By
Nashwa Ibrahim
Mona Mansour
Practical pharma 2
CNS CVS
Animals
CNS stimulant CNS depressants Cases for Hypertension
Strychnine Thiopental
Picrotoxin Chloral hydrate Cases for Ischemic Heart Disease
Caffeine Chlorpromazine (CPZ)
Cases for Congestive Heart failure
Cases
Cases for Opioids analgesic
Nerve cells (neurons) are capable of conducting impulses.
Connection between nerve cells are synaptic in nature
Nervous system uses neurotransmitters to bridge the synapse.
The Resting Potential
The inside of the cell is (-) ve with respect to the outside
(polarization) in the resting state.
Na+ is outside & k+ is inside.
Assistant lecturer /Mona Mansour Ali
Section (1 )
When the nerve action potential reaches the nerve
terminals, Ca 2+ influx occur and fuses with the vesicles
storing the neurotransmitters with the membrane that
leads to exocytosis and release of the
chemical transmitter in the synaptic cleft.
The chemical transmitter reacts with the postsynaptic
receptor and form a neurotransmitter-receptor complex
that changes the permeability of the postsynaptic
membrane and causes either:-
Stimulation excitatory neurotransmitter.
Inhibition inhibitory neurotransmitter .
Assistant lecturer /Mona Mansour Ali
Section (1 )
Assistant lecturer /Mona Mansour Ali
Section (1 )
Resting Potential
Polarized state
+ + + + + + + + Na+
- - - - - - - - - - - K+
The inside of the cell is (-) ve with respect to the outside.
Na+ is outside & k+ is inside.
Effect of NT in action potential at post synaptic receptor
Excitatory NT Inhibitory NT
Depolarized state
Hyperpolarized state
- - - - - - - - - - - K+
+ + + + + + + + Na+
++++ + + + + + + + Na+
+ + + + + + + +K+
- - - - - - - - - - Cl
Ion channel opening with Na+ influx & K+ outflux
(K+ goes to the outside & Cl- to the inside)
depolarization
(hyperpolarization)
leads to an excitatory postsynaptic
potential ( EPSP ) and stimulation
leads to an inhibitory postsynaptic potential ( IPSP ) and inhibition.
Mona Mansour Ali
e.g., Ach action on the intestine Section (1 ) e.g., Ach action on the heart
Chemical Transmitters in the CNS
(Neurotransmitters)
MAP
Peptides
1. Substance P
Amino Acids 2. Endothelins
3. Neuropeptide Y
Mono amines (Biogenic 4. Vasoactive intestinal peptide ( VIP)
amines):- Inhibitory Excitatory 5. Morphinomimetic peptides
1. Norepinephrine 1. GABA ( endorphin, enkephalins, dynorphin)
1. Glutamic acid
2. Dopamine 2. Glycine 6. Hypothalamic releasing factors
2. Aspartic acid
3. Serotonin 3. Taurine
4. Histamine
Acetyl choline(Ach)
Purine compounds:-
1. Adenosine
2. Adenosine triphosphate
Assistant lecturer /Mona Mansour Ali
Section (1 )
Depressant Stimulant
Benzodiazepines
General anesthetics
Analgesic → Opioids Strychnine Picrotoxin
Caffine
Sedative-Hypnotic drugs Barbiturates Thiopental
(minor tranquilizers)
Miscellaneous agents→ Chloral hydrate
First generation.→ chlorpromazine (CPZ)
Antipsychotic drugs → neuroleptics
(major tranquilizers)
Second generation (atypical)
Assistant lecturer /Mona Mansour Ali
Section (1 )
CNS depressants
Sedative-Hypnotic drugs
Benzodiazepines Barbiturates Miscellaneous agents
Ultra-short-acting: e.g., thiopental
Short acting: e.g., triazolam Short-acting: e.g., secobarbital, amobarbital Chloral hydrate
intermediate acting: e.g., alprazolam Long-acting: e.g. phenobarbital
long acting: e.g., diazepam, flurazep
Mechanism of action
Act on GABAA receptors 1-Act on GABA rec by
BY → ↑ number of chloride channel openings ↑ duration of the chloride-channel openings. Its pro drug absorb from GIT
↓ converted to the active metabolite
hyperpolarization 2- block excitatory glutamate receptors. trichloroethanol,
↓
inhibits the formation of action potentials
Clinical uses
1. Anxiety 1. Induction of anesthesia
2. Sleep disorders 2. Seizure disorders
3. Muscle spasticity
Side effects
1. Drowsiness & impaired concentration S.E → skin irritation &vomiting
1. Drowsiness & confusion 2. Hang over
2. Rebound insomnia 3. Physical dependence & addiction Tolerance
Assistant lecturer /Mona Mansour Ali
Section (1 )
CNS depressants
Antipsychotic drugs (neuroleptics or major tranquilizers)
chlorpromazine (CPZ)
Clinical uses
1- Treatment of schizophrenia
Mechanism of action 2- Prevention of severe nausea and vomiting
Block dopamine receptors in the brain
Adverse effects
D2 receptor in the hypothalamus & limbic system
-Improve thought ,behavioural and conduction .
1. Extrapyramidal side effects
-Relieves hallucination .
2. Tardive dyskinesia
-Decrease the hyperactive psychotic patient .
3. Antipsychotic malignant syndrome
D1 receptors in the basal ganglia &the substantianigra which 4-Drowsiness
is a part of the extrapyramidal system 5-dry mouth, urinary retention, constipation
(control the skeletal muscle movement& tone regulation)……….. 6-lowered blood pressure and orthostatic hypotension
- That make Parkinson's like action .(motor restlessness—
unwanted effect .)
D2 receptors in the CTZ →.Antiemetic in all vomiting cases EXCEPT in motion sickness .
Anticholinergic Atropine like action so , benefit in small doses .
Assistant lecturer /Mona Mansour Ali
Section (1 )
What's CNS depressant
drugs that give to
animals in lab
Thiopental Chloral hydrate Chlorpromazine
(CPZ)
Causes sedation with no hypnosis
Produce staggering gait Produce staggering gait
Causes hypnosis of frog after seconds
Causes hypnosis of frog after minutes
Produces creeping gait
Catalepsy in mice
Assistant lecturer /Mona Mansour Ali
Section (1 )
How to calculate dose of drug?
First you must known
1- Dose of drug the give to animal, according to its weight.
2-Concentration of drug
For example
suppose that we want to administer drug in a dose of 100 mg/kg and in 1% concentration to a mouse
weighing 20 gm.
The calculation of the dose is done in two steps.
First step Second step
Calculate dose of drug Calculate conc
that give to mouse
1%conc of drug
100mg/kg
100mg → 1 kg 1gm → 100 ml
100mg → 1000gm
𝒙𝟏 mg ← 20 gm. 1000 mg→100 ml 𝟐∗𝟏𝟎𝟎
2mg← 𝒙𝟐 ml 𝒙𝟐 𝒎𝒍 = = 0.2 ml
𝟏𝟎𝟎𝟎
𝟐𝟎∗𝟏𝟎𝟎
𝒙𝟏 𝒎𝒈 = = 2 mg Assistant lecturer /Mona Mansour Ali
𝟏𝟎𝟎𝟎
Section (1 )
Rout of injection to mice and frog
Assistant lecturer /Mona Mansour Ali
Section (1 )
Assistant lecturer /Mona Mansour Ali
Section (1 )