Comparative safety and tolerability of endothelin receptor antagonists in pulmonary arterial hypertension

Drug Safety : an International Journal of Medical Toxicology and Drug Experience
Meghan AversaJohn Granton

Abstract

Pulmonary arterial hypertension (PAH) is a condition that leads to progressive right heart failure and death unless recognized and treated early. Endothelin, a potent endogenous vasoconstrictor, has been identified as an important mediator of PAH. Endothelin receptor antagonists (ERAs) have been associated with an improvement in exercise capacity and time to clinical worsening in patients with Group 1 PAH, and three different ERAs are currently approved for use in this population: bosentan, ambrisentan, and macitentan. While all three ERAs are generally well-tolerated, they each have important adverse effects that need to be recognized and monitored. In particular, they may cause anemia, peripheral edema, and mild cardiac, respiratory, neurologic, and gastrointestinal adverse effects to varying degrees. Although bosentan increases a patient's risk of developing liver transaminitis, ambrisentan and macitentan do not appear to confer the same risk of hepatotoxicity at this time. Important drug-drug interactions, particularly involving other drugs metabolized via the cytochrome P450 pathway, are important to recognize when prescribing ERAs. In this review, we provide a brief overview of the current state of knowledge as it relates...Continue Reading

References

Jul 31, 1992·Biochemical and Biophysical Research Communications·M ClozelR Osterwalder
Jun 17, 1993·The New England Journal of Medicine·A GiaidD J Stewart
Aug 12, 1999·European Journal of Pharmacology·T MasakiY Okamoto
Apr 5, 2000·The Journal of Clinical Investigation·C E GariepyM Yanagisawa
Mar 22, 2002·The New England Journal of Medicine·Lewis J RubinGerald Simonneau
May 10, 2002·Journal of Cardiovascular Pharmacology and Therapeutics·Nick H S Kim, Lewis J Rubin
Jan 11, 2003·Journal of Clinical Pharmacology·Paul L M van GiersbergenJasper Dingemanse
Jun 15, 2004·Journal of the American College of Cardiology·Marc HumbertMarlene Rabinovitch
Dec 1, 2004·Clinical Pharmacokinetics·Jasper Dingemanse, Paul L M van Giersbergen
Mar 8, 2005·American Journal of Respiratory and Critical Care Medicine·Martin R WilkinsJ Simon R Gibbs
Aug 2, 2005·Journal of the American College of Cardiology·Nazzareno GaliéLewis J Rubin
Oct 20, 2005·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·Eleanor S SegalCinda van Lierop
Feb 4, 2006·American Journal of Respiratory and Critical Care Medicine·Marc HumbertGérald Simonneau
May 16, 2006·Journal of the American College of Cardiology·Robyn J BarstUNKNOWN STRIDE-2 Study Group
Jun 28, 2006·Circulation·Nazzareno GalièUNKNOWN Bosentan Randomized Trial of Endothelin Antagonist Therapy-5 (BREATHE-5) Investigators
Mar 16, 2007·The European Respiratory Journal·A J PeacockS Stewart
May 17, 2007·The European Respiratory Journal·M HumbertM M Hoeper
Jul 31, 2007·International Journal of Cardiology·Michael A GatzoulisUNKNOWN BREATHE-5 Investigators
Nov 28, 2007·European Journal of Clinical Pharmacology·Gary BurgessJasper Dingemanse
May 29, 2008·Circulation·Nazzareno GalièUNKNOWN Ambrisentan in Pulmonary Arterial Hypertension, Randomized, Double-Blind, Placebo-Controlled, Multicenter, Efficacy Studies
Sep 12, 2008·American Journal of Physiology. Renal Physiology·Yuqiang GeDonald E Kohan
Nov 17, 2009·Journal of the American College of Cardiology·Ronald J OudizUNKNOWN ARIES Study Group
Feb 9, 2011·Expert Opinion on Drug Metabolism & Toxicology·Mitchell S BuckleyJeremy P Feldman
Oct 28, 2011·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·Zahra HanaiziFrancesco Pignatti
May 15, 2012·Journal of the American College of Cardiology·Ori Ben-YehudaTobias Peschel
Jun 2, 2012·The European Respiratory Journal·Laurent SavaleOlivier Sitbon
Aug 4, 2012·The American Journal of Cardiology·Shelley ShapiroDonald E Kohan
Aug 31, 2012·Therapeutic Advances in Respiratory Disease·Michele D'Alto
Dec 13, 2012·Circulation Research·Jayan NagendranEvangelos D Michelakis
Aug 30, 2013·The New England Journal of Medicine·Tomás PulidoUNKNOWN SERAPHIN Investigators
Dec 4, 2013·Drugs·Trina Patel, Kate McKeage
Dec 21, 2013·Journal of the American College of Cardiology·Gerald SimonneauRogiero Souza
Dec 21, 2013·Journal of the American College of Cardiology·Nazzareno GalièAnne Keogh

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Citations

Nov 26, 2015·Expert Review of Respiratory Medicine·Nathan Hambly, John Granton
Sep 2, 2016·American Journal of Cardiovascular Drugs : Drugs, Devices, and Other Interventions·Gillian M Keating
Sep 7, 2016·Therapeutic Advances in Respiratory Disease·Stella S HahnGulrukh Zaidi
Apr 6, 2017·Journal of Clinical Pharmacology·Milena IssacPatricia N Sidharta
May 18, 2019·Journal of Sleep Research·Carolina Gonzaga CarvalhoClodagh M Ryan
Jul 9, 2020·Pediatric Critical Care Medicine : a Journal of the Society of Critical Care Medicine and the World Federation of Pediatric Intensive and Critical Care Societies·Kevin D HillChristoph P Hornik
Jun 1, 2018·Canadian Respiratory Journal : Journal of the Canadian Thoracic Society·Su-Gang GongCai-Cun Zhou
May 11, 2017·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Ranjeet Prasad DashNuggehally R Srinivas
Aug 1, 2018·Frontiers in Physiology·Victor Segura-IbarraElvin Blanco
Aug 25, 2021·Pulmonary Pharmacology & Therapeutics·Rosario RossiGiuseppe Boriani

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