Melatonin possesses potential efficacy in perinatal brain injuries, and has been proposed as adjunctive pharmacological therapy in combination with hypothermia in the clinical setting. However, the pharmacokinetics of melatonin in preterm and term newborns is still unknown. The aim of this study was to analyze the pharmacokinetics of melatonin after intragastric administration in preterm infants. Preterm newborns were enrolled 24-72 h after birth, and randomly assigned to three groups receiving a single bolus of 0.5 mg·kg-1melatonin, or 3 boluses of 1 or 5 mg·kg-1of melatonin at 24-h intervals. Blood samples were collected before and at selective times after melatonin administration. The half-life of melatonin in plasma ranged from 7.98 to 10.94 h, and the area under the curve (AUC) from 10.48 to 118.17 μg·mL-1·h-1. Our results indicate a different pharmacokinetic profile in premature newborns, compared to adults and experimental animals. The high peak plasma concentrations and the long half-life indicate that in the neonatal clinical setting, it is possible to obtain and maintain high serum concentrations using a single administration of melatonin repeated every 12/24 h.

Carloni, S., Proietti, F., Rocchi, M., Longini, M., Marseglia, L., D'Angelo, G., et al. (2017). Melatonin pharmacokinetics following oral administration in preterm neonates. MOLECULES, 22(12), 1-12 [10.3390/molecules22122115].

Melatonin pharmacokinetics following oral administration in preterm neonates

Carloni, Silvia
Writing – Original Draft Preparation
;
Proietti, Fabrizio;Longini, Mariangela;Buonocore, Giuseppe
Writing – Original Draft Preparation
2017-01-01

Abstract

Melatonin possesses potential efficacy in perinatal brain injuries, and has been proposed as adjunctive pharmacological therapy in combination with hypothermia in the clinical setting. However, the pharmacokinetics of melatonin in preterm and term newborns is still unknown. The aim of this study was to analyze the pharmacokinetics of melatonin after intragastric administration in preterm infants. Preterm newborns were enrolled 24-72 h after birth, and randomly assigned to three groups receiving a single bolus of 0.5 mg·kg-1melatonin, or 3 boluses of 1 or 5 mg·kg-1of melatonin at 24-h intervals. Blood samples were collected before and at selective times after melatonin administration. The half-life of melatonin in plasma ranged from 7.98 to 10.94 h, and the area under the curve (AUC) from 10.48 to 118.17 μg·mL-1·h-1. Our results indicate a different pharmacokinetic profile in premature newborns, compared to adults and experimental animals. The high peak plasma concentrations and the long half-life indicate that in the neonatal clinical setting, it is possible to obtain and maintain high serum concentrations using a single administration of melatonin repeated every 12/24 h.
2017
Carloni, S., Proietti, F., Rocchi, M., Longini, M., Marseglia, L., D'Angelo, G., et al. (2017). Melatonin pharmacokinetics following oral administration in preterm neonates. MOLECULES, 22(12), 1-12 [10.3390/molecules22122115].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/1035718