The discovery and use of antibiotics to fight against bacterial infection have let to overrun many diseases. However overuse and/or incorrect use of the antibiotics increase the concentration of these compounds in the environment and create the selective pressure, which promotes antibiotic resistant microorganisms. Multidrug resistant pathogenic bacteria are a huge problem of the modern medical science because of the infections, which they cause, are almost incurable. Researches show that the one of the most important mechanism responsible for the multidrug resistance in bacteria is the active transport (efflux system) of the antibiotics out of the cell. Bacterial drug efflux transporters are classified into the five groups: SMR (Small Multidrug Resistance), MFS (Major Facilitator Superfamily), RND (Resistance- Nodulation-Cell Division), MATE (Multidrug And Toxic Compound Extrusion) and ABC transporters (ATP-binding Cassette Superfamily). Currently scientists are working on recognition of molecular mechanisms of these transporters action, detection of their spatial structure and creation the model of drug transport. Additionally, new strategy of elimination of multidrug resistant bacteria focus on detecting of efflux pump inhibitors. It seems to be promising future strategy to control the bacterial diseases.