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8/8/2019 ANTIPSYCHOTIC 2003
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ANTIPSYCHOTICS
PREPARED BY
SIMEON L. CRUZ JR.
BSN-102 A
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ANATOMY
ANDPHYSIOLOGY
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Brain - it collects, integrates, and interprets all stimuli- it initiates & monitors voluntary & involuntary motor
activity
CEREBRUM (cerbral cortex)
BRAIN STEMCEREBELLUM
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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 thelimbic system
Occipital lobe- vision
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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 emotionalresponse
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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 cranialnerves- 5,6,7,8
Medulla oblongata- respiratory and cardiovascular centers,nucleus of cranial nerves 9,10,11,12
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Peripheral Nervous System
Includes:Peripheral sensory nerves transmit stimuli from sensory
receptors in the skin, muscles, sensory organs, & theviscera to the dorsal horn of the spinal cord
The upper motor neurons of the brain & the lower motorneurons of cell bodies in the ventral horn of the spinalcord carry impulses that affect the movement
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Autonomic Nervous System
Contains motor neurons that regulate visceral organs &innervate ( supply nerves to ) smooth & cardiac muscles& the glands
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TWO PARTS OF ANS
1. sympathetic nervous systemControls the fight or flight response
2. parasympathetic nervous system
Maintains the baseline of the body functions
Responsible for the rest & digest response
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>or nervous system is the bodyscommunication network
>it coordinates and organizes the
functions of all other body systems
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NERVOUS SYSTEM
Central Nervous SystemPeripheral Nervous System
Brain Spinal Cord Motor (Efferent)
Neurons
Sensory (Afferent )
Neuron
Autonomic NervousSystem
Somatic NervousSystem
Sympathetic NervousSystem
Parasympathetic
Nervous System
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Each neuron communicates with each
other to a specific target tissue throughneurotransmitters
These neurotransmitters are produced
& stored in the synaptic vesicles;they
enable conduction of impulses across the
synaptic cleft
The action of neurotransmitters is to
potentiate, terminate or modulate a
specific action & can either excite or
inhibit the target cell¶s activity.
MAJOR NEUROTRANSMITTERS:
1. Acetycholine
2. Serotonin3. Dopamine
4. Norepinephrine
5. Gamma-aminobutyric acid (GABA)
6. Enkephalin,endorphin
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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 rigidskull , 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.
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Introduction:
Antipsychotic drugs are used to treat schizophrenia, bipolar disorder, and otherpsychoses.
Discover accidentally around 1950. A French scientist was hoping to develop a
new antihistamine and, in the process,formulated chlorpromazine
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Classification System
Antipsychotics are generallyconceptualized in three ways :
Traditional Antipsychotics or First Generation
Drugs
Atypical Antipsychotics or Second Generation
Drug
Novel Antipsychotic Drugs
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T raditional Antipsychotic Drugs
Developed from 1950 1990
SUBCLASSIFICATION BASED ON
POTENCY
HIGH-POTENCY DRUG - Halop eridol ( Haldol )
MODERATE-POTENCY DRUG - Lo xapin e ( Mo ban )
LOW-POTENCY DRUG Chlorpromazin e ( Thorazin e )
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Low Potency Drug
Anticholigernic Effect
( e.g., DRY MOUTH , BLURRED VISION )
Antiadregernic Effect
( e.g., orthostatic hypotension )
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High Potency Drug
Cause EPSEs
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ATYPICAL ( Second Generation )
The newer agents ( from 1990 on )
Characteristics
Reduce or no risks of EPESs
Increase effectiveness in treatingnegative and cognitive signs
Minimal risk of tardive diskinesia Absence of prolactin level elevation and
associative side effects
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Novel Antipsychotics ( 3rd Generation )
This category is currently composedof just one drug ( Aripiprazole ( Ability )
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Major T raditional and Atypical Antipsychotics Drug
Drug Usual
Adultmainten
aceRange
mg/day
Rate of
EPSEs
Rate of
Anticholigernic Effect
Rate of
Weight Gain
TraditionalHigh Potency
Fluphenazine( Proxilin )
0.5 40
High Low Low
Haloperidol
( Haldol )
1-15 High Low Low
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ModeratePotency
Pherphenazine
12-64 High Low Low
Low
Potency
Chlorpromazine
200-1000
Moderate Moderate Low
Thrioridazine 200-
800
Low High High
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AtypicalSecond
Generation
Clozapine
( Clozaril)
75-900 Low High High
Risperidone(Riperdal)
0.5-6 Low Low Moderate
Olanzapine
(Zyprexa)
5-20 Low Moderate High
Ziprasidone 40-160 Low Low Low
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NOVEL
( THIRDGENERATION)
Aripiprazole( Abilify )
10-30 Low Low Low
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Positive Signs of Schizoprenia Caused by excessive Dopamine in Mesolimbic Tract.
A bnormal t hought
A gitation
Ass ociativ e Di s tur banc e
Bizarr e behavior
D elu s ion
E xcit em ent
Hallucination
Illu s ion In s omnia
Su s piciou s n ess
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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 withdrawalPoor grooming
Poor rapport
Poverty Speech
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Neurochemical Theory of Schizophrenia
This theory states that increase level of Dopamine in the limbric area of the brain causeschizophrenia and its psychotic symptoms ( e.g.,hallucinations, delusions ) . Bec. Antipsychotics
drugs are Dopamine blockers.
Supported by clinical research, both of whichdemonstrate that high dose ofs of dopaminergic
drug levodopa and amphetamines can produceschizophrenia.
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Four major Dopaminergic T rack
Dopamine is synthesized primarily in thesu bstantia nig ra and v entral teg mal area and isdeliv ered to the distant sites v ia dopaminerg ictracts.
To appreciate the complexity of psychopharmacolog ic treatment of schizophreniaf u lly, the st u dents may recog nized the existenceof DOP AMINE-DEPENDENT areas of the brain
that commu nicate dopamine synthesizing areasv ia different neu ronal tracts.
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Neural T racts
Tract 1 : Nigro s triatal Tract i s i nvol ved i nmo vement . Tra ditio nal a nti ps yc hotic bloc ka deca n ca us e EPSEs .
Tract 2 : T he T uberoi nfundi bular Tract mo dulat es pit uitar y functio ns . Tra ditio nal Anti ps yc hotic s ca n l ea d to el evatio n prolactic l evel .
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Neural T rack
Tract 3 : The M es olim bic Tract i s i nvol ved i nemotio nal a nd s ens or y proc ess . Tra ditio nal a nti ps yc hotic s bloc ka de normali zes t hes e
proc ess i n i ndi vi dual s wit h s c hi zo phr enia , r eli vi ngor elimi nati ng hall uci natio ns a nd del us io n.
Tract 4 : The M es ocortical tract i nvol ve i nco gniti ve proc ess es . Tra ditio nal a nti ps yc hotic s bloc ka de ca n i nt ens i fy negati ve a nd co gniti vepro bl em s .
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The Ultimate Antipsychotic Agent
Blocks the Dopamine receptors in themesolimbic area ( dec. Hallucination andDelusion )
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 )
A typical antipsychosis can DO this.
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Pharmacokinetics
Absorption for these drugs is variable.
Oral drugs 1 to 6 hrs
newly disintegrating tablets 2mins.
These are highly fat soluble and can accumulatein fatty tissue and release slowly.
90 - 99 % protein bound.
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Oral administration
preferred route in variety of reasonsincluding the fact generally prefer this.
PROBLEM :
CHEEK ING
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Parenteral Drugs
Usually used to treat acutely disturb individuals
or patience who represents significant compliance risk.
Long acting injectables forms are availableand required injections only once every 2-4weeks or less frequent.
Fluphenazine deconate ( Proxilin Deconate )
Haloperidol deconate ( Haldol Deconate ) Risperidone deconate ( Riperdal Consta )
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ANTICHOLIGERNIC EFFECTS
PNS anticholigernic effects are result from theblocking of CNs with parasympatheticcomponents.
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 )
l
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Extrapyramidal Effect
Akathisia
- subjective feeling of restlessnessdemonstrated by result restless legs, jitteryfeelings.
Akinesia and Bradykinesia- refers to an absence of movements ;slowed movements.
Dystonia
- abnormal postures caused by involuntarymuscle spasm
d f
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Kinds of Dystonia
Torticollis contracted positioning of the neck
Oculogyric contracted positioning of the eyesUPW ARD
Writerss cramp fatigue spasm affecting hand.
Laryngeal-pharyngeal constriction ( potentially lifethreatening )
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T oxicity
Overdose of antipsychotic drugs areseldom fatal. An overdose can causesevere CNS DEPRESSANT,H YPOTENSION, and EPSEs.
Restlessness or agitation, convulsions,hyperthermia, increased anticholigernicsymptoms are other indicators of an
overdose.
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End
By ; Semi
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