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Pharmacokinetic study of metopimazine by oral route in children.

Mallet E, Bounoure F, Skiba M, Saussereau E, Goullé JP, Castanet M - Pharmacol Res Perspect (2015)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: CIC INSERM 204, Department of Pediatrics, Rouen University Hospital Charles Nicolle, 76031, Rouen, France.

ABSTRACT
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.

No MeSH data available.


Related in: MedlinePlus

Plasmatic concentration of metopimazine in eight children.
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fig01: Plasmatic concentration of metopimazine in eight children.

Mentions: Children received a single dose of 0.33 mg/kg of MPZ by oral route according the recommended dose of the CTD. The MPZ median pharmacokinetics parameters are shown in Table2. MPZ given by oral route is quickly absorbed with a Tmax of 1 h and Cmax 17.2 ng/mL (6.4–92.2). The half time was 2.18 h with a clearance of 86 mL/min and a distribution volume of 16.28 L. The plasmatic concentrations of MPZ for each child are shown in Figure1. These plasmatic concentrations seem to be close to concentrations in adults. The comparison between the MPZ pharmacokinetic parameters in adults and children is shown in Table3. Herrstedt et al. (1990) showed that the median Cmax was 43 ng/mL [14–69] for an oral dose of 20 mg and 59 ng/mL [28; 182] for an oral dose of 40 mg. The doses used by Herrstedt et al. are higher than the CTD which recommends a dose ranging from 15 to 30 mg per day in one or two doses.


Pharmacokinetic study of metopimazine by oral route in children.

Mallet E, Bounoure F, Skiba M, Saussereau E, Goullé JP, Castanet M - Pharmacol Res Perspect (2015)

Plasmatic concentration of metopimazine in eight children.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4492748&req=5

fig01: Plasmatic concentration of metopimazine in eight children.
Mentions: Children received a single dose of 0.33 mg/kg of MPZ by oral route according the recommended dose of the CTD. The MPZ median pharmacokinetics parameters are shown in Table2. MPZ given by oral route is quickly absorbed with a Tmax of 1 h and Cmax 17.2 ng/mL (6.4–92.2). The half time was 2.18 h with a clearance of 86 mL/min and a distribution volume of 16.28 L. The plasmatic concentrations of MPZ for each child are shown in Figure1. These plasmatic concentrations seem to be close to concentrations in adults. The comparison between the MPZ pharmacokinetic parameters in adults and children is shown in Table3. Herrstedt et al. (1990) showed that the median Cmax was 43 ng/mL [14–69] for an oral dose of 20 mg and 59 ng/mL [28; 182] for an oral dose of 40 mg. The doses used by Herrstedt et al. are higher than the CTD which recommends a dose ranging from 15 to 30 mg per day in one or two doses.

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: CIC INSERM 204, Department of Pediatrics, Rouen University Hospital Charles Nicolle, 76031, Rouen, France.

ABSTRACT
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.

No MeSH data available.


Related in: MedlinePlus