cromolyn sodium

クロモグリク酸。クロモグリク酸ナトリウム

WordNet

1. a silvery soft waxy metallic element of the alkali metal group; occurs abundantly in natural compounds (especially in salt water); burns with a yellow flame and reacts violently in water; occurs in sea water and in the mineral halite (rock salt) (同)Na, atomic number 11

PrepTutorEJDIC

1. ソジウム,ナトリウム(金属元素;化学記号はNa)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/07/25 14:20:06」(JST)

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Cromoglicic acid

Clinical data
AHFS/Drugs.com	International Drug Names
License data	US FDA: Cromolyn
Pregnancy category	AU: B1 US: B (No risk in non-human studies)
Routes of administration	topical: oral, nasal spray, inhaled, eye drops
ATC code	A07EB01 (WHO) D11AH03 (WHO) R01AC01 (WHO) R03BC01 (WHO) S01GX01 (WHO)
Legal status
Legal status	AU: S2 (Pharmacy only) UK: inhaler POM; eye OTC US: OTC nasal; eye, inhaler: Rx only
Pharmacokinetic data
Bioavailability	1%
Biological half-life	1.3 hours
Identifiers
IUPAC name 5,5′-(2-hydroxypropane-1,3-diyl)bis(oxy)bis(4-oxo-4H-chromene-2-carboxylic acid)
CAS Number	16110-51-3 Y
PubChem CID	2882
IUPHAR/BPS	7608
DrugBank	DB01003 N
ChemSpider	2779 Y
UNII	Y0TK0FS77W
KEGG	D07753 Y
ChEBI	CHEBI:59773 Y
ChEMBL	CHEMBL74 N
ECHA InfoCard	100.036.602
Chemical and physical data
Formula	C23H16O11
Molar mass	468.367 g/mol
3D model (JSmol)	Interactive image
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
NY (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(US) ) 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, Cromolyn (Canada)) 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. MCT mast cells found in the mucosa are stabilised." 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. Cromolyn is also known to binds S100P protein and disrupts the interaction with RAGE.

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. 嚢胞性線維症：肺疾患治療の概要 cystic fibrosis overview of the treatment of lung disease
• 3. 12歳未満の小児における慢性喘息：持続性喘息の治療およびコントロール薬 asthma in children younger than 12 years treatment of persistent asthma with controller medications
• 4. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis
• 5. 妊娠中のアレルギー疾患の認識およびマネージメント recognition and management of allergic disease during pregnancy

English Journal

• Novel spectroscopic methods for determination of Cromolyn sodium and Oxymetazoline hydrochloride in binary mixture.

• Abdel-Aziz O1, El-Kosasy AM1, Magdy N1, El Zahar NM2.
• Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.Spectrochim Acta A Mol Biomol Spectrosc.2014 Apr 24;131C:59-66. doi: 10.1016/j.saa.2014.04.047. [Epub ahead of print]
• New accurate, sensitive and selective spectrophotometric and spectrofluorimetric methods were developed and subsequently validated for determination of Cromolyn sodium (CS) and Oxymetazoline HCl (OXY) in binary mixture. These methods include 'H-point standard addition method (HPSAM) and area under t
• PMID 24820323

• Cromolyn ameliorates acute and chronic injury in a rat lung transplant model.

• Chang JC1, Leung J2, Tang T3, Holzknecht ZE2, Hartwig MG2, Duane Davis R2, Parker W2, Abraham SN4, Lin SS5.
• The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation.J Heart Lung Transplant.2014 Mar 27. pii: S1053-2498(14)01069-9. doi: 10.1016/j.healun.2014.03.004. [Epub ahead of print]
• BACKGROUND: Mast cells have been associated with obliterative bronchiolitis (OB) in human pulmonary allografts, although their role in the development of OB remains unknown.METHODS: In this study, we evaluated the role of mast cells in pulmonary allograft rejection using an orthotopic rat pulmonary
• PMID 24768366

• Inhibitory effect of putranjivain A on allergic inflammation through suppression of mast cell activation.

• Kim HH1, Park SB1, Lee S1, Kwon TK2, Shin TY3, Park PH4, Lee SH4, Kim SH5.
• Toxicology and applied pharmacology.Toxicol Appl Pharmacol.2014 Feb 1;274(3):455-61. doi: 10.1016/j.taap.2013.12.006. Epub 2013 Dec 19.
• A great number of people are suffering from allergic inflammatory disease such as asthma, atopic dermatitis, and sinusitis. Therefore discovery of drugs for the treatment of these diseases is an important subject in human health. Putranjivain A (PJA), member of ellagitannin, is known to possess bene
• PMID 24361550

Japanese Journal

• The discovery of cromolyn sodium and its effect on research and practice in allergy and immunology

• EDWARD AM.
• J Allergy Clin Immunol 115, 885-888, 2005
• NAID 30016522541

• Double-masked, randomized, parallel-group study comparing olopatadine 0.1% ophthalmic solution with cromolyn sodium 2% and levocabastine 0.05% opthalmic preparations in children with seasonal allergic conjunctivitis

• CIPRANDI G
• Curr Ther Res 65, 186-199, 2004
• NAID 30003496645

Related Pictures

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★リンクテーブル★

リンク元	「クロモグリク酸」「cromoglycate」「cromoglicic acid」「cromoglycic acid」「cromoglicate lisetil hydrochloride」
関連記事	「cromolyn」

「クロモグリク酸」

　　[★]

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

「cromoglycate」

　　[★]

クロモグリク酸、クロモグリケート

関

cromoglicate lisetil hydrochloride、cromoglicic acid、cromoglycic acid、cromolyn、cromolyn sodium、disodium cromoglycate、sodium cromoglicate

「cromoglicic acid」

　　[★]

クロモグリク酸

関

cromoglicate lisetil hydrochloride、cromoglycate、cromoglycic acid、cromolyn、cromolyn sodium、disodium cromoglycate、sodium cromoglicate

「cromoglycic acid」

　　[★]

クロモグリク酸

関

cromoglicate lisetil hydrochloride、cromoglicic acid、cromoglycate、cromolyn、cromolyn sodium、disodium cromoglycate、sodium cromoglicate

「cromoglicate lisetil hydrochloride」

　　[★]

• 塩酸クロモグリカートリセチル

関

cromoglicic acid、cromoglycate、cromoglycic acid、cromolyn sodium、disodium cromoglycate、sodium cromoglicate

「cromolyn」

　　[★]

クロモリン

関

cromoglicic acid、cromoglycate、cromoglycic acid、cromolyn sodium、disodium cromoglycate、sodium cromoglicate