ambrisentan at a glance
Medicine class
Selective endothelin A receptor antagonist
Licensed role
Treatment of PAH with WHO functional class II to III symptoms
Specialist care
Treatment is started by a clinician experienced in PAH
Food
The tablet can be taken with or without food
What is ambrisentan used for?
UK-licensed uses represented by the selected product are:
PAH in adults with WHO functional class II to III symptoms, including idiopathic PAH and PAH associated with connective-tissue disease.
PAH in adolescents and children aged 8 to under 18 years with WHO functional class II to III symptoms, including idiopathic, familial, corrected congenital and connective-tissue-disease-associated PAH.
Use alone or with other PAH treatments where clinically appropriate.
How does ambrisentan work?
Endothelin causes blood-vessel narrowing and growth of vascular smooth muscle. Ambrisentan selectively blocks endothelin A receptors, reducing these effects while largely preserving endothelin B receptor activity involved in producing natural vasodilators.
ambrisentan preparations and strengths
Tablet
Route: Oral
Strengths: 2.5 mg, 5 mg, 10 mg
How to take ambrisentan
Follow the specialist team's instructions and continue treatment unless they advise otherwise.
Swallow the selected tablet whole with water.
Do not split, crush or chew the selected tablet.
It may be taken with or without food.
Tell the specialist team if swallowing tablets is difficult rather than altering the tablet.
ambrisentan side effects
Common or expected effects
- Headache or dizziness
- Ankle or leg swelling and fluid retention
- Anaemia, which may cause tiredness, weakness or breathlessness
- Palpitations or flushing
- Nasal congestion, sinus symptoms or nosebleeds
- Nausea, vomiting, diarrhoea or abdominal discomfort
- Tiredness
- Rash or itching
Get urgent medical advice
- Facial, lip, tongue or throat swelling, particularly with breathing or swallowing difficulty
- New or worsening breathlessness, rapid fluid retention or symptoms suggesting heart failure
- Fainting or severe light-headedness suggesting low blood pressure
- Yellow skin or eyes, dark urine, persistent abdominal pain or other signs of liver injury
- Marked weakness or breathlessness suggesting significant anaemia
- Sudden hearing loss
ambrisentan in pregnancy
Ambrisentan is contraindicated during pregnancy because it may harm an unborn baby. Before treatment, people who could become pregnant require a negative pregnancy test and reliable contraception; pregnancy testing is recommended during treatment. Contact the specialist team immediately if pregnancy occurs or is suspected, without stopping prescribed treatment independently.
ambrisentan while breastfeeding
Breastfeeding is contraindicated while taking ambrisentan. It is unknown whether ambrisentan enters human milk, so feeding options should be discussed with the specialist team.
ambrisentan interactions
Tell the PAH team about all prescribed, non-prescription and herbal products. Important examples include:
Cyclosporine A
It substantially increases ambrisentan exposure, requiring specialist adjustment and monitoring.
Rifampicin
It can temporarily increase ambrisentan exposure when started, so close monitoring is advised.
Other targeted PAH treatments
Some combinations are established, but evidence for certain vasodilator combinations is limited and specialist oversight is required.
Hormonal contraceptives
Common questions about ambrisentan
Answers are fully visible for fast scanning and source review.
What is ambrisentan used for?
It treats pulmonary arterial hypertension by reducing resistance in the blood vessels carrying blood from the heart to the lungs.
Can ambrisentan be taken with food?
Yes. Food does not have a clinically important effect on overall exposure.
Can ambrisentan tablets be crushed or split?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.