PHL.

322
Presented by

Dr. Khairy M A Zoheir

Associate Professor
College of Pharmacy
KSU

I- CNS Stimulants
Drugs

Nervous System
The nervous system can be classified

into
The Central Nervous System
(CNS) Brain and spinal cord
The Peripheral Nervous System
(PNS( The nervous system outside of
the brain and spinal cord

Peripheral Nervous System

PNS
- Can be divided into
Sensory division(affrent)- 1
Conducts impulses from receptors to the
CNS and Informs the CNS of the state of
the body
2- Motor division(effrent)
Conducts impulses from CNS to effectors
organs.

Motor Neurons
The motor division is also divided into
1- The somatic nervous system :
VOLUNTARY (generally) Somatic nerve

fibers that conduct impulses from the CNS

to skeletal muscles
2. The autonomic nervous system:
INVOLUNTARY (generally) Conducts
impulses from the CNS to smooth muscle,
cardiac muscle, and glands

Neurons
They are the basic functional unit of
the nervous system.
They contain three major parts:
1.cell body.
2. dendrites.
3. axon.

Structure

Neurotransmitters CNS
They can be classified into :
1. Exitatory:
- Ach, glutamate, aspartate ,
serotonin and NE.
2. Inhibitory: - GABA , glycin .

CNS Stimulants
Defination
Stimulants are a substance
which tends to increase
behavioral activity when
administered

 Signs and symptoms:

1- Elevate Mood
2- Increase Motor Activity
3- Increase Alertness
4- Decrease need for Sleep
In case of overdose lead to
convulsion and death.

MOA of CNS Stimulants

1- Block neurotransmitters reuptake
(Most reuptake inhibitors affect either NE
or 5-HT(Serotonin) : Cocaine
2- Promote neurotransmitters release :
Amphetamine
3- Block Metabolism - MAO inhibitors
(monoamine oxidase):ex. Phenelzine
4. antagonize the effect of inhibitory
neurotransmitter: Picrotoxin & Strychnine

Neuronal Synapse

Neuronal Synapse

CNS Stimulants
- They can be divided based on their site
of action:

1.Cerebral stimulants (amphetamines)

2.Medullary stimulants (picrotoxin)
3.Spinal stimulants (strychnine)

Lab Work
- Objectives:
1- To demonstrate effects of some CNS

stimulant on mice.
2- After the lab, you should able to handle
and inject the mice correctly.
3- You should able to differentiate between
amphetamine,picrotoxin and strychinine
regarding the symptoms that induced by
each of them.

1- Amphetamine
MOAs :
Block the reuptake of norepinephrine and
dopamine into the presynaptic neuron and
increase the release of these monoamines
into the extraneuronal space.
- Clinical use:
1. Narcolepsy.
2. Attention-deficit hyperactivity disorder

Amphetamine
Adverse effects:
- Cardiovascular: Hypertension (7% to 22%,

pediatric )
- Endocrine metabolic: Weight loss (4% to 9%,
pediatric; 11%, adults )
- Gastrointestinal: Abdominal pain (11% to
14%, pediatrics ), Loss of appetite (22% to 36%),
Xerostomia (35% )
- Neurologic: Headache (26% ), Insomnia
(12% to 17%, pediatric; 27%, adults )
- Psychiatric: Feeling nervous (6% )

Amphetamine
After injecting, the mice with

amphetamine you well notice:

- Hair erection
- Licking, gnawing.
- Stereotype
- Sniffing

Picrotoxin
MOA:
Non-competitive antagonist of GABA

receptors.
After injecting the mice with picrotoxin you
wellnotice:
- Clonic convulsion characterized by :
1. Asymmetric
2. Intermittent
3. Spontaneous
4. Coordinated

Strychinine
MOA:
Competitive antagonist of the glycin receptors.
After injecting the mice with Strychinine you well
notice:
- Tonic convulsion characterized by :
1. Symmetric
2. Reflex in origin
3. Continuous
4. Uncoordinated.