Tracleer (Bosentan) - Oral

Warning:

Tracleer has risks of liver damage and can potentially harm a fetus if taken during pregnancy. Due to these risks, Tracleer is only available through a special program known as Risk Evaluation and Mitigation Strategy (REMS).

If you are a woman of reproductive potential, talk to your healthcare provider about using effective contraceptive methods during treatment. Use two reliable forms of birth control and take monthly pregnancy tests while taking Tracleer and for at least one month after stopping it.

What Is Tracleer?

Tracleer (bosentan) is an oral prescription medication in the endothelin receptor antagonist drug class. It is primarily used to treat a disorder known as pulmonary arterial hypertension (PAH).

Tracleer targets natural pockets on your cells known as endothelin receptors. There are a couple of types of these receptors: Endothelin receptor subtype A and subtype B.

In PAH, endothelin has higher than normal levels in the body. Normally, endothelins cause blood vessels to get smaller or constrict. Tracleer and other drugs in its class work to block these endothelin receptors to reduce the constriction of the arteries, which relaxes the arteries and reduces the pressure.

Tracleer is available as a tablet to take by mouth.

Drug Facts

Generic Name: Bosentan

Brand Name(s): Tracleer

Drug Availability: Prescription

Administration Route: Oral

Therapeutic Classification: Endothelin antagonist

Available Generically: Yes

Controlled Substance: N/A

Active Ingredient: Bosentan

Dosage Form(s): Tablet

What Is Tracleer Used For?

The Food and Drug Administration (FDA) approved Tracleer to help improve symptoms of PAH (high blood pressure in the lungs).

Tracleer may be prescribed for the following:

  • To improve the ability to exercise
  • Decrease worsening of symptoms and progression of PAH
  • World Health Organization (WHO) classification II to IV PAH, certain types of PAH with an unknown cause, and genetic PAH
  • PAH associated with diseases related to your connective tissue
  • PAH associated with heart failure

Tracleer may be prescribed for the following in children 3 years and older:

  • Certain types of PAH with an unknown cause and genetic PAH to improve blood flow and exercise ability.

How to Take Tracleer

Always follow directions from your prescriber on how to take Tracleer

Generally, you can take Tracleer with or without food, usually twice daily, at least 12 hours apart.

The tablets for oral suspension can be mixed with water to make a liquid formulation. For the dispersal tablets, you can divide them in half, but do not break them into quarters.

People of child-bearing potential must have a negative pregnancy test before starting this medication. Tracleer has shown major birth defects in animal studies. Therefore, do a pregnancy test monthly while taking it and use two forms of birth control during treatment and at least one month after stopping it.

Storage

Store Tracleer in a cool and dry place. In general, medications should be kept away from areas of high heat, like above your stove, or in humid areas, like your bathroom. These environments can impact how well medications work.

It is also important to keep this medication out of reach of children and pets to prevent accidental consumption. This medication requires participation in the REMS program. The program is designed to ensure that the drug you’re going to be taking has benefits that outweigh its risks.

Off-Label Uses

Aside from its FDA-approved uses, bosentan may be prescribed off-label for some health conditions, such as:

  • Ulcers or open sores found in systemic sclerosis, a disease that can cause your skin to become hardened or tightened 
  • Raynaud phenomenon in systemic sclerosis. If you feel this, you may notice that your fingers, and sometimes toes, turn blue or white when it gets cold and bright red when it warms up.
  • Persistent pulmonary hypertension of the newborn, a life-threatening neonatal condition

How Long Does Tracleer Take to Work?

Studies have shown improvements in PAH symptoms in as little as four weeks. If you are not feeling better after taking it longer than 12 weeks, it is important to contact your prescriber. 

What Are the Side Effects of Tracleer?

This is not a complete list of side effects, and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your healthcare provider or a pharmacist. You may report side effects to the FDA at fda.gov/medwatch or 800-FDA-1088.

Common Side Effects

The most common side effects of Tracleer may include:

  • Infection of your airways
  • Headache
  • Fever
  • Anemia (low red blood cell levels)
  • Flushing
  • Low blood pressure (hypotension)
  • Sinusitis
  • Joint pain
  • Irregular heartbeat

Severe Side Effects

Call your healthcare provider immediately if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects can include the following:

  • Liver toxicity
  • Fluid buildup
  • Chest pain or abnormal heartbeat
  • Fetal harm: Tracleer may cause harm to the fetus if used during pregnancy.

Long-Term Side Effects

Tracleer is a relatively well-tolerated medication, and long-term side effects are limited. However, although rare, liver damage is a potentially severe complication.

Report Side Effects

Tracleer may cause other side effects. Call your healthcare provider if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your healthcare provider may send a report to the FDA's MedWatch Adverse Event Reporting Program or by phone (800-332-1088).

Dosage: How Much Tracleer Should I Take?

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The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage forms (tablets or tablets for oral suspension):
    • For pulmonary arterial hypertension:
      • Adults—At first, 62.5 milligrams (mg) two times a day (morning and evening) for 4 weeks. Your doctor may increase your dose up to 125 mg two times a day. If you are also taking this medicine with ritonavir for at least 10 days, starting dose is 62.5 mg once a day or every other day as directed by your doctor.
      • Children older than 12 years of age and weighs more than 40 kilograms (kg) (88 pounds)—At first, 62.5 mg two times a day. Your doctor may increase your dose to 125 mg two times a day after 4 weeks.
      • Children older than 12 years of age and weighs less than 40 kilograms (kg) (88 pounds)—62.5 mg two times a day.
      • Children 12 years of age and younger—Dose is based on body weight and must be determined by your doctor.
        • Weighs more than 24 to 40 kilograms (kg)—64 mg two times a day.
        • Weighs more than 16 to 24 kg—48 mg two times a day.
        • Weighs more than 8 to 16 kg—32 mg two times a day.
        • Weighs 4 to 8 kg—16 mg two times a day.

Modifications

Due to the risk of liver problems associated with Tracleer, your healthcare provider may monitor liver proteins known as AST and ALT. Increased AST and ALT can indicate liver damage. Your healthcare provider will make specific changes to your dosage or treatment regimen based on your AST and ALT values and symptoms.

Consult with your healthcare provider for any questions and only make changes as instructed by your healthcare provider. 

If AST and ALT are between three to five times above the normal level:

  • If you are an adult, your healthcare provider may decrease the dose or can also pause/stop your treatment and restart once the AST and ALT values return to the levels they were before the treatment started.
  • For children under 12 years old or adolescents less than 88 pounds, the healthcare provider may pause/stop the treatment and restart once the AST and ALT values return to the levels they were before the treatment started.

If AST and ALT are between five and eight times above the normal level, regardless of age, your healthcare provider will most likely pause or stop your treatment. You can restart once your AST and ALT values return to their normal levels.

If AST and ALT are over eight times above the normal level, regardless of age, your healthcare provider will most likely stop your treatment permanently and never restart.

Missed Dose

If you miss a dose of Tracleer, take it as soon as you remember. If you are close to the next dose, then skip the missed dose and take only the next scheduled one.

You should not take more than one dose at once. If you miss a dose of Tracleer, your symptoms may not improve.

Overdose: What Happens If I Take Too Much Tracleer?

In studies, Tracleer has been given in doses as high as 2,400 milligrams in people for two months without any major side effects.

The most commonly experienced side effect with a high dose was a headache. One case has been reported where a person took 10,000 milligrams. They reported the following adverse reactions:

  • Nausea and vomiting
  • Low blood pressure
  • Dizziness
  • Sweating
  • Blurred vision

Treatment for an overdose involves addressing the symptoms.

What Happens If I Overdose On Tracleer?

If you think you or someone else may have overdosed on Tracleer, call a healthcare provider or the Poison Control Center (800-222-1222).

If someone collapses or isn't breathing after taking Tracleer, call 911 immediately.

Precautions

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It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly. Blood tests are needed to check your liver function before you start using bosentan and each month after that. Urine tests may also be needed to check for unwanted effects.

Using this medicine while you are pregnant can cause very serious birth defects. Use two forms of effective birth control to keep from getting pregnant while you are using this medicine (even if the medicine is temporarily stopped), and for at least one month after you stop taking the medicine. The most effective forms of birth control are hormone birth control pills, patches, shots, vaginal rings, or implants, an IUD, or a vasectomy (for men). One of these forms of birth control should be combined with a condom, a diaphragm, or a cervical cap. If a woman has had tubal ligation, she does not need to use a second form of birth control. If you think you have become pregnant while using this medicine, tell your doctor right away.

You must have a negative pregnancy test before you will be allowed to take this medicine. You will also be required to have a pregnancy test every month during your treatment and for 1 month after your last dose. If you miss a period while you are using this medicine, tell your doctor right away.

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, vomiting, or yellow eyes or skin. These could be symptoms of a serious liver problem.

Bosentan may decrease the amount of sperm men make and affect their ability to have children. If you plan to have children, talk with your doctor before using this medicine.

This medicine may cause fluid retention (edema) in some patients. Check with your doctor right away if you are gaining weight rapidly, have swelling in your hands, ankles, feet, or all over the body, or if you have trouble with breathing while you are using this medicine.

Pulmonary edema may occur while using this medicine. Check with your doctor right away if you have chest pain, difficult, fast, noisy breathing, sometimes with wheezing, blue lips and fingernails, pale skin, increased sweating. coughing that sometimes produces a pink frothy sputum, or shortness of breath.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

What Are Reasons I Shouldn't Take Tracleer?

The reasons for not taking Tracleer are listed below:

  • If you are pregnant: Tracleer should be avoided because it can cause harm to the fetus.
  • If you are taking cyclosporine A, a medication that decreases how much your immune system works: This medication can increase the levels of Tracleer in your body.
  • If you are taking glyburide (brand names include Diabeta, Micronase, and Glynase), a medication used for diabetes: This combination may increase the risk of liver damage.
  • If you have ever had an allergic reaction to bosentan or any of the ingredients in Tracleer

What Other Medications Interact With Tracleer?

Tracleer has interactions with other medications. Before starting it, tell your healthcare provider about all current substances you take, including prescription and over-the-counter (OTC) medications, vitamins, and herbal supplements.

Once Tracleer is absorbed in the body, it undergoes chemical changes by a protein family known as the cytochrome P450 (CYP450) family. Generally, drugs that block how well these proteins work (known as “inhibitors”) can increase how much Tracleer is in the body. This can enhance the effects of the medication, potentially causing side effects.

Examples of CYP450 inhibitors that interact with Tracleer include:

It is not recommended to take these drugs with Tracleer. Ask your healthcare provider or pharmacist if you are unsure whether you are taking a CYP450 inhibitor.

Other drugs known as CYP450 inducers can increase the work of CYP450 proteins. When taken with Tracleer, they can decrease how well Tracleer works in the body.

Some examples of CYP450 inducers include:

Tracleer can also reduce how well hormonal contraceptives work, so you should not rely on hormonal contraception alone during treatment. Instead, use another reliable form of contraception. Ask your healthcare provider about other effective contraceptive options.

What Medications Are Similar?

Other medications in the endothelin receptor antagonist drug class include:

These medications work similarly to Tracleer, the only difference being if it targets one specific protein.

Some other medications that can be used for PAH are:

  • Calcium channel blockers, such as diltiazem and Procardia (nifedipine)
  • Prostanoids, such as Flolan or Veletri (epoprostenol), Remodulin or Orenitram (treprostinil), and Ventavis (iloprost)
  • PDE5 inhibitors, such as Viagra (sildenafil), Cialis (tadalafil), and vardenafil
  • Guanylate cyclase stimulants, such as Adempas (riociguat)

This is a list of drugs also prescribed for PAH. It is NOT a list of drugs recommended to take with Tracleer.

Frequently Asked Questions

  • What side effects should I expect with Tracleer?

    Tracleer's more common side effects include nausea, headaches, and respiratory tract infections. If you experience nausea, try taking this medication with food.

  • I see that my liver proteins (AST/ALT) are high in my lab reports. Should I adjust the dose myself?

    Your healthcare provider will monitor your liver by taking blood tests, as the medication can cause liver damage. You should not adjust or stop any medication on your own unless instructed by your healthcare provider. 

  • Is Tracleer expensive? Is there a way I can get help paying for it?

    Tracleer, and other medications in the class, are specialty drugs. You will likely need to get it from a specialty pharmacy.

    Tracleer can be an expensive medication. However, there may be prescription assistance programs that can help you afford it. If cost concerns you, ask your healthcare provider or pharmacist about available programs.

  • What classifies pulmonary arterial hypertension?

    Hypertension, or high blood pressure, occurs when your blood vessels get smaller. In the case of PAH, the blood in your pulmonary arteries reach a pressure of 25 millimeters of mercury (mmHg) or higher; the range of this type of pressure is usually between 18 to 25 millimeters of mercury.

    There are different classifications and types of PAH. The ways that PAH is classified by the WHO include the following:

    • I: You have no limitation on your usual physical activity, and ordinary physical activity does not cause an increase in shortness of breath, fatigue, chest pain, or lightheadedness.
    • II: You have mild limitations on your physical activity. You also experience no discomfort at rest, but regular physical activity causes an increase in shortness of breath, fatigue, chest pain, or lightheadedness.
    • III: You have extensive limitations of physical activity. You also experience no discomfort at rest, but less than normal physical activity causes increased shortness of breath, fatigue, chest pain, or lightheadedness.
    • IV: You cannot perform physical activity at rest and may have signs of right-sided heart failure. Shortness of breath and fatigue may also be present at rest, and any physical activity increases symptoms.

How Can I Stay Healthy While Taking Tracleer?

PAH is a serious medical condition that can be disabling and even life-threatening. This is why it's important to take care of yourself and your health while being treated.

Take your medication exactly as prescribed by your healthcare provider to keep your symptoms under control. If you have trouble remembering to take it, try using a pillbox or medication app reminders on your phone.

Stay up-to-date with vaccinations, such as for flu and pneumococcal pneumonia, and other appropriate immunizations to prevent infections that can worsen PAH.

Exercise can be an effective accessory therapy to improve functional capacity and quality of life. However, recommendations for exercise can differ from person to person, so work with a healthcare provider to create an optimal exercise plan.

Medical Disclaimer

Verywell Health's drug information is meant for educational purposes only and is not intended to replace medical advice, diagnosis, or treatment from a healthcare provider. Consult your healthcare provider before taking any new medication(s). IBM Watson Micromedex provides some of the drug content, as indicated on the page.

The author would like to recognize and thank Chong Yol Gacasan Kim for contributing to this article.

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Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
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