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Riociguat

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Information about Riociguat

Riociguat is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension.

Liver safety of Riociguat

Riociguat has not been linked to significant serum enzyme elevations during therapy or to instances of clinically apparent acute liver injury.

Mechanism of action of Riociguat

Riociguat (rye" oh sig' ue at) is small molecular weight stimulator of soluble guanylate cyclase, an enzyme responsible for synthesis of cyclic guanine monophosphate (cyclic GMP), an important mediator of endothelial cell relaxation. By stimulating cyclic GMP, riociguat leads to relaxation of vascular smooth muscle cells, particularly in the pulmonary vasculature. In humans, riociguat induces pulmonary arterial vasodilation and reduces pulmonary artery pressure. In several clinical trials, prolonged therapy with riociguat has been shown to improve exercise capacity and pulmonary function in patients with severe idiopathic as well as chronic thromboembolic pulmonary arterial hypertension (PAH).

FDA approval information for Riociguat

Riociguat was approved for use in chronic idiopathic and thromboembolic PAH in 2013 and it is currently available in tablets of 0.5, 1.0, 1.5, 2.0 and 2.5 mg under the brand name Adempas. The recommended starting dose is 1 mg three times daily which can be increased in 0.5 mg amounts every two weeks based upon tolerance to a maximum of 2.5 mg thrice daily.

Side effects of Riociguat

Side effects are generally dose related and can include hypotension, syncope, dizziness, headache, diarrhea, gastrointestinal upset, nausea, vomiting and constipation, symptoms that are frequent with most vasodilator therapies. Rare, but potentially severe adverse reactions include pulmonary hemorrhage and fetal toxicity. Women of childbearing potential can receive riociguat only as a part of a risk evaluation and mitigation strategy (REMS) program that requires regular monitoring.


Pulmonary Disease Agents

  • Pulmonary Arterial Hypertension Agents

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