Tracleer (Bosentan)

Prescription medicineOnly Available By Prescription

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Example: If you find a product on Canada Drugs Direct for $50.00 and find the same product for $40.00 at another mail order pharmacy, we will provide you with a $12.50 discount, bringing your total to $37.50.

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What is a Generic Drug?

A generic drug is a copy of the brand-name drug with the same dosage, safety, strength, quality, consumption method, performance, and intended use. Before generics become available on the market, the generic company must prove it has the same active ingredients as the brand-name drug and works in the same way and in the same amount of time in the body.

The only differences between generics and their brand-name counterparts is that generics are less expensive and may look slightly different (eg. different shape or color), as trademarks laws prevent a generic from looking exactly like the brand-name drug.

Generics are less expensive because generic manufacturers don't have to invest large sums of money to develop a drug. When the brand-name patent expires, generic companies can manufacture a copy of the brand-name and sell it at a substantial discount.

Description

Tracleer (Bosentan) is an endothelin receptor antagonist. It blocks the effects of endothelin, a substance that constricts blood vessels and raises blood pressure. Tracleer is prescribed to help lower blood pressure within the lungs, a treatment for pulmonary arterial hypertension (PAH). Patients taking Tracleer may find an improvement in their ability to engage in physical activity, and the drug also aims to prevent the worsening of their condition.

Fact Table

Formula

C27H29N5O6S

License

US FDA, EMA

Bioavailability

~50%

Legal status

Prescription only (Rx)

Chemical Name

4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl) pyrimidin-4-yl]benzenesulfonamide

Elimination half-life

5.4 hours

Dosage (Strength)

62.5 mg, 125 mg tablets

Pregnancy

Not for use in pregnancy (Category X)

Brands

Tracleer

Protein binding

>98%

PubChem CID

5282138

MedlinePlus

a603015

ChEBI

CHEBI:51287

ATC code

C02KX01

DrugBank

DB00559

KEGG

D03007

Routes of administration

Oral

Directions

Tracleer is taken orally, and the dosage is determined by the healthcare provider based on individual needs and response to the medication. Generally, adults start with 62.5 mg taken twice daily for the first 4 weeks, followed by an increased maintenance dosage of 125 mg twice daily depending on tolerability. It’s important to consult a healthcare provider for exact dosing instructions.

Ingredients

Tracleer contains the active ingredient Bosentan. The medication may also include inactive ingredients, such as corn starch, hydroxypropyl cellulose, low substituted hydroxypropyl cellulose, povidone, and sodium starch glycolate.

Contraindications

The list below details the specific circumstances under which a patient should avoid this medication:

  • Pregnancy: Tracleer carries significant risks of birth defects
  • Use with Cyclosporine A: Increased risk of side effects due to higher levels of Bosentan
  • Use with Glyburide: Can potentially lead to liver injury when taken together
  • Hypersensitivity to Bosentan: Should not be used by individuals with known allergies to this medication

Cautions

  • Before starting treatment with Tracleer, consult a healthcare provider about the following:
    • Any medications you take
    • Other medical conditions you have
    • Allergies to any medications
    • Whether you’re pregnant or breastfeeding
  • Tracleer has the potential to cause fluid retention, which might necessitate medical intervention. Be alert for signs like swelling in your legs or sudden weight gain, as these could indicate fluid retention.
  • One serious concern is the development of pulmonary veno-occlusive disease (PVOD), a type of lung disease. If you experience symptoms like difficulty breathing or shortness of breath, it could indicate PVOD, and you may need to stop taking Tracleer.
  • It has been noted that Tracleer can reduce sperm count in some patients. This is a crucial consideration for men who plan to have children.
  • Tracleer can cause a decrease in hemoglobin and hematocrit. It's important to check your hemoglobin levels one month and three months after starting treatment and then every three months.

Side Effects

Like other medications, Tracleer may cause certain side effects. The most common side effects include respiratory tract infections, headaches, fainting, flushing, low blood pressure, sinusitis, joint pain, and irregular heartbeats.

Tracleer may also cause potentially severe side effects, such as fluid retention, resulting in swelling of the ankles and legs, and lower sperm counts in men, potentially affecting fertility. Anemia, indicated by low red blood cell levels, is another serious side effect. Patients should report any swelling, difficulty in breathing, or concerns about fertility to their healthcare provider. Regular blood tests are recommended to monitor for anemia. Immediate medical attention may be necessary for severe symptoms.

References:

  1. Tracleer (Bosentan) Product Monograph. San Francisco: Actelion Pharmaceuticals, Inc.; 2023.
  2. Tracleer (Bosentan) Drug Label Information. San Francisco: Actelion Pharmaceuticals, Inc.; 2023.



IMPORTANT NOTE: The above information is intended to increase awareness of health information and does not suggest treatment or diagnosis. This information is not a substitute for individual medical attention and should not be construed to indicate that use of the drug is safe, appropriate, or effective for you. See your health care professional for medical advice and treatment.

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