Human gut microbiota plays a role in the metabolism of drugs.

BACKGROUND AND AIMS The gut microbiome, an aggregate genome of trillions of microorganisms residing in the human gastrointestinal tract, is now known to play a critical role in human health and predisposition to disease. It is also involved in the biotransformation of xenobiotics and several recent studies have shown that the gut microbiota can affect the pharmacokinetics of orally taken drugs with implications for their oral bioavailability. METHODS Review of Pubmed, Web of Science and Science Direct databases for the years 1957-2016. RESULTS AND CONCLUSIONS Recent studies make it clear that the human gut microbiota can play a major role in the metabolism of xenobiotics and, the stability and oral bioavailability of drugs. Over the past 50 years, more than 30 drugs have been identified as a substrate for intestinal bacteria. Questions concerning the impact of the gut microbiota on drug metabolism, remain unanswered or only partially answered, namely (i) what are the molecular mechanisms and which bacterial species are involved? (ii) What is the impact of host genotype and environmental factors on the composition and function of the gut microbiota, (iii) To what extent is the composition of the intestinal microbiome stable, transmissible, and resilient to perturbation? (iv) Has past exposure to a given drug any impact on future microbial response, and, if so, for how long? Answering such questions should be an integral part of pharmaceutical research and personalised health care.

• Publication year

  2016

• Venue

  Biomedical papers of the Medical Faculty of the University Palacky, Olomouc, Czechoslovakia

• Publication date

  2016-08-02

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.5507/bp.2016.039PMID 27485182
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Brain-gut-microbiota axis: challenges for translation in psychiatry.

  2016cited by this paper
• Gut microbiome as a novel cardiovascular therapeutic target.

  2016cited by this paper
• Effects of orally administered antibiotics on the bioavailability of amlodipine: gut microbiota-mediated drug interaction

  2016cited by this paper
• The influence of gut microbiota on drug metabolism and toxicity

  2016cited by this paper
• The role of the intestinal microbiota in type 1 diabetes mellitus

  2016cited by this paper
• Agent Based Modeling of Human Gut Microbiome Interactions and Perturbations

  2016cited by this paper
• Gut microbiota in autism and mood disorders.

  2016cited by this paper
• The microbiome in asthma.

  2015cited by this paper
• The Microbiota and Microbiome in Aging: Potential Implications in Health and Age‐Related Diseases

  2015cited by this paper
• Influence and effect of the human microbiome in allergy and asthma

  2015cited by this paper
• Gut barrier in health and disease: focus on childhood.

  2015cited by this paper
• Gut microbiota and aging

  2015cited by this paper
• Disentangling the effects of type 2 diabetes and metformin on the human gut microbiota

  2015cited by this paper
• P14-035Imipenem, a carbapenem type antibiotic, does not alter pharmacokinetics of a model drug nabumetone

  2015cited by this paper
• Gut Microbiota-Mediated Drug Interactions between Lovastatin and Antibiotics

  2014cited by this paper
• Effect of MMX® mesalamine coadministration on the pharmacokinetics of amoxicillin, ciprofloxacin XR, metronidazole, and sulfamethoxazole: results from four randomized clinical trials

  2014cited by this paper
• The Influence of Intestinal Tract and Probiotics on the Fate of Orally Administered Drugs.

  2014cited by this paper
• The Central Role of the Gut Microbiota in Chronic Inflammatory Diseases

  2014cited by this paper
• Intestinal microbiota in health and disease: role of bifidobacteria in gut homeostasis.

  2014cited by this paper
• Microbiome Diversity and Asthma and Allergy Risk

  2014cited by this paper
• Analytical power of LLE-HPLC-PDA-MS/MS in drug metabolism studies: identification of new nabumetone metabolites.

  2013cited by this paper
• The influence of diet on the gut microbiota.

  2013cited by this paper
• Supplemental materials for: Intestinal microbiota metabolism of L-carnitine, a nutrient in red meat, promotes atherosclerosis

  2013cited by this paper
• Oral drug delivery systems using chemical conjugates or physical complexes.

  2013cited by this paper
• Long-term ecological impacts of antibiotic administration on the human intestinal microbiota

  2013cited by this paper
• Xenobiotics shape the physiology and gene expression of the active human gut microbiome.

  2013cited by this paper
• The effect of gut microbiota on drug metabolism

  2013cited by this paper
• Gut microbiota protects against gastrointestinal tumorigenesis caused by epithelial injury.

  2013cited by this paper
• Update on rifampin, rifabutin, and rifapentine drug interactions

  2013cited by this paper
• Gut microbiota disturbance during antibiotic therapy: a multi-omic approach

  2012cited by this paper
• Gut microbiota composition correlates with diet and health in the elderly

  2012cited by this paper
• Structure, Function and Diversity of the Healthy Human Microbiome

  2012cited by this paper
• Gut Pharmacomicrobiomics: the tip of an iceberg of complex interactions between drugs and gut-associated microbes

  2012cited by this paper
• Nabumetone

  2012cited by this paper
• Health impact of probiotics - vision and opportunities

  2012cited by this paper
• Enterotypes of the human gut microbiome

  2011cited by this paper
• Human Health and Disease in a Microbial World

  2011cited by this paper
• A human gut microbial gene catalogue established by metagenomic sequencing

  2010cited by this paper
• Incomplete recovery and individualized responses of the human distal gut microbiota to repeated antibiotic perturbation

  2010cited by this paper
• Reshaping the gut microbiome with bacterial transplantation and antibiotic intake.

  2010cited by this paper
• Composition, variability, and temporal stability of the intestinal microbiota of the elderly

  2010cited by this paper
• Mode of delivery affects the bacterial community in the newborn gut.

  2010cited by this paper
• Pharmacometabonomic identification of a significant host-microbiome metabolic interaction affecting human drug metabolism

  2009cited by this paper
• Towards the human intestinal microbiota phylogenetic core.

  2009cited by this paper
• The gastrointestinal microbiota as a site for the biotransformation of drugs.

  2008cited by this paper
• Long-term ecological impacts of antibiotic administration on the human intestinal microbiota

  2007cited by this paper
• Effect of Ketoconazole and Rifampicin on the Pharmacokinetics of Ranitidine in Healthy Human Volunteers: A Possible Role of P-Glycoprotein

  2006cited by this paper
• RNA Viral Community in Human Feces: Prevalence of Plant Pathogenic Viruses

  2005cited by this paper
• Obesity alters gut microbial ecology.

  2005cited by this paper
• Bacterial acetylation of 5-aminosalicylic acid in faecal suspensions cultured under aerobic and anaerobic conditions

  2005cited by this paper
• Host-Bacterial Mutualism in the Human Intestine

  2005cited by this paper
• Resilience of the Dominant Human Fecal Microbiota upon Short-Course Antibiotic Challenge

  2005cited by this paper
• The use of formulation technology to assess regional gastrointestinal drug absorption in humans.

  2004cited by this paper
• Regulation of short-chain fatty acid production

  2003cited by this paper
• An in vitro Study on the Active Conversion of Flucytosine to Fluorouracil by Microorganisms in the Human Intestinal Microflora

  2003cited by this paper
• Susceptibility of the H2-receptor antagonists cimetidine, famotidine and nizatidine, to metabolism by the gastrointestinal microflora.

  2002cited by this paper
• Colonic metabolism of ranitidine: implications for its delivery and absorption.

  2001cited by this paper
• A possible mechanism of eighteen patient deaths caused by interactions of sorivudine, a new antiviral drug, with oral 5-fluorouracil prodrugs.

  1998cited by this paper
• The Role of Mammalian Intestinal Bacteria in the Reductive Metabolism of Zonisamide

  1997cited by this paper
• Intestinal flora and endogenous vitamin synthesis

  1997cited by this paper
• Intestinal anaerobic bacteria hydrolyse sorivudine, producing the high blood concentration of 5-(E)-(2-bromovinyl)uracil that increases the level and toxicity of 5-fluorouracil.

  1997cited by this paper
• Reduction of nitrazepam by Clostridium leptum, a nitroreductase-producing bacterium isolated from the human intestinal tract.

  1997cited by this paper
• Interactions between genetic and environmental factors in colorectal carcinogenesis.

  1997cited by this paper
• Metabolism of omeprazole by gut flora in rats.

  1995cited by this paper
• A pharmacological, pharmacokinetic and clinical overview of risperidone, a new antipsychotic that blocks serotonin 5‐HT2 and dopamine D2 receptors

  1995cited by this paper
• The estimation of paracetamol and its major metabolites in both plasma and urine by a single high-performance liquid chromatography assay.

  1994cited by this paper
• The metabolism of drugs by the gut flora

  1994cited by this paper
• The metabolism and excretion of risperidone after oral administration in rats and dogs.

  1994cited by this paper
• Metabolism of 5'-ether prodrugs of 1-beta-D-arabinofuranosyl-E-5-(2-bromovinyl)uracil in rats.

  1993cited by this paper
• The role of the gastrointestinal microflora in the metabolism of drugs

  1993cited by this paper
• Comparative developmental toxicity and metabolism of nitrazepam in rats and mice.

  1993cited by this paper
• Involvement of the intestinal microflora in nitrazepam-induced teratogenicity in rats and its relationship to nitroreduction.

  1991cited by this paper
• Metabolism of levamisole, an anti-colon cancer drug, by human intestinal bacteria.

  1991cited by this paper
• Olsalazine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in inflammatory bowel disease.

  1991cited by this paper
• Metabolism of lovastatin by rat and human liver microsomes in vitro.

  1988cited by this paper
• Role of the intestinal flora in the acetylation of sulfasalazine metabolites.

  1987cited by this paper
• The reduction of sulphinpyrazone and sulindac by intestinal bacteria.

  1987cited by this paper
• Methanogens in human and animal intestinal Tracts

  1986cited by this paper
• Microbial phosphorylation of compactin (ML-236B) and related compounds.

  1985cited by this paper
• Role of the intestinal microflora in clonazepam metabolism in the rat.

  1984cited by this paper
• Studies of two novel sulfasalazine analogs, ipsalazide and balsalazide

  1983cited by this paper
• 6 alpha-Hydroxy-iso-ML-236B (6 alpha-hydroxy-iso-compactin) and ML-236A, microbial transformation products of ML-236B.

  1983cited by this paper
• 3 alpha-Hydroxy-ML-236B (3 alpha-hydroxycompactin), microbial transformation product of ML-236B (compactin).

  1983cited by this paper
• Metabolism of digoxin and absorption site.

  1982cited by this paper
• Inactivation of digoxin by the gut flora: reversal by antibiotic therapy.

  1981cited by this paper
• A metronidazole metabolite in human urine and its risk.

  1981cited by this paper
• Role of the intestinal flora in the metabolism of misonidazole.

  1980cited by this paper
• Kinetics and metabolism of paracetamol and phenacetin.

  1980cited by this paper
• The anaerobic metabolism of metronidazole forms N-(2-hydroxyethyl)-oxamic acid.

  1979cited by this paper
• Acetamide--a metabolite of metronidazole formed by the intestinal flora.

  1979cited by this paper
• Bioavailability of Drugs: The Digoxin Dilemma

  1976cited by this paper
• [Comparison of bacterial and microsomal azo- and nitro-reductases (author's transl)].

  1975cited by this paper
• Metabolism of N-acylated and O-alkylated drugs by the intestinal microflora during anaerobic incubation in vitro.

  1974cited by this paper
• The metabolism of salicylazosulphapyridine in ulcerative colitis

  1973cited by this paper
• Contributions of host and intestinal microflora in the metabolism of L-dopa by the rat.

  1973cited by this paper
• Distribution studies of salicylazosulfapyridine and its metabolites.

  1973cited by this paper
• Metabolism of foreign compounds by gastrointestinal microorganisms.

  1973cited by this paper
• The role of intestinal bacteria in the metabolism of salicylazosulfapyridine.

  1972cited by this paper
• The role of the gut flora in the metabolism of prontosil and neoprontosil in the rat.

  1971cited by this paper
• Lactulose in the treatment of chronic portal-systemic encephalopathy. A double-blind clinical trial.

  1969cited by this paper

• GutBugDB: a web resource to predict the human gut microbiome-mediated biotransformation of biotic and xenobiotic molecules

  2025cites this paper
• Impact of Gut Microbiota on Drug Metabolism and Absorption

  2025cites this paper
• The Role Played by Imidazole Propionic Acid in Modulating Gut-Heart Axis and the Development of Atherosclerosis: An Explorative Review

  2025cites this paper
• Unraveling the pharmaceutical excipient-drug interactions: The effects of polyethylene glycol copolymers on drug metabolism and transport systems.

  2025cites this paper
• The impact of Cephalexin on Pharmacokinetic of Rosuvastatin In Induced Hyperlipidemia In Rabbits

  2025cites this paper
• The Gut Microbiota’s Role in Drug Absorption, Metabolism and Efficacy: Implications for Personalized Medicine

  2025cites this paper
• Gut microbiome perturbation and its correlation with tylosin pharmacokinetics in healthy and infected pigs

  2024cites this paper
• Gut Microbiota Disruption in Hematologic Cancer Therapy: Molecular Insights and Implications for Treatment Efficacy

  2024cites this paper
• New Perspectives on the Risks of Hydroxylated Polychlorinated Biphenyl (OH-PCB) Exposure: Intestinal Flora α-Glucosidase Inhibition

  2024cites this paper
• Assessment of the impact of intravenous antibiotics treatment on gut microbiota in patients: Clinical data from pre-and post-cardiac surgery

  2023cites this paper
• Pharmacomicrobiomics and Drug–Infection Interactions: The Impact of Commensal, Symbiotic and Pathogenic Microorganisms on a Host Response to Drug Therapy

  2023cites this paper
• Influence of Different Diets on the Degradation of Sulfasalazine by Colon Bacteria Determined Using MimiCol3

  2023cites this paper
• GutBug: A Tool for Prediction of Human Gut Bacteria Mediated Biotransformation of Biotic and Xenobiotic Molecules Using Machine Learning.

  2023cites this paper
• Clinical Relevance of Gut Microbiota Alterations under the Influence of Selected Drugs—Updated Review

  2023cites this paper
• Dexmedetomidine alleviates host ADHD-like behaviors by reshaping the gut microbiota and reducing gut-brain inflammation.

  2023cites this paper
• Evolving interplay between natural products and gut microbiota.

  2023cites this paper
• The Effect of the Gut Microbiota on Transplanted Kidney Function

  2023cites this paper
• Opportunities and Challenges for Nanotherapeutics for the Aging Population

  2022cites this paper
• Hepatic drug metabolism and gut microbiome.

  2022cites this paper
• Effect of DSS-Induced Ulcerative Colitis and Butyrate on the Cytochrome P450 2A5: Contribution of the Microbiome

  2022cites this paper
• Gut microbiome: A potential indicator for predicting treatment outcomes in major depressive disorder

  2022cites this paper
• Butyrate Treatment of DSS-Induced Ulcerative Colitis Affects the Hepatic Drug Metabolism in Mice

  2022cites this paper
• Marked shifts in gut microbial structure and neurotransmitter metabolism in fresh inmates revealed a close link between gut microbiota and mental health: A case-controlled study

  2022cites this paper
• Butyrate, a typical product of gut microbiome, affects function of the AhR gene, being a possible agent of crosstalk between gut microbiome and hepatic drug metabolism.

  2022cites this paper
• Development of an in vitro Model of Human Gut Microbiota for Screening the Reciprocal Interactions With Antibiotics, Drugs, and Xenobiotics

  2022cites this paper
• Consensus Prediction of Human Gut Microbiota-Mediated Metabolism Susceptibility for Small Molecules by Machine Learning, Structural Alerts, and Dietary Compounds-Based Average Similarity Methods

  2022cites this paper
• Pharmacomicrobiomics: Exploiting the Drug-Microbiota Interactions in Antihypertensive Treatment

  2022cites this paper
• Research progress on intestinal mucosal injury induced by traditional Chinese medicine

  2021cites this paper
• A comprehensive review for gut microbes: technologies, interventions, metabolites and diseases.

  2021cites this paper
• Assessment of Oral Vancomycin-Induced Alterations in Gut Bacterial Microbiota and Metabolome of Healthy Men

  2021cites this paper
• Biomodification of acenocoumarol by bifidobacteria.

  2021cites this paper
• Comprehensive Gut Microbiota and Drug Processing

  2021cites this paper
• Gut microbiome affects the metabolism of metronidazole in mice through regulation of hepatic cytochromes P450 expression

  2021cites this paper
• Presence or absence of microbiome modulates the response of mice organism to administered drug nabumetone.

  2020cites this paper
• Gut Microbiome Alters the Activity of Liver Cytochromes P450 in Mice With Sex-Dependent Differences

  2020cites this paper
• An in vitro evaluation of the effects of different statins on the structure and function of human gut bacterial community

  2020cites this paper
• Effects of intestinal flora on the pharmacokinetics and pharmacodynamics of aspirin in high-altitude hypoxia

  2020cites this paper
• Correlations between Microbiota Bioactivity and Bioavailability of Functional Compounds: A Mini-Review

  2020cites this paper
• Impact of Vancomycin‐Induced Changes in the Intestinal Microbiota on the Pharmacokinetics of Simvastatin

  2020cites this paper
• Characterization of the Gut Microbiota of Individuals at Different T2D Stages Reveals a Complex Relationship with the Host

  2020cites this paper
• Catabolic Machinery of the Human Gut Microbes Bestow Resilience Against Vanillin Antimicrobial Nature

  2020cites this paper
• Can Gut Microbiota Modulation Could Reduce the Signs and Complications of COVID-19?

  2020cites this paper
• Bioavailability Based on the Gut Microbiota: a New Perspective

  2020cites this paper
• Crosstalk between gut microbiota and antidiabetic drug action

  2019cites this paper
• Gut microbiota metabolizes nabumetone in vitro: Consequences for its bioavailability in vivo in the rodents with altered gut microbiome

  2019cites this paper
• Chemo-Preventive Potential of Falcarindiol-Enriched Fraction from Oplopanax elatus on Colorectal Cancer Interfered by Human Gut Microbiota.

  2019cites this paper
• Prescribed Drugs and the Microbiome.

  2019cites this paper
• From Petri Dish to Patient: Bioavailability Estimation and Mechanism of Action for Antimicrobial and Immunomodulatory Natural Products

  2019cites this paper
• Interaction of the microbiota with the human body in health and diseases

  2019cites this paper
• The Role of the Gut Microbiota in the Metabolism of Polyphenols as Characterized by Gnotobiotic Mice

  2018cites this paper
• N-Acetyltransferase-2 (NAT2) phenotype is influenced by genotype-environment interaction in Ethiopians

  2018cites this paper
• The Promise of Personalized Medicine

  2018cites this paper
• Genomics and Drug-Metabolizing Enzymes and Its Application in Drug Delivery: Evaluating the Influence of the Microbiome

  2018cites this paper
• Gut microbes as future therapeutics in treating inflammatory and infectious diseases: Lessons from recent findings

  2018cites this paper
• An Ex Vivo Fermentation Screening Platform to Study Drug Metabolism by Human Gut Microbiota

  2018cites this paper
• Interaction of antidiabetic α‐glucosidase inhibitors and gut bacteria α‐glucosidase

  2018cites this paper
• Pharmacomicrobiomics: a novel route towards personalized medicine?

  2018cites this paper
• Developmental pattern of hepatic drug-metabolizing enzymes in pediatric population and its role in optimal drug treatment

  2017cites this paper
• Nutrikinetic study of genistein metabolites in ovariectomized mice

  2017cites this paper
• Impact of gut microbiota on drug metabolism: an update for safe and effective use of drugs

  2017influential citation
• RNA-Seq Profiling of Intestinal Expression of Xenobiotic Processing Genes in Germ-Free Mice

  2017cites this paper
• The Gut, Its Microbiome, and Hypertension

  2017cites this paper
• Colonization by non-pathogenic bacteria alters mRNA expression of cytochromes P450 in originally germ-free mice

  2017cites this paper
• The Open Repository @ Binghamton (The ORB) The Open Repository @ Binghamton (The ORB)

  year unknowncites this paper