riociguat at a glance
Medicine class
Soluble guanylate cyclase stimulator
Main role
Specialist treatment for selected forms of pulmonary hypertension
Form
Oral film-coated tablets
Food
Generally taken with or without food; consistent food timing is advised when prone to low blood pressure
What is riociguat used for?
The selected tablets are licensed for:
Adults with inoperable chronic thromboembolic pulmonary hypertension, or disease that persists or returns after surgery, with WHO functional class II–III.
Adults with pulmonary arterial hypertension and WHO functional class II–III, used alone or with an endothelin receptor antagonist.
Children and adolescents aged 6 to under 18 years with pulmonary arterial hypertension and WHO functional class II–III, used with an endothelin receptor antagonist.
How does riociguat work?
Riociguat sensitises soluble guanylate cyclase to nitric oxide and also stimulates the enzyme directly. This increases cyclic GMP signalling, relaxing pulmonary blood vessels and reducing resistance to blood flow through the lungs.
riociguat preparations and strengths
Tablet
Route: Oral
Strengths: 0.5 mg, 1.0 mg, 1.5 mg, 2.0 mg, 2.5 mg
How to take riociguat
Take riociguat exactly as directed by the specialist team. It can generally be taken with or without food, but people prone to low blood pressure should avoid switching between fed and fasting administration. A tablet may be crushed and mixed with water or soft food immediately before swallowing.
Do not change or stop treatment without speaking to the specialist team.
Tell the team if you start or stop smoking because this can change riociguat exposure.
Dizziness may affect driving, cycling or operating machinery.
riociguat side effects
Common or expected effects
- Headache or dizziness
- Indigestion, nausea, vomiting or diarrhoea
- Swelling of the limbs
- Low blood pressure
- Palpitations
- Nosebleeds or nasal congestion
- Abdominal discomfort, heartburn, constipation or bloating
- Anaemia
Get urgent medical advice
- Coughing up blood or bleeding from the lungs
- Fainting or severe symptoms of low blood pressure
- New or rapidly worsening breathlessness, which may indicate fluid in the lungs
riociguat in pregnancy
Riociguat is contraindicated during pregnancy because animal studies showed reproductive toxicity and placental transfer. Effective contraception is required for those who could become pregnant, and monthly pregnancy testing is recommended. Contact the specialist team promptly if pregnancy occurs or is suspected.
riociguat while breastfeeding
Riociguat should not be used during breastfeeding because human data are unavailable and serious effects in a breastfed child cannot be excluded. Feeding and treatment options require specialist discussion.
riociguat interactions
Check all prescribed, non-prescribed and recreational substances with the specialist team. Important interactions include:
Nitrates and nitric oxide donors, including amyl nitrite or “poppers”
Contraindicated because the combination can cause a dangerous fall in blood pressure.
PDE5 inhibitors such as sildenafil, tadalafil or vardenafil
Contraindicated because combined vasodilation substantially increases the risk of hypotension.
Other soluble guanylate cyclase stimulators, such as vericiguat
Concomitant use is contraindicated.
Common questions about riociguat
Answers are fully visible for fast scanning and source review.
What is riociguat used for?
It is used by specialist pulmonary-hypertension services for selected cases of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension.
Can riociguat be taken with food?
Yes. It can generally be taken with or without food, although consistent food timing is advised for people prone to low blood pressure.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.