Understanding the Primary Indications for Adempas
Adempas, with the active ingredient riociguat, is a prescription medication primarily used to manage two serious forms of high blood pressure in the arteries of the lungs. The active substance, riociguat, belongs to a novel class of drugs known as soluble guanylate cyclase (sGC) stimulators.
Chronic Thromboembolic Pulmonary Hypertension (CTEPH)
For adult patients with CTEPH (classified as WHO Group 4), Adempas is indicated for inoperable CTEPH or persistent/recurrent CTEPH after surgery (pulmonary thromboendarterectomy). It aims to improve exercise capacity and the World Health Organization (WHO) functional class.
Pulmonary Arterial Hypertension (PAH)
Adempas is also used to treat adults and some pediatric patients with PAH (classified as WHO Group 1). Its purpose is to improve exercise capacity, improve WHO functional class, and delay clinical worsening in patients with idiopathic, heritable, or connective tissue disease-associated PAH. It can be used alone or with other PAH medications.
Mechanism of Action: How Adempas Works
Adempas, as an sGC stimulator, works by enhancing the production of cyclic guanosine monophosphate (cGMP) in the blood vessels, leading to relaxation and widening, particularly in the lungs. It achieves this through a dual mechanism: sensitizing sGC to nitric oxide (NO) and directly stimulating sGC independently of NO. This results in reduced pulmonary pressure and improved blood flow, helping to alleviate symptoms and increase exercise capacity.
Potential Risks and Contraindications
Several significant risks and contraindications are associated with Adempas:
- Embryo-Fetal Toxicity: Adempas has a black box warning due to the severe risk of harm to a fetus. A mandatory REMS program requires pregnancy testing and contraception for female patients.
- Drug Interactions: Avoid taking Adempas with nitrates, nitric oxide donors, or certain phosphodiesterase (PDE-5) inhibitors (like sildenafil and tadalafil) due to the risk of dangerously low blood pressure.
- Pulmonary Veno-Occlusive Disease (PVOD): Not recommended for PVOD patients as it can worsen their condition.
- Other Contraindications: Should not be used for pulmonary hypertension associated with idiopathic interstitial pneumonias (PH-IIP).
Common Side Effects
Common side effects observed in clinical trials include headache, indigestion, dizziness, nausea, vomiting, diarrhea, hypotension, anemia, peripheral edema, and constipation.
Comparison of Adempas vs. PDE-5 Inhibitors
Adempas and PDE-5 inhibitors like sildenafil are different classes of drugs for PAH.
Feature | Adempas (Riociguat) | PDE-5 Inhibitors (e.g., Sildenafil) |
---|---|---|
Drug Class | Soluble Guanylate Cyclase (sGC) Stimulator | Phosphodiesterase-5 (PDE-5) Inhibitor |
Mechanism | Dual action: Sensitizes sGC to NO and directly stimulates sGC. | Blocks cGMP breakdown, extending NO effects. |
Primary Use | CTEPH and PAH. | PAH. |
Action | Stimulates pathway regardless of NO levels. | Effective when NO is present. |
Clinical Efficacy | Improvements in 6-minute walk distance (6MWD) for CTEPH and PAH. | Improves 6MWD in PAH. |
Drug Interaction | Contraindicated with nitrates and PDE-5 inhibitors. | Contraindicated with nitrates. |
Conclusion
Adempas is an important treatment for adults with specific forms of pulmonary hypertension, including CTEPH and PAH, and some pediatric PAH patients. Its sGC stimulation mechanism promotes vasodilation and improves blood flow in the lungs, leading to better exercise capacity and functional class. However, prescribers must be vigilant about potential side effects, serious risks like embryo-fetal toxicity requiring a REMS program, contraindications, and drug interactions to ensure safe and effective use. For more detailed information, consult the full prescribing information from the FDA.