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Mast Cell Inhibitor
Mast cell stabilizers are medications used to prevent or control certain allergic disorders. They block mast cell degranulation, stabilizing the cell and thereby preventing the release of histamine and related mediators. One suspected pharmacodynamic mechanism is the blocking of IgE-regulated calcium channels. Without intracellular calcium, the histamine vesicles cannot fuse to the cell membrane and degranulate. As inhalers they are used to treat asthma, as nasal sprays to treat hay fever (allergic rhinitis) and as eye drops for allergic conjunctivitis. Finally, in oral form, they are used to treat the rare condition of mastocytosis. Examples Mast cell stabilizer medications include: * β2-adrenergic agonists * Cromoglicic acid * Ketotifen * Loratadine * Desloratadine * Methylxanthines * Olopatadine * Rupatadine *Mepolizumab * Omalizumab * Pemirolast * Quercetin * Nedocromil * Azelastine * Tranilast * Palmitoylethanolamide * Vitamin D * Bilastine Bilastine is an antihist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cromolyn
Cromoglicic acid (INN)—also referred to as cromolyn (USAN), cromoglycate (former BAN), or cromoglicate—is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate or cromolyn sodium. This drug prevents the release of inflammatory chemicals such as histamine from mast cells. Cromoglicic acid has been the non-corticosteroid treatment of choice in the treatment of asthma, for which it has largely been replaced by leukotriene receptor antagonists because of their convenience (and perceived safety). Cromoglicic acid requires administration four times daily, and does not provide additive benefit in combination with inhaled corticosteroids. History Cromolyn sodium was discovered in 1965 by Roger Altounyan, a pharmacologist who had asthma. It is considered a breakthrough drug in management of asthma, as the patients can be freed from steroids in many cases; however, it is mainly effective as a prophylaxis for allergic and e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Desloratadine
Desloratadine (trade names Clarinex and Aerius) is a tricyclic H1 inverse agonist that is used to treat allergies. It is an active metabolite of loratadine. It was patented in 1984 and came into medical use in 2001. Medical uses Desloratadine is used to treat allergic rhinitis, nasal congestion and chronic idiopathic urticaria (hives). It is the major metabolite of loratadine and the two drugs are similar in safety and effectiveness. Desloratadine is available in many dosage forms and under many trade names worldwide. An emerging indication for desloratadine is in the treatment of acne, as an inexpensive adjuvant to isotretinoin and possibly as maintenance therapy or monotherapy. Side effects The most common side-effects are fatigue (1.2%), dry mouth (3%), and headache (0.6%). Interactions Co-administration with erythromycin, ketoconazole, azithromycin, fluoxetine or cimetidine resulted in elevated blood plasma concentrations of desloratadine and its metabolite 3-h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bilastine
Bilastine is an antihistamine medication used to treat hives (urticaria) and inflammation of the eye (allergic conjunctivitis) caused by an allergy. It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H1 receptor, preventing these allergic reactions. Bilastine has an effectiveness similar to cetirizine, fexofenadine, and desloratadine. It was originally developed in Spain by FAES Farma. Bilastine is sold by several pharmaceutical companies under the brand names shown in the table. Bilastine is approved in the European Union for the symptomatic treatment of allergic conjunctivitis and urticaria. It is not approved for any use in the United States. Evidence has shown that bilastine is effective in treating skin and eye symptoms of allergic reactions, improving patient's quality of life. Bilastine meets the treatment criteria for allergic rhinitis, as published by the European Academy of Allergy and Clinical Immunology (EAACI) and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vitamin D
Vitamin D is a group of fat-soluble secosteroids responsible for increasing intestinal absorption of calcium, magnesium, and phosphate, and many other biological effects. In humans, the most important compounds in this group are vitamin D3 (cholecalciferol) and vitamin D2 (ergocalciferol). The major natural source of the vitamin is synthesis of cholecalciferol in the lower layers of epidermis of the skin through a chemical reaction that is dependent on sun exposure (specifically UVB radiation). Cholecalciferol and ergocalciferol can be ingested from the diet and supplements. Only a few foods, such as the flesh of fatty fish, naturally contain significant amounts of vitamin D. In the U.S. and other countries, cow's milk and plant-derived milk substitutes are fortified with vitamin D, as are many breakfast cereals. Mushrooms exposed to ultraviolet light contribute useful amounts of vitamin D2. Dietary recommendations typically assume that all of a person's vitamin D is taken ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Palmitoylethanolamide
Palmitoylethanolamide (PEA) is an endogenous fatty acid amide, and lipid modulator PEA has been studied in ''in vitro'' and ''in vivo'' systems using exogenously added or dosed compound; there is evidence that it binds to a nuclear receptor, through which it exerts a variety of biological effects, some related to chronic inflammation and pain. A main target of PEA is proposed to be the peroxisome proliferator-activated receptor alpha (PPAR-α). PEA also has affinity to cannabinoid-like G-coupled receptors GPR55 and GPR119. PEA cannot strictly be considered a classic endocannabinoid because it lacks affinity for the cannabinoid receptors CB1 and CB2. However, primary research supports the conclusion that the presence of PEA (or other structurally related N-acylethanolamines) enhances anandamide activity by an "entourage effect". Some primary research reports support the conclusion that PEA levels are altered and that the endocannabinoid system (ECS) is "imbalanced" in acute and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tranilast
Tranilast (INN, brand name Rizaben) is an antiallergic drug. It was developed by Kissei Pharmaceuticals and was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in the 1980s. Medical uses It is used in Japan, South Korea, and China to treat asthma, keloid scars, and hypertrophic scars, and as an ophthalmic solution for allergic pink eye. It should not be taken by women who are or might become pregnant, and it is secreted in breast milk. Interactions People who are taking warfarin should not also take tranilast, as they interact. It appears to inhibit UGT1A1 so will interfere with metabolism of drugs that are affected by that enzyme. Adverse effects When given systemically, tranilast appears to cause liver damage; in a large well-conducted clinical trial it caused elevated transaminases three times the upper limit of normal in 11 percent of patients, as well as anemia, kidney failure, rash, and pro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azelastine
Azelastine, sold under the brand name Optivar among others, is a H1 receptor-blocking medication primarily used as a nasal spray to treat allergic rhinitis (hay fever) and as eye drops for allergic conjunctivitis. Other uses may include asthma and skin rashes for which it is taken by mouth. Onset of effects is within minutes when used in the eyes and within an hour when used in the nose. Effects last for up to 12 hours. Common side effects include headache, sleepiness, change in taste, and sore throat. It is unclear if use is safe during pregnancy or breastfeeding. It is a second-generation antihistamine and works by blocking the release of a number of inflammatory mediators including histamine. Azelastine was patented in 1971 and came into medical use in 1986. It is available as a generic medication in the United States. In 2020, it was the 173rd most commonly prescribed medication in the United States, with more than 3million prescriptions. Medical uses Azelastine nasal s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quercetin
Quercetin is a plant flavonol from the flavonoid group of polyphenols. It is found in many fruits, vegetables, leaves, seeds, and grains; capers, red onions, and kale are common foods containing appreciable amounts of it. It has a bitter flavor and is used as an ingredient in dietary supplements, beverages, and foods. Occurrence Quercetin is a flavonoid widely distributed in nature. The name has been used since 1857, and is derived from ''quercetum'' (oak forest), after the oak genus ''Quercus''. It is a naturally occurring polar auxin transport inhibitor. Quercetin is one of the most abundant dietary flavonoids, with an average daily consumption of 25–50 milligrams. In red onions, higher concentrations of quercetin occur in the outermost rings and in the part closest to the root, the latter being the part of the plant with the highest concentration. One study found that organically grown tomatoes had 79% more quercetin than non-organically grown fruit. Quercetin is presen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pemirolast
Pemirolast (INN) is a mast cell stabilizer used as an anti-allergic drug therapy. It is marketed under the tradenames Alegysal and Alamast. Clinical trials studying treatments for allergic conjunctivitis have found that an ophthalmic solution containing levocabastine with pemirolast potassium may be more effective in alleviating symptoms than levocabastine alone. It has also been studied for the treatment of asthma. Pemirolast has appeared as a possible candidate for SARS-CoV-2 (COVID-19) spike protein disruption and interference. Such results were ascertained by molecular dynamics calculations executed on the Summit supercomputer. By simulating compounds with FDA or similar regulatory approval, the authors found 4 interfacial molecules that could potentially disrupt the SARS-CoV-2 interface with ACE-2 receptors, suggesting that such small molecules could mitigate SARS-CoV-2 infection. The 4 candidate interfacial molecules included pemirolast, isoniazid pyruvate, nitrofuranto ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Omalizumab
Omalizumab, sold under the brand name Xolair, is a medication used to treat asthma, nasal polyps, and urticaria (hives). Omalizumab is a recombinant DNA-derived humanized IgG1k monoclonal antibody that specifically binds to free human immunoglobulin E (IgE) in the blood and interstitial fluid and to the membrane-bound form of IgE (mIgE) on the surface of mIgE-expressing B lymphocytes. Unlike an ordinary anti-IgE antibody, it does not bind to IgE that is already bound by the high affinity IgE receptor (FcεRI) on the surface of mast cells, basophils, and antigen-presenting dendritic cells. Medical uses In the United States, omalizumab is Indication (medicine), indicated to treat moderate to severe persistent asthma, nasal polyps, and chronic idiopathic urticaria. In the European Union, omalizumab is indicated to treat allergic asthma, chronic (long-term) spontaneous urticaria (itchy rash), and severe chronic rhinosinusitis with nasal polyps. In Australia, omalizumab is indica ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mepolizumab
Mepolizumab, sold under the brand name Nucala, is a humanized monoclonal antibody used for the treatment of severe eosinophilic asthma, eosinophilic granulomatosis, and hypereosinophilic syndrome (HES). It recognizes and blocks interleukin-5 (IL-5), a signalling protein of the immune system. The most common side effects include headache, injection site reactions, and back pain. Medical uses Mepolizumab is approved by the U.S. Food and Drug Administration (FDA) for the maintenance treatment of severe asthma in patients aged six years or older and with an eosinophilic phenotype in combination with other medicines used to treat asthma. In the European Union it is approved as an add-on treatment for severe refractory eosinophilic asthma in adults. In studies, mepolizumab cut the necessity for hospitalisation due to asthma exacerbations in half, as compared to placebo. In December 2017, the FDA expanded mepolizumab's indication to treat adults with eosinophilic granulomatosis with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rupatadine
Rupatadine is a second generation antihistamine and platelet-activating factor antagonist used to treat allergies. It was discovered and developed by and is marketed as Rupafin and under several other trade names. Medical uses Rupatadine fumarate has been approved for the treatment of allergic rhinitis and chronic urticaria in adults and children over 12 years. It is available as round, light salmon coloured tablets containing 10 mg of rupatadine (as fumarate) to be administered orally, once a day. The efficacy of rupatadine as treatment for allergic rhinitis (AR) and chronic idiopathic urticaria (CIU) has been investigated in adults and adolescents (aged over 12 years) in several controlled studies, showing a rapid onset of action and a good safety profile even in prolonged treatment periods of a year. Side effects Rupatadine is a non-sedating antihistamine. However, as in other non sedating second-generation antihistamines, the most common side effects in controlled ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
