Bosentan

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Bosentan
Systematic (IUPAC) name
N-[6-(2-hydroxyethoxy)-5- (2-methoxyphenoxy) -2-pyrimidin-2-yl-pyrimidin-4-yl] -4-tert- butyl-benzenesulfonamide
Identifiers
CAS number	147536-97-8
ATC code	C02KX01
PubChem	104865
DrugBank	APRD00829
Chemical data
Formula	C27H29N5O6S
Mol. mass	551.615 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	50%
Protein binding	>98%
Metabolism	Hepatic
Half life	5 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	X
Legal status	℞ Prescription only
Routes	Oral

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Bosentan (BOZENTAN) is a dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension (PAH). It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer®.

Indications

Bosentan is used to treat pulmonary hypertension by blocking the action of endothelin molecules that would otherwise promote narrowing of the blood vessels and lead to high blood pressure.

Mechanism of action

Bosentan works by competitively and specifically binding to ET_A and ET_B receptor sites in the endothelium and vascular smooth muscle. In so binding, it prevents the neurohormone endothelin-1 (ET-1) from binding to these same receptor sites and triggering vasoconstriction. Bosentan shows somewhat higher affinity for ET_A receptors than ET_B receptors.

Dosage

This medication is normally given in pill form. Administration of bosentan is normally initiated at a dosage of 62.5 mg twice daily for a period of four weeks. If no adverse drug reactions are observed, the dosage is raised to a maintenance level of 125 mg twice daily. Studies have not shown sufficient benefit from higher doses to counter the increased risk of liver damage.

Pharmacokinetic Data

• t_cmax = 3 to 5 hours after oral dosing (time elapsed before maximal concentration in the blood plasma is reached)

Warnings and precautions

Bosentan can cause liver damage, so patients taking it should have their liver function tested monthly while on the medication.

Bosentan can cause major birth defects, so women of childbearing-age must be tested for pregnancy prior to taking this medication, and use non-hormonal means of contraception (i.e. birth control pills cannot be relied upon in this situation).

See also

• Sitaxsentan
  
• Ambrisentan

v • d • e Medications used in the management of pulmonary arterial hypertension (B01, C02)
Prostacyclin analogues	Beraprost, Epoprostenol, Iloprost, Treprostinil
Endothelin receptor antagonists	Ambrisentan, Bosentan, Sitaxsentan
PDE5 inhibitors	Sildenafil, Tadalafil
Adjunctive therapy	Calcium channel blockers, Diuretics, Digoxin, Oxygen therapy, Warfarin

v • d • e Antihypertensives (C02) and diuretics (C03)
Sympatholytic agents	Centrally acting/antiadrenergics α2 agonist (Clonidine, Guanfacine, Methyldopa) imidazoline receptor agonist (Moxonidine, Rilmenidine) adrenergic uptake inhibitor (Rescinnamine, Reserpine) Ganglion-blocking/nicotinic antagonist Mecamylamine, Trimethaphan Peripherally acting/antiadrenergics Alpha blockers: Prazosin • Indoramin • Trimazosin • Doxazosin • Urapidil Guanidine derivatives: Betanidine • Guanethidine • Guanoxan • Debrisoquine • Guanoclor • Guanazodine • Guanoxabenz
Vasodilators	Diazoxide • hydrazinophthalazine (Hydralazine, Dihydralazine, Endralazine, Cadralazine) • Minoxidil • Nitroprusside • Phentolamine
Other antihypertensives	serotonin antagonist (Ketanserin) • endothelin receptor antagonist (Bosentan, Ambrisentan, Sitaxsentan) • MAOI (Pargyline) • THI (Metirosine)
Diuretics	Low ceiling Thiazides Bendroflumethiazide • Hydroflumethiazide • Hydrochlorothiazide • Chlorothiazide • Polythiazide • Trichlormethiazide • Cyclopenthiazide • Methyclothiazide • Cyclothiazide • Mebutizide Sulfonamides Quinethazone • Clopamide • Chlortalidone • Mefruside • Clofenamide • Metolazone • Meticrane • Xipamide • Indapamide • Clorexolone • Fenquizone Other Mersalyl • Theobromine • Cicletanine High ceiling Loop diuretic (Bumetanide, Furosemide, Torsemide) Potassium-sparing ESC blockers (Amiloride, Triamterene) • aldosterone antagonists (Spironolactone, Eplerenone, Potassium canrenoate, Canrenone)

de:Bosentan

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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .