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Titolo:
PHARMACODYNAMICS AND PHARMACOKINETICS OF BAY-X-7195 AEROSOL, A NEW AND SELECTIVE RECEPTOR ANTAGONIST OF CYSTEINYL-LEUKOTRIENES, IN NORMAL VOLUNTEERS
Autore:
WENSING G; HEINIG R; KUHLMANN J;
Indirizzi:
BAYER AG,PHARMA RES CTR,INST CLIN PHARMACOL D-42096 WUPPERTAL GERMANY
Titolo Testata:
British journal of clinical pharmacology
fascicolo: 2, volume: 42, anno: 1996,
pagine: 171 - 178
SICI:
0306-5251(1996)42:2<171:PAPOBA>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
ALLERGEN-INDUCED BRONCHOCONSTRICTION; INHALED LEUKOTRIENE-D4; D4-INDUCED BRONCHOCONSTRICTION; URINARY LEUKOTRIENE-E4; AIRWAY RESPONSIVENESS; BRONCHIAL-ASTHMA; ICI-204,219; INHALATION; METHACHOLINE; OBSTRUCTION;
Keywords:
POWDER AEROSOL; BRONCHIAL CHALLENGE; LEUKOTRIENE-D-4;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
32
Recensione:
Indirizzi per estratti:
Citazione:
G. Wensing et al., "PHARMACODYNAMICS AND PHARMACOKINETICS OF BAY-X-7195 AEROSOL, A NEW AND SELECTIVE RECEPTOR ANTAGONIST OF CYSTEINYL-LEUKOTRIENES, IN NORMAL VOLUNTEERS", British journal of clinical pharmacology, 42(2), 1996, pp. 171-178

Abstract

1 The safety, tolerability and pharmacokinetics of BAY x 7195 aerosol, a new selective receptor antagonist of cysteinyl-leukotrienes, were investigated in healthy male volunteers in two observational studies (1 and 2 mg; n = 5 each) and two double blind, placebo-controlled two way crossover studies (4 and 8 mg; n = 6 each) using the commercially available Inhaler Ingelheim M(R). 2 The pharmacodynamic effect was assessed by testing the ability of BAY x 7195 aerosol to inhibit leukotriene-D-4 (LTD(4)) induced bronchoconstriction in healthy volunteers. Using a double-blind, placebo-controlled three way crossover design, volunteers received 2 and 4 mg of BAY x 7195 by means of a newly developedmetered dose dry powder inhaler. Bronchoprovocation with nebulized LTD(4) was performed 20 min and 8 h (n = 6 each) after drug administration. Specific airways conductance (SGaw) served to assess the airway's response. 3 BAY x 7195 aerosol was safe and well tolerated. Inhalationof the aerosol had no effect on baseline lung function. Only one volunteer reported cough following the inhalation of the 8 mg dose. 4 The pharmacokinetics of unchanged drug following the administration of BAYx 7195 aerosol were linear in the investigated range of doses and in general very similar to a previously investigated tablet formulation. Plasma-concentration vs time courses followed a two-compartment body model. Compared with oral administration of the tablet formulation absorption tended to be more rapid with the aerosol formulation. 5 Compared with placebo, 2 and 4 mg BAY x 7195 increased the concentration of LTD(4) needed to produce a 35% decrease in SGaw 20 min after drug administration by a mean (geometric) of 14.2 and 29.7 fold, respectively. For both doses only three volunteers showed a protective effect againstLTD(4) induced bronchoconstriction 8 h after drug administration. Individual shifts in the concentration-response curve ranged between 0.4 and 7.2 fold. 6 In conclusion, the present results suggest that BAY x 7195 aerosol is a safe and potent but short acting receptor antagonistof cysteinyl leukotrienes in man.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/11/20 alle ore 15:48:37