Pharmacokinetics of Caffeine: A Systematic Analysis of Reported Data for Application in Metabolic Phenotyping and Liver Function Testing
Grzegorzewski J, Bartsch F, Köller A, König M
Frontiers in pharmacology · 74 citations
How it was studied
- Design
- Systematic review (classified by our AI screen)
- Studied in
- People
- Main outcome
- Health markers and function
Who paid for it
- Funding
- Independent funding
- Government
- Deutsche Forschungsgemeinschaft
- Government
- Bundesministerium für Bildung und Forschung
- University or hospital
- Humboldt-Universität zu Berlin
- Government
- German Network for Bioinformatics Infrastructure
- Grants
- German Network for Bioinformatics Infrastructure (031A533A); German Network for Bioinformatics Infrastructure (031A534A); German Network for Bioinformatics Infrastructure (031A538A); German Network for Bioinformatics Infrastructure (031 A535 A); Bundesministerium für Bildung und Forschung (031 A 534A); Bundesministerium für Bildung und Forschung (031A533A); Bundesministerium für Bildung und Forschung (031 A538A); Deutsche Forschungsgemeinschaft (031A533B); Deutsche Forschungsgemeinschaft (031A537C); German Network for Bioinformatics Infrastructure (031 A537B); Bundesministerium für Bildung und Forschung (# 031A537C); German Network for Bioinformatics Infrastructure (031A537B, 031A533A, 031A538A, 031A533B, 031A535A, 031A537C, 031A534A, 031A532B); Bundesministerium für Bildung und Forschung (031 A535A); Deutsche Forschungsgemeinschaft (031A534A); Bundesministerium für Bildung und Forschung (#031A537B); Bundesministerium für Bildung und Forschung (031A537B, 031A533A, 031A538A, 031A533B, 031A535A, 031A537C, 031A534A, 031A532B); German Network for Bioinformatics Infrastructure (031 A532B); German Network for Bioinformatics Infrastructure (031 A533B); Deutsche Forschungsgemeinschaft (031A537B); German Network for Bioinformatics Infrastructure (#031A537C); Deutsche Forschungsgemeinschaft (FOR 5151); Deutsche Forschungsgemeinschaft (031A535A); Deutsche Forschungsgemeinschaft (031A538A); Deutsche Forschungsgemeinschaft (031A532B); Bundesministerium für Bildung und Forschung (031A532B); Deutsche Forschungsgemeinschaft (031A533A); Bundesministerium für Bildung und Forschung (031L0054); Bundesministerium für Bildung und Forschung (031A533B)
Based on 4 listed funder(s) and full-text disclosure statement.
Publication
- Published
- 2022-02-25 · Front Pharmacol · vol. 12 · p. 752826
- Publisher
- Frontiers Media
- Cited
- 104 citations · more than 99% of similar papers · 12.9× the field average
- Impact
- Top 10% most cited in its field
- References
- 196 works
- Access
- Open access (journal) · CC-BY
- Research areas
- Coffee research and impacts · Pharmacogenetics and Drug Metabolism · Tea Polyphenols and Effects
- Keywords
- Caffeine, Paraxanthine, CYP1A2, Pharmacokinetics, Theobromine, Theophylline, Pharmacology, Context (archaeology), Physiologically based pharmacokinetic modelling, Medicine, Drug, Cytochrome P450, Biology, Internal medicine, Metabolism
4 authors
From DE
- Jan GrzegorzewskiHumboldt-Universität zu Berlin
- Florian BartschHumboldt-Universität zu Berlin
- Adrian KöllerHumboldt-Universität zu Berlin
- Matthias KönigHumboldt-Universität zu Berlin
Abstract
Caffeine is by far the most ubiquitous psychostimulant worldwide found in tea, coffee, cocoa, energy drinks, and many other beverages and food. Caffeine is almost exclusively metabolized in the liver by the cytochrome P-450 enzyme system to the main product paraxanthine and the additional products theobromine and theophylline. Besides its stimulating properties, two important applications of caffeine are metabolic phenotyping of cytochrome P450 1A2 (CYP1A2) and liver function testing. An open challenge in this context is to identify underlying causes of the large inter-individual variability in caffeine pharmacokinetics. Data is urgently needed to understand and quantify confounding factors such as lifestyle (e.g., smoking), the effects of drug-caffeine interactions (e.g., medication metabolized via CYP1A2), and the effect of disease. Here we report the first integrative and systematic analysis of data on caffeine pharmacokinetics from 141 publications and provide a comprehensive high-quality data set on the pharmacokinetics of caffeine, caffeine metabolites, and their metabolic ratios in human adults. The data set is enriched by meta-data on the characteristics of studied patient cohorts and subjects (e.g., age, body weight, smoking status, health status), the applied interventions (e.g., dosing, substance, route of application), measured pharmacokinetic time-courses, and pharmacokinetic parameters (e.g., clearance, half-life, area under the curve). We demonstrate via multiple applications how the data set can be used to solidify existing knowledge and gain new insights relevant for metabolic phenotyping and liver function testing based on caffeine. Specifically, we analyzed 1) the alteration of caffeine pharmacokinetics with smoking and use of oral contraceptives; 2) drug-drug interactions with caffeine as possible confounding factors of caffeine pharmacokinetics or source of adverse effects; 3) alteration of caffeine pharmacokinetics in disease; and 4) the applicability of caffeine as a salivary test substance by comparison of plasma and saliva data. In conclusion, our data set and analyses provide important resources which could enable more accurate caffeine-based metabolic phenotyping and liver function testing.
Abstract via Europe PMC. Copyright remains with the authors or publisher (CC BY).
Community trust
Loading…
How much do you trust this study's findings?
Comments
Sign in to rate, comment on or flag this study.Sign inSomething wrong here?
Flag this study if its information, labels or funding look wrong. An editor reviews every flag.
Sign in to rate, comment on or flag this study.Sign inEducational information about published research. Not medical advice, and not a recommendation to start or stop anything.