riociguat: clinical use

Prescribing considerations

• Initiation and monitoring should be undertaken by a clinician experienced in PAH or CTEPH.
• Assess operability before treating CTEPH because pulmonary endarterectomy may be potentially curative.
• Review baseline blood pressure, bleeding risk, renal and hepatic function, smoking status, pregnancy potential and interacting medicines.
• Avoid use after serious haemoptysis or bronchial arterial embolisation; reassess benefit and risk if respiratory bleeding occurs.
• Consider pulmonary veno-occlusive disease if pulmonary oedema develops.

Contraindications and cautions

• Pregnancy
• Concomitant PDE5 inhibitors
• Nitrates or nitric oxide donors in any form
• Other soluble guanylate cyclase stimulators
• Severe hepatic impairment
• Blood pressure below the product-specific initiation threshold
• Pulmonary hypertension associated with idiopathic interstitial pneumonias
• Hypersensitivity to riociguat or an excipient

Monitoring

• Blood pressure and symptoms of hypotension during initiation and ongoing treatment
• Pregnancy testing monthly where pregnancy is possible
• Respiratory bleeding, particularly with anticoagulant treatment
• Renal and hepatic function where impairment is present or suspected
• Smoking status and relevant medicine changes
• Clinical response, exercise capacity and signs of worsening pulmonary hypertension

Clinical pharmacology

Riociguat directly stimulates soluble guanylate cyclase and increases its sensitivity to endogenous nitric oxide, increasing cyclic GMP. Oral bioavailability is high, protein binding is extensive, and elimination involves CYP-mediated metabolism plus renal and biliary/faecal routes.

Formulation and product differences

• Film-coated tablets are available in several strengths and are visually differentiated.
• Tablets contain lactose and may be crushed into water or soft food immediately before use.
• A separate granules-for-oral-suspension product exists for some paediatric patients and has its own product information.

Tablet

Route: Oral

Strengths: 0.5 mg, 1.0 mg, 1.5 mg, 2.0 mg, 2.5 mg