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Bosentan is used to treat pulmonary arterial hypertension. It helps lower blood pressure in the lungs. Common side effects include infections of the nose or throat and low levels of red blood cells (anemia). Serious side effects may include liver damage and fluid retention. Bosentan is available as an oral tablet and a tablet that you dissolve in water before swallowing.

Uses

What is bosentan used for?

Bosentan is commonly used for pulmonary arterial hypertension (PAH). PAH is a condition where you have high pressure in the blood vessels (arteries) that carry blood into your lungs. Over time, this pressure strains your heart and makes it harder for you to breathe and be physically active.

Bosentan may also be used for other conditions as determined by your health care provider.

How does bosentan work (mechanism of action)?

Bosentan blocks the effects of endothelin-1, a substance that tightens blood vessels and worsens lung damage in people with pulmonary arterial hypertension. By blocking endothelin-1, bosentan helps relax the blood vessels and lower the blood pressure in the lungs. This can help prevent the damage from getting worse.

How is bosentan supplied (dosage forms)?

Brands and other names

  • Tracleer

Dosage forms and strengths

  • 62.5 mg, 125 mg oral tablets
  • 32 mg tablets for oral suspension

How should I store bosentan?

Bosentan should be stored at room temperature, between 68 F and 77 F (20 C and 25 C). It can be exposed to temperatures between 59 F and 86 F (15 C and 30 C) for shorter periods of time, such as when transporting it. Store in a cool, dry place.

Side Effects

What are the most common side effects of bosentan?

The most common side effects of bosentan are listed below. These side effects may vary depending on the product you are taking. Tell your health care provider if you have any of these side effects that bother you.

  • Infection in the nose or throat, sore throat, or common cold symptoms
  • Low levels of red blood cells (anemia; see below)
  • Fever
  • Inflamed nasal passages (sinusitis)
  • Headache
  • Fainting
  • Flushing
  • Joint pain
  • Low blood pressure
  • Irregular heartbeat

There may be other side effects of bosentan that are not listed here. Contact your health care provider if you think you are having a side effect of a medicine. In the U.S., you can report side effects to the FDA at www.fda.gov/medwatch or by calling 800-FDA-1088 (800-332-1088). In Canada, you can report side effects to Health Canada at www.health.gc.ca/medeffect or by calling 866-234-2345.

What are the serious side effects of bosentan?

While less common, the most serious side effects of bosentan are described below, along with what to do if they happen.

Severe Allergic Reactions. Bosentan may cause allergic reactions, which can be serious. Stop taking bosentan and get help right away if you have any of the following symptoms of a serious allergic reaction.

  • Breathing problems or wheezing
  • Racing heart
  • Fever or general ill feeling
  • Swollen lymph nodes
  • Swelling of the face, lips, mouth, tongue, or throat
  • Trouble swallowing or throat tightness
  • Itching or skin rash
  • Bumps on the skin called hives, which can be red, pink, white, or brown depending on your skin tone
  • Nausea or vomiting
  • Dizziness, feeling lightheaded, or fainting
  • Stomach cramps
  • Joint pain

Liver Damage. Liver damage, also called hepatotoxicity, can happen when taking bosentan. This medicine is only available through a special program partly because of the risk of liver damage. You will need to have blood tests before starting bosentan and for each month during treatment to monitor for signs of liver problems. Call your health care provider right away if you have any of the following symptoms of liver damage.

  • Nausea or vomiting
  • Stomach or belly pain
  • Fever
  • Weakness or unusual tiredness
  • Itching
  • Loss of appetite
  • Light-colored poop
  • Dark-colored urine (pee)
  • Your skin or the whites of your eyes turning yellowish (also called jaundice)

Fluid Retention (Edema). Bosentan can cause fluid retention, also called edema. Fluid retention can cause serious issues in people with certain conditions, such as heart failure. Call your health care provider right away if you have any of the following symptoms.

  • Chest pain
  • Shortness of breath that is worse than usual
  • Stretched or shiny skin
  • Unusual weight gain
  • Swelling of your ankles, legs, belly, or other body areas

Anemia. Bosentan may cause anemia, which is when you have low levels of red blood cells and low hemoglobin. Hemoglobin is a protein in red blood cells that carries oxygen throughout your body. Keep all appointments for blood tests while you are taking bosentan. Tell your health care provider if you have any of the following symptoms of anemia.

  • Unusual weakness or tiredness
  • Cold hands and feet
  • Fast or abnormal heartbeat
  • Pale or yellowish skin 
  • Dizziness, lightheadedness, or feeling like you are about to pass out

Warnings & Precautions

Who should not take bosentan?

Allergies to Ingredients. People who are allergic to any of the following should not take bosentan.

  • Bosentan 
  • Tracleer
  • Any of the ingredients in the specific product dispensed

Your pharmacist can tell you all of the ingredients in the specific bosentan products they stock.

Pregnancy. Do not take bosentan if you are pregnant or plan to become pregnant. If you become pregnant or think you might be pregnant, contact your health care provider right away. See the Pregnancy section for more details.

Drug Interactions. Bosentan should not be taken while you are taking certain other medicines. Before taking bosentan, tell your health care provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. See the Interactions section for more details.

What should I know about bosentan before taking it?

Do not take bosentan unless it has been prescribed to you by a health care provider. Take it as prescribed.

Do not share bosentan with other people, even if they have the same condition as you. It may harm them.

Keep bosentan out of the reach of children.

Due to bosentan’s risk of liver damage and harm to a fetus, this medicine is only available through a special program, from certain pharmacies, and to certain people. It is important that you keep all of your appointments, including labs or other testing, while taking bosentan. For more information about this program, visit www.BosentanREMSProgram.com or call 866-359-2612.

There are multiple forms of bosentan available. Certain bosentan products should be dissolved in water before each dose. If you are prescribed bosentan tablets for oral suspension, follow the Instructions for Use that come with the medicine. If you have any questions about how to take your medicine or whether it is okay to split the tablets, talk to your pharmacist or other health care provider.

Bosentan may lower sperm count and could make it hard for you to get your partner pregnant. If you have concerns, talk to your health care provider.

Do not stop taking bosentan unless your health care provider tells you to. Stopping bosentan abruptly may cause your symptoms to get worse.

What should I tell my health care provider before taking bosentan?

Tell your health care provider about all of your health conditions and any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. This will help them know if bosentan is right for you.

In particular, make sure that you discuss any of the following.

Current and Past Health Conditions. Tell your health care provider if you have any of the following.

  • Liver problems
  • Low levels of red blood cells (anemia)
  • Heart failure
  • Pulmonary veno-occlusive disease, a condition where certain blood vessels in the lungs are blocked or narrowed

Phenylketonuria (PKU). Some forms of bosentan (the tablets for oral suspension) contain phenylalanine, which can be dangerous for people with phenylketonuria (PKU). Tell your pharmacist and other health care providers if you have PKU.

Pregnancy. Bosentan may cause harm to a fetus. You must not be pregnant before starting bosentan. If you can become pregnant, you must have a pregnancy test before starting bosentan, every month while taking it, and one month after stopping it to make sure you are not pregnant. You must also use a highly effective birth control method (such as tubal ligation) or a combination of a hormonal method (such as the pill) plus a barrier method (such as condoms) while taking bosentan and for one month after your last dose. Talk to your health care provider about your birth control options. If you become pregnant or think you might be pregnant, contact your health care provider right away. 

Breastfeeding. Bosentan passes into breast milk. Tell your health care provider if you are breastfeeding or plan to breastfeed. Your health care provider will let you know if you should stop breastfeeding or stop bosentan.

Interactions

Does bosentan interact with foods or drinks?

Your health care provider may recommend limiting or avoiding grapefruit while taking bosentan. Eating grapefruit or drinking grapefruit juice may raise blood levels of the medicine in your body, which could increase the side effects of bosentan.

It is unknown if drinking alcohol will affect bosentan. The risk of certain side effects, such as headache and liver problems, may be higher if you drink alcohol while taking bosentan.

Does bosentan interact with other medicines (drug interactions)?

Always tell your health care provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using.

In particular, make sure that you discuss if you are using any of the following before taking bosentan.

  • Cyclosporine (Gengraf, Neoral, Sandimmune, and others), which is a medicine that suppresses your immune system
  • Glyburide, which is a medicine used for diabetes
  • A birth control pill, patch, vaginal ring, implant, injection, or intrauterine device (IUD)
  • Fluconazole (Diflucan), itraconazole (Sporanox, Tolsura), ketoconazole, posaconazole (Noxafil), or voriconazole (Vfend), which are medicines used for fungal infections
  • An antibiotic, such as clarithromycin or erythromycin (Ery-Tab and others), which is a medicine used for bacterial infections
  • Rifampin (Rifadin), which is a medicine commonly used to treat an infection called tuberculosis
  • Amiodarone (Pacerone and others), which is a medicine used for an irregular heart rhythm
  • A medicine for HIV or AIDS
  • Warfarin, which is a blood thinner
  • A statin, such as simvastatin (Zocor), which is a medicine used to lower cholesterol

Many other medicines may alter the blood levels of bosentan, and vice versa. Tell your health care provider about all medicines that you take or have recently taken.

This may not be a complete list of medicines that can interact with bosentan. Always check with your health care provider.

Does interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose/Missed Dose

What should I do if I accidentally use too much bosentan?

If you or someone else has taken too much bosentan, get medical help right away, call 911, or contact a Poison Control center at 800-222-1222.

What should I do if I miss a dose of bosentan?

If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and only take the next dose. Do not take double or extra doses.