Revision as of 14:15, 5 December 2011 editBeetstra (talk | contribs)Edit filter managers, Administrators172,031 edits Saving copy of the {{drugbox}} taken from revid 456883970 of page Prilocaine for the Chem/Drugbox validation project (updated: 'DrugBank'). |
Latest revision as of 19:23, 20 December 2023 edit JJMC89 bot III (talk | contribs)Bots, Administrators3,656,711 editsm Moving Category:AstraZeneca brands to Category:Drugs developed by AstraZeneca per Misplaced Pages:Categories for discussion/Log/2023 December 9#Category:AstraZeneca brands |
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{{short description|Local anesthetic of the amino amide type}} |
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{{ambox | text = This page contains a copy of the infobox ({{tl|drugbox}}) taken from revid of page ] with values updated to verified values.}} |
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{{Drugbox |
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{{Drugbox |
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| verifiedrevid = 464214246 |
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| Verifiedfields = changed |
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| image = Prilocaine.svg |
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| verifiedrevid = 418550175 |
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| IUPAC_name = (''RS'')-''N''-(2-methylphenyl)-''N''<sup>2</sup>-propylalaninamide |
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| image = Prilocaine.png |
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| width = 200px |
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| width = 200px |
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| imagename = 1 : 1 mixture (racemate) |
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| chirality = ] |
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| drug_name = Prilocaine |
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<!--Clinical data--> |
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<!--Clinical data--> |
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| tradename = |
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| tradename = Citanest |
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| Drugs.com = {{drugs.com|monograph|prilocaine-hydrochloride}} |
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| Drugs.com = {{drugs.com|monograph|prilocaine-hydrochloride}} |
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| MedlinePlus = a603026 |
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| MedlinePlus = a603026 |
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| licence_EU = yes |
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| pregnancy_category = B <small>(])</small> |
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| DailyMedID = Prilocaine |
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| legal_status = |
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| licence_US = <!-- FDA may use generic or brand name (generic name preferred) --> |
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| routes_of_administration = |
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| pregnancy_AU = A |
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| pregnancy_AU_comment = |
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| pregnancy_US = B |
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| pregnancy_US_comment = |
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| pregnancy_category= |
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| dependency_liability = |
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| addiction_liability = |
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| routes_of_administration = ] |
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| class = |
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| ATCvet = |
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| ATC_prefix = N01 |
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| ATC_suffix = BB04 |
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| ATC_supplemental = |
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<!-- Legal status --> |
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| legal_AU = S4 |
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| legal_AU_comment = |
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| legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F --> |
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| legal_BR_comment = |
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| legal_CA = <!-- OTC, Rx-only, Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_CA_comment = |
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| legal_DE = <!-- Anlage I, II, III or Unscheduled --> |
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| legal_DE_comment = |
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| legal_NZ = <!-- Class A, B, C --> |
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| legal_NZ_comment = |
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| legal_UK = <!-- GSL, P, POM, CD, CD Lic, CD POM, CD No Reg POM, CD (Benz) POM, CD (Anab) POM or CD Inv POM / Class A, B, C --> |
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| legal_UK_comment = |
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| legal_US = Rx-only |
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| legal_US_comment = |
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| legal_EU = |
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| legal_EU_comment = |
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| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV --> |
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| legal_UN_comment = |
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| legal_status = <!-- For countries not listed above --> |
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<!--Pharmacokinetic data--> |
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<!-- Pharmacokinetic data --> |
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| bioavailability = |
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| bioavailability = |
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| protein_bound = 55% |
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| protein_bound = 55% |
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| metabolism = Hepatic and renal |
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| metabolism = ] and ] |
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| elimination_half-life = 10-150 minutes, longer with impaired hepatic or renal function |
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| elimination_half-life = 10-150 minutes, longer with impaired liver or kidney function |
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<!--Identifiers--> |
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<!--Identifiers--> |
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| index2_label = as HCl |
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| CASNo_Ref = {{cascite|correct|CAS}} |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 721-50-6 |
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| CAS_number = 721-50-6 |
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| ATC_prefix = N01 |
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| ATC_suffix = BB04 |
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| ATC_supplemental = |
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| PubChem = 4906 |
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| PubChem = 4906 |
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| IUPHAR_ligand = 7276 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = DB00750 |
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| DrugBank = DB00750 |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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| KEGG = D00553 |
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| KEGG = D00553 |
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| ChEBI_Ref = {{ebicite|changed|EBI}} |
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| KEGG2_Ref = {{keggcite|correct|kegg}} |
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| KEGG2 = D01243 |
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| ChEBI_Ref = {{ebicite|correct|EBI}} |
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| ChEBI = 8404 |
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| ChEBI = 8404 |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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<!--Chemical data--> |
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<!--Chemical data--> |
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| IUPAC_name = (''RS'')-''N''-(2-methylphenyl)-''N''<sup>2</sup>-propylalaninamide |
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| C=13 | H=20 | N=2 | O=1 |
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| C=13 | H=20 | N=2 | O=1 |
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| molecular_weight = 220.311 g/mol |
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| smiles = O=C(Nc1ccccc1C)C(NCCC)C |
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| smiles = O=C(Nc1ccccc1C)C(NCCC)C |
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| InChI = 1/C13H20N2O/c1-4-9-14-11(3)13(16)15-12-8-6-5-7-10(12)2/h5-8,11,14H,4,9H2,1-3H3,(H,15,16) |
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| InChIKey = MVFGUOIZUNYYSO-UHFFFAOYAP |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI = 1S/C13H20N2O/c1-4-9-14-11(3)13(16)15-12-8-6-5-7-10(12)2/h5-8,11,14H,4,9H2,1-3H3,(H,15,16) |
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| StdInChI = 1S/C13H20N2O/c1-4-9-14-11(3)13(16)15-12-8-6-5-7-10(12)2/h5-8,11,14H,4,9H2,1-3H3,(H,15,16) |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey = MVFGUOIZUNYYSO-UHFFFAOYSA-N |
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| StdInChIKey = MVFGUOIZUNYYSO-UHFFFAOYSA-N |
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| melting_point = 37 |
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| melting_high = 38 |
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}} |
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}} |
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'''Prilocaine''' ({{IPAc-en|ˈ|p|r|aɪ|l|ə|ˌ|k|eɪ|n}}{{refn|{{MerriamWebsterDictionary|access-date=2016-01-21|Prilocaine}}}}) is a ] of the ] ] type first prepared by ] and ]. In its ] form (trade name '''Citanest'''), it is often used in ]. It is also often combined with lidocaine as a topical preparation for dermal anesthesia (] or ]), for treatment of conditions like ]. As it has low cardiac toxicity, it is commonly used for ] (IVRA). |
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== Contraindications == |
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In some patients, ortho-toluidine, a metabolite of prilocaine, may cause ], which may be treated with ]. Prilocaine may also be contraindicated in people with ], ], or symptomatic ].<ref>{{Cite book|title = Practical and Professional Clinical Skills|url = https://books.google.com/books?id=_DY5PCOFH4EC&pg=PA267|publisher = Oxford University Press|date = 2011-09-15|isbn = 9780199585618 | vauthors = Patel V, Morrissey J |page = 267}}</ref> |
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== Combinations == |
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It is given as a ] ] under the trade name ''Citanest Forte''. It is used as a ] mixture with ], 50% w/w, as ]. The mixture is an oil with a melting point of {{convert|18|C|F}}. A 5% ] preparation, containing 2.5% each of lidocaine/prilocaine, is marketed by ] under the ] EMLA (an abbreviation for eutectic mixture of local anesthetics).<ref>{{cite web|url=http://www.medscape.com/viewarticle/704761_2 |title=Topical Anesthesia Use in Children: Eutectic Mixture of Local Anesthetics |publisher=Medscape.com |access-date=2014-01-07}}</ref> |
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== Compendial status == |
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* ] 31 <ref name=rblp>{{citation| last =The United States Pharmacopeial Convention| title =Revision Bulletin: Lidocaine and Prilocaine Cream–Revision to Related Compounds Test| url =http://www.usp.org/USPNF/notices/lidocaineAndPrilocaine.html| access-date =10 July 2009| url-status =dead| archive-url =https://web.archive.org/web/20100705213713/http://www.usp.org/USPNF/notices/lidocaineAndPrilocaine.html| archive-date =5 July 2010}}</ref> |
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==Synthesis== |
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] |
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The amidation between ] ('''1''') and 2-bromopropionyl bromide ('''2''') leads to 2-bromo-N-(2-methylphenyl)propanamide ('''3'''). Displacement of the remaining halide with ] ('''4''') completed the synthesis of prilocaine ('''5'''). |
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== See also == |
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* ] |
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== References == |
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{{Reflist}} |
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== External links == |
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* {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/name/prilocaine | publisher = U.S. National Library of Medicine | work = Drug Information Portal | title = Prilocaine }} |
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* {{cite web | url = https://druginfo.nlm.nih.gov/drugportal/name/prilocaine%20hydrochloride | publisher = U.S. National Library of Medicine | work = Drug Information Portal | title = Prilocaine hydrochloride }} |
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{{Local anesthetics}} |
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{{Portal bar | Medicine}} |
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] |
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] |
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] |
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] |
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] |
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{{nervous-system-drug-stub}} |