Pharmacokinetics in children

In the study by Lundin et al. of children with Crohn's disease (n=8, 9-14 years), the absolute bioavailability after oral administration of 9 mg Entocort per day was 9% on average, compared to 11% in adults (very big first-pass-effect). The tmax value found did not differ significantly between children and adults. The average tmax ± SD in children was 4.7 ± 2.6 hours. The budesonide AUC and Cmax values were higher for children than for adults. The average Cmax ± SD in children was 6.0 ± 3.4 nmol/l. The difference in AUC and Cmax values is not considered to be clinically relevant.
Dilger et al. (n=12, 5–15 years) also show comparable pharmacokinetics between children and adults but report that there might be increased systemic exposure in young children.

dose recommendation of formulary compared to licensed use (on-label versus off-label)

No information is present at this moment.

Available formulations

No information is present at this moment.

Dosages

Renal impaiment in children > 3 months

No information available on dose adjustment in renal impairment.

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

Diarrhoea, nausea, flatulence, dyspepsia, skin reactions, Cushingoid syndrome, pseudotumor cerebri (including papilloedema) in adolescents, growth disorders

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 in children

Corticosteroids can disrupt the hypothalamic-pituitary functions. Be aware of an increased risk of the suppression of the hypothalamic-pituitary-adrenal axis in children.
Check the growth in height regularly in children who are treated long-term with corticosteroids. If growth retardation is observed, the therapy should be reassessed. Carefully weigh the benefits of the corticosteroid therapy and the possible risk of growth retardation against each other.
Release of budesonide from capsules is pH-dependent. Entocort coating is stable up to pH < 5.5 and is therefore released from the duodenum onwards. Budenofalk coating is stable up to pH < 6.4 and is released from the ileum onwards. When prescribing an oral budesonide preparation, the different release profiles of Entocort and Budenofalk can be utilized depending on the location of the abnormality in the intestines. Capsules should be taken in their entirety without chewing and with enough water. If necessary, an Entocort capsule can be opened, after which the contents can be mixed with e.g. a spoonful of apple sauce. The contents of the capsules must not be chewed or crushed.
 

Interactions

The complete list of all interactions can be found in the national Summary of Product Characteristics (SmPC) – click here

• ALIMENTARY TRACT AND METABOLISM
• ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS

INTESTINAL ANTIINFLAMMATORY AGENTS

This pages provides a list of drugs from the same ATC class for comparison. This does not necessarily mean that these drugs are interchangeable.

References

1. Rademaker C.M.A. et al, Geneesmiddelen-Formularium voor Kinderen, 2007
2. Centraal BegeleidingsOrgaan (CBO), Richtlijn Diagnostiek en behandeling van Inflammatoire darmziekten bij Kinderen, 2008, Geraadpleegd 22 april 2013
3. Escher JC; European Collaborative Research Group on Budesonide in Paediatric IBD, Budesonide versus prednisolone for the treatment of active Crohn\'s disease in children: a randomized, double-blind, controlled, multicentre trial, Eur J Gastroenterol Hepatol., 2004, 16, 47-54
4. Dilger K, et al, Pharmacokinetics and pharmacodynamic action of budesonide in children with Crohn\'s disease, Aliment Pharmacol Ther, 2006, 23, 387-96
5. Levine A, et al, Evaluation of oral budesonide for treatment of mild and moderate exacerbations of Crohn\'s disease in children, J Pediatr., 2002, 140, 75-80
6. Levine A, et al. Israeli Pediatric Gastroenterology Association Budesonide Study Group, A comparison of budesonide and prednisone for the treatment of active pediatric Crohn disease, J Pediatr Gastroenterol Nutr, 2003, 36, 248-52
7. Lundin PD, et al, Pharmacokinetics of budesonide controlled ileal release capsules in children and adults with active Crohn\'s disease, Aliment Pharmacol Ther., 2003, 17, 85-92
8. Wilson D, et al.; and the IBD Working Group of the British Society of Paediatric Gastroenterology, Hepatology, and Nutrition, Systematic Review of the Evidence Base for the Medical Treatment of Paediatric Inflammatory Bowel Disease, J Pediatr Gastroenterol Nutr., 2010, 50, S1-S34
9. AstraZeneca B.V., SPC Entocort Klysma (RVG 15660), www.cbg-meb.nl;, geraadpleegd 22 april 2013, http://db.cbg-meb.nl/IB-teksten/h15660.pdf
10. AstraZeneca B.V. , SPC Entocort capsules (RVG 18765). , www.cbg-meb.nl, geraadpleegd 22 april 2013, http://db.cbg-meb.nl/IB-teksten/h18765.pdf
11. Dr. Falk Pharma Benelux B.V. , SPC Budenofalk (RVG 22557). , www.cbg-meb.nl, geraadpleegd 22 april 2013, http://db.cbg-meb.nl/IB-teksten/h22557.pdf
12. Dr. Falk Pharma Benelux B.V., SPC Budenofalk (RVG 22557)., www.cbg-meb.nl, geraadpleegd 22 april 2013, http://db.cbg-meb.nl/IB-teksten/h22557.pdf
13. AstraZeneca B.V., SPC Entocort capsules (RVG 18765)., www.cbg-meb.nl, geraadpleegd 22 april 2013, http://db.cbg-meb.nl/IB-teksten/h18765.pdf

Changes

Therapeutic Drug Monitoring

Overdose