Bosentan (Oral route)
Use of bosentan may result in hepatotoxicity or liver failure. Measure serum aminotransferase levels prior to initiation of treatment and then monthly. Stop treatment if liver aminotransferase elevations are accompanied by clinical symptoms of hepatotoxicity, or increases in bilirubin greater than or equal to 2 times ULN occur. Use of bosentan is very likely to produce major birth defects if used by pregnant women. Exclude pregnancy before initiation of therapy and prevent pregnancy thereafter by the use of 2 forms of reliable contraception for the duration of treatment and for 1 month after stopping bosentan. If the patient has a tubal sterilization or Copper T 380A IUD or LNg 20 IUS inserted, no other contraception is needed. Monthly pregnancy tests should be obtained. Bosentan may be prescribed only through the Tracleer(R) Access Program (TAP) .
Endothelin Receptor Antagonist
Uses of This Medicine:
Bosentan is used to treat the symptoms of pulmonary arterial hypertension. This is the high blood pressure that occurs in the main artery that carries blood from the right side of the heart (the ventricle) to the lungs. When the smaller blood vessels in the lungs become more resistant to blood flow, the right ventricle must work harder to pump enough blood through the lungs. Bosentan works by blocking a hormone (a naturally occurring substance), that is found in the blood and lungs in large quantities of the people with pulmonary arterial hypertension. Bosentan helps by increasing the supply of blood to the lungs and reducing the workload of the heart.
This medicine is available only under a special restricted distribution program called the Tracleer Access Program (T.A.P.).
Before Using This Medicine:
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Appropriate studies have not been performed on the relationship of age to the effects of bosentan in the pediatric population. Safety and efficacy have not been established.
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of bosentan in the elderly. However, elderly patients are more likely to have age-related heart, liver, or kidney problems, which may require caution in patients receiving bosentan.
|All Trimesters||X||Studies in animals or pregnant women have demonstrated positive evidence of fetal abnormalities. This drug should not be used in women who are or may become pregnant because the risk clearly outweighs any possible benefit.|
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Doxorubicin Hydrochloride Liposome
Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Estradiol Cypionate
- Estradiol Valerate
- Ethinyl Estradiol
- Ethynodiol Diacetate
- Medroxyprogesterone Acetate
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Other medical problems—
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
- Edema (fluid retention or body swelling) or
- Heart failure or
- Liver disease, mild or
- Lung problems—Use with caution. Bosentan may make these conditions worse.
- Liver disease, moderate or severe—Should not be used in patients with this condition.
Proper Use of This Medicine:
Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. Also, do not change the dose or stop using this medicine without checking first with your doctor.
It is very important that you understand the requirements of the Tracleer® access program, and become familiar with the Tracleer® educational materials and Patient Medication Guide. Direct any questions to your doctor or pharmacist before starting bosentan therapy.
You may take this medicine with or without food.
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 form (tablets):
- 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 above 12 years of age and weighing less than 40 kilograms (kg) (88 pounds)—62.5 mg two times a day.
- Children below 12 years of age—Use and dose must be determined by your doctor.
- For pulmonary arterial hypertension:
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Precautions While Using This Medicine:
It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and to check for unwanted effects.
It is also important that your doctor does a blood test to check your liver function before you start bosentan and each month after that.
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 a 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. If you miss a period while you are using this medicine, tell your doctor right away.
Liver problems may occur while you are using this medicine. Stop using this medicine and check with your doctor right away if you are having more than one of these symptoms: dark urine, fever with or without chills, light colored stools, loss of appetite, nausea and vomiting, skin rash, stomach pain, unusual tiredness, or yellow eyes or skin.
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. Stop using this medicine and 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.
Side Effects of This Medicine:
- More common
- Blurred vision
- dark urine
- faintness or lightheadedness when getting up from a lying or sitting position
- fever with or without chills
- light-colored stools
- loss of appetite
- nausea and vomiting
- stomach pain
- sudden sweating
- unusual tiredness or weakness
- yellow eyes or skin
- Less common
- Incidence not known
- Black, tarry stools
- bleeding gums
- blood in the urine or stools
- blue lips and fingernails
- chest pain
- clay-colored stools
- coughing that sometimes produces a pink frothy sputum
- coughing up blood
- dark urine
- decrease in the amount of urine
- difficult, fast, or noisy breathing, sometimes with wheezing
- fast heartbeat
- fatigue on exertion
- increased sweating
- joint pain, stiffness, or swelling
- large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
- noisy, rattling breathing
- pale skin
- pinpoint red spots on the skin
- redness of the skin
- shortness of breath
- swelling of the eyelids, face, lips, hands, fingers, legs, ankles, or feet
- tightness in the chest
- troubled breathing at rest
- troubled breathing or swallowing
- troubled breathing with exertion
- unpleasant breath odor
- unusual bleeding or bruising
- vomiting of blood
- weight gain
- Symptoms of overdose
- Increased heart rate
- More common
- Fast, irregular, pounding, or racing heartbeat or pulse
- feeling of warmth
- muscle aches
- redness of the face, neck, arms, and occasionally upper chest
- sore throat
- stuffy or runny nose
- Less common
- Acid or sour stomach
- stomach discomfort, upset, or pain
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:
Get emergency help immediately if any of the following symptoms of overdose occur:
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
Last Updated: 11/4/2014