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Stereoconfiguration of antiallergic and immunologic drugs
Leonard Bielory1, Andrey Leonov
1Division of Allergy, Immunology and Rheumatology, UMDNJ-New Jersey Medical School, Newark, New Jersey 07103, USA. bielory@umdnj.edu
Objective:
To review the concept of chirality and its current role in the pharmacology of antiallergic, antiasthmatic, and immunologic agents.
Data Sources:
Ovid MEDLINE and PubMed databases from 1950 to the present time were searched.
Study Selection:
Articles that described the pharmacology of chiral antiallergic, antiasthmatic, and immunologic medications were used for this review.
Results:
Stereoselectivity affects the pharmacologic profiles of medications in different ways from class to class and within the classes. This summary illustrates that enantiomers differ not only in potency in receptor binding and physiologic effects but also in pharmacokinetic parameters such as volume of distribution, plasma protein binding, metabolism, and clearance. Different enantiomers may produce unrelated pharmacologic effects as well. This review summarizes the variety of possible effects that different stereoisomers may produce and further underlines the importance of the purification and in-depth analysis of chiral compounds.
Conclusion:
Chirality plays an important role in pharmacokinetics and pharmacodynamics of various pharmaceutical agents. The importance of stereoisomeric purity in the pharmacologic industry has increased during the past decade as demonstrated by the increased number of studies that examined the in vivo and in vitro effects produced by changes in stereoconfiguration of pharmaceutical agents. This review highlights such effects in certain frequently used medications used in the treatment of asthma and various allergic and immunologic disorders.
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