ANTIPSYCHOTIC 2003

8/8/2019 ANTIPSYCHOTIC 2003

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ANTIPSYCHOTICS

PREPARED BY

SIMEON L. CRUZ JR.

BSN-102 A



ANATOMY

ANDPHYSIOLOGY



Brain - it collects, integrates, and interprets all stimuli- it initiates & monitors voluntary & involuntary motor

activity

CEREBRUM (cerbral cortex)

BRAIN STEMCEREBELLUM



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



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



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



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



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 systemControls 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 bodyscommunication network

>it coordinates and organizes the

functions of all other body systems



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





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



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.













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



Classification System

Antipsychotics are generallyconceptualized in three ways :

Traditional Antipsychotics or First Generation

Drugs

Atypical Antipsychotics or Second Generation

Drug

Novel Antipsychotic Drugs



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 )



Low Potency Drug

Anticholigernic Effect

( e.g., DRY MOUTH , BLURRED VISION )

Antiadregernic Effect

( e.g., orthostatic hypotension )



High Potency Drug

Cause EPSEs



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



Novel Antipsychotics ( 3rd Generation )

This category is currently composedof just one drug ( Aripiprazole ( Ability )



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



ModeratePotency

Pherphenazine

12-64 High Low Low

Low

Potency

Chlorpromazine

200-1000

Moderate Moderate Low

Thrioridazine 200-

800

Low High High



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



NOVEL

( THIRDGENERATION)

Aripiprazole( Abilify )

10-30 Low Low Low



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



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



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.



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.



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 .



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 .



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.









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.



Oral administration

preferred route in variety of reasonsincluding the fact generally prefer this.

PROBLEM :

CHEEK ING



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 )



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



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



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 )



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.



End

By ; Semi



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ANTIPSYCHOTIC 2003