Ambrisentan (Oral)

Ambrisentan is an oral medication also known as the brand name Letairis and is prescribed by doctors for the treatment of pulmonary arterial hypertension. It works by relaxing muscle tissue found in blood vessels, which regulates blood pressure.

Overview

What is Ambrisentan?

Ambrisetan, also known under the brand names of Letairis, Volibris and Pulmonext, is a drug prescribed by physicians to treat pulmonary hypertension. Ambrisentan relaxes the muscles found in blood vessels that are reacting to the peptide known as endothelin and increasing blood pressure. Relaxing these muscles improves lung capacity in patients suffering from pulmonary arterial hypertension.

Ambrisentan may be prescribed with the drug tadalafil, which will work in tandem to reduce hospital visits due to symptoms of pulmonary arterial hypertension, reduce the risk of your condition getting worse and improve your breathing and, therefore, your quality of life. Tadalafil, also known by its marketed name of Cialis, has clinical applications that also relax and widen blood vessels in the lungs.

The idea of using these two drugs, Ambrisentan and tadalafil, together is that targeting multiple pathways may increase the overall effect on the disease. These two drugs target different cellular pathways without having any adverse reactions to each other, which is a form of combination therapy. Combination therapy such as this is considered a breakthrough, especially in patients undergoing treatment for the first time. As with Ambrisentan, tadalafil has its own set of cautions and side effects. Follow all advice given by your health care provider and read all information provided with each prescription.

How does Ambrisentan work?

Ambrisentan is an endothelin receptor antagonist that selectively affects the peptide endothelin and blocks the receptors. This eases the muscles in the blood vessels, relaxing them and regulating blood pressure as well as improving lung capacity.

What is pulmonary arterial hypertension?

Pulmonary arterial hypertension is a condition of high blood pressure within the arteries located in the lungs. Patients who are diagnosed with pulmonary arterial hypertension often exhibit symptoms such as:

  • Shortness of breath
  • Fainting
  • Fatigue
  • Chest Pain
  • Swelling of the legs
  • Rapid heartbeat

The cause of pulmonary arterial hypertension is often unknown but it is believed to be hereditary and/or the result of blood clots in the lungs sometime in the medical history of the patient. People who have been diagnosed with HIV/AIDS, sickle cell disease, COPD, sleep apnea are all at risk for developing pulmonary arterial hypertension. People who use cocaine or who live at high altitudes or those that have been diagnosed with mitral valve issues are also at risk.

There is no known cure for pulmonary arterial hypertension and treatment, dosage and medication use depends on the patient's circumstances and overall health condition. In addition to easing symptoms with treatment by Ambrisentan, patients may also be prescribed oxygen therapy, diuretics and anti-clotting drugs. The worst cases of pulmonary arterial hypertension may lead to lung transplant exploration.

Conditions treated

  • Pulmonary arterial hypertension

Type of medicine

  • Endothelin receptor antagonist

Side Effects

The following is a list of possible side effects most commonly experienced with treatment of Ambrisentan. Keep in mind that not all patients experience side effects that are severe in nature or prolonged in duration. If your side effects are prolonged or severe, report them to your health care professional immediately.

The most common side effects of Ambrisentan include:

  • Swollen, bloated face, arms or hands, lower legs or feet
  • Rapid weight gain
  • Tingling of the hands or feet
  • Unusual weight gain or loss
  • Cough
  • Fast, irregular, pounding, or racing heartbeat or pulse
  • Fever
  • Headache
  • Muscle aches
  • Tender, painful eyes and/or cheekbones
  • Sore throat
  • Stuffy or runny nose
  • Tightness of the chest
  • Trouble breathing
  • Decreased sperm counts
  • Anemia (red blood cell counts low)
  • Hot flashes or flushing
  • Unusual tiredness or weakness

Ambrisentan may cause problems in the liver and therefore it should be reported to your health care professional immediately if you experience any of the following symptoms:

  • Appetite loss
  • Vomiting, nausea
  • High body temperature
  • Body Aches
  • Generally unwell feeling
  • Painful abdomen, typically upper right area
  • Yellowing skin or eyes
  • Urine darkness

This is not a complete list of possible side effects and every patient is different, so any changes to your overall health while using Ambrisentan should be discussed with your doctor immediately. To improve the success of the effectiveness of treatment with Ambrisentan as well as insure your safety, you should disclose your full medical history to your doctor prior to treatment. This includes any prescription, non-prescription, vitamin, herbal or holistic medications or treatments you are currently taking or have taken in the past.

Dosage

Patients and their symptoms, overall health and lifestyles are different and therefore the dosage of Ambrisentan will depend on what your doctor feels is the correct amount, frequency and treatment regime that is right for you. Always follow your doctor's instructions as well as those written on the label of the Ambrisentan packaging.

As a general rule, for treatment of pulmonary arterial hypertension in adults, initial dosage will typically be 5 milligrams once per day. Your dosage may be increased by your doctor to 10 milligrams once per day if required. Dosage for children suffering from pulmonary arterial hypertension will be determined by your health care provider.

It is best to take Ambrisentan at the same time of day every day. To benefit the most from the treatment regime, do not miss a dose or take it as soon as you remember; if it is close to the time for your next dose, skip the missed dose instead of doubling up. Ambrisentan may be taken with or without food but do not chew, break or crush the tablet.

Interactions

Use of other drugs when on a treatment regimen with Ambrisentan can decrease the effectiveness of one or both drugs and/or cause unwanted health risks and side effects. Inform your health care provider of any prescription, non-prescription, vitamin, herbal or holistic medications or remedies you are taking now or have taken in the past to determine if they will cause unwanted interactions with Ambrisentan during treatment.

Certain medications should not be used together under any circumstances, however use of Ambrisentan as part of a treatment program with tadalafil may be prescribed to stop the progression of your pulmonary arterial hypertension and reduce incidences of hospitalization due to symptoms. Following your doctor's prescribed treatment regimen is absolutely necessary for a better chance of success and safety of Ambrisentan treatment.

Use of Ambrisentan with the following drugs is usually not recommended. If required, your doctor may adjust dosage of either medication accordingly.

  • Eliglustat
  • Simeprevir

Increased side effects have been experienced by patients who use Cyclosporine while being treated with Ambrisentan. Use of these drugs together should be closely monitored by your health care professional.

While this is not a complete list of drugs known to interact with Ambrisentan, it is a basic guideline of known interactions. Patients are advised to fully inform their health care provider of any and all health conditions or treatments they are currently experiencing before they undergo treatment with this or any other drug. This includes any prescription or non-prescription medications or herbal, holistic or vitamin supplements or treatments. Inform your doctor of any pre-existing health conditions that you are suffering from now or have been treated for in the past. Be certain to pass on your important family medical history to your health care provider as well so any possible increased risks of side effects can be determined before you begin this drug therapy.

The following medical issues can have unwanted affects on the safety and effectiveness of treatment with Ambrisentan. Inform your health care provider if you have:

  • Anemia (low red blood cells)
  • Heart failure (history of)
  • Liver disease
  • Idiopathic pulmonary fibrosis (not recommended for these patients)
  • Liver disease (not recommended for these patients)

Patients who have been diagnosed with liver disease, whether mild or severe, may experience a worsening of their condition if they continue a treatment with Ambrisentan. Informing your health care professional of any medical conditions you have currently or have had in the past is important to the effectiveness and safety of treatment with Ambrisentan or, indeed, any other drug as well.

Warnings

Your doctor will want to have regular checks on your progress over the course of your treatment with Ambrisentan, which will require office visits and, possibly, blood tests. These progress checks will not only assure you and your doctor that your symptoms are being eased by the medicine working properly, but it will also help insure the safety of the treatment on your overall health.

Ambrisentan can cause serious birth defects if taken while pregnant; if you are able to become pregnant when on a treatment regimen that includes Ambrisentan, your doctor will want you to have a pregnancy test monthly. At least two acceptable forms of birth control must be used during treatment with Ambrisentan as well as one month after treatment stops. Females who are able to get pregnant include those who have entered puberty, even if they have not started their period, have a uterus and have not gone through menopause. Do not have unprotected sex while in treatment with Ambrisentan; if you miss a period or fear you are pregnant, tell your doctor immediately.

Breastfeeding during treatment with a course of Ambrisentan is not advised as it is unknown if the medication is passed on via breast milk.

Edema may be a side effect of Ambrisentan in some patients. If you experience rapid weight gain, swollen hands, ankles, feet or entire body or if you have trouble breathing, inform your doctor immediately.

Pulmonary edema is another risk associated with Ambrisentan treatment. If you experience chest pain, difficult breathing, wheezing, blue lips and fingernails, pale skin, increased sweating, productive cough or shortness of breath, you should inform your health care professional immediately.

Inform your doctor of any symptoms of liver disease such as nausea, vomiting, fever, dark colored urine, pale stools, appetite loss or pain in your upper stomach, yellow eyes or skin.

Men being treated with Ambrisentan may experience a decrease in their sperm count, which will affect their ability to have children. If you plan to have children, prior to using Ambrisentan, consult with your doctor on the best treatment advice.

The use of Ambrisentan with other medications should be discussed with your doctor prior to starting treatment. Remember to discuss all prescription, non-prescription, vitamin, herbal or holistic remedies that you are now taking or have taken in the past with your health care provider so that the best decisions can be made for your future treatment with Ambrisentan. Informing your doctor of all medications as well as family history of diseases and any diagnoses will insure a safe, effective course of treatment.

Storage

Ambrisentan, as with other medications, should be kept out of sight and reach of children. Unused or expired Ambrisentan should be disposed of properly according to the advice given to you by your health care provider. Store the Ambrisentan medication at room temperature away from direct sunlight, heat or moisture in the original packaging. Do not allow the Ambrisentan to freeze.

Summary

Ambrisentan, also known by the brand names Letairis, Volibris and Pulmonext, is a doctor prescribed drug effective for use in the treatment of pulmonary arterial hypertension. Ambrisentan relaxes the muscles found in the blood vessels, thereby regulating blood pressure and easing symptoms such as shortness of breath, fainting, fatigue, chest pain, swelling in the legs and rapid heartbeat.

Ambrisentan may be prescribed in conjunction with a drug named tadalafil, for a combination therapy that works to improve your breathing and reduce the risk of your pulmonary arterial hypertension getting worse as time goes on. This drug combination will also reduce the number of hospital visits due to symptoms that you experience. Combination therapy such as this is considered a breakthrough treatment, especially in patients who have not previously been treated for pulmonary arterial hypertension.

Ambrisentan may give patients side effects such as bloating or swelling, rapid weight gain, unusual weight loss, cough, irregular heartbeat, fever, headache, body ache, sore throat, chest tightness or other symptoms. If prolonged or severe, these symptoms should be reported to your health care provider immediately.

Ambrisentan has been proven to cause severe birth defects; for this reason, women who are pregnant or may become pregnant are not advised to undergo treatment with Ambrisentan. Pregnancy tests before treatment and during the course that the patient is on the drug will be required. Ambrisentan also presents a risk of increasing liver disease and/or peripheral edema. Signs of these conditions including yellowing eyes or skin, darkening urine, pain in the abdomen or swelling in the body should be reported to your health care professional immediately. Men may experience a decrease in sperm count, which will affect their ability to father a child while taking Ambrisentan.

Storage of Ambrisentan should be in the original packaging and out of sight and reach of children. Do not expose Ambrisentan to excessive heat, moisture or direct sunlight or allow it to freeze. Disposal of unused or expired quantities of Ambrisentan should be as instructed by professional health care providers or pharmacists.

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Last Reviewed:
December 10, 2017
Last Updated:
April 04, 2018
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