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Versione delle 21:43, 7 apr 2019

Olanzapina, un esempio di antipsicotico di seconda generazione.

Il termine neurolettico (o antipsicotico) indica una famiglia di psicofarmaci che agiscono su precisi obiettivi neurotrasmettitoriali (notoriamente diminuendo l’attività della dopamina nel cervello) e vengono principalmente utilizzati per il trattamento delle psicosi anche in fase acuta, della schizofrenia, della fase maniacale del disturbo bipolare, degli stati di agitazione e a volte nel disturbo depressivo cronico. Vengono anche definiti sedativi maggiori (in contrapposizione alle benzodiazepine dette tranquillanti minori).

Non sono indicati per il trattamento dell'insonnia in quanto non vi sono evidenze cliniche a favore del loro impiego.^[1]

Sono storicamente raggruppati in due differenti classi in base al loro meccanismo di azione: quelli di prima generazione e quelli di seconda generazione, i quali presentano generalmente un miglior profilo di effetti collaterali e sono perciò più comunemente prescritti.

Storia

Nei primi del '900 si scoprì che un derivato dell'anilina, la prometazina, possedeva interessanti proprietà sedative e antiallergiche. Da questa fu sintetizzata la clorpromazina che inizialmente fu utilizzata come sedativo fino a quando il medico francese Henri Laborit non scoprì di essere in grado di indurre una particolare forma di indifferenza agli stimoli ambientali senza alterare particolarmente lo stato di vigilanza (effetto atarassizzante). La clorpromazina fu perciò sperimentata nel trattamento dei diversi stati di agitazione e divenne il primo neurolettico.

A causa dell'enorme successo commerciale della clorpromazina, fu avviata la ricerca dei nuovi neurolettici che nel giro di una decina di anni portò all'individuazione e alla messa a punto delle maggiori classi di antipsicotici oggi definiti "tipici" o di prima generazione: in tutto una ventina di fenotiazine (prodotti assai simili strutturalmente alla Cloropromazina) e anche Tioxanteni, Dibenzazepine, il Butirrofenone, le Difenilbutilpiperidine e altre ancora. Questi farmaci sono caratterizzati dall’avere un’elevata affinità e selettività per i recettori della dopamina.

In seguito si è vista l'introduzione di nuovi antipsicotici, dotati di una affinità ad ampio spettro per i siti dopaminergici e serotoninergici, definiti perciò "atipici" o di seconda generazione e dotati di un migliorato profilo di efficacia ed effetti collaterali: ne fanno parte Risperidone, Clozapina, Olanzapina, Quetiapina. Questi nuovi antipsicotici sembrano determinare con frequenza sensibilmente minore i sintomi extra piramidali e sono efficaci nel trattamento dei sintomi sia positivi sia negativi (anche se in misura minore) così come delle psicosi gravi e croniche.

Negli ultimi anni, nuove classi di farmaci definiti genericamente antipsicotici di terza generazione o "multimodali" sono entrati nella pratica clinica e caratterizzati da un ancor più complesso meccanismo di azione. Ne fanno parte aripiprazolo, asenapina e caripiprazina. La loro efficacia e sicurezza è ancora oggetto di approfondimento.

Usi medici

Schizofrenia

L'effetto principale di un trattamento con antipsicotici è quello di ridurre i cosiddetti sintomi "positivi" della schizofrenia, ovvero deliri e allucinazioni.^[2] Tuttavia gli studi indicano che conseguentemente all'assunzione di neurolettici, specie quelli di prima generazione, peggiorano gli episodi di apatia, mancanza di affetto emotivo, mancanza di interesse nelle interazioni sociali (sintomi negativi della schizofrenia) mentre dal punto di vista cognitivo si possono avere effetti come pensieri disordinati e una ridotta capacità di pianificare ed eseguire attività.^[3]^[4] In generale, l'efficacia del trattamento con antipsicotici nella schizofrenia sembra aumentare con la gravità dei sintomi di base.^[5] Le applicazioni di questi farmaci nel trattamento della schizofrenia includono il trattamento del primo episodio di psicosi, la successiva terapia di mantenimento e trattamento di episodi ricorrenti di psicosi acuta.

È doveroso ricordare che i neurolettici non curano il disturbo all'origine, bensì dovrebbero attenuare i sintomi esteriori della malattia, quali deliri, allucinazioni e disforia.^[6]

Disturbo bipolare

Gli antipsicotici sono usati comunemente nel trattamento di prima linea negli episodi maniacali e misti associati a disturbo bipolare, spesso in combinazioni con stabilizzanti dell'umore come litio o valproato.^[7] Il motivo di questa combinazione è il ritardo terapeutico degli stabilizzatori dell'umore di cui sopra (per ottenere gli effetti terapeutici del valproato sono di solito necessari circa cinque giorni dall'inizio del trattamento, mentre il litio solitamente richiede almeno una settimana^[8] prima di dare gli effetti terapeutici).

Alcuni antipsicotici atipici (lurasidone, olanzapina, asenapina e quetiapina) si ritiene che siano efficaci in monoterapia nel trattamento della depressione bipolare e dei deliri maniacali, cioè senza l'aggiunta di altri farmaci di supporto.^[9]

Altri utilizzi

Oltre alle predette finalità gli antipsicotici possono essere usati come farmaci di seconda scelta nella cura delle seguenti affezioni: disturbo ossessivo-compulsivo (il risperidone in particolare^[10]), disturbo post-traumatico da stress, disturbi della personalità, sindrome di Tourette, autismo ed agitazione in corso di demenza, ma solo nel caso in cui i farmaci di prima scelta non abbiano avuto effetto.^[10] Le prove scarseggiano sull'utilità degli antipsicotici atipici nei disturbi del comportamento alimentare.

Meccanismo di azione

Gli antipsicotici presentano un'azione prevalentemente antidelirante e antiallucinatoria. Vengono impiegati soprattutto nel trattamento della schizofrenia e di altre manifestazioni psicotiche.

Possono essere somministrati per via orale, intramuscolare o endovenosa: in particolare le forme farmaceutiche che richiedono iniezione vengono utilizzate o quando è necessario ottenere un rapido effetto per il trattamento delle crisi acute, oppure per la somministrazione dei farmaci depot cioè delle formulazioni a lunghissima durata d’azione che permettono somministrazioni del farmaco molto distanziate nel tempo, da utilizzare ad esempio nel trattamento di pazienti con scarsa aderenza al trattamento.

A dosaggi adeguati riducono il delirio, le allucinazioni, le anomalie comportamentali degli psicotici favorendone il reinserimento sociale. Se assunti da un soggetto non psicotico, non producono uno stato di sedazione quanto piuttosto una estrema indifferenza agli stimoli ambientali e un fortissimo appiattimento emotivo (effetto atarassizzante).^[11]

I siti d'azione principali dei farmaci antipsicotici sono le vie dopaminergiche, più in particolare quelle che da livello mesencefalico si proiettano verso l'area del pensiero situata nella corteccia. I bersagli sono i recettori della dopamina che vengono inibiti, in particolare è il blocco dei recettori D2 post sinaptici a generare i maggiori effetti terapeutici (gli altri target dopaminergici sono i recettori D1, D3, D4).^[12]

I farmaci neurolettici vengono classicamente divisi in due categorie:^[13]

i tipici, che hanno una affinità pressoché selettiva verso i recettori dopaminergici, in particolare sul sottotipo D2, su cui agiscono come potenti antagonisti. Essendo molto attivi in tal senso e poco selettivi per le diverse aree cerebrali, mostrano una elevata incidenza di effetti collaterali di tipo extrapiramidale. Data la loro efficacia sono spesso preferiti nella gestione delle crisi acute.
gli atipici, sviluppati in modo da migliorare il profilo di effetti collaterali perché esercitano sia un antagonismo verso i recettori dopaminergici, in particolare i D2 per i quali mostrano una affinità minore rispetto ai neurolettici tipici, sia un antagonismo verso alcuni recettori serotoninergici, in particolare i sottotipi 5HT2A e 5HT2C. Quest'ultime attività si ipotizza possano migliorare sia i sintomi della malattia (nella schizofrenia sembra coinvolta anche un'alterazione dell'attività serotoninergica) che diminuire l'incidenza di effetti collaterali extrapiramidali per modulazione indiretta del tono dopaminergico. Non tutti condividono pienamente questo meccanismo d'azione, dato che la modulazione di altri target neuronali (ad esempio il recettore GHB nelle benzammidi sostituite) o enzimatici (come l'inibizione della Amminoacido Ossidasi da parte del Risperidone) sembrano contribuire all'effetto complessivo. Inoltre molti presentano una distribuzione preferenziale proprio nelle aree coinvolte nella genesi del disturbo, migliorando quindi ulteriormente il profilo di effetti collaterali. Sono perciò preferiti, rispetto ai tipici, nelle terapie di mantenimento anche se alcuni studi sembrano indicare una efficacia leggermente minore.

Recentemente è stata proposta una nuova classe per raccogliere i farmaci come l'aripiprazolo che si comportano come agonisti parziali dei recettori dopaminergici piuttosto che come antagonisti puri, definendoli neurolettici di terza generazione. Nonostante l'incidenza di effetti collaterali extrapiramidali e discinesia tardiva sia più elevata tra gli antipsicotici di prima generazione, anche nelle altre classi possono comunemente verificarsi tali effetti collaterali.

Effetti indesiderati

Gli effetti collaterali sia di tipo fisico che di tipo neuropsichiatrico descritti per questa classe di farmaci sono numerosi, perciò la scelta di sottoporre un paziente ad un trattamento con antipsicotici deve necessariamente passare per una attenta valutazione del rapporto rischi-benefici. Per tale motivo questi farmaci dovrebbero essere utilizzati solo nei casi strettamente necessari, alla dose minima e per il tempo minimo necessari, al fine di poter provocare meno effetti collaterali alcuni dei quali anche potenzialmente gravi come le sindromi metaboliche e i danni neurologici. Tuttavia, specie i farmaci di più recente commercializzazione, sono generalmente ben tollerati e mostrano una buona tollerabilità in particolare nel trattamento a breve e medio termine.^[14]^[15]

Incidenza e gravità degli effetti collaterali dipendono oltre che dal tipo di molecola utilizzata e dal dosaggio, anche dalla sensibilità individuale e dalla durata del trattamento. Quelli più comunemente riportati includono:

Effetti extrapiramidali (tremori, rigidità, movimenti involontari)
Irrequietezza motoria, lentezza o blocco dei movimenti, rallentamento della ideazione e dei riflessi
Effetti cognitivi (confusione mentale, deficit di attenzione)
Effetti anticolinergici (bocca secca, costipazione, visione offuscata; in particolare con olanzapina e clozapina)
Sedazione (in particolare con asenapina, clorpromazina, olanzapina, quetiapina, zotepina)
Ottundimento emotivo e atarassia
Alterazioni endocrine e metaboliche (iperprolattinemia che può causare osteoporosi, galattorrea, ginecomastia; sindromi metaboliche con aumento del rischio di diabete di tipo 2 ed aumento di peso specie dopo trattamento prolungato)
Mal di testa
Vertigini
Ansia

Meno comunemente possono verificarsi:

Gli antipsicotici possono provocare anche la discinesia tardiva, una patologia iatrogena spesso irreversibile caratterizzata da movimenti involontari o semivolontari rapidi simili a tic, lente contorsioni muscolari di lingua, volto, collo, del tronco, dei muscoli della deglutizione e della respirazione. Un alto aspetto generalmente poco indagato sono gli effetti collaterali sula sfera emotiva dei pazienti sottoposti a trattamento che in alcuni casi possono essere confusi come un sintomo della patologia trattata e non identificati come un effetto collaterale della terapia. Questi effetti riguardano soprattutto depressione, attacchi d’ansia (disforia da neurolettici), blocco delle funzioni cognitive, emotive e volitive (che in termini psicoanalitici potrebbe venire descritto come una perdita di funzioni dell'Io).^[15]

Altri effetti collaterali riguardano l'incremento del rischio di morte per qualsiasi causa nei pazienti con demenza trattati con antipsicotici. Uno studio ha rilevato che l'istituzione di un trattamento a base di aloperidolo negli anziani conduce ad un incremento del rischio di morte del 30% nei 6 mesi successivi.^[18]

Risultati delle ricerche scientifiche sugli effetti dei neurolettici sulla massa cerebrale

Diverse ricerche scientifiche, indicano l’esistenza di un nesso causale tra l'uso prolungato dei neurolettici e il restringimento della massa cerebrale.^[17]^[19]^[20] Uno studio del 2012 ha evidenziato che la perdita di materia grigia è maggiore nei pazienti trattati cronicamente con i tipici rispetto a quelli trattati con gli atipici, ma in entrambi i casi le variazioni erano evidenziabili.^[21]^[22] In sintesi gli studi indicano che:

La diminuzione della materia grigia, a cui si associa un conseguente aumento di volume del fluido cerebrospinale e quindi un potenziale degrado delle funzioni cognitive del paziente, è correlato alla dose assunta e alla durata del trattamento.^[23]
In uno studio effettuato sui macachi, a cui era stato somministrato Aloperidolo a dosi elevate, è stata riportata una perdita parziale delle funzioni intellettive con effetti, in alcuni domìni cognitivi, vicini a quelli della demenza.^[24]^[25]
La risonanza magnetica nucleare permette di visualizzare concretamente i cambiamenti reversibili nel cervello di questi farmaci.^[26]

La diminuzione progressiva del volume di materia grigia era più evidente nei pazienti sottoposti a più trattamenti con antipsicotici. In generale, il numero di trattamenti con antipsicotici, la dose e la durata è direttamente proporzionale alla diminuzione dei volumi di materia grigia.^[27]^[28]

A causa di questi e altri effetti indesiderati, alcuni dei quali potenzialmente non reversibili, l'utilizzo di antipsicotici è sconsigliato al di fuori dei casi strettamente necessari, utilizzandoli per il tempo minimo e alla dose minima efficace. Per quel che riguarda la reversibilità dei danni causati da farmaci neurolettici è necessario sospendere il trattamento per poter avere dei miglioramenti significativi che tuttavia variano a seconda della tipologia di farmaco assunto.

Classificazione

antipsicotici tipici o di prima generazione
- butirrofenoni
  - Aloperidolo, molto potente ed efficace, associa all'effetto terapeutico un'alta incidenza di effetti collaterali extrapiramidali
  - Droperidolo
- fenotiazine
  - Alifatiche
    - Clorpromazina
    - Prometiazina
    - Acepromazina, utilizzata in ambito veterinario
  - piperaziniche
    - Perfenazina
    - Porcloperazina
    - Tioproperazina
    - Trifluoperazina
  - Piperidiniche
- Tioxanteni
  - Zuclopentixolo
  - Clopentixolo
  - Tiotixene
Antipsicotici atipici o di seconda generazione
- Benzammidi sostituite
  - Amisulrpide, associa l'antagonismo D2 (a basse dosi preferenzialmente presinaptico), all'agonismo per il recettore GHB e potente antagonismo per il recettore serotoninergico 5-HT7.
  - Sulpiride, simile al composto correlato amisulpride.
  - Tiapride, mostra elevata selettività verso i recettori dopaminergici e una affinità preferenziale per il sistema limbico rispetto a quello striatriale
  - Varelipride, utilizzata però in ambito veterinario.
- Dibenzodiazepine
  - Quetiapina, ha struttura simil dibenzodiazepinica, è considerato quello a maggior potenziale sedativo.
  - Clozapina, considerato un farmaco di seconda linea per i potenziali effetti collaterali anche gravi.
  - Olanzapina
- Scheletro simil Azapironi
  - Lurasidone
  - Risperidone
  - Paliperidone, principale metabolita del risperidone
  - Ziprasidone, causa un minore aumento di peso rispetto ad altri antipsicotici
  - Perospirone
Terza generazione
- Aripiprazolo, agonista parziale dei recettori D2 e di alcuni sottotipi serotoninergici. La sua efficacia è ancora oggetto di approfondimento.
- caripirazina
- bexpiprazolo
- primvanserina

Altri composti che non sono chimicamente o farmacologicamente correlati agli antipsicotici hanno mostrato in diversi studi potenziale neurolettico, tra questi ci sono farmaci approvati per altri disturbi psichiatrici (come il tofisopam) o composti di derivazione naturale come la sarcosina.

Tabelle comparative

Overview
Generic name	Class	Type	Brand name(s)	Launch	Developer/Originator(s)	Refs
Amisulpride	Benzamide	Disputed	Solian	1986	Sanofi-Synthélabo	^[29]^[30]^[31]
Aripiprazole	Phenylpiperazine/Quinolinone	Atypical	Abilify	2002	Otsuka/Bristol-Myers Squibb	^[29]^[32]
Aripiprazole lauroxil	Phenylpiperazine/Quinolinone	Atypical	Aristada	2015	Alkermes	^[33]
Asenapine	Tricyclic/Dibenzoxapinopyrrole	Atypical	Saphris/Sycrest	2009	Organon/Merck	^[29]^[34]
Benperidol	Butyrophenone	Typical	Anquil	1966	Janssen	^[29]
Blonanserin	Pyridinylpiperazine	Atypical	Lonasen	2008	Sumitomo Dainippon/Mitsubishi Tanabe	^[29]^[35]
Brexpiprazole	Phenylpiperazine/Quinolinone	Atypical	Rexulti	2015	Otsuka/Lundbeck	^[36]
Bromperidol	Butyrophenone	Typical	Impromem	1981	Janssen	^[32]^[29]
Cariprazine	Phenylpiperazine	Atypical	Vraylar/Reagila	2015	Gedeon Richter/Actavis	^[37]
Carpipramine	Tricyclic/Dibenzazepine	Disputed	Defecton/Prazinil	1977	Pierre Fabre	^[29]
Chlorpromazine	Tricyclic/Phenothiazine	Typical	Thorazine	1952	Rhône-Poulenc/GlaxoSmithKline	^[32]^[29]
Chlorprothixene	Tricyclic/Thioxanthene	Disputed	Truxal	1959	Roche	^[29]^[32]^[38]
Clocapramine	Tricyclic/Dibenzazepine	Disputed	Clofekton/Padrasen	1974	Yoshitomi	^[39]
Clopenthixol	Tricyclic/Thioxanthene	Typical	Sordinol/Ciatyl	1961	Lundbeck	^[40]
Clorotepine	Tricyclic/Dibenzothiepin	Disputed	Clotepin	1971	Spofa	^[41]^[42]
Clotiapine	Tricyclic/Dibenzothiazepine	Disputed	Etumine	1966	Sandoz/Wander	^[43]^[44]
Clozapine	Tricyclic/Dibenzodiazepine	Atypical	Clozaril	1972	Sandoz-Novartis	^[32]^[29]
Cyamemazine	Tricyclic/Phenothiazine	Disputed	Tercian	1972	Aventis	^[29]^[45]
Droperidol	Butyrophenone	Typical	Dridol/Droleptan/Inapsine	1963	Janssen-Cilag	^[29]^[46]
Flupentixol	Tricyclic/Thioxanthene	Typical	Fluanxol	1965	Lundbeck	^[29]^[47]
Fluphenazine	Tricyclic/Phenothiazine	Typical	Prolixin	1959	Bristol-Myers Squibb	^[32]^[29]
Fluspirilene	Diphenylbutylpiperidine	Typical	Imap	1970	Janssen	^[29]
Haloperidol	Butyrophenone	Typical	Haldol	1959	Janssen	^[32]^[29]
Iloperidone	Benzisoxazole	Atypical	Fanapt	2010	Novartis	^[29]^[48]
Levomepromazine	Tricyclic/Phenothiazine	Disputed	Nozinan/Levoprome	1957	Rhône-Poulenc	^[29]^[49]^[38]
Levosulpiride	Benzamide	Disputed	Levopraid	1987	Abbott	^[29]
Loxapine	Tricyclic/Dibenzoxazepine	Disputed	Loxitane/Loxapac	1975	Wyeth	^[32]^[29]^[50]
Lurasidone	Benzisothiazole	Atypical	Latuda	2010	Sumitomo Dainippon/Sunovion	^[51]
Melperone	Butyrophenone	Disputed	Buronil	1967	Lundbeck	^[32]
Mesoridazine	Tricyclic/Phenothiazine	Typical	Serentil	1967	Novartis-Boehringer	^[32]
Molindone	Dihydroindolone	Disputed	Moban	1975	Abbott	^[32]
Mosapramine	Tricyclic/Dibenzazepine	Disputed	Cremin	1991	Mitsubishi Pharma	^[29]
Nemonapride	Benzamide	Disputed	Emilace/Emirace	1991	Yamanouchi	^[29]^[52]
Olanzapine	Tricyclic/Thienobenzodiazepine	Atypical	Zyprexa	1996	Lilly	^[32]^[29]
Paliperidone	Benzisoxazole	Atypical	Invega	2007	Janssen-Cilag/Johnson & Johnson	^[29]^[53]
Paliperidone palmitate	Benzisoxazole	Atypical	Invega Sustenna/Xeplion	2009	Janssen-Cilag/Johnson & Johnson	^[54]
Penfluridol	Diphenylbutylpiperidine	Typical	Semap	1973	Janssen	^[55]^[56]
Perazine	Tricyclic/Phenothiazine	Typical	Taxilan	1958	Promonta	^[57]
Periciazine	Tricyclic/Phenothiazine	Typical	Neuleptil/Neulactil	1964	Rhône-Poulenc	^[29]^[58]
Perospirone	Benzisothiazole	Atypical	Lullan	2001	Sumitomo Dainippon/Mitsubishi Tanabe	^[29]^[59]
Perphenazine	Tricyclic/Phenothiazine	Typical	Trilafon	1957	Schering-Plough	^[32]^[29]
Pimavanserin	Dibenzylpiperidinylurea	Atypical	Nuplazid	2016	ACADIA Pharmaceuticals	^[60]
Pimozide	Diphenylbutylpiperidine	Typical	Orap	1969	Janssen	^[32]^[29]
Pipamperone	Butyrophenone	Disputed	Dipiperon	1961	Janssen	^[43]^[55]
Pipotiazine	Tricyclic/Phenothiazine	Typical	Piportil	1973	Rhône-Poulenc/Aventis	^[29]^[61]
Prochlorperazine	Tricyclic/Phenothiazine	Typical	Compazine	1956	Rhône-Poulenc/GlaxoSmithKline	^[32]^[49]^[29]
Promazine	Tricyclic/Phenothiazine	Typical	Sparine	1956	Wyeth	^[29]
Quetiapine	Tricyclic/Dibenzothiazepine	Atypical	Seroquel	1997	AstraZeneca	^[32]^[29]
Remoxipride	Benzamide	Disputed	Roxiam	1990	AstraZeneca	^[32]^[29]^[31]
Risperidone	Benzisoxazole	Atypical	Risperdal	1993	Janssen	^[32]^[29]
Sertindole	Imidazolidinone	Atypical	Serdolect	1996	Lundbeck	^[32]^[29]
Spiperone	Butyrophenone	Typical	Spiropitan	1969	Eisai	^[62]
Sulpiride	Benzamide	Disputed	Dogmatil	1968	Delagrange/Fujisawa	^[32]^[29]^[31]
Sultopride	Benzamide	Disputed	Barnetil	1976	Delagrange/Sanofi-Synthélabo	^[29]^[63]
Thioridazine	Tricyclic/Phenothiazine	Typical	Melleril	1958	Novartis	^[32]^[29]
Tiapride	Benzamide	Disputed	Tiapridal	1975	Sanofi-Synthélabo	^[29]
Tiotixene	Tricyclic/Thioxanthene	Typical	Navane	1967	Pfizer	^[32]^[29]^[64]
Trifluoperazine	Tricyclic/Phenothiazine	Typical	Stelazine	1958	GlaxoSmithKline	^[32]^[29]
Triflupromazine	Tricyclic/Phenothiazine	Typical	Vesprin	1957	Bristol-Myers Squibb	^[29]
Veralipride	Benzamide	Disputed	Agreal	1980	Sanofi-Synthélabo	^[29]
Ziprasidone	Benzisothiazole	Atypical	Geodon	2000	Pfizer	^[32]^[29]
Zotepine	Tricyclic/Dibenzothiepin	Atypical	Zoleptil	1982	Fujisawa	^[32]^[29]
Zuclopenthixol	Tricyclic/Thioxanthene	Typical	Clopixol/Cisordinol	1978	Lundbeck	^[40]^[47]^[29]

Tolerability
Generic name ^[65]^[66]^[67]^[67]^[68]^[69]^[70]	Discontinuation rate^[67] (OR with 95% CI in brackets)	Anticholinergic effects	Sedation	EPSE	Weight Gain	Metabolic AEs	QTc prolongation (ORs & 95% CIs)	PE	Hypotension	Notes (e.g. notable AEs*)
Amisulpride	0.43 (0.32-0.57)	-	-	+	+	+/-	+++ (0.66 [0.39-0.91])	+++/++	-	Torsades de Pointes common on overdose.^[71] Has a comparatively low penetrability of the blood-brain barrier.
Amoxapine	?	++	++	+/-	++/+	++/+	++/+	++/+	++/+	Amoxapine is also an antidepressant. Very toxic in overdose due to the potential for renal failure and seizures.
Aripiprazole	0.61 (0.51-0.72)	-	+	+/- (Akathisia mostly)	+	+/-	- (0.01 [–0.13-0·15])	- (can reduce prolactin levels)	-	Only clinically-utilised antipsychotic that does not act by antagonising the D₂ receptor and rather partially agonises this receptor.
Asenapine	0.69 (0.54-0.86)	-	++	+	+	+/-	++/+ (0.30 [–0.04-0.65])	+	+	Oral hypoesthesia. Has a complex pharmacologic profile.
Blonanserin^[72]^[73]	~0.7	+	+	++/+	+/-	+/-	-	++/+	+/-	Only used in a few East Asian countries.
Chlorpromazine	0.65 (0.5-0.84)	+++	+++	++	++	++	++	+++	+++	First marketed antipsychotic, sort of the prototypical low-potency first-generation (typical) antipsychotic.
Clozapine	0.46 (0.32-0.65)	+++	+++	-	+++	+++	+	-	+++	Notable AEs: Agranulocytosis, neutropaenia, leukopaenia and myocarditis. Dose-dependent seizure risk.^[74] Overall the most effective antipsychotic, on average. Usually reserved for treatment-resistant cases or highly suicidal patients.
Droperidol	?	+/-	+/-	+++	+/-	+/-	?	+++	?	Mostly used for postoperative nausea and vomiting.
Flupenthixol	?	++	+	++	++	++	+	+++	+	Also used in lower doses for depression.
Fluphenazine	0.69 (0.24-1.97)^[75]	++	+	+++	+	+	+	+++	+	High-potency first-generation (typical) antipsychotic.
Haloperidol	0.8 (0.71-0.90)	+	+	+++	+	+/-	+ (0.11 [0.03-0.19])	+++	+	Prototypical high-potency first-generation (typical) antipsychotic.
Iloperidone	0.69 (0.56-0.84)	-	+/-	+	++	++	++ (0.34 [0.22-0.46])	++/+	+	?
Levomepromazine	?	+++	+++	++/+	++	++	?	+++	+++	Also used as an analgesic, agitation, anxiety and emesis.
Loxapine	0.52 (0.28-0.98)^[76]	+	++	+++	+	+/-	?	+++	++	?
Lurasidone	0.77 (0.61-0.96)	-	-	++/+	-	-	- (–0.10 [–0.21-0.01])	++/+	-	May be particularly helpful in ameloriating the cognitive symptoms of schizophrenia, likely due to its 5-HT₇ receptor.^[77]
Melperone	?	-	+/-	-	+/-	+/-	++	-	++/+	Several smaller low-quality clinical studies have reported its efficacy in the treatment of treatment-resistant schizophrenia. Only approved for use in a few European countries. It is known that off-licence prescribing of melperone is occurring in the United Kingdom.^[78] Is a butyrophenone, low-potency atypical antipsychotic that has been tried as a treatment for Parkinson's disease psychosis, although with negative results.
Molindone^[79]	?	-	++/+	+	-	-	?	+++	+/-	Withdrawn from the market. Seems to promote weight loss (which is rather unusual for an antipsychotic seeing how they tend to promote weight gain).^[79]
Olanzapine	0.46 (0.41-0.52)	+	++	+	+++	+++	+ (0.22 [0.11-0.31])	+	+	?
Paliperidone	0.48 (0.39-0.58)	-	-	++/+ (dose-dependent)	++	+	- (0.05 [–0.18-0.26])	+++	++	Active metabolite of risperidone.
Perazine	0.62 (0.4-1.10)^[80]	?	?	?	?	?	?	?	?	Limited data available on adverse effects.
Periciazine	?	+++	+++	+	++	+	?	+++	++	Also used to treat severe anxiety. Not licensed for use in the US.
Perospirone^[81]	?	+/-	+	++/+^[82]	+/-	?	-	++/+	-	Usually grouped with the atypical antipsychotics despite its relatively high propensity for causing extrapyramidal side effects.^[82]
Perphenazine	0.30 (0.04, 2.33)^[83]	+	+	+++	+	+	+	+++	+	Has additional antiemetic effects.
Pimozide	1.01 (0.30 to 3.39)^[84]	+	+	+	+	+	+++	+++	+	High potency first-generation (typical) antipsychotic.
Pipotiazine	?	++	++	++	++	+	?	+++	++	Only available in the UK.
Prochlorperazine	?	?	?	+++	?	?	+	+++	?	Primarily used in medicine as an antiemetic.
Quetiapine	0.61 (0.52-0.71)	++/+	++	-	++	++/+	+ (0.17 [0.06-0.29])	-	++	Binds to the D₂ receptor in a hit and run fashion. That is it rapidly dissociates from said receptor and hence produces antipsychotic effects but does not bind to the receptor long enough to produce extrapyramidal side effects and hyperprolactinaemia.
Remoxipride	?	-	+/-	-	+/-	+/-	-	-	-	Removed from the market amidst concerns about an alarmingly high rate of aplastic anaemia.
Risperidone	0.53 (0.46-0.60)	-	++/+ (dose-dependent)	++	++	++/+	++ (0.25 [0.15-0.36])	+++	++	?
Sertindole	0.78 (0.61-0.98)	-	-	-	++	++/+	+++ (0.90 [0.76-1.02])	-	+++	Not licensed for use in the US.
Sulpiride	1.00 (0.25-4.00)^[85]	-	-	+	+	+/-	+	+++/++	-	Not licensed for use in the US.
Thioridazine	0.67 (0.32-1.40)^[86]	+++	+++	+	++	++	+++	+++	+++	Dose-dependent risk for degenerative retinopathies.^[87] Found utility in reducing the resistance of multidrug and even extensively resistant strains of tuberculosis to antibiotics.
Tiotixene	?	-	+	+++	++	++/+	+	+++	+	?
Trifluoperazine	0.94 (0.59-1.48)^[88]	+/-	+	+++	+	+/-	?	+++	+	?
Ziprasidone	0.72 (0.59 to 0.86)	-	++	+	-	-	++ (0.41 [0.31 to 0.51])	++/+	+	?
Zotepine	0.69 (0.41 to 1.07)	+	+++	++	+++/++	+++/++	++	+++	++	Dose-dependent risk of seizures.^[89] Not licensed for use in the US.
Zuclopenthixol	?	++	++	+++	++	++	?	+++	+	Not licensed for use in the US.
Note: "Notable" is to mean side-effects that are particularly unique to the antipsychotic drug in question. For example, clozapine is notorious for its ability to cause agranulocytosis. If data on the propensity of a particular drug to cause a particular AE is unavailable an estimation is substituted based on the pharmacologic profile of the drug. Template:Col-begin Acronyms used: AE - Adverse effect OR - Odds ratio CI - Confidence Interval EPSE - Extrapyramidal Side Effect QTc - Corrected QT interval PE - Prolactin elevation Legend: - very low propensity for this AE + low propensity/severity for this AE ++ moderate propensity/severity for this AE +++ high propensity/severity for this AE Template:Col-end

Efficacy
Generic drug name	Schizophrenia^[65]^[67]	Mania^[90]^[91]	Bipolar depression^[92]	Bipolar maintenance^[93]^[94]	Adjunct in major depression^[95]
Amisulpride	+++	?	?	?	? (+++ in dysthymia)
Aripiprazole	++	++	-	++ (prevents manic and mixed but not depressive episodes)	+++
Asenapine	++/+	++	?	++	?
Chlorpromazine	++	?	?	?	?
Clozapine	+++	?	?	?	?
Haloperidol	++	+++	?	?	?
Iloperidone	+	?	?	?	?
Loxapine	+++/++	+++ (only in the treatment of agitation)	?	?	?
Lurasidone	+	?	+++	?	?
Melperone	+++	?	?	?	?
Olanzapine	+++	+++/++	++	++ (most effective at preventing manic/mixed relapse)	++
Paliperidone	++	+++/++	?	?	?
Perospirone^[96]	+	?	?	?	?
Quetiapine	++	++	+++	+++	++
Risperidone	+++	+++	-	++	+++
Sertindole	++	?	?	?	?
Ziprasidone	++/+	+	?	+	?
Zotepine	++	?	?	?	?

Binding affinity
K_i [nM] toward cloned human receptors (unless otherwise specified)^{[Note 1]}
Drug name^[97]^[98]	SERT	5-HT_1A	5-HT_2A	5-HT_2C	5-HT₆	5-HT₇	α_1A	α_2A	α_2C	NET	D₁	D₂	D₃	D₄	5-HT_2A/D₂	H₁	M₁	M₃
Amisulpride	>10,000	>10,000	8,304	>10,000	4,154	73.5	>10,000	1,114	1,540	>10,000	>10,000	2.2	2.4	2,370	3774.5	>10,000	>10,000	>10,000
Aripiprazole	1,081	5.6	8.7	22.4	642.4	9.97	25.85	74.1	37.63	2091.5	1,173.5	1.64	5.35	514	5.3	27.93	6,778	4,678
Asenapine^[99]	ND	2.5	0.06	0.03	0.25	0.13	1.2	1.2	1.2	ND	1.4	1.3	0.42	1.1	0.0462	1.0	8,128	8,128
Blonanserin^[100]	ND	804	0.812	26.4	41.9	183	26.7 (RB)	530 (RC)	ND	ND	1,070	0.142	0.494	150	5.72	765	100	ND
N-DEBN^[72]	ND	ND	1.28	4.50	5.03	206 (RC)	ND	ND	ND	ND	1,020	1.38	0.23	ND	0.93	ND	ND	ND
Chlorpromazine	1,296	2,115.5	4.5	15.6	17.0	28.4	0.28	184	46	2,443	76.3	1.40	4.65	5.33	3.21	3.09	32.3	57.0
Clozapine	1,624	123.7	5.35	9.44	13.5	17.95	1.62	37	6.0	3,168	266.3	157	269.1	26.4	0.0341	1.13	6.17	19.25
Norclozapine	316.6	13.9	10.9	11.9 (RC)	11.6	60.1	104.8	137.6	117.7	493.9	14.3	94.5	153	63.94	0.115	3.4	67.6	95.7
cis-Flupenthixol	ND	8,028	87.5 (HFC)	102.2 (RC)	ND	ND	ND	ND	ND	ND	3.5	0.35	1.75	66.3	250	0.86	ND	ND
Fluphenazine	5,950	1,039.9	37.93	982.5	34.67	8.00	6.45	314.1	28.9	3,076	17.33	0.30	1.75	40.0	126.4	14.15	1,095	1,441
Haloperidol	3,256	2,066.83	56.81	4,801	5,133	377.6	12.0	801.5	403	2,112	121.8	0.7	3.96	2.71	81.2	1698	>10,000	>10,000
Iloperidone	ND	93.21	1.94	147	63.09	112	0.3	160	16.2	1479	129.32	10.86	10.55	13.75	0.179	12	4,898	>10,000
Loxapine	>10,000	2,456	6.63	13.25	31.0	87.6	31.0	150.9	80.0	5,698	54	28.1	19.33	7.80	0.236	4.90	119.45	211.33
Amoxapine	58	ND	0.5	2.0 (RC)	50	40.21	50	ND	ND	16	ND	20.8	21.0	21.0	0.0240	25	1,000	1,000
Lurasidone^[100]^[101]	ND	6.8	2.0	415	ND	0.5	48	1.6	10.8	ND	262	1.7	ND	ND	1.18	>10,000	>10,000	>10,000
Melperone	ND	2,200 (HB)	230	2,100 (HB)	1,254 (RC)	578 (HB)	180 (HB)	150 (HB)	ND	ND	ND	194	8.95	555	1.186	580	>10,000	>10,000
Molindone	ND	3,797	3773	>10,000	1,008	3,053	2,612	1,097	172.6	ND	ND	6.0	72.5	2,950	628.83	2,130	ND	>10,000
Olanzapine	3,676	2282	3.73	10.2	8.07	105.2	112	314	28.9	>10,000	70.33	34.23	47.0	14.33	0.109	2.19	2.5	56.33
Paliperidone	3,717	616.6	0.71	48	2,414	2.7	2.5	17.35	7.35	>10,000	41.04	0.7	0.5	54.3	1.104	18.8	>10,000	>10,000
Perphenazine	ND	421	5.6	132	17	23	10	810.5	85.2	ND	ND	0.14	0.13	17	40	8	1,500	1,848
Pimozide	ND	650	48.35	2,112	71	0.5	197.7	1,593	376.5	ND	>10,000	1.45	0.25	1.8	33.34	692.2	800 (HB)	1,955
Prochlorperazine	ND	5,900 (HC)	15 (HC)	122	148 (RC)	196 (RC)	23.8 (HB)	1,694.91 (HB)	ND	ND	ND	0.65	2.90	5.40	23.1	18.86 (HB)	555.55 (HB)	ND
Quetiapine	>10,000	394.2	912	1,843	948.75	307.6	22	3,630	28.85	>10,000	994.5	379	340	2,019	2.41	6.90	489	1631.5
Norquetiapine^[102]	ND	45	48	107	ND	76	144	237	ND	12	99.8 (RC)	196	ND	ND	0.245	3.5	38.3 (RC)	ND
Risperidone	>10,000	422.88	0.17	12	2057.17	6.6	5	16.5	1.3	>10,000	243.53	3.57	2.0	4.66	0.0476	20.05	>10,000	>10,000
Sertindole	ND	280	0.39	0.9	5.4	28	1.8	640	450	ND	ND	2.35	2.30	4.92	0.166	130	>5,000	2,692
Sulpiride	ND	>10,000	>10,000 (RC)	>10,000 (RC)	5,000 (RC)	4,000 (RC)	>10,000 (RB)	4,893 (RB)	ND	ND	>10,000	9.80	8.05	54	>1,000	>10,000 (RB)	>10,000 (RB)	>10,000 (RB)
Thioridazine	1,259	144.35	27.67	53	57.05	99	3.15	134.15	74.9	842	94.5	2.20	1.50	6.00	12.58	16.5	12.8	29
Tiotixene	3,878	410.2	50	1355.5	245.47	15.25	11.5	79.95	51.95	>10,000	51	0.12	0.40	203	416.7	8	>10,000	>10,000
Trifluoperazine	ND	950	74	378	144	290.8	24	653.7	391.5	ND	ND	1.12	ND	38.1	66.07	63	ND	1,001
Ziprasidone	112	54.67	0.73	13	60.95	6.31	18	160	68	44	30	4.35	7.85	52.9	0.1678	62.67	>10,000	>10,000
Zotepine	151	470.5	2.7	3.2	6	12	7	208	106	530	71	25	6.4	18	0.108	3.21	18	73
Acronyms used: Template:Col-begin HFC - Human frontal cortex receptor RB - Rat brain receptor RC - Cloned rat receptor ND - No data HB - Human brain receptor HC - Human cortex receptor N-DEBN - N-desethylblonanserin Template:Col-end

Pharmacokinetics
Drug^[103]^[104]^[105]^[106]	Bioavailability	t_1/2 parent drug (active metabolite)	Protein binding	t_max	C_max	V_d	Excretion	Routes	Metabolism enzymes^[97]	Active metabolites
Amisulpride	48%	12 h	16%	3-4 h	54 ± 4 ng/mL	5.8 L/kg	Faeces (20%), urine (50%, when given IV)	Oral	?	None
Aripiprazole	87% (Oral), 100% (IM)	75 h (94 h)	99%	3-5 h	?	4.9 L/kg	Faeces (55%), urine (25%)	Oral, IM (including depot)	CYP2D6, CYP3A4	Dehydroaripiprazole
Asenapine	35% (sublingual)	24 h	95%	0.5-1.5 h	4 ng/mL	20-25 L/kg	Urine (50%), faeces (40%)	Sublingual	CYP1A2, UGT1A4, CYP2D6	None
Blonanserin^[72]^[73]^[107]	55%	10.7-16.2 h (single dosing), 67.9 h (repeated dosing)	≥ 99.7%	1.5-2 h	0.14-0.76 ng/mL (0.57 ng/mL for repeated dosing)	8560-9500 L	Urine (59%), faeces (30%)	Oral	CYP3A4	N-desethylblonanserin
Chlorpromazine	20%	30 h	92-97%	?	?	20 L/kg	Urine	Oral, IM, IV	CYP2D6	Several active metabolites
Clozapine	50-60%	12 h	97%	1.5-2.5 h	102-771 ng/mL	4.67 L/kg	Urine (50%), faeces (30%)	Oral	CYP1A2, CYP2D6, CYP3A4	Norclozapine
Droperidol	?	2 h (8-12 h)	Extensive	60 min (IM)	?	2 L/kg (adults), 0.58 L/kg (children)	Urine (75%), faeces (22%)	IM, IV	?	None
Flupentixol	40-55% (Oral)	35 h	?	7 days (depot)	?	12-14 L/kg	Urine	Oral, IM (including depot)	?	None
Fluphenazine	2.7% (Oral)	14-16 h, 14 days (depot)	?	2 h (Oral), 8-10 h (depot)	?	?	Urine, faeces	Oral, IM (including depot)	?	None
Haloperidol	60-70% (Oral)	10-20 h (short-acting IM), 3 weeks (depot)	92%	2-6 h (Oral), 10-20 min (short-acting IM), 6–7 days (depot)	?	8-18 L/kg	Urine (30%), faeces (15%)	Oral, IM, IV	CYP3A4	None
Iloperidone	96%	?	95%	2-4 h	?	1340-2800 L	Urine (45-58%), faeces (20-22%)	Oral	CYP3A4, CYP2D6	None notable.
Levomepromazine	?	30 h	?	2-3 h	?	?	Urine, faeces	IM, IV	?	Methotrimeprazine sulfoxide
Loxapine	High	6-8 h (Inhaled), 4-12 h (Oral)	96.6%	2 min (inhaled), 2 h (oral), 5 h (IM)	257 ng/mL (inhaled), 6-13 ng/mL (Oral)	?	Urine (56-70%), faeces [Only oral data available]	Oral, IM, Inhalation	CYP1A2, CYP3A4, CYP2D6	Amoxapine (a tricyclic antidepressant), 7-OH loxapine, 8-OH loxapine
Lurasidone	9-19%	18 h	99%	1-3 h	?	6173 L	Urine (9%), faeces (80%)	Oral	CYP3A4	2 active
Melperone^[108]	54% (Oral via syrup), 65% (Oral via tablets), 87% (IM)	2.1-6.4 h (Oral), 6.6 ± 3.7 h (IM)	50%	1.6-2.4 h (Oral, tablets), 1 h (Oral, syrup)	1132 ± 814 ng/mL (25 mg, orally), 2228-3416 ng/mL (50 mg, orally), 89539 ± 37001 ng/mL (100 mg, orally)	9.9 ± 3.7 L/kg (10 mg), 7 ± 1.61 L/kg (20 mg)	Urine (70% as metabolites, 5.5-10.4% as parent drug)	Oral, IM	?	None
Olanzapine	87% (Oral)	30 h	93%	6 h (Oral), 15-45 min (short-acting IM), 7 days (depot)	4-20.4 mg/mL^[109]	1000 L	Urine (57%), faeces (30%)	Oral, IM (including depot)	CYP1A2	None
Paliperidone	28% (Oral)	23 h (Oral), 25–49 days (IM)	74%	24 h (Oral), 13 days (IM)	8.85-11.7 ng/mL^[110]	390-487 L	Urine (80%), faeces (11%)	Oral, IM (depot)	CYP3A4, CYP2D6	None
Periciazine	?	12 h	?	2 h	150 ng/mL	?	Urine	Oral	?	?
Perospirone^[111]	?	1.9-2.5 h	92%	1.5 h	5.7 ng/mL	?	Urine (0.4% as unchanged drug)	Oral	?	None
Perphenazine	?	9-12 h (10-19 h)	?	1-3 h; 2-4 h (metabolite)	0.984 ng/mL; 0.509 ng/mL	?	Urine, faeces	Oral	CYP2D6	7-OH perphenazine
Pimozide	40-50%	55 h	?	6-8 h	4-19 ng/mL (dose-dependent)	?	Urine	Oral	CYP3A4, CYP2D6	None
Prochlorperazine	12.5%	6.8-9 h	High	?	?	12.9-17.7 L/h	Urine, bile	Oral, IM, IV	?	N-desmethylprochlorperazine
Quetiapine	100%	6 h (IR), 7 h (XR); active metabolite: 12 h	83%	1.5 h (IR), 6 h (XR)	@ 250 mg q8hr 778 ng/mL (male), 879 ng/mL (female)^[112]	6-14 L/kg	Urine (73%), faeces (20%)	Oral	CYP3A4	Norquetiapine (a norepinephrine reuptake inhibitor and 5-HT_1A receptor partial agonist)
Risperidone	70%	3-17 h (24 h)	90% (active metabolite: 77%)	3-17 h	?	1-2 L/kg	Urine (70%), faeces (14%)	Oral, IM (including depot)	CYP2D6	Paliperidone
Sertindole	?	3 days	99.5%	10 h	?	20 L/kg	Urine (4%), faeces (46-56%)	Oral	CYP2D6	None
Sulpiride^[113]	27 ± 9%	8 h	40%	3-6 h	?	2.72 ± 0.66 L/kg	Urine, faeces	Oral	?	None
Thioridazine	?	24 h	95%	?	?	?	?	Oral	CYP2D6	None
Tiotixene	?	24 h	90%	?	?	?	?	Oral	CYP1A2	None
Trifluoperazine	?	24 h	?	?	?	?	?	Oral	?	None
Ziprasidone	60% (Oral), 100% (IM)	7 h (Oral), 2-5 h (IM)	99%	6-8 h (Oral), ≤ 60 min (IM)	?	1.5 L/kg	Faeces (66%), urine (20%)	Oral, IM	CYP3A4, CYP1A2	None
Zotepine^[114]^[115]	7-13%	13.7-15.9 h (12 h)	97%	1-4 h	31-240	10 L/kg	Urine (17%)	Oral	CYP1A2, CYP3A4	Norzotepine (a norepinephrine reuptake inhibitor)
Zuclopenthixol	49%	20 h	98%	2-12 h (mean: 4 h)	?	20 L/kg	Faeces, urine (10%)	Oral, IM (including depot)	CYP2D6	None

Note

^ American Psychiatric Association Five Things Physicians and Patients Should Question, su choosingwisely.org, 23 settembre 2013.
^ Psychosis and schizophrenia in adults (CG178), su guidance.nice.org.uk.
^ Miyamoto S, Miyake N, Jarskog LF, Fleischhacker WW, Lieberman JA, Pharmacological treatment of schizophrenia: a critical review of the pharmacology and clinical effects of current and future therapeutic agents, in Mol. Psychiatry, December 2012, DOI:10.1038/mp.2012.47, PMID 22584864.
^ Antipsychotics in adults with schizophrenia: comparative effectiveness of first-generation versus second-generation medications: a systematic review and meta-analysis, in Annals of Internal Medicine, vol. 157, n. 7, DOI:10.7326/0003-4819-157-7-201210020-00525, PMID 22893011.
^ Toshi A. Furukawa, Stephen Z. Levine, Shiro Tanaka, Yair Goldberg, Myrto Samara, John M. Davis, Andrea Cipriani & Stefan Leucht, Initial Severity of Schizophrenia and Efficacy of Antipsychotics: Participant-Level Meta-analysis of 6 Placebo-Controlled Studies, in JAMA psychiatry, vol. 72, p. 14, DOI:10.1001/jamapsychiatry.2014.2127, PMID 25372935.
^ Evidence-based guidelines for the pharmacological treatment of schizophrenia: recommendations from the British Association for Psychopharmacology, in J. Psychopharmacol. (Oxford), vol. 25, n. 5, p. 567–620, DOI:10.1177/0269881110391123, PMID 21292923.
^ Young LL, Kradjan WA, Guglielmo BJ, Corelli RL, Williams BR, Koda-Kimble MA, Applied therapeutics: the clinical use of drugs, 2009, ISBN 0-7817-6555-2.
^ Wolters Kluwer Health/Lippincott Williams & Wilkins, Applied therapeutics: the clinical use of drugs, Philadelphia, 2009, ISBN 0-7817-6555-2.
^ Lurasidone Approved for Bipolar Depression, su medscape.com, Medscape, 2 ottobre 2013.
^ ^a ^b Maher AR, Theodore G, Summary of the comparative effectiveness review on off-label use of atypical antipsychotics, in J Manag Care Pharm, June 2012, PMID 22784311.
^ Leucht S, Cipriani A, Spineli L, Mavridis D, Orey D, Richter F, Samara M, Barbui C, Engel RR, Geddes JR, Kissling W, Stapf MP, Lässig B, Salanti G, Davis JM, Comparative efficacy and tolerability of 15 antipsychotic drugs in schizophrenia: a multiple-treatments meta-analysis., in Lancet, vol. 382, n. 9896, September 2013, DOI:10.1016/S0140-6736(13)60733-3, PMID 23810019.
^ The new genetics of schizophrenia., su ncbi.nlm.nih.gov.
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Wikizionario contiene il lemma di dizionario «neurolettico»
Wikimedia Commons contiene immagini o altri file su neurolettico

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(EN) antipsychotic drug, su Enciclopedia Britannica, Encyclopædia Britannica, Inc.
Il trattamento antipsicotico con neurolettici classici: l’esperienza del paziente - in psychiatryonline.it

Controllo di autorità	Thesaurus BNCF 23549 · LCCN (EN) sh89002390 · GND (DE) 4041885-6 · BNF (FR) cb119422132 (data) · J9U (EN, HE) 987007546309505171 · NDL (EN, JA) 01037224

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Portale Medicina

Errore nelle note: Sono presenti dei marcatori <ref> per un gruppo chiamato "Note" ma non è stato trovato alcun marcatore <references group="Note"/> corrispondente

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[2] Psychosis and schizophrenia in adults (CG178), su guidance.nice.org.uk.

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[4] Antipsychotics in adults with schizophrenia: comparative effectiveness of first-generation versus second-generation medications: a systematic review and meta-analysis, in Annals of Internal Medicine, vol. 157, n. 7, DOI:10.7326/0003-4819-157-7-201210020-00525, PMID 22893011.

[5] Toshi A. Furukawa, Stephen Z. Levine, Shiro Tanaka, Yair Goldberg, Myrto Samara, John M. Davis, Andrea Cipriani & Stefan Leucht, Initial Severity of Schizophrenia and Efficacy of Antipsychotics: Participant-Level Meta-analysis of 6 Placebo-Controlled Studies, in JAMA psychiatry, vol. 72, p. 14, DOI:10.1001/jamapsychiatry.2014.2127, PMID 25372935.

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[13] (EN) Current Antipsychotics - Springer, DOI:10.1007/978-3-642-25761-2/page/1. URL consultato l'8 maggio 2017.

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[trattamento-15] Il trattamento antipsicotico con neurolettici classici: l’esperienza del paziente | www.psychiatryonline.it, su www.psychiatryonline.it. URL consultato il 16 dicembre 2017.

[16] O'Keane V1, Meaney AM., Antipsychotic drugs: a new risk factor for osteoporosis in young women with schizophrenia?, su ncbi.nlm.nih.gov, PMID 15643097.

[:1-17] Dr. Beng-Choon Ho, MRCPsych, Dr. Nancy C. Andreasen, MD, PhD, Messr. Steven Ziebell, BS, Messr. Ronald Pierson, MS, and Dr. Vincent Magnotta, PhD, Long-term Antipsychotic Treatment and Brain Volumes, su ncbi.nlm.nih.gov.

[18] Christine M. Campanelli, American Geriatrics Society Updated Beers Criteria for Potentially Inappropriate Medication Use in Older Adults, in Journal of the American Geriatrics Society, vol. 60, n. 4, 2012-4, pp. 616–631, DOI:10.1111/j.1532-5415.2012.03923.x. URL consultato il 16 dicembre 2017.

[19] David Cyranoski, Antipsychotic drugs could shrink patients' brains, su nature.com.

[20] Antipsychotics and brain shrinkage: an update, su joannamoncrieff.com, 13 dicembre 2013.

[21] Deborah Brauser, Antipsychotic-Related Brain Loss: Does Class Matter?, su medscape.com, 26 febbraio 2015.

[22] Antipsychotics and Brain Damage: Shrinkage & Volume Loss, su mentalhealthdaily.com.

[23] Antipsychotics for schizophrenia associated with subtle loss in brain volume, su sciencedaily.com, 8 febbraio 2011. URL consultato il JAMA and Archives Journals.

[24] The Influence of Chronic Exposure to Antipsychotic Medications on Brain Size before and after Tissue Fixation: A Comparison of Haloperidol and Olanzapine in Macaque Monkeys, su nature.com, DOI:10.1038/sj.npp.1300710.

[25] Neuroleptics shrink brains in monkeys, su mindfreedom.org.

[26] Karandeep Singh Nandra & Mark Agius, The difference beteween typical and atypical antipsychotics: the effect on neurogenesis (PDF), su hdbp.org.

[27] Development of Psychosis: Gray Matter Loss and the Inflamed Brain, su elsevier.com, Research And Journals.

[28] Antipsychotics and the Shrinking Brain, su psychiatrictimes.com.

[Sanchez2012-29] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r ^s ^t ^u ^v ^w ^x ^y ^z ^aa ^ab ^ac ^ad ^ae ^af ^ag ^ah ^ai ^aj ^ak ^al ^am ^an ^ao ^ap ^aq ^ar ^as ^at Manuel Sanchez, Farmacología y endocrinología del comportamiento, Editorial UOC, May 2012, pp. 148–149, ISBN 978-84-9788-424-2.

[IUPACFischer2006-30] Analogue-based Drug Discovery, John Wiley & Sons, 13 December 2006, pp. 305–, ISBN 978-3-527-60749-5.

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[Leucht_2013-67] Errore nelle note: Errore nell'uso del marcatore <ref>: non è stato indicato alcun testo per il marcatore Leucht_2013

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V · D · M Sistema di classificazione anatomico, terapeutico e chimico: maggiori gruppi di farmaci
Apparato gastrointestinale/ metabolismo (A)	Acidità di stomaco (Antiacidi · H2 antagonisti · Inibitori di pompa protonica) · Antiemetici · Lassativi · Antidiarroici · Farmaci anti-obesità · Farmaci antidiabetici · Vitamine · Sali minerali
Sangue e Sistema emopoietico (B)	Antitrombotici: Farmaci antiaggreganti piastrinici · Anticoagulante · Fibrinolitico · Antiemorragici (Piastrine · Coagulazione · Antifibrinolitici)
Apparato circolatorio (C)	Terapia cardiaca (Antianginosi · Digitalici · Farmaci antiaritmici · Inotropi) · Farmaci antipertensivi (Diuretici · Vasodilatatore · Betabloccanti · Calcio-antagonisti) · sistema renina-angiotensina (ACE inibitori · Antagonista del recettore per l'angiotensina II · Inibitori della renina Aliskiren) Ipolipemizzanti (Statine · Fibrati · Sequestranti degli acidi biliari)
Apparato tegumentario e Pelle (D)	Crema idratante · Cicatrizzante · Antipruriginoso · Antipsoriasi
Apparato urogenitale (G)	Contraccezione · Farmaci per la fertilità · Modulatori selettivi del recettore degli estrogeni · Ormone sessuale
Sistema endocrino (H)	Ormoni ipotalamico-pituitari · Corticosteroidi · (Glucocorticoidi · Mineralcorticoidi) · Ormoni tiroidei · Farmaci antitiroidei
Infezione e Infestazione (J, P, QI)	Antimicrobico : Antibiotico (Antimicobatterico) · Antimicotico · Antivirale · Farmaci antiparassitosi (Antiprotozoari · Antielmintici · Ectoparassiticida) · Immunoglobuline iperimmuni · Vaccino
Disturbi Neoplastici (L01-L02)	Chemioterapia (Antimetabolita · Alchilanti · Farmaci antimitotici · Inibitori della topoisomerasi)
Disturbi del Sistema immunitario (L03-L04)	Immunoterapia (Immunostimolante · Immunosoppressore)
Sistema muscolare, Sistema scheletrico, e Articolazioni (M)	Steroide anabolizzante · Antinfiammatorio (Farmaci antinfiammatori non steroidei o FANS) · Farmaci antireumatici modificanti la malattia · Corticosteroidi · Miorilassante · Bifosfonati
Cervello umano e sistema nervoso (N)	Analgesico · Anestetico (Anestetico generale · Anestetico locale) · Anoressizzante · Sindrome da deficit di attenzione e iperattività · Medicina per le dipendenze fisiche · Anticonvulsivante · farmaci anti demenza · Antidepressivi · Farmaci anticefalalgici · Farmaci antiparkinsoniani · Antipsicotici · Ansiolitici · Farmaci depressivi centrali · Entactogeno · Enteogeno · Euforizzanti · Allucinogeni (Farmaci psichedelici · Farmaci che producono dissociazione · Farmaci che producono delirio) · Ipnotici/Sedativi · Stabilizzatori dell’umore · Neuroprotettori · Nootropo · Neurotossina · Oressizzante · Farmaci antiaggressività · Psicostimolanti · Farmaci stimolanti la vigilanza
Sistema respiratorio (R)	Decongestionante nasale · Broncodilatatore · Antitussivi · Antagonista dei recettori H1
Organi di senso (S)	Oftalmologia · Otologia
Altri ATC (V)	Antidoto · Mezzo di contrasto · Radiofarmacologia · Medicazione

Neurolettico: differenze tra le versioni

Versione delle 21:43, 7 apr 2019

Indice

Storia

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Schizofrenia

Disturbo bipolare

Altri utilizzi

Meccanismo di azione

Effetti indesiderati

Risultati delle ricerche scientifiche sugli effetti dei neurolettici sulla massa cerebrale

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@@ Riga 129: / Riga 129: @@
 **primvanserina
 {{div col end}}Altri composti che non sono chimicamente o farmacologicamente correlati agli antipsicotici hanno mostrato in diversi studi potenziale neurolettico, tra questi ci sono farmaci approvati per altri disturbi psichiatrici (come il [[tofisopam]]) o composti di derivazione naturale come la [[sarcosina]].
+==  Tabelle comparative ==
+{| class="wikitable sortable collapsible collapsed" style="font-size:small; width:100%;"
+! colspan="7" | Overview
+|-
+! Generic name !! Class !! Type !! Brand name(s) !! Launch !! Developer/Originator(s) !! Refs
+|-
+| [[Amisulpride]] || Benzamide || Disputed || Solian || 1986 || Sanofi-Synthélabo || <ref name="Sanchez2012" /><ref name="IUPACFischer2006">{{cite book| name-list-format = vanc | first1= János | last1 = Fischer | first2 = C. Robin | last2 = Ganellin | title = Analogue-based Drug Discovery|url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA305|date=13 December 2006|publisher=John Wiley & Sons|isbn=978-3-527-60749-5|pages=305–}}</ref><ref name="Lidow2000">{{cite book|first = Michael S. | last = Lidow | name-list-format = vanc |title=Neurotransmitter Receptors in Actions of Antipsychotic Medications|url=https://books.google.com/books?id=HIHLBQAAQBAJ&pg=PA23|date=22 June 2000|publisher=CRC Press|isbn=978-1-4200-4177-4|pages=23–}}</ref>
+|-
+| [[Aripiprazole]] || Phenylpiperazine/Quinolinone || Atypical || Abilify || 2002 || Otsuka/Bristol-Myers Squibb || <ref name="Sanchez2012" /><ref name="pmid16082416">{{cite journal | vauthors = Silvestre JS, Prous J | title = Research on adverse drug events. I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes | journal = Methods and Findings in Experimental and Clinical Pharmacology | volume = 27 | issue = 5 | pages = 289–304 | date = June 2005 | pmid = 16082416 | doi = 10.1358/mf.2005.27.5.908643 }}</ref>
+|-
+| [[Aripiprazole lauroxil]] || Phenylpiperazine/Quinolinone || Atypical || Aristada || 2015 || Alkermes || <ref name="AdisInsight-Aripiprazole-Lauroxil">{{Cite web | url=http://adisinsight.springer.com/drugs/800033484 | title=Aripiprazole lauroxil - Alkermes - AdisInsight}}</ref>
+|-
+| [[Asenapine]] || Tricyclic/Dibenzoxapinopyrrole || Atypical || Saphris/Sycrest || 2009 || Organon/Merck || <ref name="Sanchez2012" /><ref name="AdisInsight-Asenapine">{{Cite web | url=http://adisinsight.springer.com/drugs/800001124 | title=Asenapine - AdisInsight}}</ref>
+|-
+| [[Benperidol]] || Butyrophenone || Typical || Anquil || 1966 || Janssen || <ref name="Sanchez2012">{{cite book|first=Manuel | last = Sanchez| name-list-format = vanc |title=Farmacología y endocrinología del comportamiento|url=https://books.google.com/books?id=oV1VVH_AE-kC&pg=PA148|date=May 2012|publisher=Editorial UOC|isbn=978-84-9788-424-2|pages=148–149|deadurl=no|archiveurl=https://web.archive.org/web/20171125213437/https://books.google.com/books?id=oV1VVH_AE-kC&pg=PA148|archivedate=25 November 2017|df=dmy-all}}</ref>
+|-
+| [[Blonanserin]] || Pyridinylpiperazine || Atypical || Lonasen || 2008 || Sumitomo Dainippon/Mitsubishi Tanabe || <ref name="Sanchez2012" /><ref name="AdisInsight-Blonanserin">{{Cite web | url=http://adisinsight.springer.com/drugs/800001321 | title=Blonanserin - Sumitomo Dainippon Pharma - AdisInsight}}</ref>
+|-
+| [[Brexpiprazole]] || Phenylpiperazine/Quinolinone || Atypical || Rexulti || 2015 || Otsuka/Lundbeck || <ref name="AdisInsight-Brexpiprazole">{{cite web |url=http://adisinsight.springer.com/drugs/800029282 |title=Brexpiprazole - Lundbeck/Otsuka - AdisInsight |accessdate=2017-09-27 |deadurl=no |archiveurl=https://web.archive.org/web/20161011194233/http://adisinsight.springer.com/drugs/800029282 |archivedate=11 October 2016 |df=dmy-all }}</ref>
+|-
+| [[Bromperidol]] || Butyrophenone || Typical || Impromem || 1981 || Janssen || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Cariprazine]] || Phenylpiperazine || Atypical || Vraylar/Reagila || 2015 || Gedeon Richter/Actavis || <ref name="AdisInsight-Cariprazine">{{cite web |url=http://adisinsight.springer.com/drugs/800021768 |title=Cariprazine - Gedeon Richter - AdisInsight |accessdate=2017-05-07 |deadurl=no |archiveurl=https://web.archive.org/web/20170818092946/http://adisinsight.springer.com/drugs/800021768 |archivedate=18 August 2017 |df=dmy-all }}</ref>
+|-
+| [[Carpipramine]] || Tricyclic/Dibenzazepine || Disputed || Defecton/Prazinil || 1977 || Pierre Fabre || <ref name="Sanchez2012" />
+|-
+| [[Chlorpromazine]] || Tricyclic/Phenothiazine || Typical || Thorazine || 1952 || Rhône-Poulenc/GlaxoSmithKline || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Chlorprothixene]] || Tricyclic/Thioxanthene || Disputed || Truxal || 1959 || Roche || <ref name="Sanchez2012" /><ref name="pmid16082416" /><ref name="Csernansky2012">{{cite book|first = John G. | last =  Csernansky | name-list-format = vanc | title=Antipsychotics|url=https://books.google.com/books?id=hiz6CAAAQBAJ&pg=PA360|date=6 December 2012|publisher=Springer Science & Business Media|isbn=978-3-642-61007-3|pages=360–}}</ref>
+|-
+| [[Clocapramine]] || Tricyclic/Dibenzazepine || Disputed || Clofekton/Padrasen || 1974 || Yoshitomi || <ref name="Publishing2013">{{cite book|author=William Andrew Publishing|title=Pharmaceutical Manufacturing Encyclopedia|url=https://books.google.com/books?id=_J2ti4EkYpkC&pg=PA1077|date=22 October 2013|publisher=Elsevier|isbn=978-0-8155-1856-3|pages=1077–}}</ref>
+|-
+| [[Clopenthixol]] || Tricyclic/Thioxanthene || Typical || Sordinol/Ciatyl || 1961 || Lundbeck || <ref name="Publishing2013-Clopenthixol">{{cite book|author=William Andrew Publishing|title=Pharmaceutical Manufacturing Encyclopedia|url=https://books.google.com/books?id=_J2ti4EkYpkC&pg=PA1102|date=22 October 2013|publisher=Elsevier|isbn=978-0-8155-1856-3|pages=1102–}}</ref>
+|-
+| [[Clorotepine]] || Tricyclic/Dibenzothiepin || Disputed || Clotepin || 1971 || Spofa || <ref name="Protiva2010">{{cite journal|last1=Protiva|first1=M.|title=ChemInform Abstract: Fifty Years in Chemical Drug Research|journal=ChemInform|volume=23|issue=9|year=2010|pages=no|issn=0931-7597|doi=10.1002/chin.199209338}}</ref><ref name="pmid5576292">{{cite journal | vauthors = Melich H | title = [Clotepin] | language = Czech | journal = Casopis Lekaru Ceskych | volume = 110 | issue = 17 | pages = 404–5 | date = April 1971 | pmid = 5576292 | doi =  }}</ref>
+|-
+| [[Clotiapine]] || Tricyclic/Dibenzothiazepine || Disputed || Etumine || 1966 || Sandoz/Wander || <ref name="GaleResearch1991" /><ref name="pmid16126373">{{cite journal | vauthors = Geller V, Gorzaltsan I, Shleifer T, Belmaker RH, Bersudsky Y | title = Clotiapine compared with chlorpromazine in chronic schizophrenia | journal = Schizophrenia Research | volume = 80 | issue = 2–3 | pages = 343–7 | date = December 2005 | pmid = 16126373 | doi = 10.1016/j.schres.2005.07.007 }}</ref>
+|-
+| [[Clozapine]] || Tricyclic/Dibenzodiazepine || Atypical || Clozaril || 1972 || Sandoz-Novartis || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Cyamemazine]] || Tricyclic/Phenothiazine || Disputed || Tercian || 1972 || Aventis || <ref name="Sanchez2012" /><ref name="pmid15492772">{{cite journal | vauthors = Bourin M, Dailly E, Hascöet M | title = Preclinical and clinical pharmacology of cyamemazine: anxiolytic effects and prevention of alcohol and benzodiazepine withdrawal syndrome | journal = CNS Drug Reviews | volume = 10 | issue = 3 | pages = 219–29 | year = 2004 | pmid = 15492772 | doi =  10.1111/j.1527-3458.2004.tb00023.x}}</ref>
+|-
+| [[Droperidol]] || Butyrophenone || Typical || Dridol/Droleptan/Inapsine || 1963 || Janssen-Cilag || <ref name="Sanchez2012" /><ref name="LamberthDinges2012">{{cite book | first1 = Clemens | last1 = Lamberth | first2 = Jörgen | last2 = Dinges | name-list-format = vanc |title=Bioactive Heterocyclic Compound Classes: Pharmaceuticals|url=https://books.google.com/books?id=35uKnWKD9V8C&pg=PA3|date=16 August 2012|publisher=John Wiley & Sons|isbn=978-3-527-66447-4|pages=3–}}</ref>
+|-
+| [[Flupentixol]] || Tricyclic/Thioxanthene || Typical || Fluanxol || 1965 || Lundbeck || <ref name="Sanchez2012" /><ref name="Pedersen1996">{{cite journal|last1=Pedersen|first1=V. | name-list-format = vanc |title=Thioxanthene antipsychotics|journal=European Psychiatry|volume=11|year=1996|pages=236s|issn=0924-9338|doi=10.1016/0924-9338(96)88706-2}}</ref>
+|-
+| [[Fluphenazine]] || Tricyclic/Phenothiazine || Typical || Prolixin || 1959 || Bristol-Myers Squibb || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Fluspirilene]] || Diphenylbutylpiperidine || Typical || Imap || 1970 || Janssen || <ref name="Sanchez2012" />
+|-
+| [[Haloperidol]] || Butyrophenone || Typical || Haldol || 1959 || Janssen || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Iloperidone]] || Benzisoxazole || Atypical || Fanapt || 2010 || Novartis || <ref name="Sanchez2012" /><ref name="AdisInsight-Iloperidone">{{cite web |url=http://adisinsight.springer.com/drugs/800001330 |title=Iloperidone - Vanda Pharmaceuticals - AdisInsight |accessdate=2017-09-27 |deadurl=no |archiveurl=https://web.archive.org/web/20151211102105/http://adisinsight.springer.com/drugs/800001330 |archivedate=11 December 2015 |df=dmy-all }}</ref>
+|-
+| [[Levomepromazine]] || Tricyclic/Phenothiazine || Disputed || Nozinan/Levoprome || 1957 || Rhône-Poulenc || <ref name="Sanchez2012" /><ref name="Shorter2009">{{cite book|first = Edward | last = Shorter| name-list-format = vanc |title=Before Prozac: The Troubled History of Mood Disorders in Psychiatry|url=https://books.google.com/books?id=nCtnDAAAQBAJ&pg=PR14|year=2009|publisher=Oxford University Press, USA|isbn=978-0-19-536874-1|pages=14–}}</ref><ref name="Csernansky2012" />
+|-
+| [[Levosulpiride]] || Benzamide || Disputed || Levopraid ||| 1987 || Abbott || <ref name="Sanchez2012" />
+|-
+| [[Loxapine]] || Tricyclic/Dibenzoxazepine || Disputed || Loxitane/Loxapac || 1975 || Wyeth || <ref name="pmid16082416" /><ref name="Sanchez2012" /><ref name="pmid10340686">{{cite journal | vauthors = Glazer WM | title = Does loxapine have "atypical" properties? Clinical evidence | journal = The Journal of Clinical Psychiatry | volume = 60 Suppl 10 | issue =  | pages = 42–6 | year = 1999 | pmid = 10340686 | doi =  }}</ref>
+|-
+| [[Lurasidone]] || Benzisothiazole || Atypical || Latuda || 2010 || Sumitomo Dainippon/Sunovion || <ref name="AdisInsight-Lurasidone">{{cite web |url=http://adisinsight.springer.com/drugs/800007206 |title=Lurasidone - Sumitomo Dainippon Pharma - AdisInsight |accessdate=2017-05-07 |deadurl=no |archiveurl=https://web.archive.org/web/20160510014459/http://adisinsight.springer.com/drugs/800007206 |archivedate=10 May 2016 |df=dmy-all }}</ref>
+|-
+| [[Melperone]] || Butyrophenone || Disputed || Buronil || 1967 || Lundbeck || <ref name="pmid16082416" />
+|-
+| [[Mesoridazine]] || Tricyclic/Phenothiazine || Typical || Serentil || 1967 || Novartis-Boehringer || <ref name="pmid16082416" />
+|-
+| [[Molindone]] || Dihydroindolone || Disputed || Moban || 1975 || Abbott || <ref name="pmid16082416" />
+|-
+| [[Mosapramine]] || Tricyclic/Dibenzazepine || Disputed || Cremin || 1991 || Mitsubishi Pharma || <ref name="Sanchez2012" />
+|-
+| [[Nemonapride]] || Benzamide || Disputed || Emilace/Emirace || 1991 || Yamanouchi || <ref name="Sanchez2012" /><ref name="AdisInsight-Nemonapride">{{Cite web | url=http://adisinsight.springer.com/drugs/800007270 | title=Nemonapride - AdisInsight}}</ref>
+|-
+| [[Olanzapine]] || Tricyclic/Thienobenzodiazepine || Atypical || Zyprexa || 1996 || Lilly || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Paliperidone]] || Benzisoxazole || Atypical || Invega || 2007 || Janssen-Cilag/Johnson & Johnson || <ref name="Sanchez2012" /><ref name="AdisInsight-Paliperidone">{{Cite web | url=http://adisinsight.springer.com/drugs/800020763 | title=Paliperidone - Johnson & Johnson - AdisInsight}}</ref>
+|-
+| [[Paliperidone palmitate]] || Benzisoxazole || Atypical || Invega Sustenna/Xeplion || 2009 || Janssen-Cilag/Johnson & Johnson || <ref name="AdisInsight-Paliperidone-Palmitate">{{cite web |url=http://adisinsight.springer.com/drugs/800040526 |title=Paliperidone palmitate - Johnson & Johnson - AdisInsight |accessdate=2017-09-27 |deadurl=no |archiveurl=https://web.archive.org/web/20161030135731/http://adisinsight.springer.com/drugs/800040526 |archivedate=30 October 2016 |df=dmy-all }}</ref>
+|-
+| [[Penfluridol]] || Diphenylbutylpiperidine || Typical || Semap || 1973 || Janssen || <ref name="Vardanyan2017" /><ref name="pmid4604881">{{cite journal | vauthors = Roelofs GA | title = Penfluridol (R 16341) as a maintenance therapy in chronic psychotic patients: a double-blind clinical evaluation | journal = Acta Psychiatrica Scandinavica | volume = 50 | issue = 2 | pages = 219–24 | year = 1974 | pmid = 4604881 | doi = 10.1111/j.1600-0447.1974.tb08210.x }}</ref>
+|-
+| [[Perazine]] || Tricyclic/Phenothiazine || Typical || Taxilan || 1958 || Promonta || <ref name="pmid24425538">{{cite journal | vauthors = Leucht S, Helfer B, Hartung B | title = Perazine for schizophrenia | journal = The Cochrane Database of Systematic Reviews | volume =  | issue =  1| pages = CD002832 | date = Jan 2014 | pmid = 24425538| doi = 10.1002/14651858.CD002832.pub3 }}</ref>
+|-
+| [[Periciazine]] || Tricyclic/Phenothiazine || Typical || Neuleptil/Neulactil || 1964 || Rhône-Poulenc || <ref name="Sanchez2012" /><ref name="pmid24825770">{{cite journal | vauthors = Matar HE, Almerie MQ, Makhoul S, Xia J, Humphreys P | title = Pericyazine for schizophrenia | journal = The Cochrane Database of Systematic Reviews | volume =  | issue = 5 | pages = CD007479 | date = May 2014 | pmid = 24825770 | doi = 10.1002/14651858.CD007479.pub2 }}</ref>
+|-
+| [[Perospirone]] || Benzisothiazole || Atypical || Lullan || 2001 || Sumitomo Dainippon/Mitsubishi Tanabe || <ref name="Sanchez2012" /><ref name="AdisInsight-Perospirone">{{Cite web | url=http://adisinsight.springer.com/drugs/800000573 | title=Perospirone - AdisInsight}}</ref>
+|-
+| [[Perphenazine]] || Tricyclic/Phenothiazine || Typical || Trilafon || 1957 || Schering-Plough || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Pimavanserin]] || Dibenzylpiperidinylurea || Atypical || Nuplazid || 2016 || ACADIA Pharmaceuticals || <ref name="AdisInsight-Pimavanserin">{{cite web |url=http://adisinsight.springer.com/drugs/800014997 |title=Pimavanserin - ACADIA Pharmaceuticals - AdisInsight |accessdate=2017-09-27 |deadurl=no |archiveurl=https://web.archive.org/web/20170925225849/http://adisinsight.springer.com/drugs/800014997 |archivedate=25 September 2017 |df=dmy-all }}</ref>
+|-
+| [[Pimozide]] || Diphenylbutylpiperidine || Typical || Orap || 1969 || Janssen || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Pipamperone]] || Butyrophenone || Disputed || Dipiperon || 1961 || Janssen || <ref name="GaleResearch1991">{{cite book|title=Drugs Available Abroad|year=1991|publisher=Gale Research|isbn=978-0-8103-7177-4|page=52,169|url=https://books.google.com/books?id=2x1tAAAAMAAJ|deadurl=no|archiveurl=https://web.archive.org/web/20170722224557/https://books.google.com/books?id=2x1tAAAAMAAJ|archivedate=22 July 2017|df=dmy-all}}</ref><ref name="Vardanyan2017">{{cite book| first = Ruben | last = Vardanyan| name-list-format = vanc |title=Piperidine-Based Drug Discovery|url=https://books.google.com/books?id=szxHDgAAQBAJ&pg=PA195|date=12 June 2017|publisher=Elsevier Science|isbn=978-0-12-813428-3|pages=158, 195–}}</ref>
+|-
+| [[Pipotiazine]] || Tricyclic/Phenothiazine || Typical || Piportil || 1973 || Rhône-Poulenc/Aventis || <ref name="Sanchez2012" /><ref name="Publishing2013-Pipotiazine">{{cite book|author=William Andrew Publishing|title=Pharmaceutical Manufacturing Encyclopedia|url=https://books.google.com/books?id=_J2ti4EkYpkC&pg=PA2935-IA349|date=22 October 2013|publisher=Elsevier|isbn=978-0-8155-1856-3|pages=2935–}}</ref>
+|-
+| [[Prochlorperazine]] || Tricyclic/Phenothiazine || Typical || Compazine || 1956 || Rhône-Poulenc/GlaxoSmithKline || <ref name="pmid16082416" /><ref name="Shorter2009" /><ref name="Sanchez2012" />
+|-
+| [[Promazine]] || Tricyclic/Phenothiazine || Typical || Sparine || 1956 || Wyeth || <ref name="Sanchez2012" />
+|-
+| [[Quetiapine]] || Tricyclic/Dibenzothiazepine || Atypical || Seroquel || 1997 || AstraZeneca || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Remoxipride]] || Benzamide || Disputed || Roxiam || 1990 || AstraZeneca || <ref name="pmid16082416" /><ref name="Sanchez2012" /><ref name="Lidow2000" />
+|-
+| [[Risperidone]] || Benzisoxazole || Atypical || Risperdal || 1993 || Janssen || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Sertindole]] || Imidazolidinone || Atypical || Serdolect || 1996 || Lundbeck || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Spiperone]] || Butyrophenone || Typical || Spiropitan || 1969 || Eisai || <ref name="Publishing2007-Spiperone">{{cite book|author=William Andrew Publishing|title=Pharmaceutical Manufacturing Encyclopedia|url=https://books.google.com/books?id=dXpUAAAAMAAJ|year=2007|publisher=William Andrew Pub.|isbn=978-0-8155-1526-5|page=3059}}</ref>
+|-
+| [[Sulpiride]] || Benzamide || Disputed || Dogmatil || 1968 || Delagrange/Fujisawa || <ref name="pmid16082416" /><ref name="Sanchez2012" /><ref name="Lidow2000" />
+|-
+| [[Sultopride]] || Benzamide || Disputed || Barnetil || 1976 || Delagrange/Sanofi-Synthélabo || <ref name="Sanchez2012" /><ref name="Publishing2013-Sultopride">{{cite book|author=William Andrew Publishing|title=Pharmaceutical Manufacturing Encyclopedia|url=https://books.google.com/books?id=_J2ti4EkYpkC&pg=PA3129|date=22 October 2013|publisher=Elsevier|isbn=978-0-8155-1856-3|pages=3129–}}</ref>
+|-
+| [[Thioridazine]] || Tricyclic/Phenothiazine || Typical || Melleril || 1958 || Novartis || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Tiapride]] || Benzamide || Disputed || Tiapridal || 1975 || Sanofi-Synthélabo || <ref name="Sanchez2012" />
+|-
+| [[Tiotixene]] || Tricyclic/Thioxanthene || Typical || Navane || 1967 || Pfizer || <ref name="pmid16082416" /><ref name="Sanchez2012" /><ref name="Publishing2013-Tiotixene">{{cite book|author=William Andrew Publishing|title=Pharmaceutical Manufacturing Encyclopedia|url=https://books.google.com/books?id=_J2ti4EkYpkC&pg=PA3214|date=22 October 2013|publisher=Elsevier|isbn=978-0-8155-1856-3|pages=3214–}}</ref>
+|-
+| [[Trifluoperazine]] || Tricyclic/Phenothiazine || Typical || Stelazine || 1958 || GlaxoSmithKline || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Triflupromazine]] || Tricyclic/Phenothiazine || Typical || Vesprin || 1957 || Bristol-Myers Squibb || <ref name="Sanchez2012" />
+|-
+| [[Veralipride]] || Benzamide || Disputed || Agreal || 1980 || Sanofi-Synthélabo || <ref name="Sanchez2012" />
+|-
+| [[Ziprasidone]] || Benzisothiazole || Atypical || Geodon || 2000 || Pfizer || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Zotepine]] || Tricyclic/Dibenzothiepin || Atypical || Zoleptil || 1982 || Fujisawa || <ref name="pmid16082416" /><ref name="Sanchez2012" />
+|-
+| [[Zuclopenthixol]] || Tricyclic/Thioxanthene || Typical || Clopixol/Cisordinol || 1978 || Lundbeck || <ref name="Publishing2013-Clopenthixol" /><ref name="Pedersen1996" /><ref name="Sanchez2012" />
+|}
+{| class="wikitable collapsible collapsed" style="font-size:small; width:100%;"
+! colspan=11 | Tolerability
+|-
+! Generic name<br/><ref name=Lancet2009/><ref name = "Maudsley"/><ref name = "Leucht_2013" /><ref name = "Leucht_2013" /><ref name = "AMH">{{cite book | name-list-format = vanc | title = Australian Medicines Handbook | year = 2013 | publisher = The Australian Medicines Handbook Unit Trust | isbn = 978-0-9805790-9-3 | edition = 2013 | place = Adelaide | editor = Rossi, S }}</ref><ref name = "BNF">{{cite book | name-list-format = vanc | last1 = Joint Formulary Committee | title = British National Formulary (BNF) | year = 2013  | isbn = 978-0-85711-084-8 | edition = 65 | oclc =  | editor2-link =  | location = London, UK  | publisher = Pharmaceutical Press  }}</ref><ref>{{cite web|title=Approximate relative frequency (not intensity) of common adverse effects of antipsychotics (Table 8.21) [NB1] |date=February 2013 |accessdate=2 November 2013 |url=http://etg.tg.com.au/conc/desktop/index.htm?id=75114e7800512079b341de7fb82c953c |work=eTherapeutic Guidelines complete |publisher=Therapeutic Guidelines Limited }}{{dead link|date=July 2017 |bot=InternetArchiveBot |fix-attempted=yes }}</ref>!! Discontinuation rate<ref name = "Leucht_2013" />
+(OR with 95% CI in brackets)
+!Anticholinergic effects !! Sedation !!  EPSE !! Weight Gain !! Metabolic AEs !! QTc prolongation
+(ORs & 95% CIs)
+!PE !! Hypotension !! Notes (e.g. notable AEs*)
+|-
+| [[Amisulpride]] || 0.43 (0.32-0.57) || - || - || + || + || +/- || +++ (0.66 [0.39-0.91]) || +++/++ || - || [[Torsades de Pointes]] common on overdose.<ref>{{cite journal | vauthors = Isbister GK, Balit CR, Macleod D, Duffull SB | title = Amisulpride overdose is frequently associated with QT prolongation and torsades de pointes | journal = Journal of Clinical Psychopharmacology | volume = 30 | issue = 4 | pages = 391–5 | date = August 2010 | pmid = 20531221 | doi = 10.1097/JCP.0b013e3181e5c14c }}</ref> Has a comparatively low penetrability of the [[blood-brain barrier]].
+|-
+| [[Amoxapine]] || ? || ++ || ++ || +/- || ++/+ || ++/+ || ++/+ || ++/+ || ++/+ || Amoxapine is also an antidepressant. Very toxic in overdose due to the potential for renal failure and seizures.
+|-
+| [[Aripiprazole]] || 0.61 (0.51-0.72) || - || + || +/- ([[Akathisia]] mostly) || + || +/- || - (0.01 [–0.13-0·15]) || - (can reduce prolactin levels) || - || Only clinically-utilised antipsychotic that does not act by antagonising the [[Dopamine D2 receptor|D<sub>2</sub> receptor]] and rather partially agonises this receptor.
+|-
+| [[Asenapine]] || 0.69 (0.54-0.86) || - || ++ || + || + || +/- || ++/+ (0.30 [–0.04-0.65]) || + || + || Oral hypoesthesia. Has a complex pharmacologic profile.
+|-
+| [[Blonanserin]]<ref name="Deeks, ED; Keating, GM 65–84">{{cite journal | vauthors = Deeks ED, Keating GM | title = Blonanserin: a review of its use in the management of schizophrenia | journal = CNS Drugs | volume = 24 | issue = 1 | pages = 65–84 | date = January 2010 | pmid = 20030420 | doi = 10.2165/11202620-000000000-00000 }}</ref><ref name="Tenjin, T; Miyamoto, S; Ninomiya, Y; Kitajima, R; Ogino, S; Miyake, N; Yamaguchi, N 2013 587–594">{{cite journal | vauthors = Tenjin T, Miyamoto S, Ninomiya Y, Kitajima R, Ogino S, Miyake N, Yamaguchi N | title = Profile of blonanserin for the treatment of schizophrenia | journal = Neuropsychiatric Disease and Treatment | volume = 9 | pages = 587–94 | year = 2013 | pmid = 23766647 | pmc = 3677929 | doi = 10.2147/NDT.S34433 }}</ref> || ~0.7 || + || + || ++/+ || +/- || +/- || - || ++/+ || +/- || Only used in a few East Asian countries.
+|-
+| [[Chlorpromazine]] || 0.65 (0.5-0.84) || +++ || +++ || ++ || ++ || ++ || ++ || +++ || +++ || First marketed antipsychotic, sort of the prototypical low-potency first-generation (''typical'') antipsychotic.
+|-
+| [[Clozapine]] || 0.46 (0.32-0.65) || +++ || +++ || - || +++ || +++ || + || - || +++ || Notable AEs: [[Agranulocytosis]], [[neutropaenia]], [[leukopenia|leukopaenia]] and [[myocarditis]]. Dose-dependent seizure risk.<ref>{{cite web|title=Clozapine|work=Martindale: The Complete Drug Reference|publisher=Royal Pharmaceutical Society of Great Britain|date=30 January 2013|accessdate=2 November 2013|url=http://www.medicinescomplete.com/mc/martindale/current/12595-x.htm}}</ref> Overall the most effective antipsychotic, on average. Usually reserved for treatment-resistant cases or highly suicidal patients.
+|-
+| [[Droperidol]] || ? || +/- || +/- || +++ || +/- || +/- || ? || +++ || ? || Mostly used for postoperative nausea and vomiting.
+|-
+| [[Flupenthixol]] || ? || ++ || + || ++ || ++ || ++ || + || +++ || + || Also used in lower doses for depression.
+|-
+| [[Fluphenazine]] || 0.69 (0.24-1.97)<ref>{{cite journal | vauthors = Matar HE, Almerie MQ, Sampson S | title = Fluphenazine (oral) versus placebo for schizophrenia | journal = The Cochrane Database of Systematic Reviews | volume = 7 | issue = 7 | pages = CD006352 | date = June 2018 | pmid = 29893410 | pmc = 3796096 | doi = 10.1002/14651858.CD006352.pub3 | editor1-last = Matar }}{{Dead link|date=December 2018 |bot=InternetArchiveBot |fix-attempted=yes }}</ref> || ++ || + || +++ || + || + || + || +++ || + || High-potency first-generation (''typical'') antipsychotic.
+|-
+| [[Haloperidol]] || 0.8 (0.71-0.90) || + || + || +++ || + || +/- || + (0.11 [0.03-0.19]) || +++ || + || Prototypical high-potency first-generation (''typical'') antipsychotic.
+|-
+| [[Iloperidone]] || 0.69 (0.56-0.84) || - || +/- || + || ++ || ++ || ++ (0.34 [0.22-0.46]) || ++/+ || + || ?
+|-
+| [[Levomepromazine]] || ? || +++ || +++ || ++/+ || ++ || ++ || ? || +++ || +++ || Also used as an analgesic, agitation, anxiety and emesis.
+|-
+| [[Loxapine]] || 0.52 (0.28-0.98)<ref>{{cite journal | vauthors = Chakrabarti A, Bagnall A, Chue P, Fenton M, Palaniswamy V, Wong W, Xia J | title = Loxapine for schizophrenia | journal = The Cochrane Database of Systematic Reviews | issue = 4 | pages = CD001943 | date = October 2007 | pmid = 17943763 | doi = 10.1002/14651858.CD001943.pub2 | editor1-last = Chakrabarti | df = dmy-all | editor1-first = Abhijit }}</ref> || + || ++ || +++ || + || +/- || ? || +++ || ++ || ?
+|-
+| [[Lurasidone]] || 0.77 (0.61-0.96) || - || - || ++/+ || - || - || - (–0.10 [–0.21-0.01]) || ++/+ || - || May be particularly helpful in ameloriating the cognitive symptoms of schizophrenia, likely due to its [[5-HT7 receptor|5-HT<sub>7</sub> receptor]].<ref>{{cite journal | vauthors = Harvey PD, Ogasa M, Cucchiaro J, Loebel A, Keefe RS | title = Performance and interview-based assessments of cognitive change in a randomized, double-blind comparison of lurasidone vs. ziprasidone | journal = Schizophrenia Research | volume = 127 | issue = 1–3 | pages = 188–94 | date = April 2011 | pmid = 21277745 | doi = 10.1016/j.schres.2011.01.004 }}</ref>
+|-
+| [[Melperone]] || ? || - || +/- || - || +/- || +/- || ++ || - || ++/+ || Several smaller low-quality clinical studies have reported its efficacy in the treatment of treatment-resistant schizophrenia. Only approved for use in a few European countries. It is known that off-licence prescribing of melperone is occurring in the United Kingdom.<ref>{{cite journal | vauthors = Röhricht F, Gadhia S, Alam R, Willis M | title = Auditing clinical outcomes after introducing off-licence prescribing of atypical antipsychotic melperone for patients with treatment refractory schizophrenia | journal = TheScientificWorldJournal | volume = 2012 | pages = 1–5 | year = 2012 | pmid = 22566771 | pmc = 3330679 | doi = 10.1100/2012/512047 }}</ref> Is a butyrophenone, low-potency atypical antipsychotic that has been tried as a treatment for [[Parkinson's disease]] psychosis, although with negative results.
+|-
+| [[Molindone]]<ref name = MD>{{cite book | name-list-format = vanc|title=Molindone Hydrochloride|date=30 January 2013|accessdate=5 November 2013|work=Martindale: The Complete Drug Reference|publisher=The Royal Pharmaceutical Society of Great Britain|url=http://www.medicinescomplete.com/mc/martindale/current/7072-k.htm}}</ref> || ? || - || ++/+ || + || - || - || ? || +++ || +/- || Withdrawn from the market. Seems to promote weight loss (which is rather unusual for an antipsychotic seeing how they tend to promote weight gain).<ref name = MD/>
+|-
+| [[Olanzapine]] || 0.46 (0.41-0.52) || + || ++ || + || +++ || +++ || + (0.22 [0.11-0.31]) || + || + || ?
+|-
+| [[Paliperidone]] || 0.48 (0.39-0.58) || - || - || ++/+ (dose-dependent) || ++ || + || - (0.05 [–0.18-0.26]) || +++ || ++ || Active metabolite of risperidone.
+|-
+| [[Perazine]] || 0.62 (0.4-1.10)<ref>{{cite journal | vauthors = Leucht S, Helfer B, Hartung B | title = Perazine for schizophrenia | journal = The Cochrane Database of Systematic Reviews | issue = 1 | pages = CD002832 | date = January 2014 | pmid = 24425538 | doi = 10.1002/14651858.CD002832.pub3 }}</ref>|| ? || ? || ? || ? || ? || ? || ? || ? || Limited data available on adverse effects.
+|-
+| [[Periciazine]] || ? || +++ || +++ || + || ++ || + || ? || +++ || ++ || Also used to treat severe anxiety. Not licensed for use in the US.
+|-
+| [[Perospirone]]<ref>{{cite journal | vauthors = Onrust SV, McClellan K | title = Perospirone | journal = CNS Drugs | volume = 15 | issue = 4 | pages = 329–37; discussion 338 | date = April 2001 | pmid = 11463136 | doi = 10.2165/00023210-200115040-00006}}</ref> || ? || +/- || + || ++/+<ref name = Mart>{{cite book | veditors = Brayfield A |title=Perospirone|work=Martindale: The Complete Drug Reference|publisher=Pharmaceutical Press|location=London, UK|date=23 September 2011|accessdate=3 November 2013|url=http://www.medicinescomplete.com/mc/martindale/current/15232-k.htm}}</ref> || +/- || ? || - || ++/+ || - || Usually grouped with the atypical antipsychotics despite its relatively high propensity for causing extrapyramidal side effects.<ref name = Mart/>
+|-
+| [[Perphenazine]] || 0.30 (0.04, 2.33)<ref>{{cite journal | vauthors = Hartung B, Sampson S, Leucht S | title = Perphenazine for schizophrenia | journal = The Cochrane Database of Systematic Reviews | issue = 3 | pages = CD003443 | date = March 2015 | pmid = 25749632 | doi = 10.1002/14651858.CD003443.pub3 }}</ref> || + || + || +++ || + || + || + || +++ || + || Has additional antiemetic effects.
+|-
+| [[Pimozide]] || 1.01 (0.30 to 3.39)<ref>{{cite journal | vauthors = Mothi M, Sampson S | title = Pimozide for schizophrenia or related psychoses | journal = The Cochrane Database of Systematic Reviews | issue = 11 | pages = CD001949 | date = November 2013 | pmid = 24194433 | doi = 10.1002/14651858.CD001949.pub3 }}</ref> || + || + || + || + || + || +++ || +++ || + || High potency first-generation (''typical'') antipsychotic.
+|-
+| [[Pipotiazine]] || ? || ++ || ++ || ++ || ++ || + || ? || +++ || ++ || Only available in the UK.
+|-
+| [[Prochlorperazine]] || ? || ? || ? || +++ || ? || ? || + || +++ || ? || Primarily used in medicine as an [[antiemetic]].
+|-
+| [[Quetiapine]] || 0.61 (0.52-0.71) || ++/+ || ++ || - || ++ || ++/+ || + (0.17 [0.06-0.29]) || - || ++ || Binds to the [[Dopamine D2 receptor|D<sub>2</sub> receptor]] in a ''hit and run'' fashion. That is it rapidly dissociates from said receptor and hence produces antipsychotic effects but does not bind to the receptor long enough to produce extrapyramidal side effects and hyperprolactinaemia.
+|-
+| [[Remoxipride]] || ? || - || +/- || - || +/- || +/- || - || - || - || Removed from the market amidst concerns about an alarmingly high rate of [[aplastic anaemia]].
+|-
+| [[Risperidone]] || 0.53 (0.46-0.60) || - || ++/+ (dose-dependent) || ++ || ++ || ++/+ || ++ (0.25 [0.15-0.36]) || +++ || ++ || ?
+|-
+| [[Sertindole]] || 0.78 (0.61-0.98) || - || - || - || ++ || ++/+ || +++ (0.90 [0.76-1.02]) || - || +++ || Not licensed for use in the US.
+|-
+| [[Sulpiride]] || 1.00 (0.25-4.00)<ref>{{cite journal | vauthors = Wang J, Sampson S | title = Sulpiride versus placebo for schizophrenia | journal = The Cochrane Database of Systematic Reviews | issue = 4 | pages = CD007811 | date = April 2014 | pmid = 24729184 | doi = 10.1002/14651858.CD007811.pub2 }}</ref>|| - || - || + || + || +/- || + || +++/++ || - || Not licensed for use in the US.
+|-
+| [[Thioridazine]] || 0.67 (0.32-1.40)<ref>{{cite journal | vauthors = Fenton M, Rathbone J, Reilly J, Sultana A | title = Thioridazine for schizophrenia | journal = The Cochrane Database of Systematic Reviews | issue = 3 | pages = CD001944 | date = July 2007 | pmid = 17636691 | doi = 10.1002/14651858.CD001944.pub2 | editor1-last = Reilly | df = dmy-all | editor1-first = Joe }}</ref>|| +++ || +++ || + || ++ || ++ || +++ || +++ || +++ || Dose-dependent risk for degenerative retinopathies.<ref>{{cite journal | vauthors = Fornaro P, Calabria G, Corallo G, Picotti GB | title = Pathogenesis of degenerative retinopathies induced by thioridazine and other antipsychotics: a dopamine hypothesis | journal = Documenta Ophthalmologica. Advances in Ophthalmology | volume = 105 | issue = 1 | pages = 41–9 | date = July 2002 | pmid = 12152801 | doi = 10.1023/A:1015768114192 }}</ref> Found utility in reducing the resistance of multidrug and even extensively resistant strains of [[tuberculosis]] to antibiotics.
+|-
+| [[Tiotixene]] || ? || - || + || +++ || ++ || ++/+ || + || +++ || + || ?
+|-
+| [[Trifluoperazine]] || 0.94 (0.59-1.48)<ref>{{cite journal | vauthors = Marques LO, Lima MS, Soares BG | title = Trifluoperazine for schizophrenia | journal = The Cochrane Database of Systematic Reviews | issue = 1 | pages = CD003545 | year = 2004 | pmid = 14974020 | doi = 10.1002/14651858.CD003545.pub2 | editor1-last = Marques | df = dmy-all | editor1-first = Luciana de Oliveira }}</ref> || +/- || + || +++ || + || +/- || ? || +++ || + || ?
+|-
+| [[Ziprasidone]] || 0.72 (0.59 to 0.86) || - || ++ || + || - || - || ++ (0.41 [0.31 to 0.51]) || ++/+ || + || ?
+|-
+| [[Zotepine]] || 0.69 (0.41 to 1.07) || + || +++ || ++ || +++/++ || +++/++ || ++ || +++ || ++ || Dose-dependent risk of seizures.<ref>{{cite web|title=Zotepine|work=Martindale: The Complete Drug Reference|publisher=Royal Pharmaceutical Society of Great Britain|date=16 August 2013|accessdate=2 November 2013|url=http://www.medicinescomplete.com/mc/martindale/current/2479-d.htm?}}</ref> Not licensed for use in the US.
+|-
+| [[Zuclopenthixol]] || ? || ++ || ++ || +++ || ++ || ++ || ? || +++ || + || Not licensed for use in the US.
+|-
+| colspan=11 style="font-size:88%;" |
+''Note: "Notable" is to mean side-effects that are particularly unique to the antipsychotic drug in question. For example, clozapine is notorious for its ability to cause agranulocytosis. If data on the propensity of a particular drug to cause a particular AE is unavailable an estimation is substituted based on the pharmacologic profile of the drug. ''
+{{col-begin|width=auto}}
+{{col-break}}
+'''Acronyms used:'''
+:AE - [[Adverse effect]]
+:OR - [[Odds ratio]]
+:CI - [[Confidence Interval]]
+:EPSE - [[Extrapyramidal symptoms|Extrapyramidal Side Effect]]
+:QTc - Corrected [[QT interval]]
+:PE - Prolactin elevation
+{{col-break|gap=5em}}
+'''Legend:'''<br/>
+:- very low propensity for this AE
+:+ low propensity/severity for this AE
+:++ moderate propensity/severity for this AE
+:+++ high propensity/severity for this AE
+{{col-end}}
+|}
+{| class="wikitable collapsible collapsed" style="font-size:small; width:100%;"
+! colspan=6 | Efficacy
+|-
+! Generic drug name !! Schizophrenia<ref name=Lancet2009/><ref name = "Leucht_2013" /> !! Mania<ref name = "Lancet 11">{{cite journal | vauthors = Cipriani A, Barbui C, Salanti G, Rendell J, Brown R, Stockton S, Purgato M, Spineli LM, Goodwin GM, Geddes JR | title = Comparative efficacy and acceptability of antimanic drugs in acute mania: a multiple-treatments meta-analysis | journal = Lancet | volume = 378 | issue = 9799 | pages = 1306–15 | date = October 2011 | pmid = 21851976 | doi = 10.1016/S0140-6736(11)60873-8 }}</ref><ref>{{cite journal | vauthors = Citrome L | title = Addressing the need for rapid treatment of agitation in schizophrenia and bipolar disorder: focus on inhaled loxapine as an alternative to injectable agents | journal = Therapeutics and Clinical Risk Management | volume = 9 | issue =  | pages = 235–45 | year = 2013 | pmid = 23723707 | pmc = 3665578 | doi = 10.2147/TCRM.S31484 }}</ref>!! Bipolar depression<ref>{{cite journal | vauthors = Cruz N, Sanchez-Moreno J, Torres F, Goikolea JM, Valentí M, Vieta E | title = Efficacy of modern antipsychotics in placebo-controlled trials in bipolar depression: a meta-analysis | journal = The International Journal of Neuropsychopharmacology | volume = 13 | issue = 1 | pages = 5–14 | date = February 2010 | pmid = 19638254 | doi = 10.1017/S1461145709990344 | hdl = 2445/53243 }}</ref>!! Bipolar maintenance<ref>{{cite journal | vauthors = Popovic D, Reinares M, Goikolea JM, Bonnin CM, Gonzalez-Pinto A, Vieta E | title = Polarity index of pharmacological agents used for maintenance treatment of bipolar disorder | journal = European Neuropsychopharmacology | volume = 22 | issue = 5 | pages = 339–46 | date = May 2012 | pmid = 22000157 | doi = 10.1016/j.euroneuro.2011.09.008 }}</ref><ref>{{cite journal | vauthors = Vieta E, Günther O, Locklear J, Ekman M, Miltenburger C, Chatterton ML, Åström M, Paulsson B | title = Effectiveness of psychotropic medications in the maintenance phase of bipolar disorder: a meta-analysis of randomized controlled trials | journal = The International Journal of Neuropsychopharmacology | volume = 14 | issue = 8 | pages = 1029–49 | date = September 2011 | pmid = 21733231 | doi = 10.1017/S1461145711000885 | url = http://diposit.ub.edu/dspace/bitstream/2445/51726/1/606281.pdf | archiveurl = https://web.archive.org/web/20170818043951/http://diposit.ub.edu/dspace/bitstream/2445/51726/1/606281.pdf | df = dmy-all | deadurl = no | archivedate = 18 August 2017 | hdl = 2445/51726 }}</ref>!! Adjunct in major depression<ref name="MDD">{{cite journal | vauthors = Komossa K, Depping AM, Gaudchau A, Kissling W, Leucht S | title = Second-generation antipsychotics for major depressive disorder and dysthymia | journal = The Cochrane Database of Systematic Reviews | volume =  | issue = 12 | pages = CD008121 | date = December 2010 | pmid = 21154393 | doi = 10.1002/14651858.CD008121.pub2 | df = dmy-all }}</ref>
+|-
+| Amisulpride || +++ || ? || ? || ? || ? (+++ in dysthymia)
+|-
+| Aripiprazole || ++ || ++ || - || ++ (prevents manic and mixed but not depressive episodes) || +++
+|-
+| Asenapine || ++/+ || ++ || ? || ++ || ?
+|-
+| Chlorpromazine || ++ || ? || ? || ? || ?
+|-
+| Clozapine || +++ || ? || ? || ? || ?
+|-
+| Haloperidol || ++ || +++ || ? || ? || ?
+|-
+| Iloperidone || + || ? || ? || ? || ?
+|-
+| Loxapine || +++/++ || +++ (only in the treatment of agitation) || ? || ? || ?
+|-
+| Lurasidone || + || ? || +++ || ? || ?
+|-
+| Melperone || +++ || ? || ? || ? || ?
+|-
+| Olanzapine || +++ || +++/++ || ++ || ++ (most effective at preventing manic/mixed relapse) || ++
+|-
+| Paliperidone || ++ || +++/++ || ? || ? || ?
+|-
+| Perospirone<ref>{{cite journal | vauthors = Kishi T, Iwata N | title = Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials | journal = CNS Drugs | volume = 27 | issue = 9 | pages = 731–41 | date = September 2013 | pmid = 23812802 | doi = 10.1007/s40263-013-0085-7 }}</ref>|| + || ? || ? || ? || ?
+|-
+| Quetiapine || ++ || ++ || +++ || +++ || ++
+|-
+| Risperidone || +++ || +++ || - || ++ || +++
+|-
+| Sertindole || ++ || ? || ? || ? || ?
+|-
+| Ziprasidone || ++/+ || + || ? || + || ?
+|-
+| Zotepine || ++ || ? || ? || ? || ?
+|}
+{| class="wikitable sortable collapsible collapsed" style="font-size:80%; text-align:center; width:100%;"
+! colspan="19" style="font-size:120%;" | Binding affinity
+|-
+! colspan="19" | K<sub>i</sub> [nM] toward cloned human receptors (unless otherwise specified)<ref group = Note>Bolded drug names indicates drugs that are metabolites of clinically-marketed antipsychotics</ref>
+|-
+! Drug name<ref name = "GG">{{cite book | name-list-format = vanc |editor1-last=Brunton |editor1-first=L. L. |editor2-last=Chabner |editor2-first=Bruce |editor3-last=Knollmann |editor3-first=Björn C. |title=Goodman & Gilman's The Pharmacological Basis of Therapeutics |edition=12th |location=New York |publisher=McGraw-Hill |year=2011 |isbn=978-0-07-162442-8|title-link=Goodman & Gilman's The Pharmacological Basis of Therapeutics }}</ref><ref>{{cite web|title=PDSP K<sub>i</sub> Database |work=Psychoactive Drug Screening Program (PDSP) | vauthors = Roth BL, Driscol J | url = http://pdsp.med.unc.edu/pdsp.php |publisher=University of North Carolina at Chapel Hill and the United States National Institute of Mental Health |accessdate=11 November 2013 |date=12 January 2011 |deadurl=yes |archiveurl=https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php |archivedate=8 November 2013 |df=dmy }}</ref>!! SERT !! 5-HT<sub>1A</sub> !! 5-HT<sub>2A</sub> !! 5-HT<sub>2C</sub> !! 5-HT<sub>6</sub> !! 5-HT<sub>7</sub> !! α<sub>1A</sub> !! α<sub>2A</sub> !! α<sub>2C</sub> !! NET !! D<sub>1</sub> !! D<sub>2</sub> !! D<sub>3</sub> !! D<sub>4</sub> !! 5-HT<sub>2A</sub>/D<sub>2</sub> !!H<sub>1</sub> !! M<sub>1</sub> !! M<sub>3</sub>
+|-
+| Amisulpride || >10,000 || >10,000 || 8,304 || >10,000 || 4,154 || 73.5 || >10,000 || 1,114 || 1,540 || >10,000 || >10,000 || 2.2 || 2.4 || 2,370 || 3774.5 || >10,000 || >10,000 || >10,000
+|-
+| Aripiprazole || 1,081 || 5.6 || 8.7 || 22.4 || 642.4 || 9.97 || 25.85 || 74.1 || 37.63 || 2091.5 || 1,173.5 || 1.64 || 5.35 || 514 || 5.3 || 27.93 || 6,778  || 4,678
+|-
+| Asenapine<ref name="pmid18308814">{{cite journal | vauthors = Shahid M, Walker GB, Zorn SH, Wong EH | title = Asenapine: a novel psychopharmacologic agent with a unique human receptor signature | journal = Journal of Psychopharmacology | volume = 23 | issue = 1 | pages = 65–73 | date = January 2009 | pmid = 18308814 | doi = 10.1177/0269881107082944 }}</ref> || ND || 2.5 || 0.06 || 0.03 || 0.25 || 0.13 || 1.2 || 1.2 || 1.2 || ND || 1.4 || 1.3 || 0.42 || 1.1 || 0.0462 || 1.0 || 8,128 || 8,128
+|-
+| Blonanserin<ref name="Ishiyama_2007">{{cite journal | vauthors = Ishiyama T, Tokuda K, Ishibashi T, Ito A, Toma S, Ohno Y | title = Lurasidone (SM-13496), a novel atypical antipsychotic drug, reverses MK-801-induced impairment of learning and memory in the rat passive-avoidance test | journal = European Journal of Pharmacology | volume = 572 | issue = 2–3 | pages = 160–70 | date = October 2007 | pmid = 17662268 | doi = 10.1016/j.ejphar.2007.06.058 }}</ref> || ND || 804 || 0.812 || 26.4 || 41.9 || 183 || 26.7 (RB) || 530 (RC) || ND || ND || 1,070 || 0.142 || 0.494 || 150 || 5.72 || 765 || 100 ||ND
+|-
+| '''''N-DEBN'''''<ref name="Deeks, ED; Keating, GM 65–84"/> || ND || ND || 1.28 || 4.50 || 5.03 || 206 (RC) || ND || ND || ND || ND || 1,020 || 1.38 || 0.23 || ND || 0.93 || ND || ND || ND
+|-
+| Chlorpromazine || 1,296 || 2,115.5 || 4.5 || 15.6 || 17.0 || 28.4 || 0.28 || 184 || 46 || 2,443 || 76.3 || 1.40 || 4.65 || 5.33 || 3.21 || 3.09 || 32.3 ||57.0
+|-
+| Clozapine || 1,624 || 123.7 || 5.35 || 9.44 || 13.5 || 17.95 || 1.62 || 37 || 6.0 || 3,168 || 266.3 || 157 || 269.1 || 26.4 || 0.0341 || 1.13 || 6.17 ||19.25
+|-
+| '''''Norclozapine''''' || 316.6 || 13.9 || 10.9 || 11.9 (RC) || 11.6 || 60.1 || 104.8 || 137.6 || 117.7 || 493.9 || 14.3 || 94.5 || 153 || 63.94 || 0.115 || 3.4 || 67.6 ||95.7
+|-
+| ''cis''-Flupenthixol || ND || 8,028 || 87.5 (HFC) || 102.2 (RC) || ND || ND || ND || ND || ND || ND || 3.5 || 0.35 || 1.75 || 66.3 || 250 || 0.86 || ND ||ND
+|-
+| Fluphenazine || 5,950 || 1,039.9 || 37.93 || 982.5 || 34.67 || 8.00 || 6.45 || 314.1 || 28.9 || 3,076 || 17.33 || 0.30 || 1.75 || 40.0 || 126.4 || 14.15 || 1,095 || 1,441
+|-
+| Haloperidol || 3,256 || 2,066.83 || 56.81 || 4,801 || 5,133 || 377.6 || 12.0 || 801.5 || 403 || 2,112 || 121.8 || 0.7 || 3.96 || 2.71 || 81.2 || 1698 || >10,000 || >10,000
+|-
+| Iloperidone || ND || 93.21 || 1.94 || 147 || 63.09 || 112 || 0.3 || 160 || 16.2 || 1479 || 129.32 || 10.86 || 10.55 || 13.75 || 0.179 || 12 || 4,898 || >10,000
+|-
+| Loxapine || >10,000 || 2,456 || 6.63 || 13.25 || 31.0 || 87.6 || 31.0 || 150.9 || 80.0 || 5,698 || 54 || 28.1 || 19.33 || 7.80 || 0.236 || 4.90 || 119.45 || 211.33
+|-
+| '''''Amoxapine''''' || 58 || ND || 0.5 || 2.0 (RC) || 50 || 40.21 || 50 || ND || ND || 16 || ND || 20.8 || 21.0 || 21.0 || 0.0240 || 25 || 1,000 || 1,000
+|-
+| Lurasidone<ref name="Ishiyama_2007"/><ref name="pmid20404009">{{cite journal | vauthors = Ishibashi T, Horisawa T, Tokuda K, Ishiyama T, Ogasa M, Tagashira R, Matsumoto K, Nishikawa H, Ueda Y, Toma S, Oki H, Tanno N, Saji I, Ito A, Ohno Y, Nakamura M | title = Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 334 | issue = 1 | pages = 171–81 | date = July 2010 | pmid = 20404009 | doi = 10.1124/jpet.110.167346 }}</ref> || ND || 6.8 || 2.0 || 415 || ND || 0.5 || 48 || 1.6 || 10.8 || ND || 262 || 1.7 || ND || ND || 1.18 || >10,000 || >10,000 || >10,000
+|-
+| Melperone || ND || 2,200 (HB) || 230 || 2,100 (HB) || 1,254 (RC) || 578 (HB) || 180 (HB) || 150 (HB) || ND || ND || ND || 194 || 8.95 || 555 || 1.186 || 580 || >10,000 || >10,000
+|-
+| Molindone || ND || 3,797 || 3773 || >10,000 || 1,008 || 3,053 || 2,612 || 1,097 || 172.6 || ND || ND || 6.0 || 72.5 || 2,950 || 628.83 || 2,130 || ND || >10,000
+|-
+| Olanzapine || 3,676 || 2282 || 3.73 || 10.2 || 8.07 || 105.2 || 112 || 314 || 28.9 || >10,000 || 70.33 || 34.23 || 47.0 || 14.33 || 0.109 || 2.19 || 2.5 || 56.33
+|-
+| Paliperidone || 3,717 || 616.6 || 0.71 || 48 || 2,414 || 2.7 || 2.5 || 17.35 || 7.35 || >10,000 || 41.04 || 0.7 || 0.5 || 54.3 || 1.104 || 18.8 || >10,000 || >10,000
+|-
+| Perphenazine || ND || 421 || 5.6 || 132 || 17 || 23 || 10 || 810.5 || 85.2 || ND || ND || 0.14 || 0.13 || 17 || 40 || 8 || 1,500 || 1,848
+|-
+| Pimozide || ND || 650 || 48.35 || 2,112 || 71 || 0.5 || 197.7 || 1,593 || 376.5 || ND || >10,000 || 1.45 || 0.25 || 1.8 || 33.34 || 692.2 || 800 (HB) || 1,955
+|-
+| Prochlorperazine || ND || 5,900 (HC) || 15 (HC) || 122 || 148 (RC) || 196 (RC) || 23.8 (HB) || 1,694.91 (HB) || ND || ND || ND || 0.65 || 2.90 || 5.40 || 23.1 || 18.86 (HB) || 555.55 (HB) || ND
+|-
+| Quetiapine || >10,000 || 394.2 || 912 || 1,843 || 948.75 || 307.6 || 22 || 3,630 || 28.85 || >10,000 || 994.5 || 379 || 340 || 2,019 || 2.41 || 6.90 || 489 || 1631.5
+|-
+| '''''Norquetiapine'''''<ref name="pmid24062697">{{cite journal | vauthors = López-Muñoz F, Alamo C | title = Active metabolites as antidepressant drugs: the role of norquetiapine in the mechanism of action of quetiapine in the treatment of mood disorders | journal = Frontiers in Psychiatry | volume = 4 | issue =  | pages = 102 | date = September 2013 | pmid = 24062697 | pmc = 3770982 | doi = 10.3389/fpsyt.2013.00102 }}</ref> || ND || 45 || 48 || 107 || ND || 76 || 144 || 237 || ND || 12 || 99.8 (RC) || 196 || ND || ND || 0.245 || 3.5 || 38.3 (RC) || ND
+|-
+| Risperidone || >10,000 || 422.88 || 0.17 || 12 || 2057.17 || 6.6 || 5 || 16.5 || 1.3 || >10,000 || 243.53 || 3.57 || 2.0 || 4.66 || 0.0476 || 20.05 || >10,000 || >10,000
+|-
+| Sertindole || ND || 280 || 0.39 || 0.9 || 5.4 || 28 || 1.8 || 640 || 450 || ND || ND || 2.35 || 2.30 || 4.92 || 0.166 || 130 || >5,000 || 2,692
+|-
+| Sulpiride || ND || >10,000 || >10,000 (RC) || >10,000 (RC) || 5,000 (RC) || 4,000 (RC) || >10,000 (RB) || 4,893 (RB) || ND || ND || >10,000 || 9.80 || 8.05 || 54 || >1,000 || >10,000 (RB) || >10,000 (RB) || >10,000 (RB)
+|-
+| Thioridazine || 1,259 || 144.35 || 27.67 || 53 || 57.05 || 99 || 3.15 || 134.15 || 74.9 || 842 || 94.5 || 2.20 || 1.50 || 6.00 || 12.58 || 16.5 || 12.8 || 29
+|-
+| Tiotixene || 3,878|| 410.2 || 50 || 1355.5 || 245.47 || 15.25 || 11.5 || 79.95 || 51.95 || >10,000 || 51 || 0.12 || 0.40 || 203 || 416.7 || 8 || >10,000 || >10,000
+|-
+| Trifluoperazine || ND || 950 || 74 || 378 || 144 || 290.8 || 24 || 653.7 || 391.5 || ND || ND || 1.12 || ND || 38.1 || 66.07 || 63 || ND || 1,001
+|-
+| Ziprasidone || 112 || 54.67 || 0.73 || 13 || 60.95 || 6.31 || 18 || 160 || 68 || 44 || 30 || 4.35 || 7.85 || 52.9 || 0.1678 || 62.67 || >10,000 || >10,000
+|-
+| Zotepine || 151 || 470.5 || 2.7 || 3.2 || 6 || 12 || 7 || 208 || 106 || 530 || 71 || 25 || 6.4 || 18 || 0.108 || 3.21 || 18 || 73
+|-
+| colspan=19 style="font-size:88%;" |
+'''Acronyms used:'''
+{{col-begin|width=auto}}
+{{col-break}}
+:HFC - Human frontal cortex receptor
+:RB - Rat brain receptor
+:RC - Cloned rat receptor
+:ND - No data
+{{col-break|gap=2em}}
+:HB - Human brain receptor
+:HC - Human cortex receptor
+:N-DEBN - N-desethylblonanserin
+{{col-end}}
+|}
+{| class="wikitable collapsible collapsed" style="font-size:85%; width:100%;"
+! colspan=11 style="font-size:115%;" | Pharmacokinetics
+|-
+! Drug<ref>{{cite web|title=Medscape home page|publisher=[[WebMD]]|website=[[Medscape]]|url=http://reference.medscape.com/medscapetoday|deadurl=no|archiveurl=https://web.archive.org/web/20131113205740/http://reference.medscape.com/medscapetoday|archivedate=13 November 2013|df=dmy-all}}</ref><ref>{{cite web|title=Therapeutic Goods Administration home page|work=[[Therapeutic Goods Administration]]|publisher=[[Department of Health (Australia)]]|url=https://www.ebs.tga.gov.au/|deadurl=no|archiveurl=https://web.archive.org/web/20130421054308/https://www.ebs.tga.gov.au/|archivedate=21 April 2013|df=dmy-all}}</ref><ref name=DM>{{cite web|title=Daily Med home page|work=[[Daily Med]]|publisher=United States National Library of Medicine|url=http://dailymed.nlm.nih.gov/dailymed/index.cfm|deadurl=no|archiveurl=https://web.archive.org/web/20130618062135/http://www.dailymed.nlm.nih.gov/dailymed/index.cfm|archivedate=18 June 2013|df=dmy-all}}</ref><ref>{{cite web|title=electronic Medicines Compendium (eMC) home page|work=electronic Medicines Compendium|publisher=Datapharm|url=http://www.medicines.org.uk/emc/|deadurl=no|archiveurl=https://web.archive.org/web/20131127215911/http://www.medicines.org.uk/emc/|archivedate=27 November 2013|df=dmy-all}}</ref>!! [[Bioavailability]] !! [[Biological half-life|t<sub>1/2</sub>]] parent drug <br/>(active metabolite) !! Protein binding !! [[Pharmacokinetics#Metrics|t<sub>max</sub>]] !![[Pharmacokinetics#Metrics|C<sub>max</sub>]] !! [[Volume of distribution|V<sub>d</sub>]] !! Excretion !! Routes !! Metabolism enzymes<ref name = GG/> !! Active metabolites
+|-
+| [[Amisulpride]] || 48% || 12&nbsp;h || 16% || 3-4&nbsp;h || {{nowrap|54 ± 4 ng/mL}} || 5.8&nbsp;L/kg || Faeces (20%), urine (50%, when given IV) || Oral || ? ||None
+|-
+| [[Aripiprazole]] || 87% (Oral), 100% (IM) || 75&nbsp;h (94&nbsp;h) || 99% || 3-5&nbsp;h || ? || 4.9&nbsp;L/kg || Faeces (55%), urine (25%) || Oral, [[Intramuscular|IM]] (including depot) || [[CYP2D6]], [[CYP3A4]] || Dehydroaripiprazole
+|-
+| [[Asenapine]] || 35% (sublingual) || 24&nbsp;h || 95% || 0.5-1.5&nbsp;h || 4&nbsp;ng/mL || 20-25&nbsp;L/kg || Urine (50%), faeces (40%) || Sublingual ||[[CYP1A2]], [[UGT1A4]], [[CYP2D6]] || None
+|-
+| [[Blonanserin]]<ref name="Deeks, ED; Keating, GM 65–84"/><ref name="Tenjin, T; Miyamoto, S; Ninomiya, Y; Kitajima, R; Ogino, S; Miyake, N; Yamaguchi, N 2013 587–594"/><ref>{{cite journal | vauthors = Wen YG, Shang DW, Xie HZ, Wang XP, Ni XJ, Zhang M, Lu W, Qiu C, Liu X, Li FF, Li X, Luo FT | title = Population pharmacokinetics of blonanserin in Chinese healthy volunteers and the effect of the food intake | journal = Human Psychopharmacology | volume = 28 | issue = 2 | pages = 134–41 | date = March 2013 | pmid = 23417765 | doi = 10.1002/hup.2290 }}</ref> || 55% || 10.7-16.2&nbsp;h (single dosing), 67.9&nbsp;h (repeated dosing) || ≥&nbsp;99.7% || 1.5-2&nbsp;h || 0.14-0.76&nbsp;ng/mL (0.57&nbsp;ng/mL for repeated dosing) || 8560-9500 L || Urine (59%), faeces (30%) || Oral || [[CYP3A4]] || N-desethylblonanserin
+|-
+| [[Chlorpromazine]] || 20% || 30&nbsp;h || 92-97% || ? || ? || 20&nbsp;L/kg || Urine || Oral, [[Intramuscular|IM]], [[Intravenous|IV]] ||[[CYP2D6]] || Several active metabolites
+|-
+| [[Clozapine]] || 50-60% || 12&nbsp;h || 97% || 1.5-2.5&nbsp;h || 102-771&nbsp;ng/mL || 4.67&nbsp;L/kg || Urine (50%), faeces (30%) || Oral || [[CYP1A2]], [[CYP2D6]], [[CYP3A4]] || [[Norclozapine]]
+|-
+| [[Droperidol]] || ? || 2&nbsp;h (8-12&nbsp;h) || Extensive || 60 min (IM) || ? || 2&nbsp;L/kg (adults), 0.58&nbsp;L/kg (children) || Urine (75%), faeces (22%) || [[Intramuscular|IM]], [[Intravenous|IV]] || ? || None
+|-
+| [[Flupentixol]] || 40-55% (Oral) || 35&nbsp;h || ? || 7 days (depot) || ? || 12-14&nbsp;L/kg || Urine || Oral, IM (including depot) || ? || None
+|-
+| [[Fluphenazine]] || 2.7% (Oral) || 14-16&nbsp;h, 14 days (depot) || ? || 2&nbsp;h (Oral), 8-10&nbsp;h (depot) || ? || ? || Urine, faeces || Oral, IM (including depot) || ? || None
+|-
+| [[Haloperidol]] || 60-70% (Oral) || 10-20&nbsp;h (short-acting IM), 3 weeks (depot) || 92% || 2-6&nbsp;h (Oral), 10-20 min (short-acting IM), 6–7 days (depot) || ? || 8-18&nbsp;L/kg || Urine (30%), faeces (15%) || Oral, IM, IV || [[CYP3A4]] || None
+|-
+| [[Iloperidone]] || 96% || ? || 95% || 2-4&nbsp;h || ? || 1340-2800 L || Urine (45-58%), faeces (20-22%) || Oral || [[CYP3A4]], [[CYP2D6]]|| None notable.
+|-
+| [[Levomepromazine]] || ? || 30&nbsp;h || ? || 2-3&nbsp;h || ? || ? || Urine, faeces || IM, IV || ? || Methotrimeprazine sulfoxide
+|-
+| [[Loxapine]] || High || 6-8&nbsp;h (Inhaled), 4-12&nbsp;h (Oral) || 96.6% || 2 min (inhaled), 2&nbsp;h (oral), 5&nbsp;h (IM) || 257&nbsp;ng/mL (inhaled), 6-13&nbsp;ng/mL (Oral) || ? || Urine (56-70%), faeces [Only oral data available] || Oral, IM, Inhalation || [[CYP1A2]], [[CYP3A4]], [[CYP2D6]]|| [[Amoxapine]] (a tricyclic antidepressant), 7-OH loxapine, 8-OH loxapine
+|-
+| [[Lurasidone]] || 9-19% || 18&nbsp;h || 99% || 1-3&nbsp;h || ? || 6173 L || Urine (9%), faeces (80%) || Oral || [[CYP3A4]] || 2 active
+|-
+| [[Melperone]]<ref>{{cite journal | vauthors = Borgström L, Larsson H, Molander L | title = Pharmacokinetics of parenteral and oral melperone in man | journal = European Journal of Clinical Pharmacology | volume = 23 | issue = 2 | pages = 173–6 | year = 1982 | pmid = 7140807 | doi = 10.1007/BF00545974 }}</ref> || 54% (Oral via syrup), 65% (Oral via tablets), 87% (IM) || 2.1-6.4&nbsp;h (Oral), {{nowrap|6.6 ± 3.7 h}} (IM) || 50% || 1.6-2.4&nbsp;h (Oral, tablets), 1&nbsp;h (Oral, syrup) || {{nowrap|1132 ± 814 ng/mL}} (25&nbsp;mg, orally), 2228-3416&nbsp;ng/mL (50&nbsp;mg, orally), {{nowrap|89539 ± 37001 ng/mL}} (100&nbsp;mg, orally) || {{nowrap|9.9 ± 3.7 L/kg}} (10&nbsp;mg), {{nowrap|7 ± 1.61 L/kg}} (20&nbsp;mg) || Urine (70% as metabolites, 5.5-10.4% as parent drug) || Oral, IM || ? || None
+|-
+| [[Olanzapine]] || 87% (Oral) || 30&nbsp;h || 93% || 6&nbsp;h (Oral), 15-45 min (short-acting IM), 7 days (depot) || 4-20.4&nbsp;mg/mL<ref>{{cite journal | vauthors = Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM | title = Olanzapine. Pharmacokinetic and pharmacodynamic profile | journal = Clinical Pharmacokinetics | volume = 37 | issue = 3 | pages = 177–93 | date = September 1999 | pmid = 10511917 | doi = 10.2165/00003088-199937030-00001 }}</ref> || 1000 L || Urine (57%), faeces (30%) || Oral, IM (including depot) || [[CYP1A2]] || None
+|-
+| [[Paliperidone]] || 28% (Oral) || 23&nbsp;h (Oral), 25–49 days (IM) || 74% || 24&nbsp;h (Oral), 13 days (IM) || 8.85-11.7&nbsp;ng/mL<ref>{{cite journal | vauthors = Vermeir M, Naessens I, Remmerie B, Mannens G, Hendrickx J, Sterkens P, Talluri K, Boom S, Eerdekens M, van Osselaer N, Cleton A | title = Absorption, metabolism, and excretion of paliperidone, a new monoaminergic antagonist, in humans | journal = Drug Metabolism and Disposition | volume = 36 | issue = 4 | pages = 769–79 | date = April 2008 | pmid = 18227146 | doi = 10.1124/dmd.107.018275 | df = dmy-all }}</ref> || 390-487 L || Urine (80%), faeces (11%) || Oral, IM (depot) ||[[CYP3A4]], [[CYP2D6]] || None
+|-
+| [[Periciazine]] || ? || 12&nbsp;h || ? || 2&nbsp;h || 150&nbsp;ng/mL || ? || Urine || Oral || ? || ?
+|-
+| [[Perospirone]]<ref name="CNS Drugs" /> || ? || 1.9-2.5&nbsp;h || 92% || 1.5&nbsp;h || 5.7&nbsp;ng/mL || ? ||Urine (0.4% as unchanged drug) || Oral || ? || None
+|-
+| [[Perphenazine]] || ? || 9-12&nbsp;h (10-19&nbsp;h) || ? || 1-3&nbsp;h; 2-4&nbsp;h (metabolite) || 0.984&nbsp;ng/mL; 0.509&nbsp;ng/mL || ? || Urine, faeces ||Oral || [[CYP2D6]] || 7-OH perphenazine
+|-
+| [[Pimozide]] || 40-50% || 55&nbsp;h || ? || 6-8&nbsp;h || 4-19&nbsp;ng/mL (dose-dependent) || ? || Urine || Oral || [[CYP3A4]], [[CYP2D6]] || None
+|-
+| [[Prochlorperazine]] || 12.5% || 6.8-9&nbsp;h || High || ? || ? || 12.9-17.7 L/h || Urine, bile || Oral, IM, IV || ? || N-desmethylprochlorperazine
+|-
+| [[Quetiapine]] || 100% || 6&nbsp;h (IR), 7&nbsp;h (XR); active metabolite: 12&nbsp;h || 83% || 1.5&nbsp;h (IR), 6&nbsp;h (XR) || @ 250&nbsp;mg q8hr 778&nbsp;ng/mL (male), 879&nbsp;ng/mL (female)<ref>{{cite journal | vauthors = DeVane CL, Nemeroff CB | title = Clinical pharmacokinetics of quetiapine: an atypical antipsychotic | journal = Clinical Pharmacokinetics | volume = 40 | issue = 7 | pages = 509–22 | year = 2001 | pmid = 11510628 | doi = 10.2165/00003088-200140070-00003 }}</ref> || 6-14&nbsp;L/kg || Urine (73%), faeces (20%) || Oral || [[CYP3A4]] || Norquetiapine (a [[norepinephrine reuptake inhibitor]] and [[5-HT1A receptor|5-HT<sub>1A</sub> receptor]] partial agonist)
+|-
+| [[Risperidone]] || 70% || 3-17&nbsp;h (24&nbsp;h) || 90% (active metabolite: 77%) || 3-17&nbsp;h || ? || 1-2&nbsp;L/kg || Urine (70%), faeces (14%) ||Oral, IM (including depot) || [[CYP2D6]] || [[Paliperidone]]
+|-
+| [[Sertindole]] || ? || 3 days || 99.5% || 10&nbsp;h || ? || 20&nbsp;L/kg || Urine (4%), faeces (46-56%) || Oral || [[CYP2D6]] || None
+|-
+| [[Sulpiride]]<ref>{{cite journal | vauthors = Wiesel FA, Alfredsson G, Ehrnebo M, Sedvall G | title = The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects | journal = European Journal of Clinical Pharmacology | volume = 17 | issue = 5 | pages = 385–91 | date = May 1980 | pmid = 7418717 | doi = 10.1007/BF00558453 }}</ref> || 27 ± 9% || 8&nbsp;h || 40% || 3-6&nbsp;h || ? || {{nowrap|2.72 ± 0.66 L/kg}} || Urine, faeces || Oral || ? || None
+|-
+| [[Thioridazine]] || ? || 24&nbsp;h || 95% || ? || ? || ? || ? || Oral || [[CYP2D6]] || None
+|-
+| [[Tiotixene]] || ? || 24&nbsp;h || 90% || ? || ? || ? || ? || Oral || [[CYP1A2]] || None
+|-
+| [[Trifluoperazine]] || ? || 24&nbsp;h || ? || ? || ? || ? || ? || Oral || ? || None
+|-
+| [[Ziprasidone]] || 60% (Oral), 100% (IM) || 7&nbsp;h (Oral), 2-5&nbsp;h (IM) || 99% || 6-8&nbsp;h (Oral), ≤ 60 min (IM) || ? || 1.5&nbsp;L/kg || Faeces (66%), urine (20%) || Oral, IM || [[CYP3A4]], [[CYP1A2]] || None
+|-
+| [[Zotepine]]<ref>{{cite journal|title=Zotepine: A Review of its Pharmacodynamic and Pharmacokinetic Properties and Therapeutic Efficacy in the Management of Schizophrenia|journal=CNS Drugs|volume=9|issue=2|pages=153–175|doi=10.2165/00023210-199809020-00006|date=January 1998| vauthors = Prakash A, Lamb HM }}</ref><ref>Product Information: Nipolept(R), zotepine. Klinge Pharma GmbH, Munich, 1996.</ref> || 7-13%|| 13.7-15.9&nbsp;h (12&nbsp;h) || 97% || 1-4&nbsp;h || 31-240 || 10&nbsp;L/kg || Urine (17%) || Oral || [[CYP1A2]], [[CYP3A4]] || Norzotepine (a norepinephrine reuptake inhibitor)
+|-
+| [[Zuclopenthixol]] || 49% || 20&nbsp;h || 98% || 2-12&nbsp;h (mean: 4&nbsp;h) || ? || 20&nbsp;L/kg || Faeces, urine (10%) || Oral, IM (including depot)|| [[CYP2D6]] || None
+|}
 == Note ==

Neurolettico: differenze tra le versioni

Versione delle 21:43, 7 apr 2019

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