Bosentan (Oral Route)

Bosentan relaxes the lungs’ blood vessels, which in turn brings down the blood pressure.

Overview:

Bosentan is a medicine that helps treat hypertension in the lungs’ vessels, medically called pulmonary arterial hypertension, in adults and kids aged 3 and over.

Bosentan belongs to a set of medicines called endothelin receptor antagonists, whose function is to help relax blood vessels, reducing blood pressure and letting the heart pump blood much more effectively.

Bosentan can be used for other reasons. For more information, consult your doctor as well as a pharmacist. This is available under the Tracleer brand name. It’s available in the form of a tablet that is taken two times daily, with food or without.

Conditions treated:

• Pulmonary arterial hypertension

Type of Medicine:

• Endothelin receptor antagonist

Side effects:

Along with its desired effects, Bosentan can trigger some undesirable effects. Of course, not all these effects do occur but for those which do, you may need to seek medical attention.

See your doctor at once if any of the effects below occur while using Tracleer:

More common:

• Yellow skin or eyes (jaundice)
• Fever with/without chills
• Dizziness
• Confusion
• Dark urine
• Blurred vision
• Lightheadedness or faintness when getting up on your feet
• Light-colored stools
• Sudden sweating
• Loss of appetite
• Stomach pain
• Nausea and vomiting
• Unusual fatigue or weakness

Less common:

• Swelling

Frequency unknown:

• Headache
• Hives
• Chills
• Chest pain
• Bleeding gums
• Black, tarry stools
• Blood in stools or urine
• Blue fingernails and lips
• Clay-colored stools
• Coughing that occasionally produces frothy, pink sputum
• Fast heartbeat
• Decrease in urine amount
• Coughing up blood
• Fainting
• Fever
• Difficult, noisy, fast breathing, occasionally with wheezing
• Fatigue on exertion
• Hives
• Irritation
• Hoarseness
• Increased sweating
• Itching
• Pale skin
• Swelling, stiffness, or joint pain
• Noisy, rattling breathing
• Huge, hive-like swelling on sex organs, legs, feet, hands, face, lips, eyelids, throat, or tongue
• Rash
• Red pinpoint spots on skin
• Shortness of breath
• Redness of skin
• Weight gain
• Troubled breathing while resting
• Swelling of the face, lips, eyelids, hands, legs, feet, ankles, or fingers
• Tightness of chest
• Trouble swallowing or breathing
• Difficult breathing with exertion
• Vomiting of blood
• Unusual bleeding/bruising
• Unpleasant odor of breath
• Wheezing

Get emergency medical attention at once should any of these overdose symptoms occur while using Bosentan:

Overdose symptoms:

• Increased heart rate

Some Tracleer side effects may happen that usually don’t need treatment. They may vanish during treatment while you adjust to Tracleer. In addition, your healthcare giver may help you prevent or ease some of the following effects. See your healthcare giver promptly if any of the side effects below persist, bother you, or you have some questions about them.

More common:

• Sore throat
• Stuffy/runny nose
• Redness of the arms, neck, face, and sometimes upper chest
• Muscle aches
• Feeling of warmth
• Racing, fast, irregular, or pounding pulse/heartbeat

Less common:

• Heartburn
• Acid/sour stomach
• Indigestion
• Stomach upset, pain, or discomfort

Monitoring Bosentan side effects

Due to the possible damage to your liver, make sure to have liver function tests carried out before starting treatment. Have the tests done every month as long as you’re using Tracleer. A doctor will help you manage your liver enzymes if they get raised. This may require that you stop taking Bosentan.

You should stop using Bosentan if your blood examinations for liver function tests are characterized by symptoms of unusual liver injury or function, or by a high level of total bilirubin (another liver function blood test) that’s more than twice the normal level.

Due to the possible harm to the unborn child, women must also test for pregnancy before starting Bosentan treatment and every month while they take the medication.

Make sure the number of your red blood cells is checked at the first and third month after starting your Tracleer treatment. You should then have this monitored once every three months so long as you’re taking Bosentan.

Dosage:

Read the drug guide given by your pharmacist prior to starting Bosentan treatment and every time you have a refill. Please consult your pharmacist/doctor if you’ve got any questions. Take Bosentan orally with or without meals, usually twice every day. You can take one dose in the morning and another in the evening or follow your doctor’s orders.

Dosage is determined by your weight, response to treatment, and medical condition. Your doctor will normally get you started on a smaller dose and then increase it after several weeks.

The recommended dosage of this medication in patients aged over 12 is 125 to 250 milligrams per day. For patients aged 12 and below, the recommended dose of Tracleer is 32 to 128 milligrams per day. In patients aged over 12 and weighing 40 kg, the recommended dosage is 125 milligram per day.

Use Bosentan on a regular basis to maximize its benefit. You should take the medication at the same intervals daily so you don’t forget a dose.

Women who may get pregnant or who are pregnant should avoid this medication completely. They shouldn’t touch the tablets or inhale its dust. Don’t crush Bosentan tablets or you’ll be badly exposed to the harmful dust of the medication.

Don’t stop using Bosentan unless you’re told to by your healthcare professional. Stopping your treatment suddenly may make your symptoms worse. If you want to stop using this medicine, speak to your healthcare professional about the best way to stop. If you have used too much Bosentan, notify your healthcare professional at once.

If you inadvertently miss a Bosentan dose, take it immediately you remember. Never take double doses at once. If it’s around time for the next dose, just wait for it and skip the missed one. If your condition gets worse or persists, please tell your doctor.

Interactions:

When you’re taking Bosentan, it’s very important to let your healthcare giver know if you’re using any of the medications below. The following interactions have been picked out depending on their possible impact and are by no means all-inclusive.

You shouldn’t use Bosentan with any of these drugs. Your doctor may opt to change some of the drugs you use or not treat you with Bosentan.

• Glyburide
• Cyclosporine

You should not use Bosentan with any of these medications, but in some cases you may need to. If both medications are prescribed at the same time, your physician may modify the dose or change your frequency of using one or both medications.

• Cobicistat
• Axitinib
• Atazanavir
• Dienogest
• Bosutinib
• Daclatasvir
• Cobimetinib
• Doxorubicin
• Darunavir
• Desogestrel
• Deflazacort
• Elbasvir
• Doxorubicin Hydrochloride Liposome
• Hemin
• Drospirenone
• Estradiol
• Elvitegravir
• Ethynodiol
• Neratinib
• Fosamprenavir
• Enzalutamide
• Etonogestrel
• Ethinyl Estradiol
• Grazoprevir
• Gestodene
• Lopinavir
• Levonorgestrel
• Lopinavir
• Nifedipine
• Mestranol
• Olaparib
• Norethindrone
• Perampanel
• Norgestimate
• Simeprevir
• Ritonavir
• Saquinavir
• Piperaquine
• Norgestrel
• Venetoclax
• Tacrolimus
• Tipranavir
• Velpatasvir
• Voxilaprevir

If Bosentan is used with any of these medicines, there may be a higher risk for some side effects, but using Bosentan with any of the medicines may be your best form of treatment. If both drugs are prescribed at the same time, your doctor may change the frequency of taking one or both drugs or change the dose.

• Simvastatin
• Rifampin
• Lovastatin
• Atorvastatin
• Ketoconazole
• Ospemifene
• Sildenafil
• Warfarin

This list is by no means complete. Bosentan may interact with other medications, for example prescription and nonprescription drugs, herbal products, minerals, and vitamins. This medication guide does not list all possible Bosentan interactions.

Some drugs shouldn’t be taken around meal times or when eating some foods because interactions might occur. Interactions may also happen when you drink alcohol or smoke cigarettes while using certain drugs. Please discuss with your physician the use of Tracleer with food, alcoholic drinks, or tobacco.

Warnings:

It’s vitally important that your physician monitors your progress on a regular basis to ensure that Bosentan is working well. You will need blood tests to assess your liver function prior to starting treatment and every month after that. You may also need urine tests to check for adverse effects.

Using Bosentan while you’re pregnant may bring about extremely serious birth defects. Therefore, make sure to use two effective methods of birth control to prevent pregnancy while you’re taking Bosentan (even if it is stopped temporarily), and for not less than one month after you discontinue treatment.

The most effective birth control methods include birth control pills, shots, patches, implants, or vaginal rings, IUD (intrauterine device), or vasectomy (for males). You should combine one of these birth control methods with a condom, cervical cap, or a diaphragm. Women who have had tubal ligation need not use a second method of birth control. If you suspect that you’ve gotten pregnant while taking Bosentan, please tell your physician as soon as you can.

You need to take a pregnancy test before you can be allowed to take Bosentan. In addition, you will be required to take a pregnancy test each month during your treatment and for another month after your final dose. If you don’t see your monthly period while using Bosentan, make sure to notify your doctor promptly.

At first, the liver damage might not cause symptoms. You’ll only find out if you have early liver damage by taking a blood test. You must take a blood exam to assess your liver function prior to starting Bosentan and every month after that. These tests will be ordered by your healthcare professional. Frequent blood tests are vital because they assist your healthcare specialist stop or adjust your treatment to prevent permanent damage.

Tell your healthcare specialist if you’ve ever had liver issues, including liver issues while using other drugs. Be sure to call up your healthcare specialist immediately if you experience any of these signs of liver issues while using Tracleer: vomiting, nausea, fever, abdominal (stomach area) pain, and jaundice (yellowing of whites of eyes or the skin).

Tracleer may reduce the quantity of sperm you make and affect your ability to sire. If you intend to have kids, talk to your doctor prior to using Bosentan.

This medication can lead to edema (fluid retention) in some people. Check with your physician immediately if you’re rapidly gaining weight, have swelling all over your body, in your hands, feet, or ankles, or you have problems with breathing while taking Bosentan.

Pulmonary edema can occur while taking Bosentan. Please check with your primary healthcare provider at once if you have pale skin, blue fingernails and lips, chest pain, difficult, noisy, fast breathing occasionally with wheezing, coughing that occasionally produces frothy pink sputum, shortness of breath, or increased sweating.

Avoid taking alcohol while using Bosentan. It may add to your risk of liver issues. You must have regular blood tests to check how Tracleer affects you. Make sure to present yourself for all these tests.

If you need dental work, surgery, or emergency care, inform your dentist or healthcare professional that you’re taking Bosentan.

This medication can affect your level of blood sugar and affect the quantity of insulin you may need. Please discuss this with your healthcare specialist.

Report these life-threatening symptoms to your doctor right away, an allergic reaction (rash, hives, itching, tightness in the chest, troubled breathing, and swelling of lips, throat, or tongue). If you can’t reach him or her right now, call 911 for assistance or get emergency medical attention.

Report these serious symptoms to your doctor straight away, vomiting, nausea, fever, fatigue, abdominal pain, yellowing of whites of eyes or the skin, light-colored stools, dark-colored urine, unusual weakness/tiredness, and fast or abnormal heartbeats.

Other serious symptoms to report include a headache, flushing, stomach upset, dizziness, swelling of ankles/legs, runny nose, and sore throat. Don’t take other drugs unless you have discussed them with your physician. This includes herbal products, vitamins, minerals, and of course prescription and nonprescription drugs (also known as over-the-counter drugs).

Storage:

Keep Tracleer in a secure place where children cannot reach it. Don’t keep out of date medicines or medicines you no longer need. Ask your healthcare provider how you should get rid of any drug you don’t use.

Keep Bosentan at room temperature in a tightly sealed container, away from direct light, heat, and moisture. Keep Bosentan from freezing.

Don’t flush Bosentan tablets down your toilet or throw them into a drain. Ask your local garbage disposal service or pharmacist how you should safely dispose of unwanted medication.

Summary:

Bosentan is prescribed only by healthcare professionals who are under a special program. It’s only available to patients who meet the requirements of this program and agree to join it.

Your healthcare professional will provide you with detailed information about this special program. A specialty pharmacy will mail Tracleer to you. You’ll only get a month’s supply of this medication at a time.

Occasionally, your healthcare giver may prescribe Tracleer for other conditions not covered in this medication guide. Some of the possible uses of this medication may include high blood pressure and Eisenmenger syndrome, a medical condition linked to pulmonary hypertension caused by a birth defect.

Bosentan helps control symptoms of PAH but doesn’t cure the condition. It may take one or two months or even longer before you fully benefit from it. Don’t stop using Bosentan all of a sudden even if you start to feel better as this can make your symptoms worse.

You may need to take regular monthly blood tests during treatment to rule out anemia and to test liver function. Tell your healthcare professional about all medical conditions you may have, including liver problems. Also, inform him or her if you plan to breastfeed or are breastfeeding.

Tell your healthcare professional about all the drugs you take, such as prescription, nonprescription, herbal supplements, and vitamins. Don’t drive or use any machines or tools while taking Bosentan as doing so can cause dizziness, impairing your ability to properly operate machinery or drive.

While using Tracleer, women must use highly effective birth control methods or combine two methods (for example, a barrier method plus contraceptive pills) to prevent pregnancy in the course of treatment.

Don’t stop using Bosentan without your doctor’s knowledge. Some conditions can get worse when you suddenly stop taking the medication. Your dose may have to be decreased, so you might need to take less and less of the medication before you stop taking it completely.

Bosentan may interact with grapefruit and its juice and result in potentially serious effects. Talk to your healthcare giver about the consumption of grapefruit while you’re using this medication.