General

Principles of
CNS
Pharmacology
CNS controls:
• Control body function.
• Behavioral abilities.
• Intellectual abilities.

CNS communication = Synapses between neurons.

Drugs = Alter neuron function.
Organization of the CNS
Anatomical/Functional
• Cerebrum.
• Basal ganglia.
• Diencephalon.
• Mesencephalon and brainstem.
• Cerebellum.
• Limbic system.
• Spinal chord.
Diencephalon (Cerebrum)
• Largest part.
• Bilateral hemispheres (left/right).
• Lobes
o Frontal (largest/memory/emotion/problem solving/motor function).
o Temporal (2nd largest/auditory information/encoding of memory).
o Parietal (sensation/perception/integrate sensory input).
o Occipital (visual processing center).
• Cerebral cortex = Outer cerebrum.
o Conscious function.
o Integration.
o Sensory/motor function.
o Intellectual/cognitive abilities.
o Short-term memory
o Speech
o Supervisory function = lower brain.
o Control of ANS

• CNS drug function:

o Alter lower brain/spinal chord.
o Cerebral cortex(anti-epileptics/Alzheimer medication).
 Basal Ganglia
Specific areas deep within the cerebral hemisphere = Control of motor activity.
• Base of forebrain/top of midbrain.
o Caudate nucleus(dorsal stratum).
o Putamen (dorsal stratum).
o Olfactory tubercle (Ventral striatum).
o Nucleus accumbens (Ventral striatum).
o Globus pallidus.
o Lentiform nucleus.
o Substantia nigra.
• Affected in motor disorders.
o Parkinson’s disease.
o Huntington chorea.
 Mesencephalon
(Midbrain)/Brainstem
• Mesencephalon = Pathway/bridge → Cerebrum + Brainstem.
• Brainstem
o Pons
o Medulla

• Midbrain + Brainstem = Vasomotor center.

o Respiratory function.
o Cardiac function.

• Consist of reticular formation (interconnected nuclie).

o Collection of neurons = Upper spinal chord → Midbrain → Thalamus.
• Control consciousness.
• Regulate arousal/ alertness in cerebral cortex.
• Drugs:
o ↓activity → Sedative hypnotics/ general anesthetics.
o Stimulate → Caffeine/amphetamines.
 Cerebellum
• Posterior to brainstem/separated by 4TH ventricle.
• 2 hemispheres.
• Each has 3 lobes.
o Anterior.
o Posterior.
o Flocculonodular.

• Function:
o Plan/Coordinate motor activity.
o Compare actual movement with intended motor pattern.
• Interpret sensory input + Modulate motor output → Actual movement resembles
intended motion.
o Vestibular mechanisms (balance/posture).

• Drugs for incoordination/movement disorders cause

cerebellum toxicity.
 Limbic System
• Functional unit (several structures) within brain.
• Major structures:
o Cortical structures:
• Amygdala.
• Hippocampus.
• Cingulate gyrus.
o Hypothalamus.
o Thalamic nuclei.
o Mamillary bodies.
o Septum pellucidum.
• Function:
o Emotional activity.
o Behavioral activity.
o Motivation.
o Aggression.
o Sexual activity.
o Intrinsic responses.
• Drugs acting on limbic system are used as:
o Anti-anxiety.
o Anti-psychotic.
 Spinal Chord
• Cylindrical in shape.
• White matter (center).
o Contains myelinated axons of neurons grouped as ascending or descending tracts
between brain → specific level of chord.
o Local anesthetics → Block action potential in white matter → Information
(ascending/descending) is blocked → SPINAL BLOCK.
• Grey matter (surrounds white matter).
o Area for synaptic connections between neurons.
o Some drugs modify synaptic interaction between grey matter.
o Narcotics → alter synaptic transmission in spinal chord + brain.
 Blood-Brain Barrier
Structure/Function of CNS Capillaries = Selective filter
• Tight junctions between capillary endothelial cells.
• Lack of gaps/fenestrations.
• Impermeability of barrier ↑ due to :
o Non-neuronal cells (astrocytes).
o Capillary basement membrane.

• Implications for pharmacotherapy:

o Non-polar/lipo-soluble drugs = Enter by passive diffusion.
o Polar/lipophobic = Facilitated diffusion (glucose) + Active transport (Drug).
• Only few can enter.
• Removal of drugs and toxins → Active transport/diffusion →
drug unable to reach therapeutic level in CNS.
 CNS Neurotransmitters
Chemical neurotransmitters → Nervous impulses → Chemical synapses
• Neurotransmitters → Excitatory/Inhibitory.
• Different effects of same neurotransmitter → Nature of post-
synaptic receptor.
• Drugs alter function → Affecting neurotransmitters + No
change in pathway/neurons.
CNS Drugs
General Mechansim
• Drugs:
o ↑ synaptic neurotransmission.
o ↓ synaptic neurotransmission.
• Eg:
o Psychotic behavior → ↑ CNS synapse activity involving dopamine.
o Parkinson’s disease → ↓ CNS synapse activity involving dopamine.

• Drugs modify synaptic transmission:

o Alter neurotransmitter quantity.
o Alter post-synaptic stimulation.
o Both.
 Mechanisms
1. Pre-synaptic action potential.
2. Synthesis of neurotransmitter.
3. Storage of neurotransmitter.
4. Release.
5. Reuptake.
6. Degradation.
7. Post-synaptic receptor.
8. Pre-synaptic auto receptors.
9. Membrane effects.
 References
• Pharmacology in rehabilitation- Charles D. Ciccone