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Gepefrine
3-Hydroxyamphetamine (INN; trade names Pressionorm, Gepefrine, and Wintonin), also known as meta-hydroxyamphetamine, and α-methyl-''meta''-tyramine, is an antihypotensive or sympathomimetic agent of the amphetamine family that is marketed in certain European countries. It is a known metabolite of amphetamine in rats. See also * 3,4-Dihydroxyamphetamine * Norfenfluramine * 4-Hydroxyamphetamine * Metaraminol Metaraminol, previously sold under the brand name Aramine among others and also known as metaradrine, is a stereoisomer of ''meta''-hydroxynorephedrine (3,β-dihydroxyamphetamine), is a potent sympathomimetic amine used in the prevention and tr ... * ''meta''-Tyramine References {{Phenethylamines Substituted amphetamines Phenols Sympathomimetics Norepinephrine-dopamine releasing agents ...
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Antihypotensive
An antihypotensive agent, also known as a vasopressor agent or simply vasopressor, or pressor, is any substance, whether endogeny (biology), endogenous or a medication, that tends to raise low blood pressure. Some antihypotensive drugs act as vasoconstrictors to increase total peripheral resistance, others sensitize adrenoreceptors to catecholamines - glucocorticoids, and the third class increase cardiac output - dopamine, dobutamine. If low blood pressure is due to blood loss, then preparations increasing volume of blood circulation—plasma-substituting solutions such as colloid and crystalloid solutions (salt solutions)—will raise the blood pressure without any direct vasopressor activity. Packed red blood cells, plasma or whole blood should not be used solely for volume expansion or to increase oncotic pressure of circulating blood. Blood products should only be used if reduced oxygen carrying capacity or coagulopathy is present. Other causes of either absolute (dehydration, ...
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Sympathomimetic
Sympathomimetic drugs (also known as adrenergic drugs and adrenergic amines) are stimulant compounds which mimic the effects of endogenous agonists of the sympathetic nervous system. Examples of sympathomimetic effects include increases in heart rate, force of cardiac contraction, and blood pressure. The primary endogenous agonists of the sympathetic nervous system are the catecholamines (i.e., epinephrine drenaline norepinephrine oradrenaline and dopamine), which function as both neurotransmitters and hormones. Sympathomimetic drugs are used to treat cardiac arrest and low blood pressure, or even delay premature labor, among other things. These drugs can act through several mechanisms, such as directly activating postsynaptic receptors, blocking breakdown and reuptake of certain neurotransmitters, or stimulating production and release of catecholamines. Mechanisms of action The mechanisms of sympathomimetic drugs can be direct-acting (direct interaction between drug ...
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Amphetamine
Amphetamine (contracted from alpha- methylphenethylamine) is a strong central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. It is also commonly used as a recreational drug. Amphetamine was discovered in 1887 and exists as two enantiomers: levoamphetamine and dextroamphetamine. ''Amphetamine'' properly refers to a specific chemical, the racemic free base, which is equal parts of the two enantiomers in their pure amine forms. The term is frequently used informally to refer to any combination of the enantiomers, or to either of them alone. Historically, it has been used to treat nasal congestion and depression. Amphetamine is also used as an athletic performance enhancer and cognitive enhancer, and recreationally as an aphrodisiac and euphoriant. It is a prescription drug in many countries, and unauthorized possession and distribution of amphetamine are often tightly controlled due to ...
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Europe
Europe is a large peninsula conventionally considered a continent in its own right because of its great physical size and the weight of its history and traditions. Europe is also considered a Continent#Subcontinents, subcontinent of Eurasia and it is located entirely in the Northern Hemisphere and mostly in the Eastern Hemisphere. Comprising the westernmost peninsulas of Eurasia, it shares the continental landmass of Afro-Eurasia with both Africa and Asia. It is bordered by the Arctic Ocean to the north, the Atlantic Ocean to the west, the Mediterranean Sea to the south and Asia to the east. Europe is commonly considered to be Boundaries between the continents of Earth#Asia and Europe, separated from Asia by the drainage divide, watershed of the Ural Mountains, the Ural (river), Ural River, the Caspian Sea, the Greater Caucasus, the Black Sea and the waterways of the Turkish Straits. "Europe" (pp. 68–69); "Asia" (pp. 90–91): "A commonly accepted division between Asia and E ...
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Metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and pheromones). A primary metabolite is directly involved in normal "growth", development, and reproduction. Ethylene exemplifies a primary metabolite produced large-scale by industrial microbiology. A secondary metabolite is not directly involved in those processes, but usually has an important ecological function. Examples include antibiotics and pigments such as resins and terpenes etc. Some antibiotics use primary metabolites as precursors, such as actinomycin, which is created from the primary metabolite tryptophan. Some sugars are metabolites, such as fructose or glucose, which are both p ...
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3,4-Dihydroxyamphetamine
α-Methyldopamine (α-Me-DA), also known as 3,4-dihydroxyamphetamine (3,4-DHA or HHA), is a research chemical of the catecholamine and amphetamine chemical classes. Its bis- glutathionyl metabolite is slightly neurotoxic when directly injected into the brain's ventricles. Interest lies in the fact that MDA and MDMA may not themselves be responsible for their neurotoxicity, as an intracerebroventricular injection does not appear to cause neurotoxicity. While many studies suggest excitotoxicity or oxidative stress as likely mechanisms, which may be an effect of MDMA itself, this has led to the search for other mechanisms for the observed toxicity of serotonin axons and subsequent reduction in 5-HT (serotonin) and 5-HIAA (its major metabolite in the body) in vivo following administration. A common theory follows that a metabolite in the periphery must be responsible, and several have been cited as responsible. Although alpha-methyldopamine is widely cited as the source of th ...
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Norfenfluramine
Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT2A, 5-HT2B, and 5-HT2C agonist. The action of norfenfluramine on 5-HT2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the tricuspid valve, known as cardiac fibrosis. This side effect led to the withdrawal of fenfluramine as an anorectic agent worldwide, and to the withdrawal of benfluorex in Europe, as both fenfluramine and benfluorex form norfenfluramine as an active metabolite. It is a human TAAR1 agonist. See also * Fenfluramine * Benfluorex Benfluorex, sold under the brand name Mediator, is an anorectic and hypolipidemic agent that is structurally related to fenfluramine (a substituted amphetamine). It may improve glycemic control and decrease insulin resistance in people with poorly ... * Norfenfluramine is the pre ...
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4-Hydroxyamphetamine
4-Hydroxyamphetamine (4HA), also known as hydroxyamfetamine, hydroxyamphetamine, oxamphetamine, norpholedrine, ''para''-hydroxyamphetamine, and α-methyltyramine, is a drug that stimulates the sympathetic nervous system. It is used medically in eye drops to dilate the pupil (a process called mydriasis), so that the back of the eye can be examined. It is also a major metabolite of amphetamine and certain substituted amphetamines. Medical use 4-Hydroxyamphetamine is used in eye drops to dilate the pupil (a process called mydriasis) so that the back of the eye can be examined. This is a diagnostic test for Horner's syndrome. Patients with Horner's syndrome exhibit anisocoria brought about by lesions on the nerves that connect to the nasociliary branch of the ophthalmic nerve. Application of 4-hydroxyamphetamine to the eye can indicate whether the lesion is preganglionic or postganglionic based on the pupil's response. If the pupil dilates, the lesion is preganglionic. If the ...
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Metaraminol
Metaraminol, previously sold under the brand name Aramine among others and also known as metaradrine, is a stereoisomer of ''meta''-hydroxynorephedrine (3,β-dihydroxyamphetamine), is a potent sympathomimetic amine used in the prevention and treatment of hypotension, particularly as a complication of anesthesia. It is an α1-adrenergic receptor agonist with some β effect. It is currently sold in its generic form by Slayback Pharma. Pharmacology and use as a vasopressor Metaraminol is given intravenously as either a bolus (often 0.5-1mg doses) or as an infusion, usually via peripheral intravenous access. Metaraminol is commonly available as 10mg in 1mL, that requires dilution prior to administration (often made up to a 0.5mg/mL solution), however pre-prepared syringes of metaraminol for bolus use for hypotension are also commonly available. Pharmacodynamics The dominant mechanism for the vasopressor action of metaraminol is indirect, with metaraminol displacing noradrena ...
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Meta-Tyramine
''meta''-Tyramine, also known as ''m''-tyramine and 3-tyramine, is an endogenous trace amine neuromodulator and a structural analog of phenethylamine. It is a positional isomer of ''para''-tyramine, and similarly to it, has effects on the adrenergic and dopaminergic systems. ''meta''-Tyramine is produced in humans via aromatic amino acid decarboxylase-mediated metabolism of ''meta''-tyrosine. meta-Tyramine can be metabolized into dopamine via peripheral or brain CYP2D6 enzyme Enzymes () are proteins that act as biological catalysts by accelerating chemical reactions. The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products ...s in humans. See also * ''para''-Tyramine * 3-Methoxytyramine References Phenethylamines Phenols TAAR1 agonists Trace amines Norepinephrine-dopamine releasing agents {{nervous-system-drug-stub ...
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Substituted Amphetamines
Substituted amphetamines are a class of compounds based upon the amphetamine structure; it includes all derivative compounds which are formed by replacing, or substituting, one or more hydrogen atoms in the amphetamine core structure with substituents. The compounds in this class span a variety of pharmacological subclasses, including stimulants, empathogens, and hallucinogens, among others. Examples of substituted amphetamines are amphetamine (itself), methamphetamine, ephedrine, cathinone, phentermine, mephentermine, bupropion, methoxyphenamine, selegiline, amfepramone (diethylpropion), pyrovalerone, MDMA (ecstasy), and DOM (STP). Some of amphetamine's substituted derivatives occur in nature, for example in the leaves of ''Ephedra'' and khat plants. Amphetamine was first produced at the end of the 19th century. By the 1930s, amphetamine and some of its derivative compounds found use as decongestants in the symptomatic treatment of colds and also occasionally as psychoac ...
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