Who is not suitable for taking aprocitentan and what are its contraindications?

Aprecitentan, as an endothelin receptor antagonist, is mainly used for the combined treatment of refractory hypertension. But not all patients are suitable for use. For people with severe hepatic insufficiency, since drugs are mainly metabolized by the liver, liver damage can lead to drug accumulation and increased toxicity. Therefore, such patients are usually classified as contraindicated or strictly restricted in use. In addition, patients who have had severe allergic reactions to similar drugs in the past should also avoid using them to avoid becoming allergic again or causing serious adverse reactions.

Caution is also warranted in patients with inherently fragile cardiovascular systems, particularly those with recent decompensation of heart failure, significant fluid retention, or those receiving vigorous diuretic therapy. Aprecitentan may cause mild edema and may worsen symptoms if the patient is prone to fluid retention. Therefore, this group of people need to assess the risks before use and use it under close medical supervision as much as possible to reduce potential complications.

Pregnant and lactating women are classified as contraindicated or highly restricted in most endothelin receptor antagonist therapies, and aprecitentan is no exception. Based on the pharmacological mechanism, this type of drug may affect fetal development, so clear risk notification is required before pregnancy, and strict contraception must be used during treatment. It is not clear whether it will be excreted through breast milk during lactation. To avoid the risk of drug exposure to infants, it is usually recommended to avoid use or stop breastfeeding.

Patients with impaired renal function should also be evaluated in advance. Although aprecitentan has low nephrotoxicity, patients with severe renal insufficiency have poor tolerance to water and sodium retention, and may cause additional burden if blood pressure fluctuations, edema, or electrolyte imbalances occur after use. If such patients need to use it, they should closely monitor changes in body fluids, electrolytes and blood pressure under the guidance of a doctor, and adjust the dosage or discontinue medication according to the situation to ensure safety.

Reference materials:https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/217686s000lbl.pdf