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

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/07/30 17:34:21」(JST)

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Mesalazine (INN, BAN), also known as mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammatory bowel disease, such as ulcerative colitis^[1] and mild-to-moderate Crohn's disease.^[2] Mesalazine is a bowel-specific aminosalicylate drug that acts locally in the gut and has its predominant actions there, thereby having few systemic side effects.^[3]

As a derivative of salicylic acid, mesalazine is also thought to be an antioxidant that traps free radicals, which are potentially damaging byproducts of metabolism.^[3]

Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.^[4]

Mesalazine is the active component of the prodrug balsalazide along with the inert carrier molecule 4-aminobenzoyl-beta-alanine.^[5]

Side effects

Commonly:

Diarrhea
Nausea
Cramping
Flatulence^[6]

Uncommonly:

Headache
Exacerbation of the colitis
Hypersensitivity reactions (including rash, urticaria aka hives, interstitial nephritis and lupus erythematosus-like syndrome)
Hair loss

Rarely:

Acute pancreatitis
Hepatitis
Nephrotic syndrome
Blood disorders (including agranulocytosis, aplastic anaemia, leukopenia, neutropenia, thrombocytopenia)
Fever ^[7]

Mesalazine avoids the sulfonamide side effects of sulfasalazine (which contains additional sulfapyridine), but carries additional rare risks of:

Allergic lung reactions
Allergic myocarditis
Methaemoglobinaemia

Monitoring

As a result of the small risks of kidney, liver and blood disorders, blood tests should be taken before and after starting treatment. Patients are advised to report any unexplained bleeding, bruising, purpura, sore throat, fever or malaise that occurs during treatment so that a full blood count can be urgently taken.

Formulations

Pentasa 250 MG Extended Release Capsule

Mesalazine is formulated for oral ingestion as tablets or granules, and for rectal administration as a rectal suppository, suspension or enemas.^[8] It is marketed under a variety of brand names:^{[citation needed]}

UK: Asacol, Ipocal, Pentasa, Salofalk, Mezavant XL, Octasa
Ireland: Asacolon, Pentasa, Salofalk, Mezavant XL
France: Asacol, Pentasa, Mezavant
US: Asacol, Canasa, Rowasa, Pentasa, Delzicol, Lialda, Apriso, Salofalk
Spain / España: Pentasa, Claversal, Lixacol, Mezavant, Salofalk
Canada: Asacol, Pentasa, Salofalk, Mezavant
India: Mesacol (available as tablets, suppositories, enema), VEGAZ-OD.
Mexico: Salofalk
Serbia: Salofalk
Uruguay: Mesacron, Mesalazina
Brazil: Mesalazina, Mesalazina Enema, Mesacol, Mesacol MNX, Asalit,
Australia: Mesasal, Pentasa, Salofalk, Mezavant (all source PBS)
Egypt: Pentasa, Salofalk
Belgium: Dipentum (olsalazine)

Chron-asa 5, Pentasa, Pentasa Enema, Mesaneo

Dosing depends on the preparation used; in particular, slow-release tablets may have quite different drug delivery characteristics and are not interchangeable.^{[citation needed]}

Preparations that lower stool pH (such as lactulose, a laxative) will possibly affect the binding of mesalazine in the bowel and will therefore reduce its efficacy.^{[citation needed]}

References

^ Kruis, W.; Schreiber, I.; Theuer, D.; Brandes, J. W.; Schütz, E.; Howaldt, S.; Krakamp, B.; Hämling, J.; Mönnikes, H.; Koop, I.; Stolte, M.; Pallant, D.; Ewald, U. (2001). "Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses". Gut 49 (6): 783–789. doi:10.1136/gut.49.6.783. PMC 1728533. PMID 11709512. edit
^ 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.
^ ^a ^b "mesalazine". PharmGKB.
^ Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark
^ Drugs & Therapy Properties 2003 Oct; Vol 19, No. 10
^ "Lialda Side Effects & Safety Information". Shire US. October 2007. Retrieved 2008-01-07.
^ "Desensitization after fever induced by mesalazine". December 2001. Retrieved 2001-12-24.
^ "MedlinePlus: Mesalamine". April 2014. Retrieved 2014-05-12.

Mehta, Dinesh K, ed. (March 2003). British National Formulary 45. London: Pharmaceutical Press. ISBN 0-85369-555-5.
Sweetman, Sean C, ed. (November 2004). Martindale: The complete drug reference (34th ed.). London: Pharmaceutical Press. ISBN 0-85369-550-4.

External links

Bickston, S. J.; Cominelli, F. (January 2003). "Optimal dosing of 5-aminosalicylic acid: 5 Decades of choosing between politicians". Clinical Gastroenterology and Hepatology 1 (1): 3–4. doi:10.1053/jcgh.2003.50001. PMID 15017510. edit
"Novel formulation increases efficacy of mesalamine for treating ulcerative colitis". Reuters. February 16, 2007.
"Once daily mesalazine effective in active ulcerative colitis: study". Reuters. January 30, 2009.
Pentasa Official Site
Asacol/Delzicol Official Site
Lialda Official Site
Apriso Official Site
Pentasa Full Prescribing Information Shire
Delzicol Full Prescribing Information Actavis
Lialda Full Prescribing Information Shire
Apriso Full Prescribing Information Salix Pharmaceuticals

UpToDate Contents

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1. 炎症性腸疾患治療におけるスルファサラジンおよび5-アミノサリチル酸 sulfasalazine and 5 aminosalicylates in the treatment of inflammatory bowel disease
2. クローン病術後の再発予防のための内科的治療 medical prophylaxis of postoperative crohn disease
3. 重症の潰瘍性大腸炎のマネージメント management of severe ulcerative colitis
4. 成人における軽症～中等症クローン病の内科的マネージメントの概要 overview of the medical management of mild to moderate crohn disease in adults
5. 軽症～中等症の潰瘍性大腸炎のマネージメント management of mild to moderate ulcerative colitis

English Journal

Once-daily Mesalamine Formulation for Maintenance of Remission in Ulcerative Colitis: A Randomized, Placebo-controlled Clinical Trial.

Gordon GL1, Zakko S, Murthy U, Sedghi S, Pruitt R, Barrett AC, Bortey E, Paterson C, Forbes WP, Lichtenstein GR.
Journal of clinical gastroenterology.J Clin Gastroenterol.2016 Apr;50(4):318-25. doi: 10.1097/MCG.0000000000000414.
GOALS: To evaluate the efficacy and safety of mesalamine granules 1.5 g once daily for maintenance of ulcerative colitis (UC) remission.BACKGROUND: Mesalamine is a first-line treatment for induction and maintenance of UC remission.STUDY: A phase 3, randomized, double-blind, placebo-controlled trial
PMID 26368296

Once-daily mesalamine granules for maintaining remission of ulcerative colitis: pooled analysis of efficacy, safety, and prognostic factors.

Zakko SF1, Gordon GL2, Murthy U3, Sedghi S4, Pruitt R5, Barrett AC6, Bortey E6, Paterson C6, Forbes WP6, Lichtenstein GR7.
Postgraduate medicine.Postgrad Med.2016 Mar 1:1-9. [Epub ahead of print]
OBJECTIVES: A capsule formulation of mesalamine granules (MG) was developed for once-daily dosing and better compliance. The study aim was to evaluate MG efficacy and tolerability in maintaining ulcerative colitis (UC) remission.METHODS: Pooled analysis of 2 identical phase 3, randomized, double-bli
PMID 26861051

Mesalamine-induced myopericarditis - A case report.

Bernardo S1, Fernandes SR2, Araújo-Correia L1.
Revista espanola de enfermedades digestivas : organo oficial de la Sociedad Espanola de Patologia Digestiva.Rev Esp Enferm Dig.2016 Feb 15;108. doi: 10.17235/reed.2016.4016/2015. [Epub ahead of print]
Myopericarditis has occasionally been reported as a side effect of mesalamine in patients with inflammatory bowel disease. We present a 20-year-old woman with ulcerative colitis admitted with chest pain. After thorough investigation she was diagnosed with myopericarditis potentially related to mesal
PMID 26876057

Japanese Journal

One Year of Infliximab Therapy Successfully Improved a Case of Refractory Pouchitis without the Use of Antibiotics

, , , ,
Internal Medicine 53(22), 2581-2583, 2014
… We administered metronidazole, mesalamine and ciprofloxacin; …
NAID 130004713250

潰瘍性大腸炎の寛解導入および維持におけるメサラミン1日1回経口投与と標準投与法の比較 : 系統的レビューとメタ解析

Feagan Brian G.,MacDonald John K.
Inflammatory bowel diseases : highlights from the official journal of the Crohn's & Colitis Foundation of America, Inc 4(1), 2-11, 2013-01
NAID 40019586549

An Orally Administered Redox Nanoparticle That Accumulates in the Colonic Mucosa and Reduces Colitis in Mice

Vong Long Binh,Tomita Tsutomu,Yoshitomi Toru,Matsui Hirofumi,Nagasaki Yukio
Gastroenterology 143(4), 1027-1036.e3, 2012-10
… The effects of RNPO were determined in mice with dextran sodium sulfate (DSS)-induced colitis and compared with those of low-molecular-weight drugs (4-hydroxyl-2,2,6,6-tetramethylpiperidine-1-oxyl [TEMPOL] or mesalamine).ResultsRNPO, with a diameter of 40 nm and a shell of poly(ethylene glycol), had a significantly greater level of accumulation in the colonic mucosa than low-molecular-weight TEMPOL or polystyrene latex particles. …
NAID 120004921506

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リンク元

「メサラミン」

Mesalazine
Systematic (IUPAC) name
	5-amino-2-hydroxybenzoic acid
Clinical data
Trade names	Pentasa, Delzicol, Canasa, Rowasa, Lialda, Apriso, Salofalk
AHFS/Drugs.com	monograph
MedlinePlus	a688021
Licence data	US Daily Med:link
Pregnancy cat.	B (US)
Legal status	℞-only (US)
Routes	oral, rectal
Pharmacokinetic data
Bioavailability	orally: 20-30% absorbed; rectally: 10-35%
Metabolism	Rapidly & extensively metabolised intestinal mucosal wall and the liver
Half-life	5 hours after initial dose.; At steady state 7 hours
Identifiers
CAS number	89-57-6
ATC code	A07EC02
PubChem	CID 4075
IUPHAR ligand	2700
DrugBank	DB00244
ChemSpider	3933
UNII	4Q81I59GXC
KEGG	D00377
ChEBI	CHEBI:6775
ChEMBL	CHEMBL704
Chemical data
Formula	C7H7NO3
Mol. mass	153.135 g/mol
	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 ;
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　　[★]

英: mesalamine
同: 5-アミノサリチル酸, 5-aminosalicylic acid, 5-ASA
関: メサラジン

[1] Kruis, W.; Schreiber, I.; Theuer, D.; Brandes, J. W.; Schütz, E.; Howaldt, S.; Krakamp, B.; Hämling, J.; Mönnikes, H.; Koop, I.; Stolte, M.; Pallant, D.; Ewald, U. (2001). "Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses". Gut 49 (6): 783–789. doi:10.1136/gut.49.6.783. PMC 1728533. PMID 11709512. edit

[2] 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.

[PharmGKB-3] "mesalazine". PharmGKB.

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

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

[Lialda-6] "Lialda Side Effects & Safety Information". Shire US. October 2007. Retrieved 2008-01-07.

[Desensitization_after_fever_induced_by_mesalazine-7] "Desensitization after fever induced by mesalazine". December 2001. Retrieved 2001-12-24.

[MedlinePlus:_Mesalamine-8] "MedlinePlus: Mesalamine". April 2014. Retrieved 2014-05-12.

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mesalamine