Ambrisentan

Information about Ambrisentan

Ambrisentan is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH).

Liver safety of Ambrisentan

Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy, but has yet to be implicated in cases of clinically apparent acute liver injury.

Mechanism of action of Ambrisentan

Ambrisentan (am" bri sen' tan) is a selective inhibitor of the endothelin receptor type A (ETA) and has little activity against ETB in the doses used in humans. Inhibition of the ETA receptor disrupts the intracellular pathways that lead to vasoconstriction, thus causing vasodilation. Because this receptor is found in highest concentration in the lungs, ambrisentan primarily causes vasodilation in the pulmonary vasculature and decreases pulmonary vascular pressure. In prospective, randomized controlled trials, ambrisentan was effective in alleviating symptoms, improving exercise tolerance and prolonging the time to clinical worsening in patients with idiopathic PAH.

FDA approval information for Ambrisentan

Ambrisentan was the second endothelin receptor antagonist to be approved in the United States (2007) and it remains in active use.

Dosage and administration for Ambrisentan

The current indications are for symptomatic pulmonary arterial hypertension, classified as WHO group 1 (idiopathic). Use of ambrisentan in other forms of PAH (due to heart failure, thromboembolic disease, or pulmonary disease) should be considered experimental as its efficacy in these forms of PAH has not been adequately shown. Because of the potential for teratogenicity, ambrisentan is available only as a part of a monitoring program in which documentation of adequate methods for birth control are required.

Dosage and administration for Ambrisentan

Ambrisentan is available in tablets of 5 and 10 mg under the brand name Letairis and the recommended dose is 5 to 10 mg once daily.

Dosage and administration for Ambrisentan

Common side effects include headaches, dizziness, edema, flushing, rhinitis and dyspepsia.

Pulmonary Disease Agents

• Chronic Obstructive Pulmonary Disease (COPD) Agents
  • Anticholinergic Agents
    • Ipratropium, Tiotropium, Aclidinium
  • Beta-2 Adrenergic Agonists
    • Albuterol, Formoterol, Salmeterol, Terbutaline
  • Corticosteroids
    • Budesonide, Fluticasone
  • Miscellaneous
    • Roflumilast, Theophylline

• Pulmonary Arterial Hypertension Agents
  

• • Endothelin Receptor Antagonists
    • • Ambrisentan, Bosentan, Macitentan
  • Phosphodiesterase Type 5 (PDE5) Inhibitors
    • Avanafil, Sildenafil, Tadalafil, Vardenafil
  •  Prostacyclin Analogs
    • Epoprostenol, Iloprost, Treprostinil
  •  Miscellaneous
    • Riociguat, Selexipag

• Pulmonary Fibrosis Agents
  • Nintedanib, Pirfenidone

• Dailymed label info on Ambrisentan
• FDA Ambrisentan

Ambrisentan Resources
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