Antipsychotics Drug; Uses, Side Effects, Drug Interactions

Antipsychotics drug
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Antipsychotics drug also known as neuroleptics or major tranquilizers, are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder. They are increasingly being used in the management of non-psychotic disorders. Antipsychotics are usually effective in relieving symptoms of psychosis in the short term.

The long-term use of antipsychotics is associated with side effects such as involuntary movement disorders, gynecomastia, and metabolic syndrome. They are also associated with increased mortality in elderly people with dementia.

Classification of Antipsychotics Drug

Generic nameBrand namesChemical classATC code
typical antipsychotics
AcepromazineAtravet, AcezinephenothiazineN05AA04
AcetophenazineTindalphenothiazineN05AB07
BenperidolFrenactylbutyrophenoneN05AD07
BromperidolBromidol, BromodolbutyrophenoneN05AD06
ButaperazineRepoise, TyrylenphenothiazineN05AB09
Carfenazinephenothiazine
ChlorproethazinephenothiazineN05AA07
ChlorpromazineLargactil, ThorazinephenothiazineN05AA01
ChlorprothixeneCloxan, Taractan, TruxalthioxantheneN05AF03
ClopenthixolSordinolthioxantheneN05AF02
CyamemazineTercianphenothiazineN05AA06
DixyrazineEsucosphenothiazineN05AB01
DroperidolDroleptan, Dridol, Inapsine, Xomolix, Innovar (+ Fentanyl)phenylbutylamine (butyrophenone)N05AD08
FluanisonebutyrophenoneN05AD09
FlupentixolDepixol, FluanxolthioxantheneN05AF01
FluphenazineProlixin, ModecatephenothiazineN05AB02
FluspirileneRedeptin, ImapdiphenylbutylpiperidineN05AG01
HaloperidolHaldolphenyl-piperidinyl-butyrophenoneN05AD01
LevomepromazineNosinan, Nozinan, LevopromephenothiazineN05AA02
LenperoneElanone-Vbutyrophenone
LoxapineLoxapac, LoxitanedibenzoxazepineN05AH01
MesoridazineSerentilphenothiazineN05AC03
Metitepinetricylic dibenzodiazepine
MolindoneMobanindole derivativeN05AE02
MoperoneLuvatrenbutyrophenoneN05AD04
OxypertineEquipertine, Forit, Integrin, Lanturil, Lotawin, OpertilphenylpiperazineN05AE01
OxyprotepineModiten (Czech republic)dibenzothiepine
PenfluridolSemap, Micefal, LongoperidoldiphenylbutylpiperidineN05AG03
PerazineTaxilanphenothiazineN05AB10
PericiazineNeuleptil, NeulactilphenothiazineN05AC01
PerphenazineTrilafonphenothiazineN05AB03
PimozideOrapdiphenylbutylpiperidineN05AG02
PipamperoneDipiperon, Dipiperal, Piperonil, Piperonyl, PropitanbutyrophenoneN05AD05
PiperacetazineQuidephenothiazine
PipotiazinePiportilphenothiazineN05AC04
ProchlorperazineCompazine, Stemzine, Buccastem, Stemetil, PhenotilphenothiazineN05AB04
PromazineSparinephenothiazineN05AA03
ProthipendylphenothiazinesN05AX07
SpiperoneSpiroperidol, Spiropitanbutyrophenone
SulforidazineImagotan, Psychoson, Inofalphenothiazine
ThiopropazateArtalan, Dartal, Dartalan, DartanphenothiazineN05AB05
ThioproperazineMajeptilphenothiazineN05AB08
ThioridazineMellaril, MellerilphenothiazineN05AC02
ThiothixeneNavanethioxantheneN05AF04
Timiperonebutyrophenone
TrifluoperazineStelazinephenothiazineN05AB06
TrifluperidolbutyrophenoneN05AD02
TriflupromazineVesprinphenothiazineN05AA05
ZuclopenthixolClopixolthioxantheneN05AF05
atypical antipsychotics
AmoxapineAsendin, Asendis, Defanyl, DemoloxdibenzoxazepineN06AA17
AmisulprideAmazeo, Amipride, Amival, Solian, Soltus, Sulpitac, Sulprixsubstituted benzamidesN05AL05
AripiprazoleAbilifyquinoloneN05AX12
AsenapineSaphrisdibenzo-oxepino pyrroleN05AH05
BlonanserinLonasen
BrexpiprazoleRexultiquinoloneN05AX16
CariprazineVraylarN05AX15
CarpipraminePrazinil, Defekton
ClocapramineClofekton, Padrasenimidobenzyl
ClorotepineClotepin, Clopibentricylic dibenzodiazepine
ClotiapineEntumineN05AH06
ClozapineClozariltricylic dibenzodiazepineN05AH02
IloperidoneFanaptbenzisoxazoleN05AX14
LevosulpiridebenzamideN05AL07
LurasidoneLatudan-arylpiperazine (piperazine)N05AE05
MelperoneBunil, Buronil, EunerpanbutyrophenoneN05AD03
MosapramineCreminN05AX10
NemonaprideEmilacebenzamide
OlanzapineZyprexa, Ozace, Lanzek, ZypadherathienobenzodiazepineN05AH03
PaliperidoneInvegapyridopyrimidineN05AX13
PerospironeLullanazapirone
QuetiapineSeroqueldibenzothiazepineN05AH04
RemoxiprideRoxiamsalicylamideN05AL04
ReserpineRaudixin, Serpalan, Serpasilyohimbine alkaloidC02AA02
RisperidoneRisperdal, ZepidonepyridopyrimidineN05AX08
SertindoleSerdolectphenylpyrroleN05AE03
SulpirideSulpirid, Eglonylbenzenesulfonamide (benzamide)N05AL01
SultoprideBarnetil, Barnotil, TopralbenzamideN05AL02
TiaprideEquilium, TiapridalbenzamideN05AL03
VeraliprideAgreal, AgradilbenzamideN05AL06
ZiprasidoneGeodon, Zeldoxn-arylpiperazine (piperazine)N05AE04
ZotepineNipolepttricylic dibenzodiazepineN05AX11
under development
perphenazine gamma-aminobutyrateBL-1020
PimavanserinACP-103
F-15063
ITI-007tetracyclic quinoxaline
Lu AF35700
RP5063
Stepholidineberberine
development abandoned
AmperozidediphenylbutylpiperazineQN05AX90
BifeprunoxDU-127,090biphenyl derivative
ButaclamolAY-23,028
CiclindoleWIN-27,147-2
ClopimozideR-29,764diphenylbutylpiperidine
ElopiprazoleDU-29894phenylpiperazine
Flucindole
FluotracenSKF-28,175
FluperlapineNB 106-689tricyclic
GevotrolineWY-47,384tricylic dibenzodiazepine
NaranolW-5494A
N-desmethylclozapineACP-104
OcaperidoneR 79598benzisoxazole
PiquindoneRo 22-1319tricyclic
PomaglumetadLY2140023
TiospironeBMY-13,859azapirone
UmespironeKC-9172azapirone
VabicaserinSCA-136
VolinanserinMDL-100,907
ZetidolineDL 308-IT
ZicronapineLu 31-130
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First-generation (typical)

Butyrophenones

  • Benperidol
  • Bromperidol
  • Droperidol
  • Haloperidol
  • Moperone
  • Pipamperone
  • Timiperone

Diphenylbutylpiperidines

  • Fluspirilene
  • Penfluridol
  • Pimozide

Phenothiazines

  • Acepromazine — although it is mostly used in veterinary medicine.
  • Chlorpromazine
  • Cyamemazine
  • Dixyrazine
  • Fluphenazine
  • Levomepromazine
  • Mesoridazine
  • Perazine
  • Pericyazine
  • Perphenazine
  • Pipotiazine
  • Prochlorperazine
  • Promazine (discontinued))
  • Promethazine
  • Prothipendyl
  • Thioproperazine(only English-speaking country it is available in is Canada)
  • Thioridazine (discontinued)
  • Trifluoperazine
  • Triflupromazine (discontinued))

Thioxanthenes

  • Chlorprothixene
  • Clopenthixol
  • Flupentixol
  • Thiothixene
  • Zuclopenthixol

Disputed/unknown

This category is for drugs that have been called both first and second-generation, depending on the literature being used.

Benzamides

  • Sulpiride
  • Sultopride
  • Veralipride

Tricyclics

  • Carpipramine
  • Clocapramine
  • Clorotepine
  • Clotiapine
  • Loxapine
  • Mosapramine

Others

  • Molindone

Second-generation (atypical)

Benzamides

  • Amisulpride  Selective dopamine antagonist. Higher doses (greater than 400 mg) act upon post-synaptic dopamine receptors resulting in a reduction in the positive symptoms of schizophrenia, such as psychosis. Lower doses, however, act upon dopamine autoreceptors, resulting in increased dopamine transmission, improving the negative symptoms of schizophrenia. Lower doses of amisulpride have also been shown to have antidepressant and anxiolytic effects in non-schizophrenic patients, leading to its use in dysthymia and social phobias.
  • Nemonapride – Used in Japan.
  • Remoxipride – Has a risk of causing aplastic anemia and, hence, has been withdrawn from the market worldwide. It has also been found to possess relatively low (virtually absent) potential to induce hyperprolactinemia and extrapyramidal symptoms, likely attributable to its comparatively weak binding to (and, hence, rapid dissociation from) the D2 receptor.
  • Sultopride – An atypical antipsychotic of the benzamide chemical class used in Europe, Japan, and Hong Kong for the treatment of schizophrenia. It was launched by Sanofi-Aventis in 1976. Sultopride acts as a selective D2 and D3 receptor antagonist.

Benzisoxazoles/benzisothiazoles

  • Iloperidone – Approved by the US FDA in 2009, it is fairly well tolerated, although hypotension, dizziness, and somnolence were very common side effects. Has not received regulatory approval in other countries, however.
  • Lurasidone – Approved by the US FDA for schizophrenia and bipolar depression. Given once daily, it has shown mixed Phase III efficacy results but has a relatively well-tolerated side effect profile. It is also licensed for use as schizophrenia treatment in Canada. Not yet licensed elsewhere, however. Has procognitive effects via its antagonism of the 5-HT7 receptor.
  • Paliperidone – Primary Metabolite of risperidone that was approved in 2006.
  • Paliperidone palmitate – Long-acting version of paliperidone for once-monthly injection.
  • Perospirone  – Has a higher incidence of extrapyramidal side effects than other atypical antipsychotics.
  • Risperidone – Divided dosing is recommended until initial titration is completed, at which time the drug can be administered once daily. Used off-label to treat Tourette syndrome and anxiety disorder.
  • Ziprasidone – Approved in 2004 to treat bipolar disorder. Side-effects include a prolonged QT interval in the heart, which can be dangerous for patients with heart disease or those taking other drugs that prolong the QT interval.

Butyrophenones

  • Melperone – Only used in a few European countries. No English-speaking country has licensed it to date.
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Phenylpiperazines/quinolinones

  • Aripiprazole – partial agonist at the D2 receptor, unlike almost all other clinically-utilized antipsychotics.
  • Aripiprazole lauroxil – Long-acting version of aripiprazole for injection.
  • Brexpiprazole – Partial agonist of the D2 receptor. The successor of aripiprazole.
  • Cariprazine – A D3-preferring D2/D3 partial agonist.

Tricyclics

  • Asenapine – Used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
  • Clozapine – Requires complete blood counts every one to four weeks due to the risk of agranulocytosis. It has unparalleled efficacy in the treatment of treatment-resistant schizophrenia.
  • Olanzapine – Used to treat psychotic disorders including schizophrenia, acute manic episodes, and maintenance of the bipolar disorder. Used as an adjunct to antidepressant therapy, especially to fluoxetine treatment in the form of Symbyax.
  • Quetiapine – Used primarily to treat bipolar disorder and schizophrenia. Also used and licensed in a few countries (including Australia, the United Kingdom, and the United States) as an adjunct to antidepressant therapy in patients with major depressive disorder. It’s the only antipsychotic that’s demonstrated efficacy as a monotherapy for the treatment of the major depressive disorder. It indirectly serves as a norepinephrine reuptake inhibitor by means of its active metabolite, no quetiapine.
  • Zotepine – An atypical antipsychotic indicated for acute and chronic schizophrenia. It is still used in Japan and was once used in Germany but it was discontinued.

Others

  • Blonanserin – Approved by the PMDA in 2008. Used in Japan and South Korea.
  • Pimavanserin – A selective 5-HT2A receptor antagonist approved for the treatment of Parkinson’s disease psychosis in 2016.
  • Sertindole  – Developed by the Danish pharmaceutical company H. Lundbeck. Like the other atypical antipsychotics, it is believed to have antagonist activity at dopamine and serotonin receptors in the brain.

Mechanism of Action of Antipsychotics Drug

Antipsychotic drugs such as haloperidol and chlorpromazine tend to block dopamine D2 receptors in the dopaminergic pathways of the brain. This means that dopamine released in these pathways has less effect. Excess release of dopamine in the mesolimbic pathway has been linked to psychotic experiences. Decreased dopamine release in the prefrontal cortex and excess dopamine release in another pathway are associated with psychotic episodes in schizophrenia and bipolar disorder. In addition to the antagonistic effects of dopamine, antipsychotics (in particular atypical neuroleptics) also antagonize 5-HT2A receptors. Different alleles of the 5-HT2A receptor have been associated with schizophrenia and other psychoses, including depression. Higher concentrations of 5-HT2A receptors in cortical and subcortical areas, in particular in the right caudate nucleus have been historically recorded. This is the same receptor that psychedelic drugs agonize to various degrees, which explains the correlation between psychedelic drugs and schizophrenia.

Typical antipsychotics are not particularly selective and also block dopamine receptors in the mesocortical pathway, tuberoinfundibular pathway, and the nigrostriatal pathway. Blocking D2 receptors in these other pathways is thought to produce some.

Atypical antipsychotic drugs have a similar blocking effect on D2 receptors, however, most also act on serotonin receptors, especially 5-HT2A and 5-HT2C receptors. Both clozapine and quetiapine appear to bind just long enough to elicit antipsychotic effects but not long enough to induce extrapyramidal side effects and prolactin hypersecretion.5-HT2A antagonism increases dopaminergic activity in the nigrostriatal pathway, leading to a lowered extrapyramidal side effect liability among the atypical antipsychotics

Indications of Antipsychotics Drug

  • Schizophrenia
  • The schizoaffective disorder most commonly in conjunction with either an antidepressant (in the case of the depressive subtype) or a mood stabilizer (in the case of the bipolar subtype).
  • Bipolar disorder (acute mania and mixed episodes) may be treated with either typical or atypical antipsychotics, although atypical antipsychotics are usually preferred because they tend to have more favorable adverse effect profiles and, according to a recent meta-analysis, they tend to have a lower liability for causing the conversion from mania to depression.
  • Psychotic depression – In this indication, it is a common practice for the psychiatrist to prescribe a combination of an atypical antipsychotic and an antidepressant as this practice is best supported by the evidence.
  • Treatment-resistant – (and not necessarily psychotic) major depression as an adjunct to standard antidepressant therapy
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Contra-Indications of Antipsychotics Drug

  • The high amount of ammonium in the blood
  • Porphyria
  • Having thoughts of suicide
  • Alcohol Intoxication
  • drug abuse
  • Depression
  • Unconsciousness resulting from liver cell deterioration
  • Severe liver disease
  • Temporarily stops breathing while sleeping
  • Pregnancy
  • Poisoning by drug

Side Effects of Antipsychotics Drug

The most common

 Common

Rare/Less common

Drug Interactions of Antipsychotics Drug

Antipsychotic drugs may interact with the following drugs, supplements & may change the efficacy of drugs

References

Antipsychotics drug

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