SPECIFICATION
Requires Prescription (YES/NO)
Yes
Generics
Bosentan Monohydrate
Used For
Hypertension
How it works
Bosentan is a dual endothelin receptor antagonist with affinity for both ETA and ETB receptors. Bosentan decreases both pulmonary and systemic vascular resistance, resulting in increased cardiac output without increasing heart rate. The neurohormone endothelin is a potent vasoconstrictor with the ability to promote fibrosis, cell proliferation, and tissue remodeling. Endothelin concentrations in plasma and tissues are increased in a number of cardiovascular disorders, including pulmonary hypertension, suggesting a pathological role for endothelin in these diseases. In pulmonary arterial hypertension, endothelin plasma concentrations strongly correlate with poor prognosis .
USAGE AND SAFETY
Dosage
Bosentan Monohydrate
Side Effects
Flushed appearance or redness of skin ; Hypersensitivity reactions (including skin inflammation, itching and rash) ; Gastrooesophageal reflux disease (acid reflux) ; Diarrhoea ; Stuffy or blocked nose ; Syncope (fainting) ; Palpitations (fast or irregular heart beats) ; Low blood pressure .
Drug Interactions
Warfarin , Simvastatin and Other Statins , Glyburide , Ketoconazole , Cyclosporine A , Tacrolimus and Sirolimus , Sildenafil , Tadalafil , Rifampicin , Epoprostenol , Antiretroviral Agents: Lopinavir + Ritonavir .
Indication
It is indicated for the treatment of pulmonary arterial hypertension in patients with WHO functional class III or IV primary pulmonary hypertension, or pulmonary hypertension secondary to scleroderma or congenital heart disease or human immunodeficiency virus in patients who did not respond adequately to conventional therapy .
When not to Use
It is contraindicated in patients: Who are hypersensitive to bosentan or to any excipient in the formulation ; Who are pregnant, or of childbearing potential unless adequate contraceptive measures are taken. Fetal malformations were reported in animals .
PRECAUTIONS
Precaution
Cases of pulmonary edema have been reported with vasodilators (mainly prostacyclins) when used in patients with pulmonary veno-occlusive disease. Consequently, should signs of pulmonary edema occur when Bosentan is administered in patients with Pulmonary arterial hypertension (PAH) , the possibility of associated veno-occlusive disease should be considered.
WARNINGS
Warning 1
The efficacy of bosentan has not been established in patients with severe Pulmonary arterial hypertension (PAH). Transfer to a therapy that is recommended at the severe stage of the disease (e.g. epoprostenol) should be considered if the clinical condition deteriorates .
Warning 2
Bosentan should only be initiated if the systemic systolic blood pressure is higher than 85 mmHg.
Warning 3
Bosentan has not been shown to have a beneficial effect on the healing of existing digital ulcers.
ADDITIONAL INFORMATION
Pregnancy category
Always consult your physician before using any medicine.
Storage (YES/NO)
Store this medicine at room temperature, away from direct light and heat.
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