Document Detail


Pharmacokinetic/pharmacodynamic modeling of corticosterone suppression and lymphocytopenia by methylprednisolone in rats.
MedLine Citation:
PMID:  17828751     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Adrenal suppression and lymphocytopenia are commonly monitored pharmacological responses during systemic exposure to exogenously administered corticosteroids. The pharmacodynamics of plasma corticosterone (CS) and blood lymphocytes were investigated in 60 normal rats which received either 50 mg/kg methylprednisolone (MPL) or vehicle intramuscularly. Blood samples were collected between 0.5 and 96 h following treatment. Plasma CS displayed a transient suppression with re-establishment of a normal circadian rhythm 24 h following drug treatment. An indirect response model with suppression of production well captured plasma CS profiles. An early stress-induced rise in CS was also factored into the model. Blood lymphocyte numbers exhibited a sharp decline and then returned to a new circadian rhythm which was half of the original baseline level. An integrated pharmacodynamic (PD) model with inhibition of lymphocyte trafficking from tissue to blood by both MPL and CS and induction of cell apoptosis by MPL reasonably captured this lymphocytopenia. Rats and humans differ in lymphocyte responses with humans showing full recovery of baselines. Modeling provides a valuable tool in quantitative assessment of dual, complex drug responses.
Authors:
Zhenling Yao; Debra C DuBois; Richard R Almon; William J Jusko
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  97     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2008 Jul 
Date Detail:
Created Date:  2008-06-04     Completed Date:  2008-10-09     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2820-32     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, State University of New York at Buffalo, 565 Hochstetter Hall, Buffalo, NY 14260, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Chromatography, High Pressure Liquid
Circadian Rhythm
Corticosterone / blood*
Glucocorticoids* / adverse effects,  pharmacokinetics,  pharmacology
Injections, Intramuscular
Lymphocyte Count
Lymphocytes / cytology
Lymphopenia / blood,  chemically induced*
Male
Methylprednisolone* / adverse effects,  pharmacokinetics,  pharmacology
Models, Biological*
Rats
Rats, Wistar
Grant Support
ID/Acronym/Agency:
GM 24211/GM/NIGMS NIH HHS
Chemical
Reg. No./Substance:
0/Glucocorticoids; 50-22-6/Corticosterone; 83-43-2/Methylprednisolone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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