ANTIPSYCHOTICS

SUBMITTED TO:
MRS. LETICIA D. SERRANO

SUBMITTED BY:
KRISTA ANGELA G. DACANAY
GENERIC NAME BRAND NAME CHEMICAL CLASS MECHANISM OF ACTION

Typical Antipsychotics

Acepromazine Atravet, Acezine phenothiazine Has a general properties similar to those of chlorpromazine. It has relatively weak antipsychotics
activity and is mainly used for the short-term management of agitated or distributed behaviour. It
has also been given to alleviate nausea and vomiting and to relieve intractable hiccup

Acetophenazine Tindal phenothiazine Acetophenazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain;
depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the
reticular activating system thus affecting basal metabolism, body temperature, wakefulness,
vasomotor tone, and emesis.

Benperidol Frenactyl butyrophenone Control of disturbing, socially unacceptable, sexual behaviour that is caused by mental illness.
Benperidol works by blocking a variety of receptors in the brain, particularly dopamine receptors.
Dopamine is a natural compound called a neurotransmitter, and is involved in transmitting
messages between brain cells. Dopamine is a neurotransmitter known to be involved in regulating
mood and behaviour, amongst other things. It is thought that over-stimulation of dopamine
receptors may result in mental illness.

Bromperidol Bromidol, Bromodol butyrophenone Bromperidol has properties similar to those of haloperidol. It is used in the treatment of
schizophrenia and other psychoses

Butaperazine Repoise, Tyrylen phenothiazine Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and
inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally
 active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of
acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance.

Carfenazine phenothiazine A yellow, powdered, phenothiazine antipsychotic agent used in the treatment of acute or chronic
schizophrenia. The term "phenothiazines" is used to describe the largest of the five main classes of
neuroleptic antipsychotic drugs. These drugs have antipsychotic and, often, antiemetic properties,
although they may also cause severe side effects such as akathisia, tardive dyskinesia and
extrapyramidal symptoms. Carphenazine blocks postsynaptic mesolimbic dopaminergic D1 and D2
receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is
believed to depress the reticular activating system thus affecting basal metabolism, body
temperature, wakefulness, vasomotor tone, and emesis.

Chlorpromazine Largactil, Thorazine phenothiazine Chlorpromazine is a neuroleptic that acts by blocking the postsynaptic dopamine receptor in the
mesolimbic dopaminergic system and inhibits the release of hypothalamic and hypophyseal
hormones. It has antiemetic, serotonin-blocking, and weak antihistaminic properties and slight
ganglion-blocking activity.

Chlorprothixene Cloxan, Taractan, Truxal thioxanthene Chlorprothixene blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain;
depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the
reticular activating system thus affecting basal metabolism, body temperature, wakefulness,
vasomotor tone, and emesis.

Clopenthixol Sordinol thioxanthene A drug that binds to but does not activate dopamine receptors, thereby blocking the actions of
dopamine or exogenous agonists.
Cyamemazine Tercian phenothiazine Cyamemazine is a phenothiazine with general properties similar to those of chlorpromazine. It is
used in the management of a variety of psychiatric disorders including anxiety disorders and
aggressive behaviour.

Dixyrazine Esucos phenothiazine

Droperidol Droleptan, Dridol, phenylbutylamine The exact mechanism of action is unknown, however, droperidol causes a CNS depression at
Inapsine, Xomolix, (butyrophenone) subcortical levels of the brain, midbrain, and brainstem reticular formation. It may antagonize the
Innovar (+ Fentanyl) actions of glutamic acid within the extrapyramidal system. It may also inhibit cathecolamine
receptors and the reuptake of neurotransmiters and has strong central antidopaminergic action and
weak central anticholinergic action. It can also produce ganglionic blockade and reduced affective
response. The main actions seem to stem from its potent Dopamine(2) receptor antagonism with
minor antagonistic effects on alpha-1 adrenergic receptors as well

Fluanisone butyrophenone

Flupentixol Depixol, Fluanxol thioxanthene Flupentixol is a thioxanthene antipsychotic that inhibits dopamine-mediated effects by blocking
postsynaptic dopamine receptors in the CNS.

Fluphenazine Prolixin, Modecate phenothiazine Fluphenazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain;
depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the
reticular activating system thus affecting basal metabolism, body temperature, wakefulness,
vasomotor tone, and emesis.
Fluspirilene Redeptin, Imap diphenylbutylpip Fluspirilene is a diphenylbutylpiperidine antipsychotic and has general properties similar to those of
eridine the phenothiazine, chlorpromazine. It is used in the treament of schizophrenia.

Haloperidol Haldol phenyl- Haloperidol inhibits the effects of dopamine and increases its turnover, however, the exact
piperidinyl- mechanism of action is not fully understood Label. Dopamine overactivity can be presynaptic (an
butyrophenone excess of dopamine release from dopamine nerve terminals) or post-synaptic (an increase in the
density of D2 receptors or an increase in post-receptor action). Traditional antipsychotics, such as
haloperidol, bind more tightly than dopamine itself to the dopamine D2 receptor, with dissociation
constants that are lower than that for dopamine

Levomepromazin Nosinan, Nozinan, phenothiazine antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition,
e Levoprome its binding to 5HT2 receptors may also play a role.

Lenperone Elanone-V butyrophenone

Loxapine Loxapac, Loxitane dibenzoxazepine Loxapine is a dopamine antagonist, and also a serotonin 5-HT2 blocker. The exact mode of action
of Loxapine has not been 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.

Mesoridazine Serentil phenothiazine Based upon animal studies, mesoridazine, as with other phenothiazines, acts indirectly on reticular
formation, whereby neuronal activity into reticular formation is reduced without affecting its
intrinsic ability to activate the cerebral cortex. In addition, the phenothiazines exhibit at least part of
their activities through depression of hypothalamic centers. Neurochemically, the phenothiazines
are thought to exert their effects by a central adrenergic blocking action.
Metitepine tricylic Inhibits dihydrofolate reductase. This inhibition prevents the conversion of dihydrofolic acid (DHF)
dibenzodiazepine to tetrahydrofolic acid (THF) in the thymidine synthesis pathway. Trimethoprim acts on bacterial
dihydrofolate reductase with thousands of times the affinity of human dihydrofolate reductase.

Molindone Moban indole derivative The exact mechanism has not been established, however, based on electroencephalogram (EEG)
studies, molindone is thought to act by occupying (antagonizing) dopamine (D2) receptor sites in
the reticular limbic systems in the brain, thus decreasing dopamine activity. Decreased dopamine
activity results in decreased physiological effects normally induced by excessive dopamine
stimulation, such as those typically seen in manifestations of psychotic disorders.

Moperone Luvatren butyrophenone

Oxypertine Equipertine, Forit, phenylpiperazine

Integrin, Lanturil,
Lotawin, Opertil

Oxyprotepine Moditen (Czech republic) dibenzothiepine [

1]

Penfluridol Semap, Micefal, diphenylbutylpip Penfluridol blocks the postsynaptic dopamine receptor in the mesolimbic dopaminergic system and
Longoperidol eridine inhibits the release of hypothalamic and hypophyseal hormones.

Perazine Taxilan phenothiazine

Periciazine Neuleptil, Neulactil phenothiazine Pericyazine, like other phenothiazines, is presumed to act principally in the subcortical areas, by
producing what has been described as a central adrenergic blockade of the alpha adrenergic
receptors as well as antagonism of the D(1) dopamine receptor.

Perphenazine Trilafon phenothiazine Binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of
the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter
receptors in the chemoreceptor trigger zone and vomiting centre. Perphenazine also binds the
alpha andrenergic receptor. This receptor's action is mediated by association with G proteins that
activate a phosphatidylinositol-calcium second messenger system.

Pimozide Orap diphenylbutylpip The ability of pimozide to suppress motor and phonic tics in Tourette's Disorder is thought to be
eridine primarily a function of its dopaminergic blocking activity. Pimozide binds and inhibits the dopamine
D2 receptor in the CNS.

Pipamperone Dipiperon, Dipiperal, butyrophenone This drug is a selective 5-HT2A, D1 and D4 antagonist. SExtrapyramidal adverse effects also appear
Piperonil, Piperonyl, to be limited in pipamperone treatment compared to traditional antipsychotic medications due to
Propitan its high receptor selectivity. Pipamperone has a 15-fold higher affinity for D4 than D2 receptors. It
has been suggested that D4 receptors may play a role in the modulation of GABAergic neuronal
activity by dopamine 5.

Piperacetazine Quide phenothiazine

Pipotiazine Piportil phenothiazine Pipotiazine antagonises postsynaptic mesolimbic dopaminergic receptors in the brain. It depresses
the release of hypothalamic and hypophyseal hormones, hence it is less sedating, has less potential
to potentiate other CNS depressants and may possess a lower propensity to cause hypotension.
Prochlorperazine Compazine, Stemzine, phenothiazine The mechanism of action of prochlorperazine has not been fully determined, but may be primarily
Buccastem, Stemetil, related to its anti-dopaminergic effects. Prochlorperazine blocks the D2 dopamine receptors in the
Phenotil brain, which are somatodendritic autoreceptors. Inhibition of D2 receptor signaling results in the
blockade of postsynaptic dopamine receptors in the mesolimbic system 11 and an increased
dopamine turnover. Nausea and vomiting are proposed to arise from peripheral or central
stimulation of serotonin type 3 (5-HT3) and dopamine type 2 receptors, the predominant receptors
expressed at the chemoreceptor trigger zone (CTZ).6,11 Prochlorperazine exerts antiemetic effects
and was shown to inhibit apomorphine-induced vomiting by blocking D2 dopamine receptors in
the CTZ.

Promazine Sparine phenothiazine Promazine has general properties similar to those of chlorpromazine. It has relatively weak
antipsychotic activity and is mainly used for the short-term management of agitated or disturbed
behavior. It has also been given to alleviate nausea and vomiting and to relieve intractable hiccup.

Prothipendyl phenothiazines An azaphenothiazine derivative, competitively binds to histamine (H1) receptors, resulting in
inhibition of the pharmacological effects of histamines. It also has some sedative, anticholinergic
and antiserotoninergic effects

Spiperone Spiroperidol, Spiropitan butyrophenone

Sulforidazine Imagotan, Psychoson, phenothiazine

Inofal

Thiopropazate Artalan, Dartal, Dartalan, phenothiazine

Dartan
Thioproperazine Majeptil phenothiazine Thioproperazine acts as an antagonist (blocking agent) on different postsysnaptic receptors -on
dopaminergic-receptors (subtypes D1, D2, D3 and D4 - different antipsychotic properties on
productive and unproductive symptoms), on serotonergic-receptors (5-HT1 and 5-HT2, with
anxiolytic, antidepressive and antiaggressive properties as well as an attenuation of extrapypramidal
side-effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation
difficulties), on histaminergic-receptors (H1-receptors, sedation, antiemesis, vertigo, fall in blood
pressure and weight gain), alpha1/alpha2-receptors (antisympathomimetic properties, lowering of
blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as
sexual dysfunction, but may also attenuate pseudoparkinsonism - controversial) and finally on
muscarinic (cholinergic) M1/M2-receptors (causing anticholinergic symptoms like dry mouth,
blurred vision, obstipation, difficulty/inability to urinate, sinus tachycardia, ECG-changes and loss of
memory, but the anticholinergic action may attenuate extrapyramidal side-effects).

Thioridazine Mellaril, Melleril phenothiazine Thioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks
alpha-adrenergic effect, depresses the release of hypothalamic and hypophyseal hormones and is
believed to depress the reticular activating system thus affecting basal metabolism, body
temperature, wakefulness, vasomotor tone, and emesis.

Thiothixene Navane thioxanthene Tiotixene is a thioxanthene antipsychotic. It has general properties similar to those of
chlorpromazine.

Timiperone butyrophenone

Trifluoperazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain;

Trifluoperazine Stelazine phenothiazine depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the
reticular activating system thus affecting basal metabolism, body temperature, wakefulness,
vasomotor tone, and emesis.
Trifluperidol butyrophenone

Triflupromazine Vesprin phenothiazine Triflupromazine is a phenothiazine with general properties similar with chlorpromazine

Zuclopenthixol Clopixol thioxanthene Zuclopenthixol has high affinity for D1 and D2 receptors and α-adrenoreceptors. It also has slight
antihistamine properties and blocks serotonergic properties.

Atypical Antipsychotics

Amoxapine Asendin, Asendis, dibenzoxazepine Amoxapine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT).
Defanyl, Demolox

Amisulpride Amazeo, Amipride, substituted Amisulpride binds selectively to dopamine D(2) and D(3) receptors in the limbic system. Low doses
Amival, Solian, Soltus, benzamides of amisulpride preferentially block presynaptic D(2)/D(3)-dopamine autoreceptors, thereby
Sulpitac, Sulprix enhancing dopaminergic transmission, whereas higher doses block postsynaptic receptors, thus
inhibiting dopaminergic hyperactivity. It may also have 5-ht7 antagonistic effect, useful in
depression treatment.

Aripiprazole Abilify quinolone The antipsychotic action of aripiprazole is likely due to the agonism of D2 and 5-HT1A receptors
though the exact mechanism has not been definedLabel,1. Some adverse effects may be due to
action on other receptors. For example, orthostatic hypotension may be explained by antagonism
of the adrenergic alpha1 receptors.
Asenapine Saphris dibenzo-oxepino
pyrrole
Asenapine is an atypical antipsychotic multireceptor neuroleptic drug which shows strong 5HT2A
(serotonin) and D2 (dopamine) receptor antagonism, which has been shown to enhance dopamine
(DA) and acetylcholine (Ach) efflux in rat brains. Asenapine may improve cognitive function and
negative symptoms in patients with schizophrenia.

Blonanserin Lonasen Blonanserin binds to and inhibits dopamine receptors D2 and D3 as well as the serotonin receptor
5-HT2A with high affinity. Blonanserin has low affinity for other dopamine and serotonin receptors
as well as muscarinic, adrenergic, and histamine receptors. This reduces dopaminergic and
serotonergic neurotransmission which is thought to produce a reduction in positive and negative
symptoms of schizophrenia respectively.

Brexpiprazole Rexulti quinolone Although the mechanism of action of brexpiprazole in the treatment of MDD and schizophrenia is
unclear, the efficacy of brexpiprazole may be attributed to partial agonist activity at serotonin 1A
and dopamine D2 receptors, and antagonist activity at serotonin 2A receptors.

Cariprazine Vraylar The mechanism of action of cariprazine in schizophrenia and bipolar I disorder is unknown.
However, the efficacy of cariprazine could be mediated through a combination of partial agonist
activity at central dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at
serotonin 5-HT2A receptors. Cariprazine forms two major metabolites, desmethyl cariprazine
(DCAR) and didesmethyl cariprazine (DDCAR), that have in vitro receptor binding profiles similar to
the parent drug.

Carpipramine Prazinil, Defekton

Clocapramine Clofekton, Padrasen imidobenzyl is a potent inhibitor of serotonin re-uptake in the brain. Significant antagonism at cholinergic and
α1-receptors. Weak antagonism at dopamine receptors. It has also antidepressant, sedative and
anticholinergic effects.

Clorotepine Clotepin, Clopiben tricylic

dibenzodiazepine

Clotiapine Entumine Clotiapine is a short-acting dibenzothiazepine antipsychotic with general properties similar to those
of phenothiazines.

Clozapine Clozaril tricylic Clozapine is a dibenzodiazepine derivative. It has a weak dopamine receptor-blocking activity at D1,
dibenzodiazepine D2, D3 and D5 but has high affinity to D4. It also possesses α-adrenergic blocking, antimuscarinic,
antihistaminic, antiserotonergic and sedative properties

Iloperidone Fanapt benzisoxazole Iloperidone is a dopamine D2 and 5-HT2A receptor antagonist and acts as a neuroleptic age

Levosulpiride benzamide

Lurasidone Latuda n-arylpiperazine Lurasidone is an atypical antipsychotic that is a D2 and 5-HT2A (mixed serotonin and dopamine
(piperazine) activity) to improve cognition. It is thought that antagonism of serotonin receptors can improve
negative symptoms of psychoses and reduce the extrapyramidal side effects that are often
associated with typical antipsychotics.
Melperone Bunil, Buronil, Eunerpan butyrophenone Melperone demonstrates antagonist activity at D2 dopaminergic and 5HT2A serotonergic
receptors. It has a weak affinity to D2 receptors and possesses less risk of inducing dopamine
receptor supersensitivity after both acute and chronic administration [L3146]. In addition, the ratio
of dopamine D4/D2 occupancy for melperone has been shown to resemble the binding profile of
clozapine

Mosapramine Cremin

Nemonapride Emilace benzamide

Olanzapine Zyprexa, Ozace, Lanzek, thienobenzodiaze Olanzapine is an atypical antipsychotic w/ affinity for serotonin 5-HT2A/2C, dopamine D1-4,
Zypadhera pine histamine H1 and adrenergic α1 receptors. Efficacy is thought to be mediated through combined
antagonism of dopamine and serotonin type 2 receptor sites.

Paliperidone Invega pyridopyrimidine Paliperidone is a benzisoxazole atypical antipsychotic which is a main active metabolite of
risperidone. It is an antagonist at dopamine D2, serotonin (5-HT2A), adrenergic (α1 and α2), and
histamine (H1) receptors

Perospirone Lullan azapirone Antagonism at D2 receptors is believed to relieve the positive symptoms of schizophrenia such as
delusions, hallucinations, and thought disorders. Perospirone targets the mesolimbic patway to
reverse the overactivity of the dopaminergic signalling via D2 receptors. 5-HT2A antagonism is
thought to allevaite the negative symptoms and cognitive impairments of schizophrenia. These
receptors are Gi/Go coupled receptors that lead to decreased neurotransmitter release and
neuronal inhibition when activated, thus play a role in dopamine release regulation. Perospirone
targets these receptors in the nigrostriatal pathway to reduce dopamine release and function. In
 contrast, 5-HT2A receptor antagonism may improve the negative symptoms by enhancing
dopamine and glutamate release in the mesocortical pathway. 5-HT1A receptor activation further
inhibits the release of 5-HT into the synaptic cleft.

Quetiapine Seroquel dibenzothiazepin Quetiapine's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in
e the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors
relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of
schizophrenia.

Remoxipride Roxiam salicylamide Remoxipride acts as an antagonist at the D2 dopamine receptor. It is believed that overactivity of
dopamine systems in the mesolimbic pathway may contribute to the "positive symptoms" of
schizophrenia (such as delusions and hallucinations), whereas problems with dopamine function in
the mesocortical pathway may be responsible for the "negative symptoms", such as avolition, flat
emotional response and alogia. Therefore, by decreasing the levels of dopamine in these pathways,
it is thought that remoxipride is able to reduce the symptoms of schizophrenia, particularily the
"positive symptoms".

Reserpine Raudixin, Serpalan, yohimbine Reserpine's mechanism of action is through inhibition of the ATP/Mg2+ pump responsible for the
Serpasil alkaloid sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The
neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by
monoamine oxidase (MAO) causing a reduction in catecholamines.

Risperidone Risperdal, Zepidone pyridopyrimidine Risperidone is a benzisoxazole atypical antipsychotic w/ mixed serotonin dopamine antagonist
activity that binds to 5-HT2-receptors in the CNS and in the periphery w/ a very high affinity; binds
to dopamine-D2 receptors w/ less affinity.
Sertindole Serdolect phenylpyrrole Sertindole is an antipsychotic drug with affinity for dopamine D2, serotonin 5-HT2A and 5-HT2C,
and alpha1-adrenoreceptors. Preclinical studies suggest that sertindole acts preferentially on limbic
and cortical dopaminergic neurons and clinical trials have confirmed that sertindole is effective at a
low dopamine D2 occupancy level.

Sulpiride Sulpirid, Eglonyl benzenesulfonam In contrast to most other neuroleptics which block both dopamine D1 and D2 receptors, Sulpiride is
ide (benzamide) more selective and acts primarily as a dopamine D2 antagonist. Sulpiride appears to lack effects on
norepinephrine, acetylcholine, serotonin, histamine, or gamma-aminobutyric acid (GABA) receptors.

Sultopride Barnetil, Barnotil, Topral benzamide Sultopride has general properties similar to those of sulpiride. It is a dopamine antagonist and is
used in the emergency management of agitation in patients who are psychotic or aggressive and in
psychoses e.g. schizophrenia. Given as the hydrochloride but doses are expressed in terms of base.
Sultopride hydrochloride 441 mg is equivalent to 400 mg sultopride.

Tiapride Equilium, Tiapridal benzamide Tiapride is an atypical neuroleptic agent with selective dopamine D2-receptor antagonist activity
and has general properties similar to sulpiride. It is unlikely to cause catalepsy and sedation and is
used in the management of behaviour disorders and to treat dyskinesias.

Veralipride Agreal, Agradil benzamide Veralipride is a substituted benzamide antipsychotic with antidopaminergic action. It was used to
reduce frequency and severity of hot flushes associated with menopause, but was withdrawn in
several European countries in 2007 as the risks of veralipride outweigh its benefits.

Ziprasidone Geodon, Zeldox n-arylpiperazine Ziprasidone, a benzylisothiazolylpiperazine is an atypical antipsychotic which may produce
(piperazine) antischizophrenic effect by the antagonism of central dopamine D2 receptors and central type 2
serotonergic (5-HT2) receptors
Zotepine Nipolept tricylic Zotepine is an atypical antipsychotic that is an antagonist at central dopamine (D1 and D2)
dibenzodiazepine receptors. It also binds to serotonin, adrenergic (α1), and histamine (H1) receptors, and inhibits
noradrenaline reuptake.

Under Development

perphenazine BL-1020
gamma-
aminobutyrate

Pimavanserin ACP-103 tetracyclic ACP-103 reduces haloperidol-induced akathisia, a debilitating extrapyramidal side effect (EPS), in
quinoxaline patients with schizophrenia. ACP-103 is a 5-HT2A inverse agonist, to reduce the side effects
F-15063 associated with antipsychotic drug treatment with haloperidol. ACP-103 reduced both the motor
disturbances and hyperprolactinemia, a condition of elevated prolactin secretion, caused by
ITI-007
haloperidol treatment.
Lu AF35700

RP5063

Stepholidine berberine