DOCSLIB.ORG

Cinqüenta Anos De Medicamentos Antipsicóticos Em Psiquiatria 1

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Cinqüenta Anos De Medicamentos Antipsicóticos Em Psiquiatria 1 CINQÜENTA ANOS DE MEDICAMENTOS ANTIPSICÓTICOS EM PSIQUIATRIA 1. FENOTIAZINAS 2.TIOXANTENOS 3. BUTIROFENONAS 4. DIFENILBUTILPIPERIDINAS/ PIPERAZINAS 5. INDÓIS 6. BENZAMIDAS 7. DIBENZOXAZEPINAS 8. DIBENZOXEPINAS 9. DIBENZAZEPINAS 10. DIBENZODIAZEPINAS 11. TIENOBENZODIAZEPINAS 12. DIBENZOTIAZEPINAS 13. DIBENZOTIEPINAS 14. BENZO-HETEROEPINAS OUTRAS 15. BENZISOXAZÓIS 16. BENZISOTIAZÓIS 17. QUINOLINONAS 18. OUTROS ANTIPSICÓTICOS LEOPOLDO HUGO FROTA REVISÃO ORTOGRÁFICA: Profa. Maria Beatriz Torres Frota Colégio Pedro II 2 Aos meus pais Eduardo e Mary; Aos meus filhos Eduardo Hugo, Lia e Camille; Aos meus irmãos, colegas, funcionários, pacientes e familiares do IPUB; À Tibá. LEOPOLDO HUGO FROTA, M.D. [email protected] MÉDICO PSIQUIATRA & PSICOTERAPEUTA Professor Adjunto do DEPARTAMENTO DE PSIQUIATRIA E MEDICINA LEGAL da Faculdade de Medicina da UNIVERSIDADE FEDERAL DO RIO DE JANEIRO (UFRJ). co-HEAD, WORLD HEALTH ORGANIZATION (WHO) COLLABORATING CENTRE IN MENTAL HEALTH - INSTITUTO DE PSIQUIATRIA IPUB/UFRJ. Preceptor do PROGRAMA DE RESIDÊNCIA MÉDICA do Instituto de Psiquiatria IPUB/UFRJ. Membro do COMITÊ DE ÉTICA EM PESQUISAS do Instituto de Psiquiatria – IPUB/UFRJ. Coordenador da DISCIPLINA DE PSICOPATOLOGIA GERAL ministrada pelo DEPARTAMENTO DE PSIQUIATRIA E MEDICINA LEGAL para alunos de graduação do INSTITUTO DE PSICOLOGIA DA UFRJ. REVISÃO ORTOGRÁFICA Profa. Maria Beatriz Torres Frota Colégio Pedro II – Rio de Janeiro 3 4 CARFENAZINA 38 SUMÁRIO - I CICLOFENAZINA 39 PREFÁCIO 11 CLORIMPIFENINA 39 DIXIRAZINA 39 FLUFENAZINA 40 INTRODUÇÃO 12 METOFENAZINA 44 OXAFLUMAZINA 45 HISTÓRICO 13 PERAZINA 45 REFERÊNCIAS 16 PERFENAZINA 46 PROCLORPERAZINA 48 I. FENOTIAZINAS 17 TIETILPERAZINA 49 TIOPROPAZATO 49 TIOPROPERAZINA 50 TRIFLUPERAZINA 51 REFERÊNCIAS 52 C. PIPERIDÍNICAS A-124 60 MEPAZINA 61 MESORIDAZINA 61 NORTIORIDAZINA 62 PERIMETAZINA 63 PIPAMAZINA 63 PIPERACETAZINA 64 PIPOTIAZINA 64 A) ALQUILAMÍNICAS OU COM PROPERICIAZINA 65 CADEIA LATERAL ALIFÁTICA SULFORIDAZINA 66 TIORIDAZINA 67 REFERÊNCIAS 71 ACEPROMAZINA 19 ALIMEMAZINA 20 D. OUTROS COMPOSTOS AMINOPROMAZINA 21 CIAMEMAZINA 22 CLOMACRAM 78 CLORPROMAZINA 22 DUOPERONA 79 ETIMEMAZINA 26 ESPICLOMAZINA 80 LEVOMEPROMAZINA 27 FLUOTRACENO 80 METIOMEPRAZINA 28 HOMOFENAZINA 81 METOPROMAZINA 29 OXIPENDIL 81 PROMAZINA 29 PROTIPENDIL 82 PROMETAZINA 30 REFERÊNCIAS 83 TRIFLUPROMAZINA 32 REFERÊNCIAS 32 II. TIOXANTENOS 85 B) PIPERAZÍNICAS CLORPROTIXENO 86 CLOTIXAMIDA 88 ACETOFENAZINA 37 FLUPENTIXOL 88 BUTAPERAZINA 37 PIFLUTIXOL 92 5 TEFLUTIXOL 93 CINUPERONA 138 TIOTIXENO 93 FENAPERONA 138 ZUCLOPENTIXOL 95 FG-5803 139 REFERÊNCIAS 99 FLUANISONA 139 REFERÊNCIAS 140 III. BUTIROFENONAS C) BUTIROFENONAS 108 4-PIPERIDILPIPERIDÍNICAS & PIPERIDÍNICAS OUTRAS INTRODUÇÃO 108 AL-449 141 BROMPERIDOL 142 CARPERONA 143 CLOFLUPEROL 143 CLOROPERONA 144 ID-4708 144 LEMPERONA 144 MELPERONA 145 MOPERONA 148 PIPAMPERONA 149 PIREMPERONA 150 PROPIPERONA 151 TRIFLUPERIDOL 151 W-6123 152 REFERÊNCIAS 153 A) O HALOPERIDOL E AS BUTIROFENONAS D) OUTRAS 4-ANILINOPIPERIDÍNICAS BUTIROFENONAS BEMPERIDOL 112 AHR-1900 158 BROMOSPIPERONA 113 NONAPERONA 159 DROPERIDOL 113 U-25927 159 ESPIPERONA 115 REFERÊNCIAS 159 FLUSPIPERONA 116 HALOPERIDOL 116 IODOSPIPERONA 123 IV.DIFENILBUTILPIPER TIMIPERONA 123 REFERÊNCIAS 124 IDINAS / PIPERAZINAS B) BUTIROFENONAS 160 4-ARILPIPERAZÍNICAS AMPEROZIDA 160 AZABUPERONA 135 CLOPIMOZIDA 161 AZAPERONA 135 FLUSPIRILENO 162 BIRIPERONA 136 PENFLURIDOL 163 BUTROPIPAZONA 137 PIMOZIDA 165 CENTPIRAQUIM 137 REFERÊNCIAS 168 6 V. INDÓIS 175 VI. BENZAMIDAS 201 INTRODUÇÃO 175 A) DERIVADOS AMINO-ETIL REFERÊNCIAS 178 BROMOPRIDA 205 METOCLOPRAMIDA 206 TIAPRIDA 207 REFERÊNCIAS 208 B) DERIVADOS 4-PIPERIDINIL CISAPRIDA 211 CLEBOPRIDA 212 PRIDEPERONA 213 REFERÊNCIAS 213 A) A RESERPINA & OS ALCALÓIDES DA C) DERIVADOS 2- RAUWOLFIA PIRROLIDINIL DESERPIDINA 179 ALPIROPRIDA 215 RESCINAMINA 179 AMISSULPRIDA 215 RESERPINA 180 LUR 2366 218 REFERÊNCIAS 183 PROSSULPRIDA 219 RACLOPRIDA 219 REMOXIPRIDA 220 B) OUTROS INDÓLICOS SULMEPRIDA 222 AL-1612 184 SULPIRIDA 223 CARBIDINA 185 SULTOPRIDA 226 FLUTROLINA 185 VERALIPRIDA 227 MILIPERTINA 186 REFERÊNCIAS 228 MOLINDONA 187 D) DERIVADOS 3- OXIPERTINA 188 PIQUINDONA 189 PIRROLIDINIL ROXINDOL 189 NEMONAPRIDA 236 SOLIPERTINA 190 REFERÊNCIAS 237 TEPIRINDOL 190 REFERÊNCIAS 191 E) OUTRAS BENZAMIDAS C) O SERTINDOL E AS 2- 5-Ome-BPAT 239 IMIDAZOLIDINONAS BRL 34778 240 BW-1192U90 240 AL-1965 195 DAZOPRIDA 241 SERTINDOL 195 HALOPEMIDA 241 ZETIDOLINA 197 Y 20024 242 REFERÊNCIAS 198 REFERÊNCIAS 242 7 SUMÁRIO - II XII. DIBENZOTIAZEPINAS INTRODUÇÃO ÀS BENZO- CLOTIAPINA 318 METIAPINA 319 HETEROEPINAS 244 QUETIAPINA 320 REFERÊNCIAS 245 REFERÊNCIAS 329 XIII. DIBENZOTIEPINAS VII. DIBENZOXAZEPINAS CITATEPINA 335 AMOXAPINA 246 CLOFLUMIDA 336 LOXAPINA 247 CLOROTEPINA 336 REFERÊNCIAS 250 DOCLOXITEPINA 337 ISOFLOXITEPINA 338 VIII. DIBENZOXEPINAS METITEPINA 338 OXIPROTEPINA 339 ASENAPINA 255 PERATIEPINA 340 CIPAZOXAPINA 256 ZOTEPINA 340 MAROXEPINA 256 REFERÊNCIAS 343 METOXEPINA 257 RMI 61140 257 RMI 61280 258 XIV. OUTRAS BENZO- REFERÊNCIAS 258 HETEROEPINAS SCH 23390 347 IX. DIBENZAZEPINAS SCH 24518 348 SKF 38393 348 CARPIPRAMINA 260 SKF 83566 348 CLOCAPRAMINA 262 SKF 83692 349 ERESEPINA 263 TREPIPAM 349 FLUPERLAPINA 263 REFERÊNCIAS 349 MOSAPRAMINA 265 PERLAPINA 266 RMI 81582 266 XV. BENZISOXAZÓIS REFERÊNCIAS 267 ABAPERIDONA 352 ILOPERIDONA 353 X. DIBENZODIAZEPINAS NEFLUMOZIDA 355 OCAPERIDONA 355 CLOZAPINA 267 RISPERIDONA 356 REFERÊNCIAS 288 REFERÊNCIAS 379 XI. TIENOBENZODIAZEPI- XVI. BENZISOTIAZÓIS NAS PEROSPIRONA 396 FLUMEZAPINA 297 SUPIDIMIDA 397 OLANZAPINA 298 TIOSPIRONA 398 REFERÊNCIAS 308 ZIPRASIDONA 399 8 REFERÊNCIAS 405 KC-5944 438 L-741,626 438 XVII. QUINOLINONAS L-745,870 438 LEK 8829 439 ARIPIPRAZOL 410 LINTITRIPT 439 OPC-4392 416 M-100907 440 REFERÊNCIAS 417 MANASSANTINA A 440 MAZAPERTINA 441 XVIII. OUTROS MEZILAMINA 442 MILACEMIDA 442 ANTIPSICÓTICOS MILEMPERONA 443 2-Daodp 420 NAFADOTRIDA 443 3-Fbpt 421 NE-100 444 8-NLE-CER(4,10) 421 ODAPIPAM 444 74-637 421 OXIPEROMIDA 445 ALENTAMOL 422 PALINDOR 445 ALTANSERINA 422 PD-112488 446 AMPACINA CX516 423 PD-143168 446 APREPIPANTO 424 PENTIAPINA 447 AXAMOZIDA 424 PINOXEPINA 447 BALAPERIDONA 425 PNU-96415E 448 BATELAPINA 425 QM 7184 448 BERUPIPAM 426 SCS 100 448 BIFEPRUNOX 426 SDZ HDC-912 449 BLONANSERINA 427 SETOPERONA 449 BMY-13980-1 428 SONEPIPRAZOL 450 BRL 20596 428 SR 31742A 451 BROFOXINA 429 SR-141716A 451 BROMERGURIDA 429 TEFLUDAZINA 452 BUTACLAMOL 430 THE-JL-13 452 CARVOTROLINA 430 TILOZEPINA 453 CI-943 431 TIMELOTEM 453 CICLINDOL 431 TRABOXOPINA 454 CICLOTIZOLAM 432 TREBENZOMINA 454 CLOPIPAZAM 432 UMESPIRONA 455 CLORMETILSILATRANO 432 XANOMELINA 455 DAPIPRAZOL 433 ZOLOPERONA 456 DN 1417 433 REFERÊNCIAS 456 Dup 734 434 ECOPIPAM 434 OUTROS COMPOSTOS COM FANANSERINA 435 POTENCIAL UTILIDADE NA FLUCINDOL 435 ESQUIZOFRENIA 456 GEVOTROLINA 436 HP 236 436 ÍNDICE REMISSIVO DE IB-503 436 ANTIPSICÓTICOS 469 JINKO-HEREMOL 437 9 10 país ou no exterior. Pretendeu-se uma obra Prefácio completa, de referência, não somente para o psiquiatra clínico como para investigadores, Vive a Psiquiatria o limiar de nova era bioquímicos, farmacólogos, médicos legistas e na História da terapêutica das psicoses com a toxicologistas, neurologistas e outros reabilitação da clozapina e o desenvolvimento, especialistas, além de estudantes de graduação e nos últimos anos, de nova e revolucionária série pós-graduação, profissinais, planejadores e de antipsicóticos: os atípicos de segunda geração. gerenciadores da Área da Saúde e da indústria Neste momento, quando simultaneamente farmacêutica. são completados 50 anos da introdução dos O estudo pretende abarcar os 250 neurolépticos ou antipsicóticos típicos, compostos mais relevantes obtidos nestes consagram-se os novos medicamentos e acaba de cinqüenta anos, estudados por 18 capítulos com ser mapeado o genoma humano -que espera-se, 36 seções ou subseções, que foram identificados a venha em futuro não muito distante permitir o partir de uma ampla revisão da literatura, da desenvolvimento de terapêuticas revolucionárias, qual estão selecionadas cerca de 5500 referências não-farmacológicas, para a esquizofrenia- nada bibliográficas. Na intenção de facilitar mais conveniente para dar-nos a correta consultas, foi incluído um Índice Remissivo com perspectiva e melhor calçar avanços futuros, do quase 2000 verbetes, contendo não somente que um amplo olhar retrospectivo a fim de nomes genéricos, como nomes de marca e nomes inventariar o alcançado até aqui, dando fecho a codificados, incluindo possíveis variações, pelos esta dura etapa de conquistas e realizações. quais cada composto tornou-se inicialmente A extensão do tema obrigou-nos à conhecido nas publicações de fases pré-clínicas divisão da matéria em duas partes. Esta divisão ou clínicas pré-licenciamento, um recurso acabou obedecendo, fortuitamente e ainda que indispensável para a precisa e abrangente com importantes exceções, à distinção em grupos localização das referências nos bancos de dados químicos tradicionais (parte I) e grupos químicos químicos, toxicológicos e bibliográficos hoje recentes (parte II). Entretanto, o leitor deve disponibilizados na Internet. estar advertido de que haverá capítulos onde são Procuramos, sempre que possível, simultaneamente examinados antipsicóticos destacar a produção científica nacional e dos típicos e atípicos, medicamentos convencionais e autores de países da Língua Portuguesa mas, novos, como por exemplo, os capítulos sobre os dadas as habituais dificuldades de registro e derivados indólicos (V) ou o das benzamidas (VI), intercâmbio entre nós,
Load more

Recommended publications
  • WO 2017/145013 Al 31 August 2017 (31.08.2017) 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 2017/145013 Al 31 August 2017 (31.08.2017) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C07D 498/04 (2006.01) A61K 31/5365 (2006.01) kind of national protection available): AE, AG, AL, AM, C07D 519/00 (2006.01) A61P 25/00 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (21) Number: International Application DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, PCT/IB20 17/050844 HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (22) International Filing Date: KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, 15 February 2017 (15.02.2017) MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (25) Filing Language: English RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, (26) Publication Language: English TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: 62/298,657 23 February 2016 (23.02.2016) US (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, New York, New York 10017 (US).
    [Show full text]
  • Metabolism and Pharmacokinetics in the Development of New Therapeutics for Cocaine and Opioid Abuse
    University of Mississippi eGrove Electronic Theses and Dissertations Graduate School 2012 Metabolism And Pharmacokinetics In The Development Of New Therapeutics For Cocaine And Opioid Abuse Pradeep Kumar Vuppala University of Mississippi Follow this and additional works at: https://egrove.olemiss.edu/etd Part of the Pharmacy and Pharmaceutical Sciences Commons Recommended Citation Vuppala, Pradeep Kumar, "Metabolism And Pharmacokinetics In The Development Of New Therapeutics For Cocaine And Opioid Abuse" (2012). Electronic Theses and Dissertations. 731. https://egrove.olemiss.edu/etd/731 This Dissertation is brought to you for free and open access by the Graduate School at eGrove. It has been accepted for inclusion in Electronic Theses and Dissertations by an authorized administrator of eGrove. For more information, please contact [email protected]. METABOLISM AND PHARMACOKINETICS IN THE DEVELOPMENT OF NEW THERAPEUTICS FOR COCAINE AND OPIOID ABUSE A Dissertation presented in partial fulfillment of requirements for the degree of Doctor of Philosophy in Pharmaceutical Sciences in the Department of Pharmaceutics The University of Mississippi by PRADEEP KUMAR VUPPALA April 2012 Copyright © 2012 by Pradeep Kumar Vuppala All rights reserved ABSTRACT Cocaine and opioid abuse are a major public health concern and the cause of significant morbidity and mortality worldwide. The development of effective medication for cocaine and opioid abuse is necessary to reduce the impact of this issue upon the individual and society. The pharmacologic treatment for drug abuse has been based on one of the following strategies: agonist substitution, antagonist treatment, or symptomatic treatment. This dissertation is focused on the role of metabolism and pharmacokinetics in the development of new pharmacotherapies, CM304 (sigma-1 receptor antagonist), mitragynine and 7-hydroxymitragynine (µ-opioid receptor agonists), for the treatment of drug abuse.
    [Show full text]
  • A Role for Histone Modification in the Mechanism of Action of Antidepressant and Stimulant Drugs: a Dissertation
    University of Massachusetts Medical School eScholarship@UMMS GSBS Dissertations and Theses Graduate School of Biomedical Sciences 2007-12-28 A Role for Histone Modification in the Mechanism of Action of Antidepressant and Stimulant Drugs: a Dissertation Frederick Albert Schroeder University of Massachusetts Medical School Let us know how access to this document benefits ou.y Follow this and additional works at: https://escholarship.umassmed.edu/gsbs_diss Part of the Amino Acids, Peptides, and Proteins Commons, Cells Commons, Enzymes and Coenzymes Commons, Genetic Phenomena Commons, Mental Disorders Commons, Nervous System Commons, and the Therapeutics Commons Repository Citation Schroeder FA. (2007). A Role for Histone Modification in the Mechanism of Action of Antidepressant and Stimulant Drugs: a Dissertation. GSBS Dissertations and Theses. https://doi.org/10.13028/7bk0-a687. Retrieved from https://escholarship.umassmed.edu/gsbs_diss/370 This material is brought to you by eScholarship@UMMS. It has been accepted for inclusion in GSBS Dissertations and Theses by an authorized administrator of eScholarship@UMMS. For more information, please contact [email protected]. A Dissertation Presented by Frederick Albert Schroeder Submitted to the Faculty of the University of Massachusetts Graduate School of Biomedical Sciences Worcester, Massachusetts, USA in partial fulfillment of the requirements for the degree of DOCTOR OF PHILOSOPHY December 28, 2007 Program in Neuroscience A Role for Histone Modification in the Mechanism of Action of Antidepressant and Stimulant Drugs A Dissertation Presented By Frederick Albert Schroeder Approved as to style and content by: _____________________________________ Alonzo Ross, Ph.D., Chair of Committee _____________________________________ Pradeep Bhide, Ph.D., Member of Committee _____________________________________ Craig L.
    [Show full text]
  • WO 2016/123576 Al 4 August 2016 (04.08.2016) P O P C T
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization I International Bureau (10) International Publication Number (43) International Publication Date WO 2016/123576 Al 4 August 2016 (04.08.2016) P O P C T (51) International Patent Classification: Unit L, Baltimore, Maryland 21209 (US). WEINBER¬ A61K 31/535 (2006.01) GER, Daniel; 3116 Davenport St. NW, Washington, Dis trict of Columbia 20008-2244 (US). (21) International Application Number: PCT/US2016/015832 (74) Agent: KELLY, Bryte; King & Spalding LLP, 1185 Av enue of the Americas, New York, New York 10036 (US). (22) International Filing Date: 29 January 2016 (29.01 .2016) (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (25) Language: English Filing AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (26) Publication Language: English BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (30) Priority Data: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 62/109,954 30 January 2015 (30.01.2015) US KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (71) Applicant: LIEBER INSTITUTE FOR BRAIN DE¬ MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, VELOPMENT [US/US]; 855 North Wolfe Street, Suite PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, 300, 3rd Floor, Baltimore, Maryland 21205 (US). SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
    [Show full text]
  • Formulary (List of Covered Drugs)
    3ODQ<HDU 202 Formulary (List of Covered Drugs) PLEASE READ: THIS DOCUMENT CONTAINS INFORMATION ABOUT THE DRUGS WE COVER IN THE FOLLOWING PLAN: $0 Cost Share AI/AN HMO Minimum Coverage HMO Silver 70 HMO Active Choice PPO Silver Opal 25 Gold HMO Silver 70 OFF Exchange HMO Amber 50 HMO Silver Opal 50 Silver HMO Silver 73 HMO Bronze 60 HDHP HMO Platinum 90 HMO Silver 87 HMO Bronze 60 HMO Ruby 10 Platinum HMO Silver 94 HMO Gold 80 HMO Ruby 20 Platinum HMO Jade 15 HMO Ruby 40 Platinum HMO This formulary was last updated on8//20. This formulary is VXEMHFWto change and all previous versions of the formulary no longer apply. For more recent information or other questions, please contact Chinese Community Health Plan Member Services at 1-888-775-7888 or, for TTY users, 1-877-681-8898, seven days a week from 8:00 a.m. to 8:00 p.m., or visit www.cchphealthplan.com/family-member -,-ϭ -,-ϭ"&* !#" + 5 5 ),-$+" %(%'.')/"+#" %&/"+ -%/"$)% "%&/"+ *& )&! %&/"+ 0 $(#" '"+ %&/"+ *& %&/"+ %&/"+ +)(2" &-%(.' %&/"+ +)(2" .1&-%(.' %&/"+ )&! .1&-%(.' !" .1&-%(.' dŚŝƐĨŽƌŵƵůĂƌLJǁĂƐůĂƐƚƵƉĚĂƚĞĚ8ͬϭͬϮϬϮϭ͘dŚŝƐĨŽƌŵƵůĂƌLJŝƐƐƵďũĞĐƚƚŽ ĐŚĂŶŐĞĂŶĚĂůůƉƌĞǀŝŽƵƐǀĞƌƐŝŽŶƐŽĨƚŚĞĨŽƌŵƵůĂƌLJŶŽůŽŶŐĞƌĂƉƉůLJ͘&ŽƌŵŽƌĞ ƌĞĐĞŶƚŝŶĨŽƌŵĂƚŝŽŶŽƌŽƚŚĞƌƋƵĞƐƚŝŽŶƐ͕ƉůĞĂƐĞĐŽŶƚĂĐƚŚŝŶĞƐĞŽŵŵƵŶŝƚLJ ,ĞĂůƚŚWůĂŶDĞŵďĞƌ^ĞƌǀŝĐĞƐĂƚϭͲϴϴϴͲϳϳϱͲϳϴϴϴŽƌ͕ĨŽƌddzƵƐĞƌƐ͕ ϭͲϴϳϳͲϲϴϭͲϴϴϵϴ͕ƐĞǀĞŶĚĂLJƐĂǁĞĞŬĨƌŽŵϴ͗ϬϬĂ͘ŵ͘ƚŽϴ͗ϬϬƉ͘ŵ͕͘ŽƌǀŝƐŝƚ ǁǁǁ͘ĐĐŚƉŚĞĂůƚŚƉůĂŶ͘ĐŽŵͬĨĂŵŝůLJͲŵĞŵďĞƌ !! %+)&,+ &%+&+&)$,#)0),# *+666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666I % + &%*6666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666666I
    [Show full text]
  • Antipsychotics (Part-4) FLUOROBUTYROPHENONES
    Antipsychotics (Part-4) FLUOROBUTYROPHENONES The fluorobutyrophenones belong to a much-studied class of compounds, with many compounds possessing high antipsychotic activity. They were obtained by structure variation of the analgesic drug meperidine by substitution of the N-methyl by butyrophenone moiety to produce the butyrophenone analogue which has similar activity as chlorpromazine. COOC2H5 N H3C Meperidine COOC2H5 N O Butyrophenone analog The structural requirements for antipsychotic activity in the group are well worked out. General features are expressed in the following structure. F AR Y O N • Optimal activity is seen when with an aromatic with p-fluoro substituent • When CO is attached with p-fluoroaryl gives optimal activity is seen, although other groups, C(H)OH and aryl, also give good activity. • When 3 carbons distance separates the CO from cyclic N gives optimal activity. • The aliphatic amino nitrogen is required, and highest activity is seen when it is incorporated into a cyclic form. • AR is an aromatic ring and is needed. It should be attached directly to the 4-position or occasionally separated from it by one intervening atom. • The Y group can vary and assist activity. An example is the hydroxyl group of haloperidol. The empirical SARs suggest that the 4-aryl piperidino moiety is superimposable on the 2-- phenylethylamino moiety of dopamine and, accordingly, could promote affinity for D2 receptors. The long N-alkyl substituent could help promote affinity and produce antagonistic activity. Some members of the class are extremely potent antipsychotic agents and D2 receptor antagonists. The EPS are extremely marked in some members of this class, which may, in part, be due to a potent DA block in the striatum and almost no compensatory striatal anticholinergic block.
    [Show full text]
  • G Protein-Coupled Receptors
    S.P.H. Alexander et al. The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors. British Journal of Pharmacology (2015) 172, 5744–5869 THE CONCISE GUIDE TO PHARMACOLOGY 2015/16: G protein-coupled receptors Stephen PH Alexander1, Anthony P Davenport2, Eamonn Kelly3, Neil Marrion3, John A Peters4, Helen E Benson5, Elena Faccenda5, Adam J Pawson5, Joanna L Sharman5, Christopher Southan5, Jamie A Davies5 and CGTP Collaborators 1School of Biomedical Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK, 2Clinical Pharmacology Unit, University of Cambridge, Cambridge, CB2 0QQ, UK, 3School of Physiology and Pharmacology, University of Bristol, Bristol, BS8 1TD, UK, 4Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK, 5Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK Abstract The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. The full contents can be found at http://onlinelibrary.wiley.com/doi/ 10.1111/bph.13348/full. G protein-coupled receptors are one of the eight major pharmacological targets into which the Guide is divided, with the others being: ligand-gated ion channels, voltage-gated ion channels, other ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading.
    [Show full text]
  • The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
    WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters.
    [Show full text]
  • Diphenylbutylpiperidine Antipsychotic Drugs Inhibit Prolactin Receptor
    Gastroenterology 2020;158:1433–1449 Diphenylbutylpiperidine Antipsychotic Drugs Inhibit Prolactin Receptor Signaling to Reduce Growth of Pancreatic Ductal Adenocarcinoma in Mice Prasad Dandawate,1 Gaurav Kaushik,2 Chandrayee Ghosh,1 David Standing,1 Afreen Asif Ali Sayed,1 Sonali Choudhury,1 Dharmalingam Subramaniam,1 Ann Manzardo,3 Tuhina Banerjee,4 Santimukul Santra,4 Prabhu Ramamoorthy,1 Merlin Butler,3 Subhash B. Padhye,1,5 Joaquina Baranda,6 Anup Kasi,6 Weijing Sun,6 Ossama Tawfik,7 Domenico Coppola,8 Mokenge Malafa,8 Shahid Umar,2 Michael J. Soares,7,9,10,11 Subhrajit Saha,12 Scott J. Weir,1,13 Animesh Dhar,1 Roy A. Jensen,1,7 Sufi Mary Thomas,1,14 and Shrikant Anant1,2,5 1Department of Cancer Biology, University of Kansas Medical Center, Kansas City, Kansas; 2Department of Surgery, University of Kansas Medical Center, Kansas City, Kansas; 3Department of Psychiatry and Behavioral Sciences, University of Kansas Medical Center, Kansas City, Kansas; 4Department of Chemistry, Pittsburg State University, Pittsburg, Kansas; 5Interdisciplinary Science and Technology Research Academy, Abeda Inamdar College, University of Pune, Pune; 6Department of Internal Medicine, University of Kansas Medical Center, Kansas City, Kansas; 7Department of Pathology and Laboratory Medicine, University of Kansas Medical Center, Kansas City, Kansas; 8Department of Gastrointestinal Oncology, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida; 9Department of Obstetrics and Gynecology, University of Kansas Medical Center, Kansas City, Kansas; 10Department
    [Show full text]
  • Estonian Statistics on Medicines 2016 1/41
    Estonian Statistics on Medicines 2016 ATC code ATC group / Active substance (rout of admin.) Quantity sold Unit DDD Unit DDD/1000/ day A ALIMENTARY TRACT AND METABOLISM 167,8985 A01 STOMATOLOGICAL PREPARATIONS 0,0738 A01A STOMATOLOGICAL PREPARATIONS 0,0738 A01AB Antiinfectives and antiseptics for local oral treatment 0,0738 A01AB09 Miconazole (O) 7088 g 0,2 g 0,0738 A01AB12 Hexetidine (O) 1951200 ml A01AB81 Neomycin+ Benzocaine (dental) 30200 pieces A01AB82 Demeclocycline+ Triamcinolone (dental) 680 g A01AC Corticosteroids for local oral treatment A01AC81 Dexamethasone+ Thymol (dental) 3094 ml A01AD Other agents for local oral treatment A01AD80 Lidocaine+ Cetylpyridinium chloride (gingival) 227150 g A01AD81 Lidocaine+ Cetrimide (O) 30900 g A01AD82 Choline salicylate (O) 864720 pieces A01AD83 Lidocaine+ Chamomille extract (O) 370080 g A01AD90 Lidocaine+ Paraformaldehyde (dental) 405 g A02 DRUGS FOR ACID RELATED DISORDERS 47,1312 A02A ANTACIDS 1,0133 Combinations and complexes of aluminium, calcium and A02AD 1,0133 magnesium compounds A02AD81 Aluminium hydroxide+ Magnesium hydroxide (O) 811120 pieces 10 pieces 0,1689 A02AD81 Aluminium hydroxide+ Magnesium hydroxide (O) 3101974 ml 50 ml 0,1292 A02AD83 Calcium carbonate+ Magnesium carbonate (O) 3434232 pieces 10 pieces 0,7152 DRUGS FOR PEPTIC ULCER AND GASTRO- A02B 46,1179 OESOPHAGEAL REFLUX DISEASE (GORD) A02BA H2-receptor antagonists 2,3855 A02BA02 Ranitidine (O) 340327,5 g 0,3 g 2,3624 A02BA02 Ranitidine (P) 3318,25 g 0,3 g 0,0230 A02BC Proton pump inhibitors 43,7324 A02BC01 Omeprazole
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2010/0081713 A1 Sharma Et Al
    US 20100081713A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0081713 A1 Sharma et al. (43) Pub. Date: Apr. 1, 2010 (54) COMPOSITIONS AND METHODS FOR (22) Filed: Mar. 18, 2009 TREATINGVIRAL INFECTIONS Related U.S. Application Data (75) Inventors: Geeta Sharma, Singapore (SG); (60) Provisional application No. 61/069,917, filed on Mar. Ralf Altmeyer, Singapore (SG); 19, 2008. Vishal Pendharker, Singapore (SG); Yu Chen, Singapore (SG); Publication Classification Michael Foley, Chestnut Hill, MA (51) Int. Cl. (US) A63L/35 (2006.01) A6II 3L/25 (2006.01) Correspondence Address: A63L/35 (2006.01) Gearhart Law LLC A6II 3/13 (2006.01) 4 Femdale Avenue A6IP3L/2 (2006.01) Chatham, NJ 07928 (US) (52) U.S. Cl. .......... 514/459; 514/529; 514/647: 514/662 (73) Assignee: CombinatoRx, (Singapore) Pte. (57) ABSTRACT Ltd. The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infec (21) Appl. No.: 12/406,716 tion caused by an influenza virus). Patent Application Publication Apr. 1, 2010 Sheet 1 of 2 US 2010/0081713 A1 ------ 80 r -0. Vehicle 0.5% HPMC g - - Sertraline-30mg/kg/day - £ 60 “A Sertraline-100mg/kg/day/kg/day i -v. Oseltamivir-30mg/kg/day ...i -0. Oseltamivir-100mg/kg/day -0. (Sertraline 30mg/kg+ . 40 Prednisolone 0.1 mg/Kg) Figure 1 Patent Application Publication Apr. 1, 2010 Sheet 2 of 2 US 2010/0081713 A1 100 468OOO 2 O Wehicle Sentraline 10 mg/kg Sentraline 30mg/kg Setraline 100mg/kg Figure 2 US 2010/008 1713 A1 Apr.
    [Show full text]
  • Repurposing Diphenylbutylpiperidine-Class Antipsychotic Drugs for Host
    bioRxiv preprint doi: https://doi.org/10.1101/2021.06.05.447191; this version posted June 6, 2021. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under aCC-BY-NC-ND 4.0 International license. 1 Repurposing diphenylbutylpiperidine-class antipsychotic drugs for host- 2 directed therapy of Mycobacterium tuberculosis and Salmonella enterica 3 infections 4 Heemskerk MT1, Korbee CJ1, Esselink J1, Carvalho dos Santos C1,2, van Veen S1, Gordijn IF1, 5 Vrieling F1, Walburg KV1, Engele CG1, Dijkman K3, Wilson L1, Verreck FAW3, Ottenhoff 6 THM1* and Haks MC1*. 7 1Department of Infectious Diseases, Leiden University Medical Center, Leiden, The 8 Netherlands. 2Laboratório Especial de Desenvolvimento de Vacinas, Instituto Butantan, São 9 Paulo, Brazil. 3TB research group, Department of Parasitology, Biomedical Primate Research 10 Centre, Rijswijk, The Netherlands. 11 * contributed equally. 12 13 14 15 Corresponding author: Tom HM Ottenhoff 16 Dept. of Infectious Diseases 17 Leiden University Medical Center (LUMC) 18 Albinusdreef 2 19 2333 ZA Leiden 20 The Netherlands 21 Tel: +31 71 526 2620 22 E-mail: [email protected] 23 ORCID ID: 0000-0003-3706-3403 24 25 1 bioRxiv preprint doi: https://doi.org/10.1101/2021.06.05.447191; this version posted June 6, 2021. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under aCC-BY-NC-ND 4.0 International license.
    [Show full text]