Nitrovasodilators
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Nitrovasodilators
A nitrovasodilator is a pharmaceutical agent that causes vasodilation (widening of blood vessels) by donation of nitric oxide (NO), and is mostly used for the treatment and prevention of angina pectoris. This group of drugs includes nitrates (esters of nitric acid), which are reduced to NO in the body, as well as some other substances. Examples Here is a list of examples of the nitrate type (in alphabetical order): #Diethylene glycol dinitrate #Glyceryl trinitrate (nitroglycerin) #Isosorbide mononitrate and dinitrate # Itramin tosilate #Nicorandil (which additionally acts as a potassium channel opener) # Pentaerithrityl tetranitrate # Propatylnitrate # Sinitrodil #Tenitramine # Trolnitrate Nitrovasodilators which aren't nitrates include molsidomine and its active metabolite linsidomine, as well as sodium nitroprusside. These substances do not need to be reduced to donate NO. Medical uses The nitrates are used for the treatment and prevention of angina and acute myocar ...
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Molsidomine
Molsidomine (trade names Corvasal, Corvaton and many others) is an orally active, long acting vasodilating drug used to treat angina pectoris. Molsidomine is metabolized in the liver to the active metabolite linsidomine. Linsidomine is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound. Medical uses Molsidomine is used for the prevention and long-term treatment of stable and unstable angina pectoris, with or without left heart failure. It is also used to treat angina in the context of an acute myocardial infarction. Contraindications The drug must not be used in patients with acute cardiac arrest or severe hypotension (low blood pressure), during lactation, and in combination with PDE5 inhibitors such as sildenafil. Side effects The most common adverse effects are headache, which occurs in 10–25% of patients, and low blood pressure. Side effects occurring in fewer than 1% of patients include dizziness, nausea, reflex tachycardi ...
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Molsidomine
Molsidomine (trade names Corvasal, Corvaton and many others) is an orally active, long acting vasodilating drug used to treat angina pectoris. Molsidomine is metabolized in the liver to the active metabolite linsidomine. Linsidomine is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound. Medical uses Molsidomine is used for the prevention and long-term treatment of stable and unstable angina pectoris, with or without left heart failure. It is also used to treat angina in the context of an acute myocardial infarction. Contraindications The drug must not be used in patients with acute cardiac arrest or severe hypotension (low blood pressure), during lactation, and in combination with PDE5 inhibitors such as sildenafil. Side effects The most common adverse effects are headache, which occurs in 10–25% of patients, and low blood pressure. Side effects occurring in fewer than 1% of patients include dizziness, nausea, reflex tachycardi ...
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Nitroglycerin (drug)
Nitroglycerin, also known as glyceryl trinitrate (GTN), is a medication used for heart failure, high blood pressure, anal fissures, painful periods, and to treat and prevent chest pain caused by decreased blood flow to the heart (angina) or due to the recreational use of cocaine. This includes chest pain from a heart attack. It is taken by mouth, under the tongue, applied to the skin, or by injection into a vein. Common side effects include headache and low blood pressure. The low blood pressure can be severe. It is unclear if use in pregnancy is safe for the baby. It should not be used together with medications within the PDE5 inhibitor family such as sildenafil due to the risk of low blood pressure. Nitroglycerin is in the nitrate family of medications. While it is not entirely clear how it works, it is believed to function by dilating blood vessels. Nitroglycerin was written about as early as 1846 and came into medical use in 1878. It is on the World Health Organizat ...
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Nitric Oxide
Nitric oxide (nitrogen oxide or nitrogen monoxide) is a colorless gas with the formula . It is one of the principal oxides of nitrogen. Nitric oxide is a free radical: it has an unpaired electron, which is sometimes denoted by a dot in its chemical formula In chemistry, a chemical formula is a way of presenting information about the chemical proportions of atoms that constitute a particular chemical compound or molecule, using chemical element symbols, numbers, and sometimes also other symbols, ... (•N=O or •NO). Nitric oxide is also a heteronuclear diatomic molecule, a class of molecules whose study spawned early modern molecular orbital theory, theories of chemical bonding. An important Reaction intermediate, intermediate in chemical industry, industrial chemistry, nitric oxide forms in combustion systems and can be generated by lightning in thunderstorms. In mammals, including humans, nitric oxide is a signaling molecule in many physiological and pathological pro ...
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Potassium Channel Opener
A potassium channel opener is a type of drug which facilitates ion transmission through potassium channels. Examples Some examples include: *Diazoxide vasodilator used for hypertension, smooth muscle relaxing activity *Minoxidil vasodilator used for hypertension, also used to treat hair loss *Nicorandil vasodilator used to treat angina *Pinacidil *Retigabine, an anticonvulsant * Flupirtine, analgesic with muscle relaxant and anticonvulsant properties See also * Potassium channel blocker Potassium channel blockers are agents which interfere with conduction through potassium channels. Medical uses Arrhythmia Potassium channel blockers used in the treatment of cardiac arrhythmia are classified as class III antiarrhythmic age ... References {{pharmacology-stub ...
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Glyceryl Trinitrate
Nitroglycerin (NG), (alternative spelling of nitroglycerine) also known as trinitroglycerin (TNG), nitro, glyceryl trinitrate (GTN), or 1,2,3-trinitroxypropane, is a dense, colorless, oily, explosive liquid most commonly produced by nitrating glycerol with white fuming nitric acid under conditions appropriate to the formation of the nitric acid ester. Chemically, the substance is an organic nitrate compound rather than a nitro compound, but the traditional name is retained. Invented in 1847 by Ascanio Sobrero, nitroglycerin has been used ever since as an active ingredient in the manufacture of explosives, namely dynamite, and as such it is employed in the construction, demolition, and mining industries. Since the 1880s, it has been used by militaries as an active ingredient and gelatinizer for nitrocellulose in some solid propellants such as cordite and ballistite. It is a major component in double-based smokeless propellants used by reloaders. Combined with nitrocellul ...
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Acute Myocardial Infarction
A myocardial infarction (MI), commonly known as a heart attack, occurs when blood flow decreases or stops to the coronary artery of the heart, causing damage to the heart muscle. The most common symptom is chest pain or 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, feeling faint, a cold sweat or 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 irregular heartbeat, cardiogenic shock or cardiac arrest. Most MIs occur due to coronary artery disease. Risk factors include high blood pressure, smoking, diabetes, lack of ...
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Nitroglycerin
Nitroglycerin (NG), (alternative spelling of nitroglycerine) also known as trinitroglycerin (TNG), nitro, glyceryl trinitrate (GTN), or 1,2,3-trinitroxypropane, is a dense, colorless, oily, explosive liquid most commonly produced by nitrating glycerol with white fuming nitric acid under conditions appropriate to the formation of the nitric acid ester. Chemically, the substance is an organic nitrate compound rather than a nitro compound, but the traditional name is retained. Invented in 1847 by Ascanio Sobrero, nitroglycerin has been used ever since as an active ingredient in the manufacture of explosives, namely dynamite, and as such it is employed in the construction, demolition, and mining industries. Since the 1880s, it has been used by militaries as an active ingredient and gelatinizer for nitrocellulose in some solid propellants such as cordite and ballistite. It is a major component in double-based smokeless propellants used by reloaders. Combined with nitrocellulose, hund ...
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Sodium Nitroprusside
Sodium nitroprusside (SNP), sold under the brand name Nitropress among others, is a medication used to lower blood pressure. This may be done if the blood pressure is very high and resulting in symptoms, in certain types of heart failure, and during surgery to decrease bleeding. It is used by continuous injection into a vein. Onset is nearly immediate and effects last for up to ten minutes. It is available as a generic medication. Side effects and mechanism Common side effects include low blood pressure and cyanide toxicity. Other serious side effects include methemoglobinemia. It is not generally recommended during pregnancy due to concerns of side effects. High doses are not recommended for more than ten minutes. It works by increasing nitric oxide levels in the blood, which increases cGMP levels in cells, and causes dilation of blood vessels. History, society and culture Sodium nitroprusside was discovered as early as 1850 and found to be useful in medicine in 1928. It i ...
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Linsidomine
Linsidomine (3-morpholinosydnonimine or SIN-1) is a vasodilator. It is a metabolite of the antianginal drug molsidomine and acts by releasing NO from the endothelial cells nonenzymatically. It also hyperpolarizes the cell membrane through influencing the sodium-potassium pump and thereby rendering it less responsive to adrenergic stimulation. Linsidomine injection at a dose of 1 mg produces usable erection in about 70% of patients and full erection in up to 50% of patients. Linsidomine does not appear to be associated with priapism. Linsidomine is neurotoxic and promotes oxidative stress on neurons. Linsidomine is a peroxynitrite-generating compound involved in the pathogenesis of neurodegenerative diseases A neurodegenerative disease is caused by the progressive loss of structure or function of neurons, in the process known as neurodegeneration. Such neuronal damage may ultimately involve cell death. Neurodegenerative diseases include amyotrophic .... References { ...
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Active Metabolite
An active metabolite is an active form of a drug after it has been processed by the body. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which continues to produce effects in the body. Usually these effects are similar to those of the parent drug but weaker, although they can still be significant (see e.g. 11-hydroxy-THC, morphine-6-glucuronide). Certain drugs such as codeine and tramadol have metabolites (morphine and ''O''-desmethyltramadol respectively) that are stronger than the parent drug and in these cases the metabolite may be responsible for much of the therapeutic action of the parent drug. Sometimes, however, metabolites may produce toxic effects and patients must be monitored carefully to ensure they do not build up in the body. This is an issue with some well-known drugs, such as pethidine (meperidine) and dextropropoxyphene. Prodrugs Sometimes drugs are formulated in an inactive form that is designe ...
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