Ambrisentan: Dosage, Side Effects, Brands & Clinical Use | MedexInfo

Ambrisentan

Rx / Oral

Therapeutic ClassEndothelin Receptor Antagonist

Common Dose5–10 mg once daily

RouteOral

PregnancyCategory X – Contraindicated

Indications ▼

Management of pulmonary arterial hypertension (PAH) to improve exercise capacity

Used in patients with WHO Group 1 PAH

Mechanism & Pharmacokinetics ▼

Mechanism: Selective endothelin-A receptor antagonist, causing vasodilation and reduced pulmonary vascular resistance.

Pharmacokinetics: Rapid oral absorption; Tmax ~2 hours. Bioavailability ~50%. Metabolized mainly by liver (CYP2C9 and CYP3A4). Half-life ~15 hours. Excreted via feces and urine.

Dosage & Administration ▼

Patient Group	Dose	Frequency
Adults	5 mg once daily, may increase to 10 mg once daily	Oral
Hepatic impairment	Use with caution, monitor liver function	Oral

Side Effects ▼

Peripheral edema, nasal congestion, headache

Flushing, dizziness

Hepatotoxicity – rare but requires monitoring

Contraindications ▼

Pregnancy (Category X)

Severe hepatic impairment

Hypersensitivity to ambrisentan or excipients

Drug Interaction ▼

Strong CYP3A4 inhibitors may increase plasma levels

Concomitant use with other endothelin receptor antagonists not recommended

Use caution with anticoagulants

Pregnancy & Lactation ▼

Category X – contraindicated in pregnancy

Not recommended during breastfeeding

Clinical / Research Summary ▼

Therapeutic Role: Ambrisentan is an oral endothelin receptor antagonist used primarily for the treatment of pulmonary arterial hypertension (PAH) to improve exercise capacity and delay disease progression.

Mechanism-Based Evidence: Ambrisentan selectively blocks endothelin type A (ETA) receptors, reducing vasoconstriction and proliferation of vascular smooth muscle cells in pulmonary arteries, which lowers pulmonary arterial pressure.

Clinical Effectiveness: Clinical trials demonstrate that Ambrisentan improves 6-minute walk distance, reduces clinical worsening, and improves functional class in patients with PAH. It is effective as monotherapy or in combination with other PAH-targeted therapies.

Safety Profile: Common adverse effects include peripheral edema, nasal congestion, headache, and flushing. Liver function monitoring is recommended, and it is contraindicated in pregnancy due to teratogenicity.

Research Directions: Ongoing studies focus on combination therapy strategies, long-term outcomes in different PAH subgroups, and cardiovascular safety profiles, including effects on right ventricular function and survival.

Patient Counseling Points ▼

Take once daily, with or without food

Regular liver function monitoring is required

Avoid pregnancy; use reliable contraception

Report swelling, dizziness, or jaundice immediately

Storage & Handling ▼

Store at 20–25°C, protect from moisture

Keep out of reach of children

Clinical / Research Summary ▼

Effective in improving exercise capacity in PAH patients

Well tolerated with proper monitoring of liver function

Overdose or misuse can lead to serious adverse effects

Clinical trials support its efficacy as a selective endothelin-A receptor antagonist

Brand Names (Bangladesh & Global) ▼

Bangladesh (Local Brands):

Volibris Ambrein Ambrisan Ambrisentan Sandoz Ambrisol

Global / International Brands:

Volibris Ambrisentan Ambrisentan Ambrisentan Ambrisentan

Medical Disclaimer: This clinical summary is for educational purposes only. Always follow guidance from a qualified healthcare professional.

Reference Hubs:

• Drug Class: Endothelin Receptor Antagonists • Conditions: Pulmonary Arterial Hypertension • Pathway: Vascular Dilation & Pulmonary Resistance