Active Substance: Bosentan (as monohydrate).
Overview
Welcome to Dwaey, specifically on TRACLEER 62.5mg page.
This medicine contains an important and useful components, as it consists of
Bosentan (as monohydrate)is available in the market in concentration
Bosentan
Hepatotoxicity and teratogenicity. Elevations of AST or ALT associated with Bosentan are dose-dependent, occur both early and late in treatment, usually progress slowly, are typically asymptomatic, and usually have been reversible after treatment interruption or cessation. Aminotransferase elevations also may reverse spontaneously while continuing treatment with Tracleer. Liver aminotransferase levels must be measured prior to initiation of treatment and then monthly and therapy adjusted accordingly .Discontinue Bosentan if liver aminotransferase elevations are accompanied by clinical symptoms of hepatotoxicity (such as nausea, vomiting, fever, abdominal pain, jaundice, or unusual lethargy or fatigue) or increases in bilirubin > 2 Lactation: Not known if excreted in breast milk; not recommended
Pulmonary Arterial Hypertension (PAH)
Patients with WHO Class II symptoms showed reduction in the rate of clinical deterioration and a trend for improvement in walk distance. Physicians should consider whether these benefits are sufficient to offset the risk of hepatotoxicity in WHO Class II patients, which may preclude future use as their disease progresses.
>10% Hgb decreased; >1 g/dL (57%),Inhibition of spermatogenesis (25%),Headache (16-22%),Nasopharyngitis (11%),Transaminses increased (12%),Respiratory tract infection (22%),Increased transaminases (12%) 1-10% Edema, lower limb (5-8%),Flushing (7-9%),Hypotension (7%),Hepatic abnormalities (4%),Palpitations (4%),Anemia (3%),Dyspepsia (4%),Edema, general (4%),Fatigue (2%),Pruritus (4%) <1% Hyperbilirubinemia,Vasculitis,Jaundice,Leukopenia,Thrombocytopenia,Leukocytoplastic
5
Competitive antagonist of endothelin-1; blocks endothelin receptors on vascular endothelium and smooth muscle resulting in inhibition of vasoconstriction
Increased bosentan levels w/ CYP3A4 inhibitors (e.g. ketoconazole, ritonavir, diltiazem), CYP2C9 inhibitors (e.g. amiodarone, fluconazole), tacrolimus. Rifampicin initially increases but subsequently decreases bosentan concentration. May decrease plasma levels of warfarin, statins (e.g. simvastatin, lovastatin), hormonal contraceptives, sildenafil, tadalafil. Potentially Fatal: Increased risk of hepatotoxicity may occur w/ glibenclamide. Ciclosporin markedly increases bosentan concentration.
Information not available