Mast cell stabilizer

Category of pharmaceutical drugs

Cromolyn Nedocromil

Mast cell stabilizers are medications used to prevent or treat certain allergic disorders. They block mast cell degranulation, stabilizing the cell and thereby preventing the release of histamine and related mediators. One suspected pharmacodynamic mechanism is the blocking of IgE-regulated calcium channels. Without intracellular calcium, the histamine vesicles cannot fuse to the cell membrane and degranulate.[1]

As inhalers they are used to treat asthma, as nasal sprays to treat hay fever (allergic rhinitis) and as eye drops for allergic conjunctivitis.[2] Finally, in oral form, they are used to treat the rare condition of mastocytosis.[3][4]

## Examples

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Mast cell stabilizer medications include:

* cromoglicic acid (cromolyn/cromoglycate)[5][1][6][4]
* ketotifen[1][6][7][8]
* lodoxamide[4][9]
* nedocromil[9]
* pemirolast[4]
* olopatadine[4]

## Research

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The following substances are studied on their potential mast cell stabilizing effects, but the current results are inconclusive:

* vitamin D[10]
* quercetin[11]

## References

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1. ^ a b c Finn DF, Walsh JJ (September 2013). "Twenty-first century mast cell stabilizers". Br J Pharmacol. 170 (1): 23–37\. doi:10.1111/bph.12138. PMC 3764846. PMID 23441583.
2. ^ Castillo M, Scott NW, Mustafa MZ, Mustafa MS, Azuara-Blanco A (2015). "Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis". Cochrane Database Syst Rev. 2015 (6): CD009566. doi:10.1002/14651858.CD009566.pub2. hdl:2164/6048. PMC 10616535. PMID 26028608.
3. ^ Castells M, Butterfield J (April 2019). "Mast Cell Activation Syndrome and Mastocytosis: Initial Treatment Options and Long-Term Management". J Allergy Clin Immunol Pract. 7 (4): 1097–1106\. doi:10.1016/j.jaip.2019.02.002. PMID 30961835.
4. ^ a b c d e Chadwick SJ (15 May 2009). "Principles of Allergy Management". Managing the Allergic Patient. pp. 19–72\. doi:10.1016/B978-141603677-7.50006-6. ISBN 978-1-4160-3677-7. "Sodium cromoglycate (cromolyn sodium) has now been available in an intranasal format OTC for almost 10 years[...] Nedocromil is much more potent [...] Other ophthalmic mast cell stabilizers include cromolyn sodium, ketotifen, and pemirolast, and topical antihistamines such as olopatadine also demonstrate mast-cell stabilizing effects. Cromolyn sodium is also used as an oral preparation for the treatment of mastocytosis and has been used off-label in the management of food allergy"
5. ^ "Mast cell stabilizers". drugs.com. Retrieved 2 April 2023.
6. ^ a b Zhang L, Song J, Hou X (April 2016). "Mast Cells and Irritable Bowel Syndrome: From the Bench to the Bedside". J Neurogastroenterol Motil. 22 (2): 181–92\. doi:10.5056/jnm15137. PMC 4819856. PMID 26755686.
7. ^ Nwaru BI, Dhami S, Sheikh A (2017). "Idiopathic Anaphylaxis". Curr Treat Options Allergy. 4 (3): 312–319\. doi:10.1007/s40521-017-0136-2. PMC 5569651. PMID 28890861.
8. ^ El-Alali EA, Abukhiran IM, Alhmoud TZ (July 2021). "Successful use of montelukast in eosinophilic gastroenteritis: a case report and a literature review". BMC Gastroenterol. 21 (1): 279. doi:10.1186/s12876-021-01854-x. PMC 8265096. PMID 34238222.
9. ^ a b Feuille EJ, Phipatanakul W, Permaul P (2022). "Conventional medications for the treatment of allergic rhinitis and conjunctivitis". Allergic and Immunologic Diseases. pp. 1077–1109\. doi:10.1016/B978-0-323-95061-9.00038-2. ISBN 978-0-323-95061-9. "Evidence is insufficient to compare the efficacy of available ocular mast cell stabilizers (cromolyn, lodoxamide, nedocromil)"
10. ^ Lui ZQ, Lii XX, Qui ZQ, Yu Y, Li MG (2017). "Vitamin D contributes to mast cell stabilization". Allergy. 72 (8): 1184–1192\. doi:10.1111/all.13110. PMID 27998003. S2CID 4643742.
11. ^ Weng Z, Zhang B, Asadi S, Sismanopoulos N, Butcher A, Fu X, et al. (28 March 2012). "Quercetin Is More Effective than Cromolyn in Blocking Human Mast Cell Cytokine Release and Inhibits Contact Dermatitis and Photosensitivity in Humans". PLOS ONE. 7 (3): e33805. Bibcode:2012PLoSO...733805W. doi:10.1371/journal.pone.0033805. PMC 3314669. PMID 22470478.

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Drugs for obstructive airway diseases: asthma/COPD (R03)

Adrenergics, inhalants|

| Short-acting β2 agonists|

* Bitolterol
* Carbuterol
* Fenoterol
* Isoetarine
* Pirbuterol
* Procaterol
* Reproterol
* Rimiterol
* Salbutamol (albuterol)#/Levosalbutamol (levalbuterol)
* Terbutaline
* Tulobuterol

|

Long-acting β2 agonists|

* Bambuterol
* Clenbuterol
* Formoterol/Arformoterol
* Salmeterol

Ultra-long-acting β2 agonists|

* Abediterol
* Carmoterol
* Indacaterol
* Olodaterol
* Vilanterol

Other|

* Clorprenaline
* Ephedrine (+theophylline, +theophylline/phenobarbital, theophylline/hydroxyzine)
* Epinephrine#
* Etafedrine
* Hexoprenaline
* Isoprenaline (isoproterenol)
* Methylephedrine
* Orciprenaline (metaproterenol)
* Racephedrine
* Tretoquinol

Glucocorticoids|

* Beclometasone#
* Betamethasone#
* Budesonide
* Ciclesonide
* Flunisolide
* Fluticasone propionate
* Mometasone
* Triamcinolone

Anticholinergics/
muscarinic antagonist|

* Aclidinium bromide
* Glycopyrronium bromide
* Ipratropium bromide#
* Oxitropium bromide
* Tiotropium bromide
* Umeclidinium bromide

Mast cell stabilizers|

* Cromoglicate
* Nedocromil

Xanthines|

* Acefylline
* Ambuphylline
* Aminophylline
* Bamifylline
* Choline theophyllinate
* Doxofylline
* Enprofylline
* Etamiphylline
* Proxyphylline
* Theophylline

Eicosanoid inhibition|

| Leukotriene antagonists|

* Montelukast
* Pranlukast
* Zafirlukast

|

Arachidonate 5-lipoxygenase inhibitors|

* Zileuton

Thromboxane receptor antagonists|

* Ramatroban
* Seratrodast

Non-xanthine PDE4 inhibitors|

* Ibudilast
* Roflumilast

Others/unknown|

* Amlexanox
* Ensifentrine
* Eprozinol
* Fenspiride‡
* Omalizumab

Combination products|

* Aclidinium bromide/formoterol
* Beclometasone/formoterol
* Beclometasone/formoterol/glycopyrronium bromide
* Budesonide/formoterol
* Budesonide/glycopyrronium bromide/formoterol
* Fluticasone furoate/umeclidinium bromide/vilanterol
* Fluticasone furoate/vilanterol
* Fluticasone propionate/salmeterol
* Glycopyrronium bromide/formoterol
* Indacaterol/glycopyrronium bromide
* Indacaterol/glycopyrronium bromide/mometasone
* Indacaterol/mometasone
* Ipratropium bromide/salbutamol
* Mometasone/formoterol
* Salbutamol (albuterol)/budesonide
* Theophylline/ephedrine
* Theophylline/ephedrine/hydroxyzine
* Theophylline/ephedrine/phenobarbital
* Umeclidinium bromide/vilanterol

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

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Decongestants and other nasal preparations (R01)

Topical|

| Sympathomimetics, plain|

* Amidephrine
* Cyclopentamine
* Ephedrine
* Epinephrine
* Fenoxazoline
* Iproheptine
* Levmetamfetamine
* Methylephedrine
* Metizoline
* Naphazoline
* Oxymetazoline
* Phenylephrine
* Propylhexedrine
* Tetryzoline
* Tramazoline
* Tuaminoheptane
* Tymazoline
* Xylometazoline

|

Antiallergic agents,
excluding corticosteroids|

* Spaglumic acid

* histamine antagonists (Levocabastine
* Antazoline
* Thonzylamine)

* mast cell stabilizer (some are also antihistamines) (Cromoglicic acid
* Nedocromil
* Azelastine
* Olopatadine
* Lodoxamide)

Corticosteroids|

* Beclometasone dipropionate
* Betamethasone#
* Budesonide
* Ciclesonide
* Dexamethasone
* Flunisolide
* Fluticasone (Fluticasone furoate, Fluticasone propionate)
* Mometasone furoate
* Prednisolone#
* Tixocortol
* Triamcinolone
* Triamcinolone acetonide

Other nasal preparations|

* Cafaminol
* Calcium hexamine thiocyanate
* Eucalyptus oil
* Framycetin
* Hexamidine
* Hyaluronan
* Ipratropium bromide
* Mupirocin
* Retinol
* Ritiometan
* Saline water

Combination products|

* Olopatadine/mometasone

Systemic use:
Sympathomimetics|

* Ephedrine
* Phenylephrine
* Phenylpropanolamine
* Pseudoephedrine (+azatadine, +carbinoxamine, +cetirizine, +dexbrompheniramine, +fexofenadine, +loratadine, +naproxen)

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

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