INTRODUCTION TO

CNS
PHARMACOLOGY

TARGETS OF CNS DRUG ACTION

Most drugs that act on the CNS appear by
changing ion flow through transmembrane
channels of nerve cells.
Types of ion channels :
Voltage-gated
respons to changes in membrane
potential. Concentrated on the axon of
nerve cells, cell bodies and dendrites
Ligand-gated
respons to chemical neurotransmitter that
bind to reseptor.

 Role of ion current carried by the channel :

EPSPs or excitatory postsinaptic potentials,
are generated by the opening of sodium or
calcium channels.
IPSPs or inhibitory postsinaptic potentials,
are generated by the opening of pottasium or
chloride channels.
Role of CNS organization :
Hierarchial system
are delimited in their anatomic distribution
and generally contain large myelinated. It
controls major sensory and motor
function. The major EPSP is aspartat and
glutamate, and the IPSP is GABA or
glycine as transmitters.

 Diffuse systems
are broadly distributed, single cell (axon)
sending processes to many different areas.
The transmitters in diffuse system are
norepinephrine, dopamin, serotonin or
peptides that action on metabotropic
receptors.
Criteria for neurotransmitter :
Must present in high concentration in
synaptic area.
Must be released by stimulation via calciumdependent mechanism
Must produce the same sort of postsynaptic
response

ACETYLCHOLINE
Brain neurons have reseptor for ACh and most
CNS response to ACh.
Drugs affecting the activity of cholinergic
system in the brain include the
acethylcholinesterase inhibitors used in
Alzheimers disease (eg.tacrine) and muscarinic
blocking agents used in parkinsonism
(eg.benztropine).
DOPAMINE
Dopamine reseptor the major in basal ganglia
neurons and widely distributed at the
supraspinal level.
Drugs affecting the activity of dopaminergic
include antipsikotics (eg.chlorpromazine), CNS
stimulants (eg.amphetamine) and
antiparkinsonsm drugs (eg.levodopa)

NOREPINEPHRINE
Are mainly located in the brain stem and the
lateral tegmental area of the pons.
Excitatory effects are caused by activation of
alpha1 and beta1 reseptors.
Inhibitory effects are caused by activation of
alpha2 and beta2 reseptors.
SEROTONIN
Serotonin pathways from cell bodies or midline
regions of the pons and upper brain stem.
Used in the treatment of major depressive
disorder (eg.tricyclic antidepressant, selective
serotonin reuptake inhibitors)

GLUTAMIC ACID
Most neurons in the brain are excited by
glutamic acid.
Subtypes of glutamate reseptors include the
NMDA reseptor which is blocked by
phencyclidine and ketamin.
GABA AND GLYCINE
Is the primary neurotransmitter IPSP in neurons
in the brain.
Drugs that influence GABAergic system include
sedative-hypnotic (eg.barbiturates,
benzodiazepines), anticonvulsants
(eg.gabapentin).
Glycine reseptors more numerous in the cord,
are blocked by strychnine (a spinal convulsant)

PEPTIDE TRANSMITTER
Identified in the CNS. Important therapeutic
action for opioid analgesics (eg.morphine)

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