Research
Print page Print page
Switch language
The Capital Region of Denmark - a part of Copenhagen University Hospital
Published

Pharmacokinetics of high-dose intravenous melatonin in humans

Research output: Contribution to journalJournal articleResearchpeer-review

DOI

  1. Mesenteric Lymphadenitis and Terminal Ileitis is Associated With Yersinia Infection: A Meta-analysis

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Intraoperative handling of spermatic cord lipomas during inguinal hernia repair: a nationwide survey

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Trends in the use of patient-reported outcome measures for inguinal hernia repair: a quantitative systematic review

    Research output: Contribution to journalReviewResearchpeer-review

  4. Watchful waiting vs repair for asymptomatic or minimally symptomatic inguinal hernia in men: a systematic review

    Research output: Contribution to journalReviewResearchpeer-review

View graph of relations

This crossover study investigated the pharmacokinetics and adverse effects of high-dose intravenous melatonin. Volunteers participated in 3 identical study sessions, receiving an intravenous bolus of 10 mg melatonin, 100 mg melatonin, and placebo. Blood samples were collected at baseline and 0, 60, 120, 180, 240, 300, 360, and 420 minutes after the bolus. Quantitative determination of plasma melatonin concentrations was performed using a radioimmunoassay technique. Pharmacokinetic parameters were estimated by a compartmental pharmacokinetic analysis. Adverse effects included assessments of sedation and registration of other symptoms. Sedation, evaluated as simple reaction times, was measured at baseline and 120, 180, 300, and 420 minutes after the bolus. Twelve male volunteers completed the study. Median (IQR) Cmax after the bolus injections of 10 mg and 100 mg of melatonin were 221,500.0 (185,637.5-326,175.0) pg/mL and 1,251,500.0 (864,375.0-1,770,500.0) pg/mL, respectively; mean (SD) t1/2 was 42.3 (5.6) minutes and 46.2 (6.2) minutes; mean (SD) Vd was 1.6 (0.9) L/kg and 2.0 (0.8) L/kg; mean (SD) CL was 0.0253 (0.0096) L/min · kg and 0.0300 (0.0120) L/min · kg; and median (IQR) AUC0- ∞ , 8,997,633.0 (6,071,696.2-11,602,811.9) pg · min/mL and 54,685,979.4 (36,028,638.6-105,779,612.0) pg · min/mL. High-dose intravenous melatonin did not induce sedation, evaluated as simple reaction times. No adverse effects were reported in the study.

Original languageEnglish
JournalJournal of Clinical Pharmacology
Volume56
Issue number3
Pages (from-to)324-9
ISSN0091-2700
DOIs
Publication statusPublished - 16 Jul 2016

ID: 46000497