Metabolism of Triamcinolone Acetonide-21 -phosphate in Dogs, Monkeys, and Rats

Kripalani, Kishin J.; Cohen, Allen I.; Weliky, I.; Schreiber, EC

doi:10.1002/jps.2600640820

Cited by 33 publications

(6 citation statements)

References 16 publications

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“…Not surprisingly, the majority of the radioactivity in the intestine was rather hydrophilic (MET1). Biliary excretion has also been reported for other glucocorticoids like triamcinolone, acetonide, and prednisolone (Kripalani et al, 1975;Mueller and Potter, 1981;Khalafallah and Jusko, 1984).…”

Section: Downloaded Frommentioning

confidence: 84%

Metabolism of Mometasone Furoate and Biological Activity of the Metabolites

Sahasranaman¹,

Issar²,

Hochhaus³

2005

Drug Metab Dispos

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ABSTRACT:To better evaluate the pharmacokinetic and pharmacodynamic properties of the new inhaled glucocorticoid mometasone furoate (MF), the metabolism of MF was evaluated in rat and human tissues and in rat after i.v. administration. Metabolic studies with 3 H-MF in human and rat plasma and S9 fractions of human and rat lung showed relatively high stability and a degradation pattern similar to that seen in buffer systems. MF was efficiently metabolized into at least five metabolites in S9 fractions of both rat and human liver. There were, however, quantitative differences in the metabolites between the two species. The apparent half-life of MF in the S9 fraction of human liver was found to be 3 times greater compared with that in rat. MET1, the most polar metabolite, was the major metabolite in rat liver fractions, whereas both MET1 and MET2were formed to an equal extent in human liver.

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Section: Downloaded Frommentioning

confidence: 84%

Metabolism of Mometasone Furoate and Biological Activity of the Metabolites

Sahasranaman¹,

Issar²,

Hochhaus³

2005

Drug Metab Dispos

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“…Following I.V. administration, TAP was rapidly hydrolyzed into TA in rats as had been described before 11…”

Section: Resultsmentioning

confidence: 99%

Microdialysis of Triamcinolone Acetonide in Rat Muscle

Rojas

Nagaraja

Webb

et al. 2003

Journal of Pharmaceutical Sciences

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“…Pharmacokineticstudies of triamcinoloneacetonide, that is a 2 nd generation fluorinated systemic CS, have, in fact, demonstrated the presence in the urine ofdogs and monkeys of various metabolites, including 5% of 6alpha-hydroxy-triamcinolone (16).…”

Section: Discussionmentioning

confidence: 99%

Anaphylaxis Induced by Intramuscular Betamethasone Disodium Phosphate: Reflections on a Clinical Case

Ventura

Sanapo

GF³

et al. 2007

Int J Immunopathol Pharmacol

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Glucocorticoids could be responsible for allergic symptoms correlated to an Ig-E mediated hypersensitivity mechanism. We describe the case of an anaphylactic reaction in a professional nurse, occurring after an intramuscular administration of Betamethasone. After performing skin prick tests, intramuscular tests and patch tests we concluded that the patient had Ig-E mediated sensitization. She was prescribed oral Prednisone and Deflazacort and shows good tolerance of these drugs. This demonstrates that in these patients it is possible to administrate glucocorticoids without the changes in the sites indicated by Wilkinson. Nevertheless, our patient showed a negative allergy test for Dexamethasone disodium phosphate, and in those patients sensitized to fluorinated glucocorticoids, tolerance to other glucocorticoids is not so easily predictable as in patients with hypersensitivity to first generation steroids or in corticosteroid contact dermatitis, according to the four patterns of cross-reactivity proposed by Coopman and Dooms-Goossens.

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Metabolism of Triamcinolone Acetonide-21 -phosphate in Dogs, Monkeys, and Rats

Cited by 33 publications

References 16 publications

Metabolism of Mometasone Furoate and Biological Activity of the Metabolites

Metabolism of Mometasone Furoate and Biological Activity of the Metabolites

Microdialysis of Triamcinolone Acetonide in Rat Muscle

Anaphylaxis Induced by Intramuscular Betamethasone Disodium Phosphate: Reflections on a Clinical Case

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