Benzamide
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Benzamide
Benzamide is a organic compound with the chemical formula of C6H5C(O)NH2. It is the simplest amide derivative of benzoic acid Benzoic acid is a white (or colorless) solid organic compound with the formula , whose structure consists of a benzene ring () with a carboxyl () substituent. It is the simplest aromatic carboxylic acid. The name is derived from gum benzoin, .... In powdered form, it appears as a white solid, while in crystalline form, it appears as colourless crystals. It is slightly soluble in water, and soluble in many organic solvents. It is a natural alkaloid found in the herbs of Berberis pruinosa. Chemical derivatives A number of substituted benzamides are commercial drugs, including: See also * References External links Physical characteristics {{Authority control Phenyl compounds ...
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Sulpiride
Sulpiride, sold under the brand name Dogmatil among others, is an atypical antipsychotic (although some texts have referred to it as a typical antipsychotic) medication of the benzamide class which is used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression. Sulpiride is commonly used in Asia, Central America, Europe, South Africa and South America. Levosulpiride is its purified levo-isomer and is sold in India for similar purpose. It is not approved in the United States, Canada, or Australia. The drug is chemically and clinically similar to amisulpride. Medical uses Sulpiride's primary use in medicine is in the management of the symptoms of schizophrenia. It has been used as both a monotherapy and adjunctive therapy (in case of treatment-resistance) in schizophrenia. It has also been used in the treatment of dysthymia. There is evidence, although low quality, th ...
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Veralipride
Veralipride (Agreal, Agradil) is a typical antipsychotic of the benzamide class. It is indicated for the treatment of vasomotor symptoms associated with menopause. It is a D2 receptor antagonist and it induces prolactin secretion without any estrogenic or progestagenic effects. It was first authorised for use in 1979. Veralipride has never gained approval in the United States. In September 2006, it was withdrawn from the Spanish market. As a result, the European Commission referred the matter to the European Medicines Agency (EMA). In July 2007, the EMA recommended the withdrawal of marketing authorisations for veralipride. See also * Typical antipsychotic * Benzamide * Levosulpiride Levosulpiride, sold under the brand name Neoprad, is a typical antipsychotic and a prokinetic agent of the benzamide class. It is a selective antagonist of the dopamine D2 receptors on both central and peripheral nervous systems. Levosulpiride ... References Allyl compounds Benzamid ...
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Remoxipride
Remoxipride (Roxiam) is an atypical antipsychotic (although according to some sources it is a typical antipsychotic) which was previously used in Europe for the treatment of schizophrenia and acute mania but was withdrawn due to toxicity concerns (incidence of aplastic anemia in 1/10,000 patients). It was initially launched by AstraZeneca in 1990 and suspension of its use began in 1993. Remoxipride acts as a selective D2 and D3 receptor antagonist and also has high affinity for the sigma receptor, possibly playing a role in its atypical neuroleptic action. Due to its short half-life twice daily (bid) dosing is required, although a once-daily controlled-release tablet has been developed. There was some interest in its use in the treatment of treatment-resistant schizophrenia. See also * Typical antipsychotic * Benzamide Benzamide is a organic compound with the chemical formula of C6H5C(O)NH2. It is the simplest amide derivative of benzoic acid Benzoic acid is a whi ...
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Nemonapride
Nemonapride (エミレース, Emilace ( JP)) is an atypical antipsychotic approved in Japan for the treatment of schizophrenia. It was launched by Yamanouchi in May 1991. Nemonapride acts as a D2 and D3 receptor antagonist, and is also a potent 5-HT1A receptor agonist. It has affinity for sigma receptors. See also * Benzamide Benzamide is a organic compound with the chemical formula of C6H5C(O)NH2. It is the simplest amide derivative of benzoic acid Benzoic acid is a white (or colorless) solid organic compound with the formula , whose structure consists of a benz ... References Atypical antipsychotics Benzamides Chloroarenes Phenol ethers Pyrrolidines {{nervous-system-drug-stub ...
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Levosulpiride
Levosulpiride, sold under the brand name Neoprad, is a typical antipsychotic and a prokinetic agent of the benzamide class. It is a selective antagonist of the dopamine D2 receptors on both central and peripheral nervous systems. Levosulpiride is claimed to have mood elevating properties. Chemically, it is the (''S'')-(−)-enantiomer of sulpiride. Uses Levosulpiride is used in the treatment of: * Psychosis * Negative symptoms of schizophrenia * Anxiety disorders * Dysthymia * Vertigo * Dyspepsia * Irritable bowel syndrome * Premature ejaculation. Levosulpiride is not currently licensed for treatment of premature ejaculation in the UK or other European countries. Side effects Side effects include amenorrhea, gynecomastia, galactorrhea, changes in libido, and neuroleptic malignant syndrome. In the U.S., as of 2013 only one case of adverse reaction to levosulpiride had been recorded on the FDA Adverse Event Reporting System Database. A case of rapid onset resistant dystonia ...
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Amisulpride
Amisulpride is an antiemetic and antipsychotic medication used at lower doses intravenously to prevent and treat postoperative nausea and vomiting; and at higher doses by mouth to treat schizophrenia and acute psychotic episodes. It is sold under the brand names Barhemsys (as an antiemetic) and Solian, Socian, Deniban and others (as an antipsychotic). At very low doses it is also used to treat dysthymia. It is usually classed with the atypical antipsychotics. Chemically it is a benzamide and like other benzamide antipsychotics, such as sulpiride, it is associated with a high risk of elevating blood levels of the lactation hormone, prolactin (thereby potentially causing the absence of the menstrual cycle, breast enlargement, even in males, breast milk secretion not related to breastfeeding, impaired fertility, impotence, breast pain, ''etc.''), and a low risk, relative to the typical antipsychotics, of causing movement disorders. Amisulpride is indicated for use in the United ...
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Itopride
Itopride (INN; brand name Ganaton) is a prokinetic benzamide derivative. These drugs inhibit dopamine and acetylcholine esterase enzyme and have a gastrokinetic effect. Itopride is indicated for the treatment of functional dyspepsia and other gastrointestinal conditions. It is a combined D2 receptor antagonist and acetylcholinesterase inhibitor. Medical uses Typically, itopride is indicated in the treatment of GI symptoms caused by reduced GI motility: *dyspepsia of a non-ulcer/dysmotility type (gastric "fullness", discomfort, and possible pain) * gastroparesis (delayed gastric emptying) *anorexia *heartburn *regurgitation *bloating *nausea and vomiting *other possible gastric, prolactin, or dopamine related conditions Itopride was shown to significantly improve symptoms in patients with functional dyspepsia and motility disorders in placebo-controlled trials. These studies concluded that the reduction in the severity of symptoms of functional dyspepsia after 8 weeks of treatm ...
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Dazopride
Dazopride (AHR-5531) is an antiemetic and gastroprokinetic agent of the benzamide class which was never marketed. It acts as a 5-HT3 receptor antagonist and 5-HT4 receptor agonist. In addition to its gastrointestinal effects, dazopride facilitates learning and memory in mice. See also * Antiemetic * Benzamide Benzamide is a organic compound with the chemical formula of C6H5C(O)NH2. It is the simplest amide derivative of benzoic acid Benzoic acid is a white (or colorless) solid organic compound with the formula , whose structure consists of a benz ... References Serotonin receptor agonists 5-HT3 antagonists Antiemetics Salicylamide ethers Anilines Chlorobenzenes Pyrazolidines {{gastrointestinal-drug-stub ...
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Renzapride
Renzapride is a prokinetic agent and antiemetic which acts as a full 5-HT4 agonist and partial 5-HT3 antagonist. It also functions as a 5-HT2B antagonist and has some affinity for the 5-HT2A and 5-HT2C receptors. Renzapride was being developed by Alizyme plc of the United Kingdom. In May 2016, EndoLogic LLC, a US-based pharmaceutical and medical device company, acquired the US and worldwide patent rights to Renzapride. Endologic confirmed the cardiac safety of renzapride through a “Thorough QTc” study and sold the rights to Atlantic Healthcare plc in 2019, a specialist pharmaceutical company. Atlantic Healthcare is focusing on the development of renzapride for the management of gastrointestinal (GI) motility in a number of rare diseases, including systemic scleroderma and cystic fibrosis, both of which are associated with chronic GI motility problems and for which there are no approved therapies. Clinical trials In nine diabetic patients with autonomic neuropathy, ...
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Cisapride
Cisapride is a gastroprokinetic agent, a drug that increases motility in the upper gastrointestinal tract. It acts directly as a serotonin 5-HT4 receptor agonist and indirectly as a parasympathomimetic. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. It has been sold under the trade names Prepulsid (Janssen-Ortho) and Propulsid (in the United States). It was discovered by Janssen Pharmaceuticals in 1980. In many countries, it has been either withdrawn from the market or had its indications limited due to incidence of serious cardiac side-effects. Propulsid was linked to children's deaths. The commercial preparations of this drug are the racemic mixture of both enantiomers of the compound. The (+) enantiomer itself has the major pharmacologic effects and does not induce many of the detrimental side-effects of the mixture. Medical uses Cisapride has been used for the treatment of gastroesophageal reflux disease (GERD). There i ...
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Cinitapride
Cinitapride (trade names Cintapro, Pemix) is a gastroprokinetic agent and antiemetic agent of the benzamide class which is marketed in India, Mexico, Pakistan and Spain. It acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors. Uses It is indicated for the treatment of gastrointestinal disorders associated with motility disturbances such as gastroesophageal reflux disease, non-ulcer dyspepsia and delayed gastric emptying. It may be also used in the management of nausea and vomiting. See also * Benzamide * Gastroprokinetic agent A prokinetic agent (also gastroprokinetic agent, gastrokinetic agent or propulsive) is a type of drug which enhances gastrointestinal motility by increasing the frequency or strength of contractions, but without disrupting their rhythm. They are us ... References 4-Amino-N-(3-(diethylamino)propyl)-2-methoxybenzamides Nitrobenzenes Piperidines Serotonin receptor agonists Cyclohexenes {{Gas ...
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Trimethobenzamide
Trimethobenzamide (trade names Tebamide, Tigan) is an antiemetic used to prevent nausea and vomiting. Mechanism of action Trimethobenzamide is an antagonist of the D2 receptor. It is believed to affect the chemoreceptor trigger zone (CTZ) of the medulla oblongata to suppress nausea and vomiting. Side effects Possible side effects include drowsiness, dizziness, headache, muscle cramps, and blurred vision. More serious adverse effects include skin rash, tremors, parkinsonism, and jaundice. Formulations Trimethobenzamide is marketed under the brand names Tebamide and Tigan, manufactured by GlaxoSmithKline and King Pharmaceuticals, respectively. It is available as oral capsules and injectable formulations. Trimethobenzamide was also available as a rectal suppository, but such formulations were banned by the U.S. Food and Drug Administration on April 6, 2007, due to unproven efficacy. Synthesis Alkylation of the sodium salt of ''p''-hydroxybenzaldehyde (1) with 2-dimethyl ...
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