Ethacizine
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Ethacizine
Ethacizine (ethacyzine) is a class Ic antiarrhythmic agent, related to moracizine. It is used in Russia and some other CIS countries for the treatment of severe and/or refractory ventricular and supraventricular arrhythmias, especially those accompanied by organic heart disease. It is also indicated as a treatment of refractory tachycardia associated with Wolff–Parkinson–White syndrome. It is manufactured under the brand name Ethacizin (Этацизин) by Latvian pharmaceutical company Olainfarm. Synthesis For the treatment of heart infarction:E I Chazov, (to 1985 to INST FARMAKOLOGII AKADEMII M). The amide formation between Phenothiazine-2-ethylcarbamate 7711-29-8(1) and 3-Chloropropionyl chloride 25-36-5(2) gives ethyl N- 0-(3-chloropropanoyl)phenothiazin-2-ylarbamate 19407-03-3 4749-22-9(3). Displacement of the remaining ω-halogen by diethylamine Diethylamine is an organic compound with the formula (CH3CH2)2NH. It is a secondary amine. It is a flammable, weakly ...
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Ethacizine Synthesis
Ethacizine (ethacyzine) is a Antiarrhythmic_agent#Class_I_agents, class Ic antiarrhythmic agent, related to moracizine. It is used in Russia and some other Commonwealth of Independent States, CIS countries for the treatment of severe and/or refractory ventricular and supraventricular Cardiac dysrhythmia, arrhythmias, especially those accompanied by organic heart disease. It is also indicated as a treatment of refractory tachycardia associated with Wolff–Parkinson–White syndrome. It is manufactured under the brand name Ethacizin (Этацизин) by Latvian pharmaceutical company Olainfarm. Synthesis For the treatment of heart infarction:E I Chazov, (to 1985 to INST FARMAKOLOGII AKADEMII M). The amide formation between Phenothiazine-2-ethylcarbamate [37711-29-8] (1) and 3-Chloropropionyl chloride [625-36-5] (2) gives ethyl N-[10-(3-chloropropanoyl)phenothiazin-2-yl]carbamate [119407-03-3] [34749-22-9] (3). Displacement of the remaining ω-halogen by diethylamine (4) then com ...
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Moracizine
Moracizine or moricizine, sold under the trade name Ethmozine, is an antiarrhythmic of class IC. It was used for the prophylaxis and treatment of serious and life-threatening ventricular arrhythmias, but was withdrawn in 2007 for commercial reasons. Pharmacology Moracizine, a phenothiazine derivative, undergoes extensive first-pass metabolism and is also extensively metabolized after it has entered the circulation. It may have pharmacologically active metabolites. A clinical study has shown that moracizine is slightly less effective than encainide or flecainide in suppressing ventricular premature depolarizations. Compared with disopyramide and quinidine, moracizine was equally or more effective in suppressing premature ventricular contractions, couplets, and nonsustained ventricular tachycardia. In the Cardiac Arrhythmia Suppression Trial (CAST), a large study testing the influence of antiarrhythmics on mortality, showed a statistically non-significant increase of mortality fro ...
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Prescription Drug
A prescription drug (also prescription medication or prescription medicine) is a pharmaceutical drug that legally requires a medical prescription to be dispensed. In contrast, over-the-counter drugs can be obtained without a prescription. The reason for this difference in substance control is the potential scope of misuse, from drug abuse to practicing medicine without a license and without sufficient education. Different jurisdictions have different definitions of what constitutes a prescription drug. In North America, ℞, usually printed as "Rx", is used as an abbreviation of the word "prescription". It is a contraction of the Latin word "''recipe''" (an imperative form of "recipere") meaning "take". Prescription drugs are often dispensed together with a monograph (in Europe, a Patient Information Leaflet or PIL) that gives detailed information about the drug. The use of prescription drugs has been increasing since the 1960s. Regulation Australia In Australia, the Standar ...
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Heart Infarction
A myocardial infarction (MI), commonly known as a heart attack, occurs when Hemodynamics, blood flow decreases or stops to the coronary artery of the heart, causing ischemia, damage to the cardiac muscle, heart muscle. The most common symptom is chest pain or Angina, discomfort which may travel into the shoulder, arm, back, neck or jaw. Often it occurs in the center or left side of the chest and lasts for more than a few minutes. The discomfort may occasionally feel like heartburn. Other symptoms may include shortness of breath, nausea, presyncope, feeling faint, a diaphoresis, cold sweat or Fatigue, feeling tired. About 30% of people have atypical symptoms. Women more often present without chest pain and instead have neck pain, arm pain or feel tired. Among those over 75 years old, about 5% have had an MI with little or no history of symptoms. An MI may cause heart failure, an Cardiac arrhythmia, irregular heartbeat, cardiogenic shock or cardiac arrest. Most MIs occur due to c ...
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Phenothiazines
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. 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. Phenothiazine-derived drugs In 1876, methylene blue, a derivative of phenothiazine, was synthesized by Heinrich Caro at BASF. The struc ...
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Sodium Channel Blockers
Sodium channel blockers are drugs which impair the conduction of sodium ions (Na+) through sodium channels. Extracellular The following naturally-produced substances block sodium channels by binding to and occluding the extracellular pore opening of the channel: * Alkaloids: ** Saxitoxin (STX) ** Neosaxitoxin (NSTX) ** Tetrodotoxin (TTX) Intracellular Drugs which block sodium channels by blocking from the intracellular side of the channel include: * Local anesthetics: ''lidocaine'' * Class I antiarrhythmic agents * Various anticonvulsants: ''phenytoin, oxcarbazepine (derivative of carbamazepine)'' Unknown mechanism * Calcium has been shown to block sodium channels which explains the effects of hypercalcemia and hypocalcemia. * Lamotrigine is known to block sodium channels but it is not known whether it is extracellular or intracellular. * Cannabidiol (CBD) has been shown to cause inhibitory effects on sodium currents. This voltage-dependent inhibition is non-selective in nature ...
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Carbamates
In organic chemistry, a carbamate is a category of organic compounds with the general formula and structure , which are formally derived from carbamic acid (). The term includes organic compounds (e.g., the ester ethyl carbamate), formally obtained by replacing one or more of the hydrogen atoms by other organic functional groups; as well as salts with the carbamate anion (e.g. ammonium carbamate). Polymers whose units are joined by carbamate groups are an important family of plastics, the polyurethanes. Properties While carbamic acids are unstable, many carbamate esters or ionic) are stable and well known. Equilibrium with carbonate and bicarbonate In water solutions, the carbamate anion slowly equilibrates with the ammonium cation and the carbonate or bicarbonate anions: : : Calcium carbamate is soluble in water, whereas calcium carbonate is not. Adding a calcium salt to an ammonium carbamate/carbonate solution will precipitate some calcium carbonate immediately, a ...
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Antiarrhythmic Agents
Antiarrhythmic agents, also known as cardiac dysrhythmia medications, are a group of pharmaceuticals that are used to suppress abnormally fast rhythms ( tachycardias), such as atrial fibrillation, supraventricular tachycardia and ventricular tachycardia. Many attempts have been made to classify antiarrhythmic agents. Many of the antiarrhythmic agents have multiple modes of action, which makes any classification imprecise. Vaughan Williams classification The Vaughan Williams classification was introduced in 1970 by Miles Vaughan Williams.Vaughan Williams, EM (1970) "Classification of antiarrhythmic drugs". In ''Symposium on Cardiac Arrhythmias'' (Eds. Sandoe E; Flensted-Jensen E; Olsen KH). Astra, Elsinore. Denmark (1970) Vaughan Williams was a pharmacology tutor at Hertford College, Oxford. One of his students, Bramah N. Singh, contributed to the development of the classification system. The system is therefore sometimes known as the Singh-Vaughan Williams classification. The ...
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Diethylamine
Diethylamine is an organic compound with the formula (CH3CH2)2NH. It is a secondary amine. It is a flammable, weakly alkaline liquid that is miscible with most solvents. It is a colorless liquid, but commercial samples often appear brown due to impurities. It has a strong ammonia-like odor. Production and uses Diethylamine is made by the alumina-catalyzed reaction of ethanol and ammonia. It is obtained together with ethylamine and triethylamine. Annual production of three ethylamines was estimated in 2000 to be 80,000,000 kg. It is used in the production of corrosion inhibitor ''N'',''N''- diethylaminoethanol, by reaction with ethylene oxide. It is also a precursor to a wide variety of other commercial products. Diethylamine is also sometimes used in the illicit production of LSD. Supramolecular structure Diethylamine is the smallest and simplest molecule that features a supramolecular helix as its lowest energy aggregate. Other similarly sized hydrogen-bonding In c ...
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Olainfarm
Olainfarm AS is a Latvian leading manufacturer in the chemical and pharmaceutical sector of the Baltic States. The company was founded in 1972 as state enterprise "Olaines ķīmiski – farmaceitiskā rūpnīca" (Olaine Chemical-Pharmaceutical Plant). The main goal of founding the company was to ensure pharmaceutical substances and intermediates to several finished drug form manufacturing plants in the Soviet Union. As a result of privatization in 1997, the company was reorganized into a joint stock company, and its shares were listed on stock exchange. Olainfarm produces over 60 final dosage forms, 25 active pharmaceutical ingredients and 20 intermediates. The product portfolio is well diversified with the main emphasis on branded products, historically unique to Olainfarm. The key areas of specialization in final dosage forms include neurology (cholinesterase inhibitors, anxiolytics, psychostimulants, nootropics), cardiology (antiarrhythmics, energy metabolism enhancers), in ...
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Russia
Russia (, , ), or the Russian Federation, is a List of transcontinental countries, transcontinental country spanning Eastern Europe and North Asia, Northern Asia. It is the List of countries and dependencies by area, largest country in the world, with its internationally recognised territory covering , and encompassing one-eighth of Earth's inhabitable landmass. Russia extends across Time in Russia, eleven time zones and shares Borders of Russia, land boundaries with fourteen countries, more than List of countries and territories by land borders, any other country but China. It is the List of countries and dependencies by population, world's ninth-most populous country and List of European countries by population, Europe's most populous country, with a population of 146 million people. The country's capital and List of cities and towns in Russia by population, largest city is Moscow, the List of European cities by population within city limits, largest city entirely within E ...
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Wolff–Parkinson–White Syndrome
Wolff–Parkinson–White syndrome (WPWS) is a disorder due to a specific type of problem with the electrical system of the heart. About 60% of people with the electrical problem developed symptoms, which may include an abnormally fast heartbeat, palpitations, shortness of breath, lightheadedness, or syncope. Rarely, cardiac arrest may occur. The most common type of irregular heartbeat that occurs is known as paroxysmal supraventricular tachycardia. The cause of WPW is typically unknown and is likely due to a combination of chance and genetic factors. A small number of cases are due to a mutation of the PRKAG2 gene which may be inherited from a person's parents in an autosomal dominant fashion. The underlying mechanism involves an accessory electrical conduction pathway between the atria and the ventricles. It is associated with other conditions such as Ebstein anomaly and hypokalemic periodic paralysis. The diagnosis of WPW occurs with a combination of palpitations and when ...
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