TRACLEER

What it is

TRACLEER contains bosentan monohydrate. The medicine is available in two tablet strengths: 62.5 mg and 125 mg bosentan. The 62.5 mg tablets are orange-white, round, biconvex, film-coated tablets, while the 125 mg tablets are orange-white, oval, biconvex, film-coated tablets.

Approved indications TRACLEER is indicated for the treatment of:

— Idiopathic pulmonary arterial hypertension — Familial pulmonary arterial hypertension — Pulmonary arterial hypertension associated with scleroderma — Pulmonary arterial hypertension associated with congenital systemic to pulmonary shunts including Eisenmenger's physiology, in patients with WHO functional Class II, III or IV symptoms

Dosing overview

TRACLEER should be administered under the supervision of a physician experienced in the management of pulmonary arterial hypertension. Treatment should be initiated at a dose of 62.5 mg twice daily for 4 weeks, with efficacy demonstrated in clinical trial subjects who increased to a maintenance dose of 125 mg twice daily. Doses above 125 mg twice daily did not appear to confer additional benefit sufficient to offset the increased risk of liver injury. Tablets should be administered morning and evening, with or without food. In children aged 3 years and over, dosing is based on body weight: for 10 to 20 kg, 31.25 mg once daily for the first 4 weeks then 31.25 mg twice daily; for >20 to 40 kg, 31.25 mg twice daily for the first 4 weeks then 62.5 mg twice daily; for >40 kg, 62.5 mg twice daily for the first 4 weeks then 125 mg twice daily.

Key safety warnings

TRACLEER causes birth defects and is contraindicated in pregnancy. Treatment should only be initiated in women of childbearing potential following a negative pregnancy test and only in those who practice reliable contraception that does not depend solely upon hormonal contraceptives, with double barrier contraception recommended. Rare cases of hepatic cirrhosis and hepatic failure have been reported in patients using bosentan. Elevations in ALT or AST by more than 3 times the upper limit of normal were observed in 11% of bosentan-treated patients compared to 2% of placebo-treated patients. Serum liver aminotransferase (AST and ALT) levels must be measured prior to initiation of treatment and monthly thereafter for the duration of treatment. Treatment with bosentan caused a dose-related decrease in haemoglobin and haematocrit, with 10% of bosentan patients having clinically significant reductions and 5% developing anaemia. Haemoglobin levels should be monitored periodically, with checks recommended after 1 and 3 months, and every 3 months thereafter.

Contraindications

Women who are pregnant or who are likely to become pregnant: bosentan is expected to cause foetal harm if administered to pregnant women. TRACLEER is contraindicated in patients with moderate or severe hepatic function impairment (Child Pugh Class B or C and/or baseline elevated aminotransferases >3 times the upper limit of normal). Concomitant use of TRACLEER and ciclosporin is contraindicated. Co-administration of glibenclamide and TRACLEER is contraindicated. TRACLEER is contraindicated in patients who are hypersensitive to bosentan or any component of the medication, with observed reactions including Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), anaphylaxis, rash and angioedema.

Regulatory history

TRACLEER 62.5 mg and 125 mg tablets were first registered on the ARTG on 20 November 2002.