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Topic:Yohimbine

Yohimbine is an alkaloid derived from the bark of the Pausinystalia johimbe tree and is used in veterinary medicine for horses primarily as a reversal agent for sedatives like xylazine and detomidine. It functions by antagonizing alpha-2 adrenergic receptors, thereby counteracting the sedative effects and facilitating recovery from anesthesia. Yohimbine's pharmacokinetics, dosage, and effects on equine physiology are subjects of ongoing research. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacological properties, clinical applications, and safety considerations of yohimbine in equine veterinary practice.
Effects of three antagonists on selected pharmacodynamic effects of sublingually administered detomidine in the horse.
Veterinary anaesthesia and analgesia    October 17, 2013   Volume 41, Issue 1 36-47 doi: 10.1111/vaa.12081
Knych HK, Stanley SD.To describe the effects of alpha2 -adrenergic receptor antagonists on the pharmacodynamics of sublingual (SL) detomidine in the horse. Methods: Randomized crossover design. Methods: Nine healthy adult horses with an average age of 7.6 ± 6.5 years. Methods: Four treatment groups were studied: 1) 0.04 mg kg(-1) detomidine SL; 2) 0.04 mg kg(-1) detomidine SL followed 1 hour later by 0.075 mg kg(-1) yohimbine intravenously (IV); 3) 0.04 mg kg(-1) detomidine SL followed 1 hour later by 4 mg kg(-1) tolazoline IV; and 4) 0.04 mg kg(-1) detomidine SL followed 1 hour later by 0.12 m...
Effect of yohimbine on detomidine induced changes in behavior, cardiac and blood parameters in the horse.
Veterinary anaesthesia and analgesia    October 6, 2012   Volume 39, Issue 6 574-583 doi: 10.1111/j.1467-2995.2012.00776.x
DiMaio Knych HK, Covarrubias V, Steffey EP.To describe selected pharmacodynamic effects of detomidine and yohimbine when administered alone and in sequence. Methods: Randomized crossover design. Methods: Nine healthy adult horses aged 9 ± 4 years and weighing 561 ± 56 kg. Methods: Three dose regimens were employed in the current study. 1) 0.03 mg kg(-1) detomidine IV, 2) 0.2 mg kg(-1) yohimbine IV and 3) 0.03 mg kg(-1) detomidine IV followed 15 minutes later by 0.2 mg kg(-1) yohimbine IV. Each horse received all three treatments with a minimum of 1 week between treatments. Blood samples were obtained and plasma analyzed for detomidin...
The effects of yohimbine on the pharmacokinetic parameters of detomidine in the horse.
Veterinary anaesthesia and analgesia    March 8, 2012   Volume 39, Issue 3 221-229 doi: 10.1111/j.1467-2995.2011.00690.x
Knych HK, Steffey EP, Stanley SD.To describe the pharmacokinetics of detomidine and yohimbine when administered in combination. Methods: Randomized crossover design. Methods: Nine healthy adult horses aged 9 ± 4 years and weighing of 561 ± 56 kg. Methods: Three dose regimens were employed in the current study. 1) 0.03 mg kg(-1) detomidine IV (D), 2) 0.2 mg kg(-1) yohimbine IV (Y) and 3) 0.03 mg kg(-1) detomidine IV followed 15 minutes later by 0.2 mg kg(-1) yohimbine IV (DY). Each horse received all three dose regimens with a minimum of 1 week in between subsequent regimens. Blood samples were obtained and plasma analyzed f...
Pharmacokinetics of yohimbine following intravenous administration to horses.
Journal of veterinary pharmacology and therapeutics    January 12, 2011   Volume 34, Issue 1 58-63 doi: 10.1111/j.1365-2885.2010.01194.x
Dimaio Knych HK, Steffey EP, Deuel JL, Shepard RA, Stanley SD.Yohimbine is an alpha 2 adrenergic receptor antagonist used most commonly in veterinary medicine to reverse the effects of the alpha 2 receptor agonists, xylazine and detomidine. Most notably, yohimbine has been shown to counteract the CNS depressant effects of alpha 2 receptor agonists in a number of species. The recent identification of a yohimbine positive urine sample collected from a horse racing in California has led to the investigation of the pharmacokinetics of this compound. Eight healthy adult horses received a single intravenous dose of 0.12 mg/kg yohimbine. Blood samples were co...
Pharmacokinetics and pharmacodynamics of three intravenous doses of yohimbine in the horse.
Journal of veterinary pharmacology and therapeutics    September 10, 2010   Volume 34, Issue 4 359-366 doi: 10.1111/j.1365-2885.2010.01234.x
Dimaio Knych HK, Steffey EP, Stanley SD.Yohimbine is an alpha 2 adrenergic receptor antagonist, which has been shown to counteract the CNS depressant effects of alpha 2 receptor agonists in a number of species. Recently, our laboratory identified yohimbine in the absence of detectable concentrations of an alpha 2 agonist in a regulatory sample collected from a horse racing in California. This coupled with anecdotal reports of CNS stimulation and documented reports of cardiovascular changes when administered in conjunction with an agonist led us to investigate the pharmacokinetics and pharmacodynamics of yohimbine when administered a...
Yohimbine ameliorates the effects of endotoxin on gastric emptying of the liquid marker acetaminophen in horses.
Canadian journal of veterinary research = Revue canadienne de recherche veterinaire    October 21, 2000   Volume 64, Issue 4 208-211 
Meisler SD, Doherty TJ, Andrews FM, Osborne D, Frazier DL.The effect of yohimbine pretreatment on gastric emptying of a liquid marker in horses was evaluated by measuring serum concentrations of acetaminophen. Gastric emptying was determined in normal, fasted horses, in horses given endotoxin (E. coli 055 B5; 0.2 microg/kg) intravenously, and in horses given yohimbine (0.25 mg/kg, IV, over 30 minutes) plus endotoxin. Acetaminophen (20 mg/kg) was given by stomach tube 15 minutes after the endotoxin infusion. Blood samples for acetaminophen analysis were collected, and time to reach the peak serum concentration (Tmax), the maximum serum concentration (...
Effects of intravenously administered yohimbine on antinociceptive, cardiorespiratory, and postural changes induced by epidural administration of detomidine hydrochloride solution to healthy mares.
American journal of veterinary research    May 3, 2000   Volume 60, Issue 10 1262-1270 
Skarda RT, Muir WW.To determine effects of i.v. administered yohimbine on perineal analgesia, cardiovascular and respiratory activity, and head and pelvic limb position in healthy mares following epidural administration of detomidine hydrochloride solution. Methods: 8 healthy mares. Methods: Each mare received detomidine hydrochloride (0.06 mg/kg of body weight), administered in the caudal epidural space, followed 61 minutes later by yohimbine (0.05 mg/kg; test) or sterile saline (0.9% NaCl) solution (control), administered i.v., in a randomized, crossover study design with > or = 2 weeks between treatments. ...
Acetaminophen as a marker of gastric emptying in ponies.
Equine veterinary journal    August 15, 1998   Volume 30, Issue 4 349-351 doi: 10.1111/j.2042-3306.1998.tb04109.x
Doherty TJ, Andrews FM, Provenza MK, Frazier DL.Gastric emptying was evaluated in ponies using the acetaminophen (AP) method. Fifteen minutes after i.v. administration of metoclopramide, erythromycin, yohimbine, atropine or saline, the ponies were given AP by stomach tube. Blood samples for AP analysis were collected at baseline and 15, 30, 45, 60, 75, 90, 105 and 120 min after AP administration. Time to reach peak serum concentration (Tmax), maximum serum concentration (Cmax) and area under the AP serum concentration vs. time curve (AUC) were determined for each treatment group. In the control group, Tmax was 31 min and this decreased sign...
Use of yohimbine to reverse prolonged effects of xylazine hydrochloride in a horse being treated with chloramphenicol.
Journal of the American Veterinary Medical Association    June 15, 1997   Volume 210, Issue 12 1771-1773 
Grubb TL, Muir WW, Bertone AL, Beluche LA, Garcia-Calderon M.A 1-year-old Standardbred gelding had received xylazine hydrochloride (0.75 to 1.00 mg/kg [0.34 to 0.45 mg/lb] of body weight, IV) during 2 surgeries for debridement of a wound. The horse was given chloramphenicol (55 mg/kg [25 mg/lb], PO, q 6 h) for 5 days, and was anesthetized a third time with xylazine (0.75 mg/kg, IM). Five hours after administration of xylazine, the horse remained markedly sedated and had clinical signs of gaseous distention of the large bowel (bloat) requiring trocharization. Administration of yohimbine (0.03 mg/kg [0.01 mg/lb], i.v.) eliminated signs of sedation within ...
Prejunctional alpha 2-adrenoceptors inhibit acetylcholine release from cholinergic nerves in equine airways.
The American journal of physiology    December 1, 1993   Volume 265, Issue 6 Pt 1 L565-L570 doi: 10.1152/ajplung.1993.265.6.L565
Yu M, Wang Z, Robinson NE.To determine the presence and function of alpha 2-adrenoceptors on cholinergic nerves innervating horse airway smooth muscle, the effects of some alpha 2-adrenoceptor agents on contractions of and acetylcholine (ACh) release from equine airway smooth muscle preparations were studied. Muscle contractions were elicited by either electrical field stimulation (EFS) or exogenous ACh. ACh release was induced by EFS and measured by high-pressure liquid chromatography and electrochemical detection. The alpha 2-adrenoceptor agonists clonidine (10(-7) to 10(-5) M) and UK-14,304 (10(-8) to 10(-6) M) conc...
Influence of yohimbine and tolazoline on the cardiovascular, respiratory, and sedative effects of xylazine in the horse.
Journal of veterinary pharmacology and therapeutics    September 1, 1993   Volume 16, Issue 3 350-358 doi: 10.1111/j.1365-2885.1993.tb00182.x
Kollias-Baker CA, Court MH, Williams LL.To determine the effects of yohimbine and tolazoline on the cardiovascular, respiratory and sedative effects of xylazine, four horses were sedated with xylazine and treated with either yohimbine, tolazoline or saline. Xylazine was administered as an intravenous (i.v.) bolus (1.0 mg/kg) followed by a continuous infusion at the rate of 12 micrograms/kg/min. Heart rate, respiratory rate, mean arterial pressure, arterial blood gases, and the chin-to-floor distance were recorded throughout the experiment. After 60 min, either yohimbine or tolazoline was administered i.v. in incremental doses until ...
Blockade of endotoxin-induced cecal hypoperfusion and ileus with an alpha 2 antagonist in horses.
American journal of veterinary research    April 1, 1993   Volume 54, Issue 4 586-590 
Eades SC, Moore JN.Stimulation of alpha 2 adrenergic receptors inhibits colonic motility and may constrict some peripheral vascular beds. Endotoxemia elicits release of sympathetic neurotransmitters and increases sympathetic nerve activity, which may result in stimulation of alpha 2 adrenergic receptors. The objective of this study was to determine whether blockade of alpha 2 adrenergic receptors would restore cecal motility and blood flow during endotoxemia in horses. Strain-gauge force transducers and ultrasonic flow probes were used to measure cecal and colonic mechanical activity and lateral cecal arterial b...
Comparative pharmacokinetics of yohimbine in steers, horses and dogs. Jernigan AD, Wilson RC, Booth NH, Hatch RC, Akbari A.In steers, horses and dogs, the comparative pharmacokinetics of yohimbine were determined using model-independent analysis. The intravenous dose of yohimbine was 0.25 mg/kg of body weight in steers, 0.075 or 0.15 mg/kg in horses, and 0.4 mg/kg in dogs. The mean residence time (+/- SD) of yohimbine was 86.7 +/- 46.2 min in steers, 106.2 +/- 72.1 to 118.7 +/- 35.0 min in horses, and 163.6 +/- 49.7 min in dogs. The mean apparent volume of distribution of yohimbine at steady state was 4.9 +/- 1.4 L/kg for steers, 2.7 +/- 1.0 to 4.6 +/- 1.9 L/kg for horses, and 4.5 +/- 1.8 L/kg for dogs. The total ...
Pharmacokinetics of xylazine in ponies: influence of yohimbine.
Archives internationales de pharmacodynamie et de therapie    September 1, 1987   Volume 289, Issue 1 5-10 
Dyer DC, Hsu WH, Lloyd WE.Twenty healthy ponies were given i.v. 1.1 mg/kg of xylazine from 2 manufacturers and the pharmacokinetic parameters calculated from the disposition curves. The disposition curves for the 2 commercial preparations were not different. Yohimbine, an antagonist of the pharmacologic effects produced by xylazine, did not alter the disposition of xylazine in the plasma. A single i.v. bolus of xylazine was completely described in 17 of 20 animals by the biexponential equation: Cp = 1.30e(-0.3955t) + 0.58e(-0.033t) where Cp represents the concentration of xylazine in the plasma at time t (min). The t1/...
Rapid reversible immobilization of feral stallions using etorphine hydrochloride, xylazine hydrochloride and atropine sulfate.
Journal of wildlife diseases    July 1, 1987   Volume 23, Issue 3 471-478 doi: 10.7589/0090-3558-23.3.471
Plotka ED, Seal US, Eagle TC, Asa CS, Tester JR, Siniff DB.Forty-eight newly captured free-ranging feral stallions (Equus caballus) from two different locations and six captive stallions were immobilized using combinations of etorphine hydrochloride, xylazine hydrochloride and atropine sulfate with or without acepromazine. Six animals were immobilized twice, 1 mo apart. The drugs were administered either intramuscularly (n = 13) or intravenously (n = 44). Mean immobilization time (+/- SE) after intravenous (i.v.) injection of etorphine, xylazine and atropine was 55 +/- 4 sec (range 20 to 185 sec) compared to 708 +/- 131 sec (range 390 to 1,140 sec) fo...
Effect of yohimbine on xylazine-induced hypoinsulinemia and hyperglycemia in mares.
American journal of veterinary research    April 1, 1987   Volume 48, Issue 4 676-678 
Greene SA, Thurmon JC, Tranquilli WJ, Benson GJ.Serum insulin and plasma glucose concentrations were determined in 8 mares. Four IV treatments were studied: xylazine (1.1 mg/kg of body weight); yohimbine (0.125 mg/kg); yohimbine (0.125 mg/kg) followed 5 minutes later by xylazine (1.1 mg/kg); and 5 ml of isotonic saline solution as a control. Blood samples were collected before (time 0) and at 5, 15, 30, 60, 120, and 180 minutes after drug administration. Serum insulin concentration decreased and plasma glucose concentration increased in mares given xylazine. Plasma glucose concentration was unchanged in control mares and in mares given yohi...
Antagonism of xylazine-pentobarbital anesthesia by yohimbine in ponies.
American journal of veterinary research    June 1, 1985   Volume 46, Issue 6 1276-1281 
McGruder JP, Hsu WH.Effects of yohimbine on xylazine-pentobarbital anesthesia were evaluated in ponies. Five minutes after the IV injection of xylazine (1.1 mg/kg of body weight), pentobarbital sodium (12.7 mg/kg, IV) and additional xylazine (2.2 mg/kg, IM) were given and produced anesthesia in 12 ponies for 64.0 +/- 16.4 minutes (mean +/- SD) as well as immobilization for 89.8 +/- 34.2 minutes. Eleven ponies were given yohimbine (0.1 mg/kg, IV) 50 minutes after pentobarbital dosing. In these 11 ponies, durations of anesthesia and immobilization were shorter, 52.0 +/- 1.4 and 65.5 +/- 14.8 minutes, respectively. ...
Trials of serotonin, substance P and alpha 2-adrenergic receptor effects on the equine large colon.
The Cornell veterinarian    April 1, 1985   Volume 75, Issue 2 319-323 
Sellers AF, Lowe JE, Cummings JF.Some support for both serotonin and substance P as biotransmitters in the equine large colon is presented. Close arterial injections of small quantities of each of these were effective, respectively, in stimulating marked increases in coordinated pressure peaks in the vicinity of the pelvic flexure, with modest (serotonin) or marked (substance P) increase in colon artery blood flow. Both the acaricide, amitraz, and the tranquilizer xylazine appeared to act on the equine large colon via yohimbine-sensitive alpha 2-adrenergic receptors.
Antagonism of xylazine and ketamine anesthesia by 4-aminopyridine and yohimbine in geldings.
American journal of veterinary research    May 1, 1984   Volume 45, Issue 5 875-879 
Kitzman JV, Wilson RC, Hatch RC, Booth NH.Thirty-six fasted, mixed horse breed geldings (6 groups of 6 animals each) were anesthetized with xylazine and ketamine, and when maximally sedated, were given 1 of the following antagonists: saline solution, 4-aminopyridine (4-AP), small-dose yohimbine, large-dose yohimbine, 4-AP plus low-dose yohimbine, or 4-AP plus high-dose yohimbine. Measured data included mean standing time (MST), heart rate, respiratory rate, rectal temperature, and mean total recovery time ( MTRT ). Emergence phenomena were also observed and recorded as smooth, fairly smooth, fairly rough, or rough. Groups given 4-AP a...