A Single‐dose pharmacokinetic study of the antisickling agent cetiedil

Eugene P. Orringer; J. Robert Powell; Robert E. Cross; John F. Rogers; Olesia Wojcieszyn; Julius C. Phillips; John Reed; Kung‐Tat ‐T Ng; Lee R. Berkowitz

doi:10.1038/clpt.1986.39

A Single‐dose pharmacokinetic study of the antisickling agent cetiedil

Eugene P. Orringer, J. Robert Powell, Robert E. Cross, John F. Rogers, Olesia Wojcieszyn, Julius C. Phillips, John Reed, Kung‐Tat ‐T Ng, Lee R. Berkowitz

Research output: Contribution to journal › Article › peer-review

7 Scopus citations

Abstract

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:

Original language	English (US)
Pages (from-to)	276-281
Number of pages	6
Journal	Clinical Pharmacology & Therapeutics
Volume	39
Issue number	3
DOIs	https://doi.org/10.1038/clpt.1986.39
State	Published - Mar 1986
Externally published	Yes

ASJC Scopus subject areas

Pharmacology
Pharmacology (medical)

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10.1038/clpt.1986.39

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title = "A Single‐dose pharmacokinetic study of the antisickling agent cetiedil",

abstract = "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:",

author = "Orringer, {Eugene P.} and Powell, {J. Robert} and Cross, {Robert E.} and Rogers, {John F.} and Olesia Wojcieszyn and Phillips, {Julius C.} and John Reed and Ng, {Kung‐Tat ‐T} and Berkowitz, {Lee R.}",

year = "1986",

month = mar,

doi = "10.1038/clpt.1986.39",

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AU - Orringer, Eugene P.

AU - Powell, J. Robert

AU - Cross, Robert E.

AU - Rogers, John F.

AU - Wojcieszyn, Olesia

AU - Phillips, Julius C.

AU - Reed, John

AU - Ng, Kung‐Tat ‐T

AU - Berkowitz, Lee R.

PY - 1986/3

Y1 - 1986/3

N2 - 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:

AB - 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:

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A Single‐dose pharmacokinetic study of the antisickling agent cetiedil

Abstract

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