Aprocitentan : Uses, Interactions, Mechanism Of Action

Aprocitentan: Uses, Interactions, Mechanism Of Action

Aprocitentan is a drug mainly utilised in the treatment of resistant hypertension, which is a condition whereby hypertension is not controlled even with the application of several antihypertensive drugs. The reported development of aprocitentan is important as it can represent a therapeutic option for patients who can not reach satisfactory blood pressure control with the help of the generally used drugs.

USES

Aprocitentan is administered as the principal drug in resistant hypertension for patients who cannot get appropriate management through other drugs such as ACE inhibitors, ARBs, diuretics, and beta-blockers. Resistant hypertension is characterised by a higher risk of heart attack, stroke and kidney disease; therefore, proper management is imperative. This drug can be combined wit other antihypertensive drugs to enhance management of high blood pressure. Some studies have established that its application can greatly lower blood pressure, which is desirable to enhance the long term status of cardiovascular disease in patients.

MECHANISM OF ACTION

Aprocitentan has been shown to function in a manner that antagonises endothelin receptors, which are very important in controlling vascular tone. ET-1 binds on these receptors and stimulates the generation of active protein including vasoconstriction as well as stimulation of smooth muscle cell proliferation characterised by chronic increase in blood pressure and vascular remodeling. For example, in patients suffering resistant hypertension, engaging therapies of other types, ET-1 activity maybe increased which leads to constant hypertension.

INTERACTIONS OF APROCITENTAN

Aprocitentan, like many medications, can interact with other drugs and should be used with caution in specific circumstances:

Other Antihypertensives: When used alongside other blood pressure-lowering medications, aprocitentan can lead to a cumulative effect, resulting in excessive hypotension. This mandates occasional checkup to ensure the required dosage needed is given while preventing low blood pressure episodes.

Potassium-Sparing Diuretics and RAAS Inhibitors: These drugs can increase potassium levels which may be further elevated by aprocitentan due to its effect on kidney function and blood vessel tone. Monitoring potassium levels is recommended when aprocitentan is combined with potassium-sparing agents.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): NSAIDs can affect kidney function and potentially reduce the efficacy of aprocitentan. Caution is advised in patients with pre-existing renal impairment.

Aprocitentan is generally well-tolerated, but it has potential side effects, particularly related to fluid retention. Common side effects include headache or nasal congestion. Aprocitentan may cause fluid retention and could exacerbate heart failure in susceptible individuals. Patients with liver impairment may require adjusted dosing since the liver can be affected by the enzyme levels. By addressing an unmet need, aprocitentan provides a promising therapeutic approach for managing resistant hypertension and improving cardiovascular outcomes.