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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/06/28 00:40:38」(JST)

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

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.^[1]

History[edit]

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[edit]

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.^[2] The maker of Intal, King Pharmaceuticals, has discontinued manufacturing the inhaled form, cromolyn sodium inhalation aerosol, due to issues involving CFC-free propellant.^[3] As stocks are depleted, this inhaler preparation will no longer be available to patients.^[4] In the EU it is manufactured without CFCs by Sanofi-Aventis, 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,^[5] 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[edit]

"Cromolyn works because it prevents the release of mediators that would normally attract inflammatory cells and because it stabilizes the inflammatory cells."^[6] 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.^[7] 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.^[7] 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%) ^[8] 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.

References[edit]

^ Fanta CH (March 2009). "Asthma". New England Journal of Medicine 360 (10): 1002–14. doi:10.1056/NEJMra0804579. PMID 19264689. Review.
^ Schwartz HJ, Blumenthal M, Brady R, et al. (April 1996). "A comparative study of the clinical efficacy of nedocromil sodium and placebo. How does cromolyn sodium compare as an active control treatment?". Chest 109 (4): 945–52. doi:10.1378/chest.109.4.945. PMID 8635375.
^ Eric Carter (July 31, 2009). "King Pharmaceuticals: Dear Healthcare Professionals". Food and Drug Administration. King Pharmaceuticals. Retrieved May 28, 2012.
^ "Intal Inhaler discontinued - MPR". Empr.com. Retrieved 2012-05-28.
^ Horan RF, Sheffer AL, Austen KF (May 1990). "Cromolyn sodium in the management of systemic mastocytosis". J. Allergy Clin. Immunol. 85 (5): 852–5. doi:10.1016/0091-6749(90)90067-E. PMID 2110198.
^ Werner's Pathophysiology page 224
^ ^a ^b H. P. Rang et al., Pharmacology, Fifth Edition. (2003) ISBN 0-443-07145-4
^ 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. PMC 1908889. PMID 8564197.

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. 思春期および成人における間欠型喘息および軽症持続型喘息の治療 treatment of intermittent and mild persistent asthma in adolescents and adults
3. 患者情報：運動誘発性喘息（詳細） exercise induced asthma beyond the basics
4. 患者情報：思春期および成人における喘息治療（詳細） asthma treatment in adolescents and adults beyond the basics

English Journal

Resveratrol efficiently improves pulmonary function via stabilizing mast cells in a rat intestinal injury model.

Huang X1, Zhao W2, Hu D3, Han X4, Wang H5, Yang J1, Xu Y1, Li Y1, Yao W6, Chen C7.
Life sciences.Life Sci.2017 Jul 18. pii: S0024-3205(17)30347-8. doi: 10.1016/j.lfs.2017.07.018. [Epub ahead of print]
PMID 28733146

Overall and specific migration from multilayer high barrier food contact materials - kinetic study of cyclic polyester oligomers migration.

Úbeda S1, Aznar M1, Vera P1, Nerín C1, Henríquez L2, Taborda L2, Restrepo C2.
Food additives & contaminants. Part A, Chemistry, analysis, control, exposure & risk assessment.Food Addit Contam Part A Chem Anal Control Expo Risk Assess.2017 Jul 12:1-11. doi: 10.1080/19440049.2017.1346390. [Epub ahead of print]
PMID 28665763

Stress induces more serious barrier dysfunction in follicle-associated epithelium than villus epithelium involving mast cells and protease-activated receptor-2.

Zhang L1, Song J1, Bai T1, Qian W1, Hou XH2.
Scientific reports.Sci Rep.2017 Jul 10;7(1):4950. doi: 10.1038/s41598-017-05064-y.
PMID 28694438

Japanese Journal

Preserved and Unpreserved 12 Anti-allergic Ophthalmic Solutions and Ocular Surface Toxicity : In Vitro Assessment in Four Cultured Corneal and Conjunctival Epithelial Cell Lines

AYAKI MASAHIKO,IWASAWA ATSUO,YAGUCHI SHIGEO,KOIDE RYOHEI
Biocontrol science 15(4), 143-148, 2010-12-10
… Intal ≥ Rizaben ≥ Tramelas ≥ Patanol Livostin. …
NAID 10027740200

Deepening economic integration in East Asia, with special reference to ASEAN countries (特集アジアベルト地帯新興国)

Intal Jr. Ponciano S.
日立総研 4-4, 24-29, 2010-02-00
NAID 40017013345

Sodium cromoglycate (Intal^( !R))as an anti-inflammatory agent for the treatment of chronic asthma

EDWARDS AM.
Clin Exp Allergy 24, 612-623, 1994
NAID 30014615951

Related Pictures

intal spinhaler.jpg Intal Intal nasal sol’ Drugs reference index « Intal Inhaler » Product Code: IntalInhal intal 5 sodium cromoglycate intal forte Samoeun Intal fled Cambodia at 16 years of Intal Cariaso.jpg Description JC Intal.jpg

★リンクテーブル★

リンク元	「クロモグリク酸」
関連記事	「intal」

「クロモグリク酸」

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
ATC code	A07EB01 D11AH03 R01AC01 R03BC01 S01GX01
PubChem	CID 2882
DrugBank	DB01003
ChemSpider	2779
UNII	Y0TK0FS77W
KEGG	D07753
ChEBI	CHEBI:59773
ChEMBL	CHEMBL74
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) ; Key:IMZMKUWMOSJXDT-UHFFFAOYSA-N ;
(what is this?) (verify);

　　[★]

英: cromoglicate
化: クロモグリク酸ナトリウム, sodium cromoglicate, natrii cromoglicas
同: クロモリンナトリウム cromolyn sodium
商: アルギノン、アレルナート、インタール、オフタルギー、クールウェイ、クモロール、クモロールPF、クリード、クロモフェロン、クロモリーク、シオミスト、シズレミン、ステリ・ネブ　クロモリン、トーワタール、ノスラン、プレント、ミタヤク、メインター、リノジェット、ルゲオン; Crolom, Intal, Gastrocrom, Nasalcrom
関: 抗アレルギー薬、鎮咳薬。気管支拡張剤、眼科用剤

分類

抗アレルギー薬

ケミカルメディエータ遊離抑制

鎮咳薬

概念

吸入、点眼、点鼻
皮膚、呼吸器系のアレルギー抑制
作用は多岐にわたる
抗ヒスタミン作用はない
作用発現に1週間以上かかる(2-6週間)

作用機序

肥満細胞の膜を安定化し、ロイコトリエンC4、ロイコトリエンD4、ロイコトリエンE4などの遊離を抑制
その他の分かっていない作用がある

適応

喘息発作の予防

即時性喘息反応と遅延性喘息反応に有効

気管支喘息
アレルギー性鼻炎、アレルギー性結膜炎、食物アレルギーによるアトピー性皮膚炎

「intal」

　　[★]

同: Crolom, Intal, Gastrocrom, Nasalcrom
関: Cromolyn sodium

[1] Fanta CH (March 2009). "Asthma". New England Journal of Medicine 360 (10): 1002–14. doi:10.1056/NEJMra0804579. PMID 19264689. Review.

[pmid8635375-2] Schwartz HJ, Blumenthal M, Brady R, et al. (April 1996). "A comparative study of the clinical efficacy of nedocromil sodium and placebo. How does cromolyn sodium compare as an active control treatment?". Chest 109 (4): 945–52. doi:10.1378/chest.109.4.945. PMID 8635375.

[3] Eric Carter (July 31, 2009). "King Pharmaceuticals: Dear Healthcare Professionals". Food and Drug Administration. King Pharmaceuticals. Retrieved May 28, 2012.

[4] "Intal Inhaler discontinued - MPR". Empr.com. Retrieved 2012-05-28.

[pmid2110198-5] Horan RF, Sheffer AL, Austen KF (May 1990). "Cromolyn sodium in the management of systemic mastocytosis". J. Allergy Clin. Immunol. 85 (5): 852–5. doi:10.1016/0091-6749(90)90067-E. PMID 2110198.

[6] Werner's Pathophysiology page 224

[rang-7] H. P. Rang et al., Pharmacology, Fifth Edition. (2003) ISBN 0-443-07145-4

[8] 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. PMC 1908889. PMID 8564197.

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案内

Intal