Drug reference

Riociguat

Vasodilator · Pulmonary arterial hypertension treatment

VasodilatorPulmonary arterial hypertension treatment

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

—

not curated

Top interactionssee all 12 →

Pde5 InhibitorsContraindicatedTextbookG&G 14e · p700
Isosorbide MononitrateContraindicatedDatabaseKimi deep-research + Cla
NicorandilContraindicatedDatabase
SildenafilContraindicatedDatabaseKimi deep-research + Cla

Mechanism

Riociguat, a small-molecule activator of soluble guanylyl cyclase, increases cGMP independently of nitric oxide. This action reduces pulmonary vascular pressure and increases exercise duration.

Indications

Pulmonary arterial hypertensionChronic thromboembolic pulmonary hypertensionpulmonary hypertensionPAHCTEPHmoderate PAH (functional class II–III)

Dosing

Adult: reduce blood pressure rapidly after the ﬁrst dose and should be introduced with caution. Doxazosin, indoramin p. 827, and terazosin have properties similar to those of prazosin. Hypertension 155 Alpha-blockers can be used with other antihypertensive drugs in the treatment of resistant hypertension. . receiving high-dose vasodilator therapy; . known renovascular disease.…

Pharmacokinetics

Half-life

12 h (in PAH patients), 7 h (in healthy subjects)

Bioavailability

Food does not affect bioavailability.

Metabolism

Metabolized by CYPs 1A1, 3A, 2C8, and 2J2. CYP1A1 forms the major active metabolite M1, which is then converted to an inactive N-glucuronide.

Contraindications

Concurrent use of nitroglycerin

Side effects

Common

headachedyspepsiadizzinessnauseadiarrheavomitinganemiarefluxconstipationpalpitationsnasal congestionepistaxisdysphagiaabdominal distensionperipheral edemasyncope

Serious