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Bosentan review
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Bosentan is a medication commonly used to treat people suffering from a high blood pressure in the lungs, or termed as Pulmonary Arterial Hypertension (PAH). This drug causes the arteries in the patient’s lungs to expand and contract to decrease the pressure. Though despite its usefulness, Bosentan is known to cause liver problems. Bosentan goes under the brand name Tracleer licensed by Actelion Pharmaceuticals.
Bosentan is used on patients who are suffering from Pulmonary Arterial Hypertension or defined as the increase in blood pressure along the arteries that carries blood to the lungs. This medication is defined as edothelin receptor antagonists.
Endothelin is a natural substance in the human body that causes the blood vessels to narrow, which inadvertently increases the pressure commonly attributed to patients suffering from PAH. Bosentan is capable of stopping the actions of Endothelin and reduces the pressure on these vessels. Bosentan may also be used on patients suffering from chronic heart failure.
Bosentan, or Tracleer, is taken orally twice a day, both of which can be administered before or after meals. Dosage for Bosentan is 62.5mg for a 4-week treatment. Doctor’s prescription might increase to 125mg for maintenance. Doctors limit the usage of Bosentan due to its side-effects. The medication is known to cause liver problems – especially when higher dosage is given to patients. Also, prolonged use of 125mg of Bosentan after the 62.5mg treatment does not have any benefits to the patient and might even increase the risk of liver abnormalities.
According to studies, 8 out of 165 patients using 125mg Bosentan after the 4-week medication are observed to have abnormal liver functions. Majority of the patients taking this medication suffers from headache, nasopharyngitis, flushing, hepatic abnormal functions, lower-limb edema, hypotension, and frequent palpitations.
Other side effects commonly experienced by patients taking in Bosentan are:
• Dyspepsia
• Edema
• Fatigue or weaknesses
• Pruritus
• Anemia
A low percentage of patients using Bosentan may suffer Post-Marketing Experience, such as rashes, hypersensitivity, thrombocytopenia, anemia, and jaundice.
Large plasma concentration is seen to occur when Bosentan is used along with CYP2C9 and CYP3A4 inhibitors. Such drugs under these families include fluconazole, ketoconazole, itraconazole, ritonavir, amprevanir, erythromycin, and dilitiazem.
Studies show that hormonal contraceptives may not have the desired results when used alongside Bosentan. It was observed that hormonal contraceptives, both oral and injectable, have its effects decreased to as low as 66% when paired with Bosentan or Tracleer.
It is highly recommended to consult a medical expert or your health care provider before taking in Bosentan. Due to the high risk of liver abnormalities attributed to this drug, experts advise a thorough medical and physical examination to avoid harmful side effects during and after treatment.
It was also observed that treatment using Bosentan causes an abnormal decrease in a patient’s hemoglobin and hematocrit count. Patients undergoing Bosentan medication should have their hemoglobin and hematocrit levels carefully monitored during the treatment and three months after the procedure.
Bosentan has the following structural formula:
• Molecular formula of bosentan is C27H29N5O6S
• Chemical IUPAC Name is N-[6-(2-hydroxyethoxy)-5- (2-methoxyphenoxy)-2-pyrimidin- 2-yl-pyrimidin-4-yl]-4-tert- butyl-benzenesulfonamide
• Molecular weight is 551.615 g/mol
• Bosentan available : 62.5mga tablets and 125mg tablets
Brand name(s): Tracleer
Review published on: 18 June 2009
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