Cromoglicate
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Cromoglicate
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| 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 | |
| ATC code | R03 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C23H16O11 |
| Mol. mass | 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 (Rynacrom®(UK), Nasalcrom®) to treat allergic rhinitis, as an inhaler (Intal®) for preventive management of 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 mechanism of action is 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 more likely that these work by inhibiting the response of sensory C fibres to the irritant capsacin, 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%) [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 chromone.
[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) | |
|---|---|
| Anticholinergics | Ipratropium, Tiotropium |
| Short acting β2-agonists | Salbutamol, Terbutaline |
| Long acting β2-agonists (LABA) | Bambuterol, Clenbuterol, Fenoterol, Formoterol, Salmeterol |
| Corticosteroids | Beclometasone, Budesonide, Ciclesonide, 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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