Pharmacokinetics of oral and intravenous melatonin in healthy volunteers

The aim was to investigate the pharmacokinetics of oral and iv melatonin in healthy volunteers. The study was performed as a cohort crossover study. The volunteers received either 10 mg oral melatonin or 10 mg intravenous melatonin on two separate study days. Blood samples were collected at differen...

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Bibliographic Details
Published in:BMC pharmacology & toxicology 2016-02, Vol.17 (8), p.8, Article 8
Main Authors: Andersen, Lars P H, Werner, Mads U, Rosenkilde, Mette M, Harpsøe, Nathja G, Fuglsang, Hanne, Rosenberg, Jacob, Gögenur, Ismail
Format: Article
Language:English
Subjects:
Absorption
Administration, Oral
Adult
Antioxidants - administration & dosage
Antioxidants - analysis
Antioxidants - pharmacokinetics
Bioavailability
Biological Availability
Catheters
Central Nervous System Depressants - administration & dosage
Central Nervous System Depressants - blood
Central Nervous System Depressants - pharmacokinetics
Cohort Studies
Cross-Over Studies
Drug dosages
Half-Life
Humans
Infusion
Infusions, Intravenous
Intestinal Absorption
Intravenous administration
Male
Melatonin
Melatonin - administration & dosage
Melatonin - blood
Melatonin - pharmacokinetics
Metabolism
Method of residuals
Oral administration
Pharmacokinetics
Pharmacology
Plasma
Plasma levels
Regression analysis
Studies
Variables
Young Adult
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Summary:The aim was to investigate the pharmacokinetics of oral and iv melatonin in healthy volunteers. The study was performed as a cohort crossover study. The volunteers received either 10 mg oral melatonin or 10 mg intravenous melatonin on two separate study days. Blood samples were collected at different time points following oral administration and short iv infusion, respectively. Plasma melatonin concentrations were determined by RIA technique. Pharmacokinetic analyses were performed by "the method of residuals" and compartmental analysis. The pharmacokinetic variables: k a, t 1/2 absorption, t max, C max, t 1/2 elimination, AUC 0-∞, and bioavailability were determined for oral melatonin. C max, t 1/2 elimination, V d, CL and AUC 0-∞ were determined for intravenous melatonin. Twelve male volunteers completed the study. Baseline melatonin plasma levels did not differ significantly between the study days (P = 0.067). Mean (SD) t 1/2 absorption of oral melatonin was 6.0 (3.1) min. Mean t max was 40.8 (17.8) min with a median (IQR) C max of 3550.5 (2500.5-8057.5) pg ml(-1). Mean t 1/2 elimination was 53.7 (7.0) min. Median absolute bioavailability was 2.5 (1.7-4.7) %. Median C max after short iv infusion of melatonin was 389,875.0 (174,775.0-440,362.5) pg ml(-1). Mean t 1/2 elimination was 39.4 (3.6) min, mean V d 1.2 (0.6) l kg(-1) and mean CL 0.0218 (0.0102) l min(-1) kg(-1). This cohort crossover study estimated pharmacokinetics of oral and iv melatonin, respectively in healthy volunteers. Bioavailability of oral melatonin was only 3 %. Eudra-CT number: 2013-000205-23 (initial registration 27.03.2013). Clinicaltrials.gov Identifier: NCT01923974 (initial registration 08.08.2013).
ISSN:2050-6511
2050-6511
DOI:10.1186/s40360-016-0052-2