Bosentan

 

Indication:

Bosentan is indicated mainly for the treatment of pulmonary hypertension (WHO Group I), in patients with WHO Class II-IV symptoms,use to improve exercise capacity and decrease the rate of clinical worsening . Numerous clinical studies are supporting the effectiveness of bosentan in: Reducing the number of new digital ulcers in patients with systemic sclerosis. Management of secondary Raynaud Phenomenon in systemic sclerosis.

Dosage and Administration:




Dose adjustment:

For Aminotransferase Elevations If aminotransferase levels increase, adjust monitoring and treatment plan according to belowTable. Discontinue Farantan 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 bilirubin) Use In Patients With Pre-existing Hepatic Impairment Avoid initiation of Farantan in patients with aminotransferases No dose adjustment is required in patients with mildly impaired liver function.
Dosage Adjustment and Monitoring in Patients Developing Aminotransferase Elevations 3x ULN< :


Contra-indications:

Intolerance to bosentan
Pregnancy

Cautions:

This product should be used with caution if the patients: are planning to become pregnant, or are breast-feeding are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement have allergies to medicines, foods, or other substances have a history of liver problems in mild liver impairment :
no dose adjustment required in moderate or severe :
avoid use abnormal liver function tests (monthly monitoring of liver function tests while taking Bosentan is required( have heart problems (e.g, congestive heart failure(
have blood problems (e.g, anemia( hematocrit and hemoglobin levels should be monitored after1and3 months of treatment and then every 3 months
have fluid retention (e.g, unusual swelling of the arms, hands, legs, or feet) drink alcohol or take medicines that may harm the liver (e.g, acetaminophen, methotrexate, isoniazid, certain medicines for HIV infection)

Pharmacokinetics:




Drug interactions:

Some medicines may interact with bosentan, especially any of the following:
Amiodarone, azole antifungals (eg, fluconazole, itraconazole, ketoconazole, voriconazole), cobicistat, cyclosporine, diltiazem, HIV protease inhibitors (eg ritonavir), macrolide antibiotics (eg, erythromycin), and tacrolimus because they may increase the risk of bosentan's side effects Glyburide and rifampin because the risk of liver problems may be increased Anticoagulants (eg, warfarin), axitinib, bosutinib, cabazitaxel, HMG-CoA reductase inhibitors (statins) (eg, simvastatin), hormonal contraceptives (eg implanted birth control), and ulipristal because their effectiveness may be decreased by bosentan Side-effects:
%5-22 Respiratory Tract Infection, Headache, Edema, Chest Pain, Syncope 3-4% Flushing, Hypotension, Sinusitis, Arthralgia, abnormal Aminotransferases, Palpitations, Anemia

 

 

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