Riociguat

What it is and how it works

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.

Mechanism class: Guanylate Cyclase Stimulators

Indications

Adempas is a soluble guanylate cyclase (sGC) stimulator 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. • Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise capacity, improve WHO functional class and to delay clinical worsening. Chronic-Thromboembolic Pulmonary Hypertension Adempas 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 . Pulmonary Arterial Hypertension Adempas 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 Adempas monotherapy or in combination with endothelin receptor antagonists or prostanoids.

Dosage and administration (summary)

• Initiate treatment at 1 mg taken three times a day. • For patients who may not tolerate the hypotensive effect of Adempas, consider a starting dose of 0.5 mg, three times a day. • Increase dosage by 0.5 mg at intervals of no sooner than 2-weeks as tolerated to a maximum of 2.5 mg three times a day. • Tablets may be crushed and mixed with water or soft foods for patients who have difficulty swallowing. Recommended Dosage in Adult Patients The recommended starting dosage is 1 mg taken 3 times a day. For patients who may not tolerate the hypotensive effect of Adempas, consider a starting dose of 0.5 mg taken three times a day.

Contraindications

• Pregnancy • Use with nitrates or nitric oxide donors in any form ( 4.2 , 7.1 ) • Use with PDE inhibitors ( 2.6 , 4.3 , 7.1 ) • Patients with concomitant use of other soluble guanylate cyclase (sGC) stimulators. ( 4.4 , 7.1 ) • Pulmonary hypertension associated with idiopathic interstitial pneumonias (PH-IIP) Pregnancy Use of Adempas is contraindicated in patients who are pregnant .

Warnings and precautions

• Symptomatic hypotension • Bleeding • Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment Embryo-Fetal Toxicity Based on data from animal reproduction studies, Adempas may cause fetal harm when administered to a pregnant patient and is contraindicated during pregnancy. The available human data for riociguat do not establish the presence or absence of major birth defects related to the use of Adempas. Counsel patients who can become pregnant on the potential risk to a fetus. Exclude pregnancy prior to initiation of treatment with Adempas.

Pregnancy

Pregnancy Risk Summary Based on data from animal reproduction studies, Adempas may cause fetal harm, including birth defects and fetal death, and miscarriage when administered to a pregnant patient and is contraindicated during pregnancy .

Storage and supply

How Supplied Adempas (riociguat) tablets are film-coated, round, and debossed with the "Bayer cross" on one side. Color Debossing Side 2 NDC 50419-xxx-xx Bottle of 9 Bottle of 90 Blister of 42 0.5 mg White R 250-91 250-01 250-03 1 mg Pale yellow 1 R 251-91 251-01 251-03 1.5 mg Yellow-orange R 252-91 252-01 252-03 2 mg Pale orange 2 R 253-91 253-01 …

Source: Riociguat (Adempas) — US FDA prescribing information, 2026-08-13, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.