1981
DOI: 10.1111/j.1365-2885.1981.tb00715.x
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The pharmacokinetics of xylazine hydrochloride: an interspecific study

Abstract: The pharmacokinetic disposition of xylazine hydrochloride is described after both intravenous and intramuscular injection of a single dose, in four domestic species: horse, cattle, sheep and dog, by an original high performance liquid chromatographic technique. Remarkably small interspecific differences are reported. After intravenous administration, systemic half-life (t1/2 beta) ranged between 22 min (sheep) and 50 min (horse) while the distribution phase is transient with half-life (t1/2 alpha) ranging from… Show more

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Cited by 150 publications
(101 citation statements)
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“…Plasma concentrations in Cases 2 (estimated dosage 3.4 mg/kg IV, 0.99 mg/mL in plasma) and 3 (estimated dosage 3.5 mg/kg IM; 0.24 mg/mL in plasma), both collected 49 min postadministration, indicate an adequate but relatively low IM bioavailability in cetaceans. Plasma concentrations corresponding to sedation and analgesia in other animals (Garcia-Villar et al 1981;Rector et al 1996;Lizarraga and Beths 2012) were achieved or exceeded in Cases 2 and 3, but not in Case 1. Oral bioavailability of xylazine is poor because of first pass metabolism, however, it may be directly absorbed from the oral and pharyngeal mucosa (Pawson 2008), making assessment of relay toxicity risk difficult.…”
Section: Discussionmentioning
confidence: 99%
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“…Plasma concentrations in Cases 2 (estimated dosage 3.4 mg/kg IV, 0.99 mg/mL in plasma) and 3 (estimated dosage 3.5 mg/kg IM; 0.24 mg/mL in plasma), both collected 49 min postadministration, indicate an adequate but relatively low IM bioavailability in cetaceans. Plasma concentrations corresponding to sedation and analgesia in other animals (Garcia-Villar et al 1981;Rector et al 1996;Lizarraga and Beths 2012) were achieved or exceeded in Cases 2 and 3, but not in Case 1. Oral bioavailability of xylazine is poor because of first pass metabolism, however, it may be directly absorbed from the oral and pharyngeal mucosa (Pawson 2008), making assessment of relay toxicity risk difficult.…”
Section: Discussionmentioning
confidence: 99%
“…Xylazine is dosed at 0.2-1 mg/kg IM as a preanesthetic in dogs, at 0.1-0.3 mg/kg IM in cattle, and at 1-10 mg/kg IM in birds (Plumb 2011). Bioavailability following IM injection is variable: 52-90% in dogs and 40-48% in horses (Garcia-Villar et al 1981). Plasma concentrations in Cases 2 (estimated dosage 3.4 mg/kg IV, 0.99 mg/mL in plasma) and 3 (estimated dosage 3.5 mg/kg IM; 0.24 mg/mL in plasma), both collected 49 min postadministration, indicate an adequate but relatively low IM bioavailability in cetaceans.…”
Section: Discussionmentioning
confidence: 99%
“…A range of xylazine doses alters respiratory mechanics and gas exchange, causing tachypnea, increased airway pressures and respiratory resistance, decreased lung compliance, pulmonary edema, and hypoxemia with or without hypercapnia (5), produced by vasoconstriction, which follows peripheral α 2 Breceptor stimulation caused by high plasma α 2 -agonist concentrations (6). In sheep, it has a short elimination half-life and it is rapidly cleared from plasma after intramuscular (IM) and intravenous (IV) administration (7). The effects of xylazine on the digestive tract are variable and include reduced rumen motility and ruminal tympany (8).…”
Section: Introductionmentioning
confidence: 99%
“…Sci. 71 (5): [539][540][541][542][543][544][545][546][547][548] 2009 Xylazine (2(2,6 dimethylphenylamino)-5,6-dihydro-4H-1,3 thiazine hydrochloride) is a potent  2 -adrenoceptor agonist, clonidine analogue and non-narcotic drug [5]. The  2 /  1 receptor binding selectivity of xylazine is 160, whereas those of medetomidine, detomidine and clonidine are 1620, 260 and 220, respectively [14].…”
mentioning
confidence: 99%