Adempas

Generic name: riociguat

Drug class: Soluble guanylate cyclase (sGC) stimulators

Dosage form: Film-coated tablets

Root of administration: Oral

Dose: The recommended starting dosage is 1 mg taken 3 times a day. For patients who may not tolerate the hypotensive effect of Adempas, consider a starting dose of 0.5 mg taken three times a day. If systolic blood pressure remains greater than 95 mmHg and the patient has no signs or symptoms of hypotension, up-titrate the dose by 0.5 mg taken three times a day.

Mechanism of action: Riociguat stimulates soluble guanylate cyclase (sGC), an enzyme in the blood vessels of the lungs, causing the blood vessels to relax and widen. This helps to lower the blood pressure in the lungs and improve symptoms of chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH).

Drug usage cases:

• Treatment of adults with persistent/recurrent chronic thromboembolic pulmonary hypertension (CTEPH) after surgical treatment or inoperable CTEPH to improve exercise capacity and World Health Organization (WHO) functional class.
• Treatment of adults with pulmonary arterial hypertension (PAH) to improve exercise capacity, improve WHO functional class, and delay clinical worsening.

Drug contraindications:

• Hypersensitivity to riociguat or any of the excipients.
• Concurrent use with nitrates or nitric oxide donors in any form, either regularly or intermittently.
• Concurrent use with phosphodiesterase type 5 inhibitors (e.g., sildenafil, tadalafil, vardenafil).
• Pregnancy.
• Severe hepatic impairment.
• Hypotension (systolic blood pressure <95 mmHg).
• Pulmonary hypertension associated with idiopathic interstitial pneumonias.

Side effects:

• Headache
• Dizziness
• Dyspepsia (heartburn)
• Peripheral edema (swelling, especially of the ankles and feet)
• Nausea
• Diarrhea
• Vomiting
• Hemoptysis (coughing up blood)
• Pulmonary hemorrhage (bleeding in the lungs)

Warnings:

• Risk of serious birth defects if taken during pregnancy.
• Risk of hypotension, especially in patients who are dehydrated, have a severe blockage of blood flow out of the heart, or have certain other medical problems.
• Increased risk of bleeding, including bleeding from the respiratory tract.
• Worsening of symptoms in people with pulmonary veno-occlusive disease (PVOD).
• Use with caution in patients with severe liver disease.
• Monitor blood pressure regularly during treatment.

Use during pregnancy or breastfeeding:

Riociguat is contraindicated during pregnancy due to the risk of serious birth defects. Women of childbearing potential must have a negative pregnancy test before starting treatment, monthly during treatment, and one month after stopping treatment. Effective contraception must be used during treatment and for at least one month after stopping treatment.

It is not known whether riociguat is excreted in human milk. Due to the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.