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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2019/06/17 07:21:40」(JST)

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Mesalazine, also known as mesalamine or 5-aminosalicylic acid (5-ASA), is a medication used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease.^[1] It is generally used for mildly to moderately severe disease.^[1] It is taken by mouth or rectally.^[1] The formulations which are taken by mouth appear to be similarly effective.^[2]

Common side effects include headache, nausea, abdominal pain, and fever.^[1] Serious side effects may include pericarditis, liver problems, and kidney problems.^[1]^[2] Use in pregnancy and breastfeeding appears safe.^[2] In people with a sulfa allergy certain formulations may result in problems.^[1] Mesalazine is an aminosalicylate and anti-inflammatory.^[1]^[2] It works by direct contact with the intestines.^[1]

Mesalazine was approved for medical use in the United States in 1987.^[1] It is available as a generic medication and sold under many brand names worldwide.^[3]^[1] A month supply in the United Kingdom costs the NHS about 43 £ as of 2019.^[2] In the United States the wholesale cost of this amount is about 288 USD.^[4] In 2016 it was the 240th most prescribed medication in the United States with more than 2 million prescriptions.^[5]

Medical uses

It is used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease.^[1] It is generally used for mildly to moderately severe disease.^[1] It is taken by mouth or rectally.^[1] The formulations which are taken by mouth appear to be similarly effective.^[2]

Side effects

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.^[6]

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.^[7]^[6]

Chemistry

Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.^[8] It is also the active component of the prodrug balsalazide along with the inert carrier molecule 4-aminobenzoyl-beta-alanine.^[9]

References

^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ "Mesalamine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists.
^ ^a ^b ^c ^d ^e ^f British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 39–41. ISBN 9780857113382.
^ "ANDA Approval Reports - 2017 First Generic Drug Approvals". www.fda.gov. Retrieved 8 April 2019.
^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
^ ^a ^b UK Electronic Medicines Compendium Suppository Label Last revised February 2016
^ UK Electronic Medicines Compendium UL Oral Label Last revised December 2015
^ Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark
^ Drugs & Therapy Properties 2003 Oct; Vol 19, No. 10

External links

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 [show details]
…folate metabolism. Non-enteric coated 5-aminosalicylic acid (5-ASA) and topical 5-ASAs also appear to be safe in pregnancy . The use of sulfasalazine and 5-ASAs in pregnancy and nursing is discussed in …
2. 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 [show details]
… disease severity and extent. Topical 5-aminosalicylic acid (5-ASA) medications are first-line treatment in those who are willing to use rectal therapy. 5-ASA suppositories and/or enemas given rectally …
3. 成人の軽症クローン病（低リスク）への内科的マネージメントの概要overview of the medical management of mild low risk crohn disease in adults [show details]
… higher rate of adverse events compared with placebo (RR 4.9, 95% CI 2.0-12.1). The use of 5-aminosalicylates (5-ASA) for Crohn disease is controversial, and we limit its use to patients with mild Crohn disease …
4. 非ステロイド性抗炎症剤（NSAIDs）（アスピリンを含む）：アレルギー反応および偽アレルギー反応nsaids including aspirin allergic and pseudoallergic reactions [show details]
… life-threatening anaphylaxis to an NSAID, since confirmed cases of anaphylaxis to ASA have not been reported. Patients with types 5 or 6 reactions may safely take NSAIDs that are structurally dissimilar to the …
5. 空置性大腸炎diversion colitis [show details]
… suggest the addition and/or substitution with topical 5-aminosalicylic acid (ASA) . In patients who fail to respond completely to SCFA and/or topical 5-ASA agents, we use topical corticosteroids. Topical glucocorticoids …

English Journal

Prevalence of Clostridium difficile infection among hospitalized inflammatory bowel disease patients in Greece.

Viazis N, Pontas C, Karmiris K, Dimas I, Fragaki M, Paspatis G, Drygiannakis I, Koutroubakis IE, Moschovis D, Tzouvala M, Theocharis G, Tsolias C, Thomopoulos K, Zampeli E, Axiaris G, Michopoulos S, Belesiotou E, Banasa M, Maraki S, Kouskoumpekou F, Apostolopoulos G, Stamouli V, Prifti H, Mantzaris GJ.
European journal of gastroenterology & hepatology. 2019 Jul;31(7)773-776.
Inflammatory bowel disease (IBD) is an independent risk factor for Clostridium difficile infection (CDI), which is associated significantly with disease severity. We aimed to determine the rates of CDI among hospitalized IBD patients in major tertiary referral hospitals in Greece. A retrospective an
PMID 30973416

Comparative Efficacy of Anti-TNF Therapies For The Prevention of Postoperative Recurrence of Crohn's Disease: A Systematic Review and Network Meta-Analysis of Prospective Trials.

Bakouny Z, Yared F, El Rassy E, Jabbour R, Hallit R, Khoury N, Honein K, Bou Jaoude J.
Journal of clinical gastroenterology. 2019 Jul;53(6)409-417.
There is a lack of studies on the optimal anti-tumor necrosis factor (anti-TNF) agent for postoperative prophylaxis of Crohn's disease (CD) recurrence. Therefore, we conducted a network meta-analysis (NMA) of prospective trials to compare the efficacy of anti-TNF agents in the prevention of postoper
PMID 29517709

Double Drug Delivery Using Capped Mesoporous Silica Microparticles for the Effective Treatment of Inflammatory Bowel Disease.

Teruel AH, Pérez-Esteve É, González-Álvarez I, González-Álvarez M, Costero AM, Ferri D, Gaviña P, Merino V, Martínez-Máñez R, Sancenón F.
Molecular pharmaceutics. 2019 Jun;16(6)2418-2429.
Silica mesoporous microparticles loaded with both rhodamine B fluorophore (S1) or hydrocortisone (S2), and capped with an olsalazine derivative, are prepared and fully characterized. Suspensions of S1 and S2 in water at an acidic and a neutral pH show negligible dye/drug release, yet a notable deliv
PMID 30991003

Japanese Journal

Influence of Pharmaceutical Formulation on the Mucosal Concentration of 5-Aminosalicylic Acid and <i>N</i>-Acetylmesalamine in Japanese Patients with Ulcerative Colitis

Yamamoto Yuki,Masuda Satohiro,Nakase Hiroshi,Matsuura Minoru,Maruyama Shihoko,Hisamatsu Tadakazu,Suzuki Yasuo,Matsubara Kazuo
Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 42(1), 81-86, 2019
… <p>The efficacy of 5-aminosalicylic acid (5-ASA) as the first-line therapy for ulcerative colitis (UC) is determined by the extent of drug delivery to the inflamed region. …
NAID 130007542208

白血球除去療法が奏効した潰瘍性大腸炎術後回腸嚢炎の1例

河島秀昭,樫山基矢
日本大腸肛門病学会雑誌 72(1), 38-42, 2019
… 49歳時，腹腔鏡下大腸全摘術，回腸嚢肛門管吻合術を施行．術後回腸嚢炎と結節性紅斑出現でステロイドを再開し5mg隔日投与としていた．術後16年目にステロイドを中止し，その6ヵ月後，腹痛，発熱，頻回の下痢を主訴に重症の回腸嚢炎を発症した．各種抗菌薬，5-ASA増量に反応せず，白血球除去療法を行ったところ著効し完全粘膜治癒に至った．（結語）重度の回腸嚢炎に対し …
NAID 130007535927

5-ASA製剤 (特集潰瘍性大腸炎の内科的治療 : 進め方と見極め方) -- (潰瘍性大腸炎における各薬物療法の進め方と薬剤・治療変更の見極め方)

石原俊治,川島耕作,木下芳一
消化器の臨床 = Clinics in gastroenterology 21(4), 246-251, 2018-11
NAID 40021734108

Related Pictures

Treatment Algorithms in Ulcerative Colitis - ppt download 5-ASA | Laboratorio Dominguez Michael Dale - Bluetrait Powerbass ASA3-700.5 ASA Series 5-Channel Amplifier with Remote Level Control - PWB14 IBD - irritated? Michael Dale - NetScreen IBD: What drugs in what patients? - ppt video online download Ulcerative Colitis: The Current Approach to Diagnosis and Care

★リンクテーブル★

リンク元	「メサラミン」
関連記事	「AS」「A」「ASA」

「メサラミン」

Mesalazine
Clinical data
Trade names	Asacol, Lialda, Pentasa, others
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	By mouth, 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
Elimination 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 ;
CompTox Dashboard (EPA)	DTXSID5024506 ;
ECHA InfoCard	100.001.745
Chemical and physical data
Formula	C7H7NO3
Molar mass	153.135 g/mol g·mol−1
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: mesalamine
同: 5-アミノサリチル酸, 5-aminosalicylic acid, 5-ASA
関: メサラジン

「AS」

　　[★]

「A」

　　[★]

「ASA」

　　[★] アセチルサリチル酸 acetyl salicylic acid

[AHFS2019-1] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ "Mesalamine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists.

[BNF76-2] ^ ^a ^b ^c ^d ^e ^f British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 39–41. ISBN 9780857113382.

[3] "ANDA Approval Reports - 2017 First Generic Drug Approvals". www.fda.gov. Retrieved 8 April 2019.

[NADAC2019-4] "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.

[5] "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.

[UKSuppLabel-6] UK Electronic Medicines Compendium Suppository Label Last revised February 2016

[UKOralLabel-7] UK Electronic Medicines Compendium UL Oral Label Last revised December 2015

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

[9] 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 Aminosalicylates Sulfasalazine Mesalazine Olsalazine Balsalazide
Antidiarrheal micro-organisms	Saccharomyces boulardii
Other antidiarrheals	Albumin tannate Ceratonia Crofelemer Octreotide Racecadotril
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

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5-ASA