Introduction to CNS

And
Sedative-Hypnotics
And
Anti-epileptics

Dr.U.P.Rathnakar
MD. DIH. PGDHM
 CNS
Humans Animals
↓ ↓
Intelligence Instinct
 [Physiology of BRAIN]
Defines differences*
 Action of drugs on CNS challenging

Major th.importance-20% of all Rx –Analgesics

Self administration-Coffee, alcohol, nicotine, canabis
Gulf between drug action at cellular level &
behavioral level is wide
“ Throwing candy-floss across Grand canyon!”*
Some actions are well established

DA pathway & Parkinsonism

NA, 5HT and depression
DA & Schizo. Less well
established
Link bet. Cellular disturbances
and epilepsy –Simple- not
established
 Anatomy of CNS

Frontal lobe→ Higher functions, motor cortex

Parietal → Somato-sensory
Thalamus →Relay center for sensory pathway
Hypo →Autonomic, emotion, circardian, thirst,
hunger- CONTROL
Limbic →Learning, memory, emotion, addiction
Basal ganglion →Extrapyramidal control
Reticular formation →Sleep-wakefullness
Midbrain →Vision, hearing
Medulla →Vital functions
Cerebellum →Posture, balance
Sp.cord →integration????? *
 BBB

Tight junction & Glial cells around capillaries

Absent- Floor of iv vent[CTZ-area post rema], Pineal
gland, around pitutary
Defecient in new born
Pathological →HTN, Inflammation, heat/cold stress,
infection, radiation
Do not cross →Mol.wt.>60000, polar, Lipid soluble cross
Imp →Precursors-levodopa, AMA-intrathecally*
Neuro-chemical transmission

Basics same as in ANS

Neurotransmitters
4 processes of
neurotransmission
EPSP & IPSP*
 Neurotransmitters

Excitatory amino acids

L-Glutamate, Aspartate, Homocystate
Inhibitory AA
GABA, Glycine
Others
NA, DA, 5HT, Ach, Purines[Adenosine &
ATP], Histamine, Melatonin, NO,
Arachidonic acid, Anandamide*
A

Neurotransmitters
NT Rec Ago Antago Exc/Inh
M1 Atr, Pirenz. Ex
M2 Bethanecol Atro Inh
ACh
N Nicotine Exc
DA D1 Phenothi
D2 Bromo Phenothi Inh

GABA GABA A Biccuculine Inh

GABAB Baclofen Saclofen
Glycine Strychnine Inh
5HT 5HT Ketanserin Exc
Ondansetron (Inh)
NT Contd….

NT Rec Ago Antago Exc/Inh

NA α1 Phenyl Prazo Exc
α2 Clonidine Yohimbine Inh

β1 Dobutamine Atenolol Exc

β2 Albuterol Inh
Histamine H1 Mepyramine Exc
H2 Ranitidine Exc

H3 Inh
Opioids Mu,delta, Naloxone Inh
Kapa
Endocanab CB1 & 2 Rimonobant Inh
 Neurotrnsmission-4 processes
1. Neurotransmission
 NT Released by neurones
 Criteria
 Immediate EPSP oR IPSP
2. Neuromodulators
 NT released by neurones and astrocytes
 Long duration
 Long term changes in synaptic transmission
[Synaptic plasticity]
 Eg. CO2, Adenosine, PG, NO*
 Neurotrnsmission-4 processes
Neuromediators:
 II messengers [cAMP, cGMP, Inositol phosphate]
Neurotropic factors:
 Released by Neurones, astrocytes, microglia
 Longer duration
 Regulates growth & morphology of neurones
 Eg.Cytokines, Chemokines, growth factors
Neurohormones: released circulation-Vsopressin,
oxytocin*