Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor.
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Chen J, Raymond K
Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor.
Ann Clin Microbiol Antimicrob. 2006 Feb 15;5:3.
- PubMed ID
- 16480505 [ View in PubMed]
- Abstract
Rifampicin, an important drug in the treatment of tuberculosis, is used extensively despite its broad effects on drug-drug interactions, creating serious problems. The clinical importance of such interactions includes autoinduction leading to suboptimal or failed treatment. The concomitantly administered effects of rifampicin on other drugs can result in their altered metabolism or transportation that are metabolised by cytochromes P450 or transported by p-glycoprotein in the gastrointestinal tract and liver. This review paper summarises recent findings with emphases on the molecular mechanisms used to explain these broad drug-drug interactions. In general, rifampicin can act on a pattern: rifampicin activates the nuclear pregnane X receptor that in turn affects cytochromes P450, glucuronosyltransferases and p-glycoprotein activities. This pattern of action may explain many of the rifampicin inducing drug-drug interactions. However, effects through other mechanisms have also been reported and these make any explanation of such drug-drug interactions more complex.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Rifampicin Nuclear receptor subfamily 1 group I member 2 Protein Humans UnknownAgonistDetails - Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Rifampicin Cytochrome P450 2C9 Protein Humans UnknownInducerDetails - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Rifampicin P-glycoprotein 1 Protein Humans UnknownInducerDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareDolutegravirRifampicin The serum concentration of Dolutegravir can be decreased when it is combined with Rifampicin. FosphenytoinRifampicin The serum concentration of Fosphenytoin can be decreased when it is combined with Rifampicin. PhenytoinRifampicin The serum concentration of Phenytoin can be decreased when it is combined with Rifampicin. RaltegravirRifabutin The serum concentration of Raltegravir can be decreased when it is combined with Rifabutin.