Generic Name and Formulations:
Riociguat 0.5mg, 1mg, 1.5mg, 2mg, 2.5mg; tabs.

Company:
Bayer Healthcare Pharmaceuticals Inc.
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.

Adult:
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.

Children:
Not established.

Contraindications:
Pregnancy (Cat. X). Concomitant nitrates or nitric oxide donors in any form, specific or non-specific phosphodiesterase (PDE) inhibitors (eg, sildenafil, tadalafil, vardenafil, dipyridamole, theophylline).

Warnings/Precautions:
In females of reproductive potential, exclude pregnancy prior to starting, monthly during, and for 1 month after treatment discontinuation; must use acceptable methods of contraception. 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.

Interactions:
See Contraindications. Potentiated by strong CYP450 and P-gp/BCRP inhibitors (eg, ketoconazole, itraconazole, ritonavir), antihypertensives; monitor for hypotension. Antagonized by smoking. May be antagonized by strong CYP3A inducers (eg, rifampin, phenytoin, carbamazepine, phenobarbital, St. John’s Wort). Separate dosing of antacids by ≥1hr of riociguat.

Pharmacological Class:
Soluble guanylate cyclase (sGC) stimulator.

Adverse Reactions:
Headache, dizziness, dyspepsia/gastritis, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, constipation.

Note:
For all female patients: available only through the Adempas REMS program. To enroll call (855) 4ADEMPAS or www.AdempasREMS.com.

REMS:
YES

How Supplied:
Tabs—42, 90