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Pharmacol Res. 2018 Apr;130:164-171. doi: 10.1016/j.phrs.2018.01.019. Epub 2018 Jan 31.

The role of gut microbiota in the pharmacokinetics of antihypertensive drugs.

Author information

1
Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do 15588, Republic of Korea.
2
Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do 15588, Republic of Korea. Electronic address: yoohh@hanyang.ac.kr.
3
Department of Life and Nanopharmaceutical Sciences and Department of Pharmacy, Kyung Hee University, 26, Kyungheedae-ro, Dongdaemun-gu, Seoul 02447, Republic of Korea. Electronic address: dhkim@khu.ac.kr.

Abstract

The intestine is one of the most important sites for the metabolism of several xenobiotic compounds. In addition to intestinal drug-metabolizing enzymes and drug transporters, gut microbial enzymes modulate the biotransformation of orally administered drugs in the gastrointestinal tract. Antihypertensive drugs such as amlodipine and nifedipine could be metabolized by gut microbial enzymes, which may influence drug absorption, leading to changes in pharmacological potency of the drug and eventual failure of the appropriate blood pressure control or unexpected side effects. This may suggest that there are additional mechanisms that can alter the therapeutic efficacy of antihypertensive drugs, especially in certain pathological conditions of the gastrointestinal tract or with concomitant use of substances such as antibiotics and probiotics that might alter the gut microbial composition. This review describes the metabolism of antihypertensive drugs by hepatic and intestinal microbial enzymes in an attempt to understand the potential effects of gut microbiota on their pharmacokinetics.

KEYWORDS:

Antihypertensive; Gut microbiota; Metabolism; Pharmacokinetics

PMID:
29391236
DOI:
10.1016/j.phrs.2018.01.019

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