Tezosentan in the management of decompensated heart failure.
Author(s): Cheng JW(1).
Affiliation(s): Author information:
(1)Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island
University, New York, NY 10029, USA. Judy.cheng@liu.edu
Publication date & source: 2005, Cardiol Rev. , 13(1):28-34
Decompensated heart failure continues to significantly impact the economics of
our healthcare system. In recent years, the focus on management of decompensated
heart failure has changed from solely improving hemodynamics to modifying
neurohormones. Endothelin (ET) is one of the important mediators in heart
failure. This article reviews the clinical pharmacology, clinical efficacy, and
tolerability of tezosentan, a dual-action ET-1 receptor antagonist. Using the
search term tezosentan, a literature review was conducted to identify
peer-reviewed articles and abstracts in MEDLINE (1966 to April 2004) and Current
Content (1966 to April 2004) databases. Citations from available articles were
also reviewed for additional references. When given as an intravenous infusion,
tezosentan achieves steady-state concentration within the first 6 hours.
Tezosentan is excreted almost entirely through the bile (>95%) and has a terminal
elimination half-life of 3 hours. The side effects of tezosentan include
headache, nausea, and hypotension. Clinical studies demonstrated mixed results
for tezosentan regarding its efficacy and tolerability in the management of
decompensated heart failure. The role or tezosentan in treating heart failure is
yet to be defined.
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