alexa The Role of Transporters in the Pharmacokinetics of Antibiotics

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The Role of Transporters in the Pharmacokinetics of Antibiotics

Antibiotics or antibacterials are a type of antimicrobial used specifically against bacteria, antibiotics are used to treat various infections and are often used in medical treatment of bacterial infections.


Various drug transporters, including efflux transporters and uptake transporters, are widely expressed in body and play an important role in the absorption, distribution, excretion and metabolism of drugs 

OATPs/Oatps and antibiotics

OATPs/Oatps are expressed in a wide range of tissues in the body and are responsible for the Na+-independent uptake of large amphipathic organic anions into cells.

Fluoroquinolones are antimicrobial drugs that are widely used for the treatment of bacterial and fungal infections. Although has hydrophilic nature, most fluoroquinolones are absorbed efficiently from the small intestine and show relatively high bioavailability.

BCRP/Bcrp and antibiotics

Breast cancer resistance protein (BCRP/ABCG2), one important member of the ABC family of transporters, is apically expressed and mediates the active and outward transport of a range of anticancer drugs, dietary compounds, food carcinogens, and antibiotics.

Other transporters (P-gp and MRP) and antibiotics

ATP dependent efflux transporter P-glycoprotein (P-gp, MDR1) and multidrug resistance associated protein (MRP) also play an important role in the pharmacokinetics of antibiotics.

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