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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.
Doping control analysis of antipsychotics and other prohibited substances in equine plasma by liquid chromatography/tandem mass spectrometry.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences    May 1, 2020   Volume 1147 122132 doi: 10.1016/j.jchromb.2020.122132
Wong ASY, Choi TLS, Kwok KY, Wong JKY, Wan TSM, Ho ENM.Antipsychotics are banned substances and considered by the Fédération Equestrian Internationale (FEI) to have no legitimate use in equine medicine and/or have a high potential for abuse. These substances are also prohibited in horseracing according to Article 6 of the International Agreement on Breeding, Racing and Wagering (published by the International Federation of Horseracing Authorities). Over the years, antipsychotics have been abused or misused in equestrian sports and horseracing. A recent review of literature shows that there is yet a comprehensive screening method for antipsychoti...
[New drugs for horses and production animals in 2019].
Tierarztliche Praxis. Ausgabe G, Grosstiere/Nutztiere    April 23, 2020   Volume 48, Issue 2 118-123 doi: 10.1055/a-1122-7849
Emmerich IU.In 2019, one novel pharmaceutical agent for horses or food-producing animals was released on the German market: An injection suspension for horses containing chondrogenic-induced equine allogeneic peripheral blood-derived mesenchymal stem cells as the active ingredient (ArtiCell Forte) is now available. Two established veterinary active pharmaceutical ingredients became accessible for additional species: a salicylanilide anthelmintic oxyclozanide (Distocur) for the treatment and control of fascioliasis in sheep as well as a type-I synthetic pyrethroid permethrin (Z-Itch), which now has additio...
Metabolism, pharmacokinetics and selected pharmacodynamic effects of codeine following a single oral administration to horses.
Veterinary anaesthesia and analgesia    April 23, 2020   Volume 47, Issue 5 694-704 doi: 10.1016/j.vaa.2020.04.004
Gretler SR, Finno CJ, McKemie DS, Kass PH, Knych HK.To describe the pharmacokinetics and selected pharmacodynamic variables of codeine and its metabolites in Thoroughbred horses following a single oral administration. Methods: Prospective experimental study. Methods: A total of 12 Thoroughbred horses, nine geldings and three mares, aged 4-8 years. Methods: Horses were administered codeine (0.6 mg kg) orally and blood was collected before administration and at various times until 120 hours post administration. Plasma and urine samples were collected and analyzed for codeine and its metabolites by liquid chromatography-mass spectrometry, and plas...
Investigation of plasma concentrations of paracetamol, metacetamol, and orthocetamol in Japanese racehorses using liquid chromatography-electrospray ionisation-tandem mass spectrometry.
Drug testing and analysis    April 1, 2020   Volume 12, Issue 7 929-937 doi: 10.1002/dta.2792
Ishii H, Obara T, Kijima-Suda I.Paracetamol is used widely as an over-the-counter analgesic and antipyretic medication for humans, but not for Japanese racehorses. Paracetamol can be an environmental substance, and is found together with its two isomers, metacetamol and orthocetamol, in equine urine. However, the sources and routes of paracetamol exposure remain unclear. To control the misuse of paracetamol, it is appropriate to establish residue limits for paracetamol to differentiate the administration of paracetamol from its environmental levels. In this study, we developed and validated a quantitative method for paraceta...
Furosemide administration results in a transient alteration in calcium balance in mature horses.
Journal of animal physiology and animal nutrition    March 18, 2020   Volume 104, Issue 3 946-953 doi: 10.1111/jpn.13348
Pritchard A, Nielsen BD, Robison C, Spooner H.Previous research documented that furosemide negatively impacted calcium balance for 3 days but did not determine when calcium balance returned to baseline. This study hypothesized that furosemide's impact on calcium would return to control values before 7 days post-administration. Ten mature geldings were assigned to either control (CON, n = 5) or treatment (FUR, n = 5) for the first of two 8-day total collections in crossover design. Treatment horses received one administration of furosemide (1 mg/kg, IV). A 10% sample of pooled faeces and urine from each day was kept. Calcium concent...
Abundant osteoclasts in the subchondral bone of the juvenile Thoroughbred metacarpus suggest an important role in joint maturation.
Equine veterinary journal    February 21, 2020   Volume 52, Issue 5 733-742 doi: 10.1111/evj.13235
Gilday R, Richard H, Beauchamp G, Fogarty U, Laverty S.The administration of bisphosphonate medications, which target osteoclastic-bone remodelling, to juvenile and adult racehorses is a matter of debate owing to concerns that these molecules remain bound to the bone-mineralised matrix and may interfere with subsequent bone growth, adaptation to exercise and healing of bone microdamage in equine athletes. Osteoclasts participate in endochondral ossification, subchondral bone remodelling and bone repair. There is a knowledge gap on the role of equine osteoclast biology in the growth and maturation of joint surfaces and this information is important...
Pharmacokinetics of multiple doses of chloramphenicol in fed adult horses.
Veterinary journal (London, England : 1997)    February 21, 2020   Volume 257 105446 doi: 10.1016/j.tvjl.2020.105446
Estell KE, Knych HK, Patel T, Edman JM, Magdesian KG.To the authors' knowledge, there have been no studies evaluating the pharmacokinetics of chloramphenicol administered orally to horses at the currently recommended dose of 50 mg/kg PO q6 h for multiple days. The published antimicrobial susceptibility breakpoint is 8.0 ug/mL; it is unknown if this concentration is achievable at the recommended dose rate in horses. The aim of this prospective multi-dose pharmacokinetic study was to perform pharmacokinetic analysis of chloramphenicol after multiple doses. The authors hypothesize that the antimicrobial susceptibility breakpoint will not be reached...
Pharmacokinetics of maropitant citrate after oral administration of multiple doses in adult horses.
Journal of veterinary pharmacology and therapeutics    February 17, 2020   Volume 43, Issue 3 282-287 doi: 10.1111/jvp.12844
Berryhill EH, Knych H, Chigerwe M, Edman J, Magdesian KG.The neurokinin-1 (NK-1) receptor antagonist, maropitant citrate, mitigates nausea and vomiting in dogs and cats. Nausea is poorly understood in horses, and clinical use of NK-1 receptor antagonists has not been reported. This study aimed to determine the pharmacokinetics and safety of maropitant after administration of multiple doses. We hypothesized that maropitant concentrations would be similar at steady state to those reported in dogs, with minimal adverse effects. Maropitant was administered at 4 mg/kg orally, once daily for 5 days in seven adult horses. Serial plasma maropitant concent...
Detection and Pharmacokinetics of Etoricoxib in Thoroughbred Horses.
Journal of equine veterinary science    February 1, 2020   Volume 88 102942 doi: 10.1016/j.jevs.2020.102942
Subhahar MB, Singh J, Albert PH, Kadry AM.Etoricoxib, a selective inhibitor of cyclooxygenase-2, is used in the treatment of many inflammatory diseases and dental pain in humans. The aim of this study was to determine the pharmacokinetics and metabolism of etoricoxib in horses. Six horses weighing an average of 475 ± 25 kg were administered a single oral dose of etoricoxib at 1 mg/kg body weight. The results show that the drug reached a maximum concentration of 505.2 ± 67.8 ng/mL in 48 minutes after administration. The elimination half-life was calculated to be 10.20 ± 1.30 hours. Mass spectrometric analysis confirmed that eto...
Investigation of the metabolism of the selective androgen receptor modulator LGD-4033 in equine urine, plasma and hair following oral administration.
Drug testing and analysis    January 5, 2020   Volume 12, Issue 2 247-260 doi: 10.1002/dta.2719
Cutler C, Viljanto M, Hincks P, Habershon-Butcher J, Muir T, Biddle S.LGD-4033 is one of a number of selective androgen receptor modulators (SARMs) that are being developed by the pharmaceutical industry to provide the therapeutic benefits of anabolic androgenic steroids, without the less desirable side effects. Though not available therapeutically, SARMs are available for purchase online as supplement products. The potential for performance enhancing effects associated with these products makes them a significant concern with regards to doping control in sports. The purpose of this study was to investigate the metabolism of LGD-4033 in the horse following oral ...
Aminorex identified in horse urine following consumption of Barbarea vulgaris; a preliminary report.
Irish veterinary journal    December 23, 2019   Volume 72 15 doi: 10.1186/s13620-019-0153-5
Maylin G, Fenger C, Machin J, Kudrimoti S, Eisenberg R, Green J, Tobin T.Aminorex, (RS)-5- Phenyl-4,5-dihydro-1,3-oxazol-2-amine, is an amphetamine-like anorectic and in the United States a Drug Enforcement Administration [DEA] Schedule 1 controlled substance. Aminorex in horse urine is usually present as a metabolite of Levamisole, an equine anthelmintic and immune stimulant. Recently, Aminorex identifications have been reported in horse urine with no history or evidence of Levamisole administration. Analysis of the urine samples suggested a botanical source, directing attention to the Brassicaceae plant family, with their contained GlucoBarbarin and Barbarin as p...
Efficacy of FDA-Approved Anti-Inflammatory Drugs Against Venezuelan Equine Encephalitis Virus Infection.
Viruses    December 12, 2019   Volume 11, Issue 12 1151 doi: 10.3390/v11121151
Risner K, Ahmed A, Bakovic A, Kortchak S, Bhalla N, Narayanan A.Venezuelan equine encephalitis virus (VEEV) is a category B select agent pathogen that can be aerosolized. Infections in murine models and humans can advance to an encephalitic phenotype which may result in long-term neurological complications or death. No specific FDA-approved treatments or vaccines are available for the treatment or prevention of VEEV infection. Neurotropic viral infections have two damaging components: neuronal death caused by viral replication, and damage from the subsequent inflammatory response. Reducing the level of inflammation may lessen neurological tissue damage tha...
Identification of metabolomic changes in horse plasma after racing by liquid chromatography-high resolution mass spectrometry as a strategy for doping testing.
Journal of equine science    October 2, 2019   Volume 30, Issue 3 55-61 doi: 10.1294/jes.30.55
Ueda T, Tozaki T, Nozawa S, Kinoshita K, Gawahara H.Recently, the illegal use of novel technologies, such as gene and cell therapies, has become a great concern for the horseracing industry. As a potential way to control this, metabolomics approaches that comprehensively analyze metabolites in biological samples have been gaining attention. However, it may be difficult to identify metabolic biomarkers for doping because physiological conditions generally differ between resting and exercise states in horses. To understand the metabolic differences in horse plasma between the resting state at training centres and the sample collection stage after...
Pharmacodynamic Effects of Pioglitazone on High Molecular Weight Adiponectin Concentrations and Insulin Response After Oral Sugar in Equids.
Journal of equine veterinary science    September 24, 2019   Volume 82 102797 doi: 10.1016/j.jevs.2019.102797
Legere RM, Taylor DR, Davis JL, Bello K, Parker C, Judd RL, Wooldridge AA.Chronic insulin dysregulation is challenging to manage with pharmaceuticals in horses. Pioglitazone improves insulin sensitivity in humans, and the pharmacokinetics of pioglitazone have been evaluated in horses. The objectives of this study were to assess the pharmacodynamic effects of oral pioglitazone on morphometric parameters, hepatic enzyme activity and function, adipokines, and enteroinsular response to oral sugar. A prospective pilot study was performed using fifteen adult equids (8 ponies, 7 horses) to evaluate the effects of short-term pioglitazone administration (2 mg/kg PO q 24 hou...
Challenging the international residue limit concept for feed contaminants in equine doping analytics.
The Veterinary record    August 24, 2019   Volume 185, Issue 8 227-229 doi: 10.1136/vr.l5134
Ammer H.No abstract available
Systematic analysis to assess the scientific validity of the international residue limits for caffeine and theophylline in horse-racing.
The Veterinary record    August 13, 2019   Volume 185, Issue 8 230 doi: 10.1136/vr.105404
Hertzsch R, Richter A.Based on their performance-enhancing potential, caffeine and theophylline are prohibited substances in equine sports. Residues in horses can be caused by wilful application or by unintended uptake of contaminated feed. The International Federation of Horseracing Authorities recently introduced international residue limits (IRLs) to facilitate the discrimination between pharmacological relevant and irrelevant concentrations in doping samples. The objective of this study was to investigate the scientific validity of these IRLs. A systematic analysis was performed to assess the IRLs by different ...
Tamoxifen in horses: pharmacokinetics and safety study.
Irish veterinary journal    June 20, 2019   Volume 72 5 doi: 10.1186/s13620-019-0143-7
Gajardo G, López-Muñoz R, Plaza A, Uberti B, Sarmiento J, Morán G, Henríquez C.Tamoxifen (TAM), a selective modulator of estrogen receptors (SERMs) has been recently explored as a therapeutic option for the oral treatment of airway inflammation in the horse. The objective of this work was to establish pharmacokinetic parameters of TAM and its main metabolites in equines, as well as to determine its clinical safety in short-term treatments. Results: We determined TAM and its three main metabolites (4-OH tamoxifen, endoxifen, and N-desmethyl tamoxifen) in plasma after single administration of 0.25 mg/kg in healthy adult horses ( = 12). A maximum concentration of TAM w...
Pharmacokinetics of single doses of maropitant citrate in adult horses.
Journal of veterinary pharmacology and therapeutics    June 12, 2019   Volume 42, Issue 4 487-491 doi: 10.1111/jvp.12768
Berryhill EH, Knych H, Edman JM, Magdesian KG.The neurokinin-1 (NK) receptor antagonist, maropitant citrate, mitigates nausea and vomiting in dogs and cats. Nausea is poorly understood and likely under-recognized in horses. Use of NK-1 receptor antagonists in horses has not been reported. The purpose of this study was to determine the pharmacokinetic profile of maropitant in seven adult horses after single intravenous (IV; 1 mg/kg) and intragastric (IG; 2 mg/kg) doses. A randomized, crossover design was performed. Serial blood samples were collected after dosing; maropitant concentrations were measured using LC-MS/MS. Pharmacokinetic pa...
Tracking main environmental factors masking a minor steroidal doping effect using metabolomic analysis of horse urine by liquid chromatography-high-resolution mass spectrometry.
European journal of mass spectrometry (Chichester, England)    May 18, 2019   Volume 25, Issue 3 339-353 doi: 10.1177/1469066719839034
Stojiljkovic N, Leroux F, Bubanj S, Popot MA, Paris A, Tabet JC, Junot C.There is an urgent need to implement holistic and untargeted doping control protocols with improved discriminatory power, compared to conventional methods that only target doping agents. Metabolomics, which aims to characterize all metabolites present in biological matrices, could fulfill this need. In this context, the aim of this study was to evaluate the impact of environmental factors on the ability to obtain a metabolic signature of stanozolol administration in horse doping situation. Urine samples from 16 horses breeded in two different places were collected over a one-year period, befor...
Pharmacokinetics and safety of repeated oral dosing of acetaminophen in adult horses.
Equine veterinary journal    April 16, 2019   Volume 52, Issue 1 120-125 doi: 10.1111/evj.13112
Mercer MA, McKenzie HC, Davis JL, Wilson KE, Hodgson DR, Cecere TE, McIntosh BJ.There are no published studies on the pharmacokinetics of acetaminophen at the dosage used clinically (20 mg/kg), nor has the safety of multiple doses in horses been investigated. Objective: Define the pharmacokinetic parameters of oral acetaminophen at 20 mg/kg in adult horses as a single dose, and twice daily for 14 days to assess the safety of multiple dosing. Methods: Pharmacokinetic study, multiple dose safety study. Methods: Eight healthy Thoroughbred geldings were given acetaminophen (20 mg/kg; 500 mg tablets) orally as a single dose followed by doses every 12 h for 14 days. Seri...
Simultaneous quantitation of 9 anabolic and natural steroidal hormones in equine urine by UHPLC-MS/MS triple quadrupole.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences    April 2, 2019   Volume 1117 36-40 doi: 10.1016/j.jchromb.2019.04.002
Genangeli M, Caprioli G, Cortese M, Laus F, Petrelli R, Ricciutelli M, Sagratini G, Sartori S, Vittori S.A new fast and easy analytical procedure for the simultaneous detection and quantification of 9 anabolic steroids (deslorelin, dexamethasone sodium phosphate, prednisolone, methylprednisolone, stanozolol, boldenone, nandrolone, dexamethasone isonicotinate and altrenogest) in horse urine for doping control have been developed by using the ultra-high-performance liquid chromatography coupled with tandem mass spectrometry technique (UHPLC-MS/MS). A total amount of 400 μl of sample was evaporated, restored and injected in the UHPLC-MS/MS. The proposed method was fully validated showing a recove...
Pharmacological Regulation in the USA and Pharmacokinetics Parameters of Firocoxib, a Highly Selective Cox-2, by Pain Management in Horses.
Journal of equine veterinary science    February 21, 2019   Volume 77 36-42 doi: 10.1016/j.jevs.2019.02.007
Rangel-Nava A, Ramírez-Uribe JM, Recillas-Morales S, Ibancovichi-Camarillo JA, Venebra-Muñoz A, Sánchez-Aparicio P.The objective of the study was to conduct a review of the pharmacological regulation and pharmacokinetic parameters of firocoxib when administered orally or intravenously in horses. A search for literature was done in SCOPUS and PubMed for studies that had to evaluate the pharmacological regulation as well as the pharmacokinetic parameters of firocoxib when administered in horses. The nonsteroidal anti-inflammatory drugs have analgesic, anti-inflammatory, antipyretics, and antiendotoxic effects. The newly developed is selective to COX2 characterized by less adverse effects in veterinary patien...
Efficacy, chondrotoxicity and plasma concentrations of tramadol following intra-articular administration in horses undergoing arthroscopy: preliminary findings.
The veterinary quarterly    February 19, 2019   Volume 38, Issue 1 129-137 doi: 10.1080/01652176.2018.1546963
Di Salvo A, Chiaradia E, Della Rocca G, Giorgi M, Mancini F, Marenzoni ML, Conti MB, Nannarone S.Intra-articular administration of analgesics is performed to ensure good perioperative pain management avoiding undesirable systemic effects. To evaluate the effect of intra-articular injection of tramadol on postoperative pain after arthroscopy in horses and to determine whether tramadol had a local effect. Before the in vivo study, an in vitro test was performed aiming to evaluate the viability of equine chondrocytes after exposure to various concentrations of tramadol. The concentration identified as most appropriate was used to treat the horses' joints. Twelve horses affected by osteochond...
Pharmacokinetics of meloxicam after oral administration of a granule formulation to healthy horses.
Journal of veterinary internal medicine    February 15, 2019   Volume 33, Issue 2 961-967 doi: 10.1111/jvim.15433
Mendoza FJ, Serrano-Rodriguez JM, Perez-Ecija A.Nonsteroidal anti-inflammatory drugs are administered in horses for several systemic diseases. Selective cyclooxygenase-2 inhibitors are preferred because of lower risk of adverse effects. Several meloxicam formulations have been tested in horses, but a recently marketed granule oral formulation has not been studied. Objective: To characterize the pharmacokinetics of a novel granule meloxicam formulation in fasted and fed horses, and to compare pharmacokinetic features with oral suspension and tablets. Methods: Seven healthy adult horses. Methods: Meloxicam was administered at 0.6 mg/kg in fas...
Retraction Note to: Analysis of loxoprofen in tablets, patches, and equine urine as tert-butyldimethylsilyl derivative by gas chromatography-mass spectrometry.
Archives of pharmacal research    February 2, 2019   Volume 42, Issue 2 191 doi: 10.1007/s12272-019-01109-0
Kim Y, Seo C, Oh S, Kwak J, Jung S, Sin E, Kim H, Ji M, Lee HS, Park HJ, Lee G, Yu J, Kim M, Lee W, Paik MJ.The authors have retracted this article [1] because after publication they became aware that the equine urine samples analysed for loxoprofen in this study were in fact equine plasma samples. Therefore the results and conclusions of this article cannot be relied upon. All authors agree to this retraction.
[Vigilance for veterinary medicinal products: Reports of adverse reactions in the year 2017].
Schweizer Archiv fur Tierheilkunde    January 31, 2019   Volume 161, Issue 2 107-112 doi: 10.17236/sat00197
Müntener C, Kupper J, Naegeli H, Gassner B.A total of 306 reports of adverse reactions to veterinary medicinal products were received during the year 2017 representing an increase of 21% compared to the previous year. The majority of these reports described reactions concerning companion animals (180 dogs and 59 cats) as well as cattle (38 reports) and horses (14 reports). Most of the reported reactions were linked to the use of antiparasitics (158 reports), hormone products (30 reports) and anti-inflammatory products (25 reports). 40 reports were generated from consultations with Tox Info Suisse in Zürich and mainly involved the ex...
Comparative study on the metabolism of the ergot alkaloids ergocristine, ergocryptine, ergotamine, and ergovaline in equine and human S9 fractions and equine liver preparations.
Xenobiotica; the fate of foreign compounds in biological systems    January 9, 2019   Volume 49, Issue 10 1149-1157 doi: 10.1080/00498254.2018.1542187
Rudolph W, Remane D, Wissenbach DK, Peters FT.1. Ergopeptine alkaloids like ergovaline and ergotamine are suspected to be associated with fescue toxicosis and ergotism in horses. Information on the metabolism of ergot alkaloids is scarce, especially in horses, but needed for toxicological analysis of these drugs in urine/feces of affected horses. The aim of this study was to investigate the metabolism of ergovaline, ergotamine, ergocristine, and ergocryptine in horses and comparison to humans. 2. Supernatants of alkaloid incubations with equine and human liver S9 fractions were analyzed by reversed-phase liquid-chromatography coupled to h...
Concentrations of indomethacin and its metabolite desmethylindomethacin in plasma and urine after repeated indomethacin topical application to Thoroughbreds.
Equine veterinary journal    December 19, 2018   Volume 51, Issue 4 506-509 doi: 10.1111/evj.13049
Kusano K, Minamijima Y, Mashita S, Kunii H, Yamashita S, Nagata S.Repeated topical application of indomethacin is common in Japanese racehorses, despite the lack of pharmacokinetic data. Objective: To determine the concentrations of indomethacin and its metabolite, desmethylindomethacin, in plasma and urine of Thoroughbreds topically treated repeatedly with indomethacin. Methods: In vivo experimental. Methods: Seven female Thoroughbreds were topically treated with 50 g of 1% indomethacin cream per horse to the back and hips (500 mg of indomethacin/head/2400 cm , 0.21 g/cm ) for 3 consecutive days. Samples were pretreated by protein precipitation for plas...
Doping control analysis of four JWH-250 metabolites in equine urine by liquid chromatography-tandem mass spectrometry.
Drug testing and analysis    December 9, 2018   Volume 11, Issue 5 649-658 doi: 10.1002/dta.2542
You Y, Proctor RM, Vasilko ED, Robinson MA.JWH-250 is a synthetic cannabinoid. Its use is prohibited in equine sport according to the Association of Racing Commissioners International (ARCI) and the Fédération Équestre Internationale (FEI). A doping control method to confirm the presence of four JWH-250 metabolites (JWH-250 4-OH-pentyl, JWH-250 5-OH-pentyl, JWH-250 5-OH-indole, and JWH-250 N-pentanoic acid) in equine urine was developed and validated. Urine samples were treated with acetonitrile and evaporated to concentrate the analytes prior to the analysis by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The chromat...
Metabolism and elimination of the catechol-o-methyltransferase inhibitor tolcapone in the horse.
Drug testing and analysis    December 3, 2018   Volume 11, Issue 4 578-585 doi: 10.1002/dta.2531
Stanley S, Van den Berg K, Foo HC, Deng D.The metabolism of the masking agent tolcapone in the horse has been investigated. This substance was found to have undergone various chemical transformations that produced a large variety of phase I metabolites, as well as glucuronide and sulfate conjugation. Confirmation of the presence of tolcapone and the 3-O-methylated metabolite in the blood samples collected up to 240 minutes and in urine obtained up to 24 hours, was successfully conducted using both gas chromatography- and liquid chromatography-tandem mass spectrometry techniques. The 3-O-methyl tolcapone is the better marker to use i...
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