Induction of influx and efflux transporters and cytochrome P450 3A4 in primary human hepatocytes by rifampin, rifabutin, and rifapentine.

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Williamson B, Dooley KE, Zhang Y, Back DJ, Owen A

Induction of influx and efflux transporters and cytochrome P450 3A4 in primary human hepatocytes by rifampin, rifabutin, and rifapentine.

Antimicrob Agents Chemother. 2013 Dec;57(12):6366-9. doi: 10.1128/AAC.01124-13. Epub 2013 Sep 23.

PubMed ID
24060875 [ View in PubMed
]
Abstract

Rifampin is a potent inducer of cytochrome P450 (CYP) enzymes and transporters. Drug-drug interactions during tuberculosis treatment are common. Induction by rifapentine and rifabutin is understudied. Rifampin and rifabutin significantly induced CYP3A4 (80-fold and 20-fold, respectively) in primary human hepatocytes. The induction was concentration dependent. Rifapentine induced CYP3A4 in hepatocytes from 3 of 6 donors. Data were also generated for ABCB1, ABCC1, ABCC2, organic anion-transporting polypeptide 1B1 (OATP1B1), and OATP1B3. This work serves as a basis for further study of the extent to which rifamycins induce key metabolism and transporter genes.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
RifapentineCytochrome P450 3A4ProteinHumans
Unknown
Substrate
Inducer
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Ledipasvir
Tipranavir		The serum concentration of Ledipasvir can be decreased when it is combined with Tipranavir.
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Levothyroxine		The serum concentration of Ledipasvir can be decreased when it is combined with Levothyroxine.
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Trazodone		The serum concentration of Ledipasvir can be decreased when it is combined with Trazodone.
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Mifepristone		The serum concentration of Ledipasvir can be decreased when it is combined with Mifepristone.
Ledipasvir
Rifampicin		The serum concentration of Ledipasvir can be decreased when it is combined with Rifampicin.