Drugs acting on the Central Nervous System

Central Neurotransmitters
GABA
- inhibitory neurotransmitter
Receptors: GABA A
GABA B
Glycine:
- inhibitory
Local interneurons in the spinal cord & brain stem
Glutamate:
-excitatory neurotransmitter
KA (kainate):
-hippocampus, cerebellum, spinal cord
mediate fast depolarization
AMPA (-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid )
-mediate fast depolarization
NMDA (N-methyl-D-aspartate)
-Long term potentiation **increase firing rate(ion channel
stimulation)
Aspartate: excitatory
Acetylcholine:
Spinal cord Renshaw cells
neurons in the neostriatum, medial septal nucleus, reticular formation
M1, M2 and Nm **stimulation of M2**
Dopamine:
Substantia nigra neostriatum
Ventral tegmental region limbic cortex
D1 D5
Norepinephrine: hypothalamus , limbic system
enhances excitatory inputs by both indirect and direct mechanisms
Attention and arousal
1, and
2(may cause inhibition)
5-Hydroxytryptamine (5HT) :neurons in the raphe or midline regions of
the pons and upper brain stem
5HT1

5HT2
5HT3 : ionotropic
5HT4
Histamine: ventral posterior hypothalamus
regulate arousal, body temperature, and vascular dynamics
H1 H2 H3
Peptides: enkephalins, endorphins, neurotensin, substance P
Diffusible Mediators
NO
Arachidonic acid
ACTIONS OF DRUGS IN THE CNS
CNS Stimulants(physical and mental)
CNS Depressants
Drugs that selectively modify CNS function

CNS Stimulants
Amphetamines - methamphetamine, dextroamphetamine (Adderal)
Displaces catecholamines*
ADHD (Attention deficit hyperactivity disorder) >>>
Methylphenidate (Ritalin) and Atomoxetine (Strattera)>>not
stimulate(a SSRI used in ADHD).
Narcolepsy >>>>>>> Modafinil (Provigil)
Respiratory stimulation after anesthesia >>>>> Doxapram