Pharmacokinetic study of metopimazine by oral route in children

Eric Mallet (1) , Fréderic Bounoure (2) , Mohamed Skiba (2) , Elodie Saussereau (3) , Jean-Pierre Goullé (4) , Mireille Castanet (2)

1 Service de pédiatrie médicale et médecine de l'adolescent [Rouen]
2 DC2N - Différenciation et communication neuronale et neuroendocrine
3 Groupe Hospitalier du Havre
4 ABTE - Aliments Bioprocédés Toxicologie Environnements

Metopimazine (MPZ) is an antiemetic considered as a currently used drug. In France, it has become the leading antiemetic mediator due to its good tolerance, however, its pharmacokinetics has never previously been studied in children. MPZ was administered by oral route to 8 children with a single dose of 0.33 mg/kg during an endocrine exploration using stimuli well known for its adverse emetic effects. We used biological remnants from sera following an hGH test in order to obtain the MPZ pharmacokinetics. Plasmatic concentrations of MPZ and the active acid metabolite AMPZ, were quantified by HPLC-MS/MS during a 270 min test period. MPZ is quickly absorbed with a median C max of 17.2 ng/mL at one hour and its half-life is 2.18 h. The plasmatic concentrations of AMPZ were higher than MPZ with a median C max of 76.3 ng/mL, a T max to 150 min and its concentration was approximately maintained at 50 ng/mL from 1 to 4 h. The plasmatic concentrations in children are similar to those observed in adults. No adverse effects, nausea or vomiting occurred during the trial. Therefore, these results confirm the MPZ dosage that should be used in children under 15 kg administered as 0.33 mg/kg up to 3 times a day.

Mots clés: Pharmacokinetics; Metopimazine; Antiemetic drug; Children

Domaines: Pharmacologie; Hépatologie et Gastroentérologie; Pédiatrie

Eric Mallet, Fréderic Bounoure, Mohamed Skiba, Elodie Saussereau, Jean-Pierre Goullé, et al.. Pharmacokinetic study of metopimazine by oral route in children. Pharmacology Research & Perspectives, 2015, 3 (3), pp.e00130. ⟨10.1002/prp2.130⟩. ⟨hal-02470837⟩