Bosentan

What is Bosentan?

• Bosentan (Tracleer) is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH).

Bosentan Structural Formula V.1

Bosentan

What are the uses of this medicine?

• Bosentan (Tracleer) a prescription medicine used to treat people with certain types of pulmonary arterial hypertension (PAH), which is high blood pressure in the vessels of the lungs.
• Bosentan tablets can improve your ability to exercise and can slow the worsening of your physical condition and symptoms.
• Bosentan tablets lowers high blood pressure in your lungs and lets your heart pump blood more efficiently.

How does this medicine work?

• Bosentan (boe sen' tan) is an inhibitor of both the type A and B (ETA and ETB) endothelin receptors.
• Inhibition of the ET receptors disrupts the intracellular pathways that lead to vasoconstriction thereby causing vasodilation. Because these receptors are found in highest concentration in the lungs, the endothelin receptor antagonists primarily cause vasodilation in the pulmonary vasculature and decrease pulmonary vascular pressure with little effect on systemic blood presssure.
• In prospective, randomized controlled trials, bosentan was effective in alleviating symptoms, improving exercise tolerance and prolonging the time to clinical worsening in patients with idiopathic pulmonary artery hypertension (PAH).

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are pregnant

take any of these medicines:

• cyclosporine A used to treat psoriasis and rheumatoid arthritis, and to prevent rejection of heart, liver, and kidney transplants
• glyburide used to treat diabetes

• are allergic to bosentan or any of the ingredients in bosentan tablets.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• amiodarone (Nexterone, Pacerone)
• cholesterol-lowering medications (statins) such as atorvastatin (Lipitor, in Caduet), lovastatin (Altoprev), and simvastatin (Flolopid, Zocor, in Vytorin)
• diltiazem (Cardizem, Cartia, Diltzac, others)
• erythromycin (E.E.S., Eryc, PCE)
• fluconazole (Diflucan)
• gemfibrozil (Lopid)
• itraconazole (Onmel, Sporanox)
• ketoconazole
• rifampin (Rifadin, Rimactane, in Rifater, Rifamate)
• ritonavir (Norvir, in Kaletra, Viekira Pak, Technivie); voriconazole (Vfend)
• warfarin (Coumadin, Jantoven)

• Do not take cyclosporine (Gengraf, Neoral, Sandimmune) or glyburide (DiaBeta, Glynase) while taking bosentan

Is this medicine FDA approved?

• Bosentan was the first endothelin receptor antagonist to be approved in the United States (2001) and it remains in active use.
• The current indications are for symptomatic PAH, classified as WHO group 1 (primary or idiopathic).
• Use of bosentan in other forms of PAH (due to heart failure, thromboembolic disease, or pulmonary disease) should be considered experimental as its efficacy in these forms of PAH has not been adequately shown.
• Because of the potential for hepatotoxicity and teratogenicity, bosentan is available only as a part of a monitoring program in which regular monthly determination of serum enzymes levels and adequate methods for birth control are require.

How should this medicine be used?

• Obtain a pregnancy test in females of reproductive potential prior to bosentan tablets treatment, monthly during treatment and one month after stopping bosentan tablets.
• Measure liver aminotransferase levels prior to initiation of treatment and then monthly.

Recommended dosage: Patients older than 12 years of age:

• initiate at 62.5 mg orally twice daily; for patients weighing greater than 40 kg, increase to 125 mg orally twice daily after 4 weeks.
• Reduce the dose and closely monitor patients developing aminotransferase elevations more than 3 X Upper Limit of Normal (ULN).

Administration:

• Bosentan tablets is only available through certified pharmacies. You will only receive a 30-day supply of bosentan tablets at one time.
• In most cases, you will take 1 tablet in the morning and 1 in the evening.
• You can take bosentan tablets orally with or without food.
• If you take more than the prescribed dose of bosentan tablets, call your healthcare provider right away.
• If you miss a dose of bosentan tablets, take your tablet as soon as you remember.
• Do not take 2 doses at the same time.
• If it is almost time for your next dose, skip the missed dose.
• Just take the next dose at your regular time.
• Do not stop taking bosentan tablets unless your healthcare provider tells you to.
• Suddenly stopping your treatment may cause your symptoms to get worse.
• If you need to stop taking bosentan tablets, speak with your healthcare provider about the right way to stop.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Film-coated tablet: 62.5 mg and 125 mg

This medicine is available in fallowing brand namesː

• Tracleer

What side effects can this medication cause?

The most common side effects of this medicine include:

• respiratory tract infection
• headache
• fainting
• flushing
• low blood pressure
• inflamed nose passages (sinusitis)
• joint pain
• irregular heart beats

Bosentan tablets can cause serious side effects including:

• Liver damage
• Serious birth defects

What special precautions should I follow?

• Elevations of AST or ALT associated with bosentan are dose-dependent, occur both early and late in treatment. 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.
• Based on data from animal reproduction studies, bosentan may cause fetal harm when administered to a pregnant female and is contraindicated in females who are pregnant.
• If clinically significant fluid retention develops, with or without associated weight gain, further evaluation should be undertaken to determine the cause, such as bosentan or underlying heart failure, and the possible need for treatment or discontinuation of bosentan.
• If signs of pulmonary edema occur, consider the possibility of associated pulmonary veno-occlusive disease and consider whether bosentan should be discontinued.
• Decreased sperm counts have been observed in patients receiving bosentan.
• Treatment with bosentan can cause a dose-related decrease in hemoglobin and hematocrit. Monitor hemoglobin levels after 1 and 3 months of treatment, then every 3 months thereafter.
• Bosentan has been associated with serum enzyme elevations during therapy and with rare instances of clinically apparent acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Nausea
• vomiting
• hypotension
• dizziness
• sweating
• blurred vision

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Bosentan is unlikely to be effectively removed by dialysis due to the high molecular weight and extensive plasma protein binding.

Can this medicine be used in pregnancy?

• Based on data from animal reproduction studies, bosentan may cause fetal harm, including birth defects and fetal death, when administered to a pregnant female and is contraindicated during pregnancy.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: Bosentan
• Inactive ingredients: Corn starch, ethyl cellulose, glyceryl behenate, hypromellose, iron oxide yellow, iron oxide red, magnesium stearate, pregelatinized starch, povidone, sodium starch glycolate type A, titanium dioxide, triacetin and talc.

Who manufactures and distributes this medicine?

Manufactured by:

• Amneal Pharmaceuticals Pvt. Ltd.
• Oral Solid Dosage Unit
• Ahmedabad, INDIA

Distributed by:

• Amneal Pharmaceuticals LLC
• Bridgewater, NJ

What should I know about storage and disposal of this medication?

• Store bosentan tablets at room temperature between 20° to 25°C (68° to 77°F).

Pulmonary Disease Agents

• Chronic Obstructive Pulmonary Disease (COPD) Agents
  • Anticholinergic Agents
    • Ipratropium, Tiotropium, Aclidinium
  • Beta-2 Adrenergic Agonists
    • Albuterol, Formoterol, Salmeterol, Terbutaline
  • Corticosteroids
    • Budesonide, Fluticasone
  • Miscellaneous
    • Roflumilast, Theophylline

• Pulmonary Arterial Hypertension Agents
  

• • Endothelin Receptor Antagonists
    • • Ambrisentan, Bosentan, Macitentan
  • Phosphodiesterase Type 5 (PDE5) Inhibitors
    • Avanafil, Sildenafil, Tadalafil, Vardenafil
  •  Prostacyclin Analogs
    • Epoprostenol, Iloprost, Treprostinil
  •  Miscellaneous
    • Riociguat, Selexipag

• Pulmonary Fibrosis Agents
  • Nintedanib, Pirfenidone

• Dailymed label info on Bosentan
• FDA Bosentan

Bosentan Resources
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