How Do PAH Endothelin Antagonists Work?

Reviewed on 10/21/2021

How do PAH endothelin antagonists work?

PAH endothelin antagonists are medications used to treat pulmonary arterial hypertension (PAH), a condition of high blood pressure in the arteries that carry deoxygenated blood from the heart to the lungs. Endothelin antagonists reduce pulmonary hypertension by preventing constriction of the pulmonary arteries.

Endothelin-1 is a natural substance secreted by cells in the inner layer (endothelium) of blood vessels. Endothelin-1 causes vasoconstriction and induces proliferation of vascular smooth muscle cells by binding to ET-A and ET-B receptors, two types of protein molecules on vascular endothelial and smooth muscle cells.

Endothelin antagonists either selectively bind to ET-A or both ET-A and ET-B receptors and prevent endothelin-1 from activating them. Endothelin antagonists primarily dilate the pulmonary arteries and have little effect on systemic blood pressure because endothelin receptors are concentrated mainly in pulmonary blood vessels.

How are PAH endothelin antagonists used?

PAH endothelin antagonists are oral tablets prescribed for the treatment of the following conditions:

FDA-approved:

Orphan designation:

SLIDESHOW

How to Lower Blood Pressure: Exercise Tips See Slideshow

What are side effects of PAH endothelin antagonists?

Side effects of PAH endothelin antagonists may include the following:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

What are names of PAH endothelin antagonist drugs?

Generic and brand names of PAH endothelin antagonist drugs include:

References
https://reference.medscape.com/drugs/pah-endothelin-antagonists

https://www.ncbi.nlm.nih.gov/books/NBK548723/

https://www.ahajournals.org/doi/10.1161/01.cir.0000094397.19932.78

Health Solutions From Our Sponsors