II. Indications
- Pumonary Arterial Hypertension
- Bosentan (Tracleer)
- Ambrisentan (Letairis)
- Macitentan (Opsumit)
- Sitaxsentan
- Hypertension (fourth-line, refractory)
- Cancer (e.g. Prostate Cancer, Colorectal Cancer, experimental)
- Endothelins inhibition may decrease tumor growth, progression, and Angiogenesis
III. Mechanism
- Endothelin is a vasonstrictor and Aldosterone mediator
- Endothelin Receptor Antagonists inhibit endothelin activity, resulting in vasodilation
IV. Dosing: Pulmonary Hypertension
- Bosentan (Tracleer)
- Start 62.5 mg orally twice daily (may increase to 125 mg twice daily)
- Ambrisentan (Letairis)
- Start 5 mg daily (may increase to 10 mg daily)
- Macitentan (Opsumit)
- Start 10 mg orally daily
- Sitaxsentan
V. Drug Interactions
-
Oral Contraceptives (OCP)
- May reduce OCP efficacy
-
Warfarin
- Increased INR
VI. Adverse Effects
- Peripheral Edema
- Flushing
- Headache
- Liver Function Test abnormalities
VII. Safety
- FDA pregnancy category X
- Monitoring
- Liver Function Testing monthly (hepatotoxicity risk)
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| Definition (NCI_NCI-GLOSS) | A family of drugs that block the hormone endothelin and may prevent prostate cancer from spreading to the bones. They may also prevent the growth and spread of other types of cancer, including colorectal cancer. |
| Definition (NCI) | A group of agents that bind to endothelin receptors, thereby inhibiting the actions of endothelins. Inhibition of endothelins may decrease tumor growth, progression, and angiogenesis. (NCI04) |
| Definition (MSH) | Compounds and drugs that bind to and inhibit or block the activation of ENDOTHELIN RECECPTORS. |
| Concepts | Pharmacologic Substance (T121) |
| MSH | D065128 |
| SnomedCT | 385560009, 385561008 |
| English | Endothelin receptor antagonist, antagonist endothelin receptor, endothelin receptor antagonist, Endothelin Receptor Antagonists, Endothelin Antagonists, Antagonists, Endothelin Receptor, Antagonists, Endothelin, Endothelin receptor antagonist (product), Endothelin receptor antagonist (substance), Endothelin Receptor Antagonist |
| Spanish | antagonista del receptor de endotelina (producto), antagonista del receptor de endotelina (sustancia), antagonista del receptor de endotelina |
