Journal
JOURNAL OF CLINICAL PHARMACOLOGY
Volume 56, Issue 3, Pages 324-329Publisher
WILEY
DOI: 10.1002/jcph.592
Keywords
adverse effects; intravenous; melatonin; pharmacokinetics; sedation
Categories
Ask authors/readers for more resources
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) 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) t(1/2) was 42.3 (5.6) minutes and 46.2 (6.2) minutes; mean (SD) V-d was 1.6 (0.9) Ukg and 2.0 (0.8) Ukg; mean (SD) CL was 0.0253 (0.0096) L/min.kg and 0.0300 (0.0120)L/min.kg; and median (IQR) AUC(0-infinity), 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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available