racecadotril

Racecadotril
Systematic (IUPAC) name
	(RS)-benzyl N-[3-(acetylthio)-2-benzylpropanoyl]glycinate
Clinical data
Trade names	Hidrasec, Tiorfan
AHFS/Drugs.com	International Drug Names
Legal status	UK: Prescription-only (POM);
Routes of; administration	Oral
Pharmacokinetic data
Protein binding	90% (active thiorphan metabolite)
Metabolism	Liver-mediated
Biological half-life	3 hours
Excretion	Urine (81.4%), faeces (8%)
Identifiers
CAS Registry Number	81110-73-8
ATC code	A07XA04
PubChem	CID: 107751
ChemSpider	96913
UNII	76K53XP4TO
ChEMBL	CHEMBL2103772
Synonyms	benzyl 2-[3-(acetylthio)-2-benzylpropanamido]acetate
Chemical data
Formula	C21H23NO4S
Molecular mass	385.47662 g/mol
	SMILES CC(=O)SCC(CC1=CC=CC=C1)C(=O)NCC(=O)OCC2=CC=CC=C2 ;
	InChI InChI=1S/C21H23NO4S/c1-16(23)27-15-19(12-17-8-4-2-5-9-17)21(25)22-13-20(24)26-14-18-10-6-3-7-11-18/h2-11,19H,12-15H2,1H3,(H,22,25) ; Key:ODUOJXZPIYUATO-UHFFFAOYSA-N ;
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/16 06:45:28」(JST)

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Racecadotril, also known as acetorphan, is an antidiarrheal drug which acts as a peripherally acting enkephalinase inhibitor.^[2] Unlike other opioid medications used to treat diarrhea, which reduce intestinal motility, racecadotril has an antisecretory effect—it reduces the secretion of water and electrolytes into the intestine.^[3] It is available in France (where it was first introduced in ~1990) and other European countries (including Germany, Italy, the UK and Spain) as well as most of South America and some South East Asian countries (including China, India and Thailand), but not in the United States. It is sold under the tradenames Hidrasec or, in France, Tiorfan.^[4] In Italy it is sold under the tradename Tiorfix.^[4]

Thiorphan is the active metabolite of racecadotril, which exerts the bulk of its inhibitory actions on enkephalinase.^[5]

References

^ ^a ^b ^c ^d "SPC-DOC_PL 39418-0003.PDF" (PDF). Medicines and Healthcare Products Regulatory Agency. Bioprojet Europe Ltd. 26 December 2012. Retrieved 7 May 2014.
^ Matheson AJ, Noble S (April 2000). "Racecadotril". Drugs 59 (4): 829–35; discussion 836–7. doi:10.2165/00003495-200059040-00010. PMID 10804038.
^ Matheson, AJ; Noble, S (April 2000). "Racecadotril.". Drugs 59 (4): 829–35; discussion 836–7. doi:10.2165/00003495-200059040-00010. PMID 10804038.
^ ^a ^b Brayfield, A, ed. (13 December 2013). "Racecadotril". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 6 May 2014.
^ Spillantini MG, Geppetti P, Fanciullacci M, Michelacci S, Lecomte JM, Sicuteri F (June 1986). "In vivo 'enkephalinase' inhibition by acetorphan in human plasma and CSF". European Journal of Pharmacology 125 (1): 147–50. doi:10.1016/0014-2999(86)90094-4. PMID 3015640.

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English Journal

Racecadotril May Reduce Diarrhoea in Microvillous Inclusion Disease.

Tran LC1, Lazonby G, Ellis D, Goldthorpe J, Iglesias N, Steele J, Zamvar V, Puntis JW, Vora R.
Journal of pediatric gastroenterology and nutrition.J Pediatr Gastroenterol Nutr.2017 Jan;64(1):e25-e26. doi: 10.1097/MPG.0000000000001421.
PMID 27682357

Impact of clinically tested NEP/ACE inhibitors on tumor uptake of [(111)In-DOTA]MG11-first estimates for clinical translation.

Kaloudi A1, Nock BA2, Lymperis E3, Valkema R4, Krenning EP5, de Jong M6,7, Maina T8.
EJNMMI research.EJNMMI Res.2016 Dec;6(1):15. doi: 10.1186/s13550-015-0158-3. Epub 2016 Feb 16.
BACKGROUND: We have recently shown that treatment of mice with the neutral endopeptidase (NEP) inhibitor phosphoramidon (PA) improves the bioavailability and tumor uptake of biodegradable radiopeptides. For the truncated gastrin radiotracer [(111)In-DOTA]MG11 ([(DOTA)DGlu(10)]gastrin(10-17)), this m
PMID 26882895

A Comprehensive Comparison of the Efficacy and Tolerability of Racecadotril with Other Treatments of Acute Diarrhea in Adults.

Fischbach W1, Andresen V2, Eberlin M3, Mueck T3, Layer P2.
Frontiers in medicine.Front Med (Lausanne).2016 Oct 14;3:44. eCollection 2016.
Racecadotril is a guideline-recommended treatment to alleviate symptoms of acute diarrhea. A systematic review of randomized studies was performed comparing efficacy and safety of treatment with racecadotril to that with placebo or active treatments in adults. In five double-blind studies, racecadot
PMID 27790616

Japanese Journal

A rapid and validated HPLC method to quantify racecadotril metabolite, thiorphan, in human plasma using solid-phase extraction

XU Fan,YANG Lingli,XU Guili
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 861(1), 130-135, 2008-01-01
NAID 10024541621

Quantitative analysis of racecadotril metabolite in human plasma using a liquid chromatography/tandem mass spectrometry

XU Yu,HUANG Jinchang,LIU Fei,GAO Shu,GUO Qingxiang
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 852(1), 101-107, 2007-06-01
NAID 10025801497

Related Pictures

[SPC-1] "SPC-DOC_PL 39418-0003.PDF" (PDF). Medicines and Healthcare Products Regulatory Agency. Bioprojet Europe Ltd. 26 December 2012. Retrieved 7 May 2014.

[2] Matheson AJ, Noble S (April 2000). "Racecadotril". Drugs 59 (4): 829–35; discussion 836–7. doi:10.2165/00003495-200059040-00010. PMID 10804038.

[3] Matheson, AJ; Noble, S (April 2000). "Racecadotril.". Drugs 59 (4): 829–35; discussion 836–7. doi:10.2165/00003495-200059040-00010. PMID 10804038.

[MD-4] Brayfield, A, ed. (13 December 2013). "Racecadotril". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 6 May 2014.

[pmid3015640-5] Spillantini MG, Geppetti P, Fanciullacci M, Michelacci S, Lecomte JM, Sicuteri F (June 1986). "In vivo 'enkephalinase' inhibition by acetorphan in human plasma and CSF". European Journal of Pharmacology 125 (1): 147–50. doi:10.1016/0014-2999(86)90094-4. PMID 3015640.

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