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Titolo:
Comparison of the long-term beta(2) sympathomimetics formoterol and salmeterol
Autore:
Reinhardt, D; von Berg, A; Lemoine, H;
Indirizzi:
Klinikum Univ Munchen, Dr von Haunerschen Kinderspital, Kinderklin & Poliklin, Munich, Germany Klinikum Univ Munchen Munich Germany erklin & Poliklin, Munich, Germany
Titolo Testata:
MONATSSCHRIFT KINDERHEILKUNDE
fascicolo: 9, volume: 149, anno: 2001,
pagine: 934 - 948
SICI:
0026-9298(200109)149:9<934:COTLBS>2.0.ZU;2-0
Fonte:
ISI
Lingua:
GER
Soggetto:
ACTING BETA(2)-ADRENOCEPTOR AGONISTS; ALBUTEROL-INDUCED BRONCHOPROTECTION; ADENYLATE-CYCLASE STIMULATION; EXERCISE-INDUCED ASTHMA; HUMAN LUNG FIBROBLASTS; DOSE INHALED STEROIDS; SMOOTH-MUSCLE CELLS; GUINEA-PIG TRACHEAS; MILD ASTHMA; ADRENOCEPTOR AGONISTS;
Keywords:
long acting-beta(2)-sympathomimetica; mechanism of action; clinical use; "add on therapy" with glucocorticoids; tolerance; extra-pulmonary side effects;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
131
Recensione:
Indirizzi per estratti:
Indirizzo: Reinhardt, D Univ Munich, Dr von Haunerschen Kinderspital, Klinikum Innenstadt, Kinderklin & Poliklin, Lindwurmstr 4, D-80337 Munich, Germany Univ Munich Lindwurmstr 4 Munich Germany D-80337 ch, Germany
Citazione:
D. Reinhardt et al., "Comparison of the long-term beta(2) sympathomimetics formoterol and salmeterol", MONATS KIND, 149(9), 2001, pp. 934-948

Abstract

A chemical modification of fenoterol and salbutamol made it possible to synthesize two new beta (2)-sympathomimetic drugs which not only show a high affinity to beta (2)-adrenoceptors but also a long-acting efficacy. The extended duration of bronchodilatation is due to a high lipophilicity of salmeterol whereas formoterol shows a very stabile "high affinity state,of the beta (2)-adrenoceptor binding and a high intrinsic activity. The duration ofa clinical relevant bronchodilatation is identical for both drugs and liesin the rank order of 12 h. The onset of action, however, differs. For formoterol initial bronchodilatation occurs already after 3 min and the time topeak action is 20-30 min, whereas for salmeterol the initial effect is obtained after 15 min,the maximum effect after I h. Because of its rapid onsetof action formoterol will receive its concession for administration in theacute asthmatic attack in near future. In relation to isoproteronol which is the reference drug formoterol has 100%, salmeterol only of 50% an intrinsic activity. Thus salmeterol is regarded to be only a partial agonist which aside from its agonistic has also an antagonistic efficacy. In case of a regular tratment over a long period salmeterol might therefore act as an antagonist against short-acting beta (2)-sympathomimetics which will be required for therapy of an acute asthmatic attack. The clinical application of long-acting beta (2)-sympathomimetic drugs might primarily consist in their use as "add on" drugs to topical glucocorticoids. Several studies,at least in adults, have shown that both long acting beta (2)-sympathomimetics exhibit additive effects which are greater than the effects of the single components. The mechanism of this action remains to be obscure. Salmeterol is already available in a combination preperation with fluticason for 3 years whereas formoterol and budesonide have received their license as a combinationpreperation in april 2001. Undesired side effects including tolerance as well as extra pulmonary effects (tachycardia, blood pressure increase) must be taken into consideration under a long term treatment.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 12/07/20 alle ore 09:37:47