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(am-bri-sen-tan) ,


(trade name),


(trade name)


Therapeutic: antihypertensives
Pharmacologic: endothelin receptor antagonists
Pregnancy Category: X


Pulmonary arterial hypertension (WHO Group 1).


Antagonizes endogenous endothelin, resulting in vasodilation.

Therapeutic effects

Improved exercise capacity and delayed clinical worsening.


Absorption: Absorbed following oral administration. Bioavailability unknown.
Distribution: Unknown.
Protein Binding: 99%.
Metabolism and Excretion: Highly metabolized.
Half-life: 15 hr (effective half-life 9 hr).

Time/action profile (blood levels)

POunknown2 hr24 hr


Contraindicated in: Obstetric / Lactation: Pregnancy or lactation; Idiopathic pulmonary fibrosisModerate/severe hepatic impairment; Significant anemia.
Use Cautiously in: Mild hepatic impairment; Pediatric: Safety and efficacy not established.

Adverse Reactions/Side Effects

Central nervous system

  • headache (most frequent)


  • peripheral edema (most frequent)


  • ↓ sperm count


  • pulmonary veno-occlusive disease (life-threatening)


  • ↓ hemoglobin (most frequent)


Drug-Drug interaction

Blood levels may be ↑ by cyclosporine ; do not exceed ambrisentan dose of 5 mg once daily.


Oral (Adults) 5 mg once daily, may ↑ to 10 mg once daily.


Tablets: 5 mg, 10 mg

Nursing implications

Nursing assessment

  • Assess for signs and symptoms of primary pulmonary hypertension (dyspnea, exercise intolerance) prior to and periodically during therapy.
  • Assess for peripheral edema during therapy. If clinically significant peripheral edema occurs, with or without weight gain, evaluate for underlying cause, such as heart failure, and treat.
  • Monitor for symptoms of acute pulmonary edema (dyspnea, cough with frothy sputum, anxiety, restlessness, palpitations) during initiation of therapy. Consider the possibility of pulmonary veno-occlusive disease; if confirmed discontinue ambrisentan.
  • Lab Test Considerations: Obtain pregnancy test prior to, monthly during therapy, and 1 month following completion of therapy.
    • Monitor hemoglobin prior to and at 1 mo and periodically during therapy. May cause ↓ hemoglobin; usually occurs during first few weeks and stabilizes. If clinically significant and other causes have been excluded, discontinue therapy.

Potential Nursing Diagnoses

Impaired gas exchange (Indications)
Deficient knowledge, related to medication regimen (Patient/Family Teaching)


  • Only available through a special restricted distribution program called Letairis REMS due to risks of birth defects. Frmale patients must be enrolled in Letarin REMS and re-enrolled after first year and then yearly. A limited number of pharmacies are certified to dispense ambrisentan. Provide patients with telephone number (1-866-664-5327) and website ( for information on how to obtain medication.
  • Oral: May be administered without regard to food. Tablets should be swallowed whole; do not crush, break or chew.

Patient/Family Teaching

  • Instruct patient to take ambrisentan as directed, at the same time each day. Review medication guide and patient education brochures with every patient. Explain Letarin REMS to patient. Take missed dose as soon as remembered that day. Take next dose at regular time; do not take two doses at the same time to make up for missed dose.
  • Advise patient to notify health care professional promptly if symptoms of fluid retention (swelling of hands, legs, ankles, feet or all over the body) or hepatotoxicity (anorexia, nausea, vomiting, fever, malaise, fatigue, right upper quadrant abdominal discomfort, jaundice, dark urine or itching) occur.
  • May cause fetal harm if taken during pregnancy. Inform patients a pregnancy test is required prior to beginning therapy and acceptable methods of contraception (one highly effective form of contraception: intrauterine devices [IUD], contraceptive implants, or tubal sterilization or a combination of methods: [hormone method with a barrier method or two barrier methods]) must be used throughout therapy and for 1 mo following discontinuationIf a partner’s vasectomy is method of contraception chosen, a hormone or barrier method must be used along with this method. Educate women of childbearing years on the use of emergency contraception in the case of unprotected sex or contraceptive failure.
  • Inform patients that ambrisentan may cause low sperm count.
  • Advise patient of the importance of regular liver and hemoglobin testing.

Evaluation/Desired Outcomes

  • Improved exercise capacity and decreased rate of clinical progression in patients with primary pulmonary hypertension.
Drug Guide, © 2015 Farlex and Partners
References in periodicals archive ?
* Other product sales, which include products from chronic hepatitis B virus (HBV), cardiovascular, oncology and other categories inclusive of Vemlidy[R] (tenofovir alafenamide 25 mg), Viread[R] (tenofovir disoproxil fumarate 300 mg), Letairis[R] (ambrisentan 5 mg and 10 mg), Ranexa[R](ranolazine 500 mg and 1000 mg), Zydelig[R] (idelalisib 150 mg), AmBisome[R] (amphotericin B liposome for injection 50 mg/vial) and Cayston[R] (aztreonam for inhalation solution 75 mg/vial), were $604 millionfor the second quarter of 2019 compared to $807 million for the same period in 2018.
Other product sales, which include products from chronic hepatitis B virus (HBV), cardiovascular, oncology and other categories inclusive of Vemlidy (tenofovir alafenamide 25 mg), Viread (tenofovir disoproxil fumarate 300 mg), Letairis (ambrisentan 5 mg and 10 mg), Ranexa(ranolazine 500 mg and 1000 mg), Zydelig (idelalisib 150 mg), AmBisome (amphotericin B liposome for injection 50 mg/vial) and Cayston (aztreonam for inhalation solution 75 mg/vial), were $604 million for the second quarter of 2019 compared to $807 million for the same period in 2018.
this month launched a generic version of Letairis (ambrisentan) tablets, 5 mg and 10 mg, in the U.S.
Teva Pharmaceutical Industries Ltd (Teva) (TASE:TEVA) (NYSE:TEVA) announced on Wednesday the launch of a generic version of Letairis (ambrisentan) Tablets, 5 mg and 10 mg, in the US.
Ambrisentan is an endothelin receptor antagonist indicated for the treatment of pulmonary arterial hypertension to improve exercise ability and delay clinical worsening.
The pharmacokinetics and pharmacodynamics of warfarin in combination with ambrisentan in healthy volunteers.
Ambrisentan for the treatment of pulmonary arterial hypertension: results of the ambrisentan in pulmonary arterial hypertension, randomized, double-blind, placebo-controlled, multicenter, efficacy (ARIES) study 1 and 2.
The patient population for that study consisted of patients who were screened for the ARTEMIS-IPF trial (a randomized, placebo-controlled study to evaluate safety and effectiveness of ambrisentan in IPF) and was, therefore, enriched for patients with IPF.
[10] There is renewed interest in the treatment of PHT because of effective pulmonary vasodilators like Sildenafil, tadalafil, Bosentan and Ambrisentan which are available worldwide.
The endothelin receptor antagonist in the included studies was bosentan, and the most frequent application for comparators was prostanoids [12, 13], ambrisentan [13-15, 19], sildenafil [13, 14], and conventional, supportive, or palliative therapy [14, 16-18].