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Cromoglicic acid
Systematic (IUPAC) name
5,5′-(2-hydroxypropane-1,3-diyl)bis(oxy)bis(4-oxo-4H-chromene-2-carboxylic acid)
Identifiers
CAS number 16110-51-3
ATC code A07EB01 D11AH03 R01AC01 R03BC01 S01GX01
PubChem 2882
DrugBank APRD00336
ChemSpider 2779
Chemical data
Formula C23H16O11 
Mol. mass 468.367 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 1%
Half life 1.3 hours
Therapeutic considerations
Pregnancy cat. B
Legal status inhaler POM, eye OTC(UK)
Routes topical: oral, nasal spray, inhaled, eye drops
 Yes check.svgY(what is this?)  (verify)

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.

Because of their convenience (and perceived safety), leukotriene receptor antagonists have largely replaced it as the non-corticosteroid treatment of choice. Cromoglicic acid requires administration four times daily, and does not provide additive benefit in combination with inhaled corticosteroids.[1]

Contents

History

Cromolyn sodium was discovered by Dr. Roger Altounyan who was himself a lifelong asthma sufferer. 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 exercise induced asthma, not as a treatment for acute attacks. Dr. Altounyan was investigating certain plants and herbs which have bronchodilating properties. One such plant was Khella (Ammi visnaga) which had been used as a muscle relaxant since ancient times in Egypt. Dr. Altounyan deliberately inhaled derivatives of the active ingredient khellin to determine if they could block his asthma attacks. After several years of trial he isolated an effective and safe asthma-preventing compound called cromolyn sodium.

The maker of Intal, King Pharmaceuticals, has discontinued manufacturing the inhaled form, cromolyn sodium inhalation aerosol, due to issues involving CFC-free propellant. As stocks are depleted, this medicine will no longer be available to patients.[2]

Despite the inhaler form of cromolyn sodium disappearing from the market, asthmatic patients should remember that the nebulizer solution of cromolyn sodium is still commercially available.

Uses

It is available in multiple forms:

Mechanism of action

"Cromolyn works because it prevents the release of mediators that would normally attract inflammatory cells and because it stabilizes the inflammatory cells."[5] The underlying mechanism of action is not fully understood; for while cromoglicate stabilizes mast cells, this mechanism is probably not why it works in asthma.[6] Pharmaceutical companies have produced 20 related compounds that are equally or more potent at stabilising mast cells and none of them have shown any anti-asthmatic effect.[6] It is more likely that these work by inhibiting the response of sensory C fibres to the irritant capsaicin, inhibiting local axon reflexes involved in asthma, and may inhibit the release of preformed T cell cytokines and mediators involved in asthma. (see review by Garland, 1991)

It is known to somewhat inhibit chloride channels (37% +/- 7%) [7] and thus may inhibit the:

  • exaggerated neuronal reflexes triggered by stimulation of irritant receptors on sensory nerve endings (e.g. exercise-induced asthma)
  • release of preformed cytokines from several type of inflammatory cells (T cells, eosinophils) in allergen-induced asthma

Note: Another chemical (NPPB: 5-nitro-2(3-phenyl) propylamino-benzoic acid) was shown, in the same study, to be a more effective chloride channel blocker.

Finally it may act by inhibiting calcium influx.

Cromoglicate is classified as a chromone.

References

  1. ^ Fanta CH (March 2009). "Asthma". New England Journal of Medicine 360 (10): 1002–14. doi:10.1056/NEJMra0804579. PMID 19264689.  Review.
  2. ^ http://www.empr.com/Intal-Inhaler-discontinued/article/141142/
  3. ^ Schwartz HJ, Blumenthal M, Brady R, et al. (April 1996). "A comparative study of the clinical efficacy of nedocromil sodium and placebo. How does cromolyn sodium compare as an active control treatment?". Chest 109 (4): 945–52. doi:10.1378/chest.109.4.945. PMID 8635375. http://www.chestjournal.org/cgi/pmidlookup?view=long&pmid=8635375. 
  4. ^ Horan RF, Sheffer AL, Austen KF (May 1990). "Cromolyn sodium in the management of systemic mastocytosis". J. Allergy Clin. Immunol. 85 (5): 852–5. doi:10.1016/0091-6749(90)90067-E. PMID 2110198. http://linkinghub.elsevier.com/retrieve/pii/0091-6749(90)90067-E. 
  5. ^ Werner's Pathophysiology page 224
  6. ^ a b H. P. Rang et al., Pharmacology, Fifth Edition. (2003) ISBN 0 443 07145 4
  7. ^ Heinke, S; Szucs G, Norris A, Droogmans G, Nilius B (August 1995). "Inhibition of volume-activated chloride currents in endothelial cells by chromones". Br J Pharmacol. 115(8): 1393–8. PMID 8564197. 
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