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New millennium bronchodilators for asthma: single-isomer beta agonists
D A Handley1, A J Anderson, J Koester
1Scientific Affairs, Sepracor Inc., Marlborough, MA 01752, USA.
Current Opinion in Pulmonary Medicine
|December 23, 1999
Summary
Pure R-isomers of beta2 agonists offer superior bronchodilation with fewer side effects compared to racemic mixtures. Developing isomerically pure drugs like (R)-albuterol and (R,R)-formoterol enhances therapeutic efficacy and duration.
Area of Science:
- Pharmacology
- Respiratory Medicine
- Medicinal Chemistry
Background:
- Racemic beta2 agonists contain R and S isomers, with R isomers primarily responsible for bronchodilation.
- S isomers are often considered inert but can potentially counteract the effects of R isomers.
Purpose of the Study:
- To evaluate the therapeutic advantages of using isomerically pure beta2 agonists.
- To explore the potential for improved efficacy and reduced side effects with single-isomer drugs.
Main Methods:
- Review of existing literature on racemic and isomerically pure beta2 agonists.
- Analysis of pharmacological and clinical data for (R)-albuterol and (R,R)-formoterol.
Main Results:
- The R isomer of albuterol provides significant bronchodilation with fewer side effects than the racemic mixture.
- (S)-albuterol may negatively impact bronchial reactivity and inflammatory responses.
- Isomerically pure (R,R)-formoterol shows promise for long-acting bronchodilation (up to 24 hours) with rapid FEV1 improvement.
Conclusions:
- Isomerically pure beta2 agonists offer a potentially improved therapeutic index over racemic formulations.
- Development of single-isomer drugs like (R)-albuterol and (R,R)-formoterol represents a significant advancement in respiratory pharmacotherapy.