Effects of caffeine intake on the pharmacokinetics of melatonin, a probe drug for CYP1A2 activity.

Article Details

Citation

Copy to clipboard

Hartter S, Nordmark A, Rose DM, Bertilsson L, Tybring G, Laine K

Effects of caffeine intake on the pharmacokinetics of melatonin, a probe drug for CYP1A2 activity.

Br J Clin Pharmacol. 2003 Dec;56(6):679-82.

PubMed ID

14616429 [ View in PubMed

]

Abstract

AIMS: The aim of this study was to assess the influence of concomitant caffeine intake on the pharmacokinetics of oral melatonin, a probe drug for CYP1A2 activity. METHODS: Twelve healthy subjects, six smokers and six nonsmokers, were given melatonin (6 mg) either alone or in combination with caffeine (3 x 200 mg). Blood samples for the analysis of melatonin or caffeine and paraxanthine were taken from 1 h before until 6 h after intake of melatonin. Subjects were genotyped with respect to the CYP1A2*1F (C734A) polymorphism. RESULTS: When caffeine was coadministered the Cmax and AUC of melatonin were increased on average by 142% (P = 0.001, confidence interval on the difference 44, 80%) and 120% (P < 0.001, confidence interval on the difference 63, 178%), respectively. The inhibitory effect of caffeine was more pronounced in nonsmokers and in individuals with the *1F/*1F genotype. CONCLUSION: The results of this study revealed a pronounced effect of caffeine on the bioavailability of orally given melatonin, most probably due to inhibition of CYP1A2 activity.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Caffeine	Cytochrome P450 1A2	Protein	Humans	Unknown	Substrate Inhibitor	Details
Melatonin	Cytochrome P450 1A2	Protein	Humans	Unknown	Substrate	Details