Synthesis and Biological Activities of Local Anesthetics Cite This: RSC Adv.,2019,9, 41173 Shiyang Zhou,A Gangliang Huang *B and Guangying Chen*A

Total Page:16

File Type:pdf, Size:1020Kb

Synthesis and Biological Activities of Local Anesthetics Cite This: RSC Adv.,2019,9, 41173 Shiyang Zhou,A Gangliang Huang *B and Guangying Chen*A RSC Advances View Article Online REVIEW View Journal | View Issue Synthesis and biological activities of local anesthetics Cite this: RSC Adv.,2019,9, 41173 Shiyang Zhou,a Gangliang Huang *b and Guangying Chen*a Local anesthetics are mainly used in stomatology, ophthalmology, gynecology and surgery to temporarily relieve pain. Local anesthetics act on nerve endings or around nerve trunks, and are combined with specific sodium ion (Na+) channel sites on the nerve membrane. They can affect the membrane potential by reducing Na+ passage through sodium ion channels, thus blocking the generation and conduction of Received 8th November 2019 nerve impulses, reversibly blocking the generation and conduction of sensory nerve impulses. Local Accepted 27th November 2019 anesthetics are used for convenience in local surgical operations and treatments. Herein, we mainly DOI: 10.1039/c9ra09287k review the research progress on local anesthetics and discuss the important aspects of design, synthesis rsc.li/rsc-advances and biological activity of various new compounds. – Creative Commons Attribution-NonCommercial 3.0 Unported Licence. 1. Introduction which is mainly used before surgery.8 11 In contrast, local anesthetics act on nerve endings or around nerve trunks, Anesthetics are a type of drug that act on the nervous system, reversibly blocking the generation and conduction of sensory causing it to be inhibited and resulting in the loss of the sense nerve impulses, and temporarily eliminating local sensation of pain.1–4 According to the different scopes of action of drugs, (mainly pain sensation) under the condition of consciousness. the department of anesthetics is divided into general anes- Moreover, it is convenient for local surgical operations and – thetics and local anesthetics.5–7 General anesthetics act on the treatments.12 14 Local anesthetics are mainly used in stomatol- central nervous system, causing it to be reversibly inhibited, ogy, ophthalmology, gynecology and surgery to relieve pain thereby resulting in a loss of consciousness and sensation. temporarily.15 Local anesthetics combine with specic sodium This article is licensed under a Especially pain sensation and reexes disappear and skeletal ion (Na+) channel sites on the nerve membrane, and they can muscle relaxes, thus achieving the effect of general anesthesia, affect the membrane potential by reducing Na+ passage through the sodium ion channels, thus blocking the generation and 16 Open Access Article. Published on 13 December 2019. Downloaded 9/25/2021 11:52:05 AM. a conduction of nerve impulses. Local anesthetics decrease the Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education, ff College of Chemistry and Chemical Engineering, Hainan Normal University, Haikou excitability of nerve membranes, but have no e ect on their 17–20 571158, China. E-mail: [email protected] resting potential. The application methods of local anes- bActive Carbohydrate Research Institute, Chongqing Key Laboratory of Green Synthesis thesia can be divided into topical anesthesia, invasive anes- and Application, College of Chemistry, Chongqing Normal University, Chongqing thesia, conduction anesthesia, subarachnoid anesthesia and 401331, China. E-mail: [email protected] epidural anesthesia.21–24 The rst local anesthetic used was an active ingredient from coca leaves in South America (Erythroxylum coca Lam.). The Shiyang Zhou is a Research Peruvians were known for chewing coca leaves to relieve pain as Scholar at the College of Chem- early as 1532. In 1860, Niemann extracted an alkaloid crystal istry and Chemical Engineering, from coca leaves and named it cocaine (1). Koller, an Austrian Hainan Normal University, ophthalmologist, rst formally used cocaine in clinical surgery China. He is pursuing PhD in in 1884. Also, he discovered a new local anesthesia technology, chemistry from the Hainan which led to the rapid development of local anesthetics.25–30 Normal University. He has Cocaine has a local anesthesia effect and vasoconstriction received his Master of Science effect, and it can reduce the bleeding of surgical wounds.31–34 degree in Chemical Biology from Additionally, cocaine can be used in the nose, nasopharynx, the Chongqing Normal Univer- mouth, throat and ear as surface anesthesia.35–39 However, sity, China. He has over six years cocaine is highly addictive, and easy to cause tissue irritation, of experience in Industry and allergic reactions and other toxic side effects. Also, its aqueous Academics. His research interests solution is not stable, and thus easily hydrolyzed during high- include the medicinal chemistry (drug design and synthesis, natural pressure disinfection; therefore, the clinical application of products semi-synthesis and full synthesis). This journal is © The Royal Society of Chemistry 2019 RSC Adv.,2019,9, 41173–41191 | 41173 View Article Online RSC Advances Review cocaine is greatly restricted, and it has long since been replaced on the structure of aromatic acid esters, amide, aminoketone, by other local anesthetics.40–43 Because of the shortcomings of aminoether and amino carbamate types of local anesthetics cocaine, researchers began to study and modify the structure of were developed (Table 1). In terms of drugs structure–activity cocaine to nd better local anesthetics. None of the three relationship (SAR), the chemical structure of local anesthetics products from the hydrolysis of cocaine, ecgonine (2), benzoic usually consists of three basic skeleton parts, a lipophilic acid and methanol, has the effect of local anesthesia.44 Substi- aromatic ring, intermediate connecting functional group and tution of benzoic acid with other carboxylic acids can form hydrophilic amine group. In recent years, the local anesthetics esters with ecgonine, resulting in reduced or complete loss of used in clinical practice are mainly used to reduce toxicity and anesthetic effects, proving that benzoic acid esters are an prolong the action time by changing the new dosage forms of important structure of cocaine with local anesthetic effects. The existing local anesthetics.60,61 Herein, we mainly review the alkaloid tropacocaine (3) isolated from the leaves of coca in Java research progress of local anesthetics (2009–2019), including had only the structure of benzoate ester and no carboxylate the design, synthesis and biological activity of various new methyl ester group in its molecular structure, which had the compounds. general effect of local anesthesia. Therefore, the local anes- thesia effect of benzoate ester was further conrmed.45–47 Aer determining the local anesthesia effect of benzoate 2. Synthesis and biological activities ester, the structure of the parent nucleus of cocaine (ecgonine) Local anesthesia is a compound that blocks the conduction of was modied and simplied. When the N-methyl of ecgonine nerve bers when applied locally to nerve tissue at appropriate was removed, there was no signicant effect on physiological concentrations. It blocks the voltage-sensitive sodium channels activities, but the toxicity increased.48 If the nitrogen atom was of each nerve ber, eliminating their action potential. The quaternized, the activity was lost. For ecgonine, Corning further greatest practical advantage of local anesthetics is that their simplied its structure, and designed and synthesized two effects can be reversed when they were removed from nerve a b Creative Commons Attribution-NonCommercial 3.0 Unported Licence. piperidol benzoate derivatives, -eucaine (4) and -eucaine (5). tissue. In this case, nerve function and action potential are Both of them had a local anesthetic effect similar to cocaine, but completely restored, with no evidence of damage to nerve bers their aqueous solution property was relatively stable, and their or cellular structures. Compounds with amino groups linked to toxicity was also low, which indicate that the ecgonine double heterocyclic nuclei, such as lipophilic molecules, were shown to ring structure is not necessary for the local anesthesia effect.49–53 be more active and less toxic than benzene analogues. It has Simultaneously, this further proves the importance of the been reported that 2-aminobenzothiazole, 2-aminothiazole benzoate ester part from the side. Due to the signicant derivatives and 3-aminobenzoazole-[d]-isothiazole derivatives research work on benzoate ester compounds, benzocaine (6) have local anesthetic activity. In 2009, Carla F. et al.62 reported was rst synthesized in 1890 and proven to have a local anes- the design and synthesis of different thiazole and isothiazole This article is licensed under a thesia effect. Subsequently, orthoform (7) and new orthoform derivatives for the study of local anesthesia. In the process of (8) were successfully synthesized. Both of them exhibited strong structural design of target compounds 1–32, they used the local anesthesia effects, but they were not water-soluble and thiazole structure as the parent structure of the target could not be injected.54–56 They could only be used for local Open Access Article. Published on 13 December 2019. Downloaded 9/25/2021 11:52:05 AM. compounds, and simultaneously retained the alkyl-acetamido anesthesia, while their salt was too acidic to be used. Because of or alkyl-propionamide groups that local anesthetic drugs their shortcomings, further structural transformation led to the have. In terms of structure–activity relationship (SAR), these successful development of the local anesthetic procaine (9)in target molecules were structurally
Recommended publications
  • Europæisk Patentskrift
    (19) DANMARK (1°) DK/EP 2968225 T3 (12) Oversættelse af europæisk patentskrift Patent- og Varemærkestyrelsen (51) lnt.CI.: A 61 K 31/137 (2006.01) A 61 K 9/00 (2006.01) A 61 K 31/245 (2006.01) A 61 K 31/445 (2006.01) A 61 K 31/519 (2006.01) A 61 K 31/52 (2006.01) A 61 P 43/00 (2006.01) (45) Oversættelsen bekendtgjort den: 2019-05-27 (80) Dato for Den Europæiske Patentmyndigheds bekendtgørelse om meddelelse af patentet: 2019-02-20 (86) Europæisk ansøgning nr.: 14719486.4 (86) Europæisk indleveringsdag: 2014-03-17 (87) Den europæiske ansøgnings publiceringsdag: 2016-01-20 (86) International ansøgning nr.: US2014030372 (87) Internationalt publikationsnr.: WO2014145580 (30) Prioritet: 2013-03-15 US 201361789054 P (84) Designerede stater: AL AT BE BG CH CY CZ DE DK EE ES Fl FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR (73) Patenthaver: The Children's Medical Center Corporation, 55 Shattuck Street, Boston, Massachusetts 02115, USA (72) Opfinder: BERDE, Charles, 14 Doran Road, Bookline, MA 02146, USA KOHANE, Daniel S., 119 Willard Street, Newton, MA 02461, USA (74) Fuldmægtig i Danmark: AWA Denmark A/S, Strandgade 56,1401 København K, Danmark (54) Benævnelse: NEOSAXITOXINKOMBINATIONSFORMULERINGER TIL FORLÆNGET LOKALANÆSTESI (56) Fremdragne publikationer: WO-A2-98/51290 ALBERTO J. RODRIGUEZ-NAVARRO ET AL: "Potentiation of Local Anesthetic Activity of Neosaxitoxin with Bupivacaine or Epinephrine: Development of a Long-Acting Pain Blocker", NEUROTOXICITY RESEARCH, vol. 16, no. 4, 28 July 2009 (2009-07-28), pages 408-415, XP055122925, ISSN: 1029-8428, DOI: 10.1007/s12640-009- 9092-3 cited in the application Anonymous: "NCT01786655 on 2013_02_11: ClinicalTrials.gov Archive",, 11 February 2013 (2013-02-11), XP055122935, Retrieved from the Internet: URL:http://clinicaltrials.gov/archive/NCTO 1786655/2013_02_11 [retrieved on 2014-06-12] CHARLES B.
    [Show full text]
  • Classification of Medicinal Drugs and Driving: Co-Ordination and Synthesis Report
    Project No. TREN-05-FP6TR-S07.61320-518404-DRUID DRUID Driving under the Influence of Drugs, Alcohol and Medicines Integrated Project 1.6. Sustainable Development, Global Change and Ecosystem 1.6.2: Sustainable Surface Transport 6th Framework Programme Deliverable 4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Due date of deliverable: 21.07.2011 Actual submission date: 21.07.2011 Revision date: 21.07.2011 Start date of project: 15.10.2006 Duration: 48 months Organisation name of lead contractor for this deliverable: UVA Revision 0.0 Project co-funded by the European Commission within the Sixth Framework Programme (2002-2006) Dissemination Level PU Public PP Restricted to other programme participants (including the Commission x Services) RE Restricted to a group specified by the consortium (including the Commission Services) CO Confidential, only for members of the consortium (including the Commission Services) DRUID 6th Framework Programme Deliverable D.4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Page 1 of 243 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Authors Trinidad Gómez-Talegón, Inmaculada Fierro, M. Carmen Del Río, F. Javier Álvarez (UVa, University of Valladolid, Spain) Partners - Silvia Ravera, Susana Monteiro, Han de Gier (RUGPha, University of Groningen, the Netherlands) - Gertrude Van der Linden, Sara-Ann Legrand, Kristof Pil, Alain Verstraete (UGent, Ghent University, Belgium) - Michel Mallaret, Charles Mercier-Guyon, Isabelle Mercier-Guyon (UGren, University of Grenoble, Centre Regional de Pharmacovigilance, France) - Katerina Touliou (CERT-HIT, Centre for Research and Technology Hellas, Greece) - Michael Hei βing (BASt, Bundesanstalt für Straßenwesen, Germany).
    [Show full text]
  • Pdf; Chi 2015 DPP Air in Cars.Pdf; Dodson 2014 DPP Dust CA.Pdf; Kasper-Sonnenberg 2014 Phth Metabolites.Pdf; EU Cosmetics Regs 2009.Pdf
    Bouge, Cathy (ECY) From: Nancy Uding <[email protected]> Sent: Friday, January 13, 2017 10:24 AM To: Steward, Kara (ECY) Cc: Erika Schreder Subject: Comments re. 2016 CSPA Rule Update - DPP Attachments: DPP 131-18-0 exposure.pdf; Chi 2015 DPP air in cars.pdf; Dodson 2014 DPP dust CA.pdf; Kasper-Sonnenberg 2014 phth metabolites.pdf; EU Cosmetics Regs 2009.pdf Please accept these comments from Toxic-Free Future concerning the exposure potential of DPP for consideration during the 2016 CSPA Rule update. Regards, Nancy Uding -- Nancy Uding Grants & Research Specialist Toxic-Free Future 206-632-1545 ext.123 http://toxicfreefuture.org 1 JES-00888; No of Pages 9 JOURNAL OF ENVIRONMENTAL SCIENCES XX (2016) XXX– XXX Available online at www.sciencedirect.com ScienceDirect www.elsevier.com/locate/jes Determination of 15 phthalate esters in air by gas-phase and particle-phase simultaneous sampling Chenchen Chi1, Meng Xia1, Chen Zhou1, Xueqing Wang1,2, Mili Weng1,3, Xueyou Shen1,4,⁎ 1. College of Environmental & Resource Sciences, Zhejiang University, Hangzhou 310058, China 2. Zhejiang National Radiation Environmental Technology Co., Ltd., Hangzhou 310011, China 3. School of Environmental and Resource Sciences, Zhejiang Agriculture and Forestry University, Hangzhou 310058, China 4. Zhejiang Provincial Key Laboratory of Organic Pollution Process and Control, Hangzhou 310058, China ARTICLE INFO ABSTRACT Article history: Based on previous research, the sampling and analysis methods for phthalate esters (PAEs) Received 24 December 2015 were improved by increasing the sampling flow of indoor air from 1 to 4 L/min, shortening the Revised 14 January 2016 sampling duration from 8 to 2 hr.
    [Show full text]
  • WO 2016/081643 Al 26 May 2016 (26.05.2016) W P O P C T
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2016/081643 Al 26 May 2016 (26.05.2016) W P O P C T (51) International Patent Classification: (71) Applicant (for AL, AT, BE, BG, CH, CN, CY, CZ, DE, DK, C07K 16/28 (2006.01) C12N 15/13 (2006.01) EE, ES, FI, FR, GB, GR, HR, HU, IE, IN, IS, IT, LT, LU, C07K 16/40 (2006.01) A61K 39/395 (2006.01) LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, C07K 16/46 (2006.01) A61P 25/00 (2006.01) SM, TR only): F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124, 4070 Basel (CH). (21) International Application Number: PCT/US20 15/06 1405 (72) Inventors: ZHANG, Yin; 1 DNA Way, South San Fran cisco, California 94080 (US). ZUCHERO, Joy Yu; 1 (22) International Filing Date: DNA Way, South San Francisco, California 94080 (US). 18 November 2015 (18.1 1.2015) ATWAL, Jasvinder; 1 DNA Way, South San Francisco, (25) Filing Language: English California 94080 (US). COUCH, Jessica; 1 DNA Way, South San Francisco, California 94080 (US). DENNIS, (26) Publication Language: English Mark S.; 1 DNA Way, South San Francisco, California (30) Priority Data: 94080 (US). ERNST, James A.; 1 DNA Way, South San 62/081,827 19 November 2014 (19. 11.2014) US Francisco, California 94080 (US). WATTS, Ryan J.; 1 DNA Way, South San Francisco, California 94080 (US). (71) Applicant (for all designated States except AL, AT, BE, LAZAR, Gregory A.; 1 DNA Way, South San Francisco, BG, BN, CH, CN, CY, CZ, DE, DK, EE, ES, FI, FR, GB, California 94080 (US).
    [Show full text]
  • Col.V.MISSION of the EUROPEAN COMMUNITIES
    COl.V.MISSION OF THE EUROPEAN COMMUNITIES SEC(90) 1985 final· Brussels, 29 October 1990 Proposa I for a COUNCIL DIRECTIVE on the approximation of the laws of the Member States relat.ing to cosmetic products -2- EXPLANATORY UEUORANDUM 1. In the context of a people's Europe, the Commission attaches great Importance to simplifying and clarifying Community law so as to make It clearer and more accessible to the ordinary citizen, thus giving hIm new opportunItIes and the chance to make use of the spec if i c rights It gives him. This aim cannot be achieved so long as numerous provisions that have been amended several times, often QUite substantially, remain scattered, so that they must be sought partly In the original Instrument and partly In later amending ones. Considerable research work, comparing many different Instruments, Is thus needed to Identify the current rules. For this reason a consot tdatton of rules that have freQuently been amended Is essential If Community law Is to be clear and transparent. 2. In Its resolution of 26 November 1974 concerning consolidation of Its acts (1), the Council recommended that those of Its acts which have been amended several times be assembled Into a single text. It stressed that, In the Interests of legal certainty, a genuine legislative consolidation, Involving the repeal of earlier acts, should wherever possible be effected (as Is being done In this case). it conseQuently Invited the Commission to let it have proposals for consol !dation and undertook ·to examine them "as Quickly as possible, whltout bringing Into QUestion, during that consol ldatlon, the substantive solutions contained In the consol !dated texts".
    [Show full text]
  • Prohibited Substances List
    Prohibited Substances List This is the Equine Prohibited Substances List that was voted in at the FEI General Assembly in November 2009 alongside the new Equine Anti-Doping and Controlled Medication Regulations(EADCMR). Neither the List nor the EADCM Regulations are in current usage. Both come into effect on 1 January 2010. The current list of FEI prohibited substances remains in effect until 31 December 2009 and can be found at Annex II Vet Regs (11th edition) Changes in this List : Shaded row means that either removed or allowed at certain limits only SUBSTANCE ACTIVITY Banned Substances 1 Acebutolol Beta blocker 2 Acefylline Bronchodilator 3 Acemetacin NSAID 4 Acenocoumarol Anticoagulant 5 Acetanilid Analgesic/anti-pyretic 6 Acetohexamide Pancreatic stimulant 7 Acetominophen (Paracetamol) Analgesic/anti-pyretic 8 Acetophenazine Antipsychotic 9 Acetylmorphine Narcotic 10 Adinazolam Anxiolytic 11 Adiphenine Anti-spasmodic 12 Adrafinil Stimulant 13 Adrenaline Stimulant 14 Adrenochrome Haemostatic 15 Alclofenac NSAID 16 Alcuronium Muscle relaxant 17 Aldosterone Hormone 18 Alfentanil Narcotic 19 Allopurinol Xanthine oxidase inhibitor (anti-hyperuricaemia) 20 Almotriptan 5 HT agonist (anti-migraine) 21 Alphadolone acetate Neurosteriod 22 Alphaprodine Opiod analgesic 23 Alpidem Anxiolytic 24 Alprazolam Anxiolytic 25 Alprenolol Beta blocker 26 Althesin IV anaesthetic 27 Althiazide Diuretic 28 Altrenogest (in males and gelidngs) Oestrus suppression 29 Alverine Antispasmodic 30 Amantadine Dopaminergic 31 Ambenonium Cholinesterase inhibition 32 Ambucetamide Antispasmodic 33 Amethocaine Local anaesthetic 34 Amfepramone Stimulant 35 Amfetaminil Stimulant 36 Amidephrine Vasoconstrictor 37 Amiloride Diuretic 1 Prohibited Substances List This is the Equine Prohibited Substances List that was voted in at the FEI General Assembly in November 2009 alongside the new Equine Anti-Doping and Controlled Medication Regulations(EADCMR).
    [Show full text]
  • Local Anesthetics – Substances with Multiple Application in Medicine
    ISSN 2411-958X (Print) European Journal of January-April 2016 ISSN 2411-4138 (Online) Interdisciplinary Studies Volume 2, Issue 1 Local Anesthetics – Substances with Multiple Application in Medicine Rodica SÎRBU Ovidius University of Constanta, Faculty of Pharmacy, Campus Corp B, University Alley No. 1, Constanta, Romania Emin CADAR UMF Carol Davila Bucharest, Faculty of Pharmacy, Str. Traian Vuia No. 6, Sector 2, Bucharest, Romania Cezar Laurențiu TOMESCU Ovidius University of Constanta, Faculty of Medicine, Campus Corp B, University Alley No. 1, Constanta, Romania Cristina-Luiza ERIMIA Corresponding author, [email protected] Ovidius University of Constanta, Faculty of Pharmacy, Campus Corp B, University Alley No. 1, Constanta, Romania Stelian PARIS Ovidius University of Constanta, Faculty of Pharmacy, Campus Corp B, University Alley No. 1, Constanta, Romania Aneta TOMESCU Ovidius University of Constanta, Faculty of Medicine, Campus Corp B, University Alley No. 1, Constanta, Romania Abstract Local anesthetics are substances which, by local action groups on the runners, cause loss of reversible a painful sensation, delimited corresponding to the application. They allow small surgery, short in duration and the endoscopic maneuvers. May be useful in soothe teething pain of short duration and in the locking of the nervous disorders in medical care. Local anesthesia is a process useful for the carrying out of surgery and of endoscopic maneuvers, to soothe teething pain in certain conditions, for depriving the temporary structures peripheral nervous control. Reversible locking of the transmission nociceptive, the set of the vegetative and with a local anesthetic at the level of the innervations peripheral nerve, roots and runners, a trunk nervous, around the components of a ganglion or coolant is cefalorahidian practice anesthesia loco-regional.
    [Show full text]
  • Ehealth DSI [Ehdsi V2.2.2-OR] Ehealth DSI – Master Value Set
    MTC eHealth DSI [eHDSI v2.2.2-OR] eHealth DSI – Master Value Set Catalogue Responsible : eHDSI Solution Provider PublishDate : Wed Nov 08 16:16:10 CET 2017 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 1 of 490 MTC Table of Contents epSOSActiveIngredient 4 epSOSAdministrativeGender 148 epSOSAdverseEventType 149 epSOSAllergenNoDrugs 150 epSOSBloodGroup 155 epSOSBloodPressure 156 epSOSCodeNoMedication 157 epSOSCodeProb 158 epSOSConfidentiality 159 epSOSCountry 160 epSOSDisplayLabel 167 epSOSDocumentCode 170 epSOSDoseForm 171 epSOSHealthcareProfessionalRoles 184 epSOSIllnessesandDisorders 186 epSOSLanguage 448 epSOSMedicalDevices 458 epSOSNullFavor 461 epSOSPackage 462 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 2 of 490 MTC epSOSPersonalRelationship 464 epSOSPregnancyInformation 466 epSOSProcedures 467 epSOSReactionAllergy 470 epSOSResolutionOutcome 472 epSOSRoleClass 473 epSOSRouteofAdministration 474 epSOSSections 477 epSOSSeverity 478 epSOSSocialHistory 479 epSOSStatusCode 480 epSOSSubstitutionCode 481 epSOSTelecomAddress 482 epSOSTimingEvent 483 epSOSUnits 484 epSOSUnknownInformation 487 epSOSVaccine 488 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 3 of 490 MTC epSOSActiveIngredient epSOSActiveIngredient Value Set ID 1.3.6.1.4.1.12559.11.10.1.3.1.42.24 TRANSLATIONS Code System ID Code System Version Concept Code Description (FSN) 2.16.840.1.113883.6.73 2017-01 A ALIMENTARY TRACT AND METABOLISM 2.16.840.1.113883.6.73 2017-01
    [Show full text]
  • P-Aminobenzoic Acid Derivatives Benzocaine
    P-aminobenzoic acid derivatives Benzocaine Mechanism of action oThe loca l anaesthe tics decrease the excitabilit y of nerve cells by decreasing the entry of Na+ ions during upstroke of action pottiltential. oThe local anaesthetics interact with a receptor situated within the voltage sensitiesensitive Na+ channel and raise the threshold of channel opening. oLocal anaesthetic blocks Na+ conductance by two possible modes of action, the tonic and the phasic inhibition. oTonic inhibition results from the binding of LA to nonactivated closed channel while phasic inhibition results from the binding of LA to open state or inactivate state of channels. Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Procaine MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Butamben IUPAC: Butyl 4-aminobenzoate MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Butacaine IUPAC: 3-(dibutylamino)propyl 4´-aminobenzoate MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Benox inate IUPAC: 2-(diethylamino)ethyl 4´-amino-3´-butoxybenzoate MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esophagus, larynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract. Tetracaine IUPAC: 2-(dimethylamino)ethyl 4´-(butylamino)benzoate MOA: Similar to benzocaine Uses: For general use as a lubricant and topical anesthetic on esoppghagus, laryyypynx, mouth, nasal cavity, rectum, respiratory tract or trachea and urinary tract..
    [Show full text]
  • Ophthaine (Proparacine Hydrochloride) a Local Anaesthetic for Ophthalmic Surgery* by P
    Br J Ophthalmol: first published as 10.1136/bjo.48.2.102 on 1 February 1964. Downloaded from Brit. J. Ophthal. (1964) 48, 102, OPHTHAINE (PROPARACINE HYDROCHLORIDE) A LOCAL ANAESTHETIC FOR OPHTHALMIC SURGERY* BY P. V. RYCROFT London THERE has long been a need in ophthalmology for a pleasant, non-irritant, safe and effective local analgesic, free from such side-effects as pupil dilatation or cycloplegia. The compounds in common use to-day, such as cocaine 4 per cent. (D.D.A.), affect the pupil and desiccate the cornea, and amethocaine (Pantocain, Ponto- caine, Tetracain) and related compound amylocaine (Dorsacaine, Phenolaine) and Benzamine (Eucaine) cause stinging, irritation, blepharospasm, and conjunctival congestion. Novesine (Wander), which has a formula similar to " Ophthaine", has proved excel- lent for tonometry, but not so successful for tonography or gonioscopy, and also has the disadvantage of stinging on application. copyright. Ophthaine underwent extensive trials in the United States in the years 1950-55, and for the past 3 years has been in regular clinical use by several colleagues and myself. During this period not a single case of sensitivity has occurred, and the drug has proved to be the most satisfactory all-round analgesic available. Chemistry http://bjo.bmj.com/ Ophthaine, which takes the form of an amorphous off-white solid, is used in 0 50 per cent. concentration and is freely soluble in water and dilute acids to yield a clear solution. It is not compatible with alkalis, since the insoluble free base is liberated. The drug is prepared as a sterile solution in combination with 02 per cent.
    [Show full text]
  • Drug and Medication Classification Schedule
    KENTUCKY HORSE RACING COMMISSION UNIFORM DRUG, MEDICATION, AND SUBSTANCE CLASSIFICATION SCHEDULE KHRC 8-020-1 (11/2018) Class A drugs, medications, and substances are those (1) that have the highest potential to influence performance in the equine athlete, regardless of their approval by the United States Food and Drug Administration, or (2) that lack approval by the United States Food and Drug Administration but have pharmacologic effects similar to certain Class B drugs, medications, or substances that are approved by the United States Food and Drug Administration. Acecarbromal Bolasterone Cimaterol Divalproex Fluanisone Acetophenazine Boldione Citalopram Dixyrazine Fludiazepam Adinazolam Brimondine Cllibucaine Donepezil Flunitrazepam Alcuronium Bromazepam Clobazam Dopamine Fluopromazine Alfentanil Bromfenac Clocapramine Doxacurium Fluoresone Almotriptan Bromisovalum Clomethiazole Doxapram Fluoxetine Alphaprodine Bromocriptine Clomipramine Doxazosin Flupenthixol Alpidem Bromperidol Clonazepam Doxefazepam Flupirtine Alprazolam Brotizolam Clorazepate Doxepin Flurazepam Alprenolol Bufexamac Clormecaine Droperidol Fluspirilene Althesin Bupivacaine Clostebol Duloxetine Flutoprazepam Aminorex Buprenorphine Clothiapine Eletriptan Fluvoxamine Amisulpride Buspirone Clotiazepam Enalapril Formebolone Amitriptyline Bupropion Cloxazolam Enciprazine Fosinopril Amobarbital Butabartital Clozapine Endorphins Furzabol Amoxapine Butacaine Cobratoxin Enkephalins Galantamine Amperozide Butalbital Cocaine Ephedrine Gallamine Amphetamine Butanilicaine Codeine
    [Show full text]
  • 761066Orig1s000
    CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 761066Orig1s000 CLINICAL REVIEW(S) Medical Officer’s Review of BLA 761066 Division of Dermatology and Dental Products Type: Biosimilar 351(k) Correspondence date: 25-MAY-2017 Serial Amendment: 000 CDER Stamp date: 25-MAY-2017 Supporting Document Number: 001 Review Date: 19-MAR-2018 Applicant: Samsung Bioepis Co., Ltd. 107 Cheomdan-daero, Yeonsu-gu Incheon, Republic of Korea 21987 Drug: SB4, a proposed biosimilar to U.S.-licensed Enbrel (etanercept) Route of Administration: Subcutaneous Dosage Form: Single-use pre-filled syringes: 50 mg/1.0 mL (50 mg/mL); 25 mg/0.5 mL (50 mg/mL) Pharmacologic Category: 1-235-tumor necrosis factor receptor (human) fusion protein with 236-467-immunoglobulin Gi (human γ1-chain Fc fragment), dimer Proposed Indications: 1) Rheumatoid Arthritis (RA) in combination with methotrexate: Reducing signs and symptoms, inhibiting the progression of structural damage, and improving physical function in patients with moderately to severely active disease. 2) Polyarticular Juvenile Idiopathic Arthritis Reducing signs and symptoms of moderately to severe active polyarticular juvenile idiopathic arthritis (JIA) in patients 2 years and older and weigh 63 kg (138 pounds) or more. 3) Ankylosing Spondylitis (AS): Reducing signs and symptoms in patients with active disease 4) Psoriatic Arthritis (PsA): Reducing signs and symptoms of active arthritis, inhibiting the progression of structural damage, and improving physical function. 5) Plaque Psoriasis (PsO): Treatment of patients 4 years and older with chronic moderate or severe plaque psoriasis who are candidates for systemic therapy or phototherapy. Project Manager: Barbara Gould Team Leader: David Kettl, MD Medical Officer: Gary Chiang, MD, MPH.
    [Show full text]