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Molecules 2017, 22(12), 2115; doi:10.3390/molecules22122115

Melatonin Pharmacokinetics Following Oral Administration in Preterm Neonates

1
Department of Biomolecular Sciences, University of Urbino Carlo Bo, Via Saffi 2, 61029 Urbino, Italy
2
Department of Molecular and Developmental Medicine, University of Siena, Viale Bracci, 53100 Siena, Italy
3
Department of Human Pathology in Adult and Developmental Age “Gaetano Barresi”—Neonatal Intensive Care Unit, University of Messina, Via Consolare Valeria 1, 98125 Gazzi Messina, Italy
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 9 November 2017 / Revised: 29 November 2017 / Accepted: 29 November 2017 / Published: 1 December 2017
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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−1 melatonin, or 3 boluses of 1 or 5 mg·kg−1 of 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. View Full-Text
Keywords: melatonin; pharmacokinetics; preterm infants; immaturity; neuroprotective agents melatonin; pharmacokinetics; preterm infants; immaturity; neuroprotective agents
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MDPI and ACS Style

Carloni, S.; Proietti, F.; Rocchi, M.; Longini, M.; Marseglia, L.; D’Angelo, G.; Balduini, W.; Gitto, E.; Buonocore, G. Melatonin Pharmacokinetics Following Oral Administration in Preterm Neonates. Molecules 2017, 22, 2115.

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