Introduction to CNS pharmacology

Most drugs that affect the central nervous system (CNS) act by altering some step in the neurotransmission process. Drugs affecting the CNS may act presynaptically by influencing the production, storage, release, or termination of action of neurotransmitters. Other agents may activate or block postsynaptic receptors.

Figure 1: neurotransmission process

Neurotransmission in the CNS
In many ways, the basic functioning of neurons in the CNS is similar to that of the autonomic nervous system. For example, transmission of information in the CNS and in the periphery both involve the release of neurotransmitters that diffuse across the synaptic space to bind to specific receptors on the postsynaptic neuron. In both systems, the recognition of the neurotransmitter by the membrane receptor of the postsynaptic neuron triggers intracellular changes. However, several major differences exist between neurons in the peripheral autonomic nervous system and those in the CNS.
The circuitry of the CNS is much more complex than that of the autonomic nervous system, and the number of synapses in the CNS is far greater. The CNS, unlike the peripheral autonomic nervous system, contains powerful networks of inhibitory neurons that are constantly active in modulating the rate of neuronal transmission. In addition, the CNS communicates through the use of more than 10 (and perhaps as many as 50) different neurotransmitters. In contrast, the autonomic nervous system uses only two primary neurotransmitters, acetylcholine and norepinephrine.