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Community data Updated 23 hours ago

Bosentan Monohydrate

Anti-hypertensive Prescription
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Indications

Bosentan Monohydrate is used to treat pulmonary arterial hypertension (PAH). It helps improve exercise capacity and symptoms in patients with WHO functional class Ill. Efficacy has been shown in: Some improvements have also been shown in patients with PAH WHO functional class ll.

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Bosentan is a dual endothelin receptor antagonist (ERA), which means it binds to both endothelin A and B (ETA and ETB) receptors. It lowers both pulmonary and systemic vascular resistance. As a result, cardiac output goes up without any rise in heart rate. The neurohormone endothelin-1 (ET-1) is one of the most potent vasoconstrictors known. It can also promote fibrosis, cell proliferation, cardiac hypertrophy and remodelling, and it is pro-inflammatory. These effects happen when endothelin binds to ETA and ETB receptors in the endothelium and the vascular smooth muscle cells. ET-1 concentrations in tissues and plasma are raised in several cardiovascular disorders and connective tissue diseases, including pulmonary arterial hypertension, scleroderma, acute and chronic heart failure, myocardial ischaemia, systemic hypertension and atherosclerosis. This suggests that ET-1 plays a pathogenic role in these diseases. In pulmonary arterial hypertension and heart failure, when endothelin receptors are not blocked, high ET-1 concentrations are strongly correlated with how severe the disease is and with its prognosis.

Absorption: In healthy subjects, the absolute bioavailability of bosentan is approximately 50%, and food does not affect it. Maximum plasma concentrations are reached within 3 to 5 hours.

Distribution: Bosentan is highly bound (>98%) to plasma proteins, mainly albumin.

Elimination: The liver metabolises bosentan through the cytochrome P450 isoenzymes CYP2C9 and CYP3A4, and it is then removed by biliary excretion. Less than 3% of an oral dose is recovered in urine.

Pregnancy & Breastfeeding

Bosentan must not be used in pregnancy. Nobody knows whether bosentan passes into human breast milk, so breast-feeding is not recommended while a woman is being treated with Bosentan.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: Take the tablets by mouth, once in the morning and once in the evening. You can take them with or without food. Pulmonary arterial hypertension: in adults, Bosentan treatment should start at 62.5 mg twice daily for 4 weeks. After that, the dose is increased to the maintenance dose of 125 mg twice daily. For children aged 2 years or older, the optimal maintenance dose has not been defined in well-controlled studies. Paediatric pharmacokinetic data have shown, however, that Bosentan plasma concentrations in children were on average lower than in adult patients. Increasing the dose above 2 mg/kg body weight twice daily did not raise them. Discontinuation of treatment: if the decision is taken to withdraw Bosentan, do it gradually while an alternative therapy is introduced.

Side Effects & Interactions

Side Effects

No side-effect data recorded yet.