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The effect of formoterol over 24 h in patients with asthma: the role of enantiomers

Lotvall, J; Palmqvist, M; Ankerst, Jaro LU ; Persson, G; Rosenborg, J; Bengtsson, T; Rott, Z; Poczi, M; Devai, A and Waldeck, B (2005) In Pulmonary Pharmacology & Therapeutics 18(2). p.109-113
Abstract
The single-dose effect of formoterol racemate and enantiomers on bronchodilatation up to 24 h was determined. Forty-six reversible asthmatic patients were randomised to this double blind, crossover study. Formoterol was inhaled by nebulizer (HaloLite(R)); 4.5 and 36 mug of the racemate (rac-formoterol), 2.25 and 18 mug of (R;R)-formoterol, 18 mug of (S;S)-formoterol, or placebo. Airway and systemic effects were assessed by serial measurements of forced expiratory volume during the first second, FEV1 (24 h), and heart rate (4 h). Rac- and (R;R)formoterol significantly and dose-dependently increased FEV1, with similar mean maximal effect. (S;S)-formoterol was without significant effects on FEV1 and heart rate. (R;R)- and rac-formoterol were... (More)
The single-dose effect of formoterol racemate and enantiomers on bronchodilatation up to 24 h was determined. Forty-six reversible asthmatic patients were randomised to this double blind, crossover study. Formoterol was inhaled by nebulizer (HaloLite(R)); 4.5 and 36 mug of the racemate (rac-formoterol), 2.25 and 18 mug of (R;R)-formoterol, 18 mug of (S;S)-formoterol, or placebo. Airway and systemic effects were assessed by serial measurements of forced expiratory volume during the first second, FEV1 (24 h), and heart rate (4 h). Rac- and (R;R)formoterol significantly and dose-dependently increased FEV1, with similar mean maximal effect. (S;S)-formoterol was without significant effects on FEV1 and heart rate. (R;R)- and rac-formoterol were still effective 22-24 h after single high doses, but this was associated with some systemic side effect (increased heart rate) initially. Average 22-24 h FEV1 was 8% (rac-formoterol 36 mug) and 11% ((R-R)-formoterol 18 mug) over placebo, respectively. No significant differences in effects were observed between rac- and (R;R)-formoterol. Thus, the single dose bronchodilatating effect of formoterol resides in (R;R)-formoterol. This study does not indicate a clinically important advantage of (R;R)-formoterol as acute bronchodilator compared to the racemate. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
enantioselectivity, bronchodilators, pharmacodynamics
in
Pulmonary Pharmacology & Therapeutics
volume
18
issue
2
pages
109 - 113
publisher
Elsevier
external identifiers
  • wos:000226697400006
  • scopus:19944427552
ISSN
1522-9629
DOI
10.1016/j.pupt.2004.10.007
language
English
LU publication?
yes
id
379f7d4d-d15d-4eb1-b19c-10e437ea96b0 (old id 254072)
date added to LUP
2007-09-28 16:28:55
date last changed
2017-07-23 04:34:53
@article{379f7d4d-d15d-4eb1-b19c-10e437ea96b0,
  abstract     = {The single-dose effect of formoterol racemate and enantiomers on bronchodilatation up to 24 h was determined. Forty-six reversible asthmatic patients were randomised to this double blind, crossover study. Formoterol was inhaled by nebulizer (HaloLite(R)); 4.5 and 36 mug of the racemate (rac-formoterol), 2.25 and 18 mug of (R;R)-formoterol, 18 mug of (S;S)-formoterol, or placebo. Airway and systemic effects were assessed by serial measurements of forced expiratory volume during the first second, FEV1 (24 h), and heart rate (4 h). Rac- and (R;R)formoterol significantly and dose-dependently increased FEV1, with similar mean maximal effect. (S;S)-formoterol was without significant effects on FEV1 and heart rate. (R;R)- and rac-formoterol were still effective 22-24 h after single high doses, but this was associated with some systemic side effect (increased heart rate) initially. Average 22-24 h FEV1 was 8% (rac-formoterol 36 mug) and 11% ((R-R)-formoterol 18 mug) over placebo, respectively. No significant differences in effects were observed between rac- and (R;R)-formoterol. Thus, the single dose bronchodilatating effect of formoterol resides in (R;R)-formoterol. This study does not indicate a clinically important advantage of (R;R)-formoterol as acute bronchodilator compared to the racemate.},
  author       = {Lotvall, J and Palmqvist, M and Ankerst, Jaro and Persson, G and Rosenborg, J and Bengtsson, T and Rott, Z and Poczi, M and Devai, A and Waldeck, B},
  issn         = {1522-9629},
  keyword      = {enantioselectivity,bronchodilators,pharmacodynamics},
  language     = {eng},
  number       = {2},
  pages        = {109--113},
  publisher    = {Elsevier},
  series       = {Pulmonary Pharmacology & Therapeutics},
  title        = {The effect of formoterol over 24 h in patients with asthma: the role of enantiomers},
  url          = {http://dx.doi.org/10.1016/j.pupt.2004.10.007},
  volume       = {18},
  year         = {2005},
}