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Pharmacological basis for duration of effect: formoterol and salmeterol versus short-acting beta 2-adrenoceptor agonists

Linden, A; Rabe, K F and Löfdahl, Claes-Göran LU (1996) In Lung 174(1). p.1-22
Abstract
The mechanisms behind the long duration of bronchodilating action of the beta 2-adrenoceptor agonists formoterol and salmeterol are only partially understood. This review compares pharmacological characteristics of long-acting versus short-acting beta 2-adrenoceptor agonists in human and animal airways. Based upon the reviewed evidence, it is concluded that for beta 2-adrenoceptor agonists, long duration of action may depend upon several factors. Both formoterol and salmeterol display a higher lipophilicity and have a higher affinity, selectivity, and potency than most short-acting agonists at the beta 2-adrenoceptor. Of these factors, lipophilicity may prove to be one of the most important ones by determining the amount of drug entering... (More)
The mechanisms behind the long duration of bronchodilating action of the beta 2-adrenoceptor agonists formoterol and salmeterol are only partially understood. This review compares pharmacological characteristics of long-acting versus short-acting beta 2-adrenoceptor agonists in human and animal airways. Based upon the reviewed evidence, it is concluded that for beta 2-adrenoceptor agonists, long duration of action may depend upon several factors. Both formoterol and salmeterol display a higher lipophilicity and have a higher affinity, selectivity, and potency than most short-acting agonists at the beta 2-adrenoceptor. Of these factors, lipophilicity may prove to be one of the most important ones by determining the amount of drug entering into the cell membrane in the vicinity of the beta 2-adrenoceptor. However, the receptor affinity, maximal relaxant effect (efficacy or intrinsic activity), potency, and receptor selectivity may also be of importance in determining how much beta 2-adrenoceptor agonist must remain at the receptor for sustained action. (Less)
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author
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Airway smooth-muscle relaxation - beta2-adrenoceptor agonists - Bronchodilator - Duration of action - Exosite - Formoterol - Microkinetic diffusion - Salmeterol
in
Lung
volume
174
issue
1
pages
1 - 22
publisher
Springer
external identifiers
  • pmid:8746998
ISSN
1432-1750
DOI
10.1007/BF00167947
language
English
LU publication?
no
id
9d7a8214-42d5-4cd9-bb70-1340fad599f0 (old id 1110645)
date added to LUP
2008-07-25 15:52:17
date last changed
2016-06-29 09:06:34
@article{9d7a8214-42d5-4cd9-bb70-1340fad599f0,
  abstract     = {The mechanisms behind the long duration of bronchodilating action of the beta 2-adrenoceptor agonists formoterol and salmeterol are only partially understood. This review compares pharmacological characteristics of long-acting versus short-acting beta 2-adrenoceptor agonists in human and animal airways. Based upon the reviewed evidence, it is concluded that for beta 2-adrenoceptor agonists, long duration of action may depend upon several factors. Both formoterol and salmeterol display a higher lipophilicity and have a higher affinity, selectivity, and potency than most short-acting agonists at the beta 2-adrenoceptor. Of these factors, lipophilicity may prove to be one of the most important ones by determining the amount of drug entering into the cell membrane in the vicinity of the beta 2-adrenoceptor. However, the receptor affinity, maximal relaxant effect (efficacy or intrinsic activity), potency, and receptor selectivity may also be of importance in determining how much beta 2-adrenoceptor agonist must remain at the receptor for sustained action.},
  author       = {Linden, A and Rabe, K F and Löfdahl, Claes-Göran},
  issn         = {1432-1750},
  keyword      = {Airway smooth-muscle relaxation - beta2-adrenoceptor agonists - Bronchodilator - Duration of action - Exosite - Formoterol - Microkinetic diffusion - Salmeterol},
  language     = {eng},
  number       = {1},
  pages        = {1--22},
  publisher    = {Springer},
  series       = {Lung},
  title        = {Pharmacological basis for duration of effect: formoterol and salmeterol versus short-acting beta 2-adrenoceptor agonists},
  url          = {http://dx.doi.org/10.1007/BF00167947},
  volume       = {174},
  year         = {1996},
}