Volume 41, Issue 4 p. 425-434

Pharmacokinetics and Pharmacodynamics of Dexamethasone Sodium-m-Sulfobenzoate (DS) after Intravenous and Intramuscular Administration: A Comparison with Dexamethasone Phosphate (DP)

Dr. Günther Hochhaus PhD, FCP

Corresponding Author

Dr. Günther Hochhaus PhD, FCP

College of Pharmacy, Department of Pharmaceutics, University of Florida, Gainesville

College of Pharmacy (Box 100494), University of Florida, Gainesville, FL 32610.Search for more papers by this author
Dr. Jürgen Barth MD

Dr. Jürgen Barth MD

Medical Clinic “Bergmannstrost,” Halle, Germany

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Suliman Al-Fayoumi PhD

Suliman Al-Fayoumi PhD

College of Pharmacy, Department of Pharmaceutics, University of Florida, Gainesville

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Dr. Sandra Suarez PhD

Dr. Sandra Suarez PhD

College of Pharmacy, Department of Pharmaceutics, University of Florida, Gainesville

Dr. Suarez's current affiliation is the Office of Clinical Pharmacology and Biopharmaceutics, Food and Drug Administration.

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Dr. Hartmut Derendorf PhD, FCP

Dr. Hartmut Derendorf PhD, FCP

College of Pharmacy, Department of Pharmaceutics, University of Florida, Gainesville

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Dr. Renate Hochhaus

Dr. Renate Hochhaus

College of Pharmacy, Department of Pharmaceutics, University of Florida, Gainesville

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Dr. Helmut Möllmann MD

Dr. Helmut Möllmann MD

Medical Clinic, University of Bochum, Germany

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First published: 08 March 2013
Citations: 33

Abstract

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.