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Tracleer
Tracleer (bosentan) is an endothelin receptor antagonist prescribed for the treatment of pulmonary arterial hypertension (PAH), a condition in which the blood pressure in the lungs' arteries is abnormally high. By blocking the action of endothelin, a substance that causes blood vessels to constrict, Tracleer helps relax the blood vessels in the lungs, thereby reducing blood pressure and improving the ability to exercise and delay the progression of PAH.
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Frequently Asked Questions
How long does it take for Tracleer to start working?
It may take a few weeks to notice the effects of Tracleer. Improvement in exercise capacity and reduction in symptoms may occur after 4 to 8 weeks of treatment.
Can Tracleer be taken with food?
Yes, Tracleer can be taken with or without food. It’s important to take it at the same times each day for consistency.
Can I stop taking Tracleer abruptly?
No, stopping Tracleer suddenly can worsen PAH symptoms. Consult your healthcare provider before making any changes to your medication.
Is Tracleer safe for long-term use?
Tracleer can be used long-term under close medical supervision. Regular monitoring of liver function and blood counts is necessary to avoid serious side effects.
What should I do if I become pregnant while on Tracleer?
If you become pregnant while taking Tracleer, stop the medication immediately and contact your healthcare provider. Two forms of contraception are recommended while on Tracleer due to the high risk of birth defects.
Comprehensive Drug Guide
How Does Tracleer Work?
Tracleer works by blocking endothelin-1 (ET-1), a chemical in the body that causes blood vessels to tighten and narrow. By inhibiting the endothelin receptors, Tracleer prevents blood vessel constriction, leading to relaxation of the pulmonary arteries. This helps to lower blood pressure in the lungs and improves the heart’s ability to pump blood, alleviating symptoms of PAH.
Common Dosages
- Tablets: 62.5 mg and 125 mg
Typical Dosing
- Initial dose: 62.5 mg twice daily for the first 4 weeks.
- Maintenance dose: After 4 weeks, the dose is typically increased to 125 mg twice daily, based on the patient’s response and tolerance to the medication.
Typical Dosing
FDA Approved Indications
- Pulmonary arterial hypertension (PAH) to improve exercise ability and reduce symptoms such as shortness of breath and fatigue.
Who Shouldn't Take Tracleer?
- Severe liver impairment
- Pregnancy or plans to become pregnant (due to the risk of birth defects)
- Concomitant use of cyclosporine A or glyburide
Advice From The Pharmacist
- Tracleer should be taken exactly as prescribed, usually twice daily, with or without food.
- Women of childbearing potential must use two reliable forms of contraception during treatment due to the high risk of birth defects.
- Regular blood tests are required to monitor liver function, as Tracleer can cause liver damage.
- If a dose is missed, take it as soon as possible, but do not double the dose to make up for a missed one.
Side Effects of Tracleer
Common Side Effects
- Headache
- Fatigue
- Respiratory infections
- Edema (swelling of the legs or ankles)
Uncommon/Severe Side Effects
- Liver damage (elevated liver enzymes)
- Decreased hemoglobin (anemia)
- Birth defects if taken during pregnancy
Risks and Warnings of Tracleer
- Liver Toxicity: Tracleer can cause liver damage, which is why regular monitoring of liver function tests is crucial.
- Pregnancy Risk: Tracleer can cause serious birth defects. Women must take a pregnancy test before starting the medication and use two forms of contraception during treatment.
- Anemia: Tracleer can lower red blood cell counts, leading to anemia, so regular blood monitoring is important.
Interactions with Tracleer
Common Drug Interactions
- Cyclosporine A and glyburide: These drugs should not be used with Tracleer due to potential serious interactions.
- Rifampin: May reduce the effectiveness of Tracleer.
- Warfarin: Tracleer may reduce the effectiveness of blood thinners like warfarin, requiring dose adjustments.
Alternatives to Tracleer
- Revatio (sildenafil): A phosphodiesterase-5 inhibitor used for treating PAH.
- Adcirca (tadalafil): Another phosphodiesterase-5 inhibitor for PAH.
- Opsumit (macitentan): An alternative endothelin receptor antagonist for treating PAH.
- Letairis (ambrisentan): Another endothelin receptor antagonist for pulmonary arterial hypertension.
