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)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/254072
- author
- Lotvall, J
; Palmqvist, M
; Ankerst, Jaro
LU
; Persson, G
; Rosenborg, J
; Bengtsson, T
; Rott, Z
; Poczi, M
; Devai, A
and Waldeck, B
- organization
- publishing date
- 2005
- 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
- 2016-04-01 15:52:34
- date last changed
- 2024-01-10 21:21:30
@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}},
keywords = {{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}},
doi = {{10.1016/j.pupt.2004.10.007}},
volume = {{18}},
year = {{2005}},
}