Soluble guanylate cyclase (sGC) stimulator
Brand names: Adempas
Updated · Methodology
Second line
Riociguat is second-line for pulmonary arterial hypertension (PAH) and the only approved drug for chronic thromboembolic pulmonary hypertension (CTEPH) in inoperable patients or after endarterectomy. /ERS 2022 recommend it as alternative to PDE-5 inhibitors or in combination therapy. Dose titrated from 1 mg three times daily to maximum 2.5 mg three times daily.
Sources
ICD-10: I27.0 · ICD-11: BB01.0
Directly activates soluble guanylate cyclase independently of nitric oxide and simultaneously sensitises the enzyme to endogenous NO. Raises cGMP in pulmonary vascular smooth muscle, producing pulmonary artery vasodilation. Used for pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. Metabolised by CYP1A1 and CYP3A4.
Contraindicated in pregnancy due to teratogenicity (animal data). REMS program requires confirmed contraception in women of childbearing age.
Breastfeeding not recommended.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
4 pairs found. Sorted from critical to minor.
Mechanism
Riociguat activates sGC independently of NO. Nitrate adds NO – synergistic systemic hypotension. Adempas Section 4.3.
Symptoms
Severe hypotension.
Management
Combination contraindicated.
Mechanism
Riociguat activates sGC independently of NO. Nitrate adds NO – synergistic systemic hypotension. Section 4.3.
Symptoms
Severe hypotension.
Management
Combination contraindicated.
Sources
Mechanism
Both activate cGMP pathway. Synergistic hypotension. Adempas Section 4.3 strict contraindication.
Symptoms
Severe hypotension.
Management
Combination contraindicated.
Sources
Mechanism
Both raise cGMP. Synergistic systemic hypotension. Adempas Section 4.3 strict contraindication.
Symptoms
Severe hypotension, syncope.
Management
Combination contraindicated.
Sources
Verbatim lines from the interaction sections, in the language of the label
«CONTRAINDICATIONS: • Use with nitrates or nitric oxide donors in any form ( 4.2 , 7.1 )»FDA, section 4 · Open on DailyMed
«Phosphodiesterase Inhibitors: Concomitant administration of Adempas with specific PDE-5 inhibitors (such as sildenafil, tadalafil, or vardenafil) or nonspecific PDE-5 inhibitors (such as dipyridamole…»FDA, section 4 · Open on DailyMed
«Phosphodiesterase Inhibitors: Concomitant administration of Adempas with specific PDE-5 inhibitors (such as sildenafil, tadalafil, or vardenafil) or nonspecific PDE-5 inhibitors (such as dipyridamole…»FDA, section 4 · Open on DailyMed
«Phosphodiesterase Inhibitors: Concomitant administration of Adempas with specific PDE-5 inhibitors (such as sildenafil, tadalafil, or vardenafil) or nonspecific PDE-5 inhibitors (such as dipyridamole…»FDA, section 4 · Open on DailyMed
«Phosphodiesterase Inhibitors: Concomitant administration of Adempas with specific PDE-5 inhibitors (such as sildenafil, tadalafil, or vardenafil) or nonspecific PDE-5 inhibitors (such as dipyridamole…»FDA, section 4 · Open on DailyMed
«Phosphodiesterase Inhibitors: Concomitant administration of Adempas with specific PDE-5 inhibitors (such as sildenafil, tadalafil, or vardenafil) or nonspecific PDE-5 inhibitors (such as dipyridamole…»FDA, section 4 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Antacids: Antacids such as aluminum hydroxide/FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Antacids: Antacids such as aluminum hydroxide/FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Strong CYP and P-gp/FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Strong CYP and P-gp/FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Strong CYP and P-gp/FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Strong CYP and P-gp/FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Strong CYP3A inducers: Strong inducers of CYP3A (for example, rifampin, phenytoin, carbamazepine, phenobarbital or St. John's Wort) may significantly reduce…»FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Strong CYP3A inducers: Strong inducers of CYP3A (for example, rifampin, phenytoin, carbamazepine, phenobarbital or St. John's Wort) may significantly reduce…»FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Strong CYP3A inducers: Strong inducers of CYP3A (for example, rifampin, phenytoin, carbamazepine, phenobarbital or St. John's Wort) may significantly reduce…»FDA, section 7 · Open on DailyMed
«Pharmacokinetic Interactions with Adempas: Strong CYP3A inducers: Strong inducers of CYP3A (for example, rifampin, phenytoin, carbamazepine, phenobarbital or St. John's Wort) may significantly reduce…»FDA, section 7 · Open on DailyMed
«CONTRAINDICATIONS: Do not use isosorbide dinitrate in patients who are taking the soluble guanylate cyclase stimulator riociguat. Concomitant use can cause hypotension.»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Do not use isosorbide mononitrate in patients who are taking the soluble guanylate cyclase stimulator riociguat. Concomitant use can cause hypotension.»FDA, section 4 · Open on DailyMed
«Durante el tratamiento con nitratos, no se debe usar riociguat, un estimulador de la guanilato ciclasa soluble (ver sección 4.5).»AEMPS, section 4.3 · Open on CIMA
«PDE-5-Inhibitors and sGC-Stimulators: Do not use nitroglycerin sublingual tablets in patients who are taking the soluble guanylate cyclase stimulators, such as riociguat. Concomitant use can cause…»FDA, section 4 · Open on DailyMed
«La administración conjunta de inhibidores de la PDE5, incluyendo sildenafilo, con estimuladores de la guanilato-ciclasa, como riociguat, está contraindicado ya que puede producir hipotensión…»AEMPS, section 4.3 · Open on CIMA
«Concomitant Guanylate Cyclase (GC) Stimulators: Do not use sildenafil tablets in patients who are using a GC stimulator, such as riociguat. PDE5 inhibitors, including sildenafil tablets, may…»FDA, section 4 · Open on DailyMed
«La administración conjunta de inhibidores de la fosfodiesterasa tipo 5 (PDE5), incluyendo tadalafilo, con estimuladores de la guanilato ciclasa, como riociguat, está contraindicada ya que puede…»AEMPS, section 4.3 · Open on CIMA
«CONTRAINDICATIONS: Administration with guanylate cyclase (GC) stimulators, such as riociguat ( 4.3 ).»FDA, section 4 · Open on DailyMed
«La administración conjunta de inhibidores de la PDE5, incluyendo vardenafilo, con estimuladores de la guanilato ciclasa, como riociguat, está contraindicada ya que puede producir hipotensión…»AEMPS, section 4.3 · Open on CIMA
«CONTRAINDICATIONS: Administration with guanylate cyclase (GC) stimulators, such as riociguat ( 2.4 , 4.2 )»FDA, section 4 · Open on DailyMed
«Antagonistas de la endotelina: Las concentraciones séricas pueden aumentar debido a la inhibición de CYP3A y P-gp por Ritonavir. No se recomienda la administración conjunta de riociguat con Ritonavir…»AEMPS, section 4.5 · Open on CIMA
«Antivirales para uso sistémico: Riociguat, Tadalafilo (hipertensión pulmo nar)»AEMPS, section 4.5 · Open on CIMA
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Riociguat is evaluated for the following indications with varying evidence strength: Pulmonary arterial hypertension (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Riociguat (≥ 1 in 100): Headache, Dizziness, Dyspepsia, Peripheral edema, Hypotension. See the Safety section for uncommon and serious reactions.
Contraindicated in pregnancy due to teratogenicity (animal data). REMS program requires confirmed contraception in women of childbearing age.
Breastfeeding not recommended.
Riociguat is contraindicated in: Pregnancy; Combination with any nitrate or NO donor (fatal hypotension); Combination with PDE-5 inhibitors (sildenafil, tadalafil, vardenafil); Severe hepatic impairment; Systolic BP below 95 mmHg. Full list in the Safety section.
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