Ambrisentan powder is a selective antagonist of ETAR. Clinically, this drug can treat pulmonary hypertension (PAH). Many people don't know about this drug, Abe Shengtan. In fact, its clinical effect in the use of high pressure is very significant. And what are the medicinal values and uses of Abe Shengtan? In view of this problem, we will introduce it to you in detail below. "
What are the pharmacological effects of this product?
Endothelin -1(ET-1) is an effective autocrine and paracrine peptide. Two receptor subtypes (ETA and ETB) jointly regulate the role of ET-1 in vascular smooth muscle and endothelial cells. The main functions of ETA are vasoconstriction and cell proliferation, while the main functions of ETB are vasodilation, inhibition of proliferation and elimination of ET-1.
Ambrisentan is a receptor antagonist that highly binds to ETA. Compared with ETB, ETA has high selectivity (> 4000 times), and its clinical effect on ETA's high selectivity is unknown.
What is chronic obstructive pulmonary disease?
Chronic obstructive pulmonary disease (COPD) is a serious respiratory disease commonly seen in clinical practice, with a incidence rate of more than 50%. Pulmonary arterial hypertension (PH) is one of the complications of COPD, which is related to chronic hypoxia leading to pulmonary vascular contraction and remodeling. Severe PH can lead to increased right ventricular pressure, right ventricular hypertrophy, myocardial congestion and edema, interstitial fibrosis, and even right ventricular remodeling and right heart failure.
Lowering pulmonary artery pressure treatment is crucial for patients with COPD, as it not only improves the ventilation flow ratio, but also reduces the right heart load, which is beneficial for slowing down the occurrence of pulmonary heart disease.
At present, there are not many kinds of drugs to reduce pulmonary artery pressure.
Ambrisentan raw material is a selective endothelin receptor antagonist, which has the effects of reducing endogenous vasoconstriction, anti-proliferation and anti-inflammation.
Ambrisentan is a specific endothelin receptor A(ETA receptor) inhibitor developed by Gilead Scientific Company. It is a highly selective ETA receptor antagonist, which can block the combination of ET and ETA, thus blocking ETA-mediated pulmonary vasoconstriction and smooth muscle cell proliferation. In June, 2007, it was approved and marketed by FDA under the trade name Letairis, which is used to treat pulmonary hypertension orally. This is the third endothelin receptor antagonist listed after Bosentan and Sitaxsentan, and it has the advantages of high efficiency and low toxicity.
Clinical usage and what should be noted?
This product has a significant effect in treating pulmonary hypertension with WHO II grade or III symptoms, improving exercise ability and delaying clinical deterioration. Clinically, it has been shown to have better tolerance compared to bosentan and Sitaxsentan, with low liver toxicity, high oral bioavailability, and long half-life. However, it also has disadvantages such as vascular edema, nasal congestion, upper respiratory tract infection, headache, blushing, nausea, liver function damage, etc. During the medication process, liver function needs to be tested. If the transaminase level rises more than three times the normal value, the medication should be discontinued. The research results abroad show that the rate of transaminase elevation caused by Ambrisentan is significantly lower than that of bosentan. The one-year follow-up results of patients using Ambrisentan show that the incidence of transaminase elevation caused by Ambrisentan exceeding three times is 0% to 3%. Overall, It is a safe, effective, and targeted drug for the treatment of pulmonary hypertension.
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