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Trade names | Pacatal, Pacatol, Paxital, Lacumin, Nothiazine |
Routes of administration | Oral, parenteral |
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ECHA InfoCard | 100.000.446 |
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Formula | C19H22N2S |
Molar mass | 310.46 g·mol−1 |
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Pecazine (INN), also known as mepazine (trade name Pacatal), is a phenothiazine formerly used as a neuroleptic drug or major tranquilizer.
Pecazine was first synthesized in 1953 by Wilhelm Schuler and Otto Nieschulz and was quickly incorporated into psychiatric practice as an ataractic, i.e., a true tranquilizer rather than a hypnotic or depressant. It was considered interchangeable with chlorpromazine, albeit with a different side effect profile, which included less sedation and a lower risk of extrapyramidal symptoms due to its potent parasympatholytic and anticholinergic effect. [1]
As early as 1958, however, studies reported inferiority to other phenothiazines in the treatment of schizophrenia and questioned its place in the clinic; [2] [3] in 1960, a double-blind, randomized controlled trial found pecazine to be no more effective than placebo. [4] Subsequent research found that, like the structurally related promethazine, pecazine is essentially devoid of antipsychotic activity. [5]
Pecazine was implicated in a number of cases of agranulocytosis and was subsequently withdrawn from the market. [6] [7] [8] [9] More recently, it has become a subject of research interest as a MALT1 and RANKL inhibitor. [10] [11]
Antipsychotics, also known as neuroleptics, are a class of psychotropic medication primarily used to manage psychosis, principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder.
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 derivatives chlorpromazine and promethazine revolutionized the fields of psychiatry and allergy treatment, respectively. 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.
Serotonin syndrome (SS) is a group of symptoms that may occur with the use of certain serotonergic medications or drugs. The degree of symptoms can range from mild to severe, including a potentiality of death. Symptoms in mild cases include high blood pressure and a fast heart rate; usually without a fever. Symptoms in moderate cases include high body temperature, agitation, increased reflexes, tremor, sweating, dilated pupils, and diarrhea. In severe cases body temperature can increase to greater than 41.1 °C (106.0 °F). Complications may include seizures and extensive muscle breakdown.
Clozapine is a psychiatric medication and is the first atypical antipsychotic. It is primarily used to treat people with schizophrenia and schizoaffective disorders who have had an inadequate response to other antipsychotics or who have been unable to tolerate other drugs due to extrapyramidal side effects. It is also used for the treatment of psychosis in Parkinson's disease. Clozapine is regarded as the gold-standard treatment when other medication has been insufficiently effective and its use is recommended by multiple international treatment guidelines, after resistance to earlier neuroleptic treatment is established.
Neuroleptic malignant syndrome (NMS) is a rare but life-threatening reaction that can occur in response to neuroleptic or antipsychotic medication. Symptoms include high fever, confusion, rigid muscles, variable blood pressure, sweating, and fast heart rate. Complications may include rhabdomyolysis, high blood potassium, kidney failure, or seizures.
Trifluoperazine, marketed under the brand name Stelazine among others, 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.
Chlorpromazine (CPZ), marketed under the brand 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, severe behavioral problems in children including those with attention deficit hyperactivity disorder, nausea and vomiting, anxiety before surgery, and hiccups that do not improve following other measures. It can be given orally, by intramuscular injection, or intravenously.
Haloperidol, sold under the brand name Haldol among others, is a typical antipsychotic medication. Haloperidol is used in the treatment of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal. It may be used by mouth or injection into a muscle or a vein. Haloperidol typically works within 30 to 60 minutes. A long-acting formulation may be used as an injection every four weeks by people with schizophrenia or related illnesses, who either forget or refuse to take the medication by mouth.
Typical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis. Typical antipsychotics may also be used for the treatment of acute mania, agitation, and other conditions. The first typical antipsychotics to come into medical use were the phenothiazines, namely chlorpromazine which was discovered serendipitously. Another prominent grouping of antipsychotics are the butyrophenones, an example of which is haloperidol. The newer, second-generation antipsychotics, also known as atypical antipsychotics, have largely supplanted the use of typical antipsychotics as first-line agents due to the higher risk of movement disorders in the latter.
Perphenazine is a typical antipsychotic drug. Chemically, it is classified as a piperazinyl phenothiazine. Originally marketed in the United States as Trilafon, it has been in clinical use for decades.
Tardive dyskinesia (TD) is a disorder that results in involuntary repetitive body movements, which may include grimacing, sticking out the tongue or smacking the lips. Additionally, there may be rapid jerking movements or slow writhing movements. In about 20% of people with TD, the disorder interferes with daily functioning.
Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorders. It is sold under the brand names Nitoman and Xenazine among others. On August 15, 2008, the U.S. Food and Drug Administration approved the use of tetrabenazine to treat chorea associated with Huntington's disease. Although other drugs had been used "off label," tetrabenazine was the first approved treatment for Huntington's disease in the U.S. The compound has been known since the 1950s.
Melperone is an atypical antipsychotic of the butyrophenone chemical class, making it structurally related to the typical antipsychotic haloperidol. It first entered clinical use in 1960s.
Olanzapine/fluoxetine is a fixed-dose combination medication containing olanzapine (Zyprexa), an atypical antipsychotic, and fluoxetine (Prozac), a selective serotonin reuptake inhibitor (SSRI). Olanzapine/fluoxetine is primarily used to treat the depressive episodes of bipolar I disorder as well as treatment-resistant depression.
Loren Richard Mosher was an American psychiatrist, clinical professor of psychiatry, expert on schizophrenia and the chief of the Center for Studies of Schizophrenia in the National Institute of Mental Health (1968–1980). Mosher spent his professional career advocating for humane and effective treatment for people diagnosed as having schizophrenia and was instrumental in developing an innovative, residential, home-like, non-hospital, non-drug treatment model for newly identified acutely psychotic persons.
Setoperone is a compound that is a ligand to the 5-HT2A receptor. It can be radiolabeled with the radioisotope fluorine-18 and used as a radioligand with positron emission tomography (PET). Several research studies have used the radiolabeled setoperone in neuroimaging for the studying neuropsychiatric disorders, such as depression or schizophrenia.
Pipotiazine (Piportil), also known as pipothiazine, is a typical antipsychotic of the phenothiazine class used in the United Kingdom and other countries for the treatment of schizophrenia. Its properties are similar to those of chlorpromazine. A 2004 systematic review investigated its efficacy for people with schizophrenia:
An active placebo is a placebo that produces noticeable side effects that may convince the person being treated that they are receiving a legitimate treatment, rather than an ineffective placebo.
Cetadiol, also known as androst-5-ene-3β,16α-diol, is a drug described as a "steroid tranquilizer" which was briefly investigated as a treatment for alcoholism in the 1950s. It is an androstane steroid and analogue of 5-androstenediol (androst-5-ene-3β,17β-diol) and 16α-hydroxy-DHEA (androst-5-ene-3β,16α-diol-17-one), but showed no androgenic or myotrophic activity in animal bioassays. The drug was reported in 1956 and studied until 1958.
Irvin M. Cohen, M.D. (1922–2019) was a psychiatrist specializing in psychopharmacology, recognized for his role in the early use of chlorpromazine in the treatment of schizophrenia, the development of the first benzodiazepine (Librium) treatments in depressive patients, and in the adoption of lithium to treat bipolar disorder.