Formulary
Riociguat: Indications, Dosing, Side Effects and Interactions
Riociguat clinical drug profile including indications, dosing, side effects, cautions and interactions.
MedNext Academy | 3 min read
Riociguat: Indications, Dosing, Side Effects and Interactions
Riociguat clinical drug profile including indications, dosing, side effects, cautions and interactions.
Indications and dose
**Chronic thromboembolic pulmonary hypertension that is recurrent or persistent following surgery, or is inoperable (initiated under specialist supervision),Monotherapy or in combination with an endothelin receptor antagonist**
- **Adult** (By Mouth): for idiopathic or hereditary pulmonary arterial hypertension, or pulmonary arterial hypertension associated with connective tissue disease (initiated under specialist supervision) Initially 1 mg 3 times a day for 2 weeks, increased in steps of 0.5 mg 3 times a day, dose to be increased every 2 weeks, increased to up to 2.5 mg 3 times a day (max. per dose 2.5 mg 3 times a day), increase up to maximum dose only if systolic blood pressure 95 mmHg and no signs of hypotension, if treatment interrupted for 3 or more days, restart at 1 mg three times daily for 2 weeks and titrate as before, during titration, reduce dose by 0.5 mg three times daily if systolic blood pressure falls below 95 mmHg and patient shows signs of hypotension.
Cautions
Autonomic dysfunction; elderly (risk of hypotension); hypotension (do not initiate if systolic blood pressure below 95 mmHg); hypovolaemia; severe left ventricular outflow obstruction Cautions, further information Smoking Smoking cessation advised (response possibly reduced); dose adjustment may be necessary if smoking started or stopped during treatment.
Contraindications
History of serious haemoptysis; previous bronchial artery embolisation; pulmonary hypertension associated with idiopathic interstitial pneumonias; pulmonary veno-occlusive disease
Side effects
Common or very common Anaemia; constipation; diarrhoea; dizziness; dysphagia; gastroenteritis; gastrointestinal discomfort; gastrointestinal disorders; haemorrhage; headache; hypotension; nasal congestion; nausea; palpitations; peripheral oedema; vomiting
Interactions
**Severe interactions:**
- Therefore, clinically relevant drug-drug interactions with co-treatment which are significantly cleared by CYP1A1-mediated biotransformation, such as erlotinib or granisetron cannot be ruled out.
**Other interactions (32):**
- Pharmacodynamic interactions Nitrates In a clinical study the highest dose of riociguat (2.5 mg tablets 3 times daily) potentiated the blood pressure lowering effect of sublingual nitroglycerin (0.4...
- PDE5 inhibitors Preclinical studies in animal models showed additive systemic blood pressure lowering effect when riociguat was combined with either sildenafil or vardenafil.
- In an exploratory interaction study in 7 patients with PAH on stable sildenafil treatment (20 mg 3 times daily) single doses of riociguat (0.5 mg and 1 mg sequentially) showed additive haemodynamic...
- Doses above 1 mg riociguat were not investigated in this study.
- A 12 week combination study in 18 patients with PAH on stable sildenafil treatment (20 mg 3 times daily) and riociguat (1.0 mg to 2.5 mg 3 times daily) compared to sildenafil alone was performed.
- In the long term extension part of this study (non controlled) the concomitant use of sildenafil and riociguat resulted in a high rate of discontinuation, predominately due to hypotension.
Pregnancy
Avoid-toxicity in animal studies.
Breast feeding
Manufacturer advises avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises caution in moderate impairment; avoid in severe impairment (no information available). Dose adjustments Manufacturer advises cautious dose titration in moderate impairment.
Renal impairment
Avoid if creatinine clearance less than 30 mL/minute (limited information available). M Dose adjustments Titrate dose cautiously if creatinine clearance 30-80 mL/minute (risk of hypotension), M see Prescribing in renal impairment .
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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