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Topic:Drug
The topic of drugs and horses encompasses the study of various pharmacological agents used in equine medicine for therapeutic purposes. This includes the administration of medications for pain management, disease treatment, and performance enhancement. The pharmacokinetics and pharmacodynamics of drugs in horses are key areas of research, as they determine the absorption, distribution, metabolism, and excretion of these substances. Additionally, the topic covers the detection and regulation of substances in competitive equestrian sports to ensure fair play and animal welfare. This page compiles peer-reviewed research studies and scholarly articles that explore the effects, safety, and regulatory aspects of drug use in equine health and performance.
The Early Ophthalmic Effects of Vatinoxan in Healthy Detomidine-Sedated Horses. To evaluate the short-term ophthalmic effects of vatinoxan, a peripherally selective alpha2-adrenoceptor antagonist, in detomidine-sedated horses. Methods: Seven healthy horses without ophthalmic disease in a randomized, masked, two-period crossover study design, with a ≥ 7-day rest period. Methods: After a bilateral palpebral block (lidocaine 40 mg) and baseline data collection, horses received intravenous detomidine (20 μg/kg [DET]) or DET with vatinoxan (200 μg/kg [DET-VAT]). Intraocular pressure (IOP) was measured from the left eye while tear production (Schirmer tear test -1; ...
Oclacitinib for Controlling Pruritus and Associated Skin Lesions in 16 Horses With Allergic Dermatitis. Oclacitinib is a Janus kinase inhibitor approved for the treatment of pruritus associated with allergic dermatitis in dogs and may be effective in horses. Objective: To evaluate the efficacy of oclacitinib in reducing pruritus and skin lesions in horses with allergic dermatitis. Methods: Sixteen horses aged ≥ 18 months. Methods: Horses received oclacitinib at 0.25 mg/kg orally once daily for 21 days. Changes in haematological and biochemical parameters were measured on Day (D)0 and D21. The owners were instructed to evaluate the horses using the pruritus Visual Analog Scale (PVAS) on...
A Genetic Algorithm-Based Approach for Quantitative Prediction of Drug-Drug Interactions Caused by Cytochrome P450 3A Inhibition or Induction in Horses. A genetic algorithm (GA)-based approach was designed to predict drug-drug interactions (DDIs) triggered by cytochrome P450 3A (CYP3A) inhibition or induction in horses. Area under the concentration-time curve ratios (AUCRs), obtained from published in vivo DDI studies in horses, were used to compute the following parameters: (1) the contribution ratio (CR), i.e., the fraction of the substrate dose metabolized via the CYP3A pathway, and (2) the interacting drug's inhibitory potency or inducing efficacy (IR or IC, respectively). AUCRs for 9 substrates, 12 inhibitors, and 1 inducer of equine C...
Pharmacokinetics of Diclazuril in the Plasma and Cerebrospinal Fluid of Healthy Adult Horses After a Single Oral Dose Administered as a Pelleted Topdressing. Equine protozoal myeloencephalitis can cause acute infections with rapid onset of neurologic signs, necessitating immediate empiric therapy with antiprotozoal medication. The objective of the study was to identify when concentrations of diclazuril reached the MIC of Sarcocystis neurona in CSF (1 ng/mL) of healthy adult horses after a single oral dose. Six healthy adult horses were used. Blood and CSF were collected from indwelling intravenous jugular catheters and intrathecal catheters in the lumbosacral space prior to drug administration and then at 1-, 4-, 8-, 12-, 16-, 24-, 48-, 72-, 96-,...
Pharmacokinetics of Ertugliflozin, a Sodium-Glucose Co-Transporter-2 Inhibitor (SGLT2i) in Horses After Enteral Administration. Ertugliflozin is a sodium-glucose co-transporter-2 inhibitor that has demonstrated promise as a treatment for hyperinsulinaemia in horses. Despite the frequent use of ertugliflozin in equine clinical practice, the pharmacokinetics of this drug in horses has not been established. The aim of the present study was to determine the pharmacokinetics of one supratherapeutic dose (0.25 mg/kg) of ertugliflozin in eight horses. Horses were defined as being healthy by physical examination, haematological, blood biochemical and oral sugar test (OST) results. Plasma concentrations of ertugliflozin were qu...
Clodronate disodium reduced TRAP5b independent of affecting other systemic biomarkers of bone resorption or formation in yearling, exercising Quarter Horses. Clodronate disodium (CD), a bisphosphonate, modulates bone metabolism. Though extra-label use in juvenile horses is anecdotally reported, impacts on skeletal development are unknown. The objective was to determine the effects of CD on systemic markers of bone turnover in yearling horses undergoing exercise, hypothesizing that biomarkers of bone resorption would decrease while biomarkers of bone formation would not change, and that repeat CD treatments would have greater effect. To test this, 32 yearling Quarter Horses were used in a 168-d trial. Horses were stratified by age (500 ± 13 d),...
Effects of vatinoxan in horses sedated with detomidine and butorphanol for gastroscopy: a randomized clinical study. The peripheral alpha2-adrenoceptor antagonist vatinoxan attenuated the side effects of alpha2-adrenergic sedatives in experimental studies in horses. This clinical study investigated the effects of vatinoxan in horses sedated for gastroscopy with detomidine and butorphanol. Client-owned horses were randomly allocated to receive one of the following two intravenous treatments: detomidine hydrochloride (HCl) (12μg/kg) + butorphanol tartrate (12μg/kg) (DB; n=11) or DB + vatinoxan HCl (200μg/kg) (DBV; n=11). Borborygmi score and heart rate were recorded by auscultation. Sedation level was evalu...
Erythrocyte sequestration of metformin in horses: impact on matrix-specific pharmacokinetics and detection windows. BACKGROUND: Metformin is used for the treatment of type 2 diabetes and is one of the most prescribed medications in human medicine. It is less commonly prescribed in equine medicine, and its use is tightly regulated in several performance horse disciplines. In horseracing, it is considered a banned substance. A previous pharmacokinetic study of metformin in horses demonstrated a prolonged, unpredictable elimination phase. In the current study it was hypothesized that this was due to sequestration of metformin in a “deep” compartment, specifically red blood cells. This could result in pharm...
Atropine induces narrowing of the superior and inferior iridocorneal angle and ciliary cleft in normal horse eyes. To investigate the effects of atropine on the iridocorneal angle (ICA) and ciliary cleft (CC) of normal equine eyes using ultrasound biomicroscopy (UBM). Unassigned: 12 normal adult horses underwent measurement of intraocular pressure (IOP), vertical and horizontal pupil diameter, and UBM of the superior, temporal, inferior, and nasal ICA/CC in both eyes. Measurements were repeated 2 hours following ophthalmic atropine 1% solution application. Measurements of the ICA and CC, including pectinate ligament distance (PLD), CC length (CCL), height of opening distance (HOD), CC area (CCA), and pecti...
Behavioral and cardiorespiratory effects of a medetomidine and tramadol combination in horses. The use of combinations of sedative and analgesic drugs during standing procedures in horses is necessary to provide reliable sedation with minimal ataxia and reduced responses to surgical or other stimuli in horses. Objective: This study assessed the behavioral and cardiorespiratory effects of medetomidine (M) administered with and without tramadol (T) in horses. Methods: Eight horses were sedated intravenously with M (5 µg/kg) alone or with T (2 mg/kg) in a arandomized, blind, two-way crossover trial. Behavioral responses, including head height above the ground (HHAG), postural instability ...
Periovulatory administration of therapeutic and supratherapeutic doses of firocoxib does not impair induced ovulation or follicular dynamics in mares treated with a GnRH analogue. To evaluate the effects of therapeutic and supratherapeutic periovulatory doses of firocoxib on ovulation and follicular dynamics in mares. Methods: Seventy cycling mares were randomly assigned to receive firocoxib at 0.1 mg/kg (n = 27), firocoxib at 0.3 mg/kg (n = 22), or no treatment (control; n = 21). Treatments were initiated on Day 0, defined as the day of ovulation induction with a GnRH analogue administered intramuscularly, with firocoxib administered intravenously on Day 0 and Day 1 (24 h apart). Follicular diameter and ovulation timing were assessed by transrectal ultrasonography. Res...
Pharmacokinetics of 2 mg/kg Bupivacaine in a Rectus Abdominis Sheath Block in Horses. Administering large volumes of bupivacaine in the rectus abdominis sheath (RAS) block in horses could cause local anesthetic toxicity. This study aimed to evaluate the pharmacokinetics of 2 mg/kg bupivacaine in RAS blocks and the associated toxicity risk. Six healthy adult horses were sedated with xylazine and received an ultrasound-guided bilateral 2-point RAS block. Plasma samples were collected at baseline and from 5 min to 24 h after the block and analyzed using liquid chromatography-tandem mass spectrometry. A noncompartmental analysis was performed to determine the maximum concentr...
Nitric oxide and its role in the management of hypoxaemia in the anaesthetised horse-a narrative review. To outline historical aspects of nitric oxide, including its discovery and biological effects, to describe the current use of inhaled nitric oxide (iNO) in human healthcare, and to review the available evidence on the use of pulsed iNO (PiNO) for the management of hypoxaemia in anaesthetised horses. Methods: Google Scholar and PubMed databases were searched using the search terms nitric oxide, PiNO, environment, discovery, acute respiratory distress syndrome, COVID-19, SARS-CoV-2, horse, pony, hypoxaemia, and anaesthesia. Conclusions: Inhaled NO is licensed in the management of hypoxic respira...
Pharmacokinetics of Intramuscularly Administered Ketamine at Subanaesthetic Dosage in Horses. Subanaesthetic doses of ketamine (0.5 mg kg) provide analgesia in several species, but there is limited information on the pharmacokinetics and clinical effects of intramuscularly administered ketamine in horses. This study investigated the pharmacokinetics of ketamine and norketamine, and evaluated clinical effects, ataxia, and vital parameters, following intramuscular and intravenous administration of 0.5 mg kg ketamine in nine healthy horses, using a randomized two-period crossover design with a 1-week washout period. Plasma concentrations were analyzed using Ultra-High Performance ...
Synthesis and Characterization of Deuterated Detomidine for Use in Equine Medication Regulation. Detomidine, 5-[(2,3-dimethylphenyl)methyl]-1H-imidazole, is a tranquilizer/sedative/analgesic widely used in equine medicine and regulated by several different analyte concentrations of detomidine and its hydroxydetomidine and carboxydetomidine metabolites in plasma and urine. Accurate regulatory quantitation of detomidine at low picogram/mL concentrations requires the availability of a stable isotope internal standard of detomidine; however, to the best of our knowledge, no certified deuterated internal standard of detomidine is commercially available and its synthesis has not been reported. ...
Supramolecular Solvent Extraction for Doping Control Analysis of Prohibited Substances in Horse Urine. Despite the recent success in introducing supramolecular solvents (SUPRAS)-based extraction to drug analysis, its application and robustness in day-to-day regular urine testing have yet to be demonstrated. Moreover, the applicability of SUPRAS in equine doping control testing remains unexplored. In this work, we have successfully developed for the first time a simple, rapid, inexpensive, and environmentally friendly SUPRAS extraction method for analyzing 76 prohibited substances of different classes (selective androgen receptor modulators, hypoxia-inducible factor prolyl hydroxylase inhibitors...
A randomized, masked, crossover, clinical trial of the efficacy and safety of nebulized albuterol sulfate and dexamethasone sodium phosphate in asthmatic horses. Nebulization of injectable dexamethasone sodium phosphate (DSP; 0.01 mg/kg) to horses with severe equine asthma (SEA) was previously found to be ineffective. Horses with SEA have marked bronchoconstriction that decreases peripheral lung deposition of nebulized drugs. Administration of a bronchodilator immediately before nebulizing dexamethasone may improve efficacy. Objective: Evaluate the therapeutic effects and optimal dose of nebulized DSP after nebulized albuterol in horses with SEA. Methods: Seven horses with SEA from a research herd. Methods: In this masked randomized crossover trial, h...
Long term safety and efficacy of a functionalized nanogel with endothelin-1 and bradykinin receptor antagonist peptides for treatment of osteoarthritis of the metacarpophalangeal and distal interphalangeal joints in horses: a descriptive clinical pilot study. Intra-articular drug delivery systems (DDS) are emerging as promising therapies for osteoarthritis (OA), yet their efficacy in spontaneous clinical cases remains largely untested. This uncontrolled, descriptive pilot study was designed to provide a proof of concept for the feasibility, safety, and preliminary clinical effects of intra-articular administration in sport horses with naturally occurring OA. The study involved a peptide-functionalized nanogel composed of chitosan and hyaluronic acid, delivering endothelin type A (BQ-123) and bradykinin B1 (R-954) receptor antagonists, which have pr...
Pharmacokinetic analysis and steady-state predictions of different preparations of metronidazole administered per rectum in adult horses. Manipulation of forms of rectally administered metronidazole to improve bioavailability in horses has not been reported. Objective: Evaluate the pharmacokinetics of 3 rectal metronidazole preparations compared to nasogastric (NG) administration. Methods: Seven healthy horses. Methods: Phase 1A was a randomized, 3-way crossover, single-dose pharmacokinetic study, and Phases 1B and 2 were non-randomized, single-dose follow-up studies. Metronidazole (20 mg/kg) was administered NG and rectally in water (RW20), as a rectal gel (RG), and in dimethyl sulfoxide (DMSO). Metronidazole (80 mg/kg) was a...
Pharmacokinetics of Topical Administration of Altrenogest in Mares and Implications for Human Health. Altrenogest is a synthetic progestogen widely used in equine reproductive management. Adverse effects to altrenogest have been reported in people with cutaneous exposure reported as the highest exposure pathway. Despite these reports, there has been no quantitative research to determine the capacity for altrenogest to be absorbed through skin. This study aimed to determine if cutaneous application of oral altrenogest results in systemic absorption in mares and to evaluate the influence of application site. A randomized, two-period, two-treatment crossover study was undertaken in eight mares. M...
Repeated intravenous dexamethasone administration causes transient changes in leukocyte parameters in healthy warmblood horses. To determine the effect of repeated IV administration of dexamethasone (0.06 mg/kg, q 24 h, twice) on WBC parameters in healthy adult horses. Unassigned: This prospective, longitudinal study was conducted from October 7 through November 5, 2024. Five warmblood mares received an IV dexamethasone sodium phosphate injection (DMI) at 0 and 24 hours and an IV injection with 0.9% sodium chloride solution at 48 and 72 hours. Blood samples were collected at 0, 6, 12, 24, 30, 36, 48, 72, 96, and 168 hours, and WBC parameters were evaluated using linear mixed-effects models. Unassigned: Leukocyte count,...
Antibiofilm and resistance-modulating properties of tt-farnesol against Streptococcus equi subsp. equi and zooepidemicus. The aim of this study was to investigate the antibacterial, antibiofilm and modulating activities of trans-trans-farnesol (tt-farnesol) on two strains of Streptococcus equi subsp. equi and two strains of S. equi subsp. zooepidemicus, pathogenic or commensal bacteria of horses. Tt-farnesol showed bactericidal activity against all tested strains, with a minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) between 8 and 4 μg/mL. The sesquiterpene caused significant damage to the bacterial membrane, and its antibacterial activity did not appear to depend on oxidat...
Pharmacokinetics and Anti-Inflammatory Effects of Intramuscular Betamethasone in Exercised Thoroughbred Horses. The pharmacokinetics and pharmacodynamics of betamethasone following intra-articular administration to horses have been described; however, studies characterizing intramuscular administration are lacking. Twenty-four horses received an intramuscular dose of 12 mg betamethasone sodium phosphate/betamethasone acetate. Blood and urine were collected at post administration for up to 408 h. Concentrations of betamethasone were determined using LC-MS/MS and pharmacokinetic parameters determined using a Population PK three-compartment model. The duration of pharmacodynamic effects was assessed by...
Pharmacopuncture with low-dose dexmedetomidine and saline aquapuncture at acupoint Governing Vessel 24 provides sedation in healthy adult horses. To evaluate sedation in horses following pharmacopuncture with dexmedetomidine at acupoint Governing Vessel 24 (GV-24) compared to aquapuncture at GV-24 or an equivalent dose of dexmedetomidine administered via IV or SC routes. Unassigned: 10 adult mares received 4 treatments in a blinded, randomized, crossover design: (1) dexmedetomidine administered at GV-24 (DexmedGV24; 1 μg/kg); (2) saline administered at GV-24 (SalineGV24; 1.5 mL); (3) dexmedetomidine administered SC on the lateral neck (DexmedSC; 1 μg/kg); or (4) dexmedetomidine administered IV (DexmedIV; 1 μg/kg). Sedation scores (fa...
Exposure to Subcutaneously Administered Butorphanol in Horses Pre-Treated With Detomidine or Detomidine-Vatinoxan. The aim of the study was to determine the exposure to subcutaneously administered butorphanol in horses pre-treated with intravenous (IV) detomidine, with or without vatinoxan, a peripherally selective alpha-adrenoceptor antagonist. Five healthy, adult horses received three IV treatments 7 days apart, in a randomized, cross-over design: detomidine 20 μg/kg (DET-B), detomidine 20 μg/kg with vatinoxan 200 μg/kg (DETVAT-B) and saline (S-B), all followed by 0.1 mg/kg of butorphanol administered subcutaneously 30 min later. Venous samples were collected between 10 and 270 min after...
Tafenoquine succinate inhibits the growth of the equine piroplasmosis hemoparasites Theileria equi and Babesia caballi. Equine piroplasmosis (EP) is a tick-borne disease of equids caused by the intraerythrocytic apicomplexan parasites Theileria equi, Babesia caballi and the recently identified Theileria haneyi. Acute cases can be severe, with anemia, jaundice, abortion or sudden death. Survivors remain lifelong carriers, serving as reservoirs for tick-borne and iatrogenic transmission. No vaccines are currently available, and control strategies rely heavily on accurate diagnostics and chemotherapeutic intervention. Imidocarb dipropionate (ID) is the current standard of care for both acute treatment and radical ...
Pharmacokinetics of Intragastric Ursodeoxycholic Acid and Its Impact on Bile Acid Profiles in Horses. Ursodeoxycholic acid (UDCA), a secondary bile acid (BA) with therapeutic applications, is standard therapy for cholestatic hepatopathies in humans. In recent years, its use has been increasingly explored in equine medicine for similar indications. Pharmacokinetic data for UDCA in horses are currently lacking. This study aimed to describe the pharmacokinetic parameters following a single intragastric administration of 15 mg/kg in nine healthy, fasted horses and to characterize the changes in their BA profiles. Plasma concentrations of UDCA were measured at specific time points using liquid ch...
Detection and Longitudinal Monitoring of Cyclosporine in Horse Plasma and Urine After Ocular Implant Administration. This paper describes the detection and longitudinal monitoring of cyclosporine in plasma and urine after subconjunctival implant administration in a horse. Sensitive liquid chromatography tandem mass spectroscopy (LC-MS/MS) methods for detecting cyclosporine in horse plasma and urine have been developed and validated, with estimated limits of detection down to 1 pg/mL in both matrices. The developed methods enabled longitudinal monitoring of cyclosporine levels in blood and urine samples collected over 6 months from a horse that had received an ocular cyclosporine implant.
Vonoprazan pharmacokinetics and effects on gastric pH following administration to fed and fasted horses. Current treatment options for equine gastric ulcer syndrome (EGUS), such as omeprazole-a proton pump inhibitor (PPI)-have notable limitations, including the need for administration on an empty stomach. Potassium-competitive acid blockers (P-CABs), such as vonoprazan, are a newer class of acid suppressants that offer several advantages over PPIs in humans and may provide similar benefits in horses. Objective: To describe the pharmacokinetics and effect of a single oral dose of vonoprazan on intragastric pH in horses. We hypothesised that vonoprazan would follow linear kinetics across the doses ...
