Pharmacokinetics in children

The pharmacokinetics of ezetimibe are comparable in children and adults:
Resorption: rapid. Tmax = 1–2 hours (active metabolite), 4–12 hours (ezetimibe). Plasma protein binding: 88–92% (active metabolite), 99.7% (ezetimibe). Metabolization: glucuronidated in the liver to the active compound, ezetimibe glucuronide. Ezetimibe and its active metabolite undergo enterohepatic circulation. Elimination: approx. 78% in the faeces, primarily as ezetimibe and approx. 11% in the urine, primarily as the active metabolite. T½el = approx. 22 hours (ezetimibe, active metabolite).

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

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.

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

In a study in children (6 to 10 years) with heterozygous familial or non-familial hypercholesterolaemia (n = 138), increases in ALT and/or AST (≥ three times the upper normal value consecutively) were observed in 1.1% (1 patient) of patients taking ezetimibe compared to 0% of patients in the placebo group. No CPK elevations (≥ ten times the upper normal value) occurred. No cases of myopathy were reported. [SmPC Ezetrol 02/2021 GER]

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

Clinical experience in children and adolescents (ages 6 to 17 yrs) is limited to homozygous and heterozygous familial hypercholesterolaemia and sitosterolaemia. Treatment in children should be adjusted by a specialist doctor. The long-term effects on use for > 33 weeks have not been determined in children aged between 10 and 18 years and for > 12 weeks in children from 6-10 years.

Interactions

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

• CARDIOVASCULAR SYSTEM
• LIPID MODIFYING AGENTS

LIPID MODIFYING AGENTS, PLAIN

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. MSD, SPC Ezetrol (RVG 28626) 05-02-2016, www.geneesmiddeleninformatiebank.nl
2. Kusters D et al, Efficacy and Safety of Ezetimibe Monotherapy in Children with Heterozygous Familial or Nonfamilial Hypercholesterolemia, J Pediatr., 2015, Jun;166(6), 1377-84

Changes

Therapeutic Drug Monitoring

Overdose