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 name Brand names Chemical class ATC code
typical antipsychotics
Acepromazine Atravet, Acezine phenothiazine N05AA04
Acetophenazine Tindal phenothiazine N05AB07
Benperidol Frenactyl butyrophenone N05AD07
Bromperidol Bromidol, Bromodol butyrophenone N05AD06
Butaperazine Repoise, Tyrylen phenothiazine N05AB09
Carfenazine phenothiazine
Chlorproethazine phenothiazine N05AA07
Chlorpromazine Largactil, Thorazine phenothiazine N05AA01
Chlorprothixene Cloxan, Taractan, Truxal thioxanthene N05AF03
Clopenthixol Sordinol thioxanthene N05AF02
Cyamemazine Tercian phenothiazine N05AA06
Dixyrazine Esucos phenothiazine N05AB01
Droperidol Droleptan, Dridol, Inapsine, Xomolix, Innovar (+ Fentanyl) phenylbutylamine (butyrophenone) N05AD08
Fluanisone butyrophenone N05AD09
Flupentixol Depixol, Fluanxol thioxanthene N05AF01
Fluphenazine Prolixin, Modecate phenothiazine N05AB02
Fluspirilene Redeptin, Imap diphenylbutylpiperidine N05AG01
Haloperidol Haldol phenyl-piperidinyl-butyrophenone N05AD01
Levomepromazine Nosinan, Nozinan, Levoprome phenothiazine N05AA02
Lenperone Elanone-V butyrophenone
Loxapine Loxapac, Loxitane dibenzoxazepine N05AH01
Mesoridazine Serentil phenothiazine N05AC03
Metitepine tricylic dibenzodiazepine
Molindone Moban indole derivative N05AE02
Moperone Luvatren butyrophenone N05AD04
Oxypertine Equipertine, Forit, Integrin, Lanturil, Lotawin, Opertil phenylpiperazine N05AE01
Oxyprotepine Moditen (Czech republic) dibenzothiepine
Penfluridol Semap, Micefal, Longoperidol diphenylbutylpiperidine N05AG03
Perazine Taxilan phenothiazine N05AB10
Periciazine Neuleptil, Neulactil phenothiazine N05AC01
Perphenazine Trilafon phenothiazine N05AB03
Pimozide Orap diphenylbutylpiperidine N05AG02
Pipamperone Dipiperon, Dipiperal, Piperonil, Piperonyl, Propitan butyrophenone N05AD05
Piperacetazine Quide phenothiazine
Pipotiazine Piportil phenothiazine N05AC04
Prochlorperazine Compazine, Stemzine, Buccastem, Stemetil, Phenotil phenothiazine N05AB04
Promazine Sparine phenothiazine N05AA03
Prothipendyl phenothiazines N05AX07
Spiperone Spiroperidol, Spiropitan butyrophenone
Sulforidazine Imagotan, Psychoson, Inofal phenothiazine
Thiopropazate Artalan, Dartal, Dartalan, Dartan phenothiazine N05AB05
Thioproperazine Majeptil phenothiazine N05AB08
Thioridazine Mellaril, Melleril phenothiazine N05AC02
Thiothixene Navane thioxanthene N05AF04
Timiperone butyrophenone
Trifluoperazine Stelazine phenothiazine N05AB06
Trifluperidol butyrophenone N05AD02
Triflupromazine Vesprin phenothiazine N05AA05
Zuclopenthixol Clopixol thioxanthene N05AF05
atypical antipsychotics
Amoxapine Asendin, Asendis, Defanyl, Demolox dibenzoxazepine N06AA17
Amisulpride Amazeo, Amipride, Amival, Solian, Soltus, Sulpitac, Sulprix substituted benzamides N05AL05
Aripiprazole Abilify quinolone N05AX12
Asenapine Saphris dibenzo-oxepino pyrrole N05AH05
Blonanserin Lonasen
Brexpiprazole Rexulti quinolone N05AX16
Cariprazine Vraylar N05AX15
Carpipramine Prazinil, Defekton
Clocapramine Clofekton, Padrasen imidobenzyl
Clorotepine Clotepin, Clopiben tricylic dibenzodiazepine
Clotiapine Entumine N05AH06
Clozapine Clozaril tricylic dibenzodiazepine N05AH02
Iloperidone Fanapt benzisoxazole N05AX14
Levosulpiride benzamide N05AL07
Lurasidone Latuda n-arylpiperazine (piperazine) N05AE05
Melperone Bunil, Buronil, Eunerpan butyrophenone N05AD03
Mosapramine Cremin N05AX10
Nemonapride Emilace benzamide
Olanzapine Zyprexa, Ozace, Lanzek, Zypadhera thienobenzodiazepine N05AH03
Paliperidone Invega pyridopyrimidine N05AX13
Perospirone Lullan azapirone
Quetiapine Seroquel dibenzothiazepine N05AH04
Remoxipride Roxiam salicylamide N05AL04
Reserpine Raudixin, Serpalan, Serpasil yohimbine alkaloid C02AA02
Risperidone Risperdal, Zepidone pyridopyrimidine N05AX08
Sertindole Serdolect phenylpyrrole N05AE03
Sulpiride Sulpirid, Eglonyl benzenesulfonamide (benzamide) N05AL01
Sultopride Barnetil, Barnotil, Topral benzamide N05AL02
Tiapride Equilium, Tiapridal benzamide N05AL03
Veralipride Agreal, Agradil benzamide N05AL06
Ziprasidone Geodon, Zeldox n-arylpiperazine (piperazine) N05AE04
Zotepine Nipolept tricylic dibenzodiazepine N05AX11
under development
perphenazine gamma-aminobutyrate BL-1020
Pimavanserin ACP-103
F-15063
ITI-007 tetracyclic quinoxaline
Lu AF35700
RP5063
Stepholidine berberine
development abandoned
Amperozide diphenylbutylpiperazine QN05AX90
Bifeprunox DU-127,090 biphenyl derivative
Butaclamol AY-23,028
Ciclindole WIN-27,147-2
Clopimozide R-29,764 diphenylbutylpiperidine
Elopiprazole DU-29894 phenylpiperazine
Flucindole
Fluotracen SKF-28,175
Fluperlapine NB 106-689 tricyclic
Gevotroline WY-47,384 tricylic dibenzodiazepine
Naranol W-5494A
N-desmethylclozapine ACP-104
Ocaperidone R 79598 benzisoxazole
Piquindone Ro 22-1319 tricyclic
Pomaglumetad LY2140023
Tiospirone BMY-13,859 azapirone
Umespirone KC-9172 azapirone
Vabicaserin SCA-136
Volinanserin MDL-100,907
Zetidoline DL 308-IT
Zicronapine Lu 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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