Bosentan
- Atc Codes:C02KX01
- CAS Codes:157212-55-0#147536-97-0
- PHARMGKB ID:157212-55-0#147536-97-0
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Tracleer; Belgium: Tracleer; Bulgaria: Tracleer; Cyprus: Tracleer; Czech Republic: Tracleer; Denmark: Tracleer; Estonia: Tracleer; Finland: Tracleer; France: Tracleer; Germany: Tracleer; Greece: Tracleer; Hungary: Tracleer; Ireland: Tracleer; Italy: Tracleer; Latvia: Tracleer; Lithuania: Tracleer; Luxembourg: Tracleer; Malta: Tracleer; Netherlands: Tracleer; Poland: Tracleer; Portugal: Tracleer; Romania: Tracleer; Slovakia: Tracleer; Slovenia: Tracleer; Spain: Tracleer; Sweden: Tracleer; UK: Tracleer.
North America
Canada: Tracleer; USA: Tracleer.
Latin America
Argentina: Usenta; Brazil: Tracleer.
Asia
Japan: Tracleer.
Drug combinations
Chemistry
Bosentan: C~27~H~29~N~5~O~6~S.H~2~O. Mw: 569.63. (1) Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2′-bipyrimidin]-4-yl]-, monohydrate; (2) p-tert-Butyl-N-[6-(2-hydroxyethoxy)-5-(o-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzenesulfonamide monohydrate. CAS-157212-55-0; CAS-147536-97-0 (anhydrous)(1995).
Pharmacologic Category
Vasodilating Agents, Miscellaneous; Endothelin Antagonist. (ATC-Code: C02KX01).
Mechanism of action
Acts as a competitive antagonist and blocks endothelin receptors on vascular endothelium and smooth muscle. Stimulation of endothelin receptors is associated with vasoconstriction and proliferation. Although bosentan blocks both ET~A~ and ET~B~ receptors, the affinity is slightly higher for ET~A~.
Therapeutic use
Adjunctive therapy for the treatment of pulmonary arterial hypertension (WHO group I), in patients with WHO class III or IV symptoms.
Pregnancy and lactiation implications
Use in pregnancy is contraindicated. Based on animal studies, bosentan is likely to produce major birth defects if used by pregnant women. Women of childbearing potential should avoid exposure to dust generated from broken or split tablets. Lactation is not recommended during treatment.
Unlabeled use
Contraindications
Hypersensitivity to bosentan or any component of the formulation. Concurrent use of cyclosporine or glyburide. Pregnancy.
Warnings and precautions
Treatment should be stopped in patients who develop elevated transaminases (ALT or AST) in combination with symptoms of hepatic injury or elevated serum bilirubin ≥2 times upper limit of normal. Caution in low hemoglobin levels (may cause decreases in hemoglobin and hematocrit). Discontinue in pulmonary edema suggestive of pulmonary veno-occlusive disease. May cause fluid retention evidenced by signs and symptoms of peripheral edema, weight gain, and heart failure. Caution in ischemic cardiovascular disease. Angioedema reported. Irreversible testicular atrophy and decreased fertility in males observed in animal studies with long-term exposure.