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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Antihypertensive Drugs: Direct Renin Inhibitors01:25

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Antihypertensive Drugs: Angiotensin II Receptor Blockers01:30

Antihypertensive Drugs: Angiotensin II Receptor Blockers

In the renin-angiotensin-aldosterone system, a hormone called angiotensin II plays a crucial role. It binds to the AT1 receptors in vascular smooth muscles coupled with Gq proteins. The activation of these receptors activates an enzyme called phospholipase C, which releases two molecules: inositol trisphosphate and diacylglycerol. These molecules cause a chain reaction that leads to the phosphorylation of myosin light chains and promotes interaction between actin and myosin, leading to smooth...

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Catheter-based Endovascular Angioplasty for Fibrosing Mediastinitis-associated Pulmonary Vein Stenosis
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Catheter-based Endovascular Angioplasty for Fibrosing Mediastinitis-associated Pulmonary Vein Stenosis

Published on: August 26, 2025

Ambrisentan.

James E Frampton1

  • 1Adis, a Wolters Kluwer Business, Auckland, New Zealand.

American Journal of Cardiovascular Drugs : Drugs, Devices, and Other Interventions
|June 1, 2011
PubMed
Summary
This summary is machine-generated.

Ambrisentan significantly improves exercise capacity and reduces dyspnea in pulmonary arterial hypertension (PAH) patients. This endothelin receptor antagonist demonstrates sustained efficacy and a favorable safety profile, including minimal liver injury risk.

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Area of Science:

  • Pharmacology
  • Cardiology
  • Pulmonology

Background:

  • Pulmonary arterial hypertension (PAH) is a severe condition requiring effective treatment.
  • Ambrisentan is a selective endothelin type A receptor antagonist.
  • Current PAH treatments aim to improve exercise capacity and reduce clinical worsening.

Purpose of the Study:

  • To evaluate the efficacy and safety of ambrisentan in treating PAH.
  • To assess ambrisentan's impact on exercise capacity (6-minute walk distance) and dyspnea.
  • To determine the long-term safety and tolerability of ambrisentan.

Main Methods:

  • Two double-blind, placebo-controlled studies (ARIES-1, ARIES-2) assessed ambrisentan (2.5-10 mg/day) over 3 months.
  • A 2-year extension study (ARIES-E) evaluated sustained efficacy and safety.
  • An open-label study (ARIES-3) assessed ambrisentan (5 mg/day) in PAH and non-PAH patients.

Main Results:

  • Ambrisentan significantly improved 6-minute walk distance and reduced dyspnea compared to placebo.
  • Sustained improvements in exercise capacity and dyspnea were observed in the extension study.
  • Ambrisentan demonstrated a low risk of clinical worsening, death, and liver injury.

Conclusions:

  • Ambrisentan is an effective and well-tolerated treatment for PAH.
  • The drug offers sustained benefits and a favorable safety profile, with minimal risk of liver injury.
  • Ambrisentan represents a valuable therapeutic option for patients with PAH.