The gastrointestinal microbiota as a site for the biotransformation of drugs

There are 100 trillion microbes in the human gastrointestinal tract with numbers increasing distally. These microbiota secrete a diverse array of enzymes (primarily for carbohydrate and protein fermentation) giving them substantial metabolic potential which can have major implications for drug stability. At least thirty drugs which are, or have been, available commercially, were subsequently shown to be substrates for these bacterial enzymes, and with increasing numbers of new and existing drugs having the potential for contact with the distal gut (through modified release systems or poor solubility/permeability), many more are expected to be discovered. The major concern with bacterial drug degradation is the behaviour of the metabolite; is it more or less active than the parent compound, or has toxicity resulted? For example, there were eighteen deaths in 1993 due to a drug interaction in which a toxic drug metabolite was produced by bacterial fermentation. Thus, the objective of this review is the provision of a comprehensive overview of this area; the gastrointestinal microbiota, their drug substrates and metabolic mechanisms, and approaches to studying this further are discussed.

MEDICIN OCH HÄLSOVETENSKAP Medicinska och farmaceutiska grundvetenskaper Farmaceutiska vetenskaper hsv//swe
MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmaceutical Sciences hsv//eng
Large intestine
Bacteria
Microbiota
Microflora
Xenobiotics
Stability
Fermentation
Metabolism
Bioavailability
Colonic delivery
PHARMACY
FARMACI

Paterson, Ronnie (författare)
Moore, Vanessa (författare)
Carlsson, Anders (författare)
Abrahamsson, BertilUppsala universitet,Institutionen för farmaci(Swepub:uu)berab705 (författare)
Basit, Abdul W (författare)
Uppsala universitetInstitutionen för farmaci (creator_code:org_t)

Ingår i:International Journal of Pharmaceutics: Elsevier BV363:1-2, s. 1-250378-51731873-3476

Av författaren/redakt...: Sousa, Tiago; Paterson, Ronnie; Moore, Vanessa; Carlsson, Anders; Abrahamsson, Ber ...; Basit, Abdul W

Om ämnet

MEDICIN OCH HÄLSOVETENSKAP: MEDICIN OCH HÄLS ...; och Medicinska och f ...; och Farmaceutiska ve ...

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