Methods and compositions are described for the modulation of central
nervous system and/or fetal effects of substances. Methods and
compositions are described for the modulation of efflux transporter
activity to increase the efflux of drugs and other compounds out of a
physiological compartment and into an external environment. In
particular, the methods and compositions disclosed herein provide for the
increase of efflux transporter activity at blood-brain, blood-CSF and
placental-maternal barriers to increase the efflux of drugs and other
compounds from physiological compartments, including central nervous
system and fetal compartments.