Imidafenacin
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Imidafenacin
Imidafenacin (INN) is a urinary antispasmodic of the anticholinergic class. Pharmacol: Synthesis *The sidechain is a versatile precursor also used in the synthesis of: Bezitramide, Piritramide, Diphenoxylate, & others. The alkylation of Diphenylacetonitrile 6-29-3(1) with 1,2-dibromoethane 1,2-Dibromoethane, also known as ethylene dibromide (EDB), is an organobromine compound with the chemical formula . Although trace amounts occur naturally in the ocean, where it is formed probably by algae and kelp, it is mainly synthetic. It is ... (2) gives 4-Bromo-2,2-Diphenylbutyronitrile 9186-58-8(3). Alkylation with 2-Methylimidazole (4) gives 4-(2-Methyl-1H-imidazol-1-yl)-2,2-diphenylbutanenitrile 14777-43-2(5). Partial hydrolysis of the nitrile to the amide completes the synthesis of ' (6). References Muscarinic antagonists Imidazoles Carboxamides {{genito-urinary-drug-stub ...
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Imidafenacin Synthesis
Imidafenacin ( INN) is a urinary antispasmodic of the anticholinergic class. Pharmacol: Synthesis *The sidechain is a versatile precursor also used in the synthesis of: Bezitramide, Piritramide, Diphenoxylate, & others. The alkylation of Diphenylacetonitrile 6-29-3(1) with 1,2-dibromoethane (2) gives 4-Bromo-2,2-Diphenylbutyronitrile 9186-58-8(3). Alkylation with 2-Methylimidazole 2-Methylimidazole is an organic compound that is structurally related to imidazole with the chemical formula CH3C3H2N2H. It is a white or colorless solid that is highly soluble in polar organic solvents and water. It is a precursor to a range of d ... (4) gives 4-(2-Methyl-1H-imidazol-1-yl)-2,2-diphenylbutanenitrile 14777-43-2(5). Partial hydrolysis of the nitrile to the amide completes the synthesis of ' (6). References Muscarinic antagonists Imidazoles Carboxamides {{genito-urinary-drug-stub ...
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Piritramide
Piritramide(R-3365, trade names Dipidolor, Piridolan, Pirium and others) is a synthetic opioid analgesic (narcotic painkiller) that is marketed in certain European countries including: Austria, Belgium, Czech Republic, Slovenia, Germany and the Netherlands. It comes in free form, is about 0.75x times as potent as morphine and is given parenterally (by injection) for the treatment of severe pain. Nausea, vomiting, respiratory depression and constipation are believed to be less frequent with piritramide than with morphine (the gold standard opioid against which other opioids are compared and contrasted), and it produces more rapid-onset analgesia (pain relief) when compared to morphine and pethidine. After intravenous administration the onset of analgesia is as little as 1–2 minutes, which may be related to its great lipophilicity. The analgesic and sedative effects of piritramide are believed to be potentiated with phenothiazines and its emetic (nausea/vomiting-inducing) effects ...
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By Mouth
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mou ...
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Urinary
The urinary system, also known as the urinary tract or renal system, consists of the kidneys, ureters, bladder, and the urethra. The purpose of the urinary system is to eliminate waste from the body, regulate blood volume and blood pressure, control levels of electrolytes and metabolites, and regulate blood pH. The urinary tract is the body's drainage system for the eventual removal of urine. The kidneys have an extensive blood supply via the renal arteries which leave the kidneys via the renal vein. Each kidney consists of functional units called nephrons. Following filtration of blood and further processing, wastes (in the form of urine) exit the kidney via the ureters, tubes made of smooth muscle fibres that propel urine towards the urinary bladder, where it is stored and subsequently expelled from the body by urination (voiding). The female and male urinary system are very similar, differing only in the length of the urethra. Urine is formed in the kidneys through a filtratio ...
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Antispasmodic
An antispasmodic (synonym: spasmolytic) is a pharmaceutical drug or other agent that suppresses muscle spasms. Smooth muscle spasm One type of antispasmodics is used for smooth muscle relaxation, especially in tubular organs of the gastrointestinal tract. The effect is to prevent spasms of the stomach, intestine or urinary bladder. Both dicyclomine and hyoscyamine are antispasmodic due to their anticholinergic action. Both of these drugs have general side effects and can worsen gastroesophageal reflux disease. Mebeverine is a musculotropic spasmolytic with a strong and selective action on the smooth muscle spasm of the gastrointestinal tract, particularly of the colon. It does not have the acetylcholine side effect commonly seen in an anticholinergic antispasmodic. Papaverine is an opium alkaloid used to treat visceral spasms, erectile dysfunction and investigated as antipsychotic drug due to its potency to inhibit phosphodiesterase PDE10A. Peppermint oil has been traditio ...
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Anticholinergic
Anticholinergics (anticholinergic agents) are substances that block the action of the neurotransmitter called acetylcholine (ACh) at synapses in the central and peripheral nervous system. These agents inhibit the parasympathetic nervous system by selectively blocking the binding of ACh to its receptor in nerve cells. The nerve fibers of the parasympathetic system are responsible for the involuntary movement of smooth muscles present in the gastrointestinal tract, urinary tract, lungs, sweat glands, and many other parts of the body. In broad terms, anticholinergics are divided into two categories in accordance with their specific targets in the central and peripheral nervous system and at the neuromuscular junction: antimuscarinic agents, and antinicotinic agents ( ganglionic blockers, neuromuscular blockers). The term "anticholinergic" is typically used to refer to antimuscarinics which competitively inhibit the binding of ACh to muscarinic acetylcholine receptors; such agen ...
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Bezitramide
Bezitramide is an opioid analgesic. Bezitramide itself is a prodrug which is readily hydrolyzed in the gastrointestinal tract to its active metabolite, despropionyl-bezitramide. Bezitramide was discovered at Janssen Pharmaceutica in 1961. It is most commonly marketed under the trade name Burgodin. The drug was pulled from the shelves in the Netherlands in 2004 after fatal overdose cases, including one where a five-year-old child took one tablet from his mother's purse, ate it, and promptly died. Bezitramide is regulated much the same as morphine in all known jurisdictions and is a Schedule II substance under the United States' Controlled Substances Act of 1970, with an ACSCN of 9800 and zero annual manufacturing quota. However, as of May 2021, it has never been marketed in the United States. Synthesis The Sn2 alkylation between 4-bromo-2,2-diphenylbutyronitrile 9186-58-8(1) and 4-(2-oxo-1-benzimidazolinyl)-piperidine 0662-53-7(2) with affords depropionylbezitramide 3898-28- ...
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Diphenoxylate
Diphenoxylate is a centrally active opioid drug of the phenylpiperidine series that is used as a combination drug with atropine for the treatment of diarrhea. Diphenoxylate is an opioid and acts by slowing intestinal contractions; the atropine is present to prevent drug abuse and overdose. It should not be given to children due to the risk that they will stop breathing and should not be used in people with ''Clostridium difficile'' infection. Medical use Diphenoxylate is used to treat diarrhea in adults; it is only available as a combination drug with a subtherapeutic dose of atropine to prevent abuse. It should not be used in children due to the risk of respiratory depression. It does not appear harmful to a fetus but the risks have not been fully explored. It should not be taken with other central depressants like alcohol, as they can increase its risks. It should not be used for people with diarrhea caused by an infection, for example with ''Clostridium difficile'' infec ...
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1,2-dibromoethane
1,2-Dibromoethane, also known as ethylene dibromide (EDB), is an organobromine compound with the chemical formula . Although trace amounts occur naturally in the ocean, where it is formed probably by algae and kelp, it is mainly synthetic. It is a dense colorless liquid with a faint sweet odor, detectable at 10 ppm, is a widely used and sometimes-controversial fumigant. The combustion of 1,2-dibromoethane produces hydrogen bromide gas that is significantly corrosive. Preparation and use It is produced by the reaction of ethylene gas with bromine, in a classic halogen addition reaction: :CH=CH + Br → BrCH–CHBr Historically, 1,2-dibromoethane was used as a component in anti-knock additives in leaded fuels. It reacts with lead residues to generate volatile lead bromides, thereby preventing fouling of the engine with lead deposits. Pesticide It has been used as a pesticide in soil and on various crops. The applications were initiated after the forced retirement of 1,2-dibrom ...
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2-Methylimidazole
2-Methylimidazole is an organic compound that is structurally related to imidazole with the chemical formula CH3C3H2N2H. It is a white or colorless solid that is highly soluble in polar organic solvents and water. It is a precursor to a range of drugs and is a ligand in coordination chemistry. Synthesis and reactions It is prepared by condensation of glyoxal, ammonia and acetaldehyde, a Radziszewski reaction. Nitration gives 5-nitro derivative.Ebel, K., Koehler, H., Gamer, A. O., & Jäckh, R. "Imidazole and Derivatives." In Ullmann’s Encyclopedia of Industrial Chemistry; 2002 Wiley-VCH, 2-Methylimidazole is a sterically hindered imidazole that is used to simulate the coordination of histidine to heme complexes. It can be deprotonated to make imidazolate-based coordination polymers. Applications 2-Methylimidazole is a precursor to the several members of the nitroimidazole antibiotics that are used to combat anaerobic bacterial and parasitic infections. File:Dimetridazole ...
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