Stereoselective pharmacokinetics of ketamine and norketamine after racemic ketamine or S-ketamine administration in Shetland ponies sedated with xylazine

Larenza, M. Paula; Knobloch, Monika; Landoni, M. F.; Levionnois, Olivier; Kronen, Peter W; Theurillat, Regula; Schatzmann, U.; Thormann, Wolfgang

doi:10.1016/j.tvjl.2007.05.005

Cited by 36 publications

(54 citation statements)

References 8 publications

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“…Thus, interdisciplinary research efforts are undertaken to assess the use of ketamine (as racemic mixture) versus S-ketamine for anesthesia and pain therapy in horses. This work required the development of stereoselective assays for a variety of applications [25][26][27][28][29][30][31]. Enantioselective CE assays were found to be attractive approaches for the assessment of the stereoselectivity of drug metabolism [32][33][34].…”

Section: Introductionmentioning

confidence: 99%

CE provides evidence of the stereoselective hydroxylation of norketamine in equines

et al. 2009

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CE provides evidence of the stereoselective hydroxylation of norketamine in equinesCE with multiple isomer sulfated-CD as selector was used for the simultaneous analysis of the stereoisomers of ketamine, norketamine, 5,6-dehydronorketamine and hydroxylated metabolites of norketamine in liquid/liquid extracts of (i) in vitro incubations with ketamine or norketamine and equine liver microsomes and (ii) plasma and urine of ponies receiving a target-controlled infusion of ketamine under isoflurane anesthesia. Hydroxynorketamine metabolites with the hydroxy group at the cyclohexanone ring could be shown to be formed stereoselectively both in vitro and in vivo. Due to the lack of standard compounds, urinary extracts were fractionated by HPLC followed by characterization of the collected fractions with CE and LC-MS n with 0.7 mmu mass discrimination. Comparison of LC-MS n data obtained with the fractions, an in vitro microsomal sample, and both pony urine and hydrolyzed pony urine led to the identification of four hydroxylated norketamine metabolites with hydroxylation at the cyclohexanone ring, two with hydroxylation at the aromatic ring and four hydroxylated metabolites of ketamine. Due to the lower detection sensitivity, only the four hydroxynorketamine metabolites with hydroxylation at the cyclohexanone ring were observed by CE. The data suggest that demethylation of ketamine followed by hydroxylation of norketamine at the cyclohexanone ring is the major metabolic pathway in equine species and that the ketamine metabolism is highly stereoselective.

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Section: Introductionmentioning

confidence: 99%

CE provides evidence of the stereoselective hydroxylation of norketamine in equines

et al. 2009

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“…Em medicina, é muito utilizada como medicação pré-anestésica pela via intranasal, com boa eficácia e sem efeitos adversos para sedação em crianças (Diaz 1997). A cetamina S+ é o enantiômero levógiro da cetamina racêmica e apresenta maior afinidade a receptores NMDA, maior potência analgésica e menos efeitos adversos com menores doses quando comparada a cetamina racêmica (Duque et al 2008, Larenza et al 2008a, 2008b. Pelas características peculiares da cetamina S+, optou-se, no presente estudo, pela utilização da menor dose deste fármaco (20mg/kg) preconizada para anestesia de pombos.…”

Section: Resultsunclassified

“…Esta discrepância entre resultados pode ser decorrente da grande variedade intra e interespécies de pássaros (Samour et al 1984), considerando que diferentes famílias de pássaros foram avaliadas nos outros estudos, o que pode resultar em particularidades na biotransformação dos fármacos e na ação farmaco-lógica destes. Outra diferença importante é que a dose da cetamina S+ deste estudo (20mg/kg) foi metade da dose utilizada em periquitos (40 mg/kg), o que também poderia justificar a menor duração de ação nos pombos, apesar de alguns autores afirmarem que a cetamina S+, por apresentar maior efeito analgésico e maior potência, pode ter sua dose reduzida como o observado para gatos, cães e pôneis (Duque et al 2008, Larenza et al 2008a, 2008b.…”

Section: Discussionunclassified

Efeitos anestésicos da administração intranasal ou intramuscular de cetamina S+ e midazolam em pomba-rola (Streptotelia sp.)

et al. 2013

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Pesq. Vet. Bras. 33(4):517-522, abril 2013 517 RESUMO.-A via intranasal é uma boa alternativa por ser indolor e de fácil aplicação em aves. O objetivo deste estudo foi avaliar os efeitos anestésicos da associação de cetamina S+ e midazolam pela via intranasal (IN) The intranasal route is a good alternative because is painless and easy to perform in birds. The objective of this study was to evaluate the anesthetic effects of S+ ketamine and midazolam administered by intranasal or intramuscular route in pigeons. Twelve animals were used in a randomized and crossover design. Animals received two treatments with 2-weeks interval. IM group: animals received 20mg/kg of S+ ketamine and 3.5mg/kg of midazolam by intramuscular route (pectoral muscles); IN group: animals received the same protocol by intranasal route. Parameters evaluated were: onset of action, time of duration in dorsal recumbency; total time of anesthesia and side effects. Statistical analysis was performed using Wilcoxon test and the differences were considered significant when P<0. 05 IN (15 [4,5]) comparado ao IM (32 [28,[25][26][27][28][29][30][31][32][33][34][35][36][37][38]25] minutos). Dois animais de cada

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“…As with our previous compilation 10 years ago [26], insight into the achievements is presented via distinction between enantiomer analysis in fortified body fluids (Table 1), body fluids and tissues of humans and animals (Tables 2 and 3), in vitro preparations (Table 4) and in forensic biosamples (Table 5 [ ). Furthermore, the stereoselective CE work associated with a multidisciplinary ketamine project is presented separately (Table 6 [ [154][155][156][157][158][159][160][161][162][163][164][165][166][167][168][169]). Major focus is given on systems in which stereoisomers of parent drug and metabolites are analyzed together in one run.…”

Section: Drugmentioning

confidence: 99%

“…Compared to the previous decade, during which mostly uncharched CDs were employed [26], we noted a strong increase of the use of charged CDs. S-␤-CD, with 7-11 mol sulfate/mol ␤-CD, was most often used [58,60,63,69,71,79,80,83,95,97,99,101,108,110,118,123,131,134,135,139,[154][155][156][157][158][159][160][161][162][163][164][165][166][167][168][169] whereas the better defined highly sulfated CD derivatives (HS-␤-CD and HS-␥-CD [170]) were only used in a few assays [50,51,72,111,144,145]. These and other selectors, such as phosphated-␥-CD (PH-␥-CD) [94,106,126], carboxymethyl-␤-CD (CM-␤-CD) or carboxymethyl-␥-CD (CM-␥-CD) …”

Section: Principlesmentioning

confidence: 99%

Stereoselective determination of drugs and metabolites in body fluids, tissues and microsomal preparations by capillary electrophoresis (2000–2010)

Caslavska

Thormann

2011

Journal of Chromatography A

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Stereoselective pharmacokinetics of ketamine and norketamine after racemic ketamine or S-ketamine administration in Shetland ponies sedated with xylazine

Cited by 36 publications

References 8 publications

CE provides evidence of the stereoselective hydroxylation of norketamine in equines

CE provides evidence of the stereoselective hydroxylation of norketamine in equines

Efeitos anestésicos da administração intranasal ou intramuscular de cetamina S+ e midazolam em pomba-rola (Streptotelia sp.)

Stereoselective determination of drugs and metabolites in body fluids, tissues and microsomal preparations by capillary electrophoresis (2000–2010)

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