Sodium Cromoglycate (Cromolyn Sodium)

Brogden, Rex N.; Speight, T. M.; Avery, G. S.

doi:10.2165/00003495-197407030-00002

Cited by 102 publications

(16 citation statements)

References 144 publications

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“…However, this drug is investigational and thus not available for prescription. Cromolyn sodium is another mast cell stabilizing agent that inhibits degranulation of mast cells and the release of histamine and leukotrienes 22 . It is used in the therapy of asthma, allergic rhinitis, and systemic mastocytosis (reviewed by Berman and Ross 23 ).…”

Section: Introductionmentioning

confidence: 99%

Cromolyn sodium: A potential therapy for uremic pruritus?

Rosner

2006

Hemodialysis International

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Uremic pruritus occurs in up to 50% of patients undergoing chronic hemodialysis. The pathogenesis of this disabling condition is unknown but likely involves multiple pathways involving the peripheral and central nervous system as well as local chemical and inflammatory mediators. Therapy has involved modification of the dialysis procedure, topical medications such as emollients, physical treatments such as ultraviolet light, and several oral medications such as antihistamines, activated charcoal, and gabapentin. Unfortunately, most of these therapies have not been subjected to rigorous clinical trials and clinical success has been variable. Two patients with disabling uremic pruritus refractory to multiple interventions are reported, who showed significant improvement in pruritus severity as assessed by a visual analog scale when they were treated with the mast cell stabilizer cromolyn sodium. Cessation of cromolyn resulted in return of pruritus, which improved with rechallenge with the medication. Cromolyn sodium may offer an alternative therapy for patients with refractory uremic pruritus, and should be subjected to a randomized placebo-controlled trial.

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Section: Introductionmentioning

confidence: 99%

Cromolyn sodium: A potential therapy for uremic pruritus?

Rosner

2006

Hemodialysis International

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“…Its properties have been covered in detail in several reviews (94,95). DSCG was discovered by testing by an allergic man without the support of animal models (94,96). This uncommon approach is now viewed as unacceptable.…”

Section: Inhibitors Of Mediator Releasementioning

confidence: 99%

“…DSCG is very poorly absorbed following oral dosing and is therefore administered by aerosol inhalation, four times a day (94,95). Metabolism is minimal: DSCG is excreted mostly as unchanged drug.…”

Section: Inhibitors Of Mediator Releasementioning

confidence: 99%

“…Thus, although it is considered one of the safest available antiasthmatic agents, it is not a cure-all and seems to work best as an adjunct to other therapy, allowing a reduction in the dosage of the other agents (94). Clinical studies show that DSCG offers no protection if administered following antigen challenge (94,95), but if administered prophylactically, it protects both extrinsic and intrinsic asthmatics (94,102,103). DSCG is uniquely effective against both the early and late-phase asthmatic responses; it also protects against exercise-induced asthma (45,104,105).…”

Section: Inhibitors Of Mediator Releasementioning

confidence: 99%

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Antiasthmatic Agents

Bernstein¹

2000

Kirk-Othmer Encyclopedia of Chemical Technology

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Asthma is an extremely complex condition characterized by variable and reversible airways obstruction combined with nonspecific bronchial hypersensitivity. Asthma affects 3–5% of the population and is one of the most common chronic illnesses. Clinically, there are several ways of classifying asthma, and treatment varies depending upon the classification. In extrinsic asthma, also called allergic asthma, experienced by adults and, most commonly, by children, it is possible to demonstrate specific causal agents, usually antigens, eg, animal danders, foods, drugs, house dust, pollens, or mold spores. Intrinsic asthma, also called idiopathic asthma, usually develops in adulthood; allergic factors are not demonstrable in intrinsic asthma. Episodes may be triggered by a variety of stimuli, eg, emotional state, exposure to cold air, or inert dusts. Both intrinsic and extrinsic asthmatics can be prone to exercise‐induced attacks. Individuals who experience a combination of extrinsic and intrinsic asthmatic reactions have mixed asthma. Current asthma treatments are not curative and historically have relied on pharmacologic intervention with bronchodilators. More recently the focal points of both treatment and research efforts have shifted from bronchodilators to agents which reduce the underlying inflammatory state. Management of extrinsic asthma usually includes manipulation of the patient's environment to minimize or completely eliminate the causal agent. Improvements in asthma treatment include the development of more effective, safer formulations of known drugs. Also, the use of reliable sustained release formulations has revolutionized the use of oral xanthines which have a very narrow therapeutic index. For many individuals, asthma symptoms tend to worsen at night and the inhaled bronchodilators do not usually last through an entire night's sleep. β 2 ‐Agonists are widely used in the symptomatic treatment of asthma. Although both oral and aerosol formulations of these bronchodilators have been available for many years, advances have occurred in delivery technology with the development of dry powder aerosols. Nonselective β‐agonists can produce many undesirable side effects. Some selectivity in action was needed. Isoproterenol is a selective agonist at the β receptor. Aerosol administration of isoproterenol produces a prompt (2–5 min) intense bronchodilatation of relatively short (1‐h) duration, and has been widely used for many years. A significant advance in β‐agonist therapy occurred with the discovery of metaproterenol, C 11 H 17 NO 3 , which has a longer (4‐h) duration of action. Terbutaline, C 12 H 19 NO 3 , is an orally active agent having a duration of action of from 6–7 h. Terbutaline has about six times the selectivity of isoproterenol and is claimed to produce fewer side effects. Albuterol, C 13 H 21 NO 3 , also called salbutamol, is the most widely prescribed β 2 ‐agonist for either aerosol or oral administration both in the United States and worldwide. There are several longer acting agents currently under clinical evaluation, eg, bitolterol, C 28 H 31 NO 5 ; clenbuterol, C 12 H 18 Cl 2 N 2 O; and salmeterol, C 25 H 37 NO 4 . For many years oral xanthines were the preferred first‐line treatment for asthma in the United States. Within this class of compounds theophylene, ie, 1,3‐dimethylxanthine, is one member of a class of naturally occurring alkaloids. Common side effects of theophylline therapy for asthma include headache, dyspepsia, and nausea. More serious side effects can occur if blood levels are too high. Many derivatives of theophylline have been prepared. However, the most universal solution has resulted from the development of reliable sustained‐release formulations. The effectiveness of theophylline in the treatment of asthma seems to result from a combination of biological properties not clearly understood. Its predominant mode of action appears to be bronchodilation. Although the benefit of theophylline treatment is without question, its use is decreasing. Steroids use for the preventative treatment of asthma appears to be increasing, because of the identification of asthma as an inflammatory disease. It is known that steroids bind to cytosolic receptors. The steroid–receptor complex then enters the cell nucleus where the complex acts at specific sites and affects protein synthesis. The effect is to reduce the inflammatory response. While disodium chromoglycate (DSCG), C 23 H 14 Na 2 O 11 , enjoys modest success as a preventative antiasthmatic agent, it has never achieved the same level of popularity in the United States as in other markets, eg, the United Kingdom. Although it is considered one of the safest available antiasthmatic agents, it seems to work best as an adjunct to other therapy. The beneficial effect of atropine, used for centuries, is in preventing exercise‐induced asthma; it and other anticholinergic agents have no effect on bronchial hyperresponsiveness, the release of other mediators, or on the inflammatory process. Ipratropium bromide, C 20 H 30 BrNO 3 , a newer anticholinergic agent, seems to be useful in patient populations that show limited response to β 2 ‐adrenergic agonists.

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“…Chromone scaffold has been recognized as a pharmacophore of a number of bioactive molecules. Disodium cromoglycate, the sodium salt of cromoglycic acid, is a clinically useful antiallergic agent, particularly for bronchial asthma, and reported to inhibit the release of mediators such as histamine, several kinins, and so on, of immediate hypersensitivity reactions , which contain a chromone ring. Heterocyclic analogues of ritonavir, HIV‐1 protease inhibitor are amide derivatives of chromone‐2‐carboxylic acid .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Amide and Ester Derivatives of Naphthopyrone Carboxylic Acid

Soni

Soman

2013

Journal of Heterocyclic Chem

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in Wiley Online Library (wileyonlinelibrary.com).The synthesis of various amide and ester derivatives of naphthopyrone-2-carboxylic acid has been carried out by reaction of 1-naphthol with dimethyl acetylenedicarboxylate, which gave a mixture of E and Z isomers of naphthoxy diester. The diester on hydrolysis with KOH gave corresponding diacid, which was a mixture of E and Z isomers. The E and Z isomers were difficult to separate, which were subjected to cyclization in sulfuric acid to get cyclized naphthopyrone carboxylic acid. This acid is converted into titled compounds.

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Sodium Cromoglycate (Cromolyn Sodium)

Cited by 102 publications

References 144 publications

Cromolyn sodium: A potential therapy for uremic pruritus?

Cromolyn sodium: A potential therapy for uremic pruritus?

Antiasthmatic Agents

Synthesis of Amide and Ester Derivatives of Naphthopyrone Carboxylic Acid

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