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Muscarinic Agonists
A muscarinic acetylcholine receptor agonist, also simply known as a muscarinic agonist or as a muscarinic agent, is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation. Clinical significance M1 M1-type muscarinic acetylcholine receptors play a role in cognitive processing. In Alzheimer disease (AD), amyloid formation may decrease the ability of these receptors to transmit signals, leading to decreased cholinergic activity. As these receptors themselves appear relatively unchanged in the disease process, they have become a potential therapeutic target when trying to improve cognitive function in patients with AD. A number of muscarinic agonists have been developed and are under investigation to treat AD. These agents show promise as they are neurotrophic, decrease amyloid depositions, and improve damage due to oxidative stress. Tau-phosphorylation ...
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Skeletal Formula
The skeletal formula, line-angle formula, bond-line formula or shorthand formula of an organic compound is a type of minimalist structural formula representing a molecule's Atom, atoms, structural isomer, bonds and some details of its molecular geometry, geometry. The lines in a skeletal formula represent bonds between carbon atoms, unless labelled with another element. Labels are optional for carbon atoms, and the hydrogen atoms attached to them. An early form of this representation was first developed by organic chemist August Kekulé, while the modern form is closely related to and influenced by the Lewis structure of molecules and their valence electrons. Hence they are sometimes termed Kekulé structures or Lewis–Kekulé structures. Skeletal formulas have become ubiquitous in organic chemistry, partly because they are relatively quick and simple to draw, and also because the Arrow pushing, curved arrow notation used for discussions of reaction mechanisms and Resonance ( ...
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Arecoline
Arecoline is a cholinergic agent, stimulant, and natural product, naturally occurring alkaloid found in areca nut, areca (betel) nuts of the areca palm (''Areca catechu'') found in South Asia, South and Southeast Asia. Its effects, depending on the dose, include stimulation, alertness, increased concentration, nootropic, cognitive enhancement, mood lift, elation, euphoriant, euphoria, aphrodisiac, pro-sexual effects, mental relaxation, relaxation, anxiolytic, reduced anxiety, and sedation, as well as drug addiction, addiction and drug withdrawal, withdrawal symptoms upon drug discontinuation, discontinuation. Its effects are described as subtle and it has been likened to a strong cup of coffee. There are also active constituents of areca nuts, but arecoline is the key active component, with a percentage of ~0.3 to 0.6%. Areca nuts are drug administration, administered by chewing for 5 to 20minutes without swallowing. Side effects of arecoline include hypersalivation, hypotensio ...
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Methacholine
Methacholine ( INN, USAN) (trade name Provocholine), also known as acetyl-β-methylcholine, is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system. Medical uses Methacholine is primarily used to diagnose bronchial hyperreactivity, which is the hallmark of asthma and also occurs in chronic obstructive pulmonary disease. This is accomplished through the bronchial challenge test, or methacholine challenge, in which a subject inhales aerosolized methacholine, leading to bronchoconstriction. Other therapeutic uses are limited by its adverse cardiovascular effects, such as bradycardia and hypotension, which arise from its function as a cholinomimetic. Pharmacology It is highly active at all of the muscarinic receptors, but has little effect on the nicotinic receptors. Methacholine has a charged quaternary amine structure, rendering it insoluble in lipid cell membranes. Clinically, this means that it will not cros ...
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Carbachol
Carbachol, also known as carbamylcholine and sold under the brand name Miostat among others, is a cholinomimetic drug that binds and activates acetylcholine receptors. Thus it is classified as a cholinergic agonist. It is primarily used for various ophthalmic purposes, such as for treating glaucoma, or for use during ophthalmic surgery. It is generally administered as an ophthalmic solution (i.e., eye drops). Carbachol produces effects comparable to those of sarin if a massive overdose is administered (as may occur following industrial and shipping accidents) and therefore it is classified as an extremely hazardous substance in the United States as defined in Section 302 of the U.S. Emergency Planning and Community Right-to-Know Act (42 U.S.C. 11002), and is subject to strict reporting requirements by facilities which produce, store, or use it in significant quantities. It is on the World Health Organization's List of Essential Medicines. Chemistry and pharmacology Ca ...
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Acetylcholine
Acetylcholine (ACh) is an organic compound that functions in the brain and body of many types of animals (including humans) as a neurotransmitter. Its name is derived from its chemical structure: it is an ester of acetic acid and choline. Parts in the body that use or are affected by acetylcholine are referred to as cholinergic. Acetylcholine is the neurotransmitter used at the neuromuscular junction. In other words, it is the chemical that motor neurons of the nervous system release in order to activate muscles. This property means that drugs that affect cholinergic systems can have very dangerous effects ranging from paralysis to convulsions. Acetylcholine is also a neurotransmitter in the autonomic nervous system, both as an internal transmitter for both the sympathetic nervous system, sympathetic and the parasympathetic nervous system, and as the final product released by the parasympathetic nervous system. Acetylcholine is the primary neurotransmitter of the parasympathet ...
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Acetylcholinesterase
Acetylcholinesterase (HUGO Gene Nomenclature Committee, HGNC symbol ACHE; EC 3.1.1.7; systematic name acetylcholine acetylhydrolase), also known as AChE, AChase or acetylhydrolase, is the primary cholinesterase in the body. It is an enzyme that catalysis, catalyzes the breakdown of acetylcholine and some other choline esters that function as neurotransmitters: : acetylcholine + H2O = choline + acetate It is found at mainly neuromuscular junctions and in chemical synapses of the cholinergic type, where its activity serves to terminate cholinergic neurotransmission, synaptic transmission. It belongs to the carboxylesterase family of enzymes. It is the primary target of inhibition by organophosphorus compounds such as nerve agents and pesticides. Enzyme structure and mechanism AChE is a hydrolase that hydrolyzes choline esters. It has a very high catalytic activity—each molecule of AChE degrades about 5,000 molecules of acetylcholine (ACh) per second, approaching the limit ...
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Psychosis
In psychopathology, psychosis is a condition in which a person is unable to distinguish, in their experience of life, between what is and is not real. Examples of psychotic symptoms are delusions, hallucinations, and disorganized or incoherent thoughts or speech. Psychosis is a description of a person's state or symptoms, rather than a particular mental illness, and it is not related to psychopathy (a personality construct characterized by impaired empathy and remorse, along with bold, disinhibited, and egocentric traits). Common causes of chronic (i.e. ongoing or repeating) psychosis include schizophrenia or schizoaffective disorder, bipolar disorder, and brain damage (usually as a result of alcoholism). Acute (temporary) psychosis can also be caused by severe distress, sleep deprivation, sensory deprivation, some medications, and drug use (including alcohol, cannabis, hallucinogens, and stimulants). Acute psychosis is termed primary if it results from a ...
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Dry Mouth
Xerostomia, also known as dry mouth, is a subjective complaint of dryness in the mouth, which may be associated with a change in the composition of saliva, reduced salivary flow, or have no identifiable cause. This symptom is very common and is often seen as a side effect of many types of medication. It is more common in older people (mostly because individuals in this group are more likely to take several medications) and in people who breathe through their mouths. Dehydration, radiotherapy involving the salivary glands, chemotherapy and several diseases can cause reduced salivation (hyposalivation), or a change in saliva consistency and hence a complaint of xerostomia. Sometimes there is no identifiable cause, and there may sometimes be a psychogenic reason for the complaint. Definition Xerostomia is the subjective sensation of dry mouth, which is often (but not always) associated with hypofunction of the salivary glands. The term is derived from the Greek words ξηρός (' ...
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Approved Drug
An approved drug is a Medicine, medicinal preparation that has been validated for a therapeutic use by a Regulation of therapeutic goods, ruling authority of a government. This process is usually specific by country, unless specified otherwise. Process by country United States In the United States, the Food and Drug Administration, FDA approves medication, drugs. Before a drug can be prescribed, it must undergo the FDA's approval process. While a drug can feasibly be used off-label (for non-approved indications), it still is required to be approved for a specific disease or medical condition. Drug companies seeking to sell a drug in the United States must first test it. The company then sends the Food and Drug Administration's Center for Drug Evaluation and Research (CDER) evidence from these tests to prove the drug is safe and effective for its intended use. A fee is required to make such FDA submission. For financial year 2020, this fee was: for an application requiring clini ...
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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). However, 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 ...
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Cevimeline
Cevimeline (trade name Evoxac) is a synthetic analog of the natural alkaloid muscarine with a particular agonistic effect on M1 and M3 receptors. It is used in the treatment of dry mouth and Sjögren's syndrome. Medical uses Cevimeline is used in the treatment of xerostomia (dry mouth) and Sjögren's syndrome. It increases the production of saliva. Side effects Known side effects include nausea, vomiting, diarrhea, excessive sweating, rash, headache, runny nose, cough, drowsiness, hot flashes, blurred vision, and difficulty sleeping. Contraindications include asthma and angle closure glaucoma. Mechanism of action Cevimeline is a cholinergic agonist. It has a particular effect on M1 and M3 receptors. By activating the M3 receptors of the parasympathetic nervous system, cevimeline stimulates secretion by the salivary glands, thereby alleviating dry mouth. See also * Pilocarpine — a similar parasympathomimetic medication for dry mouth (xerostomia) * Bethanechol ...
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