Dexamethasone metabolism in the horse

Skrabalak, Dale S.; Maylin, G. A.

doi:10.1016/0039-128x(82)90144-1

Cited by 20 publications

(7 citation statements)

References 5 publications

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“…11(5. 16(5 trihydroxy-l,4-androstadiene-3.17 dione [22], For mation of 6-OH-Dexa in the rat was verified by English et al [23] who in addition to unme tabolized Dexa detected 6-OH-Dcxa and 20-dihydro-Dexa in rat urine after oral adminis tration. The site of formation of the excreted metabolites was not defined.…”

Section: Discussionmentioning

confidence: 92%

Metabolism of Dexamethasone: Sites and Activity in Mammalian Tissues

Siebe

Baude²,

Lichtenstein

et al. 1993

Kidney Blood Press Res

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We have used in vitro techniques to study the metabolism of dexamethasone. Tissue slices, homogenates and microsomal fractions of various mammalian organs from rats and humans have been used. We focused particularly on the question of whether or not dexamethasone (Dexa) is oxidized at the C11-OH group by 11β-hydroxysteroid-dehydrogenase. High activities of this enzyme system for Dexa were localized in renal cortex and rectum. Material from both human and murine liver was ineffective. The main metabolite formed from Dexa in renal and intestinal systems was identified by different mass-spectrometric techniques including on line HPLC mass spectrometry as 11-dehydro-dexamethasone. This finding was corroborated by the observation that both corticosterone and glycyrrhetinic acid block the metabolic transformation of Dexa.

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Section: Discussionmentioning

confidence: 92%

Metabolism of Dexamethasone: Sites and Activity in Mammalian Tissues

Siebe

Baude²,

Lichtenstein

et al. 1993

Kidney Blood Press Res

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“…The chemical shifts of both the "H and "*F spectra were in agreement with those of the pure compounds. Regarding the "H NMR spectroscopy of dexamethasone and its derivative dexamethasone phosphate, a direct comparison with the literature values for the "H chemical shifts of dexamethasone was difficult, because of the variations in the spectroscopy techniques and the use of different solvents (Cohen, 1973 ;Skrabalak and Maylin, 1982 ;Kartashov, Shorshnev and Arzamastsev, 1991 ;Yasuda and Shibata, 1994 ;Liu et al, 1995). Generally, several different methods have often been combined for the assignment of steroids in "H NMR spectra, including heteronuclear shift-correlated spectroscopy and special two dimensional techniques (Schneider et al, 1985 ;Marat, Templeton and Kumar, 1987).…”

Section: Discussionmentioning

confidence: 99%

Dexamethasone and Dexamethasone Phosphate Detected by1H and19F NMR Spectroscopy in the Aqueous Humour

Midelfart

Dybdahl

Müller

et al. 1998

Experimental Eye Research

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“…Its detection and metabolism in the horse was first described in the 1970s (Dumasia et al. , 1976; Skrabalak & Maylin, 1982). Owing to its poor aqueous solubility, DXM is commonly formulated as a phosphate ester, which is rapidly hydrolyzed in blood to form free alcohols (Petersen et al.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of dexamethasone following intra‐articular, intravenous, intramuscular, and oral administration in horses and its effects on endogenous hydrocortisone

Soma

Uboh

Liu

et al. 2012

Vet Pharm & Therapeutics

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This study investigated and compared the pharmacokinetics of intra-articular (IA) administration of dexamethasone sodium phosphate (DSP) into three equine joints, femoropatellar (IAS), radiocarpal (IAC), and metacarpophalangeal (IAF), and the intramuscular (IM), oral (PO) and intravenous (IV) administrations. No significant differences in the pharmacokinetic estimates between the three joints were observed with the exception of maximum concentration (Cmax ) and time to maximum concentration (Tmax ). Median (range) Cmax for the IAC, IAF, and IAS were 16.9 (14.6-35.4), 23.4 (13.5-73.0), and 46.9 (24.0-72.1) ng/mL, respectively. The Tmax for IAC, IAF, and IAS were 1.0 (0.75-4.0), 0.62 (0.5-1.0), and 0.25 (0.08-0.25) h, respectively. Median (range) elimination half-lives for IA and IM administrations were 3.6 (3.0-4.6) h and 3.4 (2.9-3.7) h, respectively. A 3-compartment model was fitted to the plasma dexamethasone concentration-time curve following the IV administration of DSP; alpha, beta, and gamma half-lives were 0.03 (0.01-0.05), 1.8 (0.34-2.3), and 5.1 (3.3-5.6) h, respectively. Following the PO administration, the median absorption and elimination half-lives were 0.34 (0.29-1.6) and 3.4 (3.1-4.7) h, respectively. Endogenous hydrocortisone plasma concentrations declined from a baseline of 103.8 ± 29.1-3.1 ± 1.3 ng/mL at 20.0 ± 2.7 h following the administration of DSP and recovered to baseline values between 96 and 120 h for IV, IA, and IM administrations and at 72 h for the PO.

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Dexamethasone metabolism in the horse

Cited by 20 publications

References 5 publications

Metabolism of Dexamethasone: Sites and Activity in Mammalian Tissues

Metabolism of Dexamethasone: Sites and Activity in Mammalian Tissues

Dexamethasone and Dexamethasone Phosphate Detected by1H and19F NMR Spectroscopy in the Aqueous Humour

Pharmacokinetics of dexamethasone following intra‐articular, intravenous, intramuscular, and oral administration in horses and its effects on endogenous hydrocortisone

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