The transporter mediated uptake of various drugs and toxic compounds by choroid plexuses has been extensively described over the last decades. In conjunction with several other specific features of the choroidal tissue such as its drug metabolism and antioxidant capacities, these transport activities contribute to the neuroprotective functions attributed to the choroid plexus. Recently, the molecular identity and localization of the proteins responsible for the influx and efflux of drugs and metabolites at the choroid plexus has started to be deciphered, thus allowing a better understanding of the directionality and significance of the transport processes observed at the choroid plexus. Transport of drugs and metabolites involves mainly the SLC (solute carrier) and ABC (ATP-Binding Cassette) transporter super-families. In this review, we describe the identity and mechanism of transport of the SLC and ABC members so far characterized at the choroid plexus.