Bosentan

Generic name: Pronounced as (boe sen' tan)
Brand names
  • Tracleer®
Click on drug name to hear pronunciation

Medical Content Reviewed By HelloPharmacist Staff

Last Revised - 01/15/2022

For male and female patients:

Bosentan may cause liver damage. Tell your doctor if you have or have ever had liver disease. Your doctor will order a blood test to be sure your liver is working normally before you start taking bosentan and every month during your treatment. Keep all appointments with your doctor and the laboratory. Bosentan may damage the liver before causing symptoms. Regular blood tests are the only way to find liver damage before it becomes permanent and severe. If you experience any of the following symptoms, call your doctor immediately: nausea, vomiting, fever, stomach pain, yellowing of the skin or eyes, or extreme tiredness. Your doctor may reduce your dose, or temporarily or permanently stop your treatment with bosentan if you experience side effects or have abnormal lab results.

For female patients:

Do not take bosentan if you are pregnant or plan to become pregnant. Bosentan may harm the fetus. If you are able to become pregnant, you will need to take a pregnancy test before starting treatment, every month during treatment, and for 1 month after your treatment to show that you are not pregnant. Your doctor will order the pregnancy tests for you. You must use a reliable method of birth control during your treatment and for 1 month after your treatment. Hormonal contraceptives (birth control pills, patches, rings, shots, implants, and intrauterine devices) may not work well when used with bosentan and should not be used as your only method of birth control. Talk to your doctor about birth control methods that will work for you. In most cases you will be required to use two forms of birth control.

Call your doctor immediately if you have unprotected sex, think your birth control failed, miss a period or think that you may be pregnant while you are taking bosentan. Do not wait until your next appointment to discuss this with your doctor.

If you are a parent or guardian of a female patient who had not yet reached puberty, check your child regularly to see if she is developing any signs of puberty (breast buds, pubic hair) and let her doctor know about any changes.

Because of the risks of liver damage and birth defects, bosentan is only available through a restricted program called the Tracleer Risk Evaluation and Mitigation Strategy Program (Tracleer REMS). In order to receive bosentan you and your doctor must be registered with Tracleer REMS, and follow the programs requirements such as once a month liver function and pregnancy testing. Your doctor will register you in the program. Bosentan is only available at certain pharmacies that are registered with Tracleer REMS. Ask your doctor or pharmacist if you have any questions about how you can fill your prescription.

You will receive the manufacturer's patient information sheet (Medication Guide) when you begin treatment with bosentan and each time you refill the prescription. Read the information carefully each time and ask your doctor or pharmacist if you have any questions. You also can obtain the Medication Guide from the FDA website: http://www.fda.gov/Drugs/DrugSafety/ucm085729.htm.

Talk to your doctor about the risks of taking bosentan.

Bosentan is used to treat pulmonary arterial hypertension (PAH, high blood pressure in the vessels that carry blood to the lungs) in adults and children 3 years of age and older. Bosentan may improve the ability to exercise and slow the worsening of symptoms in patients with PAH. Bosentan is in a class of medications called endothelin receptor antagonists. It works by stopping the action of endothelin, a natural substance that causes blood vessels to narrow and prevents normal blood flow in people who have PAH.

Bosentan comes as a tablet and as a dispersible tablet (tablet that can be dissolved in liquid) to take by mouth. It is usually taken with or without food twice a day in the morning and evening. To help you remember to take bosentan, take it at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take bosentan exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

If you are taking the dispersible tablet, place the tablet in a small amount of liquid right before you take it. If your doctor has told you to take a half tablet, break the dispersible tablet carefully on the line. Take the half tablet as directed, and put the other half back in the opened blister in the package. Use the other half tablet within 7 days. Do not break the dispersible tablet into quarters.

Your doctor will probably start you on a low dose of bosentan and increase your dose after 4 weeks.

Bosentan controls the symptoms of PAH but does not cure it. It may take 1 to 2 months or longer before you feel the full benefit of bosentan. Continue to take bosentan even if you feel well. Do not stop taking bosentan without talking to your doctor. If you suddenly stop taking bosentan, your symptoms may get worse. Your doctor may decrease your dose gradually.

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

Before taking bosentan,

  • tell your doctor and pharmacist if you are allergic to bosentan, any other medications, or any of the ingredients in bosentan tablets or dispersible tablets.

  • do not take cyclosporine (Gengraf, Neoral, Sandimmune) or glyburide (DiaBeta, Glynase) while taking bosentan.

  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking. Be sure to mention any of the following: amiodarone (Nexterone, Pacerone); cholesterol-lowering medications (statins) such as atorvastatin (Lipitor, in Caduet), lovastatin (Altoprev), and simvastatin (Flolopid, Zocor, in Vytorin); diltiazem (Cardizem, Cartia, Diltzac, others); erythromycin (E.E.S., Eryc, PCE); fluconazole (Diflucan); gemfibrozil (Lopid); itraconazole (Onmel, Sporanox); ketoconazole ; rifampin (Rifadin, Rimactane, in Rifater, Rifamate); ritonavir (Norvir, in Kaletra, Viekira Pak, Technivie); voriconazole (Vfend); and warfarin (Coumadin, Jantoven). Many other medications may also interact with bosentan, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.

  • tell your doctor if you have or have ever had heart failure (condition in which the heart is unable to pump enough blood to the other parts of the body).

  • tell your doctor if you are breastfeeding or plan to breastfeed. Your doctor will probably tell you not to breastfeed while taking bosentan.

  • if you have phenylketonuria (PKU, an inherited condition in which a special diet must be followed to prevent damage to your brain that can cause severe intellectual disability), you should know that the dispersible tablets are sweetened with aspartame, a source of phenylalanine.

Talk to your doctor about drinking grapefruit juice while taking this medication.

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

  • Bosentan may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

    • headache

    • flushing

    • runny nose, sore throat, and other cold symptoms

    • joint pain

  • Some side effects can be serious. The following symptoms are uncommon, but if you experience any of them or those listed in the IMPORTANT WARNING section, call your doctor immediately or get emergency medical treatment:

    • hives; rash; itching; difficulty breathing or swallowing; swelling of the face, throat, tongue, lips, and eyes; hoarseness; fever; swollen lymph nodes; tiredness

    • swelling of the feet, ankles, or lower legs, sudden weight gain, more trouble with breathing than normal

    • new or worsening shortness of breath; new or worsening cough with or without blood; chest pain; fast, pounding, or irregular heartbeat

    • fainting

    • dizziness; pale skin; shortness of breath; weakness; fast, pounding, or irregular heartbeat

  • Male laboratory animals who were given medications similar to bosentan developed problems with their testicles and produced fewer sperm (male reproductive cells) than normal. It is not known if bosentan will damage the testicles or decrease the number of sperm produced in men. Talk to your doctor about the risks of taking bosentan if you would like to have children in the future.

  • Bosentan may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

  • If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA's Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services at 911.

Symptoms of overdose may include the following:

  • headache

  • nausea

  • vomiting

  • fast heartbeat

  • fainting

  • sweating

  • dizziness

  • blurred vision

Do not let anyone else take your medication. Ask your doctor any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Drug Interaction
Naratriptan Naratriptan Naratriptan may decrease the antihypertensive activities of Bosentan.
Zolmitriptan Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Bosentan.
Zidovudine Injection Zidovudine Injection The metabolism of Zidovudine can be increased when combined with Bosentan.
Trimipramine Trimipramine The metabolism of Trimipramine can be decreased when combined with Bosentan.
Tenofovir Tenofovir The metabolism of Tenofovir can be increased when combined with Bosentan.
Apomorphine Injection Apomorphine Injection Apomorphine may increase the hypotensive activities of Bosentan.
Tinidazole Tinidazole Bosentan may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Voriconazole Voriconazole The metabolism of Voriconazole can be increased when combined with Bosentan.
Pramlintide Injection Pramlintide Injection The therapeutic efficacy of Pramlintide can be increased when used in combination with Bosentan.
Insulin Detemir (rDNA Origin) Injection Insulin Detemir (rDNA Origin) Injection The therapeutic efficacy of Insulin detemir can be increased when used in combination with Bosentan.
Rasagiline Rasagiline Rasagiline may increase the hypotensive activities of Bosentan.
Rituximab Injection Rituximab Injection Bosentan may increase the hypotensive activities of Rituximab.
Dronabinol Dronabinol The metabolism of Dronabinol can be increased when combined with Bosentan.
Tretinoin Tretinoin The metabolism of Tretinoin can be increased when combined with Bosentan.
Everolimus Everolimus The metabolism of Everolimus can be increased when combined with Bosentan.
Ulipristal Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Bosentan.
Lurasidone Lurasidone Lurasidone may decrease the antihypertensive activities of Bosentan.
Vilazodone Vilazodone Vilazodone may decrease the antihypertensive activities of Bosentan.
Terbutaline Injection Terbutaline Injection Terbutaline may decrease the antihypertensive activities of Bosentan.
Azilsartan Azilsartan Azilsartan medoxomil may increase the hypotensive activities of Bosentan.
Roflumilast Roflumilast The metabolism of Roflumilast can be increased when combined with Bosentan.
Linagliptin Linagliptin The metabolism of Linagliptin can be increased when combined with Bosentan.
Rilpivirine Rilpivirine The excretion of Bosentan can be decreased when combined with Rilpivirine.
Abiraterone Abiraterone The metabolism of Bosentan can be decreased when combined with Abiraterone.
Ticagrelor Ticagrelor The metabolism of Bosentan can be decreased when combined with Ticagrelor.
Brentuximab Vedotin Injection Brentuximab Vedotin Injection The metabolism of Brentuximab vedotin can be increased when combined with Bosentan.
Ruxolitinib Ruxolitinib The metabolism of Ruxolitinib can be increased when combined with Bosentan.
Vandetanib Vandetanib The metabolism of Vandetanib can be increased when combined with Bosentan.
Vemurafenib Vemurafenib The metabolism of Bosentan can be increased when combined with Vemurafenib.
Vismodegib Vismodegib The metabolism of Vismodegib can be increased when combined with Bosentan.
Axitinib Axitinib The metabolism of Bosentan can be increased when combined with Axitinib.
Crizotinib Crizotinib The metabolism of Crizotinib can be increased when combined with Bosentan.
Enzalutamide Enzalutamide The metabolism of Enzalutamide can be increased when combined with Bosentan.
Mirabegron Mirabegron Mirabegron may decrease the antihypertensive activities of Bosentan.
Regorafenib Regorafenib The metabolism of Bosentan can be increased when combined with Regorafenib.
Bosutinib Bosutinib The metabolism of Bosutinib can be increased when combined with Bosentan.
Teriflunomide Teriflunomide The excretion of Bosentan can be decreased when combined with Teriflunomide.
Cabozantinib (thyroid cancer) Cabozantinib (thyroid cancer) The metabolism of Cabozantinib can be decreased when combined with Bosentan.
Alogliptin Alogliptin The therapeutic efficacy of Alogliptin can be increased when used in combination with Bosentan.
Ponatinib Ponatinib The metabolism of Ponatinib can be increased when combined with Bosentan.
Pomalidomide Pomalidomide The metabolism of Pomalidomide can be increased when combined with Bosentan.
Ado-trastuzumab Emtansine Injection Ado-trastuzumab Emtansine Injection The metabolism of Trastuzumab emtansine can be increased when combined with Bosentan.
Apixaban Apixaban The metabolism of Apixaban can be increased when combined with Bosentan.
Canagliflozin Canagliflozin The therapeutic efficacy of Bosentan can be increased when used in combination with Canagliflozin.
Dabrafenib Dabrafenib The metabolism of Bosentan can be increased when combined with Dabrafenib.
Ospemifene Ospemifene The metabolism of Ospemifene can be increased when combined with Bosentan.
Levomilnacipran Levomilnacipran The metabolism of Levomilnacipran can be increased when combined with Bosentan.
Vortioxetine Vortioxetine The metabolism of Vortioxetine can be increased when combined with Bosentan.
Perampanel Perampanel The metabolism of Perampanel can be increased when combined with Bosentan.
Lomitapide Lomitapide The metabolism of Lomitapide can be increased when combined with Bosentan.
Avanafil Avanafil Avanafil may increase the antihypertensive activities of Bosentan.
Testosterone Injection Testosterone Injection The metabolism of Testosterone can be increased when combined with Bosentan.
Caspofungin Injection Caspofungin Injection The excretion of Bosentan can be decreased when combined with Caspofungin.
Riociguat Riociguat Bosentan may increase the hypotensive activities of Riociguat.
Macitentan Macitentan Bosentan may increase the hypotensive activities of Macitentan.
Ziprasidone Injection Ziprasidone Injection Bosentan may increase the antihypertensive activities of Ziprasidone.
Cobicistat Cobicistat The serum concentration of Bosentan can be increased when it is combined with Cobicistat.
Lixisenatide Injection Lixisenatide Injection The therapeutic efficacy of Lixisenatide can be increased when used in combination with Bosentan.
Progestin-Only (drospirenone) Oral Contraceptives Progestin-Only (drospirenone) Oral Contraceptives The serum concentration of Drospirenone can be decreased when it is combined with Bosentan.
Theophylline Theophylline The metabolism of Theophylline can be increased when combined with Bosentan.
Tolmetin Tolmetin The therapeutic efficacy of Bosentan can be decreased when used in combination with Tolmetin.
Sulindac Sulindac The therapeutic efficacy of Bosentan can be decreased when used in combination with Sulindac.
Trazodone Trazodone Trazodone may decrease the antihypertensive activities of Bosentan.
Tranylcypromine Tranylcypromine Tranylcypromine may increase the hypotensive activities of Bosentan.
Thioridazine Thioridazine Thioridazine may decrease the antihypertensive activities of Bosentan.
Trifluoperazine Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Bosentan.
Sulfadiazine Sulfadiazine The metabolism of Bosentan can be decreased when combined with Sulfadiazine.
Warfarin Warfarin The metabolism of Warfarin can be increased when combined with Bosentan.
Triamterene Triamterene Triamterene may increase the hypotensive activities of Bosentan.
Sulfinpyrazone Sulfinpyrazone Bosentan may decrease the excretion rate of Sulfinpyrazone which could result in a higher serum level.
Valproic Acid Valproic Acid The metabolism of Bosentan can be decreased when combined with Valproic acid.
Tamoxifen Tamoxifen The metabolism of Tamoxifen can be increased when combined with Bosentan.
Tolbutamide Tolbutamide The metabolism of Tolbutamide can be increased when combined with Bosentan.
Tolazamide Tolazamide The metabolism of Tolazamide can be increased when combined with Bosentan.
Baclofen Baclofen The risk or severity of adverse effects can be increased when Baclofen is combined with Bosentan.
Thiotepa Injection Thiotepa Injection The metabolism of Thiotepa can be increased when combined with Bosentan.
Vincristine Injection Vincristine Injection The metabolism of Vincristine can be increased when combined with Bosentan.
Vinblastine Vinblastine The metabolism of Vinblastine can be increased when combined with Bosentan.
Aspirin Aspirin The metabolism of Bosentan can be increased when combined with Acetylsalicylic acid.
Trimethoprim Trimethoprim The metabolism of Trimethoprim can be increased when combined with Bosentan.
Timolol Timolol Timolol may increase the hypotensive activities of Bosentan.
Verapamil Verapamil The metabolism of Bosentan can be increased when combined with Verapamil.
Atenolol Atenolol Bosentan may decrease the excretion rate of Atenolol which could result in a higher serum level.
Teniposide Injection Teniposide Injection The metabolism of Bosentan can be increased when combined with Teniposide.
Tramadol Tramadol The metabolism of Tramadol can be increased when combined with Bosentan.
Ticlopidine Ticlopidine The metabolism of Ticlopidine can be increased when combined with Bosentan.
Indinavir Indinavir The serum concentration of Bosentan can be increased when it is combined with Indinavir.
Zafirlukast Zafirlukast The metabolism of Zafirlukast can be increased when combined with Bosentan.
Donepezil Donepezil The metabolism of Donepezil can be increased when combined with Bosentan.
Nelfinavir Nelfinavir The metabolism of Bosentan can be decreased when combined with Nelfinavir.
Sildenafil Sildenafil The metabolism of Sildenafil can be increased when combined with Bosentan.
Celecoxib Celecoxib The risk or severity of liver damage can be increased when Bosentan is combined with Celecoxib.
Tolterodine Tolterodine The metabolism of Tolterodine can be increased when combined with Bosentan.
Thalidomide Thalidomide The metabolism of Thalidomide can be increased when combined with Bosentan.
Colesevelam Colesevelam Colesevelam can cause a decrease in the absorption of Bosentan resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabeprazole Rabeprazole The metabolism of Bosentan can be decreased when combined with Rabeprazole.

Content provided by: AHFS® Patient Medication Information™. © Copyright, 2021. The American Society of Health-System Pharmacists