Soluble guanylate cyclase (sGC) stimulator
ATC code: C02KX05 (Riociguat)
Brand names
Adempas
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.
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.
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.
Mechanism
Both activate cGMP pathway. Synergistic hypotension. Adempas Section 4.3 strict contraindication.
Symptoms
Severe hypotension.
Management
Combination contraindicated.
Mechanism
Both raise cGMP. Synergistic systemic hypotension. Adempas Section 4.3 strict contraindication.
Symptoms
Severe hypotension, syncope.
Management
Combination contraindicated.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
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.
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.
FDA category X. 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.