Portal:Antipsychotics
Portal maintenance status: (October 2018)
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Introduction
Antipsychotics, also known as neuroleptics or major tranquilizers, are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder. They are increasingly being used in the management of non-psychotic disorders. Antipsychotics are usually effective in relieving symptoms of psychosis in the short term.
The long-term use of antipsychotics is associated with side effects such as involuntary movement disorders, gynecomastia, and metabolic syndrome. They are also associated with increased mortality in elderly people with dementia.
Selected general articles
Blonanserin, sold under the brand name Lonasen, is a relatively new atypical antipsychotic (approved by PMDA in January 2008) commercialized by Dainippon Sumitomo Pharma in Japan and Korea for the treatment of schizophrenia. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension. As with many second-generation (atypical) antipsychotics it is significantly more efficacious in the treatment of the negative symptoms of schizophrenia compared to first-generation (typical) antipsychotics such as haloperidol. Read more...
Quetiapine, marketed as Seroquel among other names, is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder. It is also sometimes used as a sleep aid due to its sedating effect, but this use is not recommended. It is taken by mouth.
Common side effects include sleepiness, constipation, weight gain, and dry mouth. Other side effects include low blood pressure with standing, seizures, prolonged erection, high blood sugar, and neuroleptic malignant syndrome. In elderly people with dementia, its use increases the risk of death. Use during the later part of pregnancy may result in a movement disorder in the baby for a period of time after birth. Quetiapine is believed to work by blocking a number of receptors including serotonin and dopamine receptors. Read more...
Diphenylbutylpiperidines are a class of typical antipsychotic drugs which were all synthesized, developed, and marketed by Janssen Pharmaceutica.
They include:- Clopimozide (R-29,764)
- Fluspirilene (Redeptin)
- Penfluridol (Semap, Micefal, Longoperidol)
- Pimozide (Orap)
Flupentixol (INN), also known as flupenthixol (former BAN), marketed under brand names such as Depixol and Fluanxol is a typical antipsychotic drug of the thioxanthene class. It was introduced in 1965 by Lundbeck. In addition to single drug preparations, it is also available as flupentixol/melitracen—a combination product containing both melitracen (a tricyclic antidepressant) and flupentixol.
Flupentixol is not approved for use in the United States. It is, however, approved for use in the UK, Australia, Canada, Russian Federation, South Africa, New Zealand, Philippines and various other countries. Read more...
Clocapramine (Clofekton, Padrasen), also known as 3-chlorocarpipramine, is an atypical antipsychotic of the imidobenzyl class which was introduced in Japan in 1974 by Yoshitomi for the treatment of schizophrenia. In addition to psychosis, clocapramine has also been used to augment antidepressants in the treatment of anxiety and panic.
Clocapramine has been reported to act as an antagonist of the D2, 5-HT2A, α1-adrenergic, and α2-adrenergic receptors, and does not inhibit the reuptake of either serotonin or norepinephrine. It has also been shown to have affinity for the σ receptors. Clocapramine's affinity for the 5-HT2A receptor is greater than that for the D2 receptor and it has a lower propensity for inducing extrapyramidal symptoms compared to typical antipsychotics, thus underlying its atypical nature. Read more...
Loxapine (several trade names worldwide) is a typical antipsychotic medication, used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines). Several researchers have argued that loxapine may behave as an atypical antipsychotic.
Loxapine may be metabolized by N-demethylation to amoxapine, a tetracyclic antidepressant. Read more...
Prochlorperazine is a dopamine (D2) receptor antagonist that belongs to the phenothiazine class of antipsychotic agents that are used for the antiemetic treatment of nausea and vertigo. It is also a highly potent typical antipsychotic, 10–20 times more potent than chlorpromazine. It is also used to treat migraine headaches. Intravenous administration can be used to treat status migrainosus. Read more...
Perospirone (Lullan) is an atypical antipsychotic of the azapirone family. It was introduced in Japan by Dainippon Sumitomo Pharma in 2001 for the treatment of schizophrenia and acute cases of bipolar mania. Read more...
Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain. It is used to treat a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. A derivative of benzamide, tiapride is chemically and functionally similar to other benzamide antipsychotics such as sulpiride and amisulpride known for their dopamine antagonist effects. Read more...
Zotepine (brand names: Losizopilon (JP), Lodopin (ID, JP), Setous (JP), Zoleptil (CZ, PT, TR, UK†); where † indicates a formulation that has been discontinued) is an atypical antipsychotic drug indicated for acute and chronic schizophrenia. It has been used in Germany since 1990 (although it has been discontinued in Germany) and Japan since 1982.
Zotepine is not approved for use in the United States, United Kingdom, Australia, Canada or New Zealand. Read more...
Butyrophenone is a chemical compound; some of its derivatives (called commonly butyrophenones) are used to treat various psychiatric disorders such as schizophrenia, as well as acting as antiemetics.
Examples of butyrophenones include:- Haloperidol, the most widely used classical antipsychotic drug in this class
- Benperidol, the most potent commonly used antipsychotic (200 times more potent than chlorpromazine)
- Droperidol, a commonly used antiemetic for postoperative nausea and vomiting
Ziprasidone, sold under the brand name Geodon among others, is an atypical antipsychotic that is used for the treatment of schizophrenia as well as acute mania and mixed states associated with bipolar disorder. Its immediate release intramuscular injection form is approved for acute agitation in people with schizophrenia. Ziprasidone is also used off-label for depression, bipolar maintenance, and post-traumatic stress disorder (PTSD).
Common side effects include dizziness, drowsiness, dry mouth, and twitches. Although it can also cause weight gain, the risk is much lower than for other antipsychotics. Read more...
Zuclopenthixol (brand names Cisordinol, Clopixol, Acuphase), also known as zuclopentixol, is a medication used to treat schizophrenia and other psychoses. It is classed, pharmacologically, as a typical antipsychotic. Chemically it is a thioxanthene. It is the cis-isomer of clopenthixol (Sordinol, Ciatyl). Clopenthixol was introduced in 1961, while zuclopenthixol was introduced in 1978.
Zuclopenthixol is a D1 and D2 antagonist, α1-adrenergic and 5-HT2 antagonist. While it is approved for use in Australia, Canada, Ireland, India, New Zealand, Singapore, South Africa and the UK it is not approved for use in the United States. Read more...
Droperidol /droʊˈpɛrIdɔːl/ (Inapsine, Droleptan, Dridol, Xomolix, Innovar [combination with fentanyl]) is an antidopaminergic drug used as an antiemetic (that is, to prevent or treat nausea) and as an antipsychotic. Droperidol is also often used as a sedative in intensive-care treatment. Read more...
Tricyclics are chemical compounds that contain three interconnected rings of atoms.
Many compounds have a tricyclic structure, but in pharmacology, the term has traditionally been reserved to describe heterocyclic drugs. Among these are antidepressants, antipsychotics, anticonvulsants, and antihistamines (as antiallergens, anti-motion sickness drugs, antipruritics, and hypnotics/sedatives) of the dibenzazepine, dibenzocycloheptene, dibenzothiazepine, dibenzothiepin, phenothiazine, and thioxanthene chemical classes, and others. Read more...
Lurasidone (/ljʊəˈræsɪdoʊn/; trade name Latuda) is an atypical antipsychotic developed by Dainippon Sumitomo Pharma and marketed by Sunovion in the U.S. It has been an FDA approved treatment for schizophrenia since 2010 and for treating depressive episodes in adults with bipolar I disorder since 2013, and is frequently prescribed for the treatment of major depressive disorder (MDD). It can be used alone or in combination with mood stabilizers such as lithium or valproate (e.g., Depakote). Read more...
Thioxanthene is a chemical compound in which the oxygen atom in xanthene is replaced with a sulfur atom. It is also related to phenothiazine. Several of its derivatives are used as typical antipsychotics in the treatment of schizophrenia and other psychoses. Read more...
Trifluoperazine, sold under a number of brand names, is a typical antipsychotic primarily used to treat schizophrenia. It may also be used short term in those with generalized anxiety disorder but is less preferred to benzodiazepines. It is of the phenothiazine chemical class. Read more...
Thioridazine (Mellaril or Melleril) is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis. The branded product was withdrawn worldwide in 2005 because it caused severe cardiac arrhythmias. However, generic versions are still available in the US. Read more...
Tricyclics are chemical compounds that contain three interconnected rings of atoms.
Many compounds have a tricyclic structure, but in pharmacology, the term has traditionally been reserved to describe heterocyclic drugs. Among these are antidepressants, antipsychotics, anticonvulsants, and antihistamines (as antiallergens, anti-motion sickness drugs, antipruritics, and hypnotics/sedatives) of the dibenzazepine, dibenzocycloheptene, dibenzothiazepine, dibenzothiepin, phenothiazine, and thioxanthene chemical classes, and others. Read more...
Pipamperone (INN, USAN, BAN), also known as carpiperone and floropipamide or fluoropipamide, and as floropipamide hydrochloride (JAN), is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia. It is or has been marketed under brand names including Dipiperon, Dipiperal, Piperonil, Piperonyl, and Propitan. Pipamperone was discovered at Janssen Pharmaceutica in 1961, and entered clinical trials in the United States in 1963. Read more...
Brexpiprazole, sold under the brand name Rexulti, is an atypical antipsychotic. It is a dopamine D2 receptor partial agonist and has been described as a "serotonin–dopamine activity modulator" (SDAM). The drug received FDA approval on July 13, 2015 for the treatment of schizophrenia, and as an adjunctive treatment for depression. It has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD).
The drug was developed by Otsuka and Lundbeck, and is considered to be a successor of Otsuka's top-selling atypical antipsychotic aripiprazole (Abilify). Otsuka's U.S. patent on aripiprazole expired on October 20, 2014; and a generic was approved in April, 2015. Read more...
Clorotepine (INN; brand names Clotepin, Clopiben), also known as octoclothepin or octoclothepine, is an antipsychotic of the tricyclic group which was derived from perathiepin in 1965 and marketed in the Czech Republic by Spofa in or around 1971 for the treatment of schizophrenic psychosis.
Clorotepine is known to have high affinity for the dopamine D1, D2, D3, and D4 receptors, the serotonin 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, and 5-HT7 receptors, the α1A-, α1B-, and α1D-adrenergic receptors, and the histamine H1 receptors, where it has been it has been confirmed to act as an antagonist (or inverse agonist) at most sites (and likely is as such at all of them based on structure–activity relationships), and it also blocks the reuptake of norepinephrine via inhibition of the norepinephrine transporter. Read more...
Levosulpiride is a substituted benzamide antipsychotic, reported to be a selective antagonist of dopamine D2 receptor activity on both central and peripheral levels. It is an atypical neuroleptic and a prokinetic agent. Levosulpiride is also claimed to have mood elevating properties.
Chemically, it is the (S)-(−)-enantiomer of sulpiride. Read more...
Phenothiazine, abbreviated PTZ, is an organic compound that has the formula S(C6H4)2NH and is related to the thiazine-class of heterocyclic compounds. Derivatives of phenothiazine are highly bioactive and have widespread use and rich history. The derivative chlorpromazine revolutionized the field of psychiatry and allergy treatment. An earlier derivative, methylene blue, was one of the first antimalarial drugs, and derivatives are under investigation as possible anti-infective drugs. Phenothiazine is a prototypical pharmaceutical lead structure in medicinal chemistry. Read more...
Reserpine (also known by trade names Raudixin, Serpalan, Serpasil) is an indole alkaloid, antipsychotic, and antihypertensive drug that has been used for the control of high blood pressure and for the relief of psychotic symptoms, although because of the development of better drugs for these purposes and because of its numerous side-effects, it is rarely used today. The antihypertensive actions of reserpine are a result of its ability to deplete catecholamines (among other monoamine neurotransmitters) from peripheral sympathetic nerve endings. These substances are normally involved in controlling heart rate, force of cardiac contraction and peripheral vascular resistance.
Reserpine-mediated depletion of monoamine neurotransmitters in the synapses is often cited as evidence to the theory that depletion of the monoamine neurotransmitters causes subsequent depression in humans (c.f. monoamine hypothesis). However, this claim is not without controversy. The reserpine-induced depression is considered by some researchers to be a myth, while others claim that teas made out of the plant roots containing reserpine have a calming, sedative action that can actually be considered antidepressant. Notably, reserpine was the first compound shown to be an effective antidepressant in a randomized placebo-controlled trial. Read more...
Chlorpromazine (CPZ), marketed under the trade names Thorazine and Largactil among others, is an antipsychotic medication. It is primarily used to treat psychotic disorders such as schizophrenia. Other uses include the treatment of bipolar disorder, attention deficit hyperactivity disorder, nausea and vomiting, anxiety before surgery, and hiccups that do not improve following other measures. It can be given by mouth, by injection into a muscle, or into a vein.
Common side effects include movement problems, sleepiness, dry mouth, low blood pressure upon standing, and increased weight. Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, neuroleptic malignant syndrome, and low white blood cell levels. In older people with psychosis as a result of dementia it may increase the risk of death. It is unclear if it is safe for use in pregnancy. Chlorpromazine is in the typical antipsychotic class. Its mechanism of action is not entirely clear but believed to be related to its ability as a dopamine antagonist. It also has anti-serotonergic and antihistaminergic properties. Read more...
Cannabidiol (CBD) is a naturally occurring cannabinoid constituent of cannabis. It was discovered in 1940 and initially thought not to be pharmaceutically active. It is one of at least 113 cannabinoids identified in hemp plants, accounting for up to 40% of the plant's extract.
Cannabidiol can be taken into the body in multiple different ways, including by inhalation of cannabis smoke or vapor, as an aerosol spray into the cheek, and by mouth. It may be supplied as an oil containing only CBD as the active ingredient (no added THC or terpenes), a full-plant CBD-dominant hemp extract oil, capsules, dried cannabis, or as a prescription liquid solution. Read more...
1,2-Benzisoxazole is an aromatic organic compound with a molecular formula C7H5NO containing a benzene-fused isoxazole ring structure. The compound itself has no common applications; however, functionalized benzisoxazoles and benzisoxazoyls have a variety of uses, including pharmaceutical drugs such as some antipsychotics (including risperidone, paliperidone, ocaperidone, and iloperidone) and the anticonvulsant zonisamide.
Its aromaticity makes it relatively stable; however, it is only weakly basic. Read more...
Clozapine, sold under the brand name Clozaril among others, is an atypical antipsychotic medication. It is mainly used for schizophrenia that does not improve following the use of other antipsychotic medications. In those with schizophrenia and schizoaffective disorder it may decrease the rate of suicidal behavior. It is more effective than typical antipsychotics and effective for those who are treatment resistant. It is taken by mouth.
Clozapine is associated with a relatively high risk of low white blood cells (agranulocytosis), a condition of suppressed immunity which may result in death. To decrease this risk it is recommended that the blood be regularly monitored. Other serious risks include seizures, inflammation of the heart, high blood sugar levels, and, in older people with psychosis as a result of dementia, an increased risk of death. Common side effects include drowsiness, decreased or increased saliva production, low blood pressure, trouble seeing, and dizziness. The potentially permanent movement disorder tardive dyskinesia occurs in about 5% of people. Its mechanism of action is not entirely clear. Read more...
Butyrophenone is a chemical compound; some of its derivatives (called commonly butyrophenones) are used to treat various psychiatric disorders such as schizophrenia, as well as acting as antiemetics.
Examples of butyrophenones include:- Haloperidol, the most widely used classical antipsychotic drug in this class
- Benperidol, the most potent commonly used antipsychotic (200 times more potent than chlorpromazine)
- Droperidol, a commonly used antiemetic for postoperative nausea and vomiting
Molindone, sold under the brand name Moban, is an antipsychotic which is used in the United States in the treatment of schizophrenia. It works by blocking the effects of dopamine in the brain, leading to diminished psychoses. It is rapidly absorbed when taken orally.
It is sometimes described as a typical antipsychotic, and sometimes described as an atypical antipsychotic. Read more...
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Selected images
Olanzapine, an example of a second-generation antipsychotic
Advertisement for Thorazine (chlorpromazine) from the 1950s, reflecting the perceptions of psychosis, including the now-discredited perception of a tendency towards violence, from the time when antipsychotics were discovered
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