What is the application of phenothiazine in everyday life?
Phenothiazine itself is only of theoretical interest, but its derivatives revolutionized psychiatry, other fields of medicine, and pest management. Other derivatives have been studied for possible use in advanced batteries and fuel cells.
Who deduced the structure of phenothiazine?
The structure was deduced in 1885 by Heinrich August Bernthsen. Bernthsen synthesized phenothiazine in 1883. In the mid 1880s, Paul Ehrlich began to use methylene blue in his cell staining experiments that led to pioneering discoveries about different cell types. He was awarded a Nobel Prize based in part on that work.
How are phenothiazine antipsychotics classified?
Phenothiazine antipsychotics are classified into three groups that differ with respect to the substituent on nitrogen: the aliphatic compounds (bearing acyclic groups), the "piperidines" (bearing piperidine -derived groups), and the piperazine (bearing piperazine -derived substituents).
How effective is Thorazine for treating psychotic episodes?
'Thorazine' is especially effective when the psychotic episode is triggered by delusions or hallucinations. At the outset of treatment, Thorazine's combination of antipsychotic and sedative effects provides both emotional and physical calming.
What was Thorazine originally used for?
In 1951, Henri Laborit, a surgeon in the French navy, began experimenting with chlorpromazine, which was originally intended to be used as a surgical anesthetic.
What were phenothiazines originally used for?
Chlorpromazine was the first of the phenothiazines used clinically as an antipsychotic. Phenothiazines are used to treat psychosis including schizophrenia; violent, agitated, disturbed behavior; and mania secondary to bipolar disorder.
When was Thorazine used?
By 1954, chlorpromazine was being used in the United States to treat schizophrenia, mania, psychomotor excitement, and other psychotic disorders. Rhône-Poulenc licensed chlorpromazine to Smith Kline & French (today's GlaxoSmithKline) in 1953.
How does Thorazine treat schizophrenia?
Chlorpromazine is in a class of medications called conventional antipsychotics. It works by changing the activity of certain natural substances in the brain and other parts of the body.
How does phenothiazine treat schizophrenia?
Although, the exact mechanism of phenothiazine antipsychotics is unknown, scientists believe that they may work by blocking the action of dopamine in the brain. Dopamine is a neurotransmitter (chemical) that nerves use to communicate with one another.
Which antipsychotics are phenothiazines?
Generic and brand names of phenothiazine antipsychotic drugs include: chlorpromazine. Compro (prochlorperazine maleate rectal suppository) fluphenazine.
Is the drug Thorazine still used?
The brand name Thorazine is discontinued in the U.S. Generic forms may be available.
How was schizophrenia treated in the 1960s?
Neuroleptic medications were first used in the early 1950s. Deinstitutionalization, beginning in the 1960s, resulted in medicated, stable schizophrenics being released from state hospitals.
How was schizophrenia treated in the 1940s?
Treatment of schizophrenia in the 1940s included insulin therapy – which was introduced by Sakel in Vienna in 1933, Metrazol (a convulsant) by Meduna in Budapest in 1934, prefrontal leucotomy by Moniz in Portugal in 1937 and electroconvulsive therapy by Cerletti and Bini in Italy in 1938.
What is the main drug used to treat schizophrenia?
Haloperidol, fluphenazine, and chlorpromazine are known as conventional, or typical, antipsychotics and have been used to treat schizophrenia for years. However, they sometimes have movement-related side effects, such as tremors and dystonia, a condition that causes involuntary muscle contractions.
Which of the following drug is phenothiazine?
Examples of phenothiazines include: chlorpromazine (brand name: Thorazine), fluphenazine (Duraclon), mesoridazine (Serentil), perphenazine (Etrafon and Trilafon), prochlorperazine (Compazine), promazine (Robinul and Anectine), thioridazine (Mellaril), trifluoperazine (Stelazine) and triflupromazine (Robinul).
How does chlorpromazine treat schizophrenia?
This medication is used to treat certain mental/mood disorders (such as schizophrenia, psychotic disorders, manic phase of bipolar disorder, severe behavioral problems in children). Chlorpromazine helps you to think more clearly, feel less nervous, and take part in everyday life.
What is phenothiazine?
26.5.2 Phenothiazine (PTZ) Phenothiazine is a heterocyclic compound from thiazine family. The derivatives of phenothiazine are highly bioactive and have a wide spread use as antipsychotropic [139], antimalarial [140], antimicrobial [141], antitumor [142, 143], antitubercular [144, 145], and analgesic [146].
Why are phenothiazines important?
Phenothiazines are important classes of compounds with a variety of biological activities and are useful for many classes of drug discovery.215–217 The syntheses of these compounds have been developed using several strategies.
What is the most commonly prescribed psychotropic drug?
The phenothiazine group of drugs is among the most widely prescribed psychotropic drugs in the world [17]. The phenothiazines are classified as typical antipsychotics because of their high potency to blockade the D 2 receptor. These drugs can be effective in treating the positive symptoms but not the negative signs of schizophrenia. Phenothiazines are highly sedating but with time, some tolerance to this effect develops. They have α-adrenergic blocking activity and can cause orthostatic hypotension. They have also moderate anticholinergic activity. The most popular phenothiazines ( Fig. 6.1 .) are the simple phenothiazin-10-yl-propan-1-amines-chlorpromazine ( 6.1.1 ), promazine ( 6.1.2 ), and levomepromazine ( 6.1.3 ); a little bit more complex are piperazin-1-yl-propyl-10H-phenothiazines-prochlorperazine ( 6.1.4 ), trifluoperazine ( 6.1.5 ), perphenazine ( 6.1.6 ), fluphenazine ( 6.1.7 ); piperidin-2-yl-ethyl-10H-phenothiazines-thioridazine ( 6.1.8 ), mesoridazine ( 6.1.9 ), pericyazine ( 6.1.10 ), and cyamemazine ( 6.1.11 ).
What is the ring scaffold of phenothiazine?
The fused tricyclic phenothiazine is an important ring scaffold present in CNS agents such as chlorpromazine and fluphenazine , which are used in therapy to treat psychotic disorders [97]. As such, phenothiazines are known to exhibit ChE inhibition and antioxidant activity [98].
What are some antipsychotics?
Clinically effective antipsychotic agents include tricyclic phenothiazines, thixanthenes, and dibenzepines, as well as butyrophenones and congeners, other hetrocyclics, and experimental benzamides. Virtually all of these drugs block D2 –dopamine receptors and reduce dopamine nuerotranamission in forebrain; some also interact with D 1 -and D 4 -dopaminergic, 5-HT 2A - and5 -HT 2c - serotonergic, and α-adrenergic receptors. Antipsychotic drugs are relatively lipophilic, mainly metabolized by hepatic oxidative mechanisms [ 155 ].
Is cyamemazine an antipsychotic?
Despite being classified as a typical antipsychotic, it actually behaves like an atypical antipsychotic.
When was phenothiazine introduced?
Phenothiazine was superseded by other drugs in the 1950s.
What is phenothiazine?
From Wikipedia, the free encyclopedia. Jump to navigation Jump to search. Heterocyclic compound containing a ring of four carbon, one nitrogen and one sulfur atom.
When was methylene blue first used?
The structure was deduced in 1885 by Heinrich August Bernthsen. Bernthsen synthesized phenothiazine in 1883. In the mid 1880s , Paul Ehrlich began to use methylene blue in his cell staining experiments that led to pioneering discoveries about different cell types. He was awarded a Nobel Prize based in part on that work. He became particularly interested in its use to stain bacteria and parasites such as Plasmodiidae – the genus that includes the malaria pathogen – and found that it could be stained with methylene blue. He thought methylene blue could possibly be used in the treatment of malaria, tested it clinically, and by the 1890s methylene blue was being used for that purpose.
What was the name of the drug that was made in the 1940s?
This work led to promethazine which had no activity against infective organisms, but did have good antihistamine activity, with a strong sedative effect.
When was thiabendazole first used?
As of July 2015 it is not registered for pesticide use in the US, Europe, or Australia. It was introduced as anthelminthic in livestock in 1940 and is considered, with thiabendazole, to be the first modern anthelminthic. The first instances of resistance were noted in 1961.
Is phenothiazine bioactive?
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.
Why was chlorpromazine first tested?
It freed many people with severe schizophrenia from mental asylums, but that's not why it was developed. It was first tested because it's an antihistamine. Yes, like the allergy medications.
How long did it take for a schizophrenic to go home after taking chlorpromazine?
Up until then, the psychiatrists had been doing nothing more than knocking their patients out with sedatives, which were the only known way to treat mania and schizophrenia. When a schizophrenic patient took chlorpromazine, he was calm and rational in three weeks. In another few weeks, he went home.
Does chlorpromazine cause hallucinations?
Today, the most popular theory is that chlorpromazine, better known as Thorazine, treats schizophrenia by doing just what antihistamines are meant to do — blocking an overactive bodily response. Too much dopamine can cause visual and auditory hallucinations.
Who was the doctor who discovered the autonomic nervous system?
In 1949, a Henri Lavorit , a French doctor working in Tunisia, saw huge potential in antihistamine's suppression of bodily systems — including the autonomic nervous system responsible for many unconscious body responses.
Does Lavorit help with blood pressure?
If Lavorit could suppress that response, he could save many lives. One particular antihistamine, known as chlorpromazine, seemed to do a good job lowering blood pressure, but it also rendered patients utterly indifferent to their upcoming surgery.
Does thorazine block dopamine?
Thorazine blocks dopamine receptors. Some doctors disagree, and the "dopamine theory" of schizophrenia isn't universal, but few disagree with the notion that chlorpromazine was a revolution in psychiatric treatment at the time. Advertisement. Top Image: Epsos.de.
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Take this medication by mouth with or without food as directed by your doctor, usually 2-4 times daily.
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What is phenothiazine used for?
In the 1940s, phenothiazine and its derivatives were used as insecticides and for deworming due to their remarkably effective toxicity characteristics.
How long has chlorpromazine been around?
Since the drug has been around for three-quarters of a century, a considerable body of data has accumulated on chlorpromazine. Below is an outline of various topics of information and might be considered recommended reading for anyone considering starting or stopping the drug.
What is chlorpromazine used for?
Chlorpromazine is used to treat schizophrenia and manic or mixed episodes in bipolar disorders. The drug can interact with other drugs, and also can change the metabolism of the body. When too much of the drug is taken, either purposefully or accidentally, it can result in an overdose.
What is the name of the drug that makes you salivate?
Thorazine (discontinued), Largactil, Megaphen, are all brand or trade names for the generic drug chlorpromazine. Sometimes antipsychotic drugs are nicknamed “drool drugs” as they can induce profuse salivation, and decrease the ability to swallow as the throat may become constricted.
What is a pre-surgical calming medication?
As a pre-surgical calming medication. To prevent nausea and vomiting. For treating a group of diseases called porphyria. Acute porphyria is thought to be genetic in origin, involving imbalances of red blood cells, causing blisters, rash, fever, abdominal pain, and other symptoms.
What is a dystonic reaction?
Dystonic reactions, i.e., twisted spasmodic or fixed unusual body postures or motions. Anticholinergic effects, where a drug aggressively blocks the neurotransmitter called acetylcholine resulting in dry mouth, dental problems, lung disease, digestive, and many other systemic dysfunctions, can lead to death.
Is thorazine an antipsychotic?
Thorazine is a drug from the early ( 1950s) era of pharmaceutical discoveries and was the first medication ever to be named an “antipsychotic” drug. The brand name “Thorazine” is no longer used, but chlorpromazine is still very much in use.
What is CPZ used for?
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 by mouth, by injection into a muscle, or into a vein.
What drugs can be used to prolong the QT interval?
Other drugs that prolong the QT interval such as quinidine, verapamil, amiodarone, sotalol and methadone may also interact with chlorpromazine to produce additive QT interval prolongation.
How to reduce chlorpromazine absorption?
Consuming food prior to taking chlorpromazine orally limits its absorption, likewise cotreatment with benztropine can also reduce chlorpromazine absorption. Alcohol can also reduce chlorpromazine absorption. Antacids slow chlorpromazine absorption. Lithium and chronic treatment with barbiturates can increase chlorpromazine clearance significantly. Tricyclic antidepressants (TCAs) can decrease chlorpromazine clearance and hence increase chlorpromazine exposure. Cotreatment with CYP1A2 inhibitors like ciprofloxacin, fluvoxamine or vemurafenib can reduce chlorpromazine clearance and hence increase exposure and potentially also adverse effects. Chlorpromazine can also potentiate the CNS depressant effects of drugs like barbiturates, benzodiazepines, opioids, lithium and anesthetics and hence increase the potential for adverse effects such as respiratory depression and sedation.
What was the name of the drug that replaced electroconvulsive therapy?
From chlorpromazine a number of other similar antipsychotics were developed. It also led to the discovery of antidepressants. Chlorpromazine largely replaced electroconvulsive therapy, hydrotherapy, psychosurgery, and insulin shock therapy. By 1964, about 50 million people worldwide had taken it.
What is chlorpromazine used for?
Chlorpromazine is used in the treatment of both acute and chronic psychoses, including schizophrenia and the manic phase of bipolar disorder, as well as amphetamine-induced psychosis. In a 2013 comparison of 15 antipsychotics in schizophrenia, chlorpromazine demonstrated mild-standard effectiveness.
What is Laborit's drug?
Laborit thought this would allow the body to better tolerate major surgery by reducing shock, a novel idea at the time. Known colloquially as "Laborit's drug", chlorpromazine was released onto the market in 1953 by Rhône-Poulenc and given the trade name Largactil, derived from large "broad" and acti* "activity.
How much chlorpromazine is excreted?
Less than 1% of the unchanged drug is excreted via the kidneys in the urine, in which 20–70% is excreted as conjugated or unconjugated metabolites, whereas 5–6% is excreted in feces. Three common metabolites of chlorpromazine.
What are mood stabilizers?
mood stabilizers. Many studies have found structural and functional brain pathology in patients suffering from affective disorders. Although there is little consensus about the exact location of the brain pathology, it is most commonly observed in three structures. These structures include the.
What is the neuroplasticity theory of depression?
The neuroplasticity theory of depression is that depression is caused by . A) an increase in neuroplastic processes in the prefrontal cortex. B) a decrease in neuroplastic processes in the prefrontal cortex, hippocampus, and amygdala. C) abnormal neuroplastic processes in the hypothalamus.
Overview
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, met…
Uses
Phenothiazine itself is only of theoretical interest, but its derivatives revolutionized psychiatry, other fields of medicine, and pest management. Other derivatives have been studied for possible use in advanced batteries and fuel cells.
In 1876, methylene blue, a derivative of phenothiazine, was synthesized by Heinrich Caro at BASF. The structure was deduced in 1885 by Heinrich August Bernthsen. Bernthsen synthesized pheno…
Trade names
Like many commercially significant compounds, phenothiazine has numerous trade names, including AFI-Tiazin, Agrazine, Antiverm, Biverm, Dibenzothiazine, Orimon, Lethelmin, Souframine, Nemazene, Vermitin, Padophene, Fenoverm, Fentiazine, Contaverm, Fenothiazine, Phenovarm, Ieeno, ENT 38, Helmetina, Helmetine, Penthazine, XL-50, Wurm-thional, Phenegic, Phenovis, Phenoxur, and Reconox.
Former uses
Phenothiazine was formerly used as an insecticide and as a drug to treat infections with parasitic worms (anthelminthic) in livestock and people, but its use for those purposes has been superseded by other chemicals.
Phenothiazine was introduced by DuPont as an insecticide in 1935. About 3,500,000 pounds were sold in the US in 1944. However, because it was degraded by sunlight and air, it was difficult to d…
Structure and synthesis
The central C4SN ring is folded in phenothiazines.
The compound was originally prepared by Bernthsen in 1883 via the reaction of diphenylamine with sulfur, but more recent syntheses rely on the cyclization of 2-substituted diphenyl sulfides. Few pharmaceutically significant phenothiazines are prepared from phenothiazine, although some of them are.
External links
• MSDS
• Hendricks, Christensen, J.B., and Kristiansen, Jette E. Sonderborg, Denmark. "Antibakterielle Eigenschaften der Phenothiazine: Eine Behandlungsoption für die Zukunft?" Chemotherapie Journal. 13.5. (2004): 203–205. Wissenschaftliche Verlagsgesesellschaft mbH. 21 August 2005. (PDF).