This document provides information about antipsychotic drugs. It discusses that antipsychotics are mainly used to treat mental illnesses such as schizophrenia and bipolar disorder. There are two main types of antipsychotics: newer atypical antipsychotics and older typical antipsychotics. Antipsychotics are thought to work by altering chemicals in the brain like dopamine and serotonin. The document also summarizes schizophrenia, bipolar disorder, and different types of antipsychotic drugs.

2. ANTIPSYCHOTIC DRUGS
JAI NARAIN VYAS UNIVERSITY, JODHPUR
ASSISTANT PROFESSOR:- ASHWIN SINGH
CHOUHAN
DEPARTMENT:- PHARMACOLOGY
E-mail:- anshukavya1993@gmail.com

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ANTIPSYCHOTICS
Antipsychotics are a group of medicines that are mainly
used to treat mental health illnesses such
as schizophrenia, or mania (where you feel high or
elated) caused by bipolar disorder. They can also be used
to treat severe depression and severe anxiety.
Antipsychotics are sometimes also called major
tranquillisers.

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THERE ARE TWO MAIN TYPES OF ANTIPSYCHOTICS
Newer or atypical antipsychotics. These are
sometimes called second-generation antipsychotics and
include: amisulpride, aripiprazole, clozapine, olanzapine,
quetiapine and risperidone.
Older typical well-established antipsychotics. These
are sometimes called first-generation antipsychotics and
include: chlorpromazine, flupentixol, haloperidol, levomep
romazine,pericyazine,perphenazine, sulpiride and zuclope
nthixol.

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HOW DO ANTIPSYCHOTICS WORK
Antipsychotics are thought to work by altering the effect
of certain chemicals in the brain, called dopamine,
serotonin, noradrenaline and acetylcholine. These
chemicals have the effect of changing your behaviour,
mood and emotions. Dopamine is the main chemical that
these medicines have an effect on.
By altering the effects of these chemicals in the brain
they can suppress or prevent you from experiencing:
Hallucinations (such as hearing voices).
Delusions (having ideas not based on reality).
Thought disorder.
Extreme mood swings that are associated with bipolar
disorder

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PSYCHOSIS
Psychosis is a condition that affects the way your
brain processes information. It causes you to lose touch
with reality. You might see, hear, or believe things that
aren’t real. Psychosis is a symptom, not an illness. A
mental or physical illness, substance abuse, or
extreme stress or trauma can cause it.
Psychotic disorders, like schizophrenia, involve psychosis
that usually affects you for the first time in the late teen
years or early adulthood. Young people are especially
likely to get it, but doctors don’t know why. Even before
what doctors call the first episode of psychosis (FEP), you
may show slight changes in the way you act or think. This
is called the prodromal period and could last days, weeks,
months, or even years.

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Symptoms of a psychotic episode: Usually you’ll
notice all of the above plus.
Hallucinations
Auditory hallucinations: Hearing voices when no one is
around Tactile hallucinations: Strange sensations or
feelings you can’t explain Visual hallucinations: You see
people or things that aren’t there, or you think the shape
of things looks wrong
Delusions
Beliefs that aren’t in line with your culture and that don’t
make sense to others, like: Outside forces are in control
of your feelings and actions Small events or comments
have huge meaning You have special powers, are on a
special mission, or actually are a god

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PSYCHOTHERAPY
Counseling, along with medicines, can also help manage
psychosis.
Cognitive behavioral therapy (CBT) can help you
recognize when you have psychotic episodes. It also
helps you figure out whether what you see and hear is
real or imagined. This kind of therapy also stresses the
importance of antipsychotic medications and sticking with
your treatment.
Supportive psychotherapy helps you learn to live with
and manage psychosis. It also teaches healthy ways of
thinking.

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Cognitive enhancement therapy (CET) uses computer
exercises and group work to help you think and
understand better.
Family psychoeducation and support involves your
loved ones. It helps you bond and improves the way you
solve problems together.
Coordinated specialty care (CSC) creates a team
approach in treating psychosis when it’s first diagnosed.
CSC combines medication and psychotherapy with social
services and work and education support.

10. BIPOLAR DISORDER
Bipolar disorder, also known as manic depression, is
a mental illness that brings severe high and low moods
and changes in sleep, energy, thinking, and behavior.
People who have bipolar disorder can have periods in
which they feel overly happy and energized and other
periods of feeling very sad, hopeless, and sluggish. In
between those periods, they usually feel normal. You can
think of the highs and the lows as two "poles" of mood,
which is why it's called "bipolar" disorder.
The word "manic" describes the times when someone
with bipolar disorder feels overly excited and confident.
These feelings can also involve irritability and impulsive
or reckless decision-making.
JNVU PHARMACY, JODHPUR

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"Hypomania" describes milder symptoms of mania, in
which someone does not have delusions or hallucinations,
and their high symptoms do not interfere with their
everyday life.
The word "depressive" describes the times when the
person feels very sad or depressed. Those symptoms are
the same as those described in major depressive disorder
or "clinical depression," a condition in which someone
never has manic or hypomanic episodes.
Most people with bipolar disorder spend more time with
depressive symptoms than manic or hypomanic
symptoms.
About half of people during mania can also have
delusions (believing things that aren't true and that they
can't be talked out of) or hallucinations (seeing or
hearing things that aren't there).

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SCHIZOPHRENIA
Schizophrenia is a chronic, severe mental disorder that
affects the way a person thinks, acts, expresses
emotions, perceives reality, and relates to others. Though
schizophrenia isn’t as common as other major mental
illnesses, it can be the most chronic and disabling.
People with schizophrenia often have problems doing well
in society, at work, at school, and in relationships. They
might feel frightened and withdrawn, and could appear to
have lost touch with reality. This lifelong disease can’t be
cured but can be controlled with proper treatment.
Contrary to popular belief, schizophrenia is not a split or
multiple personality.
Schizophrenia involves a psychosis, a type of mental
illness in which a person can’t tell what’s real from what’s
imagined.

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At times, people with psychotic disorders lose touch with
reality.
The world may seem like a jumble of confusing thoughts,
images, and sounds. Their behavior may be very strange
and even shocking. A sudden change in personality and
behavior, which happens when people who have it lose
touch with reality, is called a psychotic episode.
How severe schizophrenia is varies from person to
person. Some people have only one psychotic episode,
while others have many episodes during a lifetime but
lead relatively normal lives in between. Still others may
have more trouble functioning over time, with little
improvement between full-blown psychotic
episodes. Schizophrenia symptoms seem to worsen and
improve in cycles known as relapses and remissions.

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TYPES OF SCHIZOPHRENIA
There are five types of schizophrenia (discussed in the
following slides). They are categorized by the types of
symptoms the person exhibits when they are assessed:
Paranoid schizophrenia
Disorganized schizophrenia
Catatonic schizophrenia
Undifferentiated schizophrenia
Residual schizophrenia
PARANOID SCHIZOPHRENIA
Paranoid-type schizophrenia is distinguished by paranoid
behavior, including delusions and auditory hallucinations.
Paranoid behavior is exhibited by feelings of persecution,
of being watched, or sometimes this behavior is
associated with a famous or noteworthy person a
celebrity or politician, or an entity such as a corporation.

15. People with paranoid-type schizophrenia may display
anger, anxiety, and hostility.
The person usually has relatively normal intellectual
functioning and expression of affect.
DISORGANIZED SCHIZOPHRENIA
A person with disorganized-type schizophrenia will exhibit
behaviors that are disorganized or speech that may be
bizarre or difficult to understand. They may display
inappropriate emotions or reactions that do not relate to
the situation at-hand. Daily activities such as hygiene,
eating, and working may be disrupted or neglected by
their disorganized thought patterns.

16. CATATONIC SCHIZOPHRENIA
Disturbances of movement mark catatonic - type
schizophrenia. People with this type of schizophrenia may
vary between extremes: they may remain immobile or
may move all over the place. They may say nothing for
hours, or they may repeat everything you say or do.
These behaviors put these people with catatonic-type
schizophrenia at high risk because they are often unable
to take care of themselves or complete daily activities.

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UNDIFFERENTIATED SCHIZOPHRENIA
Undifferentiated-type schizophrenia is a classification
used when a person exhibits behaviors which fit into two
or more of the other types of schizophrenia, including
symptoms such as delusions, hallucinations, disorganized
speech or behavior, catatonic behavior.
RESIDUAL SCHIZOPHRENIA
When a person has a past history of at least one episode
of schizophrenia, but the currently has no symptoms
(delusions, hallucinations, disorganized speech or
behavior) they are considered to have residual-type
schizophrenia. The person may be in complete remission,
or may at some point resume symptoms.

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CLASSIFICATION OF ANTIPSYCHOTIC DRUG
Typical Antipsychotics
Atypical Antipsychotics

19. PHARMACOLOGICAL CLASSIFICATION
First Generation Antipsychotic (Low Potency)
First Generation Antipsychotic ( High Potency)
Second Generation Antipsychotic

20. MECHANISM ACTION OF
ANTIPSYCHOTIC DRUG
The major action of all
antipsychotics in the nervous system
is to block receptors for the
neurotransmitter dopamine.
The typical antipsychotic drugs 1st
generation are potent antagonists
(blockers) of dopamine receptors
d2,d3 & d4.
This makes them effective in
treating target symptoms but also
produces many extra pyramidal side
effect.
The atypical antipsychotic drugs 2nd
generation block both dopaminergic
and serotonergic receptors and
5HT2A receptors
Antipsychotic
Drugs

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FIRST GENERATION OF
ANTIPSYCHOTIC DRUGS

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CHLORPROMAZINE
ACTIONS:- Antipsychotic. Apathy and inertia. Reduced aggression.
Antiemetic
MOA:- Competitive antagonism of dopamine D2 receptors in the
mesolimbic/mesocortical pathways. Clinical benefits are delayed although
receptor block is immediate, suggesting that slower changes in
neurotransmission occur.
ABS/DISTRIB/ELIM:- Given orally or by i.m. injection. t½ 16–32h.
Fluphenazine decanoate available as i.m. depot formulation.
CLINICAL USE:- Schizophrenia (less effective against –ve symptoms)
and other psychotic states. Manic phase of bipolar disorder. Tourette’s
syndrome. Nausea & vomiting. Aggression in children. Persistent hiccups.
ADVERSE EFFECTS:- Marked sedation. EPS (dystonias and
Parkinsonian symptoms) reduced by antimuscarinic action. Endocrine
effects (e.g. galactorrhoea, gynaecomastia, weight gain). Antimuscarinic
effects (e.g constipation, dry mouth). Hypotension (-adrenoceptor
antagonism). Rare, but serious, neuroleptic malignant syndrome.
Hypersensitivity reactions. Agranulocytosis. Hepatotoxicity.

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HALOPERIDOL
ACTIONS:- Antipsychotic. Apathy. Reduced aggression. Antiemetic
MOA:- Competitive antagonism of dopamine D2 receptors in the
mesolimbic/mesocortical pathways. Clinical benefits are delayed
although receptor block is immediate, suggesting that more
complex changes in neurotransmission occur. Higher potency
compared to chlorpromazine.
ABS/DISTRIB/ELIM :- Oral or i.m. admin. (Also i.m. depot.) t½
12–36h.
CLINICAL USE:- Schizophrenia (less e•ffective against negative
symptoms) and other psychotic states. Mania. Aggressive
behaviour. Tourette’s syndrome. Nausea & vomiting. Persistent
hiccup.
ADVERSE EFFECTS :- Marked EPS. Hyperprolactinaemia. Little
sedative, hypotensive or antimuscarinic actions. Neuroleptic
malignant syndrome.

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FLUPENAZINE
ACTIONS:- Antipsychotic. Antidepressant (tricyclic-like)
activity.
MOA:- Competitive antagonism of dopamine D2
receptors in the mesolimbic/mesocortical pathways.
Clinical benefits are delayed although receptor block is
immediate, suggesting that more complex changes in
neurotransmission occur.
ABS/DISTRIB/ELIM:- Effective orally but most often
used as i.m. depot formulation. T0.5 19–39h.
CLINICAL USE:- Schizophrenia and other psychotic
states. Bipolar disorder. Depression.
ADVERSE EFFECTS:- EPS. Hyperprolactinaemia.
Neuroleptic malignant syndrome.

27. Extrapyramidal side effects (EPS), commonly referred to
as drug-induced movement disorders are among the
most common adverse drug effects patients experience
from dopamine-receptor blocking agents.
EXTRA PYRAMIDAL SYMPTOMS (EPS)

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SECOND GENERATION OF
ANTIPSYCHOTIC DRUGS

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CLOZAPINE
ACTIONS:- Antipsychotic – effective against +ve and -ve
symptoms.
MOA:- MOA less well established than for typical agents. Action
on 5HT2A receptors may be important. Antagonist action at
muscarinic, 5HT2, 1 adrenoceptors, and H1 histamine receptors.
Higher affinity for D4 than other dopamine receptors.
ABS/DISTRIB/ELIM:- Orally active. t½ 12h.
CLINICAL USE:- Schizophrenia. Because of toxicity, used
mainly in patients resistant to other drugs, for whom it is very
effective.
ADVERSE EFFECTS :- Little EPS (reduced D2 antagonism
coupled with antimuscarinic action). Antimuscarinic actions (e.g.
constipation). Agranulocytosis (not with olanzapine) – blood
testing needed. Sedation. Epileptic seizures. Weight gain (more
than with other antipsychotics). Hyperglycaemia.

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RISPERIDONE
ACTIONS:- Antipsychotic. Effective against +ve and -ve
symptoms of schizophrenia.
MOA:- Potent antagonist of D2 and 5HT2A receptors and 1
adrenoceptors. As for other atypical agents, a combination of
D2 and 5HT2A antagonism may be important in modifying
activity in the mesolimbic and mesocortical pathways.
ABS/DISTRIB/ELIM:- Oral and i.m. depot admin. Hepatic
P450 metabolism. t½ 3–20h. Active metabolite is longer
acting.
CLINICAL USE:- Schizophrenia and other psychotic states.
Manic phase of bipolar disorder.
ADVERSE EFFECTS:- EPS (more than with other atypicals).
Insomnia and sedation. Anxiety. Hyperprolactinaemia. Weight
gain. Hypotension.

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QUETIAPINE
ACTIONS:- Antipsychotic. Effective against +ve and -ve
symptoms.
MOA:- Competitive antagonism of dopamine D2 and
5HT2A receptors in the mesolimbic/mesocortical
pathways is likely to be important. Antagonism of
histamine H1 receptors may underlie sedative action.
ABS/DISTRIB/ELIM:- Oral admin. Short (6h) half-life.
CLINICAL USE:- Schizophrenia and other psychotic
states. Bipolar disorder.
ADVERSE EFFECTS :- Weight gain. Minor EPS and
hyperprolactinaemia, Sedation, Postural hypotension,
Constipation, dry mouth (antimuscarinic actions), Rarely,
neuroleptic malignant syndrome.

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ARIPIPRAZOLE
ACTIONS:- Antipsychotic. Effective against +ve and -ve
symptoms
MOA:- Modication of dopaminergic transmission in the
mesolimbic/mesocortical pathways. Aripiprazole binds
strongly to dopamine D2 receptors but has partial agonist
activity which may explain its low incidence of EPS. 5HT2A
antagonism is probably important.
ABS/DISTRIB/ELIM:- Oral admin. Long (75h) half-life.
CLINICAL USE:- Schizophrenia and other psychotic states.
Manic phase of bipolar disorder.
ADVERSE EFFECTS:- Fewer side effects than many other
antipsychotics (e.g. minor EPS (some akathisia), less weight
gain, less antimuscarinic, less prolactin secretion). Some
hypotension and nausea & vomiting.

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AMISULPRIDE
ACTIONS: Antipsychotic. Effective against +ve and -ve
symptoms of schizophrenia.
MOA: Dopamine D2 and D3 receptor antagonist.
Preferential action on dopamine auto receptors may
explain lower incidence of EPS and effectiveness against
-ve symptoms. Low affinity for 5HT, histamine,
muscarinic and 1 adrenergic receptors.
ABS/DISTRIB/ELIM: Mostly excreted unchanged in
kidney. t½ 12h.
CLINICAL USE:- Schizophrenia.
ADVERSE EFFECTS: Hyperprolactinaemia. Insomnia.
Anxiety. Weight gain. Constipation and dry mouth.

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