PharmacyCodes



Bosentan en es it fr

Bosentan Brand names, Bosentan Analogs

Bosentan Brand Names Mixture

  • No information avaliable

Bosentan Chemical_Formula

C27H29N5O6S

Bosentan RX_link

http://www.rxlist.com/cgi/generic3/tracleer.htm

Bosentan fda sheet

Bosentan FDA

Bosentan msds (material safety sheet)

Bosentan Synthesis Reference

No information avaliable

Bosentan Molecular Weight

551.615 g/mol

Bosentan Melting Point

No information avaliable

Bosentan 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).

Bosentan State

Solid

Bosentan LogP

4.625

Bosentan Dosage Forms

62.5 mg and 125 mg film-coated tablets

Bosentan 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).

Bosentan 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.

Bosentan Absorption

Absolute bioavailability is approximately 50% and food does not affect absorption.

Bosentan 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.

Bosentan Patient Information

Bosentan Organisms Affected

Humans and other mammals