Determination of constituents of Telazol®—tiletamine and zolazepam by a gas chromatography/mass spectrometry-based method

Kumar, Akshay; Mann, Henry J.

doi:10.1016/j.jchromb.2006.05.014

Cited by 8 publications

(12 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Tiletamine and zolazepam were isolated from a vial of Telazol Õ as described previously (Kumar et al, 2006b). Desmethyl diazepam, ketamine and b-glucuronidase (from Helix pomatia) were obtained from Sigma Corporation of Saint Louis, MO.…”

Section: Methodsmentioning

confidence: 99%

“…The concentrations of tiletamine and zolazepam and their metabolites in the plasma samples and in vitro incubations were determined by slight modifications to a validated GC/MS assay previously developed in our laboratory (Kumar et al, 2006b). Each plasma sample (500 ml) was incubated with 500 ml of b-glucuronidase solution (2000 U/ml in 0.2 M pH 5 acetate buffer) overnight at 37 C to cleave the glucuronide of 6-hydroxy zolazepam.…”

Section: Analytical Methodologymentioning

confidence: 99%

“…The details of GC/MS instrumentation have been described previously (Kumar et al, 2006b). The mass spectrometer was operated in selective positive-ion monitoring mode and the target ions for desethyl tiletamine, tiletamine, ketamine, zolazepam, 8-desmethyl zolazepam, 6-hydroxy zolazepam, desmethyl diazepam and 1-desmethyl zolazepam were 138, 166, 180, 285, 243, 273, 242 and 271, respectively.…”

Section: Analytical Methodologymentioning

confidence: 99%

See 2 more Smart Citations

Pharmacokinetic study in pigs andin vitrometabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol)

Kumar¹,

Mann

Beilman

et al. 2013

Xenobiotica

View full text Add to dashboard Cite

1. An equal-dose combination of tiletamine and zolazepam (Telazol®) is used as a veterinary anesthetic. There also have been reports of human abuse of Telazol®. The pharmacokinetics and metabolic fate of tiletamine and zolazepam and the rationale for their administration as an equal-dose combination are unclear. 2. The single-dose pharmacokinetics of intramuscular tiletamine and zolazepam (3 mg/kg each) in 16 Yorkshire-crossbred pigs were determined. The metabolites of tiletamine and zolazepam in pig plasma and urine were identified by mass spectrometry. The metabolic stability of tiletamine and zolazepam and the kinetics of formation of their metabolites by pig- and human-liver microsomes were determined. 3. Higher concentrations of zolazepam were observed in pig plasma and it was cleared more slowly compared to tiletamine (apparent clearance: 11 versus 134 l/h; half-life: 2.76 versus 1.97 h). Three metabolites of zolazepam and one metabolite of tiletamine were identified in pig urine, plasma and in microsomal incubations. In vitro formation of each of these metabolites in microsomes was biphasic involving a high-affinity/low-capacity and a low-affinity/high-capacity enzyme. The in vitro metabolic stability of tiletamine was considerably lower compared to zolazepam. 4. These results collectively point to major pharmacokinetic and metabolic differences between the two components of this fixed-dose anesthetic combination.

show abstract

Section: Methodsmentioning

confidence: 99%

Section: Analytical Methodologymentioning

confidence: 99%

Section: Analytical Methodologymentioning

confidence: 99%

See 1 more Smart Citation

Pharmacokinetic study in pigs andin vitrometabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol)

Kumar¹,

Mann

Beilman

et al. 2013

Xenobiotica

View full text Add to dashboard Cite

show abstract

“…Telazol is a fi xed-ratio combination of zolazepam with tiletamine, used for injection anesthesia in dogs, cats, wild and zoo animals [25]. Tiletamine is a dissociative anesthetic similar to ketamine and phencyclidine, and zolazepam is a diazepine derivative tranquilizer used to minimize the muscle hypertonicity and seizures associated with tiletamine [26].…”

Section: Discussionmentioning

confidence: 99%

Atipamezole Attenuated Telazol/Xylazine-Induced Expression of C-Fos in Rat Thalamencephal and Cerebral Cortex

Yin

et al. 2016

Acta Veterinaria

View full text Add to dashboard Cite

The aim of this study was to assess whether atipamezole can restrain telazol/xylazine induced expression of c-fos in the rat brain. Rats were injected with a mixture of 13.81 mg/kg telazol and 5.21 mg/kg xylazine, following 10 min later 0.522 mg/kg atipamezole. Thereon, the thalamencephal and cerebral cortex were removed one hour after the last injection. The level of Fos protein was measured in the brain tissue by Westernblot. The results revealed that atipamezole attenuates telazol/xylazine induction of c-fos expression in the thalamencephal and cerebral cortex. The results indicated that atipamezole is able to inhibit telazol/xylazine-induced c-fos expression in the rat brain, thus protecting it from nerve damage.

show abstract

“…Plasma samples were analyzed for tiletamine and zolazepam concentrations with a gas chromatography–mass spectroscopy (GC/MS) assay developed in our laboratory. The details of the chemicals and materials used in this study, plasma extraction procedure, calibration curves, and GC/MS analysis strategy are provided elsewhere (Kumar et al. , 2006).…”

Section: Pharmacokinetic Parameters Calculated By Noncompartmental Amentioning

confidence: 99%

Pharmacokinetics of tiletamine and zolazepam (Telazol^®) in anesthetized pigs

Kumar¹,

Mann²

2006

Vet Pharm & Therapeutics

View full text Add to dashboard Cite

Determination of constituents of Telazol®—tiletamine and zolazepam by a gas chromatography/mass spectrometry-based method

Cited by 8 publications

References 11 publications

Pharmacokinetic study in pigs andin vitrometabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol)

Pharmacokinetic study in pigs andin vitrometabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol)

Atipamezole Attenuated Telazol/Xylazine-Induced Expression of C-Fos in Rat Thalamencephal and Cerebral Cortex

Pharmacokinetics of tiletamine and zolazepam (Telazol^®) in anesthetized pigs

Contact Info

Product

Resources

About

Determination of constituents of Telazol®—tiletamine and zolazepam by a gas chromatography/mass spectrometry-based method

Cited by 8 publications

References 11 publications

Pharmacokinetic study in pigs andin vitrometabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol)

Pharmacokinetic study in pigs andin vitrometabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol)

Atipamezole Attenuated Telazol/Xylazine-Induced Expression of C-Fos in Rat Thalamencephal and Cerebral Cortex

Pharmacokinetics of tiletamine and zolazepam (Telazol®) in anesthetized pigs

Contact Info

Product

Resources

About

Pharmacokinetics of tiletamine and zolazepam (Telazol^®) in anesthetized pigs