine serum albumin and injected into a horse to produce antibodies to the drug. A competitive ELISA was developed whereby ACP attached to the solid phase via lysozyme competed with free ACP present in phosphate buffered saline, horse serum or horse urine for limiting amounts of antibody. The assay could detect the presence of ACP and, or, some of its metabolites in horse urine for at least 25 hours after intravenous injection of 0.1 mg kg-1 ACP maleate, but because of non-specific interference, horse serum could not be used. As little ...
Principles of drug disposition in the horse. This article is intended to give the reader an understanding of the mathematic and conceptual framework underlying equine pharmacology. The methods by which the veterinary practitioner determines drug concentrations, disposition, and bioavailability are discussed.
Clinical pharmacology of the gastrointestinal tract. This article discusses the various drugs that affect the equine gastrointestinal tract. Drugs that alter intestinal motility, that protect the gastrointestinal tract, and that alter secretions, as well as analgesics, appetite stimulants, and orally administered antimicrobial agents are reviewed.
Cardiovascular drugs. Their pharmacology and use in horses. Knowledge of the dosage, rate and route of administration, and potential side effects of drugs used to treat cardiac disease in horses has been refined. The judicious use of these drugs can increase exercise capacity, improve health, and potentially prolong life. Currently, antiarrhythmics (quinidine, lidocaine), positive inotropies (digoxin), and diuretics (furosemide) are the primary agents used to treat cardiovascular disease in horses. The development of newer drugs (verapamil, milrinone, bumetanide) and their usefulness in therapy for horses with cardiovascular disease require further inv...
Rational selection of antimicrobial drugs for treatment of infections of horses. The goal of antimicrobial drug use is quite specific. Consideration of many microbe-related, host-related, and drug-related factors is necessary for appropriate selection and use of antimicrobial drugs in equine patients. The concepts and data presented in this article demonstrate that fact. At the risk of oversimplification, "The bug denotes the drug, and the horse directs the course."
The bioavailability of phenylbutazone in the horse. [phenyl-14C]-Phenylbutazone was administered to 2 horses p.o. and i.v. on separate occasions. Plasma levels and urinary and faecal elimination of 14C were monitored for up to 7 days after dosing. Phenylbutazone was rapidly and extensively absorbed after oral administration, and its bioavailability was 91% assessed by comparison of plasma AUCs of unchanged drug after p.o. and i.v. administration. The plasma elimination half-life of phenylbutazone was 9.7 h and this was independent of the route of administration. The pattern of elimination of phenylbutazone was independent of the route of admini...
Injectable anesthetics and anesthetic adjuncts. The purpose of this article is to review the use of selected anesthetics and anesthetic adjuncts in horses. Emphasis is placed on the pharmacologic bases of their use.
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...
Pharmacokinetics of intravenously administered ketamine in the horse. The metabolism and distribution of ketamine and its two major metabolites (norketamine and dehydronorketamine) was investigated in 10 horses undergoing airway surgery. Following premedication with xylazine (1.1 mg kg-1 intravenously) anaesthesia was induced by the rapid injection of ketamine at a dose of 2.2 mg kg-1 intravenously. Anaesthesia was maintained with halothane vaporized in oxygen and nitrous oxide (50:50). Serially collected blood samples were analysed by a sensitive gas liquid chromatographic technique. Plasma ketamine concentrations declined biexponentially with a rapid initial d...
