Riociguat

Class
Vasoactive agents
Subclass
Soluble guanylyl cyclase stimulators
Substance name
Riociguat
Brand names
Adempas®
Common formulations
Film-coated tablet
Dosage and administration
Adults patients
Chronic thromboembolic pulmonary hypertension
•
Start at: 1 mg PO TID
•
Maintenance: 1-2.5 mg PO TID
•
Maximum: 7.5 mg per day
Consider starting at 0.5 mg TID if 1 mg three times daily is not tolerated. Titrate by 0.5 mg three times daily no sooner than 2 weeks.
Pulmonary arterial hypertension
•
Start at: 1 mg PO TID
•
Maintenance: 1-2.5 mg PO TID
•
Maximum: 7.5 mg per day
Consider starting at 0.5 mg TID if 1 mg three times daily is not tolerated. Titrate by 0.5 mg three times daily no sooner than 2 weeks.
Pulmonary hypertension in patients with systemic sclerosis • Off-label
•
Start at: 1 mg PO TID
•
Maintenance: 2.5 mg PO TID
Indications for use
Labeled indications
Adults
•
Treatment of chronic thromboembolic pulmonary hypertension
•
Treatment of pulmonary arterial hypertension
Off-label indications
Adults
•
Treatment of pulmonary hypertension in patients with systemic sclerosis
Safety risks
Boxed warnings
Fetal toxicity
•
Do not use in pregnant patients. Discontinue riociguat as soon as possible when pregnancy is detected.
Contraindications
Hypersensitivity to riociguat or its components
Pulmonary hypertension associated with idiopathic interstitial pneumonia
Pulmonary veno-occlusive disease
Concomitant use of nitrates, nitric oxide donors, sGC stimulators, PDE5 inhibitors, or nonselective phosphodiesterase inhibitors, such as dipyridamole or theophylline
•
Do not administer riociguat within 24 hours of sildenafil or 24 hours before or within 48 hours after tadalafil.
Warnings and precautions
Bleeding
•
Maintain a high level of suspicion, as riociguat has been associated with an increased risk of serious bleeding.
Hypotension
•
Use caution in patients with volume depletion, resting hypotension, severe LV outflow obstruction, autonomic dysfunction, or taking antihypertensive medications or strong CYP, P-glycoprotein, or BCRP inhibitors.
Specific populations
Renal impairment
CrCl ≥ 15 mL/min
•
No guidance available.
CrCl < 15 mL/min
•
Do not use. Safety and efficacy unknown.
Renal replacement therapy
Any modality
•
Do not use. Safety and efficacy unknown.
Hepatic impairment
Child-Pugh A (mild)
•
Use acceptable. No dose adjustment required.
Child-Pugh B (moderate)
•
Use acceptable. No dose adjustment required.
Child-Pugh C (severe)
•
Do not use.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: X
•
Do not use. Evidence of fetal harm in humans. Obtain a negative pregnancy test before initiation, monthly during treatment, and for 1 month after discontinuation. Advise adequate methods of contraception during and for 1 month after discontinuing treatment.
Breastfeeding
Do not use during breastfeeding.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
•
Gastritis, diarrhea, dizziness, dyspepsia, headache, nausea
Common 1-10%
•
Anemia, bleeding, gastroesophageal reflux disease, hypotension, constipation, hemoptysis, vomiting
Unknown frequency
•
Palpitations, peripheral edema, dysphagia, bloating, nosebleed, nasal congestion
Interactions
Drug(s)
Check Interactions
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