The blood-brain barrier (BBB) is a highly selective semi-permeable membrane that separates the cerebral blood circulation from the brain and extracellular fluid in the central nervous system (CNS). The BBB is composed of endothelial cells, astrocyte end-feet and pericytes embedded in the capillary basement membrane. This system allows the passage of water, some gases and lipid-soluble molecules by passive diffusion, as well as, selective molecules such as glucose and amino acids. This review discusses pharmacodynamic concepts and methods that allow drugs to penetrate the BBB structure and enter the CNS and spinal nervous systems (SNS).