Skip to Main Content

++

INTRODUCTION

++

ambrisentan (am-bri-sen-tan)

Letairis

Classification

Therapeutic: antihypertensives

Pharmacologic: endothelin receptor antagonists

++
Indications
++

Pulmonary arterial hypertension.

++
Action
++

Antagonizes endogenous endothelin, resulting in vasodilation. Therapeutic Effects: Improved exercise capacity and delayed clinical worsening.

++
Adverse Reactions/Side Effects
++

CNS: headache. GI: HEPATOTOXICITY. F and E: fluid retention. Hemat: hemoglobin. Misc: ↓ sperm count.

++

PHYSICAL THERAPY IMPLICATIONS

++
Examination and Evaluation
++

  • Be alert for signs of hepatotoxicity including anorexia, abdominal pain, severe nausea and vomiting, yellow skin or eyes, fever, sore throat, malaise, weakness, facial edema, lethargy, and unusual bleeding or bruising. Report these signs to the physician immediately.

  • Assess exercise tolerance, and document possible benefits of drug therapy in reducing pulmonary hypertension and improving exercise capacity.

++
Interventions
++

  • Design and implement aerobic exercise and endurance training programs as tolerated to improve exercise tolerance, reduce pulmonary impairments, and augment the effects of drug therapy.

++
Patient/Client-related Instruction
++

  • Instruct patient or family/caregivers to report other troublesome side effects such as severe or prolonged headache or fluid retention.

++
Pharmacokinetics
++

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).

++

Table Graphic Jump Location
Favorite Table | Download (.pdf) | Print

TIME/ACTION PROFILE (blood levels)

ROUTE ONSET PEAK DURATION
PO unknown 2 hr 24 hr

++
Contraindications/Precautions
++

Contraindicated in: OB: Pregnancy or lactation; Moderate/severe hepatic impairment.

++

Use Cautiously in: Mild hepatic impairment; Concurrent use of cyclosporine or strong inhibitors of CYP2C19 and CYP3A; Pedi: safety and efficacy in children has not been established.

++
Interactions
++

Drug-Drug: Blood levels may be ↑ by cyclosporine, strong CYP3A inhibitors including ketoconazole and strong 2C19 inhibitors including omeprazole.

++
Route/Dosage
++

PO (Adults): 5 mg once daily, may be increased to 10 mg once daily.

++
Availability
++

Tablets: 5 mg, 10 mg.

Want remote access to your institution's subscription?

Sign in to your MyAccess profile while you are actively authenticated on this site via your institution (you will be able to verify this by looking at the top right corner of the screen - if you see your institution's name, you are authenticated). Once logged in to your MyAccess profile, you will be able to access your institution's subscription for 90 days from any location. You must be logged in while authenticated at least once every 90 days to maintain this remote access.

Ok

About MyAccess

If your institution subscribes to this resource, and you don't have a MyAccess profile, please contact your library's reference desk for information on how to gain access to this resource from off-campus.

Pop-up div Successfully Displayed

This div only appears when the trigger link is hovered over. Otherwise it is hidden from view.