Cromoglicate
From Wikipedia, the free encyclopedia
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
- ^ 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: | ||
Short acting β2-agonists: | ||
Long acting β2-agonists (LABA): | Clenbuterol, Formoterol, Salmeterol | |
Corticosteroids: | ||
Leukotriene antagonists: | ||
Xanthines: | ||
Mast cell stabilizers: |
Cromoglicate, Nedocromil |
|
Combination products: |
Budesonide/formoterol, Fluticasone/salmeterol, Ipratropium/salbutamol |