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Albuterol enantiomers have comparable therapeutic ratio in asthma patients

EW YORK (Reuters Health) – Contrary to previous evidence, new study findings indicate that the therapeutic ratio of the R-enantiomer of albuterol is no greater than that of racemic (RS) albuterol.

Dr. Jan Lotvall from Goteborg University in Sweden, and colleagues, note in the November issue of The Journal of Allergy and Clinical Immunology that "it has been suggested that R-albuterol produces bronchodilation that is comparable with that of racemic albuterol on a 4:1 dose-for-dose basis but systemic side effects on a 2:1 basis, implying better therapeutic ratio for R-albuterol."

To test this, the researchers examined the effects of R-, S-, and RS-albuterol in 20 asthmatic patients in a double-blind, placebo-controlled, crossover study.

A significant dose-related improvement in FEV1 was noted with R- and RS-albuterol but not with S-albuterol or placebo, the authors report. At higher doses, R- and RS-albuterol were associated with increased heart rate and decreased plasma potassium levels.

The potency ratios of R- albuterol/RS-albuterol for the local and systemic effects were similar, and the S-enantiomer of RS-albuterol appears to be inert, the authors say. They conclude that the findings indicate "a comparable therapeutic ratio for R-albuterol and RS-albuterol in asthmatic subjects."

In a related editorial, Dr. Richard Ahrens and Dr. Miles Weinberger, from the University of Iowa in Iowa City, comment that "the available data provide no evidence that levalbuterol is any safer or more effective than doses of racemic albuterol that contain equimolar doses of R-albuterol."

Furthermore, "considering the greater cost that is currently associated with Xopenex [R-albuterol], routine use of this product has the potential to increase the cost of asthma care without identified benefit," the editorialists conclude.

J Allergy Clin Immunol 2001;108:681-684, 726-731.

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