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Prednisone ADME

Summary

Organism

Homo sapiens (human)

Reactome

R-HSA-9757110

PubChem

R-HSA-9757110

Description

Prednisone (PREDN) is a prodrug of prednisolone (PREDL), and is rapidly absorbed. To achieve high uptake of the near water-insoluble molecule the highest dose 50 mg has to be dissolved in 250 ml water. Its conversion to the highly active prednisolone (PREDL) in liver cells is reversible but represents the favored reaction direction (Pickup, 1979).
Prednisone and prednisolone are considered to be fully therapeutically equivalent. The theoretical advantage of avoiding high GI concentrations of prednisone by administering prednisolone directly has never been shown to be clinically relevant (Vogt et al, 2007).
Only 2–5% of a given dose of prednisone is excreted unchanged in urine. After hydrogenation to prednisolone at least 20 metabolites and their conjugates are formed and excreted. The main metabolites both after systemic and topical use are 20alpha- and 20beta-dihydro-prednisone, as well as 20alpha- and 20beta-dihydro-prednisolone (20AH-PREDN, 20BH-PREDN, 20AH-PREDL, 20BH-PREDL), in addition to the 6beta-hydroxy compounds 6B-OH-PREDN and 6B-OH-PREDL (Matabosch et al, 2015; Mazzarino et al, 2019). Hydrogenation of PREDN and dehydrogenation of PREDL are complementary reactions that are dominant in different cell types. While liver and fat cells convert PREDN to PREDL, colon and kidney cells partly convert PREDL back to PREDN (Jamieson et al, 1995; Ricketts et al, 1998; Diederichs et al, 2002). We have depicted this equilibrium by showing example reactions in hepatocytes and kidney cells in the diagram.

Click on a node on the pathway to see its details. Glycoproteins are marked with a glycoprotein icon in their name.

SPV: a JavaScript Signaling Pathway Visualizer, Bioinformatics, 2018

Displaying **all 7** entries
UniProt ID	Protein Name	Gene Symbol	Pathway Viewer
O75795	UDP-glucuronosyltransferase 2B17	UGT2B17	view
P02768	Albumin	ALB GIG20 GIG42 PRO0903 PRO1708 PRO2044 PRO2619 PRO2675 UNQ696/PRO1341	view
P08183	ATP-dependent translocase ABCB1	ABCB1 MDR1 PGY1	view
P08185	Corticosteroid-binding globulin	CBG SERPINA6	view
P16662	UDP-glucuronosyltransferase 2B7	UGT2B7 UGTB2B9	view
P28845	11-beta-hydroxysteroid dehydrogenase 1	HSD11 HSD11B1 HSD11L SDR26C1	view
P35503	UDP-glucuronosyltransferase 1A3	GNT1 UGT1 UGT1A3	view

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