Products
Bosentan is commercially available in the form of tablets and dispersible tablets (Tracleer). It has been approved in many countries since 2002. Generic versions were registered in 2017.
Structure and properties
Bosentan (C27H29N5O6S, Mr = 551.6 g/mol) is present in drugs as bosentan monohydrate, a white to yellowish powder that is poorly soluble in water. It is a bipyrimidine and a benzenesulfonamide derivative.
Effects
Bosentan (ATC C02KX01) is a competitive and dual antagonist at the ETA and ETB receptors. It abolishes the effects of endothelin, thereby decreasing pulmonary and systemic vascular resistance, resulting in increased blood flow without increasing heart rate.
Indications
- Pulmonary arterial hypertension
- To reduce the number of new digital ulcers in patients with systemic sclerosis and active digital ulcer disease.
Dosage
According to the professional information. The tablets are taken in the morning and evening and independently of meals.
Contraindications
- Hypersensitivity
- Liver dysfunction
- Pregnancy
- Combination with ciclosporin and glibenclamide
Full details of precautions and interactions can be found in the drug label.
Interactions
Bosentan is metabolized by CYP2C9 and CYP3A4 and is an inducer of these isoenzymes. Corresponding drug-drug interactions are possible.
Adverse effects
The most common potential adverse effects include headache, edema and fluid retention, altered liver enzymes, and anemia. Bosentan may rarely cause hepatoxic side effects. Therefore, liver enzymes must be monitored during treatment.
