Tracleer
Tracleer Brand names, Tracleer Analogs
Tracleer Brand Names Mixture
- No information avaliable
Tracleer Chemical_Formula
C27H29N5O6S
Tracleer RX_link
http://www.rxlist.com/cgi/generic3/tracleer.htm
Tracleer fda sheet
Tracleer msds (material safety sheet)
Tracleer Synthesis Reference
No information avaliable
Tracleer Molecular Weight
551.615 g/mol
Tracleer Melting Point
No information avaliable
Tracleer H2O Solubility
Poorly soluble in water (1.0 mg/100 ml) and in aqueous solutions at low pH (0.1 mg/100 ml at pH 1.1 and 4.0; 0.2 mg/100 ml at pH 5.0). Solubility increases at higher pH values (43 mg/100 ml at pH 7.5).
Tracleer State
Solid
Tracleer LogP
4.625
Tracleer Dosage Forms
62.5 mg and 125 mg film-coated tablets
Tracleer Indication
Used in the treatment of pulmonary arterial hypertension (PAH), to improve exercise ability and to decrease the rate of clinical worsening (in patients with WHO Class III or IV symptoms).
Tracleer Pharmacology
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.
Tracleer Absorption
Absolute bioavailability is approximately 50% and food does not affect absorption.
Tracleer side effects and Toxicity
Bosentan has been given as a single dose of up to 2400 mg in normal volunteers, or up to 2000 mg/day for 2 months in patients, without any major clinical consequences. The most common side effect was headache of mild to moderate intensity. In the cyclosporine A interaction study, in which doses of 500 and 1000 mg b.i.d. of bosentan were given concomitantly with cyclosporine A, trough plasma concentrations of bosentan increased 30-fold, resulting in severe headache, nausea, and vomiting, but no serious adverse events. Mild decreases in blood pressure and increases in heart rate were observed. There is no specific experience of overdosage with bosentan beyond the doses described above. Massive overdosage may result in pronounced hypotension requiring active cardiovascular support.
Tracleer Patient Information
Tracleer Organisms Affected
Humans and other mammals
