Titre du document / Document title

Pharmacokinetic-pharmacodynamic profile of angiotensin II receptor antagonists

Auteur(s) / Author(s)

CSAJKA C. ; BUCLIN T. ; BRUNNER H. R. ; BIOLLAZ J. ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

Divisions de Pharmacologie Clinique et d'Hypertension, Département de Médecine, Centre Hospitalier Universitaire Vaudois, Lausanne, SUISSE

Résumé / Abstract

The pharmacokinetic and pharmacodynamic properties of nonpeptide angiotensin antagonists in humans are reviewed in this paper. Representatives of this new therapeutic class share common features: lipophilia, intermediate bioavailability, high affinity for plasma proteins and liver metabolism; some have active metabolites. Angiotensin II antagonists block the blood pressure response to exogenous angiotensin II in healthy volunteers, decrease baseline blood pressure in both normal and hypertensive patients, produce a marked rise in plasma renin activity and endogenous angiotensin II and increase renal blood flow without altering glomerular filtration rate. These effects are dose-dependent, but their time course varies between the drugs owing to pharmacokinetic and pharmacodynamic differences. Additionally, the extent of blood pressure reduction is dependent on physiological factors such as sodium and water balance. The characterisation of their pharmacokinetic-pharmacodynamic relationships deserves further refinement for designing optimal therapeutic regimens and proposing dosage adaptations in specific conditions.

Revue / Journal Title

Clinical pharmacokinetics   ISSN 0312-5963   CODEN CPKNDH 

Source / Source

1997, vol. 32, n^o1, pp. 1-29 (112 ref.)

Langue / Language

Anglais

Editeur / Publisher

Adis international, Auckland, NOUVELLE-ZELANDE  (1976) (Revue)

Mots-clés anglais / English Keywords

Angiotensin antagonist ; Angiotensin II ; Non peptide compound ; Antihypertensive agent ; Pharmacokinetics ; Biological activity ; Hemodynamics ; Human ; Review ; Losartan ; Valsartan ; Pharmacokinetic pharmacodynamic relationship ;

Mots-clés français / French Keywords

Antagoniste angiotensine ; Angiotensine II ; Composé non peptide ; Antihypertenseur ; Pharmacocinétique ; Activité biologique ; Hémodynamique ; Homme ; Article synthèse ; Losartan ; Valsartan ; TCV 116 ; Relation pharmacocinétique pharmacodynamie ;

Mots-clés espagnols / Spanish Keywords

Antagonista angiotensina ; Angiotensina II ; Compuesto no péptido ; Antihipertensivo ; Farmacocinética ; Actividad biológica ; Hemodinámica ; Hombre ; Artículo síntesis ; Losartán ; Valsartán ;

Localisation / Location

INIST-CNRS, Cote INIST : 15599, 35400006228259.0010