Archives of Pharmacal Research

, Volume 40, Issue 12, pp 1345–1355 | Cite as

Impact of gut microbiota on drug metabolism: an update for safe and effective use of drugs

  • Keumhan Noh
  • You Ra Kang
  • Mahesh Raj Nepal
  • Rajina Shakya
  • Mi Jeong Kang
  • Wonku Kang
  • Sangkyu Lee
  • Hye Gwang Jeong
  • Tae Cheon JeongEmail author


The intestinal mucosa and liver have long been considered as the main sites of drug metabolism, and the contribution of gut microbiota to drug metabolism has been under-estimated. However, it is now generally accepted that the gut microbiota plays an important role in drug metabolism prior to drug absorption or during enterohepatic circulation via various microbial enzymatic reactions in the intestine. Moreover, some drugs are metabolized by gut microbiota to specific metabolite(s) that cannot be formed in the liver. More importantly, the metabolism of drugs by gut microbiota prior to absorption can alter the systemic bioavailability of certain drugs. Therefore, understanding drug metabolism by gut microbiota is critical for explaining changes in the pharmacokinetics of drugs, which may cause significant alterations in drug-induced pharmacodynamics and toxicities. In this review, we describe recent progress with regard to the role of metabolism by gut microbiota in some drug-induced alterations of either pharmacological or toxicological effects to emphasize the clinical importance of gut microbiota for safe and effective use of drugs.


Gut microbiota Drug metabolism Pharmacokinetics Pharmacodynamics Toxicity 



This work was supported by grants from National Research Foundation of Korea (NRF-2017R1D1A3B04033313) and from Yeungnam University (214-A-345-027).

Compliance with ethical standards

Conflict of interest

The authors declare no conflict of interest.


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© The Pharmaceutical Society of Korea 2017

Authors and Affiliations

  1. 1.Department of Pharmaceutical Sciences, Leslie Dan Faculty of PharmacyUniversity of TorontoTorontoCanada
  2. 2.College of PharmacyYeungnam UniversityGyeongsanRepublic of Korea
  3. 3.College of PharmacyChung-Ang UniversitySeoulRepublic of Korea
  4. 4.College of PharmacyKyungpook National UniversityDaeguRepublic of Korea
  5. 5.College of PharmacyChungnam National UniversityDaejeonRepublic of Korea

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