Cromoglicate

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Cromoglicate chemical structure
Cromoglicate
Systematic (IUPAC) name
5-[3-(2-carboxy-4-oxo-chromen-6-yl) oxy-2-hydroxy-propoxy]- 4-oxo-chromene-2-carboxylic acid
Identifiers
CAS number 16110-51-3
ATC code R03BC01
PubChem 27686
DrugBank APRD00336
Chemical data
Formula C23H16O11 
Mol. weight 468.367 g/mol
Pharmacokinetic data
Bioavailability 1%
Metabolism  ?
Half life 1.3 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status

inhaler POM, eye OTC(UK)

Routes topical: oral, nasal spray, inhaled, eye drops

Cromoglicate (INN) (also referred to as cromolyn (USAN) or cromoglycate (former BAN)) is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate. This drug prevents the release of inflammatory chemicals such as histamine from mast cells.

[edit] Uses

It is available as a nasal spray (Rhynacrom®(UK), Nasalcrom®) to treat allergic rhinitis, as an inhaler (Intal®) to treat asthma, as eye drops (Opticrom® and Optrex Allergy® (UK), Crolom®) for allergic conjunctivitis, or in an oral form (Gastrocrom®) to treat mastocytosis, dermatographic urticaria and ulcerative colitis.

Sodium cromoglicate has also been shown to reduce symptoms of food allergies, including some cases of chronic migraines.[citation needed]

[edit] Mechanism of action

The underlying mechanisms of action are not fully understood; for while cromoglicate stabilizes mast cells, this mechanism is probably not why it works in asthma.[citation needed] 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.[citation needed]

It is known to somewhat inhibit chloride channels (37% +/- 7%) [1] 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 cromone.

[edit] References

  1. ^ 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.


Medications commonly used in asthma and COPD (primarily R03) edit
Anticholinergics:

Ipratropium, Tiotropium

Short acting β2-agonists:

Salbutamol, Terbutaline

Long acting β2-agonists (LABA): Clenbuterol, Formoterol, Salmeterol
Corticosteroids:

Beclometasone, Budesonide, Fluticasone

Leukotriene antagonists:

Montelukast, Pranlukast, Zafirlukast

Xanthines:

Aminophylline, Theobromine, Theophylline

Mast cell stabilizers:

Cromoglicate, Nedocromil

Combination products:

Budesonide/formoterol, Fluticasone/salmeterol, Ipratropium/salbutamol


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