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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.
Effect of neostigmine on contractility of equine pre-ovulatory follicles: An in vitro study.
Theriogenology    November 29, 2016   Volume 90 74-77 doi: 10.1016/j.theriogenology.2016.11.025
Piccinno M, Rizzo A, Cariello G, Sciorsci RL.In this study, the Authors investigated the modulatory effect of three single doses (10, 10, and 10 M) of neostigmine on the spontaneous contractility of equine pre-ovulatory follicles in an isolated organ bath, to establish the relationship between this acetylcholinesterase inhibitor and ovulation, in the mare. The results indicate that neostigmine increases pre-ovulatory contractility in equine follicles at each dose, but in a different manner. Indeed, the rise in contractility induced by neostigmine at 10 M and 10 M was phasic, while at 10 M it was tonic. The data obtained indicate poss...
Repeated oral administration of a cathepsin K inhibitor significantly suppresses bone resorption in exercising horses with evidence of increased bone formation and maintained bone turnover.
Journal of veterinary pharmacology and therapeutics    November 24, 2016   Volume 40, Issue 4 327-334 doi: 10.1111/jvp.12368
Hussein H, Dulin J, Smanik L, Drost WT, Russell D, Wellman M, Bertone A.Our investigations evaluated the effect of VEL-0230, a highly specific irreversible inhibitor of cathepsin K (CatK). The objectives of our study were to determine whether repeated dosing of a CatK inhibitor (CatKI) produced a desired inhibition of the bone resorption biomarker (CTX-1), and document the effect of repeated dosing on bone homeostasis, structure, and dynamics of bone resorption and formation in horses. Twelve young exercising horses were randomized in a prospective, controlled clinical trial and received 4 weekly doses of a CatKI or vehicle. Baseline and poststudy nuclear scintigr...
Pharmacokinetics of oral terbinafine in adult horses.
Journal of veterinary pharmacology and therapeutics    November 24, 2016   Volume 40, Issue 4 342-347 doi: 10.1111/jvp.12367
Younkin TJ, Davis EG, Kukanich B.The primary study objective was to compare the pharmacokinetics of p.o. terbinafine alone to p.o. terbinafine administered with p.o. cimetidine in healthy adult horses. The second objective was to assess the pharmacokinetics of terbinafine when administered per rectum in two different suspensions at 30 mg/kg to adult horses. Six healthy adult horses were included in this crossover study. Plasma terbinafine concentrations were quantified with liquid chromatography and mass spectrometry. The half-life (geometric mean) was 8.38 and 10.76 h, for p.o. alone and p.o. with cimetidine, respectively....
Pharmacokinetics and tolerability of a new formulation of omeprazole in the horse.
Journal of veterinary pharmacology and therapeutics    November 24, 2016   Volume 40, Issue 4 348-355 doi: 10.1111/jvp.12371
Di Salvo A, Busechian S, Zappulla F, Marchesi MC, Pieramati C, Orvieto S, Boveri M, Predieri PG, Rueca F, Della Rocca G.A new formulation of omeprazole in gastro-resistant granules was tested with regard to its pharmacokinetics and tolerability. Twenty-four horses were randomly divided into three groups (8 horses/group) and treated, according a parallel study design, as follows: Group A untreated (control group), Group B received 4 mg/kg of omeprazole, and Group C received 12 mg/kg of omeprazole, both of which were treated orally once a day for 90 days. Blood samples, taken from Group B subjects during the 1st and the 29th day of treatment at pre-established time points, were used to determine the concentrat...
Antimicrobial stewardship in the treatment of equine bacterial infections.
Veterinary journal (London, England : 1997)    November 21, 2016   Volume 219 4-5 doi: 10.1016/j.tvjl.2016.11.009
Johns I.No abstract available
Repeated injectable anesthesia in six horses for cobalt therapy.
Veterinary anaesthesia and analgesia    November 16, 2016   Volume 27, Issue 2 106 doi: 10.1016/S1467-2987(16)31356-3
Matthews NS, Carroll GL, Hartsfield SM, Martinez EA.No abstract available
Changes in the equine EEG during surgery: The effect of an intravenous infusion of thiopentone.
Veterinary anaesthesia and analgesia    November 16, 2016   Volume 27, Issue 2 113 doi: 10.1046/j.1467-2995.2000.00018.x
Murrell JC, Johnson CB, Waterman-Pearson AE, Jones A.No abstract available
Comparative evaluation of the analgesic effects of epidural morphine, alfentanil, butorphanol, tramadol and U50488H in horses.
Veterinary anaesthesia and analgesia    November 16, 2016   Volume 27, Issue 2 109 doi: 10.1016/S1467-2987(16)31364-2
Natalini CC, Robinson EP.No abstract available
Pharmacokinetics and toxicity of intravenously administered lithium chloride in horses.
Veterinary anaesthesia and analgesia    November 16, 2016   Volume 27, Issue 2 108 doi: 10.1016/S1467-2987(16)31361-7
Hatfield C, McDonell W, Black W.No abstract available
Cardiovascular effects of desflurane in horses.
Veterinary anaesthesia and analgesia    November 16, 2016   Volume 27, Issue 2 106-107 doi: 10.1016/S1467-2987(16)31358-7
Steffey EP, Woliner MJ.No abstract available
Effects of thiopentone on the equine electroencephalogram during anaesthesia with halothane in oxygen.
Veterinary anaesthesia and analgesia    November 16, 2016   Volume 27, Issue 2 82-88 doi: 10.1046/j.1467-2995.2000.00022.x
Johnson CB, Bloomfield M, Taylor PM.To characterise the effects of thiopentone on the equine electroencephalogram during halothane anaesthesia. Methods: Prospective controlled study. Methods: Eight healthy Welsh mountain pony geldings between 5 and 9 years old and weighing between 270 and 330 kg (mean 301 kg). Methods: Anaesthesia was induced with thiopentone and maintained using halothane in oxygen. End tidal halothane was maintained above 0.75 and below 0.85%. EEG was recorded continuously and a binaural broad band click stimulus was provided throughout the experiment at 6.1224 Hz. An infusion of 500 mg thiopentone was given o...
The isoflurane sparing effect of a medetomidine constant rate infusion in horses.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 30, Issue 2 92-93 doi: 10.1046/j.1467-2995.2003.00132_8.x
Neges K, Bettschart-Wolfensberger R, Müller J, Fürst A, Kästner S.No abstract available
Clinical responses and plasma drug concentrations associated with different infusions of xylazine and ketamine in horses.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 27, Issue 1 58-59 doi: 10.1046/j.1467-2995.2000.00008-9.x
Mama KR, Wagner AE, Steffey EP, Kollias-Baker C, Hellyer PW, Golden AE, Brevard LF.No abstract available
Changes in the EEG in horses during surgery: the effect of an intravenous infusion of alfentanil.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 29, Issue 2 90 doi: 10.1046/j.1467-2995.2002.00701.x
Murrell JC, White KL, Johnson CB, Taylor PM, Waterman-Pearson AE.No abstract available
Ketamine-guaiphenesin infusion to supplement halothane anaesthesia in horses.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 27, Issue 1 54-55 doi: 10.1046/j.1467-2995.2000.00008-1.x
Spadavecchia C, Stucki F, Schatzmann U.No abstract available
Comparison of romifidine-ketamine-midazolam and romifidine-tiletamine-zolazepam total intravenous anaesthesia (TIVA) for clinical anaesthesia in horses.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 29, Issue 2 92-93 doi: 10.1046/j.1467-2995.2002.00705.x
Bouts T, Gasthuys F, Vlaminck L, Van Branteghem L.No abstract available
Quantification of dose-dependent respiratory depression in isoflurane-anesthetized horses.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 29, Issue 2 104 doi: 10.1046/j.1467-2995.2002.00078_17.x
Brosnan RJ, Imai A, Steffey EP.No abstract available
Epidural administration of tiletamine-zolazepam in horses.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 29, Issue 2 109 doi: 10.1046/j.1467-2995.2002.00078_29.x
Natalini CC, Alves S, Robinson EP.No abstract available
Detomidine reduces isoflurane anesthetic requirement (MAC) in horses.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 29, Issue 4 223-227 doi: 10.1046/j.1467-2995.2002.00107.x
Steffey EP, Pascoe PJ.To quantitate the dose- and time-related magnitude of the anesthetic sparing effect of, and selected physiological responses to detomidine during isoflurane anesthesia in horses. Methods: Randomized cross-over study. Methods: Three, healthy, young adult horses weighing 485 ± 14 kg. Methods: Horses were anesthetized on two occasions to determine the minimum alveolar concentration (MAC) of isoflurane in O and then to measure the anesthetic sparing effect (time-related MAC reduction) following IV detomidine (0.03 and 0.06 mg kg). Selected common measures of cardiopulmonary function, blood glucos...
Effects of guaiphenesin on the equine electroencephalogram during anaesthesia with halothane in oxygen.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 27, Issue 1 6-12 doi: 10.1046/j.1467-2995.2000.00011.x
Johnson CB, Bloomfield M, Taylor PM.To identify and characterize the effects of guaiphenesin (GGE) on the electroencephalogram during halothane anaesthesia. Methods: Prospective controlled study. Methods: Eight healthy Welsh mountain pony geldings between 5 and 9 years old and weighing between 270 and 330 kg (mean 301 kg). Methods: Anaesthesia was induced with thiopentone and maintained using halothane in oxygen. End tidal halothane was maintained above 0.75 and below 0.85%. The EEG was recorded continuously and a binaural broad band click stimulus was provided throughout the experiment at 6.1224 Hz. An infusion of 1500 mg GGE w...
Serum concentrations and effects of detomidine delivered orally to horses in three different mediums.
Veterinary anaesthesia and analgesia    November 15, 2016   Volume 29, Issue 4 219-222 doi: 10.1046/j.1467-2995.2002.00096.x
Ramsay EC, Geiser D, Carter W, Tobin T.To compare the effect of orally delivered detomidine on head posture when administered alone or in combination with two different food items, and to determine the serum concentrations of detomidine after oral delivery. Methods: Prospective randomized experimental study. Methods: Fifteen adult grade mares weighing 328-537 kg. Methods: The horses were randomly assigned to one of the three treatment groups (five horses each). The groups were given detomidine (0.06 mg kg): alone; mixed with 3 mL of an apple sauce and gum mixture; or mixed with 3 mL molasses. Head droop, measured before treatment a...
Control of methylxanthines in the competition horse: pharmacokinetic/pharmacodynamic studies on caffeine, theobromine and theophylline for the assessment of irrelevant concentrations.
Drug testing and analysis    November 4, 2016   Volume 9, Issue 9 1372-1384 doi: 10.1002/dta.2097
Machnik M, Kaiser S, Koppe S, Kietzmann M, Schenk I, Düe M, Thevis M, Schänzer W, Toutain PL.Methylxanthines positives in competition samples have challenged doping control laboratories and racing jurisdictions since methylxanthines are naturally occurring prohibited substances and often constituents of feed. For theobromine, an international threshold (renamed in International Residue Limit, IRL) of 2 µg/mL in urine has been established. On the basis of the data presented herein, a threshold or rather an IRL for theobromine in plasma of 0.3 µg/mL was proposed and was thereupon approved by the International Federation of Horseracing Authorities (IFHA). Official recommendations f...
Quantification of dimethylsulfoxide (DMSO) in equine plasma and urine using HILIC-MS/MS.
Drug testing and analysis    November 4, 2016   Volume 9, Issue 6 935-941 doi: 10.1002/dta.2098
Salomonsson ML, Bondesson U, Hedeland M.This paper describes quantitative methods for the determination of dimethylsulfoxide (DMSO) in equine plasma and urine based on simple precipitation and dilution followed by hydrophilic interaction liquid chromatography coupled to tandem mass spectrometry (HILIC-MS/MS). DMSO is a polar solvent with analgesic and anti-inflammatory properties. Its pharmacological features make it prohibited in horse racing. However, since DMSO is naturally present in the horses' environment, international threshold values have been implemented for plasma and urine (1 and 15 µg/mL, respectively). Previously pr...
The stability and microbial contamination of bupivacaine, lidocaine and mepivacaine used for lameness diagnostics in horses.
Veterinary journal (London, England : 1997)    October 25, 2016   Volume 218 7-12 doi: 10.1016/j.tvjl.2016.10.008
Adler DM, Cornett C, Damborg P, Verwilghen DR.Local anaesthetics (LAs) are frequently used for diagnostic procedures in equine veterinary practice. The objective of this study was to investigate the physico-chemical stability and bacterial contamination of bupivacaine, lidocaine and mepivacaine used for lameness examinations in horses. The LAs were stored in 12 different groups at different temperatures (-18 °C to 70 °C), light intensities and in common veterinary field conditions for up to 16 months. The pH, presence of bacterial contamination and concentrations of LAs and methylparaben (a preservative present in lidocaine) were de...
Selective inhibition of Sarcocystis neurona calcium-dependent protein kinase 1 for equine protozoal myeloencephalitis therapy.
International journal for parasitology    October 8, 2016   Volume 46, Issue 13-14 871-880 doi: 10.1016/j.ijpara.2016.08.003
Ojo KK, Dangoudoubiyam S, Verma SK, Scheele S, DeRocher AE, Yeargan M, Choi R, Smith TR, Rivas KL, Hulverson MA, Barrett LK, Fan E, Maly DJ....Sarcocystis neurona is the most frequent cause of equine protozoal myeloencephalitis, a debilitating neurological disease of horses that can be difficult to treat. We identified SnCDPK1, the S. neurona homologue of calcium-dependent protein kinase 1 (CDPK1), a validated drug target in Toxoplasma gondii. SnCDPK1 shares the glycine "gatekeeper" residue of the well-characterized T. gondii enzyme, which allows the latter to be targeted by bumped kinase inhibitors. This study presents detailed molecular and phenotypic evidence that SnCDPK1 can be targeted for rational drug development. Recombinant ...
Evaluation of an oral direct factor Xa inhibitor anticoagulant in healthy adult horses.
Journal of veterinary emergency and critical care (San Antonio, Tex. : 2001)    October 6, 2016   Volume 27, Issue 1 82-88 doi: 10.1111/vec.12540
Rodríguez-Pozo ML, Armengou L, Monreal L, Viu J, Cesarini C, Jose-Cunilleras E.To assess whether an oral direct factor Xa inhibitor (DiXaI) anticoagulant drug used at the low end of the recommended dose in people achieves presumed prophylactic plasma concentrations and does not induce bleeding in horses. Methods: Experimental study. Methods: Field study. Methods: Ten healthy adult horses. Methods: A DiXaI was administered at a dose of 0.125 mg/kg every 24 h orally for 4 days. Following a wash-out period of 2 weeks, 8 of 10 horses received daily subcutaneous doses of a low molecular weight heparin (dalteparin) for 4 consecutive days at 50 IU/kg. In both trials, antifactor...
A survey of UK prescribers’ experience of, and opinions on, anthelmintic prescribing practices for livestock and equines.
Preventive veterinary medicine    October 5, 2016   Volume 134 69-81 doi: 10.1016/j.prevetmed.2016.10.001
Easton S, Pinchbeck GL, Bartley DJ, Hotchkiss E, Hodgkinson JE, Matthews JB.The aim of this study was to determine practices, attitudes and experiences of UK prescribers of anthelmintics for horses and livestock. A questionnaire was sent by direct email to groups licenced to prescribe these medicines. These were veterinarians, Suitably Qualified Persons (SQPs, registered with the Animal Medicines Training Regulatory Authority) and veterinary pharmacists. The survey was also advertised through social media. It comprised questions relating to demographics, training experiences, current prescribing practices, as well as personal opinions on anthelmintic selection, diagno...
Use of large-scale veterinary data for the investigation of antimicrobial prescribing practices in equine medicine.
Equine veterinary journal    October 5, 2016   Volume 49, Issue 4 425-432 doi: 10.1111/evj.12638
Welsh CE, Parkin TDH, Marshall JF.As antimicrobial resistant bacterial strains continue to emerge and spread in human and animal populations, understanding prescription practices is key in benchmarking current performance and setting goals. Antimicrobial prescription (AP) in companion veterinary species is widespread, but is neither monitored nor restricted in the USA and Canada. The veterinary use of certain antimicrobial classes is discouraged in some countries, in the hope of preserving efficacy for serious human infections. Objective: The aim of this study was to ascertain the rate of prescription of a number of 'reserved'...
Confirmatory analysis of etanercept in equine plasma by LC-MS for doping control.
Drug testing and analysis    October 5, 2016   Volume 9, Issue 9 1421-1431 doi: 10.1002/dta.2091
Guan F, Robinson MA, Soma LR.Etanercept is a protein-based medication for the treatment of human patients with rheumatoid arthritis and other autoimmune-based diseases; its pharmacological action is to inhibit and antagonize tumour necrosis factor alpha. Etanercept was rumoured to be used in horse racing in North America. To detect such use, the aim of this study was to develop a liquid chromatography-mass spectrometry (LC-MS) method for confirmation of etanercept in equine plasma. Etanercept was extracted from plasma by anti-human IgG antibody linked to magnetic beads. The analyte was reduced and alkylated, and then dige...
The effects of dose and diet on the pharmacodynamics of omeprazole in the horse.
Equine veterinary journal    October 3, 2016   Volume 49, Issue 4 525-531 doi: 10.1111/evj.12630
Sykes BW, Underwood C, Greer R, McGowan CM, Mills PC.Conflicting data are presented in the current literature regarding the efficacy of omeprazole for suppressing gastric acidity in the horse. Objective: The objective of this study was to investigate the duration of intraday acid suppression achieved with two doses of omeprazole under two different dietary conditions. Methods: A four-way crossover design. Methods: Six adult Thoroughbred horses instrumented with percutaneous gastrotomy tubes were used. Intragastric pH was measured for continuous 23 h periods (08.00-07.00 h) for six consecutive days (Days 0-5). Baseline data was recorded on Day 0 ...
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