Topic:Clenbuterol
Clenbuterol is a beta-2 adrenergic agonist commonly used in veterinary medicine to manage respiratory conditions in horses due to its bronchodilator properties. It facilitates breathing by relaxing the muscles in the airways, thereby improving airflow to the lungs. Clenbuterol is also known to have anabolic effects, which has led to its misuse in some contexts for enhancing muscle mass and performance in horses. The use of clenbuterol is regulated in competitive equestrian sports due to its potential impact on performance. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacology, therapeutic applications, regulatory considerations, and potential side effects of clenbuterol in equine practice.
Comparison of time-resolved fluoroimmunoassay and immunoenzymometric assay for clenbuterol. A time-resolved fluoroimmunoassay (TR-FIA) for the direct determination of clenbuterol residues in horse urine using a highly specific monoclonal antibody has been compared with an immunoenzymometric assay (IEMA). The sensitivity of both methods was 10 pg; the calibration curve was linear between 10 and 10(5) pg for the TR-FIA and between 10 and 10(4) pg for the IEMA.
Detection of clenbuterol (Ventipulmin) in the horse. An enzyme linked immunosorbent assay (ELISA) was developed to detect the beta 2-agonist clenbuterol in equine blood and urine. The antiserum was raised in rabbits, employing clenbuterol-diazo-BSA as antigen. Clenbuterol-diazo-horseradish peroxidase served as enzyme conjugate. The concentration of clenbuterol to decrease tracer binding by 50% (IC50 value) was found to be 27.50 +/- 4.20 pg/well (1.37 ng/ml). The antibody cross-reacted with salbutamol (30%), terbutaline (14%) and cimaterol (1%). Horse serum was used directly to screen for clenbuterol, while urine was employed diluted. Positive sc...
Clinical efficacy and safety of clenbuterol HCl when administered to effect in horses with chronic obstructive pulmonary disease (COPD). A field study of 239 horses was conducted to determine the efficacy and safety of clenbuterol HCl, a beta 2-adrenergic bronchodilator, when administered incrementally to effect in the treatment of chronic obstructive pulmonary disease (COPD). The severity of COPD (heaves) and response to treatment was determined by clinical evaluation; an overall 'heaveiness rating' (OHR) was assigned at each observation. The horses were treated orally b.i.d. with clenbuterol (as Ventipulmin Syrup), beginning with the lowest dosage of 0.8 micrograms/kg. On day 10 of treatment at the effective dose (0.8, 1.6, 2...
Review of 115 cases of colic in the pregnant mare. The medical records of pregnant mares over a 3-year period were reviewed. In all cases persistent pain or progressive abdominal distension were the main reason for referral. The overall survival rate for the 115 mares treated for colic was 73.9% (85 cases). The abortion rate was 20.5% in surgical patients (34 cases), 40% (5 cases) for mares with uterine torsions and 10.8% (46 cases) after medical treatment. The total abortion rate was 16.4%. Clinical evidence of endotoxaemia was, except for 1 mare, present in all the aborting mares after colic treatment. Anaesthesia did not appear to be a prob...
Effects of clenbuterol hydrochloride on pulmonary gas exchange and hemodynamics in anesthetized horses. We evaluated the effects of clenbuterol HCl (0.8 micrograms/kg, of body weight, IV), a beta 2 agonist, on ventilation-perfusion matching and hemodynamic variables in anesthetized (by IV route), laterally recumbent horses. The multiple inert gas elimination technique was used to assess pulmonary gas exchange. Clenbuterol HCl induced a decrease in arterial oxygen tension (from 57.0 +/- 1.8 to 49.3 +/- 1.2 mm of Hg; mean +/- SEM) as a result of increased shunt fraction (from 6.6 +/- 2.1 to 14.4 +/- 3.1%) and ventilation to regions with high ventilation-perfusion ratios. In contrast, no changes in...
Evaluation of clinical signs of disease, bronchoalveolar and tracheal wash analysis, and arterial blood gas tensions in 13 horses with chronic obstructive pulmonary disease treated with prednisone, methyl sulfonmethane, and clenbuterol hydrochloride. We evaluated the efficacy of 3 treatments for chronic obstructive pulmonary disease in horses: prednisone (400 mg/horse, PO, daily; n = 7), methyl sulfonmethane (10 g/horse, PO, q 12 h; n = 6), and clenbuterol hydrochloride (0.4 mg/horse, PO, q 12 h; n = 7). A fourth group acted as controls (n = 6) and was not treated. The treatment period lasted 10 days. Each horse was a member of 2 different groups for 10 days, separated by an 18-day interval of no treatment. All horses were housed together in an outdoor pen without bedding. Horses were fed alfalfa/grass hay mix ad libitum from a large feede...
Respiratory mucociliary clearance in the horse in health and disease, and its pharmaceutical modification. The structure and possible functions of respiratory secretions are reviewed. In the equine, goblet (mucus producing) cells are the main source but little information is available on the volume or composition of equine respiratory secretions. Airway mucus has complex and incompletely understood physical characteristics which can be partially assessed by a wide range of in vitro and biological techniques. The complex relationship between mucus structure and its propulsion by the airway cilia are discussed, both in health and with pulmonary disease. Mucokinesis in the horse has been assessed visu...
Respiratory mechanics of horses during stepwise treadmill exercise tests, and the effect of clenbuterol pretreatment on them. Normal Standardbred horses were given an incremental exercise test on a horizontal treadmill to evaluate the influence of exercise on gas exchange, resistance, dynamic compliance and inertance of the respiratory system. The exercise test consisted of 2 min exercise steps at each of the following speeds: 2.4 m/sec (walk), 4.5 m/sec (slow trot), 7.0 m/sec (fast trot) and 10 m/sec (gallop). At rest and after 1 min of exercise at each step, airflow, tidal volume, respiratory frequency, pharyngeal, mid-oesophageal and transdiaphragmatic pressures and arterial blood gas tensions were measured. The s...
Clenbuterol plasma concentrations after repeated oral administration and its effects on cardio-respiratory and blood lactate responses to exercise in healthy Standardbred horses. To evaluate the effects of clenbuterol on cardio-respiratory parameters and blood lactate relation to exercise tolerance, experimental horses performed standardized exercise tests on a high-speed treadmill before and after administration of the drug. Clenbuterol was administered in feed to six healthy Standardbreds at a dose rate of 0.8 micrograms/kg b.wt twice daily for 5.5 days. Each horse was tested twice, without and with a respiratory mask, during two consecutive days. One week elapsed between the baseline tests without drug and the tests with clenbuterol treatment (each horse served as i...
Relaxant effects of theophylline and clenbuterol on tracheal smooth muscle from horse and rat in vitro. A comparison between the relaxant effects of clenbuterol and theophylline on horse tracheal smooth muscle has been made in vitro. Rat tracheal smooth muscle was also investigated as a reference. The tracheal preparations were initially contracted with carbachol since the smooth muscle did not spontaneously develop tone. The response of the carbachol-contracted preparations to theophylline was the same in the two species. The response to clenbuterol varied. In only five out of eleven horses were the tracheal smooth muscles sensitive to clenbuterol (mean pD2 = 7.92 M). In the remaining six horse...
Beta-adrenergic receptor activity in ponies with recurrent obstructive pulmonary disease. Pulmonary function measurements were made in control ponies and in ponies with recurrent obstructive pulmonary disease (principals) during clinical remission and during an attack of acute airway obstruction. The ponies were given beta-adrenergic antagonists and agonists to determine the role of beta receptors in recurrent obstructive pulmonary disease, and to determine the subtypes of beta receptors mediating bronchodilation in ponies. Aerosol administration of the beta antagonists, propranolol (beta 1 and beta 2), atenolol (beta 1), and butoxamine (beta 2) decreased dynamic compliance (Cdyn) ...
Screening and confirmatory analysis of beta-agonists, beta-antagonists and their metabolites in horse urine by capillary gas chromatography-mass spectrometry. A method for the screening and confirmatory analysis of beta-agonists and -antagonists in equine urine is described. Following initial enzymic hydrolysis, the basic drugs and metabolites are extracted using Clean Screen DAU or Bond Elut Certify cartridges, and analysed as their trimethylsilyl ether or 2-(dimethyl) silamorpholine derivatives by capillary gas chromatography-mass spectrometry. The method proved to be very sensitive and selective for basic drugs. After administration of therapeutic doses of propranolol, metoprolol, timolol, isoxsuprine and clenbuterol to thoroughbred horses, the p...
Action of sympathomimetic drugs on the bronchial circulation of the horse. In the quietly standing horse I.V. administration of adrenaline decreased, and of dobutamine increased, bronchial artery flow. These changes paralleled changes in arterial pressure. With phenylephrine and noradrenaline bronchial artery flow decreased while arterial pressure increased, indicating active vasoconstriction in the bronchial circulation. With clenbuterol an increase in bronchial artery flow was accompanied by a decrease in systemic blood pressure, indicating bronchial arterial vasodilatation. We conclude that alpha-constrictor and beta 2-dilator receptors are present in the bronchia...
Treatment of low arterial oxygen tension in anesthetized horses with clenbuterol. Clenbuterol (0.8 microgram/kg intravenously) was administered to 10 anesthetized horses with an abnormally low PaO2 (less than 90 mm Hg) despite controlled ventilation with an oxygen-rich gas mixture. Results were compared with those from 10 controls to which no clenbuterol was given and in which conventional methods to increase PaO2 were ongoing. Horses treated with clenbuterol had higher PaO2 values for at least 90 minutes. Clenbuterol was associated with increased heart rate and profuse sweating. Clenbuterol can be administered intravenously to increase the PaO2 of mechanically ventilated h...
Some physiological and pharmacological factors affecting uterine motility as measured by electromyography in the mare. Two intact and 2 ovariectomized mares aged 3-16 years had bipolar electrodes implanted in the myometrium to measure electromyographic (emg) activity during normal and exogenously simulated (with oestrogen and progesterone) cyclical activity (anoestrus, transition, oestrus and dioestrus). Oxytocin, cloprostenol, propantheline bromide and clenbuterol were administered during each cycle stage. In 1 mare, emg activity was recorded during natural breeding (4 times) and through the first 20 days of pregnancy. Simultaneous intrauterine pressure recordings (IUP) using an open tipped catheter system we...
Effect of clenbuterol on arterial oxygen tension in the anaesthetised horse. In horses in dorsal recumbency, spontaneously breathing oxygen, with halothane at a constant end-tidal concentration, the arterial oxygen tension (PO2) increased from 9.9 +/- 0.3 SEM kPa to 21.7 +/- 4.0 kPa with 0.8 micrograms kg-1 clenbuterol and to 29.1 +/- 3.8 kPa with 2.4 micrograms kg-1 clenbuterol. In horses initially in dorsal recumbency then turned to sternal recumbency the PaO2 rose to 54.0 +/- 3.0 kPa, but this rise was unaffected by clenbuterol administration. The response in dorsal recumbency was consistent with clenbuterol counteracting the factor postulated to direct the pulmonar...
The influence of furosemide on plasma elimination and urinary excretion of drugs in standardbred horses. A study of the effects of intravenous administration of either 150 mg or 250 mg of furosemide to standardbred mares pre-treated with other drugs was undertaken to determine whether a unique pattern of drug elimination into urine and from plasma for each compound occurred. Furosemide significantly reduced the plasma concentrations of codeine compared to control 2-6 h after furosemide administration. In contrast, the plasma concentrations of theophylline, phenylbutazone, pentazocine, guaifenesin and flunixin were not markedly altered by furosemide. In the case of acepromazine, clenbuterol and fe...
Radioimmunoassay for albuterol using a monoclonal antibody: application for direct quantification in horse urine. A monoclonal antibody was synthesized in mouse against the O-(3-carboxypropionyl) derivative of albuterol linked to bovine serum albumin. Isotyping of this material revealed the IgG1 class characterized by an affinity constant of 1.03 nM-1 and a density of sites of 0.55 nM. This antibody was found specific as its cross-reactivity to structurally related molecules was less than 1% except for clenbuterol (75%). A radioimmunoassay was set up with culture supernatant (final dilution 1/1000) and [3H] albuterol. The calibration curve was characterized by a maximum binding of 28%, an ED50 of 1.15 pmo...
Influence of clenbuterol on mucociliary transport in healthy horses and horses with chronic obstructive pulmonary disease. The mucociliary tracheal transport rate and clearance index were measured in 16 healthy horses and 16 horses suffering from chronic obstructive pulmonary disease. A marker, Indian ink in syrup, was placed in the mucus layer of the interior wall of the trachea, just in front of the carina, and its displacement was measured after 30 and 60 minutes. The same procedure was repeated 30 minutes after the intravenous administration of 0.8 microgram clenbuterol/kg bodyweight. In the diseased horses the mucociliary transport rate was significantly lower than in the healthy horses. After clenbuterol adm...
Determination of clenbuterol and mabuterol in equine plasma by ion-pair liquid chromatography with electrochemical detection. Chromatographic and electrochemical characteristics. A method for the routine determination of the beta-adrenergic drugs clenbuterol and mabuterol in equine plasma has been developed. The drugs were isolated from alkalinized plasma by liquid-liquid extraction. The organic phase was evaporated to dryness and the residue was dissolved in the mobile phase prior to injection. The recoveries were 98% and 95% for clenbuterol and mabuterol, respectively. The drugs were separated by reversed-phase high-performance liquid chromatography and quantitated by a use of a coulometric detector set at +0.75 V vs. the internal reference electrode. The influence o...
[The use of a beta 2-mimetic agent (clenbuterol) in equine pregnancy disorders and obstetrics]. A clinical study about the effects of a beta 2-mimetic agent (Clenbuterol) in mares with pregnancy disorders or disorders during the periparturient period (n = 34) is reported. In general, a single dose of 0.3 mg Clenbuterol given i.v. induces sufficient tocolysis. Subsequent doses or follow-up treatment depend upon individual development during dystocia, indication of treatment and clinical preparturient status (dorsoflexio uteri ante partum, abortus imminens, preparturient labor pains).
Effect of clenbuterol on histamine-induced airway obstruction in ponies. We determined the effect of IV administered beta 2-adrenergic receptor agonist clenbuterol on pulmonary function and on the response to histamine in 12 healthy ponies. Measurements were made at base line and after saline solution or clenbuterol was administered IV at a dosage of 0.2, 0.8, or 1.6 micrograms/kg. The dosage of clenbuterol used in each study was unknown to the investigators until all the data had been analyzed. Intravenous administration of saline solution or clenbuterol did not alter base-line pulmonary function significantly. Aerosol histamine administration significantly decrea...
Phalangeal and navicular bone hypoplasia and hoof malformation in the hind limbs of a foal. Anatomical anomalies in the hind feet of a seven month old Appaloosa foal were identified and investigated through the use of gross anatomical dissection, radiography and angiography. Abnormalities were restricted to the distal aspect of both hind legs, the right hind leg being more severely affected. Anatomically the right foot resembled that of an equine fetus of approximately 120 days gestational age. Disruption of vascular perfusion to hoof structures was evident in both hind legs and was related to areas of abnormal bone conformation as well as to areas of abnormal ossification and calcif...
Effects of clenbuterol hydrochloride on certain respiratory and cardiovascular parameters in horses performing treadmill exercise. Five standardbred geldings received intravenous clenbuterol hydrochloride and saline in a crossover experiment to evaluate the effects of clenbuterol on certain cardiorespiratory parameters during and after treadmill exercise. The exercise test consisted of four steps. Step 1 at a speed of 76 m per minute, step 2 at 129 m per minute, step 3 at 190 m per minute and step 4 at 236 m per minute. The duration of each step was two minutes, except step 4 which was four minutes. The treadmill was set at a grade of 19 per cent. Before exercise, 30 minutes after clenbuterol or saline administration, art...
Cardiopulmonary effects of clenbuterol in the horse. Clenbuterol, a bronchospasmolytic agent (beta 2 agonist) was studied in terms of its hemodynamic and airflow response in eight, healthy horses. Four animals were instrumented to record intrapleural pressure and air flow, these were used to compute pulmonary resistance, peak flow rates, and tidal volumes. Four animals were instrumented to record pulmonary arterial pressure, carotid arterial pressure, cardiac output, and arterial gas tensions. After control values were recorded, clenbuterol (0.8 microgram/kg) was intravenously administered to each horse in each experiment group. Following clenbu...