Ambrisentan — uses, dosing, side effects & the brands that sell it · pharmaranks
Ambrisentan: uses, dosing, side effects & brands
Ambrisentan is an endothelin receptor antagonist sold in the U.S. under 2 brand and generic names, for pulmonary hypertension. Below: what the FDA label says, every product that contains it, what the pills look like, and its recall record.
By the pharmaranks editorial team·Reviewed against the FDA (openFDA label, NDC Directory & Enforcement) sources·How we research
From the FDA label for Letairis (application NDA022081). Other ambrisentan products — different forms, different strengths — are dosed differently. Follow the label for the one you were prescribed.
Initiate treatment at 5 mg once daily ( 2.1 ). May be started with tadalafil ( 2.1 ). Titrate at 4-week intervals as needed and tolerated ( 2.1 ). Do not split, crush, or chew tablets ( 2.1 ). 2.1 Adult Dosage Initiate treatment at 5 mg once daily, with or without tadalafil 20 mg once daily. At 4-week intervals, either the dose of Letairis or tadalafil can be increased, as needed and tolerated, to Letairis 10 mg or tadalafil 40 mg. Do not split, crush, or chew tablets. 2.2 Pregnancy Testing in Females of Reproductive Potential Exclude pregnancy before initiating treatment with Letairis in females of reproductive potential [see Warnings and Precautions (5.1) , Use in Specific Populations (8.1 , 8.3) ].
Ambrisentan side effects
Clinically significant adverse reactions that appear in other sections of the labeling include: Embryo-fetal Toxicity [see Warnings and Precautions (5.1) , Use in Specific Populations (8.1) ] Fluid Retention [see Warnings and Precautions (5.2) ] Pulmonary Edema with PVOD [see Warnings and Precautions (5.3) ] Decreased Sperm Count [see Warnings and Precautions (5.4) ] Hematologic Changes [see Warnings and Precautions (5.5) ] Most common adverse reactions (>3% compared to placebo) are peripheral edema, nasal congestion, sinusitis, and flushing ( 6.1 ). When used in combination with tadalafil, most common adverse reactions (>5% compared with either monotherapy) are peripheral edema, headache, nasal congestion, cough, anemia, dyspepsia, and bronchitis ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Gilead Sciences, Inc. at (1-800-445-3235, Option 3) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Safety data for Letairis are presented from two 12-week, placebo-controlled studies (ARIES-1 and ARIES-2) in patients with pulmonary arterial hypertension (PAH), and one randomized,…
Who shouldn’t take ambrisentan
Pregnancy ( 4.1 ) Idiopathic Pulmonary Fibrosis ( 4.2 ) 4.1 Pregnancy Letairis may cause fetal harm when administered to a pregnant female. Letairis is contraindicated in females who are pregnant. Letairis was consistently shown to have teratogenic effects when administered to animals. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus [see Dosage and Administration (2.2) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1) ] . 4.2 Idiopathic Pulmonary Fibrosis Letairis is contraindicated in patients with Idiopathic Pulmonary Fibrosis (IPF), including IPF patients with pulmonary hypertension (WHO Group 3) [see Clinical Studies (14.4) ].
Every ambrisentan product we track (2)
Same active ingredient — different manufacturer, form, price and FDA recall record. That last one is what our independent score measures.
Imprint codes, colour and shape from the FDA’s labelling data. Match the imprint on your pill — or search any imprint.
Ambrisentan pill imprints
Imprint
Strength
Colour
Shape
Maker
5;405
5 mg
white
oval
—
10;406
10 mg
white
oval
—
M;AN
5 mg
pink
round
—
M;AN1
10 mg
pink
oval
—
APO;A5
5 mg
pink
square
—
APO;A10
10 mg
pink
Frequently asked questions
What is ambrisentan?
Letairis contains ambrisentan, an endothelin receptor antagonist. The chemical name of ambrisentan is (+)-(2 S )-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid. It has a molecular formula of C 22 H 22 N 2 O 4 and a molecular weight of 378.42 and has the following structural formula: Figure 1 Ambrisentan Structural Formula Ambrisentan is a white to off-white, crystalline solid. It is a carboxylic acid with a pKa of 4.0. Ambrisentan is practically insoluble in water and in aqueous solutions at low pH. Solubility increases in aqueous solutions at higher pH. In the solid state ambrisentan is very stable, is not hygroscopic, and is not light sensitive. Letairis is available as 5 mg and 10 mg film-coated tablets for once daily oral administration. The tablets include the following inactive ingredients: croscarmellose sodium, lactose monohydrate, magnesium stearate and microcrystalline cellulose. The tablets are film-coated with a coating material containing FD&C Red #40 aluminum lake, lecithin, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide. Each square, pale pink Letairis tablet contains 5 mg of ambrisentan. Each oval, deep pink Letairis tablet contains 10 mg of ambrisentan. Letairis tablets are unscored. Chemical Structure
What kind of drug is ambrisentan?
The FDA classifies ambrisentan as an endothelin receptor antagonist. Endothelin receptor antagonists block endothelin-1, a natural substance that powerfully tightens blood vessels. By stopping it from acting on its receptors, these drugs let vessels relax and widen, lowering pressure in the lung arteries in conditions like pulmonary arterial hypertension. If you are checking whether it is safe to combine with something else, the class is what matters — two drugs from the same class usually should not be stacked.
Can you take ambrisentan with other medicines?
It depends on the medicine. We check it against the FDA labels rather than guessing: our interaction checker searches each drug's own label for the other and quotes what it says, naming the section it came from. Run ambrisentan against whatever else you take — and remember that a label not naming a drug is not the same as that combination being safe.
What brand names is ambrisentan sold under?
Sources: FDA openFDA drug label, National Drug Code Directory, and Enforcement (recall) database. This page reproduces public FDA data and is not medical advice. Dosing is set by your prescriber.
Ambrisentan drug interactions
Multiple dose coadministration of ambrisentan and cyclosporine resulted in an approximately 2-fold increase in ambrisentan exposure in healthy volunteers; therefore, limit the dose of ambrisentan to 5 mg once daily when coadministered with cyclosporine [see Clinical Pharmacology (12.3) ] . Cyclosporine increases ambrisentan exposure; limit ambrisentan dose to 5 mg once daily ( 7 ).
We track 2 ambrisentan-containing products in the U.S.: Letairis and Ambrisentan. They are the same active ingredient; they differ in form, manufacturer, price and FDA recall record.
What forms does ambrisentan come in?
Across the brands we track, ambrisentan is currently marketed as tablet, per the FDA's National Drug Code Directory. Each form is dosed differently — follow the label for the exact product you were prescribed.
Is there a generic ambrisentan?
Yes. Our catalog lists 1 generic ambrisentan product alongside the brand versions. A generic has the same active ingredient and must meet the FDA's bioequivalence standard; it usually costs less. Ask your pharmacist which one your plan covers.