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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 antipyrine, acetaminophen and lidocaine in fed and fasted horses. Previous studies demonstrated that plasma clearance of organic anions such as bilirubin, bile acid, sulfobromophthalein (BSP) and indocyanine green (ICG), was reduced from 36% (bile acid) to 55% (ICG) in fasted (3 days) horses. It is believed that a general decline in carrier-mediated hepatic uptake may have accounted for those changes. However, fasting may also affect hepatic blood flow, thereby contributing to reduced clearance of these compounds. In order to test this hypothesis, plasma clearance of antipyrine, acetaminophen and lidocaine, drugs known to be cleared by the liver yet not susp...
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...
Antimicrobial selection and dosage in the treatment of equine bacterial infections. The success of antimicrobial therapy depends on administration of an agent to which the pathogenic microorganisms are susceptible at the concentrations attained at the site of infection. The route of administration, size of the dose and dosing interval must be appropriate for the drug preparation selected. With penicillins in particular, dosage can be tailored to the severity of the infection and quantitative susceptibility of the microorganism. This approach cannot be applied to aminoglycosides because their relatively narrow margin of safety limits the amount which can be administered. In se...
Single- and repeat-dose pharmacokinetic studies of chloramphenicol in horses: values and limitations of pharmacokinetic studies in predicting dosage regimens. A single-dose pharmacokinetic study of chloramphenicol in propylene glycol was done in 6 horses after 22 mg/kg was administered IV. Serum drug concentrations obtained at various predetermined intervals were determined by an electroncapture gas-chromatographic technique. The time-concentration data were described by a 2-compartment open model, and various pharmacokinetic variables were estimated. The median elimination rate constant was estimated to be -0.0185 minute-1 (-0.0225 to -0.0148 minute-1), and the median half-life was 37.36 minutes (30.74 to 46.90 minutes). The median apparent volume ...
Effect of topical phenylephrine on the equine pupil. The mydriatic effect of 10% phenylephrine was evaluated in 9 horses. Base-line pupillary size in mesopic conditions and during light stimulation was ascertained before application of pharmacologic agents. In study 1, 10% phenylephrine was applied to each eye (n = 5 horses). After 15 minutes, the pupillary size was determined in both lighting conditions. Phenylephrine was again applied to each eye, and after an additional 15 minutes, the pupillary size was determined. In study 2, 1% tropicamide was applied to each eye (n = 4 horses), and after 30 minutes, the pupillary size was determined in bo...
Systemic and centrally mediated angiotensin II effects in the horse. The primary aim of the study was to evaluate the potential value of intravenous (i.v.) infusion of angiotensin II (AII) for phonocardiographic differential diagnosis of equine valvular insufficiency. Ten-minute AII infusions at 4.5-33 pmol kg-1 min-1 induced clear-cut dose-dependent rises in systemic arterial blood pressure (aBP), whereas the pulmonary aBP remained largely unaffected. It implies that i.v. infusion of AII at about 10 pmol kg-1 min-1 could be a valuable tool for the acoustic differentiation between mitral and tricuspid valvular dysfunction in the horse. The infusion at, and abov...
Pharmacological manipulation of sexual behaviour in stallions. Series of experiments and clinical trials were conducted to evaluate the effects of psychoneurotropic agents on sexual behaviour of stallions. The benzodiazepine derivative, diazepam (Valium), effectively reversed experimentally suppressed precopulatory arousal and response. Diazepam treatment also blocked the negative effect of novel environment on sexual response. The dibenzazepines imipramine and clomipramine induced erection, masturbation, and ejaculation in the absence of a sexual stimulus.
Effect of aspirin on ex vivo generation of thromboxane in healthy horses. Different dosages of aspirin were administered (by nasogastric tube) to 3 groups of 5 healthy adult horses to determine the minimal effective dosage needed to decrease serum thromboxane B2 (TxB2) concentrations and to determine the duration of this decrease. When compared with their base-line serum TxB2 concentrations, horses in group 1 (given 5 mg/kg) had a 71% decrease in TxB2 concentrations at 24 hours after aspirin was given and a 86% decrease at 48 hours; serum TxB2 concentrations were back to base-line values by 120 hours. Horses in group 2 (given 10 mg/kg) had a 60% decrease in TxB2 con...
Effects of cromolyn in horses with chronic obstructive pulmonary disease. The effect of disodium cromoglycate (cromolyn) in preventing the pulmonary dysfunction caused by the inhalation of barn and hay dust was studied in 5 horses with confirmed chronic obstructive pulmonary disease (COPD). The horses were studied before (Con) and after exposure to hay and dust allergens (Expos) and after pretreatment with cromolyn followed by exposure (Cr-Expos). There was a significant reduction in PaO2 from 86.8 +/- 8.3 to 73.1 +/- 8.8 when the horses were exposed to hay and dust allergens. The PaO2 after pretreatment with cromolyn and exposures was 78.1 +/- 5.5. There were no si...
Comparison of progesterone and progesterone + oestrogen on total and specific uterine proteins in pony mares. Eight ovariectomized pony mares were used to test the effect of various doses of progesterone (0, 50, 150, 450 mg/day, in oil, i.m., for 10 days) on progesterone and LH in the peripheral circulation, and on total protein and uteroferrin in uterine secretions. Progesterone increased uteroferrin, but there were no differences amongst doses of progesterone. Progesterone treatment decreased LH, and tended to increase total protein. Eighteen ovariectomized mares were given vehicle, oestradiol (10 mg/day, in oil, i.m.), progesterone or progesterone + oestradiol for 28 days. Both the last two steroid...
Antipyrine and lidocaine are cleared faster in horses than in humans: acetaminophen may be handled similarly. The following studies were designed to evaluate plasma elimination kinetics of intravenously administered antipyrine, acetaminophen and lidocaine among 9 healthy adult horses and 9 healthy drug-free humans (3 each per drug group), in order to compare potential species differences in drug-metabolizing ability. Acetaminophen is largely biotransformed in humans by hepatic glucuronide and sulfate conjugation, whereas both antipyrine and lidocaine are oxidized by hepatic microsomal mixed-function oxidases. Thus, plasma clearances of these drugs are thought to reflect differences in hepatic oxidativ...
Use of a novel non-steroidal anti-inflammatory drug in the horse. In a two-part cross-over experiment in six ponies, an acute inflammatory reaction was generated by injecting carrageenin solution into subcutaneously-implanted tissue-cages lined with fibrovascular granulation tissue. In each part of the cross-over, half of the ponies received a novel phenylpyrazoline anti-inflammatory agent (BW540C) orally and half received a placebo treatment. BW540C inhibited platelet cyclo-oxygenase for 24 h but the reductions in exudate eicosanoid concentrations were less pronounced. A significant suppression in the rise of surface skin temperature in BW540C-treated ponie...
Effects of chronic administration of a monoclonal antibody against human renin in the marmoset. In this study, the hypotensive efficacy of R-3-36-16, a monoclonal antibody against human kidney renin, was investigated during chronic administration to a primate. R-3-36-16 was given by continuous intraperitoneal infusion with osmotic minipumps to normotensive marmosets fed a low-sodium diet in doses of 30 or 300 micrograms/kg/day for 14 days. The lower dose had no effect on blood pressure (BP) or plasma renin activity (PRA). After two days of treatment, the higher dose reduced PRA by 57% and lowered BP by 13 +/- 7 mm Hg. Although the hypotensive response persisted after 14 days of treatment...
Body fluid concentrations and pharmacokinetics of chloramphenicol given to mares intravenously or by repeated gavage. Serum concentrations and the pharmacokinetics of chloramphenicol were determined in 6 healthy mares after a single IV administration (50 mg/kg of body weight) or after the 1st and 5th sequential intragastric (IG) administration (50 mg/kg/6 hours) of chloramphenicol. Synovial fluid, peritoneal fluid, CSF, and urinary concentrations of chloramphenicol after the IG administrations also were determined. Mean (+/- SEM) overall elimination rate constant (K) values for the IV, 1st IG, and 5th IG dosages were 0.42 +/- 0.064/hr, 0.42 +/- 0.049/hr, and 0.29 +/- 0.074/hr, respectively, and were not signi...
[The clinical pharmacology of glycerol guaiacolate ether in the horse–a review]. The physical and chemical properties, administration, biotransformation, pharmacological effects, clinical applications, side-effects, toxicity and contraindications of glyceryl guaiacolate ether in the horse are reviewed.
The lack of effect of inoculation with equine influenza vaccine on theophylline pharmacokinetics in the horse. Several studies conducted during the past few years have shown that the pharmacokinetics of a variety of drugs may be altered following viral infection or vaccination. The elimination of drugs which are extensively metabolized, such as theophylline, may be prolonged, especially following exposure to RNA viruses such as Type A influenza or similar orthomyxoviruses. The purpose of this study was to determine whether vaccination of horses with equine influenza virus affected pharmacokinetic parameters describing the distribution and elimination of intravenously administered theophylline. Three th...
Pharmacokinetics of rifampin given as a single oral dose in foals. Six foals from 6 to 8 weeks of age were given a single oral dose of rifampin at a dosage of 10 mg/kg of body weight. Serum rifampin concentrations were measured serially during a 24-hour period. The mean peak serum rifampin concentration was 6.7 micrograms/ml at 4 hours after treatment. The concentration decreased slowly, and at 24 hours the mean value was 2.7 micrograms/ml. The elimination half-life was 17.5 hours, and the elimination rate constant was 0.04/hr.
Pharmacokinetics and endometrial tissue concentrations of ticarcillin given to the horse by intravenous and intrauterine routes. Plasma and endometrial tissue concentrations of ticarcillin were measured in healthy mares. In the first of the 3 separate phases comprising the study, ticarcillin disodium (30 mg/kg) was administered IV. The mean peak concentration in endometrial tissue, 12.9 micrograms/g, was attained at 30 minutes. The plasma half-life of the drug in the 6 mares was 0.83 +/- 0.22 hour. Six grams of the drug was diluted in 250 ml of sodium chloride injection USP (2nd phase) and in 60 ml of sodium chloride injection USP (3rd phase). These dilutions were administered by intrauterine infusion. In phase 2, the m...
Effects of propranolol on cardiopulmonary function in the pony during submaximal exercise. Cardiopulmonary responses of four ponies were monitored during standard exercise tests (SET), before and after beta-adrenergic receptor blockade with propranolol. The SET consisted of four 5 min increments of increasing speed from 1.0 to 2.8 m/sec on a treadmill at a 7 degrees incline. Data were collected at rest, throughout the SET and recovery. Administration of propranolol to ponies at rest had no effect on cardiopulmonary function. During the SET, increases in heart rate, mean pulmonary artery flow velocity (an index of cardiac output) and right ventricular dP/dt (an index of myocardial co...
Effect of the injection site on the pharmacokinetics of procaine penicillin G in horses. The plasma penicillin concentrations were determined in 5 horses given an IV injection of sodium penicillin G; plasma penicillin concentrations were also determined in a crossover experiment, where animals were given procaine penicillin G subcutaneously at 1 site and IM at 4 sites. The mean penicillin plasma peak concentration and bioavailability were highest after the drug was injected in the neck and biceps musculature. Injections in the gluteal muscle and in the subcutaneous sites resulted in similar, but lower, more persistent penicillin plasma concentrations and a lower bioavailability th...
Cardiopulmonary effects of continuous intravenous infusion of guaifenesin, ketamine, and xylazine in ponies. Eight ponies were anesthetized with a solution containing 50 mg of guaifenesin, 1 mg of ketamine, and 0.5 mg of xylazine X ml-1 of 5% dextrose in water. Anesthesia was induced by IV injection (1.1 ml X kg-1), followed by continuous IV infusion at 2.75 ml X kg-1 X hr-1. Heart rate, rate-pressure product, mean pulmonary artery pressure, and standard bicarbonate were not significantly changed throughout the study. Systolic, diastolic, and mean arterial pressures and left ventricular stroke work index were significantly decreased at 5 and 15 minutes after a bolus of the anesthetic solution was inj...
Effects of a phenylbutazone paste in ponies: model of acute nonimmune inflammation. In a 12-day treatment schedule, 5 ponies were given orally a paste formulation of phenylbutazone (PBZ) and 5 matched ponies were given equivalent doses of a placebo paste. On day 12, a mild, nonimmune inflammatory reaction was induced subcutaneously in the neck of each pony by inserting sterile, polyester sponge strips soaked in a 2% carrageenan solution. Exudate was collected at 4, 8, 12, and 24 hours by serial removal of sponges. There were no significant (P less than 0.05) differences in exudate protein concentration and leukocyte numbers between the treatment groups, but the group given PB...
Pharmacokinetics of sodium amoxicillin in foals after intramuscular administration. Pharmacokinetic values of sodium amoxicillin (22 mg/kg of body weight) in foals were determined after a single IM injection in 6 Quarter Horse foals at 3, 10, and 30 days of age. Serum amoxicillin concentrations were measured serially over a 24-hour period. The absorption of amoxicillin was rapid and followed a 1st-order elimination. Mean peak serum concentrations occurred 30 minutes after the injection in foals at all ages and were 17.31 +/- 9.59 micrograms/ml when the foals were 3 days old, 23.28 +/- 9.86 micrograms/ml when the foals were 10 days old, and 21.35 +/- 6.39 micrograms/ml when th...
Cardiovascular and pharmacokinetic effects of isoxsuprine in the horse. 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...
Pharmacokinetic adjustment of gentamicin dosing in horses with sepsis. Serum gentamicin concentrations were measured and pharmacokinetic values were calculated for 12 equine patients receiving parenteral gentamicin therapy. Horses were selected for monitoring of gentamicin pharmacokinetics if they met several criteria of high risk for gentamicin-induced toxicosis. Two blood samples were obtained, one immediately before gentamicin dosing and one at 1 hour after dosing. Gentamicin serum concentrations were analyzed and dosage adjustments were made on the basis of calculated one-compartment pharmacokinetic values. Nine of the 12 horses required dosage adjustment to ...
