Buflomedil Synthesis
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Buflomedil Synthesis
Buflomedil, sold under the brand name Loftyl, is a vasoactive drug used to treat claudication or the symptoms of peripheral arterial disease. It is currently not approved by the Food and Drug Administration (FDA) for use in the United States. Toxicity This drug has been suspended from marketing in the European Union, because of concerns about severe neurological and cardiac toxicity. In its press release dated 17 November 2011 EMA suggested that doctors "should stop using buflomedil and consider alternative treatment options". The European Commission advised all member states to revoke marketing authorisation. Various adverse effect An adverse effect is an undesired harmful effect resulting from a medication or other intervention, such as surgery. An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. The term complica ...s have been reported to the FDA.http://www.drugcite.com/?q=BUFLOMEDIL&s=&a= Synthesis ] Acylation ...
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Vasoactive
A vasoactive substance is an endogenous agent or pharmaceutical drug that has the effect of either increasing or decreasing blood pressure and/or heart rate through its vasoactivity, that is, vascular activity (effect on blood vessels). By adjusting vascular compliance and vascular resistance, typically through vasodilation and vasoconstriction, it helps the body's homeostatic mechanisms (such as the renin–angiotensin system) to keep hemodynamics under control. For example, angiotensin, bradykinin, histamine, nitric oxide, and vasoactive intestinal peptide are important endogenous vasoactive substances. Vasoactive drug therapy is typically used when a patient has the blood pressure and heart rate monitored constantly. The dosage is typically titrated (adjusted up or down) to achieve a desired effect or range of values as determined by competent clinicians. Vasoactive drugs are typically administered using a volumetric infusion device (IV pump). This category of drugs re ...
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Claudication
Claudication is a medical term usually referring to impairment in walking, or pain, discomfort, numbness, or tiredness in the legs that occurs during walking or standing and is relieved by rest. The perceived level of pain from claudication can be mild to extremely severe. Claudication is most common in the calves but it can also affect the feet, thighs, hips, buttocks, or arms. The word ''claudication'' comes from the Latin ''claudicare'' meaning 'to limp'. Claudication that appears after a short amount of walking may sometimes be described by US medical professionals by the number of typical city street blocks that the patient can walk before the onset of claudication. Thus, "one-block claudication" appears after walking one block, "two-block claudication" appears after walking two blocks, etc. The term ''block'' would be understood more exactly locally but is on the order of 100 metres. Types Intermittent vascular Intermittent vascular (or arterial) claudication (Latin: ' ...
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Peripheral Arterial Disease
Peripheral artery disease (PAD) is an abnormal narrowing of arteries other than those that supply the heart or brain. When narrowing occurs in the heart, it is called coronary artery disease, and in the brain, it is called cerebrovascular disease. Peripheral artery disease most commonly affects the legs, but other arteries may also be involved – such as those of the arms, neck, or kidneys. The classic symptom is leg pain when walking which resolves with rest, known as intermittent claudication. Other symptoms include skin ulcers, bluish skin, cold skin, or abnormal nail and hair growth in the affected leg. Complications may include an infection or tissue death which may require amputation; coronary artery disease, or stroke. Up to 50% of people with PAD do not have symptoms. The greatest risk factor for PAD is cigarette smoking. Other risk factors include diabetes, high blood pressure, kidney problems, and high blood cholesterol. The most common underlying mechanism of peri ...
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Food And Drug Administration
The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food safety, tobacco products, caffeine products, dietary supplements, Prescription drug, prescription and Over-the-counter drug, over-the-counter pharmaceutical drugs (medications), vaccines, biopharmaceuticals, blood transfusions, medical devices, electromagnetic radiation emitting devices (ERED), cosmetics, Animal feed, animal foods & feed and Veterinary medicine, veterinary products. The FDA's primary focus is enforcement of the Federal Food, Drug, and Cosmetic Act (FD&C), but the agency also enforces other laws, notably Section 361 of the Public Health Service Act, as well as associated regulations. Much of this regulatory-enforcement work is not d ...
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Neurotoxicity
Neurotoxicity is a form of toxicity in which a biological, chemical, or physical agent produces an adverse effect on the structure or function of the central and/or peripheral nervous system. It occurs when exposure to a substance – specifically, a neurotoxin or neurotoxicant– alters the normal activity of the nervous system in such a way as to cause permanent or reversible damage to nervous tissue. This can eventually disrupt or even kill neurons, which are cells that transmit and process signals in the brain and other parts of the nervous system. Neurotoxicity can result from organ transplants, radiation treatment, certain drug therapies, recreational drug use, and exposure to heavy metals, bites from certain species of venomous snakes, pesticides, certain industrial cleaning solvents, fuels and certain naturally occurring substances. Symptoms may appear immediately after exposure or be delayed. They may include limb weakness or numbness, loss of memory, vision, and/or ...
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Cardiac Toxicity
Cardiotoxicity is the occurrence of heart dysfunction as electric or muscle damage, resulting in heart toxicity. The heart becomes weaker and is not as efficient in pumping blood. Cardiotoxicity may be caused by chemotherapy (a usual example is the class of anthracyclines) treatment and/or radiotherapy; complications from anorexia nervosa; adverse effects of heavy metals intake; the long-term abuse of or ingestion at high doses of certain strong stimulants such as cocaine; or an incorrectly administered drug such as bupivacaine. One of the ways to detect cardiotoxicity at early stages when there is a subclinical dysfunction is by measuring changes in regional function of the heart using strains. See also * Cardiotoxin III * Batrachotoxin * Heart failure * Drug interaction Drug interactions occur when a drug's mechanism of action is disturbed by the concomitant administration of substances such as foods, beverages, or other drugs. The cause is often the inhibition of the speci ...
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Adverse Effect
An adverse effect is an undesired harmful effect resulting from a medication or other intervention, such as surgery. An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. The term complication is similar to adverse effect, but the latter is typically used in pharmacological contexts, or when the negative effect is expected or common. If the negative effect results from an unsuitable or incorrect dosage or procedure, this is called a medical error and not an adverse effect. Adverse effects are sometimes referred to as "iatrogenic" because they are generated by a physician/treatment. Some adverse effects occur only when starting, increasing or discontinuing a treatment. Adverse effects can also be caused by placebo treatments (in which case the adverse effects are referred to as nocebo effects). Using a drug or other medical intervention which is contraindicated may increase the risk of adverse effects. Adverse effects may c ...
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Buflomedil Synthesis
Buflomedil, sold under the brand name Loftyl, is a vasoactive drug used to treat claudication or the symptoms of peripheral arterial disease. It is currently not approved by the Food and Drug Administration (FDA) for use in the United States. Toxicity This drug has been suspended from marketing in the European Union, because of concerns about severe neurological and cardiac toxicity. In its press release dated 17 November 2011 EMA suggested that doctors "should stop using buflomedil and consider alternative treatment options". The European Commission advised all member states to revoke marketing authorisation. Various adverse effect An adverse effect is an undesired harmful effect resulting from a medication or other intervention, such as surgery. An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. The term complica ...s have been reported to the FDA.http://www.drugcite.com/?q=BUFLOMEDIL&s=&a= Synthesis ] Acylation ...
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Hoesch Reaction
The Hoesch reaction or Houben–Hoesch reaction is an organic reaction in which a nitrile reacts with an arene compound to form an aryl ketone. The reaction is a type of Friedel-Crafts acylation with hydrogen chloride and a Lewis acid catalyst. The synthesis of 2,4,6-Trihydroxyacetophenone (THAP) from phloroglucinol is representative: If two-equivalents are added, 2,4-Diacetylphloroglucinol is the product. : An imine can be isolated as an intermediate reaction product. The attacking electrophile is possibly a species of the type R-C+=NHCl−. The arene must be electron-rich i.e. phenol or aniline type. A related reaction is the Gattermann reaction in which hydrocyanic acid not a nitrile is used. The reaction is named after Kurt Hoesch and Josef Houben''Über die Kern-Kondensation von Phenolen und Phenol-äthern mit Nitrilen zu Phenol- und Phenol-äther-Ketimiden und -Ketonen (I.)'' Berichte der deutschen chemischen Gesellschaft (A and B Series) Volume 59, Issue 11, Date: 8. ...
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Alpha-1 Blockers
Alpha 1 or Alpha-1 may refer to: *Alpha-1 adrenergic receptor, a G protein-coupled receptor *Alpha-1 antitrypsin, a protein **Alpha-1 antitrypsin deficiency, a genetic disorder *Alpha-1-fetoprotein or Alpha-fetoprotein, a protein *Alpha-One, a fictional spacecraft in '' Buzz Lightyear of Star Command: The Adventure Begins'' * ''Alpha 1'' (Robert Silverberg anthology), a 1970 book See also * * *Alpha (other) *AMY1A Alpha-amylase 1 is an enzyme that in humans is encoded by the ''AMY1A'' gene In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth' ... or Alpha-1A or, an enzyme found in humans and other mammals * List of A1 genes, proteins or receptors {{disambiguation ...
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Piceol Ethers
Piceol is a phenolic compound found in the needles and in mycorrhizal roots of Norway spruces (''Picea abies''). Picein is the glucoside of piceol. Uses Piceol is used in the synthesis of several pharmaceutical drugs including octopamine, sotalol, bamethan, and dyclonine. Piceol can be used to make acetaminophen by oxime formation with hydroxylamine and subsequent Beckmann rearrangement in acid. Anticonvulsants are also possible by Mannich reaction: Metabolism Diprenylated derivatives of piceol can be isolated from ''Ophryosporus macrodon''. 4-Hydroxyacetophenone monooxygenase is an enzyme that transforms piceol into O-acetylhydroquinone. This enzyme is found in ''Pseudomonas fluorescens''. See also *Paroxypropione, where the acetyl group is replaced by a propionyl group. *Apocynin Apocynin, also known as acetovanillone, is a natural organic compound structurally related to vanillin. It has been isolated from a variety of plant sources and is being studied for its vari ...
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