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Adrenergic Release Inhibitors
Adrenergic release inhibitors are a class of drugs which inhibit the release of epinephrine (adrenaline) and/or norepinephrine (noradrenaline) from adrenergic nerve terminals and are used as antihypertensives. Examples of these agents include bethanidine, bretylium, debrisoquine, guanadrel, guanazodine, guancydine, guanethidine, guanoclor, and guanoxan. Most agents of this class are guanidinium Guanidine is the compound with the formula HNC(NH2)2. It is a colourless solid that dissolves in polar solvents. It is a strong base that is used in the production of plastics and explosives. It is found in urine predominantly in patients experie ... compounds and have little capacity to cross the blood–brain barrier. References {{Sympatholytic antihypertensives Adrenergic release inhibitors ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Guanethidine
Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as norepinephrine. Guanethidine is transported across the sympathetic nerve membrane by the same mechanism that transports norepinephrine itself (NET, uptake 1), and uptake is essential for the drug's action. Once guanethidine has entered the nerve, it is concentrated in transmitter vesicles, where it replaces norepinephrine. It may also inhibit the release of granules by decreasing norepinephrine. Medical uses Guanethidine was once a mainstay for hypertension resistant to other agents, and was often used safely during pregnancy, but it is no longer used in the US due to lack of availability. It is still licensed in some countries, e.g., UK, for the rapid control of blood pressure in a hypertensive emergency. Intravenous nerve block (Bier block) using guanethidine has been used to treat chronic pain caused by complex regional pain syndrome. Side effects Side effects include postural and e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Guanadrel
Guanadrel is an antihypertensive agent. It is used in the form of its sulfate. Mechanism of action Guanadrel is a postganglionic adrenergic blocking agent. Uptake of guanadrel and storage in sympathetic neurons occurs via the norepinephrine pump; guanadrel slowly displaces norepinephrine from its storage in nerve endings and thereby blocks the release of norepinephrine normally produced by nerve stimulation. The reduction in neurotransmitter release in response to sympathetic nerve stimulation, as a result of catecholamine depletion, leads to reduced arteriolar vasoconstriction, especially the reflex increase in sympathetic tone that occurs with a change in position. Guanadrel is rapidly and well absorbed from gastrointestinal tract. from Pharmacogenetics Knowledge Base In 1981 the |
Guanidinium
Guanidine is the compound with the formula HNC(NH2)2. It is a colourless solid that dissolves in polar solvents. It is a strong base that is used in the production of plastics and explosives. It is found in urine predominantly in patients experiencing renal failure. A guanidine moiety also appears in larger organic molecules, including on the side chain of arginine. Structure Guanidine can be thought of as a nitrogenous analogue of carbonic acid. That is, the C=O group in carbonic acid is replaced by a C=NH group, and each OH is replaced by a group. Isobutene can be seen as the carbon analogue in much the same way. A detailed crystallographic analysis of guanidine was elucidated 148 years after its first synthesis, despite the simplicity of the molecule. In 2013, the positions of the hydrogen atoms and their displacement parameters were accurately determined using single-crystal neutron diffraction. Production Guanidine can be obtained from natural sources, being first isolate ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Guanoxan
Guanoxan is a sympatholytic drug that was marketed as Envacar by Pfizer in the UK to treat high blood pressure Hypertension (HTN or HT), also known as high blood pressure (HBP), is a long-term medical condition in which the blood pressure in the arteries is persistently elevated. High blood pressure usually does not cause symptoms. Long-term high bl .... It was not widely used and was eventually withdrawn from the market due to liver toxicity. References Adrenergic release inhibitors Benzodioxans Guanidines Hepatotoxins Withdrawn drugs {{antihypertensive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Guanoclor
Guanoclor (INN), also known as guanochlor, is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes. Synthesis When β-(2,6-dichlorophenoxy)ethyl bromide (1) is reacted with hydrazine to give 2, and this is reacted with S-methylthiourea, guanochlor (3) results.Prepn of free base and sulfate: (1963 to Pfizer Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Street in Manhattan, New York City. The company was established in 1849 in New York by two German entrepreneurs, Charles Pfizer ...), C.A. 60, 14437d (1964). References Abandoned drugs Adrenergic release inhibitors Antihypertensive agents Chloroarenes Guanidines Phenol ethers {{Antihypertensive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Guanethidine
Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as norepinephrine. Guanethidine is transported across the sympathetic nerve membrane by the same mechanism that transports norepinephrine itself (NET, uptake 1), and uptake is essential for the drug's action. Once guanethidine has entered the nerve, it is concentrated in transmitter vesicles, where it replaces norepinephrine. It may also inhibit the release of granules by decreasing norepinephrine. Medical uses Guanethidine was once a mainstay for hypertension resistant to other agents, and was often used safely during pregnancy, but it is no longer used in the US due to lack of availability. It is still licensed in some countries, e.g., UK, for the rapid control of blood pressure in a hypertensive emergency. Intravenous nerve block (Bier block) using guanethidine has been used to treat chronic pain caused by complex regional pain syndrome. Side effects Side effects include postural and e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Debrisoquine
Debrisoquine is a derivative of guanidine. It is an antihypertensive drug similar to guanethidine. Debrisoquine is frequently used for phenotype, phenotyping the CYP2D6 enzyme, a drug-metabolizing enzyme. See also * Isoquinoline#Applications of derivatives The guanidine part of the molecule also appears in guanoxan and guanadrel. * The 7-bromo analog of Debrisoquine is called Guanisoquin. References Adrenergic release inhibitors Antihypertensive agents Guanidines Tetrahydroisoquinolines {{antihypertensive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epinephrine
Adrenaline, also known as epinephrine, is a hormone and medication which is involved in regulating visceral functions (e.g., respiration). It appears as a white microcrystalline granule. Adrenaline is normally produced by the adrenal glands and by a small number of neurons in the medulla oblongata. It plays an essential role in the fight-or-flight response by increasing blood flow to muscles, heart output by acting on the SA node, pupil dilation response, and blood sugar level. It does this by binding to alpha and beta receptors. It is found in many animals, including humans, and some single-celled organisms. It has also been isolated from the plant ''Scoparia dulcis'' found in Northern Vietnam. Medical uses As a medication, it is used to treat several conditions, including allergic reaction anaphylaxis, cardiac arrest, and superficial bleeding. Inhaled adrenaline may be used to improve the symptoms of croup. It may also be used for asthma when other treatments are not e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bretylium
Bretylium (also bretylium tosylate) is an antiarrhythmic agent. It blocks the release of noradrenaline from nerve terminals. In effect, it decreases output from the peripheral sympathetic nervous system. It also acts by blocking K+ channels and is considered a class III antiarrhythmic. The dose is 5–10 mg/kg and side effects are high blood pressure followed by low blood pressure and ventricular ectopy. Originally introduced in 1959 for the treatment of hypertension. Its use as an antiarrhythmic for ventricular fibrillation was discovered and patented by Marvin Bacaner in 1969 at the University of Minnesota. The American Heart Association removed bretylium from their 2000 ECC/ACC guidelines due to its unproven efficacy and ongoing supply problems. Many have cited these supply problems as an issue of raw materials needed in the production of Bretylium. By the release of the AHA 2005 ECC/ACC guidelines there is no mention of Bretylium and it is virtually unavailable throughou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bethanidine
Bethanidine (or betanidine) is a sympatholytic drug. See also * Phenoxybenzamine Phenoxybenzamine (marketed under the trade names Dibenzyline and Dibenyline) is a non-selective, irreversible alpha blocker. Uses It is used in the treatment of hypertension, and specifically that caused by pheochromocytoma. It has a slower on ... References Adrenergic release inhibitors Guanidines {{antihypertensive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
