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GENERIC NAME BRAND INDICATIONS MOA

NAME
Aripiprazole Abilify used to treat the Aripiprazole is a partial
symptoms of agonist at D2 receptors. It
schizophrenia, bipolar I may act as an
disorder (manic antipsychotic by:
depression), and major Lowering dopaminergic
depressive disorder. neurotransmission in the
Abilify may be used mesolimbic pathway.
alone or with other Enhancing dopaminergic
medications. Abilify is an activity in the
antipsychotic, antimanic mesocortical pathway.
agent.
Asenapine Saphris treat the symptoms of The exact mechanism of
schizophrenia (a mental action is unknown.
illness that causes However, it has been
disturbed or unusual suggested that the efficacy
thinking, loss of interest of asenapine in
in life, and strong or schizophrenia is mediated
inappropriate emotions). through a combination of
antagonist activity at D2
and 5-HT2A receptors.
Brexpiprazole Rexulti As an adjunctive The mechanism of action
treatment of major of brexpiprazole is
depressive disorder unknown. However, the
(MDD) and for treatment efficacy of brexpiprazole
of schizophrenia. may be mediated through
a combination of partial
agonist activity at
serotonin 5-HT1A and
dopamine D2 receptors,
and antagonist activity at
serotonin 5-HT2A
receptors. The binding
affinity of brexpiprazole
was determined in vitro in
cells overexpressing
human receptors and is
expressed as an nM
concentration with lower
values representing higher
affinity.
Cariprazine Vraylar Indicated for acute cariprazine binds to D3
treatment of manic or dopamine, D2 dopamine,
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mixed episodes and 5HT2B serotonin

associated with bipolar I receptors with high
disorde). potency, and to 5HT1A
serotonin and 5HT2A
serotonin receptors with
moderate potency
Chlorpromazine Thorazine used to treat certain Chlorpromazine belongs
mental/mood disorders to the category of typical
(such as schizophrenia, antipsychotics or
psychotic disorders, neuroleptics, also known
manic phase of bipolar as first-generation
disorder, severe antipsychotics (FGAs). It
behavioral problems in produces its antipsychotic
children effect by the post-synaptic
blockade at the D2
receptors in the
mesolimbic pathway.
However, the blockade of
D2 receptors in the
nigrostriatal pathway is
responsible for its
extrapyramidal side
effects.
Clozapine Clozaril indicated for the The mechanism by which
treatment of severely ill clozapine exerts its effects
patients with involves the blocking of 5-
schizophrenia who fail to HT2A/5-HT2C serotonin
respond adequately to receptors and the D1-4
standard antipsychotic dopamine receptors, with
treatment. the highest affinity for the
D4 dopamine receptor.
Divalproex Depakote indicated for the exerts its effects by
treatment of the manic increasing the
episodes associated with concentration of gamma-
bipolar disorder. A manic aminobutyric acid (GABA)
episode is a distinct in the brain. GABA is a
period of abnormally and neurotransmitter, a
persistently elevated, chemical that nerves use
expansive, or irritable to communicate with one
mood. another.
Fluphenazine Prolixin indicated in the Fluphenazine exerts its
management of actions by blocking
manifestations of postsynaptic dopamine D2
psychotic disorders. receptors in the limbic,
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cortical system and basal

ganglia. This prevents the
actions of dopamine,
thereby reducing the
hallucinations and
delusions that are
associated with
schizophrenia.
Haloperidol Haldol indicated for the exerts its antipsychotic
treatment of patients action by blocking
with schizophrenia dopamine D2 receptors in
the brain. When 72% of
dopamine receptors are
blocked, this drug
achieves its maximal
effect.
Haloperidol ester Haldol HALDOL Decanoate is haloperidol competitively
Decanoate indicated for the blocks post-synaptic
maintenance treatment dopamine (D2) receptors
of schizophrenia and in the brain, eliminating
schizoaffective disorder dopamine
in adult patients neurotransmission and
currently stabilised with leading to the relief of
oral haloperidol delusions and
hallucinations that are
commonly associated with
psychosis. It acts primarily
on the D2-receptors and
has some effect on 5-HT2
and α1-receptors, with
negligible effects on
dopamine D1-receptors.
Iloperidone Fanapt indicated for the Ilooperidone also binds
treatment of adults with with high affinity to
schizophrenia. Efficacy serotonin 5-HT2a and
was established in two dopamine 3 receptors.
short-term (4- and 6- Iloperidone binds with
week) placebo- and moderate affinity to
active-controlled studies dopamine D4, serotonin 5-
of adult patients with HT6 and 5-HT7, and
schizophrenia. norepinephrine NEα1
receptors
Loxapine Adasuve indicated for the acute exact mode of action of
treatment of agitation Loxapine has not been
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associated
with schizophrenia or
bipolar I disorder in
adults. To alleviate the
risk of bronchospasm,
Adasuve may be
administered only to
patients in a health care
facility enrolled in the
Adasuve Risk Evaulation
and Mitigation Strategy
(REMS) program.
Lurasidone Latuda second-generation
antipsychotic approved
for the treatment of
schizophrenia and
depressive episodes
associated with bipolar
disorder.
Molindone Moban Molindone is used to
treat certain
mental/mood disorders
(such as schizophrenia).
This medicine helps you
to think more clearly,
feel less nervous, and
take part in everyday life.
Olanzapine Zyprexa used to treat certain
mental/mood conditions
(such as schizophrenia,
bipolar disorder). It may
also be used in
combination with other
medication to treat
depression. This
medication can help to
decrease hallucinations
and help you to think
more clearly and
positively about yourself,
feel less agitated, and
take a more active part
established, however
changes in the level of
excitability of subcortical
inhibitory areas have been
observed in several animal
species in association with
such manifestations of
tranquilization as calming
effects and suppression of
aggressive behavior.
It may work by blocking
receptors for several
neurotransmitters
(chemicals that nerves use
to communicate with each
other) in the brain. It
binds to dopamine and
serotonin type 2 (5-HT2)
receptors.
act by occupying
(antagonizing) dopamine
(D2) receptor sites in the
reticular limbic systems in
the brain, thus decreasing
dopamine activity.
The activity of olanzapine
is achieved by the
antagonism of multiple
neuronal receptors
including the dopamine
receptor D1, D2, D3 and
D4 in the brain, the
serotonin receptors
5HT2A, 5HT2C, 5HT3 and
5HT6, the alpha-1
adrenergic receptor, the
histamine receptor H1 and
multiple muscarinic
receptors.its antagonistic
effect towards the
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in everyday life. dopamine D2 receptor in

the mesolimbic pathway is
key as it blocks dopamine
from having a potential
action at the post-synaptic
receptor. The binding of
olanzapine to the
dopamine D2 receptors is
easily dissociable
Paliperidone Invega indicated for the mechanism of action, like
treatment of all other atypical agents, is
schizoaffective disorder attributed to the
as monotherapy and an antagonism of brain
adjunct to mood dopamine D2 and
stabilizers and/or serotonin 5-HT2A
antidepressant therapy receptors
Perphenazine Trilafon indicated for use in the Perphenazine blocks
treatment postsynaptic dopamine
of schizophrenia and for 2(D2) receptors in the
the control of mesolimbic and medullary
severe nausea and vomi chemoreceptor trigger
ting in adults.  zone (CTZ), thereby
preventing the excess of
dopamine in the brain.
This leads to reduction in
psychotic symptoms, such
as hallucinations and
delusions.
Pimavansentrin Nuplazid indicated for the It is possible that
treatment of pimavanserin acts via
hallucinations and inverse agonist and
delusions associated antagonist activity at
with Parkinson's disease serotonin 5-HT2A
psychosis receptors with limited
effects on serotonin 5-
HT2C receptors.
Pimavanserin is an inverse
agonist and antagonist of
serotonin 5-HT2A
receptors with high
binding affinity,
demonstrating low
binding affinity to
serotonin 5-HT2C
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receptors
Pimozide Orap indicated for the Pimozide selectively
suppression of motor inhibits type 2
and phonic tics in dopaminergic receptors in
patients with Tourette's the central nervous
Disorder who have failed system (CNS), thereby
to respond satisfactorily decreasing dopamine
to standard treatment. neurotransmission and
reducing the occurrence
of motor and vocal tics
and delusions of
parasitosis. In addition,
this agent antagonizes
alpha-adrenergic and 5-
HT2 receptors.
Porchloroperazine Compazine indicated in vertigo due prochlorperazine mainly
to Meniere's syndrome, blocks D2 dopamine
labyrinthitis and other receptors in the brain. It
causes, and for nausea can also block
and vomiting from any histaminergic, cholinergic,
cause including that and noradrenergic
associated with migraine. receptors.
It may also be used for
schizophrenia (especially
in the chronic stage),
acute mania and as an
adjunct to the short term
management of anxiety.
Quetiapine Seroquel For schizophrenia, acute The mechanism of action
manic episodes, and of SEROQUEL, as with
adjunctive treatment for other drugs having
major depressive efficacy in the treatment
disorder. of schizophrenia and
acute manic episodes
associated with bipolar
disorder, is unknown.
However, it has been
proposed that this drug=s
efficacy in schizophrenia is
mediated through a
combination of dopamine
type 2 (D2) and serotonin
type 2 (5HT2) antagonism.
Antagonism at receptors
[Type here]

other than dopamine and

5HT2 with similar receptor
affinities may explain
some of the
other effects of SEROQUEL
Resperidone Risperdal Used to treat the mechanism of action of
symptoms of risperidone might involve
schizophrenia, bipolar a reduction of
mania, bipolar disorder dopaminergic
and irritability. neurotransmission in the
mesolimbic pathway
Thioridazine Mellaril indicated for the blocks DA-2 receptors in
management of the mesolimbic pathway,
schizophrenic patients diminishing positive
who fail to respond symptoms
adequately to treatment
with other antipsychotic
drugs.
Thiothixene Navane For the management of Blocks postsynaptic
schizophrenia. dopamine receptors in the
mesolimbic system and
medullary chemoreceptor
trigger zone, thereby
decreasing dopamine
activity leading to
decreased stimulation of
the vomiting center and
psychotic effects, such as
hallucinations and
delusions.
Trifluoperazine Stelazine used to treat certain exerts its antipsychotic
mental/mood disorders effect by blocking central
(such as schizophrenia, dopamine receptors,
psychotic disorders). thereby preventing effects
Trifluoperazine helps you such as delusions and
to think more clearly, hallucinations caused by
feel less nervous, and an excess of dopamine.
take part in everyday life.
It can reduce aggressive
behavior and the desire
to hurt yourself/others.
Valproic acid Depakene indicated as Valproic acid exhibits its
monotherapy and pharmacologic effects in a
[Type here]

adjunctive therapy in the couple of ways, such as by

treatment of patients acting on GABA (γ
with aminobutyric acid) levels
complex partial seizures in the CNS, blocking
that occur either in voltage-gated ion
isolation or in association channels, and also by
with other types of inhibiting histone
seizures. deacetylase
Ziprasidone Geodon indicated for the Ziprasidone binds to
treatment of serotonin-2A (5-HT2A) and
schizophrenia, as dopamine D2 receptors in
monotherapy for the a similar fashion to other
acute treatment of atypical antipsychotics;
bipolar manic or mixed however, one key
episodes, and as an difference is that
adjunct to lithium or ziprasidone has a higher 5-
valproate for the HT2A/D2 receptor affinity
maintenance treatment ratio when compared to
of bipolar disorder. other antipsychotics such
as olanzapine, quetiapine,
risperidone, and
aripiprazole.

RECEPTORS RECEPTOR FUNCTION

5-HT RECEPTOR 5-HT receptors are G-protein-coupled receptors
that exert their effects through Gi/Go proteins
inhibiting adenylyl cyclase as well as other second
messenger cascades. They mediate both
excitatory and inhibitory neurotransmission. 5-HT
receptors are clearly main players in various
physiologic and pathophysiologic situations
either directly or indirectly following long-term
effects of selective serotonin or noradrenalin
reuptake inhibitors on their transporters
D2 RECEPTOR D2 receptors are G-protein coupled
receptors/caption GPRCS are made up of seven
membrane spanning segments whereby the
amino (N) terminal is extracellular and the
carboxyl (C) terminal is intracellular. Dopamine
receptors are target of action for drugs used to
treat schizophrenia and Parkinson’s disease in
addition to other disorders such as substance
abuse, depression, Tourette’s syndrome and
[Type here]

attention deficit hyperactivity disorder (ADHD).

MUSCARINIC RECEPTOR Muscarinic receptors have been implicated in the

regulation of cognition and psychosis based on
pharmacological evidence from pre-clinical and
clinical studies. Muscarinic agonists have shown
promise in the clinic in improving cognition and
reducing psychotic episodes in Alzheimer's
patients.
HISTAMINE RECEPTOR H1R is the main target of most of the approved
drugs and is found in different tissues and cells,
including the smooth muscle, brain, and
lymphocytes. This receptor is the only member of
the family of histamine receptors, of which a co-
crystal was obtained, by using the first-
generation antagonist doxepin (PDB ID
Histamine receptors are 7-transmembrane
receptors which mediate cellular responses to
the biogenic amine histamine. Histamine may be
released as a transmitter in neuronal
preparations or as a mediator of an inflammatory
response by mast cells.

In terms of the brain, H1, H2, H3 receptors play

clear roles in neuronal function, post- and pre-
synaptically, and, interestingly, the H4R appears
to influence neuronal function indirectly through
modulating activated microglia.

GABA RECEPTOR Gamma-aminobutyric acid, or GABA, is a

neurotransmitter that sends chemical messages
through the brain and the nervous system, and is
involved in regulating communication between
brain cells. The role of GABA is to inhibit or
reduce the activity of the neurons or nerve cells.
GABA plays an important role in behavior,
cognition, and the body's response to stress.

ADRENERGIC a1 α-Adrenergic receptor function was assessed in

platelets from drug-free schizophrenic patients
and control subjects.

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