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Tracleer is indicated for the treatment of pulmonary arterial hypertension (class I) in patients with class III or IV symptoms, to improve mobility and reduce clinical deterioration. So how to use Tracleer? Learn all you need to know about Tracleer through the article below.
1. What is Tracleer?
Drug group: Cardiovascular drugs Dosage form: Film-coated tablets Packing: Box of 1 bottle of 60 tablets Ingredients: Bosentan (as Bosentan monohydrate) 62.5mg Manufacturer: Pacheon Inc - Canada
2. Uses of Tracleer
Indications
Treatment of pulmonary arterial hypertension (World Health Organization Group I) in patients with World Health Organization class III or IV symptoms, to improve exercise capacity and reduce clinical bad case rate.
3. Dosage - How to take Tracleer
Dosage:
Patients > 12 years old: initial dose of 62.5 mg x 2 times/day. For people with low body weight (<40kg), the starting and maintenance dose is 62.5 mg x 2 times/day. Children : Recommended dose for children 1 month - 12 years old. 10 - 20 kg: initially 31.25 mg/time/day, after 4 weeks increase to maintenance dose 31.25 mg x 2 times/day. 20-40 kg: initially 31.25 mg x 2 times/day, after 4 weeks increase to maintenance dose of 62.5 mg x 2 times/day. Over 40kg: start with 62.5mg x 2 times/day. after 4 weeks increase to maintenance dose 125 mg x 2 times/day. Patients with renal impairment: No dose adjustment of Tracleer is required. Dosage:
Take in the morning and afternoon, with or without food. The film-coated tablets should be swallowed whole with water.
4. Contraindications of Tracleer
Hypersensitivity to Bosentan or any of the ingredients in Tracleer Pregnancy. Concomitant use with Cyclosporin A (significant increase in plasma concentrations of Bosentan), glyburic (increased risk of elevation of liver enzymes). Moderate or severe hepatic impairment, Patients with elevated aminotransferases (>3 x ULN)
5. Tracleer . side effects
Side effects include:
Headache, Nasopharyngitis, Flushing, Edema, Low blood pressure, Dizziness, Palpitations, Digestive disturbances, Itching, Rash, Fatigue, Cramps, Anemia. Anaphylaxis and angioedema (rarely). Tracleer dose-dependent elevations of liver enzymes may occur, liver function abnormalities, cirrhosis, and liver failure have been reported. Bosentan is teratogenic in animals
6. Drug interactions
Cytochrome P450 : Bosentan is metabolised by CYP2C9 and CYP3A. Concomitant administration of a CYP2C9 inhibitor ((fluconazole or amiodarone) and a strong inhibitor of CYP3A (ketoconazole, itraconazole) or moderate inhibitors of CYP3A (amprenavir, erythromycin, fluconazole, diltiazem) with Bosentan may increase Tracleer exposure. Co-administration of a CYP2C9 inhibitor and a strong or moderate CYP3A inhibitor with Bosentan is not recommended.Cyclosporin A: Bosentan plasma concentrations are increased while those of Cyclosporin are decreased. when Bosentan and Cyclosporin A are co-administered. Tacrolimus : Concomitant administration of Bosentan and tacrolimus in animals markedly increases plasma concentrations of Bosentan. Concomitant use of bosentan and Glyburide Concomitant use of bosentan and Glyburide is contraindicated and consider other hypoglycemic agents. Concomitant use reduces plasma concentrations of Tracleer, glyburide as well as other oral hypoglycemic agents. metabolized primarily by CYP2C9 or CYP3A4. The possibility of glycemic control in patients receiving these agents should be considered. Ketoconazole: Increases plasma concentrations of Bosentan. No dose adjustment of Bosentan is required, but the potential for increased effects of Tracleer must be considered. Simvastatin and other statins: Concomitant administration reduces plasma concentrations of simvastatin and other CYP3A4-metabolized statins. The potential for reduced efficacy of statins should be considered, blood cholesterol levels monitored after initiating Bosentan, and statin dose adjustment if necessary. Warfarin: Concomitant use reduces the plasma concentration of warfarin. Clinical experience has shown no clinically relevant changes in INR or warfarin dose. Because warfarin has a narrow therapeutic index, coagulation parameters should be monitored and warfarin dose adjusted if necessary. Digoxin, nimodipine and losartan: Bosentan has no significant pharmacokinetic interaction with digoxin and nimodipine; losartan had no significant effect on Bosentan plasma concentrations. Sildenafil: Concomitant administration decreased sidenafil plasma concentrations and increased Tracleer plasma concentrations. Use caution when using combinations, monitor clinical reactions and side effects, adjust dose if necessary. Rifampicin: Concomitant administration increased Tracleer concentrations after the first concomitant dose but decreased steady-state Bosentan concentrations. Monitor liver function weekly for the first 4 weeks, then monthly. Hormonal Contraceptives: An interaction study demonstrated that co-administration of Bosentan with oral hormonal contraceptives resulted in a mean decrease in norethindrone and ethinyl estradiol concentrations by 14% and 31%, respectively. However, the exposure reductions were 56% and 66%, respectively. Therefore, hormonal contraceptives including oral, injectable, dermal and subcutaneous formulations may be uncertain when co-administered with bosentan. Lopinavir/Ritonavir or other Ritonavir-containing HIV regimens: Invitro data indicate that Bosentan is a substrate of organic anion transport protein (OATP), CYP3A, CYP2C9. Ritonavir inhibits OATP and CYP3A. However, the effect of ritonavir on bosentan pharmacokinetics is largely due to its effect on OATP. In normal volunteers, co-administration of bosentan 125 mg twice daily with lopinavir 400 mg/ritonavir 100 mg twice daily increased bosentan trough concentrations on days 4 and 10 by approximately 48-fold, respectively, and 5 times more than those taking only Bosentan. Therefore, a dose adjustment of Bosentan is required when lopinavir/ritonavir is initiated. Co-administration of Bosentan 125 mg twice daily had no significant effect on the pharmacokinetics of lopinavir 400 mg/ritonavir 100 mg twice daily.
7. Precautions when using Tracleer
Do not initiate treatment with Tracleer if the systolic blood pressure is less than 85 mmHg. Tracleer is contraindicated in patients with moderate to severe hepatic impairment. Liver aminotransferase levels should be measured prior to initiation of therapy, once a month during treatment, and 2 weeks after dose escalation. Treatment with Bosentan should not be initiated in patients with aminotransferase levels greater than 3 times the upper limit. If aminotransferase levels are 3-5 times higher during treatment, Bosentan should be discontinued or dose reduced and aminotransferase levels monitored every 2 weeks. If aminotransferase levels return to pre-treatment values, therapy can be continued or restarted, but aminotransferase levels should be checked after 3 days, 2 weeks and every month. If aminotransferase levels increase 5 to 8 times, Bosentan should be discontinued and aminotransferase levels monitored every 2 weeks. When aminotransferase levels return to pretreatment values, consider reintroduction of treatment. If levels increase more than 8 times or symptoms of hepatotoxicity or increase in total bilirubin are more than 2 times, discontinue treatment and do not consider reintroduction of Bosentan therapy. Hemoglobin levels should be monitored after 1 and 3 months of treatment and then every 3 months during treatment. If there is a marked decrease in hemoglobin levels, further evaluation is needed to determine the cause and the need for specific therapy. Bosentan should not be used in patients with hypotension. Although there is no evidence of an acute response following discontinuation of Bosentan, to avoid the possibility of clinical deterioration, the dose should be reduced gradually. If signs of pulmonary edema occur with Tracleer, the possibility of associated pulmonary venous disease should be considered and bosentan should be discontinued. Careful dose selection is required in elderly patients, considering the high frequency of decreased hepatic, renal or cardiac function, comorbidities or treatment with other drugs. Tracleer and its endothelin receptor antagonists are teratogenic in rats and should not be administered to pregnant women or to women of childbearing potential without the use of a reliable method of contraception. Hormonal contraceptives may not be adequate. The article has provided information on what Tracleer is used for, dosage and precautions for use. To ensure safety for your health and maximize the effectiveness of your treatment, you need to take Tracleer exactly as directed by your doctor. Store Tracleer in a dry place, the temperature does not exceed 30 degrees Celsius and out of the reach of small children.
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