Generic Name and Formulations:
Riociguat 0.5mg, 1mg, 1.5mg, 2mg, 2.5mg; tabs.
Indications for ADEMPAS:
Treatment of 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, WHO functional class, and to delay clinical worsening.
May crush and mix with water or soft foods (eg, applesauce). Initially 1mg three times daily; if intolerant, consider starting at 0.5mg three times daily. Increase dose by 0.5mg (three times daily) at intervals of ≥2 weeks as tolerated (SBP >95mmHg and no hypotension); max 2.5mg three times daily. If intolerant at any time, decrease dose by 0.5mg three times daily. Smokers: consider titrating to doses >2.5mg three times daily; may require dose reduction after smoking cessation. Concomitant strong CYP450 and P-gp/BCRP inhibitors: initiate at 0.5mg three times daily.
Pregnancy. Concomitant nitrates or nitric oxide donors in any form, specific or non-specific PDE-5 inhibitors (eg, sildenafil, tadalafil, vardenafil, dipyridamole, theophylline). Pulmonary hypertension associated with idiopathic interstitial pneumonias (PH-IIP).
Embryo-fetal toxicity. In females of reproductive potential, exclude pregnancy prior to starting, monthly during, and for 1 month after treatment discontinuation; use effective methods of contraception during and for 1 month after last dose. Risk of hypotension or ischemia in hypovolemia, severe left ventricular outflow obstruction, resting hypotension, autonomic dysfunction; consider dose reduction if signs/symptoms occur. Bleeding risk. Pulmonary veno-occlusive disease: not recommended; discontinue if confirmed. Severe hepatic (Child-Pugh C) or renal impairment (CrCl <15mL/min), or on dialysis: not recommended. Nursing mothers: not recommended.
See Contraindications. Potentiated by strong CYP450 and P-gp/BCRP inhibitors (eg, ketoconazole, itraconazole, ritonavir; see Adults), antihypertensives; monitor for hypotension. Antagonized by smoking (see Adults). May be antagonized by strong CYP3A inducers (eg, rifampin, phenytoin, carbamazepine, phenobarbital, St. John’s Wort). Separate dosing of antacids by ≥1hr of riociguat. Discontinue sildenafil ≥24hrs, tadalafil ≥48hrs before starting treatment. Discontinue riociguat ≥24hrs before starting phosphodiesterase-5 (PDE-5) inhibitor; monitor.
Soluble guanylate cyclase (sGC) stimulator.
Headache, dyspepsia/gastritis, dizziness, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, constipation.
For all female patients: available only through the Adempas REMS program. To enroll call (855) 4ADEMPAS or www.AdempasREMS.com.