Disodium cromoglycate

Both disodium cromoglycate and nedocromil sodium have antitussive effects in humans. In this instance, their activity occurs by increasing the depolarisation of sensory nerves, which increases the threshold for an action potential and therefore inhibits the activity of these neurons. 

MT Vidgren, PA Vidgren, TP Paronen. Comparison of physical and inhalation properties of spray-dried and mechanically micronized disodium cromoglycate. Int J Pharm 35 139-144, 1987. 

Figure 4.5. Plasma histamine levels in response to NT in rats pretreated with saline or disodium cromoglycate (100 pg). NT (5 nmol/kg) or saline (0.3 ml) was given intravenously. Mean + S.E.M. of n experiments, quoted with the column.

Curry, S.H., Taylor, A.X, Evans, S., Godfrey, S. and Zeidifard, E. (1975). Disposition of disodium cromoglycate administered in three particle sizes. Br. J. Clin. Pharmacol. 2 267-270. 

T. Mori, K. Nishimura, S. Tamaki, S. Nakamura, H. Tsuda, N. Kakeya, Prodrugs for the Oral Delivery of Disodium Cromoglycate , Chem. Pharm. Bull. 1988, 36, 338-344. 

The molecular structure of arsphenamin is a typical representative of a thermotropic mesogen. With its symmetrical arrangement of the atoms the same holds for disodium cromoglycate, DNCG [20], which forms both thermotropic liquid crystals and lyotropic mesophases in the presence of water. Micronized DNCG powder applied to the mucosa of the nose or the bronchi absorbs water from the high relative humidity of the respiration tract and is first transformed into a lyotropic mesophase and then into a solution depending on the amount of water available. 

Disodium cromoglycate Lung deposition comparison between a conventional MDI and a new DPI 34... 

Two cautious, but hopeful, reviews [362,362a] concluded, from evidence then to hand that the currently available preparation of disodium cromoglycate with isoprenaline could benefit patients with allergic asthma, but both expressed the hope that results from cromoglycic acid without isoprenaline would soon clarify the position. 

Cromolyn sodium (disodium cromoglycate) and nedocromil sodium are stable but extremely insoluble salts (see structures below). When used as aerosols (by nebulizer or metered-dose inhaler), they effectively inhibit both antigen- and exercise-induced asthma, and chronic use (four times daily) slightly reduces the overall level of bronchial reactivity. However, these drugs have no effect on airway smooth muscle tone and are ineffective in reversing asthmatic bronchospasm they are only of value when taken prophylactically. 

Disodium cromoglycate (724), marketed as Intal or Cromolyn Sodium, bears some structural resemblance to khellin (457), the spasmolytic component of seeds of Ammi visnaga. Intal is one of the more successful drugs for the prevention of asthmatic attacks, though it is not effective in the treatment of an acute attack of asthma. It appears to prevent the release of histamine and other substances which mediate hypersensitivity reactions but is ineffective once these substances have been released. The chemistry and pharmacology of Intal have been reviewed (B-70MI22402). 

Hypotension induced by APNEA could be blocked by the mast cell stabilizing agents, disodium cromoglycate and lodoxamide. 

Ketotifen is a nonspecific, oral, mast cell stabilizer introduced in 1972 (1). The prominent biochemical-pharmacological activities of ketotifen are H,-receptor antagonism, phosphodiesterase inhibition, inhibition of the formation SRS-A, and inhibition of calcium flux in smooth muscle preparations all these actions are suited to prevent a development of asthmatic conditions. Promising results were obtained in early clinical trials ketotifen was equipotent with disodium cromoglycate in prevention of asthma induced by spontaneous excer-cise or by antigens. Also, ketotifen is more specific than clemastine as a H-,-receptor antagonist. However, more recent, controled trials failed to substantiate the early therapeutic optimism. The beneficial effect of ketotifen in the treatment of asthma is only small it was noted that this effect is associated with pronounced sedation (2). 

Synonyms. Cromolyn Sodium Disodium Cromoglycate. Proprietary Names. Colimune Frenal Intal Lomudal Lomu-sol Nalcrom Opticrom Rynacrom. 

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