Bosentan Tablets

Category: Endothelin receptor antagonist
Form: Oral tablets

Uses:

• Treatment of pulmonary arterial hypertension (PAH) to improve exercise capacity and slow disease progression.

• Sometimes used in systemic sclerosis-related digital ulcers to reduce occurrence.

Mechanism of Action:

• Bosentan blocks endothelin-1 receptors (ETA and ETB).

• Endothelin-1 is a potent vasoconstrictor and promoter of vascular remodeling.

• By blocking these receptors, bosentan reduces pulmonary vascular resistance, leading to vasodilation and improved blood flow in the lungs.

Administration:

• Taken orally, usually twice daily.

• Dose adjustments depend on patient tolerance and liver function.

Side Effects:

• Common: headache, flushing, edema (swelling), nasal congestion.

• Liver-related: increased liver enzymes, risk of hepatotoxicity.

• Blood-related: anemia may occur with long-term use.

• Other: low blood pressure, heart palpitations, gastrointestinal upset.

Precautions:

• Requires regular liver function tests (monthly recommended).

• Monitor hemoglobin and hematocrit due to risk of anemia.

• Contraindicated in pregnancy (can cause birth defects) – reliable contraception is required during treatment.

• Should not be used in patients with severe liver impairment.

• Interacts with several drugs due to liver enzyme induction.

Summary:
Bosentan Tablets are used to treat pulmonary arterial hypertension and systemic sclerosis-related complications. By blocking endothelin-1 receptors, bosentan reduces pulmonary vascular resistance, improving exercise tolerance and slowing disease progression. While effective, it requires strict monitoring of liver function and blood counts, and precautions for pregnancy and drug interactions.