Ambrisentan

Pulmonary Hypertension

Drug Status

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Government Approvals

US(FDA), UK(BNF)

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WHO Essential Medicine

NO

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Known Teratogen

Definite

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Pharmaceutical Class

Endothelin Receptor Antagonist

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Controlled Drug Substance

NO

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Drug Ingredient

Ambrisentan

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Summary

  • Ambrisentan is used to treat pulmonary arterial hypertension (PAH). This is a condition characterized by high blood pressure in the arteries of the lungs. The medication aims to improve your ability to exercise and slow down the progression of symptoms.

  • Ambrisentan is an endothelin receptor antagonist. It selectively blocks the endothelin type-A (ETA) receptor. Endothelin is a substance that causes blood vessels to narrow. By inhibiting endothelin, Ambrisentan helps to relax and widen blood vessels. This improves blood flow and reduces blood pressure in the lungs.

  • For adults, the usual starting dose of Ambrisentan is 5 mg once daily. This may be increased to 10 mg daily based on your response and tolerability. For children aged 8 to less than 18 years, the dose is based on body weight, starting at 2.5 mg to 5 mg once daily.

  • Common side effects of Ambrisentan include peripheral edema (swelling), headache, and nasal congestion. Serious adverse effects can include anemia, liver enzyme elevations, and fluid retention. If you experience any severe or persistent side effects, contact your doctor immediately.

  • Ambrisentan is not recommended for use while breastfeeding or during pregnancy due to potential risks. It's also not suitable for patients with idiopathic pulmonary fibrosis or severe liver impairment. It's important to have regular monitoring of liver function and hemoglobin levels during treatment.

Indications and Purpose

What is Ambrisentan used for?

Ambrisentan is indicated for the treatment of pulmonary arterial hypertension (PAH), a condition characterized by high blood pressure in the arteries of the lungs. It is used to improve exercise ability and delay the progression of symptoms in patients with PAH.

How does Ambrisentan work?

Ambrisentan is an endothelin receptor antagonist that selectively blocks the endothelin type-A (ETA) receptor. By inhibiting endothelin, a substance that causes blood vessels to narrow, Ambrisentan helps to relax and widen blood vessels, improving blood flow and reducing blood pressure in the lungs.

Is Ambrisentan effective?

Ambrisentan has been shown to improve exercise ability and delay clinical worsening in patients with pulmonary arterial hypertension (PAH). Clinical trials, such as ARIES-1 and ARIES-2, demonstrated significant improvements in 6-minute walk distance and time to clinical worsening, supporting its effectiveness in managing PAH.

How does one know if Ambrisentan is working?

The benefit of Ambrisentan is evaluated through regular follow-up appointments with your doctor, who will monitor your symptoms, exercise ability, and any side effects. They may also order tests to assess your heart and lung function, ensuring the medication is effectively managing your pulmonary arterial hypertension.

Directions for Use

What is the usual dose of Ambrisentan?

For adults, the usual starting dose of Ambrisentan is 5 mg once daily, which may be increased to 10 mg daily based on clinical response and tolerability. For children aged 8 to less than 18 years, the dose is based on body weight, starting at 2.5 mg to 5 mg once daily, with possible titration depending on response and tolerability.

How do I take Ambrisentan?

Ambrisentan should be taken once daily, with or without food, at the same time each day. There are no specific food restrictions while taking this medication. Follow your doctor's instructions and do not alter your dose without consulting them.

For how long do I take Ambrisentan?

Ambrisentan is typically used as a long-term treatment for pulmonary arterial hypertension (PAH). It is important to continue taking it even if you feel well, as it helps manage symptoms but does not cure the condition. Always follow your doctor's guidance on the duration of use.

How long does it take for Ambrisentan to start working?

Ambrisentan may start to improve symptoms of pulmonary arterial hypertension within a few weeks, but it can take longer to experience the full benefits. Regular follow-up with your doctor will help assess how well the medication is working for you.

How should I store Ambrisentan?

Store Ambrisentan at room temperature, between 68°F to 77°F (20°C to 25°C), in its original packaging to protect it from light and moisture. Keep it out of reach of children and pets. Do not store it in the bathroom, and dispose of any unused medication properly through a take-back program.

Warnings and Precautions

Who should avoid taking Ambrisentan?

Ambrisentan is contraindicated in pregnant women due to the risk of serious birth defects. It should not be used in patients with idiopathic pulmonary fibrosis or severe liver impairment. Regular monitoring of liver function and hemoglobin levels is recommended. Women of childbearing potential must use effective contraception during treatment.

Can I take Ambrisentan with other prescription drugs?

Ambrisentan can interact with cyclosporine, leading to increased levels of Ambrisentan in the body. When taken together, the dose of Ambrisentan should be limited to 5 mg once daily. Always inform your doctor about all medications you are taking to avoid potential interactions.

Can I take Ambrisentan with vitamins or supplements?

From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.

Can Ambrisentan be taken safely while pregnant?

Ambrisentan is contraindicated during pregnancy due to the risk of serious birth defects. Women of childbearing potential must have a negative pregnancy test before starting treatment and use effective contraception during and for one month after treatment. Monthly pregnancy tests are recommended to ensure safety.

Can Ambrisentan be taken safely while breastfeeding?

Ambrisentan is not recommended for use while breastfeeding, as it is unknown if the drug passes into breast milk and could potentially harm a nursing infant. Consult your doctor to discuss alternative treatments or feeding options if you are breastfeeding.

Is Ambrisentan safe for the elderly?

Elderly patients may experience more severe side effects, such as peripheral edema, when taking Ambrisentan. It's important for older adults to be closely monitored by their healthcare provider while on this medication. Dose adjustments may be necessary based on individual tolerance and response.

Is it safe to exercise while taking Ambrisentan?

Ambrisentan is used to treat pulmonary arterial hypertension (PAH) and is intended to improve exercise ability by reducing blood pressure in the lungs. It should not limit the ability to exercise; rather, it aims to enhance it. However, if you experience any issues while exercising, consult your doctor.

Is it safe to drink alcohol while taking Ambrisentan?

From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.