- Dosages
- Side effects in children
- Warnings & precautions in children
- Contra-indications in children
-
Interactions - PK
- Renal impairment
- References
Pharmacokinetics in children
Pharmacokinetic data from research in children has shown that the plasma concentrations of bosentan were lower on average than in adult patients and were not raised by increasing the dose of Tracleer further, beyond 2 mg/kg twice daily.
The study by Barst et al. (n=18, ages 3 to 15 years) stated the following pharmacokinetic parameters after a single dose of bosentan:
| Dose | Cmax (ng/ml) | Tmax (hours) | T½ (hours) |
|---|---|---|---|
| 31.25 mg | 959 | 1.0 | 4.7 |
| 62.5 mg | 815 | 2.5 | 5.3 |
| 125 mg | 1709 | 4.0 | 4.2 |
After multiple doses, the following average pharmacokinetic parameters were stated:
| Dose | Cmax (ng/ml) | Tmax (hours) | T½ (hours) |
|---|---|---|---|
| 62.5 mg/day in 2 doses | 685 | 2.5 | 6.0 |
| 125 mg/day in 2 doses | 1136 | 1.0 | 5.6 |
| 250 mg/day in 2 doses | 1200 | 1.8 | 5.3 |
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dose recommendation of formulary compared to licensed use (on-label versus off-label)
No information is present at this moment.
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Available formulations
No information is present at this moment.
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Dosages
| Pulmonary arterial hypertension |
|---|
|
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Renal impaiment in children > 3 months
GFR ≥10 ml/min/1.73m2: Dose adjustment not required.
GFR <10 ml/min/1.73m2: A general recommendation on dose adjustment cannot be provided.
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The complete list of all undesirable drug reactions can be found in the national Summary of Product Characteristics (SmPC) – click here
Side effects in children
Elevated transaminase values, hypotension, oedema, headaches, flushing, upper respiratory tract infection, nasopharyngitis, fever, vomiting, bronchitis, abdominal pain, diarrhoea, lowered haemoglobin/anaemia, syncope, elevated bilirubin, thrombocytopenia, chest pain, fatigue, pneumonia.
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The complete list of all contra-indications can be found in the national Summary of Product Characteristics (SmPC) – click here
Contra-indications
No information available on specific contra indications in children.
The complete list of all warnings and precautions can be found in the national Summary of Product Characteristics (SmPC) – click here
Warnings & precautions
No information available on specific warnings and precautions in children.
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Interactions
The complete list of all interactions can be found in the national Summary of Product Characteristics (SmPC) – click here
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| Serotonin antagonists | ||
|---|---|---|
| C02KD01 | ||
| Antihypertensives for pulmonary arterial hypertension | ||
|---|---|---|
| C02KX02 | ||
| C02KX04 | ||
| C02KX05 | ||
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References
- Rademaker C.M.A. et al, Geneesmiddelen-Formularium voor Kinderen, 2007
- Actelion Registration Ltd, SPC Tracleer (EU/1/02/220/006) 16-07-2015, www.geneesmiddeleninformatiebank.nl
- Carter NJ et al, Bosentan: in pediatric patients with pulmonary arterial hypertension., Paediatr Drugs, 2010, 12(1), 63-73
- Maxey DM et al,, Food and Drug Administration (FDA) postmarket reported side effects and adverse events associated with pulmonary hypertension therapy in pediatric patients., Pediatr Cardiol, 2013, 34(7), 1628-36
- Barst RJ et al,, Pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonary arterial hypertension, Clin Pharmacol Ther, 2003, 73(4), 372-82
- Beghetti M et al,, Pharmacokinetic and clinical profile of a novel formulation of bosentan in children with pulmonary arterial hypertension: the FUTURE-1 study., Br J Clin Pharmacol, 2009, 68(6), 948-55
- Berger RM et al, FUTURE-2: Results from an open-label, long-term safety and tolerability extension study using the pediatric FormUlation of bosenTan in pUlmonary arterial hypeRtEnsion, Int J Cardiol, 2016, 202, 52-8
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Changes
Changes
