nasalcrom

同

Crolom, Intal, Gastrocrom, Nasalcrom

関

Cromolyn sodium

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/12/22 12:29:24」(JST)

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"Intal" redirects here. For the constructed language, see Intal language.

Cromoglicic acid

Systematic (IUPAC) name
5,5′-(2-hydroxypropane-1,3-diyl)bis(oxy)bis(4-oxo-4H-chromene-2-carboxylic acid)
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy cat.	B
Legal status	inhaler POM, eye OTC(UK) nasal OTC, eye, inhaler Rx(US)
Routes	topical: oral, nasal spray, inhaled, eye drops
Pharmacokinetic data
Bioavailability	1%
Half-life	1.3 hours
Identifiers
CAS number	16110-51-3 Y
ATC code	A07EB01 D11AH03 R01AC01 R03BC01 S01GX01
PubChem	CID 2882
DrugBank	DB01003
ChemSpider	2779 Y
UNII	Y0TK0FS77W Y
KEGG	D07753 Y
ChEBI	CHEBI:59773 Y
ChEMBL	CHEMBL74 N
Chemical data
Formula	C23H16O11
Mol. mass	468.367 g/mol
SMILES O=C(O)C=4Oc3cccc(OCC(O)COc2cccc1O/C(=C\C(=O)c12)C(=O)O)c3C(=O)C=4
InChI InChI=1S/C23H16O11/c24-11(9-31-14-3-1-5-16-20(14)12(25)7-18(33-16)22(27)28)10-32-15-4-2-6-17-21(15)13(26)8-19(34-17)23(29)30/h1-8,11,24H,9-10H2,(H,27,28)(H,29,30) Y Key:IMZMKUWMOSJXDT-UHFFFAOYSA-N Y
N (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 in the treatment of asthma. Cromoglicic acid requires administration four times daily, and does not provide additive benefit in combination with inhaled corticosteroids.

History

Cromolyn sodium was discovered by 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. 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. 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.

Preparations

Cromoglicic acid is available in multiple forms:

• as a nasal spray (Rynacrom(UK), Lomusol(France), Nasalcrom) to treat allergic rhinitis.

• in a nebulizer solution for aerosol administration to treat asthma.

• as an inhaler (Intal) for preventive management of asthma. 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 inhaler preparation will no longer be available to patients. In the EU it is manufactured without CFCs by Sanofi, although it must be imported from Canada for USA residents.

• as eye drops (Opticrom and Optrex Allergy (UK), Crolom) for allergic conjunctivitis

• in an oral form (Gastrocrom) to treat mastocytosis, dermatographic urticaria and ulcerative colitis. Another oral product, Intercron (sodium cromoglicate in distilled water, from Zambon France), is used for food allergies.

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." Nedocromil is another mast cell stabilizer that also works in controlling asthma. 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. 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. It is more likely that these work by inhibiting the response of sensory C fibers 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%) 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.

Cromolyn is also being tested as a drug to treat insulin-induced lipoatrophy.

References

UpToDate Contents

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• 1. 喘息の治療におけるクロモン（クロモグリク酸）の使用 the use of chromones cromoglycates in the treatment of asthma
• 2. 肥満細胞活性化障害 mast cell activation disorders
• 3. 精漿に対するアレルギー反応 allergic reactions to seminal plasma
• 4. 食品添加物に対するアレルギー反応および喘息反応を評価するための検査法およびチャレンジテスト testing and challenge procedures to evaluate allergic and asthmatic reactions to food additives
• 5. 壊疽性膿皮症：治療および予後 pyoderma gangrenosum treatment and prognosis

English Journal

• An evidence-based review of systemic treatments for itch.

• Pongcharoen P1, Fleischer AB Jr2.
• European journal of pain (London, England).Eur J Pain.2015 Sep 28. doi: 10.1002/ejp.766. [Epub ahead of print]
• BACKGROUND AND OBJECTIVE: Many treatment modalities are used for itch treatment in daily medical practices without adequate evidence of their efficacy. The purpose of this study was to provide an evidence-based review of the literature as to the clinical benefits of systemic anti-itch treatments.DAT
• PMID 26416344

• H1 -antihistamines for primary mast cell activation syndromes: a systematic review.

• Nurmatov UB1, Rhatigan E2, Simons FE3, Sheikh A1,4.
• Allergy.Allergy.2015 Sep;70(9):1052-61. doi: 10.1111/all.12672. Epub 2015 Jul 6.
• BACKGROUND: Primary mast cell activation syndromes (MCAS) are a group of disorders presenting with symptoms of mast cell mediator release.OBJECTIVES: To assess the effectiveness and safety of orally administered H1 -antihistamines in the treatment of primary MCAS compared with placebo and other phar
• PMID 26095756

• Mast cell stabilisers.

• Zhang T1, Finn DF1, Barlow JW2, Walsh JJ3.
• European journal of pharmacology.Eur J Pharmacol.2015 Jun 27. pii: S0014-2999(15)30097-2. doi: 10.1016/j.ejphar.2015.05.071. [Epub ahead of print]
• Mast cells play a critical role in type 1 hypersensitivity reactions. Indeed, mast cell mediators are implicated in many different conditions including allergic rhinitis, conjunctivitis, asthma, psoriasis, mastocytosis and the progression of many different cancers. Thus, there is intense interest in
• PMID 26130122

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