Riociguat (micronized)
Indications
Riociguat (micronized) is used for:
Riociguat is indicated for the treatment of adults with persistent/recurrent chronic thromboembolic pulmonary hypertension (cteph), (who group 4) after surgical treatment, or inoperable cteph, to improve exercise capacity and who functional class. Riociguat is indicated for the treatment of adults with pulmonary arterial hypertension (pah), (who group 1), to improve exercise capacity, who functional class and to delay clinical worsening. Efficacy was shown in patients on riociguat monotherapy or in combination with endothelin receptor antagonists or prostanoids. Studies establishing effectiveness included predominately patients with who functional class ii=iii and etiologies of idiopathic or heritable pah (61%) or pah associated with connective tissue diseases (25%)
Adult Dose
Child Dose
Renal Dose
Administration
Contra Indications
Precautions
Pregnancy-Lactation
Interactions
Adverse Effects
Side effects of Riociguat (micronized) :
Mechanism of Action
Riociguat is a stimulator of soluble guanylate cyclase (sgc), an enzyme in the cardiopulmonary system and the receptor for nitric oxide (no). When no binds to sgc, the enzyme catalyzes synthesis of the signaling molecule cyclic guanosine monophosphate (cgmp). Intracellular cgmp plays an important role in regulating processes that influence vascular tone, proliferation, fibrosis and inflammation. Pulmonary hypertension is associated with endothelial dysfunction, impaired synthesis of nitric oxide and insufficient stimulation of the no-sgc-cgmp pathway. Riociguat has a dual mode of action. It sensitizes sgc to endogenous no by stabilizing the no-sgc binding. Riociguat also directly stimulates sgc via a different binding site, independently of no. Riociguat stimulates the no-sgc-cgmp pathway and leads to increased generation of cgmp with subsequent vasodilation