Riociguat and sildenafil for pulmonary hypertension: similarity and difference
https://doi.org/10.18093/0869-0189-2016-26-1-85-91
Abstract
Last decades, several drugs for treatment of pulmonary hypertension have been implemented in clinical practice. Sildenafil selectively inhibits phosphodiesterase-5 (PDE-5), increases cyclic guanosine monophosphate (cGMP) level in the pulmonary vascular wall leading to vasodilation, inhibition of proliferation and other specific effects. Sildenafil is indicated as single therapy and in sequential combination therapy of pulmonary arterial hypertension (PAH) (high-level evidence, high-class recommendation). However, therapeutic response on PDE-5 inhibitors is insufficient in a certain number of patients. Soluble guanylate cyclase (sGC) activators were proposed as a good alternative for such patients. Riociguat has dual mechanism of action: firstly, it is designed to increase cGMP biosynthesis via direct activation of sGC; this pathway resembles that of nitric oxide (NO) but is independent on NO. Secondly, riociguat can sensitise sGC to NO. Riociguat is indicated as single therapy and in sequential combination therapy of PAH and to treatment of chronic thromboembolic pulmonary hypertension (high-level evidence, high-class recommendation). A clinical trial RESPITE has been initiated in February, 2014, which is intended to evaluate efficacy of switching PAH patients from PDE-5 inhibitors to riociguat. Potential advantage of this drug is the mechanism independent of NO and of other PDE enzyme isoforms. Whether this advantage is clinically significant, remains to be seen, probably, in the RESPITE trial.
About the Authors
A. A. Shmal'ts
A.N.Bakulev Federal Academic Center of Cardiovascular Surgery, Healthcare Ministry of Russia: 135, Rublevskoe roadway, Moscow, 121552, Russia;
Russian State Medical Postgraduate Academy, Healthcare Ministry of Russia: 2 / 1, Barrikadnaya str., Moscow, 123995, Russi
Russian Federation
Russian Federation
MD, Chief Scientist at Department of Surgery of Heart Diseases with Progressive Pulmonary Hypertension, A.N.Bakulev Federal Academic Center of Cardiovascular Surgery, Healthcare Ministry of Russia; Associate Professor at Department of Cardiovascular Surgery, Russian State Medical Postgraduate Academy, Healthcare Ministry of Russia; tel.: (495) 414-79-33;
S. V. Gorbachevskiy
A.N.Bakulev Federal Academic Center of Cardiovascular Surgery, Healthcare Ministry of Russia: 135, Rublevskoe roadway, Moscow, 121552, Russia;
Russian State Medical Postgraduate Academy, Healthcare Ministry of Russia: 2 / 1, Barrikadnaya str., Moscow, 123995, Russi
Russian Federation
Russian Federation
MD, Professor, Head of Department of Surgery of Heart Diseases with Progressive Pulmonary Hypertension, A.N.Bakulev Federal Academic Center of Cardiovascular Surgery, Healthcare Ministry of Russia; Professor at Department of Cardiovascular Surgery, Russian State Medical Postgraduate Academy, Healthcare Ministry of Russia; tel.: (495) 414-78-19
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Review
For citations:
Shmal'ts A.A., Gorbachevskiy S.V. Riociguat and sildenafil for pulmonary hypertension: similarity and difference. PULMONOLOGIYA. 2016;26(1):85-91. (In Russ.) https://doi.org/10.18093/0869-0189-2016-26-1-85-91
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