Premium
Pharmacokinetics and Pharmacodynamics of Dexamethasone Sodium‐m‐Sulfobenzoate (DS) after Intravenous and Intramuscular Administration: A Comparison with Dexamethasone Phosphate (DP)
Author(s) -
Hochhaus Günther,
Barth Jürgen,
AlFayoumi Suliman,
Suarez Sandra,
Derendorf Hartmut,
Hochhaus Renate,
Möllmann Helmut
Publication year - 2001
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/00912700122010285
Subject(s) - dexamethasone , pharmacokinetics , medicine , dexamethasone sodium phosphate , pharmacodynamics , pharmacology , corticosteroid , prodrug
The pharmacokinetics (PK) and pharmacodynamics (effects on blood lymphocytes) of dexamethasone (D) after intravenous (i.v.) administration of dexamethasone phosphate (DP, 10 mg, equivalent to 8.3 mg of dexamethasone) and after intravenous and intramuscular (i.m.) administration of dexamethasone sulfobenzoate sodium (DS, 9.15 mg, equivalent to 6 mg of dexamethasone) were assessed. Only 25% of DS was converted into dexamethasone with a half‐life for DS of 5.4 hours and 7.4 hours after i.v. and i.m. administration, respectively. Consequently, the mean residence time of D after both i.m. and i.v. administration of DS (10.4–11.6 h) was longer than that after DP administration (6.1 h). The smaller lymphocyte suppression induced by DS (50% of that after DP administration) was shown to be related to differences in the pharmacokinetics. This study revealed significant differences in the pharmacokinetics of D after administration of DS and DP and stresses the importance of the prodrug for the pharmacological response. Because of the slow and incomplete conversion of DS into dexamethasone, its use in emergency medicine situations should be critically evaluated.