Methods and compositions for treating a condition involving gastrointestinal symptoms comprising administering to a patient in need of such treatment an effective amount of a P-glycoprotein substrate, wherein the P-glycoprotein substrate is a compound exhibiting an efflux inhibition ratio (EIR) of greater than or equal to 0.4, wherein the P-glycoprotein substrate is administered in a manner to minimize bioavailability.

 
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