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    Home > Active Ingredient News > Drugs Articles > What is endothelin receptor blocker (antagonist)?

    What is endothelin receptor blocker (antagonist)?

    • Last Update: 2020-04-03
    • Source: Internet
    • Author: User
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    Endothelin receptor antagonist can block endothelin receptor sites in smooth muscle and organs Endothelin-1 is one of the three endothelin amino acid peptides, and has two subtypes to regulate blood pressure Researchers have developed drugs that disable both subtypes and ensure relaxation of blood vessels Patients are required to take the drug under the supervision of a doctor because of the possibility of liver damage The endothelium of vascular tissue produces endothelin-1, as well as subtypes of endothelin A and B Endothelin A binds to endothelin A receptor site at the end of smooth muscle, which promotes cell proliferation and leads to vasoconstriction The substance also binds to a protein called GQ, a priming chemical that triggers the release of calcium from the sarcoplasmic reticulum within cells Elevated calcium levels also cause vasoconstriction, vasospasm, and increased contractility and heart rate The scientists also suggested that the peptide could lead to congestive heart failure and pulmonary hypertension Endothelin B binds to the receptor site of endothelin B, which leads to the activation of the site that induces the formation of nitric oxide and the subsequent inhibition of vascular expansion and cell proliferation Studies have shown that, under normal circumstances, these two subtypes maintain sufficient cycles by performing alternate tasks when needed Researchers believe that endothelin A is the key to hypertension Scientists now believe that some points of imbalance between endothelin A and B can cause the leading hypertension effect of endothelin a Drug researchers have developed drugs such as Ambrisentan and bosentan Doctors may prescribe one of these as a treatment for pulmonary hypertension Ambrisentan blocked the receptor site of endothelin A, while bosentan blocked the sites of endothelin A and B By blocking the recipient site, the two drugs prevent the chemical reactions that contribute to high blood pressure, ensuring vasomuscular relaxation and blood pressure reduction Studies have shown that patients taking endothelin receptor blockers may have an increased risk of liver injury or failure Before receiving the prescription drug, the patient should have a liver enzyme test to determine the bottom line of liver function After taking the medicine, the patient should check the liver function every month If the examination found that the level of liver transferase increased, the drug may be stopped If the patient has anorexia, nausea, jaundice, right tenderness, and dark urine and gray stool symptoms, should immediately consult a doctor Endothelin receptor antagonists are not recommended for pregnant women because of the risk of birth defects Drug side effects * often reported include headache, skin flushing, and swelling of feet and ankles caused by urinary retention Patients may also have anemia, decreased sperm count and other problems such as respiratory tract infection.
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