ANTIPSYCHOTICS

PREPARED BY
SIMEON L. CRUZ JR.
BSN-102 A
 ANATOMY
AND
PHYSIOLOGY
Brain - it collects, integrates, and interprets all stimuli
- it initiates & monitors voluntary & involuntary motor
activity

CEREBRUM (cerbral cortex)

BRAIN STEM
CEREBELLUM
Cerebrum
Gives us the ability to think & reason
-enclosed in 3 membrane layers called meninges
is composed of lobes

Frontal lobe- personality, memory and motor function

Parietal lobe- sensory function

Temporal lobe- hearing and olfaction and emotion by the

limbic system

Occipital lobe- vision

Anatomy and Physiology
The cerebellum is involved in coordination and equilibrium
The diencephalon (a part of the cerebellum) consists of
the :

Thalamus- the relay center of all sensory input

Hypothalamus- center for endocrine regulation, sleep,

temperature, thirst, sexual arousal and emotional
response
Anatomy and Physiology
The brainstem (beneath the diencephalon)
Relays messages between the cerebrum & diencephalon &
spinal cord
Regulates automatic body functions e.g. swallowing, &
coughing
is composed of:

midbrain- for visual and auditory reflexes

Pons- respiratory apneustic center, nucleus of cranial

nerves- 5,6,7,8

Medulla oblongata- respiratory and cardiovascular centers,

nucleus of cranial nerves 9,10,11,12
Peripheral Nervous System
Includes:
Peripheral sensory nerves transmit stimuli from sensory
receptors in the skin, muscles, sensory organs, & the
viscera to the dorsal horn of the spinal cord
The upper motor neurons of the brain & the lower motor
neurons of cell bodies in the ventral horn of the spinal
cord carry impulses that affect the movement
Autonomic Nervous System
Contains motor neurons that regulate visceral organs &
innervate ( supply nerves to ) smooth & cardiac muscles
& the glands
TWO PARTS OF ANS
1. sympathetic nervous system
Controls the fight or flight response

2. parasympathetic nervous system

Maintains the baseline of the body functions
Responsible for the rest & digest response
>or nervous system is the body’s
communication network

>it coordinates and organizes the

functions of all other body systems
 NERVOUS SYSTEM

Central Nervous System Peripheral Nervous System

Brain Spinal Cord Motor (Efferent) Sensory (Afferent )

Neurons Neuron

Sympathetic Nervous
System
Autonomic Nervous
Somatic Nervous
System
System

Parasympathetic
Nervous System
 the NEURON or NERVE
CELL is the nervous system’s fundamental
unit this highly specialized conductor cell
receives and transmits electrochemical nerve
impulses

 delicate, threadlike nerve fibers called

AXONS & DENDRITES extend from the
cell body & transmit signals

 Axons carry impulses away from the

cell body;dendrites carry impulses to the
cell body

 this intricate network of interlocking

receptors & transmitters, along with
the brain & spinal cord, forms a living
computer that controls & regulates every
mental and physical function
 Each neuron communicates with each
other to a specific target tissue through
neurotransmitters

 These neurotransmitters are produced

& stored in the synaptic vesicles;they
enable conduction of impulses across the
synaptic cleft

 The action of neurotransmitters is to

MAJOR NEUROTRANSMITTERS: potentiate, terminate or modulate a
specific action & can either excite or
1. Acetycholine inhibit the target cell’s activity.
2. Serotonin
3. Dopamine
4. Norepinephrine

5. Gamma-aminobutyric acid (GABA)

6. Enkephalin,endorphin
 consists of the brain & the spinal cord that
are protected by the bony skull and vertebrae,
cerebrospinal fluid (CSF) and three
membranes: the dura mater, the arachnoid
membrane and the pia mater

The brain is contained in the rigid

skull, which protects it from injury;the
major bones of the skull are the frontal,
temporal, parietal & occipital bones;
These bones join at the suture lines

 The bones of the vertebral column

surround & protect the spinal cord &
normally consists of 7 cervical, 12
thoracic, 5 lumbar vertebrae,sacrum &
coccyx.
Introduction:
Antipsychotic drugs are used to treat
schizophrenia, bipolar disorder, and other
psychoses.

Discover accidentally around 1950. A

French scientist was hoping to develop a
new antihistamine and, in the process,
formulated chlorpromazine
Classification System
Antipsychotics are generally
conceptualized in three ways :

• Traditional Antipsychotics or First Generation

Drugs

• Atypical Antipsychotics or Second Generation

Drug

•Novel Antipsychotic Drugs

Traditional Antipsychotic Drugs

• Developed from 1950 – 1990

SUBCLASSIFICATION BASED ON
POTENCY

• HIGH-POTENCY DRUG - Haloperidol ( Haldol )

• MODERATE-POTENCY DRUG - Loxapine ( Moban )
• LOW-POTENCY DRUG – Chlorpromazine ( Thorazine )
Low Potency Drug

• Anticholigernic Effect
( e.g., DRY MOUTH , BLURRED VISION )

• Antiadregernic Effect
( e.g., orthostatic hypotension )
High Potency Drug

• Cause EPSE’s
ATYPICAL ( Second Generation )

 The newer agents ( from 1990 on )

Characteristics
• Reduce or no risks of EPES’s
• Increase effectiveness in treating negative
and cognitive signs
• Minimal risk of tardive diskinesia
• Absence of prolactin level elevation and
associative side effects
Novel Antipsychotics ( 3rd Generation )

• This category is currently composed

of just one drug – ( Aripiprazole ( Ability )
Major Traditional and Atypical Antipsychotics Drug
Drug Usual Rate of Rate of Rate of
Adult EPSE’s Anticholiger Weight Gain
mainten nic Effect
ace
Range
mg/day
Traditional
High Potency
Fluphenazine 0.5 – High Low Low
( Proxilin ) 40
Haloperidol 1-15 High Low Low
( Haldol )
 Moderate
Potency
Pherphenazin 12-64 High Low Low
e
Low
Potency
Chlorpromazi 200- Moderate Moderate Low
ne 1000
Thrioridazine 200- Low High High
800
 Atypical
Second
Generatio
n
Clozapine 75-900 Low High High
(Clozaril)
Risperidone 0.5-6 Low Low Moderate
(Riperdal)
Olanzapine 5-20 Low Moderate High
(Zyprexa)
Ziprasidone 40-160 Low Low Low
 NOVEL
( THIRD
GENERATION)
Aripiprazole 10-30 Low Low Low
( Abilify )
Positive Signs of Schizoprenia
  • Caused by excessive Dopamine in Mesolimbic Tract.
 Abnormal thought
Agitation
Associative Disturbance
Bizarre behavior
Delusion
Excitement
Hallucination
Illusion
Insomnia
Suspiciousness
Negative Symptoms of Schizophrenia

• caused by too little Dopamine in Mesocortical Tract

 Alogia
Anergia
Asocial Behavior
Attention Deficit
Avolition
Blunted affect
Communication Difficulty
Passive social withdrawal
Poor grooming
Poor rapport
Poverty Speech
Neurochemical Theory of Schizophrenia
This theory states that increase level of
Dopamine in the limbric area of the brain cause
schizophrenia and its psychotic symptoms ( e.g.,
hallucinations, delusions ) . Bec. Antipsychotics
drugs are Dopamine blockers.

Supported by clinical research, both of which

demonstrate that high dose ofs of dopaminergic
drug levodopa and amphetamines can produce
schizophrenia.
Four major Dopaminergic Track
• Dopamine is synthesized primarily in the
substantia nigra and ventral tegmal area and is
delivered to the distant sites via dopaminergic
tracts.
• To appreciate the complexity of
psychopharmacologic treatment of schizophrenia
fully, the students may recognized the existence
of DOPAMINE-DEPENDENT areas of the brain
that communicate dopamine synthesizing areas
via different neuronal tracts.
Neural Tracts

Tract 1 : Nigrostriatal Tract is involved in

movement. Traditional antipsychotic blockade
can cause EPSEs.

Tract 2 : The Tuberoinfundibular Tract

modulates pituitary functions. Traditional
Antipsychotics can lead to elevation prolactic
level.
Neural Track

Tract 3 : The Mesolimbic Tract is involved in

emotional and sensory process. Traditional
antipsychotics blockade normalizes these process in
individuals with schizophrenia, reliving or eliminating
hallucinations and delusion.

Tract 4 : The Mesocortical tract involve in cognitive

processes. Traditional antipsychotics blockade can
intensify negative and cognitive problems.
The Ultimate Antipsychotic Agent
mesolimbic
Blocks the Dopamine receptors in the
area ( dec. Hallucination and
Delusion )
 Liberates Dopamine in mesocortical area
( treating negative symptoms )
 While not obstructing the function of nigrostriatal
tract ( not causing EPSEs )
 Blocking the receptors in tuberoinfundibular tract
( not resulting In prolactin levels )

Atypical antipsychosis can DO this.

Pharmacokinetics
• Absorption for these drugs is variable.
Oral drugs – 1 to 6 hrs
newly disintegrating tablets 2mins.

•These are highly fat soluble and can accumulate

in fatty tissue and release slowly.

• 90 - 99 % protein bound.
• Oral administration
preferred route in variety of reasons
including the fact generally prefer this.

PROBLEM :

• CHEEKING
Parenteral Drugs
• Usually used to treat acutely disturb individuals
or patience who represents significant
compliance risk.

Long acting injectables forms are available

and required injections only once every 2-4
weeks or less frequent.
• Fluphenazine deconate ( Proxilin Deconate )
• Haloperidol deconate ( Haldol Deconate )
• Risperidone deconate ( Riperdal Consta )
ANTICHOLIGERNIC EFFECTS
PNS anticholigernic effects are result from the
blocking of CNs with parasympathetic
components.
• CN III : Oculomotor nerve blockade
( blurred vision )
• CN VII : Facial nerve blockade
( Dry mouth, dec. Tearing, dry nasal passage )
• CN IX : Glossopharyngeal nerve blockade
( dry mouth, dry nasal passage )
• CN X : Vagus nerve blockade
( Tachycardia, contipations, urinary hesitation )
Extrapyramidal Effect
Akathisia
- subjective feeling of restlessness
demonstrated by result restless legs, jittery
feelings.
Akinesia and Bradykinesia
- refers to an absence of movements ;
slowed movements.
Dystonia
- abnormal postures caused by involuntary
muscle spasm
Kinds of Dystonia
Torticollis – contracted positioning of the neck

Oculogyric – contracted positioning of the eyes

UPWARD

Writers’s cramp – fatigue spasm affecting hand.

Laryngeal-pharyngeal constriction ( potentially life

threatening )
Toxicity
Overdose of antipsychotic drugs are
seldom fatal. An overdose can cause
severe CNS DEPRESSANT,
HYPOTENSION, and EPSEs.
Restlessness or agitation, convulsions,
hyperthermia, increased anticholigernic
symptoms are other indicators of an
overdose.
End
By ; Semi 
Elements
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