Pulmofirst 125 tablets
Bosentan Monohydrate 129.08 mg
What it does
Bosentan is a medication that helps to relax blood vessels and improve blood flow.
Commonly used for: pulmonary hypertension (high blood pressure in the lungs), heart failure
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.
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Sourcing - Kenya onlyRegistration & product details
Source: Zambia Medicines Regulatory Authority · fetched 2026-03-12 00:05:42 · updated 2026-09-17 03:38:00
Drug Interactions
137Severe (30)
Anti-Androgens - decreases exposure
Bosentan is predicted to decrease the exposure to anti-androgens (darolutamide). Avoid.
Antifungals,azoles - decreases exposure
Bosentan is predicted to decrease the exposure to antifungals, azoles (isavuconazole). Avoid.
Antipsychotics, Second Generation - decreases exposure
Bosentan is predicted to decrease the exposure to antipsychotics, second generation (cariprazine). Avoid.
Bosentan - increases exposure
Fluconazole is predicted to increase the exposure to endothelin receptor antagonists (bosentan). Avoid.
Bosentan - increases exposure
Voriconazole is predicted to increase the exposure to endothelin receptor antagonists (bosentan). Avoid.
Moderate (19)
Amlodipine - decreases exposure
Bosentan is predicted to decrease the exposure to calcium channel blockers (amlodipine, felodipine, lacidipine, lercanidipine, nicardipine, nifedipine, nimodipine). Monitor and adjust dose.
Benzodiazepines - decreases concentration
Bosentan is predicted to decrease the concentration of benzodiazepines (midazolam). Monitor and adjust dose.
Bosentan - increases exposure
Roxadustat is predicted to increase the exposure to bosentan. Monitor adverse effects and adjust dose.
Calcium Channel Blockers - decreases exposure
Bosentan is predicted to decrease the exposure to calcium channel blockers (amlodipine, felodipine, lacidipine, lercanidipine, nicardipine, nifedipine, nimodipine). Monitor and adjust dose.
Everolimus - decreases concentration
Bosentan is predicted to decrease the concentration of everolimus. Avoid or adjust dose.
Unknown (88)
Acalabrutinib - decreases exposure
Bosentan is predicted to decrease the exposure to acalabrutinib.
Anti-Androgens - decreases efficacy
Bosentan is predicted to decrease the efficacy of anti-androgens (cyproterone) with ethinylestradiol (co-cyprindiol). Use alternative methods during treatment with, and for 28 days after, the enzyme i
Antiarrhythmics - decreases exposure
Bosentanispredictedtodecreasetheexposureto antiarrhythmics(dronedarone).rTheoretical
Atorvastatin - decreases exposure
Bosentan is predicted to decrease the exposure to statins (atorvastatin, simvastatin).
Avacopan - decreases exposure
Bosentanispredictedtodecreasetheexposuretoavacopan. rTheoretical
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About this medicine
Bosentan is a medication that helps to relax blood vessels and improve blood flow.
What it treats
- pulmonary hypertension (high blood pressure in the lungs)
- heart failure
How it works
It blocks certain receptors in the body that cause blood vessels to narrow, which helps to lower blood pressure.
Who it's for
This medication is for adults with specific types of high blood pressure affecting the lungs.
Drug class
Endothelin receptor antagonists
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Bosentan
BNF-referencedBosentan is an endothelin receptor antagonist used primarily in the treatment of pulmonary arterial hypertension (PAH), aimed at improving exercise capacity and delaying clinical worsening.
Indications
- Pulmonary arterial hypertension
- Idiopathic pulmonary arterial hypertension
- Familial pulmonary arterial hypertension
Dosage
Children: Refer to the BNF for Children for specific dosing information for paediatric patients.
Adults: The typical initial dose for adults is 62.5 mg twice daily for 4 weeks, which may be increased to 125 mg twice daily based on clinical response.
Mechanism of action
Bosentan works by blocking the action of endothelin-1, a potent vasoconstrictor, thereby promoting vasodilation, reducing vascular resistance, and improving blood flow in the pulmonary and systemic circulation.
Pharmacodynamics
Bosentan leads to decreased pulmonary and systemic arterial pressures and increased cardiac output, which helps alleviate symptoms associated with pulmonary arterial hypertension.
Pharmacokinetics
Bosentan is absorbed orally with peak plasma concentrations occurring within 3 to 5 hours. It is extensively metabolized in the liver, primarily by CYP2C9 and CYP3A4. The elimination half-life is approximately 5 hours, and it is excreted mainly as metabolites in urine and feces.
Contra-indications
- Conditions which increase risk of haemorrhage
- Congenital or acquired valvular defects of the myocardium
- Decompensated cardiac failure (unless under close medical supervision)
- Pulmonary veno-occlusive disease
- Severe arrhythmias
- Severe coronary heart disease
Interactions
- Fluconazole: Severe (increases exposure)
- Voriconazole: Severe (increases exposure)
- Endothelin receptor antagonists: Moderately decrease exposure to ciclosporin
- Ciclosporin: Moderately increases the exposure to bosentan
- Bosentan + anti-androgens: Severe (decreases exposure)
- Bosentan + darolutamide: Severe (decreases exposure)
- Bosentan + antifungals, azoles: Severe (decreases exposure)
- Bosentan + isavuconazole: Severe (decreases exposure)
- Bosentan + antipsychotics, second generation: Severe (decreases exposure)
- Bosentan + cariprazine: Severe (decreases exposure)
Precautions
- Hypotension (do not initiate if systolic blood pressure is low)
- Avoid abrupt withdrawal due to risk of rebound pulmonary hypertension and hypertensive crisis
Pregnancy
Use if potential benefit outweighs risk.
Breast-feeding
Manufacturer advises avoid; no information available.
Storage
Store in a cool, dry place away from direct sunlight.
Formulations
- Powder for solution for infusion
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Bosentan
PubChem CID 104865Molecular formula: C27H29N5O6S
Mechanism of action
Endothelin-1 (ET-1) is a neurohormone, the effects of which are mediated by binding to ET<sub>A</sub> and ET<sub>B</sub> receptors in the endothelium and vascular smooth muscle. It displays a slightly higher affinity towards ET<sub>A</sub> receptors than ET<sub>B</sub> receptors. ET-1 concentrations are elevated in plasma and lung tissue of patients with pulmonary arterial hypertension, suggesting a pathogenic role for ET-1 in this disease. Bosentan is a specific and competitive antagonist at endothelin receptor types ET<sub>A</sub> and ET<sub>B</sub>.
Pharmacodynamics
Bosentan belongs to a class of drugs known as endothelin receptor antagonists (ERAs). Patients with PAH have elevated levels of endothelin, a potent blood vessel constrictor, in their plasma and lung tissue. Bosentan blocks the binding of endothelin to its receptors, thereby negating endothelin's deleterious effects.
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.