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A Single‐dose pharmacokinetic study of the antisickling agent cetiedil
Author(s) -
Orringer Eugene P,
Powell J Robert,
Cross Robert E,
Rogers John F,
Wojcieszyn Olesia,
Phillips Julius C,
Reed John,
Ng KungTat,
Berkowitz Lee R
Publication year - 1986
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1986.39
Subject(s) - pharmacokinetics , pharmacology , sickle cell anemia , in vivo , clinical pharmacology , dosing , chemistry , medicine , cell , biochemistry , biology , microbiology and biotechnology
Cetiedil citrate is an antisickling agent shown to be effective in reducing the severity and duration of acute sickle cell crisis. With the use of a sensitive GC/MS assay, the pharmacokinetic profile of cetiedil was studied in normal men and in men with sickle cell anemia who were not in crisis at the time of study. A peak cetiedil concentration of 70 to 200 ng/ml was found immediately after a 30‐minute drug infusion. The plasma level then gradually declined to approximately 10 ng/ml during a 3‐hour distributive phase. Computer analysis of the data was most consistent with a three‐compartment model. No pharmacokinetic differences were found between the normal men and the subjects with sickle cell. Because the cetiedil plasma levels achieved during this in vivo study are well below concentrations that exhibit antisickling activity in vitro, additional clinical studies will be necessary before an optimal dosing regimen can be established. Clinical Pharmacology and Therapeutics (1986) 39, 276–281; doi: 10.1038/clpt.1986.39