What is Ambrisentan used for?

Ambrisentan is used to treat pulmonary arterial hypertension (PAH) in adults to help them exercise better and slow the disease.

Can I take Ambrisentan if I am pregnant?

No, Ambrisentan is not for use during pregnancy as it may cause serious birth defects.

What should I do if I become pregnant while taking Ambrisentan?

If you find out you are pregnant, stop taking Ambrisentan as soon as possible.

How should I take my Ambrisentan tablets?

Take your tablets once daily and do not crush, chew, or split them.

What are the most common side effects of Ambrisentan?

The most common side effects include swelling in the limbs, nasal congestion, sinus infections, and skin flushing.

Can Ambrisentan cause swelling?

Yes, fluid retention and swelling in the hands or feet are known side effects of this medication.

Does Ambrisentan affect sperm count?

Yes, decreases in sperm count have been observed in patients taking this type of medication.

Should I worry about my hemoglobin levels on Ambrisentan?

Yes, your doctor may want to check your hemoglobin levels at the start of treatment and periodically after.

Is Ambrisentan safe for elderly patients?

Elderly patients may experience more swelling and might see less improvement in walking distance than younger patients.

What happens if I take too much Ambrisentan?

A massive overdose could lead to dangerously low blood pressure.

ambrisentan | CAS 177036-94-1 | OUJTZYPIHDYQMC

Loading compound...

Endothelin receptor antagonist

Ambrisentan (brand name Letairis) is a prescription medicine used to treat pulmonary arterial hypertension (PAH) in adults. It works by blocking certain receptors in the body to help improve exercise ability and slow the progression of the disease.

How it worksAmbrisentan works by blocking endothelin receptors (ET-A and ET-B). This helps prevent the narrowing of blood vessels in the lungs, which is common in people with pulmonary arterial hypertension.

Brand names:LETAIRIS

Used for

Pulmonary arterial hypertension (PAH) in adults to improve exercise ability and delay clinical worsening.

Conditions

Pulmonary arterial hypertension (PAH)

Class

Endothelin receptor antagonistCardiovascularRespiratory

How to take

FormsOral tablet

RoutesOral

Adults usually start with 5 mg once daily. Depending on how you tolerate it, a doctor may increase the dose to 10 mg once daily after 4 weeks. Do not crush, chew, or split the tablets.

Take once daily. Do not split, crush, or chew the tablets.

Key warnings

Ambrisentan can cause serious birth defects and is not to be used during pregnancy. Females of reproductive potential should use effective birth control before, during, and for one month after treatment.

·Ambrisentan can cause serious birth defects and is not to be used during pregnancy. Females of reproductive potential should use effective birth control before, during, and for one month after treatment.
·Can cause severe fluid retention.
·May cause decreased sperm count in men.
·May cause a decrease in hemoglobin levels.
·Risk of serious birth defects if used during pregnancy.

Do not use if

·Pregnancy
·Idiopathic Pulmonary Fibrosis (IPF)

Side effects

Common

Swelling in the hands or feet (peripheral edema)Nasal congestionSinus infection (sinusitis)Flushing

Serious

·Fluid retention
·Fluid buildup in the lungs (pulmonary edema)
·Decreased sperm count
·Changes in hemoglobin levels

Seek help if

·pregnancy
·fluid_retention
·sperm_count
·hemoglobin_changes

Interactions

·Cyclosporine: Taking this with Ambrisentan can double the amount of drug in your system; the Ambrisentan dose should be limited to 5 mg once daily.
·TRYVIO
·OPSUMIT
·TRACLEER
·JUXTAPID

FoodFood does not affect how Ambrisentan is absorbed.

Special populations

PregnancyAmbrisentan should not be used during pregnancy because it may cause major birth defects or fetal death. Women who can become pregnant should have a pregnancy test before starting and use effective birth control during and for one month after treatment.

PediatricThe safety and effectiveness of Ambrisentan in children have not been established.

GeriatricElderly patients (65 and older) may see less improvement in walking distance compared to younger patients and may experience more swelling (edema).

Talk to your doctor

Monitor

·Fluid retention/swelling
·Hemoglobin levels
·Sperm count
·Pregnancy status

Questions to ask

·How often should my hemoglobin be checked?
·What should I do if I notice swelling in my legs?
·Is it safe to take cyclosporine while on Ambrisentan?
·What birth control should I use while on this medication?

Pharmacokinetics

OnsetPeak concentrations occur about 2 hours after taking it orally.

BioavailabilityThe exact absolute bioavailability is unknown, but food does not change it.

Protein bindingHighly bound to plasma proteins (99%).

MetabolismElimination is mostly through non-renal pathways.

ExcretionPrimarily non-renal elimination.

Practical

OverdoseThere is no specific experience with overdosing on Ambrisentan. High doses in studies caused headache, flushing, dizziness, nausea, and nasal congestion. Very large doses could cause dangerously low blood pressure.

Ingredients

Allergens

lactosesoyFD&C Red #40

Inactive

croscarmellose sodiumlactose monohydratemagnesium stearatemicrocrystalline celluloseFD&C Red #40lecithin (soy)polyethylene glycol 3350polyvinyl alcohol, unspecifiedtalctitanium dioxide

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.