Riociguat Dosage

Medically reviewed by Drugs.com. Last updated on Feb 8, 2024.

Usual Adult Dose for Pulmonary Hypertension

Initial dose: 1 mg orally 3 times a day
Maintenance dose: Titrate by 0.5 mg orally 3 times a day no more frequently than every 2 weeks, up to the highest tolerated dose
Maximum dose: 2.5 mg orally 3 times a day

Comments:

• Consider an initial dose of 0.5 mg orally 3 times a day for patients who may not tolerate hypotensive effects.
• Dose increases should only occur if systolic blood pressure is at least 95 mmHg and the patient has no signs/symptoms of hypotension.

Uses:

• For the 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
• As monotherapy, or in combination with endothelin receptor antagonists or prostanoids, for the treatment of pulmonary arterial hypertension (PAH) WHO Group 1, to improve exercise capacity, WHO functional class, and to delay clinical worsening

Renal Dose Adjustments

CrCl greater than 15 mL/min: Data not available
CrCl less than 15 mL/min OR on dialysis: Not recommended; safety/efficacy have not been established.

Liver Dose Adjustments

Mild to moderate liver dysfunction (Child-Pugh A or B): Data not available
Severe liver dysfunction (Child-Pugh C): Not recommended; safety/efficacy have not been established.

Dose Adjustments

Hypotension: Decrease the dosage by 0.5 mg orally 3 times a day if hypotensive symptoms occur at any time during treatment.

Concomitant use with strong CYP450 and P-gp/BCRP inhibitors (e.g., azole antifungals [ketoconazole, itraconazole] or protease inhibitors [ritonavir]): Consider a starting dose of 0.5 mg orally 3 times daily. Monitor for hypotension on initiation and during treatment.

Patients who smoke: Consider titrating to dosages higher than 2.5 mg orally 3 times a day, if tolerated. A dose decrease may be necessary in patients who stop smoking.

Precautions

The US FDA requires a Risk Evaluation and Mitigation Strategy (REMS) for riociguat. It includes elements to assure safe use and an implementation system. For additional information: http://www.accessdata.fda.gov/scripts/cder/rems/index.cfm

US BOXED WARNING:

• EMBRYOFETAL TOXICITY: Do not administer this drug to a pregnant female because it may cause fetal harm. Use is contraindicated in pregnant women.
• PREGNANCY TESTING: Female patients of reproductive potential must have a negative pregnancy test prior to starting treatment, monthly during treatment, and for 1 month after discontinuation of treatment. Females of childbearing potential must use effective methods of contraception during treatment and for 1 month after discontinuation.
• REMS PROGRAM: Female patients can only receive this drug through restricted distribution (i.e., REMS) program.

CONTRAINDICATIONS:

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

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Patients on dialysis: Not recommended.

Comments:

• Due to the extensive plasma protein binding this drug is not expected to be dialyzable.

Other Comments

Administration advice:

• For oral use
• Before starting treatment, obtain a negative pregnancy test in females of reproductive potential.
• Administer with or without food.
• For patients unable to swallow whole tablets, crush or mix with water or soft foods (e.g., applesauce) immediately before administration.
• If a dose is missed, continue with the next regularly scheduled dose.
• If therapy is interrupted for 3 days or more, re-titration is recommended.

Recommendations for transitioning between therapies:

• From sildenafil: Discontinue sildenafil at least 24 hours prior to administering this drug.
• From tadalafil: Discontinue tadalafil at least 48 hours prior to administering this drug. Consider an initial starting dose of 0.5 mg orally 3 times a day in patients at risk of hypotension.
• To PDE5-inhibitor: Discontinue this drug at least 24 hours prior to administering a PDE5-inhibitor.

Storage requirements:

• Store at 25C (77F); excursions are permitted from 15C to 30C (59F to 86F).

General:

• Clinical studies in patients with PAH predominately included those with WHO functional class II to III and etiologies of idiopathic or heritable PAH (61%) or PAH associated with connective tissue diseases (25%).
• For further information on the restricted distribution program and for a list of certified dispensing pharmacies, visit www.AdempasREMS.com or call 1-855-4 ADEMPAS.

Monitoring:

• Cardiovascular: For hypotension (during initiation and while on therapy, especially with use of strong CYP450 and P-gp/BCRP inhibitors or if transitioning from other therapies for pulmonary hypertension)
• Reproductive: Pregnancy testing (prior to therapy, monthly during treatment, and for 1 month after discontinuation)

Patient advice:

• Read the US FDA-approved patient labeling (Medication Guide).
• Inform your health care provider of all current and new medications to avoid potential drug interactions.
• Report any signs of hemoptysis to your health care provider.
• Tell your health care provider if you start or stop smoking.
• Avoid use of antacids within 1 hour of taking this drug.
• Recognize that this drug may cause dizziness and potentially impair the ability to drive or use machines.
• Female patients:
• This drug is only available to female patients through a restricted REMS program; enrollment is required.
• Comply with pregnancy testing and contraception requirements.
• Understand the risk of fetal harm if this drug is used during pregnancy.
• Contact your health care provider immediately if pregnancy occurs or is suspected.
• Breastfeeding is not recommended during treatment.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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