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.
RCT Entities:
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.
Authors: S Härtter; C Ursing; S Morita; G Tybring; C von Bahr; M Christensen; S Röjdmark; L Bertilsson Journal: Clin Pharmacol Ther Date: 2001-07 Impact factor: 6.875
Authors: Magnus Christensen; Katarina Andersson; Per Dalén; Rajaa A Mirghani; Gary J Muirhead; Anna Nordmark; Gunnel Tybring; Anneli Wahlberg; Umit Yaşar; Leif Bertilsson Journal: Clin Pharmacol Ther Date: 2003-06 Impact factor: 6.875
Authors: Susan B Brown; Susan E Hankinson; A Heather Eliassen; Katherine W Reeves; Jing Qian; Kathleen F Arcaro; Lani R Wegrzyn; Walter C Willett; Eva S Schernhammer Journal: Am J Epidemiol Date: 2015-01-13 Impact factor: 4.897
Authors: Eva S Schernhammer; Franco Berrino; Vittorio Krogh; Giorgio Secreto; Andrea Micheli; Elisabetta Venturelli; Sara Grioni; Christopher T Sempos; Adalberto Cavalleri; Holger J Schünemann; Sabrina Strano; Paola Muti Journal: Cancer Epidemiol Biomarkers Prev Date: 2010-03-03 Impact factor: 4.254
Authors: Nathja Groth Harpsøe; Lars Peter Kloster Andersen; Louise Vennegaard Mielke; Bo Jønsson; Morten Troels Jenstrup; Ismail Gögenur; Jacob Rosenberg Journal: Clin Drug Investig Date: 2016-12 Impact factor: 2.859
Authors: Seithikurippu R Pandi-Perumal; Venkatramanujan Srinivasan; D Warren Spence; Daniel P Cardinali Journal: CNS Drugs Date: 2007 Impact factor: 5.749