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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/11/20 02:11:47」(JST)

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Mesalazine (INN, BAN), also known as mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an aminosalicylate anti-inflammatory drug^[2] used to treat inflammatory bowel disease, including ulcerative colitis,^[3]^[4]^[5] or inflamed anus or rectum,^[6] and to maintain remission in Crohn's disease.^[3]^[7]

It is sold in an oral form to maintain remission in Crohn's disease,^[3] and as a rectal suppository^[4]^[6] and an enema for the lower bowel conditions.^[5] It is generic and sold under many brand names worldwide,^[1] and there are many formulations.^[8]

There are no data on use in pregnant women, but the drug does cross the placenta and is excreted in breast milk. The drug should not be used in children under two, people with kidney disease, or people who are allergic to aspirin.^[4]

Side effects are primarily gastrointestinal but may also include headache; GI effects include nausea, diarrhea and abdominal pain. There have been scattered reports of various problems when the oral form is used, including:problems caused by myelosuppression (leukopenia, neutropenia, agranulocytosis, aplastic anaemia, and thrombocytopenia), as well as hair loss, peripheral neuropathy, pancreatitis, liver problems, myocarditis and pericarditis, allergic and fibrotic lung reactions, lupus erythematosus-like reactions and rash (including urticaria), drug fever, interstitial nephritis and nephrotic syndrome, usually reversible on withdrawal. Very rarely, use of mesalazine has been associated with an exacerbation of the symptoms of colitis, Stevens Johnson syndrome and erythema multiforme.^[3]^[4]

Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.^[9] It is also the active component of the prodrug balsalazide along with the inert carrier molecule 4-aminobenzoyl-beta-alanine.^[10]

References

^ ^a ^b Drugs.com International trade names for mesalazine April 20, 2016
^ "mesalazine". PharmGKB.
^ ^a ^b ^c ^d UK Electronic Medicines Compendium UL Oral Label Last revised December 2015
^ ^a ^b ^c ^d UK Electronic Medicines Compendium Suppository Label Last revised February 2016
^ ^a ^b UK Electronic Medicines Compendium UK Enema Label Last revised January 2016
^ ^a ^b FDA. US Suppository Label Last updated Nov 2015
^ Sandborn WJ, Feagan BG, Lichtenstein GR (October 2007). "Medical management of mild to moderate Crohn's disease: evidence-based treatment algorithms for induction and maintenance of remission". Alimentary Pharmacology & Therapeutics. 26 (7): 987–1003. doi:10.1111/j.1365-2036.2007.03455.x. PMID 17877506. Retrieved 2009-12-20.
^ Ye B, van Langenberg DR. Mesalazine preparations for the treatment of ulcerative colitis: Are all created equal? World J Gastrointest Pharmacol Ther. 2015 Nov 6;6(4):137-44. PMID 26558148 PMC 4635154
^ Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark
^ Drugs & Therapy Properties 2003 Oct; Vol 19, No. 10

UpToDate Contents

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1. 抗結核薬：概要 antituberculous drugs an overview
2. 小児や青年のクローン病マネージメントの概要 overview of the management of crohn disease in children and adolescents
3. 成人における軽度～中等度の潰瘍性大腸炎のマネージメント management of mild to moderate ulcerative colitis in adults
4. スルファサラジンによる関節リウマチの治療 sulfasalazine in the treatment of rheumatoid arthritis
5. 小児や青年に生じる軽度から中等度の潰瘍性大腸炎のマネージメント management of mild to moderate ulcerative colitis in children and adolescents

English Journal

Red-Brown Urine Discolouration in Two Patients Taking Mesalamine.

Smeets T1, van Hunsel F2.
Drug safety - case reports.Drug Saf Case Rep.2016 Dec;3(1):6.
A 38-year-old male and a 36-year-old female experienced red-brown urine discolouration after 2 and 3 days, respectively, during the use of mesalamine for inflammatory bowel disease. Both patients mentioned that the urine discoloured after contact with sodium hypochlorite detergent in toilet water.
PMID 27747686

Systematic review: second-generation vs. conventional corticosteroids for induction of remission in ulcerative colitis.

D'Haens G1.
Alimentary pharmacology & therapeutics.Aliment Pharmacol Ther.2016 Nov;44(10):1018-1029. doi: 10.1111/apt.13803. Epub 2016 Sep 21.
BACKGROUND: Oral corticosteroids are the mainstay treatment for induction of ulcerative colitis remission in patients failing or intolerant to aminosalicylate therapy, but the poor tolerability profile of these drugs limits their usefulness. Second-generation, gut-selective corticosteroids may offer
PMID 27650488

Impact of Low Immunoglobulin G Levels on Disease Outcomes in Patients with Inflammatory Bowel Diseases.

Horton N1, Wu X2, Philpott J2, Garber A2, Achkar JP2, Brzezinski A2, Lashner BA2, Shen B3.
Digestive diseases and sciences.Dig Dis Sci.2016 Nov;61(11):3270-3277. Epub 2016 Sep 12.
BACKGROUND: Inflammatory bowel diseases (IBDs) are considered immune-mediated disorders with dysregulated innate and adaptive immunities. Secondary immunogloblin deficiency can occur in IBD and its impact on the disease course of IBD is not clear.AIMS: We sought to determine associations between low
PMID 27619393

Japanese Journal

Inhibitory Potency of Marketed Drugs for Ulcerative Colitis and Crohn's Disease on PEPT1

Biological & pharmaceutical bulletin 40(9), 1572-1575, 2017-09
NAID 40021298527

Inhibitory Potency of Marketed Drugs for Ulcerative Colitis and Crohn's Disease on PEPT1

Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 40(9), 1572-1575, 2017
NAID 130006038760

顆粒球吸着療法が奏効した壊疽性膿皮症合併潰瘍性大腸炎の一例

Progress of Digestive Endoscopy 90(1), 130-131, 2017
NAID 130005809563

「5-アミノサリチル酸」

Mesalazine
Clinical data
Trade names	Many names worldwide, including Azacol, Lialda, Pentasa, and Apriso
AHFS/Drugs.com	Monograph
MedlinePlus	a688021
License data	US DailyMed: 47586; US FDA: Mesalazine;
Pregnancy; category	US: B (No risk in non-human studies); ;
Routes of; administration	oral, rectal
ATC code	A07EC02 (WHO);
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Bioavailability	orally: 20–30% absorbed; rectally: 10–35%
Metabolism	Rapidly & extensively metabolised intestinal mucosal wall and the liver
Biological half-life	5 hours after initial dose.; At steady state 7 hours
Identifiers
	IUPAC name 5-Amino-2-hydroxybenzoic acid;
CAS Number	89-57-6 ;
PubChem CID	4075;
IUPHAR/BPS	2700;
DrugBank	DB00244 ;
ChemSpider	3933 ;
UNII	4Q81I59GXC;
KEGG	D00377 ;
ChEBI	CHEBI:6775 ;
ChEMBL	CHEMBL704 ;
ECHA InfoCard	100.001.745
Chemical and physical data
Formula	C7H7NO3
Molar mass	153.135 g/mol
3D model (JSmol)	Interactive image;
	SMILES O=C(O)c1cc(ccc1O)N ;
	InChI InChI=1S/C7H7NO3/c8-4-1-2-6(9)5(3-4)7(10)11/h1-3,9H,8H2,(H,10,11) ; Key:KBOPZPXVLCULAV-UHFFFAOYSA-N ;
(verify)

　　[★]

英: 5-aminosalicylic acid 5-aminosalicylate
同: アミノサリチル酸 aminosalicylic acid aminosalicylate
関: メサラジン、メサラミン

「mesalamine」

　　[★]

メサラミン

関: 5-aminosalicylate、5-aminosalicylic acid、mesalazine

「aminosalicylate」

　　[★]

アミノサリチル酸

関: aminosalicylic acid

aminosalicylic acid

[generics-1] Drugs.com International trade names for mesalazine April 20, 2016

[PharmGKB-2] "mesalazine". PharmGKB.

[UKOralLabel-3] UK Electronic Medicines Compendium UL Oral Label Last revised December 2015

[UKSuppLabel-4] UK Electronic Medicines Compendium Suppository Label Last revised February 2016

[UKEnemaLabel-5] UK Electronic Medicines Compendium UK Enema Label Last revised January 2016

[USSuppLabel-6] FDA. US Suppository Label Last updated Nov 2015

[7] Sandborn WJ, Feagan BG, Lichtenstein GR (October 2007). "Medical management of mild to moderate Crohn's disease: evidence-based treatment algorithms for induction and maintenance of remission". Alimentary Pharmacology & Therapeutics. 26 (7): 987–1003. doi:10.1111/j.1365-2036.2007.03455.x. PMID 17877506. Retrieved 2009-12-20.

[8] Ye B, van Langenberg DR. Mesalazine preparations for the treatment of ulcerative colitis: Are all created equal? World J Gastrointest Pharmacol Ther. 2015 Nov 6;6(4):137-44. PMID 26558148 PMC 4635154

[9] Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark

[10] Drugs & Therapy Properties 2003 Oct; Vol 19, No. 10

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

リンク元	「5-アミノサリチル酸」「mesalamine」
関連記事	「aminosalicylate」

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5-aminosalicylate