Mast cell cromolyn sodium

Cromones are used to prevent asthma attacks. To be effective they have to betaken continuously. Their mechanism of action is poorly understood. Cromones (cromolyn sodium, nedocromil) act as mast cell-stabilizing agents,... 

Mast cell stabilizers include cromolyn sodium (Intal) and nedocromil sodium (Tilade). 

Cromolyn sodium (Nasalcrom), a mast cell stabilizer, is available as a nonprescription nasal spray for symptomatic prevention and treatment of allergic rhinitis. 

Cromolyn sodium and nedocromil sodium have beneficial effects that are believed to result from stabilization of mast cell membranes. They inhibit the response to allergen challenge as well as EIB but do not cause bronchodilation. 

Initial observations on khellin (32), a furochromone-type compound from Ammi visnaga L., showed a mast-cell stabilizing effect. This led to the synthesis of many derivatives of this lead for the potential treatment of allergy and asthma, most notably the approved preventive antiasthma drug, cromolyn sodium (33). The precise molecular mechanism of this class of drugs is not yet clearly imderstood. ... 

Cromolyn Sodium (Intal, NasalCrom, Opticrom, Others) [Antiasthmatic/Mast Cell Stabilizer] Uses "Adjunct to the Rx of... 

IgE-medlated release of mast cell contents. Inset, Intact mast cell with histamine stored In granules. An IgE antibody molecule Is depicted adjacent to the mast cell. Two IgE molecules combine with a mast cell (sensitization). The attachment of an antigen (allergen) to the sensitized mast cell Initiates release of histamine (and other substances) from the mast cell. This degranulation can be prevented by such agents as isoproterenol, theophylline, epinephrine, and cromolyn sodium. H antihistamines do not interfere with degranulation but instead prevent actions of histamine at various pharmacological receptors. 

The chromone cromolyn sodium (5-5) was at one time considered the forerunner of a novel class of antiallergic and antiasthmatic drugs that act at one of the earliest stages of the allergic reaction. Detailed experiments, acmally conducted after the dmg s clinical effectiveness had been confirmed, suggested that the compound inhibited the release of mediators of the allergic reaction from mast cells. The dmg is not very active when taken orally and is usually applied topically to the lung by insufflation as its sodium salt. Considerable efforts to uncover additional structurally related mediator release inhibitors have had only limited success. 

Mast cell stabilizers Intal (Aventis) Cromolyn sodium Solution for inhalation 20 mg/2 mL None... 

Cromolyn sodium (sodium cromoglycate) inhibits exocytosis of mast cells, thus blocking the release of histamine and leukotrienes. It is used mainly to prevent attacks (e.g. those triggered by exercise). 

Type I immune responses are inhibited by mast cell stabilizers. They play an important role, both historically and currently, in the treatment of various allergic eye diseases. Included in this group are cromolyn sodium, lodoxamide, nedocromil, and pemirolast (Table 13-6). 

Cromolyn sodium inhibits mast cell degranulation. As a result its main mode of action is to prevent mediator release and its subsequent clinical manifestations. There is no evidence of antihistamine, anti-inflammatory, or vasoconstrictive activity. Absorption is poor. 

Mast cell stabilizers include cromolyn sodium 4% (Opticrom, Crolom) and lodoxamide tromethamine 0.1% (Alomide), which are currently approved by the U.S. Food and Drug Administration for VKC but offer off-label relief for allergic conjunctivitis. Other mast cell stabilizers include pemirolast (Alamast) and nedocromil sodium 2% (Alocril), with both approved for treatment of itching in allergic conjunctivitis. Perennial allergic conjunctivitis may be treated with mast cell stabilizers year round. 

Intractable cases ofVKC may be effectively treated with a combination of systemic aspirin and topical cromolyn sodium. Aspirin inhibits cyclooxygenase and the production of prostaglandins from mast cells in VKC Aspirin used in conjunction with the mast cell stabilizers results in improvement of both clinical signs and symptoms. 

Synonyms Cromolyn sodium Disodium cromo-glycate Disodium salt of cromolyn Nasal-crom Intal Crolom Gastrocrom Chemical/Pharmaceutical/Other Class Mast cell stabilizing antiallergic agent Chemical Formula C23Hi4Na20n Chemical Structure ... 

Synonyms cromolyn sodium disodium cromoglycate Trade names Colimune Crolom Cromlom Cromoptic Fivent Gastrocrom (Celltech) Intal (Monarch) Nalcrom Nasalcrom (Pfizer) Opticrom (Allergan) Rynacrom Indications Allergic rhinitis, asthma, mastocytosis Category Mast cell stabilizer Half-life 80 minutes... 

Cromones. Cromolyn sodium was first available for use as a therapeutic agent in the United States in 1973. Administered as an aerosol, it is widely used for the prophylactic treatment of asthma, with the onset of activity manifesting after several weeks, and it causes few side effects. Nedocromil sodium possesses cromolyn-like activity [51] and is efficacious in the treatment of asthma when administered as an aerosol [52,53]. Despite a concerted research effort, the mechanism by which cromones exert their therapeutic activity remains enigmatic. Inhibition of mediator release from mast cells and a direct suppressive action on other inflammatory cells appear to be features of their clinical actions [54,55],... 

Cromones Cromones (cromolyn sodium and nedocromil sodium, Aventis see Figure 16.6) are a unique class of compounds that are known to cause mast cell stabilization, thereby preventing the histamine release involved in local hypersensitivity of the lungs. In addition, these agents are implicated in preventing the release of other inflammatory mediators and the sensitivity of myelinated nerves... 

Chloride channels Mast cell chloride channels Cromolyn sodium (inhibitor)... 

Cromolyn sodium and ipratropium bromide offer two additional approaches for treating allergic rhinitis. Cromolyn sodium is a mast cell stabilizer. Increased interest in this product has resulted from it becoming available without a prescription. Ipratropium bromide is an anticholinergic agent useful in pereimial allergic rhinitis. 

Even though various antileukotriene drugs have been synthesized, none has reached clinical acceptability. Inhibition of histamine release by an apparent mast cell stabilizing mechanism (in lung tissue, but probably not elsewhere) is achieved with the carboxy-chromone derivative cromolyn sodium. The mechanism is believed to involve inhibition of histamine release from pulmonary mast cells by blocking Ca2+ movement through membrane channels. 

Cromolyn sodium (inhalation 20 mg/2 mL), Intal in capsules (20 mg for inhalation only), solution (20 mg per amp for nebulizer only), and aerosol spray (delivers 800 meg), Nasalcrom (nasal solution in 40 mg/mL), and Gastrocom (100 mg capsule for oral administration) are used for prophylactic management of severe bronchial asthma. As an antiasthmatic, antiallergic, and mast cell stabilizer, cromolyn has no bronchodilating, antiinflammatory, anticholinergic, or vas-oconstricting properties. 

Cromolyn Sodium (Nasalcrom) Inhibits release of histamine from mast cells. Prophylaxis of bronchial asthma seasonal allergic conjunctivitis. Well tolerated. Local irritation, headache, unpleasant taste. 

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