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

WordNet

street name for lysergic acid diethylamide (同)back breaker, battery-acid, dose, dot, Elvis, loony toons, Lucy in the sky with diamonds, pane, superman, window pane, Zen
any of various water-soluble compounds having a sour taste and capable of turning litmus red and reacting with a base to form a salt
having the characteristics of an acid; "an acid reaction"

PrepTutorEJDIC

酸性の / 酸味のある,すっぱい(sour) / (言葉・態度などが)厳しい,しんらつな / 酸 / すっぱいもの / 《俗》=LSD

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/11/19 12:08:24」(JST)

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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

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.^[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, although it must be imported from Canada for USA residents.
as eye drops (Opticrom and Optrex Allergy (UK), Crolom, Cromolyn (Canada)) for allergic conjunctivitis^[5]
in an oral form (Gastrocrom) to treat mastocytosis,^[6] 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."^[7] 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.^[8] 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.^[8] 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%)^[9] 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.^[10]^[11] Cromolyn is also known to binds S100P protein and disrupts the interaction with RAGE.^[12]^[13]

References

^ 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" (PDF). Food and Drug Administration. King Pharmaceuticals. Retrieved May 28, 2012.
^ "Intal Inhaler discontinued - MPR". Empr.com. Retrieved 2012-05-28.
^ 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. 6: CD009566. doi:10.1002/14651858.CD009566.pub2. PMID 26028608.
^ 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. doi:10.1111/j.1476-5381.1995.tb16629.x. PMC 1908889 . PMID 8564197.
^ Phua, EJ; Lopez, X; Ramus, J; Goldfine, AB (December 2013). "Cromolyn sodium for insulin-induced lipoatrophy: old drug, new use". Diabetes Care. 36 (12): e204–5. doi:10.2337/dc13-1123. PMC 3836099 . PMID 24265375.
^ http://www.empr.com/a-surprising-option-for-managing-insulin-induced-lipoatrophy/article/325863/
^ Penumutchu, Srinivasa R.; Chou, Ruey-Hwang; Yu, Chin (2014-08-01). "Structural Insights into Calcium-Bound S100P and the V Domain of the RAGE Complex". PLOS ONE. 9 (8): e103947. doi:10.1371/journal.pone.0103947. ISSN 1932-6203. PMC 4118983 . PMID 25084534.
^ Penumutchu, Srinivasa R.; Chou, Ruey-Hwang; Yu, Chin (2014-10-17). "Interaction between S100P and the anti-allergy drug cromolyn". Biochemical and Biophysical Research Communications. 454 (3): 404–409. doi:10.1016/j.bbrc.2014.10.048. ISSN 1090-2104. PMID 25450399.

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English Journal

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

A randomised, controlled trial of a 4% cutaneous emulsion of sodium cromoglicate in treatment of atopic dermatitis in children.

Berth-Jones J1, Pollock I, Hearn RM, Lewis-Jones S, Goodfield M, Griffiths CE, Gulati R, McHenry P, Abdullah A, Ott J, Wright A, Walker B, Stevens MT, Edwards AM.
The Journal of dermatological treatment.J Dermatolog Treat.2015 Jun;26(3):291-6. doi: 10.3109/09546634.2014.946380. Epub 2014 Aug 7.
INTRODUCTION: Atopic dermatitis (AD) is a chronic inflammatory skin disease. Sodium cromoglicate (SCG) is a chromone with anti-inflammatory, anti-itch and anti-allergic activity. This trial is a 12-week comparison (RCT) of a 4% SCG cutaneous emulsion with its vehicle in AD.MATERIALS AND METHODS: 208
PMID 25034003

Japanese Journal

症例ミソプロストールとクロモグリク酸ナトリウムにより誘発が抑制されたエビによる食物依存性運動誘発アナフィラキシーの1例

吉田流音,船坂陽子,藤本和久 [他]
皮膚科の臨床 55(7), 883-887, 2013-07
NAID 40019744635

「cromoglycate」

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 ;
PubChem CID	2882;
IUPHAR/BPS	7608;
DrugBank	DB01003 ;
ChemSpider	2779 ;
UNII	Y0TK0FS77W;
KEGG	D07753 ;
ChEBI	CHEBI:59773 ;
ChEMBL	CHEMBL74 ;
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) ; Key:IMZMKUWMOSJXDT-UHFFFAOYSA-N ;
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　　[★]

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

「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

[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" (PDF). Food and Drug Administration. King Pharmaceuticals. Retrieved May 28, 2012.

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

[Castillo-5] 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. 6: CD009566. doi:10.1002/14651858.CD009566.pub2. PMID 26028608.

[pmid2110198-6] 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.

[7] Werner's Pathophysiology page 224

[rang-8] H. P. Rang et al., Pharmacology, Fifth Edition. (2003) ISBN 0-443-07145-4

[9] 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. doi:10.1111/j.1476-5381.1995.tb16629.x. PMC 1908889 . PMID 8564197.

[10] Phua, EJ; Lopez, X; Ramus, J; Goldfine, AB (December 2013). "Cromolyn sodium for insulin-induced lipoatrophy: old drug, new use". Diabetes Care. 36 (12): e204–5. doi:10.2337/dc13-1123. PMC 3836099 . PMID 24265375.

[11] ttp://www.empr.com/a-surprising-option-for-managing-insulin-induced-lipoatrophy/article/325863/

[12] Penumutchu, Srinivasa R.; Chou, Ruey-Hwang; Yu, Chin (2014-08-01). "Structural Insights into Calcium-Bound S100P and the V Domain of the RAGE Complex". PLOS ONE. 9 (8): e103947. doi:10.1371/journal.pone.0103947. ISSN 1932-6203. PMC 4118983 . PMID 25084534.

[13] Penumutchu, Srinivasa R.; Chou, Ruey-Hwang; Yu, Chin (2014-10-17). "Interaction between S100P and the anti-allergy drug cromolyn". Biochemical and Biophysical Research Communications. 454 (3): 404–409. doi:10.1016/j.bbrc.2014.10.048. ISSN 1090-2104. PMID 25450399.

v t e Antidiarrheals, intestinal anti-inflammatory and anti-infective agents (A07)
Rehydration	Oral rehydration therapy
Intestinal anti-infectives	Antibiotics Amphotericin B Colistin Fidaxomicin Kanamycin Natamycin Neomycin Nystatin Paromomycin Polymyxin B Rifaximin Streptomycin Vancomycin Sulfonamides Phthalylsulfathiazole Succinylsulfathiazole Sulfaguanidine Nitrofuran Nifuroxazide Nifurzide Imidazole Miconazole Arsenical Acetarsol Oxyquinoline Broxyquinoline
Intestinal adsorbents	Charcoal Bismuth Pectin Kaolin Crospovidone Attapulgite Diosmectite
Antipropulsives (opioids)	Opium tincture (laudanum) Codeine Morphine Camphorated opium tincture (paregoric) crosses BBB: Diphenoxylate (Diphenoxylate/atropine) Difenoxin does not cross BBB: Eluxadoline Loperamide
Intestinal anti-inflammatory agents	corticosteroids acting locally Prednisolone Hydrocortisone Prednisone Betamethasone Tixocortol Budesonide Beclometasone antiallergic agents, excluding corticosteroids Cromoglicic acid aminosalicylic acid and similar agents Sulfasalazine Mesalazine Olsalazine Balsalazide
Antidiarrheal micro-organisms	Saccharomyces boulardii
Other antidiarrheals	Albumin tannate Ceratonia Crofelemer Octreotide Racecadotril

v t e Other dermatological preparations (D11)
Anti-seborrheics	Antiandrogens Bicalutamide Cyproterone acetate Flutamide Spironolactone Antifungals Bifonazole Cetrimonium bromide (cetrimide) Ciclopirox olamine (ciclopirox) Climbazole Clotrimazole Ketoconazole Miconazole Piroctone olamine Selenium disulfide (selenium sulfide) Xenysalate Zinc pyrithione (pyrithione zinc) Antihistamines Calcineurin inhibitors Cyclosporin Pimecrolimus Tacrolimus Isotretinoin Keratolytics Coal tar Resorcinol Salicylic acid Sulfur Urea (urea-containing cream) Lithium salts Lithium gluconate Lithium succinate Topical corticosteroids (e.g., hydrocortisone)
Skin lightening	Hydroquinone Mequinol Monobenzone
Skin darkening	Afamelanotide Melanotan II
Anti-inflammatories	Oxaceprol Gamolenic acid Pimecrolimus Tacrolimus Alitretinoin
Alopecia treatments	5α-Reductase inhibitors Alfatradiol Dutasteride Finasteride Saw palmetto extract Antiandrogens Bicalutamide Cyproterone acetate Flutamide Spironolactone Topilutamide (fluridil) Potassium channel openers Minoxidil Others Nepidermin
Hair growth inhibitors	5α-Reductase inhibitors Dutasteride Finasteride Antiandrogens Bicalutamide Cyproterone acetate Flutamide Spironolactone Eflornithine
Others	Androgens (e.g., testosterone) Brimonidine Calcium gluconate Estrogens (e.g., estradiol) Hyaluronic acid Magnesium sulfate Pregnenolone acetate Progestogens (e.g., progesterone) Povidone-iodine Tiratricol

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cromoglicic acid