Generic Name: Bosentan Brand Name(s): .

Uses

What is Bosentan used for?

Bosentan is commonly used to treat high blood pressure in the lungs (pulmonary arterial hypertension). This condition is thought to be caused by increased levels of a certain natural substance (endothelin-1). This medication blocks the effects of endothelin-1, thereby helping to decrease the blood pressure in the lungs, slow the worsening of symptoms from the disease, and improve your ability to exercise.

How should I take Bosentan?

Take this medication by mouth with or without food, usually twice daily (in the morning and evening) or as directed by your doctor.

Dosage is based on your medical condition, weight, and response to treatment. Your doctor will usually start you on a lower dose of this medication and then increase the dose after several weeks.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.

Do not stop taking this medication without consulting your doctor. Some conditions may become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased.

Women who are pregnant or who may become pregnant should not handle the tablets or breathe the dust from this medication. Do not crush the tablets because doing so will increase exposure to the dust.

How do I store Bosentan?

Bosentan is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Bosentan in the bathroom or the freezer. There may be different brands of Bosentan that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Bosentan down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Bosentan?

Before taking bosentan, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, anemia.

This drug may make you dizzy. Alcohol or marijuana can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana. Alcohol may also increase the risk of serious liver problems.

This medication must not be used during pregnancy. It may harm an unborn baby. Therefore, it is important to prevent pregnancy while using this medication. Discuss the use of at least two reliable forms of birth control (such as condoms, birth control pills) with your doctor. If you become pregnant or think you may be pregnant, tell your doctor right away.

It is not known whether this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this medication is not recommended. Consult your doctor before breast-feeding.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Bosentan during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking this Bosentan. This Bosentan is pregnancy risk category X according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Bosentan?

Dizziness, flushing, upset stomach, or tiredness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if any of these unlikely but serious side effects occur: fast/pounding heartbeat, extreme tiredness, swelling of the ankles/feet, sudden/unexplained weight gain.

Tell your doctor right away if any of these rare but very serious side effects occur: fainting, shortness of breath, coughing up blood.

In men, this medication can decrease sperm production, which may affect the ability to father a child. Talk to your doctor for more details.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: fever, swollen lymph nodes, rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Bosentan?

Some products that may interact with this drug include: cyclosporine, glyburide.

Other medications can affect the removal of bosentan from your body, which may affect how bosentan works. Examples include amiodarone, cimetidine, tacrolimus, St. John’s wort, azole antifungals (such as itraconazole, ketoconazole), macrolide antibiotics (such as erythromycin), HIV protease inhibitors (such as ritonavir), rifamycins (such as rifabutin), among others.

This drug can speed up the removal of other drugs from your body, which may affect how they work. Examples of affected drugs include “statin” cholesterol medications (such as simvastatin, lovastatin), warfarin, certain products used to treat chronic hepatitis C (asunaprevir, ombitasvir/paritaprevir/ritonavir), among others.

This medication may decrease the effectiveness of hormonal birth control such as pills, patch, or ring. This could cause pregnancy. Discuss with your doctor or pharmacist about using an additional reliable birth control method while using this medication. Also tell your doctor if you have any new spotting or breakthrough bleeding, because these may be signs that your birth control is not working well.

Bosentan may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Bosentan?

Bosentan may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

What health conditions may interact with Bosentan?

Bosentan may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Bosentan.

What is the dose of Bosentan for an adult?

Usual Adult Dose for Pulmonary Hypertension

Initial dose: 62.5 mg orally twice a day for 4 weeks

Maintenance dose: Following initial dose, increase to 125 mg orally twice a day

Comments:

-Doses above 125 mg twice a day did not appear to confer additional benefit sufficient enough to offset increased risk of hepatotoxicity.

Use: For the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) to improve exercise ability and to decrease clinical worsening.

What is the dose of Bosentan for a child?

Usual Pediatric Dose for Pulmonary Hypertension

3 to 12 years:

4 kg to 8 kg: 16 mg orally twice a day

Greater than 8 kg to 16 kg: 32 mg orally twice a day

Greater than 16 kg to 24 kg: 48 mg orally twice a day

Greater than 24 kg to 40 kg: 64 mg orally twice a day

Greater than 12 years:

-Less than 40 kg: 62.5 mg orally twice a day

-Greater than 40 kg: 62.5 mg orally twice a day for 4 weeks, then increase to 125 mg orally twice a day

Use: For use in pediatric patients 3 years or older with idiopathic or congenital PAH to improve pulmonary vascular resistance, which is expected to result in an improvement in exercise ability

Liver Dose Adjustments

Mild liver dysfunction: No adjustment recommended.

Moderate to severe liver dysfunction and/or elevated aminotransferases greater than 3 times the upper limit of normal: Use should be avoided.

Dose Adjustments

Patients Developing Aminotransferase Elevations:

-Discontinue this drug if liver aminotransferase elevations are accompanied by clinical symptoms of hepatotoxicity (e.g., nausea, vomiting, fever, abdominal pain, jaundice, unusual lethargy, or fatigue) or bilirubin 2 times the upper limit of normal.

Adults and Pediatric Patients Greater Than 12 Years and Greater than 40 kg:

-ALT/AST greater than 3 times the upper limit of normal (3 x ULN) and less than or equal to 5 x ULN: Confirm by another aminotransferase test; if confirmed, reduce daily dose to 62.5 mg orally twice a day or interrupt treatment, and monitor aminotransferase levels at least every 2 weeks. If aminotransferase levels return to pretreatment values, continue or reintroduce the treatment as appropriate. If this drug is reintroduced it should be at 62.5 mg orally twice a day; aminotransferase levels should be checked within 3 days and thereafter according to the recommendations above.

-ALT/AST greater than 5 x ULN but less than or equal to 8 x ULN: Confirm by another aminotransferase test; if confirmed, stop treatment and monitor aminotransferase levels at least every 2 weeks. Once the aminotransferase levels return to pretreatment values, consider reintroduction of treatment at 62.5 mg orally twice a day; aminotransferase levels should be checked within 3 days and thereafter according to the recommendations above.

-ALT/AST greater than 8 x ULN: Treatment should be stopped and reintroduction should not be considered due to lack of experience with reintroduction in these circumstances.

All Other Pediatric Patients:

-ALT/AST greater than 3 times the upper limit of normal (3 x ULN) and less than or equal to 5 x ULN: Confirm by another aminotransferase test; if confirmed, interrupt treatment with no prior dose reduction. If aminotransferase levels return to pretreatment values, reintroduce at the dose used prior to treatment interruption; aminotransferase levels should be checked within 3 days and thereafter according to the recommendations above.

-ALT/AST greater than 5 x ULN but less than or equal to 8 x ULN: Confirm by another aminotransferase test; if confirmed, stop treatment and monitor aminotransferase levels at least every 2 weeks. Once the aminotransferase levels return to pretreatment values, consider reintroduction of treatment at the dose used prior to treatment interruption; aminotransferase levels should be checked within 3 days and thereafter according to the recommendations above.

-ALT/AST greater than 8 x ULN: Treatment should be stopped and reintroduction should not be considered due to lack of experience with reintroduction in these circumstances.

Body weight below 40 kg in patients 12 years of age or older:

-Initial and maintenance dose: 62.5 mg orally twice a day; limited information on safety and efficacy of this drug in children between the ages of 12 and 18 years.

Coadministration of bosentan in patients who have been receiving ritonavir for at least 10 days:

-Initial dose: 62.5 mg orally once a day or every other day based upon individual tolerability

Coadministration of ritonavir in patients on bosentan: Discontinue bosentan at least 36 hours prior to initiation of ritonavir; after at least 10 days following initiation of ritonavir, resume bosentan at 62.5 mg orally once a day or every other day based upon individual tolerability

Pregnancy testing in females of reproductive potential: Initiate therapy only after a negative pregnancy test; obtain monthly pregnancy tests during treatment.

Treatment discontinuation: To avoid the potential for clinical deterioration, gradual dose reduction (62.5 mg orally twice a day for 3 to 7 days) should be considered.

How is Bosentan available?

Bosentan is available in the following dosage forms and strengths:

  • Tablet

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of Bosentan, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

Hello Health Group does not provide medical advice, diagnosis or treatment.

Sources

Review Date: January 11, 2018 | Last Modified: January 11, 2018

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