Tezosentan in the Treatment of Acute Heart Failure

OBJECTIVE: To evaluate the pharmacology, pharmacokinetics, clinical efficacy, and tolerability of tezosentan, a new intravenous endothelin (ET)-1 receptor antagonist. DATA SOURCES: Literature was identified through a MEDLINE search (1990–June 2003) using the search terms endothelin-1, heart failure,...

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Bibliographic Details
Published in:The Annals of pharmacotherapy 2003-12, Vol.37 (12), p.1877-1883
Main Authors: Tovar, John M, Gums, John G
Format: Article
Language:English
Subjects:
Acute Disease
Animals
Biological and medical sciences
Cardiotonic agents
Cardiovascular system
Clinical Trials as Topic - statistics & numerical data
Heart Failure - blood
Heart Failure - drug therapy
Humans
Medical sciences
Pharmacology. Drug treatments
Pyridines - blood
Pyridines - pharmacology
Pyridines - therapeutic use
Tetrazoles - blood
Tetrazoles - pharmacology
Tetrazoles - therapeutic use
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Summary:OBJECTIVE: To evaluate the pharmacology, pharmacokinetics, clinical efficacy, and tolerability of tezosentan, a new intravenous endothelin (ET)-1 receptor antagonist. DATA SOURCES: Literature was identified through a MEDLINE search (1990–June 2003) using the search terms endothelin-1, heart failure, RITZ, and tezosentan. References listed in articles and abstracts from scientific meetings were also used. STUDY SELECTION AND DATA EXTRACTION: English-language literature reporting controlled animal and human clinical studies was reviewed to evaluate the pharmacology, pharmacokinetics, therapeutic use, and adverse effects of tezosentan. Clinical trials selected for inclusion were limited to those with human subjects and included data from animal studies if human data were not available. DATA SYNTHESIS: Tezosentan is a dual ET-1 receptor antagonist that has demonstrated efficacy in improving cardiac index and reducing pulmonary capillary wedge pressure in patients with acute, decompensated heart failure. Following infusion, tezosentan's plasma concentration approaches steady-state within the first 6 hours, with a relatively small volume of distribution (17 L) and clearance (39 L/h) that are dose independent. Tezosentan is excreted almost entirely unchanged via the bile (>95%), with the rest (
ISSN:1060-0280
1542-6270
DOI:10.1345/aph.1D080