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Benzamides
Benzamide is a organic compound with the chemical formula of C6H5C(O)NH2. It is the simplest amide derivative of benzoic acid. 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 A substitution reaction (also known as single displacement reaction or single substitution reaction) is a chemical reaction during which one functional group in a chemical compound is replaced by another functional group. Substitution reactions ar ... benzamides are commercial drugs, including: See also * References External links Physical characteristics {{Authority control Phenyl compounds ...
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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 Un ...
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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, ...
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Procainamide
Procainamide (PCA) is a medication of the antiarrhythmic class used for the treatment of cardiac arrhythmias. It is classified by the Vaughan Williams classification system as class Ia; thus it is a sodium channel blocker of cardiomyocytes. In addition to blocking the ''I''Na current, it inhibits the ''I''Kr rectifier K+ current. Procainamide is also known to induce a voltage-dependent open channel block on the batrachotoxin (BTX)-activated sodium channels in cardiomyocytes. Uses Medical Procainamide is used for treating ventricular arrhythmias: ventricular ectopy and tachycardia and supraventricular arrhythmias: atrial fibrillation, and re-entrant and automatic supraventricular tachycardia. For example, it can be used to convert new-onset atrial fibrillation, and although was initially thought to be suboptimal for this purpose, a growing body of literature is amounting in support for this exact cause. It is administered by mouth, by intramuscular injection, or intravenously ...
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Mosapride
Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. The major active metabolite of mosapride, known as M1, additionally acts as a 5HT3 antagonist, which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans, and is used for the treatment of gastritis, gastroesophageal reflux disease, functional dyspepsia and irritable bowel syndrome. It is recommended to be taken on an empty stomach (i.e. at least one hour before food or two hours after food). In addition to its prokinetic properties, mosapride also exerts anti-inflammatory effects on the gastrointestinal tract which may contribute to some of its therapeutic effects. Mosapride also promotes neurogenesis Neurogenesis is the process by which nervous system cells, the neurons, are produced by neural stem cells (NSCs). It occurs in all species of animals except the porifera (sponges) and placozoans. Types of NSCs include neuroepithelial cells (NECs ... in the gast ...
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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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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-dimet ...
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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 Benzamide is a organic compound with the chemical formula of C6H5C(O)NH2. It is the simplest amide derivative of benzoic acid. In powdered form, it appears as a white solid, while in crystalline form, it appears as colourless crystals. It is slig ... * Levosulpiride References Allyl compounds Benzam ...
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Moclobemide
Moclobemide, sold under the brand names Amira, Aurorix, Clobemix, Depnil and Manerix among others, is a reversible inhibitor of monoamine oxidase A (RIMA) drug primarily used to treat depression and social anxiety. It is not approved for use in the United States, but is approved in other Western countries such as Canada, the UK and Australia ( TGA approved in December 2000). It is produced by affiliates of the Hoffmann–La Roche pharmaceutical company. Initially, Aurorix was also marketed by Roche in South Africa, but was withdrawn after its patent rights expired and Cipla Medpro's Depnil and Pharma Dynamic's Clorix became available at half the cost. No significant rise in blood pressure occurs when moclobemide is combined with amines such as tyramine-containing foods or pressor amine drugs, unlike with the older irreversible and non-selective monoamine oxidase inhibitors (MAOIs), which cause a severe rise in blood pressure with such combination. Due to the lack of anticholine ...
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Zacopride
Zacopride is a potent antagonist at the 5-HT3 receptor and an agonist at the 5-HT4 receptor. It has anxiolytic and nootropic effects in animal models, with the (''R'')-(+)-enantiomer being the more active form. It also has antiemetic and pro-respiratory effects, both reducing sleep apnea and reversing opioid-induced respiratory depression in animal studies. Early animal trials have also revealed that administration of zacopride can reduce preference for and consumption of ethanol. Zacopride was found to significantly increase aldosterone levels in human subjects for 180 minutes at a dose of 400 micrograms. It is thought to do this by stimulating the 5-HT4 receptors on the adrenal glands. Zacopride also stimulated aldosterone secretion when applied to human adrenal glands ''in vitro''. No significant changes were observed in renin, ACTH, or cortisol levels. Zacopride has been tested in clinical trials for the treatment of schizophrenia Schizophrenia is a mental diso ...
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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 treat ...
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Ethenzamide
Ethenzamide (2-ethoxybenzamide) is a common analgesic and anti-inflammatory drug that is used for the relief of fever, headaches, and other minor aches and pains. It is also an ingredient in numerous cold medications and many prescription analgesics. It is used as an over-the-counter drug in Japan, often in combination with caffeine and acetaminophen, where it is marketed for uses including toothache, menstrual cramps, headache, and fever. It is metabolized in vivo into salicylamide Salicylamide (''o''-hydroxybenzamide or amide of salicyl) is a non-prescription drug with analgesic and antipyretic properties. Its medicinal uses are similar to those of aspirin. Salicylamide is used in combination with both aspirin and ca .... References Nonsteroidal anti-inflammatory drugs Benzamides Phenol ethers {{analgesic-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 dyston ...
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