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Ambrisentan 5 mg known as Letairis & Volibris is used to treat high blood pressure in the lungs (pulmonary arterial hypertension).

Therapeutic Class

Anti-hypertensive, Endothelin receptor antagonist

Pharmacology

Endothelin-1 (ET-1) is a potent autocrine and paracrine peptide. Two receptor subtypes, ETA and ETB, mediate the effects of ET-1 in the vascular smooth muscle and endothelium.

The primary actions of ETA are vasoconstriction and cell proliferation, while the predominant actions of ETB are vasodilation, antiproliferation, and ET-1 clearance. Buy Letairis (ambrisentan) Online

In patients with PAH, plasma ET-1 concentrations are increased as much as 10-fold and correlate with increased mean right atrial pressure and disease severity.

ET-1 and ET-1 mRNA concentrations are increased as much as 9-fold in the lung tissue of patients with PAH, primarily in the endothelium of pulmonary arteries.

These findings suggest that ET-1 may play a critical role in the pathogenesis and progression of PAH.

Ambrisentan is a high-affinity (Ki=0.011 nM) ETA receptor antagonist with a high selectivity for the ETA versus ETB receptor ( > 4000-fold). The clinical impact of high selectivity for ETA is not known.

Dosage & Administration

Initial treatment is 5 mg once daily and can be increased to 10 mg once daily if 5 mg is tolerated. Ambrisentan may be administered with or without food.

This drug is controlled through a special program. A program worker will call you each month to make sure that you have gotten a pregnancy test if you are a woman who may become pregnant. See also Warning and Precautions sections. Buy Letairis (ambrisentan) Online

Read the Medication Guide provided by your pharmacist before you start using ambrisentan and each time you get a refill. If you have any questions, consult your doctor or pharmacist.

Take this medication by mouth with or without food, usually once daily or as directed by your doctor. Do not crush, chew, or break the tablets.

Interaction

Multiple dose co-administration 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 co-administered with Cyclosporine.

Contraindications

Ambrisentan may cause fetal harm when administered to a pregnant woman. Ambrisentan/Letairis is contraindicated in women who are or may become pregnant. Buy Letairis (ambrisentan) Online

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.

Pregnancy must be excluded before the initiation of treatment with Ambrisentan and prevented during treatment and for one month after stopping treatment.

Ambrisentan/Letairis is contraindicated in patients with Idiopathic Pulmonary Fibrosis (IPF) including IPF patients with pulmonary hypertension (WHO Group 3).

Side Effects

Decreases in hemoglobin concentration and hematocrit have followed administration of other endothelin receptor antagonists and were observed in clinical studies with Ambrisentan. Buy Letairis (ambrisentan) Online

Pregnancy & Lactation

Pregnancy Category X. It is not known whether Ambrisentan is excreted in human milk. Breastfeeding while receiving Ambrisentan is not recommended.

Precautions & Warnings

Fluid Retention: Peripheral edema is a known class effect of endothelin receptor antagonists, and is also a clinical consequence of PAH and worsening PAH.

Pulmonary Veno-occlusive Disease: If patients develop acute pulmonary edema during initiation of therapy with vasodilating agents such as Ambrisentan, the possibility of pulmonary veno-occlusive disease should be considered. Buy Letairis (ambrisentan) Online

Hematological Changes: Decreases in hemoglobin concentration and hematocrit have followed administration of other endothelin receptor antagonists and were observed in clinical studies with Ambrisentan.

Use in Special Populations

Pediatric patients: Safety and effectiveness of Ambrisentan in pediatric patients have not been established.

Hepatic impaired patient: Ambrisentan/Letairis is not recommended in patients with moderate or severe hepatic impairment.

Storage Conditions

Store in a cool and dry place, below 30° C. Protect from light and moisture.