Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults.

Article Details

Citation

Szefler SJ, Ebling WF, Georgitis JW, Jusko WJ

Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults.

Eur J Clin Pharmacol. 1986;30(3):323-9. doi: 10.1007/bf00541537.

PubMed ID
3732369 [ View in PubMed
]
Abstract

The disposition and plasma binding of methylprednisolone were examined in seven normal volunteers following the administration of 5, 20 and 40 mg of intravenous methylprednisolone sodium succinate. Methylprednisolone exhibits linear plasma protein binding averaging 77%. The mean plasma methylprednisolone clearance of 337 ml X h-1 X kg-1 was independent of dose. The steroid appears to moderately distribute into tissue spaces with a mean volume of distribution of 1.41 X kg-1. Methylprednisolone disposition parameters were compared with the non-transcortin bound parameters for prednisolone. The prednisolone plasma clearance based on the transcortin free-drug is similar to methylprednisolone total plasma clearance. However, the corrected volume of distribution of prednisolone is only one-half that of methylprednisolone. The disposition rate of these two steroids is thus similar, in spite of their metabolic control by different enzymatic pathways and major influence of saturable transcortin binding on prednisolone elimination.

DrugBank Data that Cites this Article

Drugs
Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
Methylprednisolone11beta-hydroxysteroid dehydrogenase (Protein Group)Protein groupHumans and other mammals
Unknown
Not AvailableDetails
Methylprednisolone20-ketosteroid reductase (20-hydroxysteroid dehydrogenase) (Protein Group)Protein groupHumans and other mammals
Unknown
Substrate
Details