Riociguat

FDA label

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Titration Increase by 0.5 mg no sooner than every 2 weeks

Renal Not recommended if CrCl <15 mL/min or on dialysis

Hepatic Not recommended in severe (Child-Pugh C) hepatic impairment

Instructions

• May crush and mix with water or soft food (e.g., applesauce) if unable to swallow whole
• If interrupted for 3 days or more, re-titrate
• Smokers may require doses >2.5 mg TID; a dose decrease may be needed on smoking cessation
• Start 0.5 mg TID with strong CYP and P-gp/BCRP inhibitors (e.g., azole antifungals, HIV protease inhibitors)
• Separate from PDE5 inhibitors: stop sildenafil >=24 h and tadalafil >=48 h before starting; stop Adempas >=24 h before a PDE5 inhibitor

Available strengths

• tab 0.5, 1, 1.5, 2, 2.5 mg

Contraindications

• Pregnancy
• Concomitant nitrates or nitric oxide donors (e.g., amyl nitrite) in any form
• Concomitant PDE inhibitors (specific PDE-5 such as sildenafil, tadalafil, vardenafil; nonspecific such as dipyridamole, theophylline)
• Concomitant other soluble guanylate cyclase (sGC) stimulators
• Pulmonary hypertension associated with idiopathic interstitial pneumonias (PH-IIP)

Cautions

• Symptomatic hypotension (reduces blood pressure)
• Bleeding, including serious hemoptysis
• Pulmonary veno-occlusive disease - discontinue if pulmonary edema occurs

Adverse reactions

• Headache
• Dyspepsia/gastritis
• Dizziness
• Nausea
• Diarrhea
• Hypotension
• Vomiting
• Anemia
• GERD
• Constipation

Pregnancy Contraindicated; may cause fetal harm based on animal data.

Lactation Advise not to breastfeed during treatment.