Bosentan
.svg)
Drug Status
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
NO
Known Teratogen
Definite
Pharmaceutical Class
Endothelin Receptor Antagonist
Controlled Drug Substance
No
Bosentan
Summary
Bosentan is used to treat pulmonary arterial hypertension (PAH), which is high blood pressure in the vessels that carry blood to the lungs. It can improve your ability to exercise and slow the progression of symptoms.
Bosentan is an endothelin receptor antagonist. It works by blocking the action of endothelin, a substance that causes blood vessels to narrow. This helps to relax and widen the blood vessels, improving blood flow and reducing blood pressure in the lungs.
For adults, the usual starting dose of Bosentan is 62.5 mg taken twice daily for 4 weeks, followed by a maintenance dose of 125 mg twice daily. For children aged 3 years and older, the recommended dose is 2 mg/kg twice daily. Always follow your doctor's instructions regarding dosage.
Common side effects of Bosentan include headache, respiratory tract infection, and edema. Serious adverse effects include liver damage, which requires regular monitoring, and potential birth defects if taken during pregnancy.
Bosentan can cause serious liver damage and birth defects. Regular liver function tests are required and it should not be used during pregnancy. Women of childbearing potential must use reliable contraception. Bosentan is contraindicated in patients with moderate to severe liver impairment and those taking cyclosporine A or glyburide.
Indications and Purpose
How does Bosentan work?
Bosentan is an endothelin receptor antagonist that blocks the action of endothelin, a substance that causes blood vessels to narrow. By blocking these receptors, Bosentan helps to relax and widen blood vessels, improving blood flow and reducing blood pressure in the lungs.
Is Bosentan effective?
Bosentan has been shown to improve exercise capacity and slow the progression of symptoms in patients with pulmonary arterial hypertension (PAH). Clinical trials demonstrated significant increases in 6-minute walk distance and improvements in hemodynamic parameters, such as cardiac index and pulmonary vascular resistance, supporting its effectiveness in treating PAH.
What is Bosentan?
Bosentan is used to treat pulmonary arterial hypertension (PAH) by improving exercise capacity and slowing symptom progression. It works by blocking endothelin receptors, which helps to relax blood vessels and improve blood flow. Regular monitoring is essential due to potential liver damage and birth defects.
Directions for Use
For how long do I take Bosentan?
Bosentan is typically used as a long-term treatment for pulmonary arterial hypertension (PAH). The duration of use depends on the patient's response to the medication and the doctor's assessment. It is important to continue taking Bosentan even if you feel well, and not to stop without consulting your doctor.
How do I take Bosentan?
Bosentan can be taken with or without food, usually twice a day in the morning and evening. There are no specific food restrictions, but it's important to take it at the same times each day to maintain consistent blood levels. Always follow your doctor's instructions regarding dosage and administration.
How long does it take for Bosentan to start working?
Bosentan may take 1 to 2 months or longer before you feel the full benefit. However, some improvement in exercise capacity can be noticed within a few weeks. It's important to continue taking the medication as prescribed, even if you don't feel immediate effects.
How should I store Bosentan?
Store Bosentan in its original container, tightly closed, at room temperature away from excess heat and moisture. Keep it out of reach of children. Do not store it in the bathroom. Dispose of unneeded medication through a take-back program, not by flushing it down the toilet.
What is the usual dose of Bosentan?
For adults, the usual starting dose of Bosentan is 62.5 mg taken twice daily for 4 weeks, followed by a maintenance dose of 125 mg twice daily. For children aged 3 years and older, the recommended dose is 2 mg/kg twice daily. Always follow your doctor's specific instructions regarding dosage.
Warnings and Precautions
Can Bosentan be taken safely while breastfeeding?
Women are advised not to breastfeed while taking Bosentan due to the potential for serious adverse reactions in the breastfed infant, such as fluid retention and hepatotoxicity. Consult your doctor for alternative treatments or feeding options.
Can Bosentan be taken safely while pregnant?
Bosentan is contraindicated during pregnancy due to the risk of serious birth defects. Women of childbearing potential must use two reliable forms of contraception and have monthly pregnancy tests. There is strong evidence from animal studies indicating fetal harm, and similar effects are expected in humans.
Can I take Bosentan with other prescription drugs?
Bosentan interacts with several medications, including cyclosporine A and glyburide, which are contraindicated. It can also affect hormonal contraceptives, making them less effective. Bosentan may interact with drugs metabolized by CYP2C9 and CYP3A4 enzymes, such as ketoconazole and warfarin, potentially altering their effectiveness.
Is Bosentan safe for the elderly?
Clinical studies of Bosentan did not include enough subjects aged 65 and older to determine if they respond differently from younger subjects. However, no specific dose adjustment is required for elderly patients. It's important for elderly patients to be monitored closely for side effects, especially liver function and fluid retention.
Is it safe to exercise while taking Bosentan?
Bosentan is used to treat pulmonary arterial hypertension and may improve the ability to exercise by reducing blood pressure in the lungs. However, if you experience any unusual symptoms during exercise, such as dizziness or shortness of breath, consult your doctor.
Who should avoid taking Bosentan?
Bosentan can cause serious liver damage and birth defects. Regular liver function tests are required, and it should not be used during pregnancy. Women of childbearing potential must use reliable contraception. Bosentan is contraindicated in patients with moderate to severe liver impairment and those taking cyclosporine A or glyburide.
Forms / Brands
