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NIH Public Access Author Manuscript Bioorg Med Chem
NIH Public Access Author Manuscript Bioorg Med Chem. Author manuscript; available in PMC 2013 February 01. NIH-PA Author ManuscriptPublished NIH-PA Author Manuscript in final edited NIH-PA Author Manuscript form as: Bioorg Med Chem. 2012 February 1; 20(3): 1291–1297. doi:10.1016/j.bmc.2011.12.019. Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents Kwakye Pepraha, Xue Y. Zhua, Suresh V. K. Eyunnia, Vincent Setolab, Bryan L. Rothb, and Seth Y. Ablordeppey*,a aDivision of Basic Pharmaceutical Sciences, Florida A&M University, College of Pharmacy and Pharmaceutical Sciences, Tallahassee, FL 32307, USA bDepartment of Pharmacology, Medicinal Chemistry and Psychiatry, University of North Carolina at Chapel Hill, School of Medicine, NC 27599, USA Abstract Using haloperidol as a scaffold, new agents were designed to investigate the structural contributions of various groups to binding at CNS receptors associated with atypical antipsychotic pharmacology. It is clear that each pharmacophoric group, the butyrophenone, the piperidine and the 4-chlorophenyl moieties contributes to changes in binding to the receptors of interest. This strategy has resulted in the identification of several new agents, compounds 16, 18, 19, 23, 24 and 25, with binding profiles which satisfy our stated criteria for agents to act as potential atypical antipsychotics. This research demonstrates that haloperidol can serve as a useful lead in the identification and design of new agents that target multiple receptors -
Centre for Reviews and Dissemination
Second-generation versus first-generation antipsychotic drugs for schizophrenia: a meta- analysis Leucht S, Corves C, D Arbter, Engel R R, Li C, Davis J M CRD summary The authors concluded that amisulpride, clozapine, olanzapine and risperidone can be effective in treating schizophrenia patients. Second-generation antipsychotic drugs can also result in fewer extrapyramidal side effects, but can induce weight gain. The authors' conclusions reflected the evidence presented, but some potential methodological flaws in the review process meant that the extent to which those conclusions were reliable was unclear. Authors' objectives To compare the effects of first and second-generation antipsychotic drugs in schizophrenia patients. Searching The search for eligible studies was started in 2005, including MEDLINE to October 2006, Cochrane Schizophrenia Group's Specialised Register and the US Food and Drugs Administration website. Search terms were reported and there were no language restrictions. Previous reviews were searched for additional relevant studies. Study selection Randomised controlled trials (RCTs) of oral second-generation antipsychotic drugs (amisulpride, aripiprazole, clozapine, olanzapine, quetiapine, risperidone, sertindole, ziprasidone and zotepine) compared with first-generation drugs in patients with schizophrenia or related disorders (schizoaffective, schizophreniform or delusional disorders) irrespective of diagnostic criteria were eligible for inclusion in the review. The optimum doses of second-generation drugs were selected -
(12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 De Juan Et Al
US 200601 10428A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 de Juan et al. (43) Pub. Date: May 25, 2006 (54) METHODS AND DEVICES FOR THE Publication Classification TREATMENT OF OCULAR CONDITIONS (51) Int. Cl. (76) Inventors: Eugene de Juan, LaCanada, CA (US); A6F 2/00 (2006.01) Signe E. Varner, Los Angeles, CA (52) U.S. Cl. .............................................................. 424/427 (US); Laurie R. Lawin, New Brighton, MN (US) (57) ABSTRACT Correspondence Address: Featured is a method for instilling one or more bioactive SCOTT PRIBNOW agents into ocular tissue within an eye of a patient for the Kagan Binder, PLLC treatment of an ocular condition, the method comprising Suite 200 concurrently using at least two of the following bioactive 221 Main Street North agent delivery methods (A)-(C): Stillwater, MN 55082 (US) (A) implanting a Sustained release delivery device com (21) Appl. No.: 11/175,850 prising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more (22) Filed: Jul. 5, 2005 bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more Related U.S. Application Data bioactive agents Subretinally; and (60) Provisional application No. 60/585,236, filed on Jul. (C) instilling (e.g., injecting or delivering by ocular ion 2, 2004. Provisional application No. 60/669,701, filed tophoresis) one or more bioactive agents into the Vit on Apr. 8, 2005. reous humor of the eye. Patent Application Publication May 25, 2006 Sheet 1 of 22 US 2006/0110428A1 R 2 2 C.6 Fig. -
2D6 Substrates 2D6 Inhibitors 2D6 Inducers
Physician Guidelines: Drugs Metabolized by Cytochrome P450’s 1 2D6 Substrates Acetaminophen Captopril Dextroamphetamine Fluphenazine Methoxyphenamine Paroxetine Tacrine Ajmaline Carteolol Dextromethorphan Fluvoxamine Metoclopramide Perhexiline Tamoxifen Alprenolol Carvedilol Diazinon Galantamine Metoprolol Perphenazine Tamsulosin Amiflamine Cevimeline Dihydrocodeine Guanoxan Mexiletine Phenacetin Thioridazine Amitriptyline Chloropromazine Diltiazem Haloperidol Mianserin Phenformin Timolol Amphetamine Chlorpheniramine Diprafenone Hydrocodone Minaprine Procainamide Tolterodine Amprenavir Chlorpyrifos Dolasetron Ibogaine Mirtazapine Promethazine Tradodone Aprindine Cinnarizine Donepezil Iloperidone Nefazodone Propafenone Tramadol Aripiprazole Citalopram Doxepin Imipramine Nifedipine Propranolol Trimipramine Atomoxetine Clomipramine Encainide Indoramin Nisoldipine Quanoxan Tropisetron Benztropine Clozapine Ethylmorphine Lidocaine Norcodeine Quetiapine Venlafaxine Bisoprolol Codeine Ezlopitant Loratidine Nortriptyline Ranitidine Verapamil Brofaramine Debrisoquine Flecainide Maprotline olanzapine Remoxipride Zotepine Bufuralol Delavirdine Flunarizine Mequitazine Ondansetron Risperidone Zuclopenthixol Bunitrolol Desipramine Fluoxetine Methadone Oxycodone Sertraline Butylamphetamine Dexfenfluramine Fluperlapine Methamphetamine Parathion Sparteine 2D6 Inhibitors Ajmaline Chlorpromazine Diphenhydramine Indinavir Mibefradil Pimozide Terfenadine Amiodarone Cimetidine Doxorubicin Lasoprazole Moclobemide Quinidine Thioridazine Amitriptyline Cisapride -
Pharmacotherapy, Drug-Drug Interactions and Potentially
medRxiv preprint doi: https://doi.org/10.1101/2021.03.31.21254518; this version posted April 6, 2021. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted medRxiv a license to display the preprint in perpetuity. It is made available under a CC-BY-NC-ND 4.0 International license . Pharmacotherapy, drug-drug interactions and potentially inappropriate medication in depressive disorders Jan Wolff1,2,3, Pamela Reißner4, Gudrun Hefner5, Claus Normann2, Klaus Kaier6, Harald Binder6, Christoph Hiemke7, Sermin Toto8, Katharina Domschke2, Michael Marschollek1, Ansgar Klimke4,9 1 Peter L. Reichertz Institute for Medical Informatics of TU Braunschweig and Hannover Medical School, Germany. 2 Department of Psychiatry and Psychotherapy, Medical Center - University of Freiburg, Faculty of Medicine, University of Freiburg, Freiburg, Germany. 3 Evangelical Foundation NeuerKerode, Germany. 4 Vitos Hochtaunus, Friedrichsdorf, Germany. 5 Vitos Clinic for Forensic Psychiatry, Eltville, Germany 6 Institute of Medical Biometry and Statistics, Medical Center - University of Freiburg, Faculty of Medicine, University of Freiburg, Germany. 7 Department of Psychiatry and Psychotherapy, University Medical Center Mainz, Germany. 8 Department of Psychiatry, Social Psychiatry and Psychotherapy, Hannover Medical School, Germany. 9 Heinrich-Heine-University Düsseldorf, Germany. ___ Correspondence Dr. Jan Wolff, Peter L. Reichertz Institute for Medical Informatics of TU Braunschweig and Hannover Medical School, Hannover, Germany. Address: Karl- Wiechert-Allee 3, 30625 Hannover. Email: [email protected], wolff.jan@mh- hannover.de, ORCID: https://orcid.org/0000-0003-2750-0606 Key words (MeSH) Depression, Polypharmacy, Antidepressants, Hospitals, Drug Interactions, Psychiatry NOTE: This preprint reports new research that has not been certified by peer review and should not be used to guide clinical practice. -
Adverse Reactions to Hallucinogenic Drugs. 1Rnstttutton National Test
DOCUMENT RESUME ED 034 696 SE 007 743 AUTROP Meyer, Roger E. , Fd. TITLE Adverse Reactions to Hallucinogenic Drugs. 1rNSTTTUTTON National Test. of Mental Health (DHEW), Bethesda, Md. PUB DATP Sep 67 NOTE 118p.; Conference held at the National Institute of Mental Health, Chevy Chase, Maryland, September 29, 1967 AVATLABLE FROM Superintendent of Documents, Government Printing Office, Washington, D. C. 20402 ($1.25). FDPS PRICE FDPS Price MFc0.50 HC Not Available from EDRS. DESCPTPTOPS Conference Reports, *Drug Abuse, Health Education, *Lysergic Acid Diethylamide, *Medical Research, *Mental Health IDENTIFIEPS Hallucinogenic Drugs ABSTPACT This reports a conference of psychologists, psychiatrists, geneticists and others concerned with the biological and psychological effects of lysergic acid diethylamide and other hallucinogenic drugs. Clinical data are presented on adverse drug reactions. The difficulty of determining the causes of adverse reactions is discussed, as are different methods of therapy. Data are also presented on the psychological and physiolcgical effects of L.S.D. given as a treatment under controlled medical conditions. Possible genetic effects of L.S.D. and other drugs are discussed on the basis of data from laboratory animals and humans. Also discussed are needs for futher research. The necessity to aviod scare techniques in disseminating information about drugs is emphasized. An aprentlix includes seven background papers reprinted from professional journals, and a bibliography of current articles on the possible genetic effects of drugs. (EB) National Clearinghouse for Mental Health Information VA-w. Alb alb !bAm I.S. MOMS Of NAM MON tMAN IONE Of NMI 105 NUNN NU IN WINES UAWAS RCM NIN 01 NUN N ONMININI 01011110 0. -
Appendix 13C: Clinical Evidence Study Characteristics Tables
APPENDIX 13C: CLINICAL EVIDENCE STUDY CHARACTERISTICS TABLES: PHARMACOLOGICAL INTERVENTIONS Abbreviations ............................................................................................................ 3 APPENDIX 13C (I): INCLUDED STUDIES FOR INITIAL TREATMENT WITH ANTIPSYCHOTIC MEDICATION .................................. 4 ARANGO2009 .................................................................................................................................. 4 BERGER2008 .................................................................................................................................... 6 LIEBERMAN2003 ............................................................................................................................ 8 MCEVOY2007 ................................................................................................................................ 10 ROBINSON2006 ............................................................................................................................. 12 SCHOOLER2005 ............................................................................................................................ 14 SIKICH2008 .................................................................................................................................... 16 SWADI2010..................................................................................................................................... 19 VANBRUGGEN2003 .................................................................................................................... -
The Effects of Antipsychotic Treatment on Metabolic Function: a Systematic Review and Network Meta-Analysis
The effects of antipsychotic treatment on metabolic function: a systematic review and network meta-analysis Toby Pillinger, Robert McCutcheon, Luke Vano, Katherine Beck, Guy Hindley, Atheeshaan Arumuham, Yuya Mizuno, Sridhar Natesan, Orestis Efthimiou, Andrea Cipriani, Oliver Howes ****PROTOCOL**** Review questions 1. What is the magnitude of metabolic dysregulation (defined as alterations in fasting glucose, total cholesterol, low density lipoprotein (LDL) cholesterol, high density lipoprotein (HDL) cholesterol, and triglyceride levels) and alterations in body weight and body mass index associated with short-term (‘acute’) antipsychotic treatment in individuals with schizophrenia? 2. Does baseline physiology (e.g. body weight) and demographics (e.g. age) of patients predict magnitude of antipsychotic-associated metabolic dysregulation? 3. Are alterations in metabolic parameters over time associated with alterations in degree of psychopathology? 1 Searches We plan to search EMBASE, PsycINFO, and MEDLINE from inception using the following terms: 1 (Acepromazine or Acetophenazine or Amisulpride or Aripiprazole or Asenapine or Benperidol or Blonanserin or Bromperidol or Butaperazine or Carpipramine or Chlorproethazine or Chlorpromazine or Chlorprothixene or Clocapramine or Clopenthixol or Clopentixol or Clothiapine or Clotiapine or Clozapine or Cyamemazine or Cyamepromazine or Dixyrazine or Droperidol or Fluanisone or Flupehenazine or Flupenthixol or Flupentixol or Fluphenazine or Fluspirilen or Fluspirilene or Haloperidol or Iloperidone -
Deanxit SPC.Pdf
SUMMARY OF PRODUCT CHARACTERISTICS 1. NAME OF THE MEDICINAL PRODUCT Deanxit film-coated tablets 2. QUALITATIVE AND QUANTITATIVE COMPOSITION Each tablet contains: Flupentixol 0.5 mg (as 0.584 mg flupentixol dihydrochloride) Melitracen 10 mg (as 11.25 mg melitracen hydrochloride) Excipients with known effect: Lactose monohydrate For the full list of excipients, see section 6.1. 3. PHARMACEUTICAL FORM Film-coated tablets. Round, biconvex, cyclamen, film-coated tablets. 4. CLINICAL PARTICULARS 4.1 Therapeutic indications Anxiety Depression Asthenia. Neurasthenia. Psychogenic depression. Depressive neuroses. Masked depression. Psychosomatic affections accompanied by anxiety and apathy. Menopausal depressions. Dysphoria and depression in alcoholics and drug-addicts. 4.2 Posology and method of administration Posology Adults Usually 2 tablets daily: morning and noon. In severe cases the morning dose may be increased to 2 tablets. The maximum dose is 4 tablets daily. Older people (> 65 years) 1 tablet in the morning. In severe cases 1 tablet in the morning and 1 at noon. Maintenance dose: Usually 1 tablet in the morning. SPC Portrait-REG_00051968 20v038 Page 1 of 10 In cases of insomnia or severe restlessness additional treatment with a sedative in the acute phase is recommended. Paediatric population Children and adolescents (<18 years) Deanxit is not recommended for use in children and adolescents due to lack of data on safety and efficacy. Reduced renal function Deanxit can be given in the recommended doses. Reduced liver function Deanxit can be given in the recommended doses. Method of administration The tablets are swallowed with water. 4.3 Contraindications Hypersensitivity to flupentixol and melitracen or to any of the excipients listed in section 6.1. -
Pharmacologyonline 2: 252-260 (2006) Colovic Et Al
Pharmacologyonline 2: 252-260 (2006) Colovic et al. THE 1-(2,3-DICHLOROPHENYL)-PIPERAZINE-TO-ARIPIPRAZOLE RATIO AT STEADY STATE IN RATS AND SCHIZOPHRENIC PATIENTS Milena Colovica, Giuseppe Campianib, Stefania Butinib, Alberto Parabiaghia and Silvio Cacciaa aIstituto di Ricerche Farmacologiche “Mario Negri”, Milan, Italy bDipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita` di Siena, Siena, Italy Summary Aripiprazole metabolism includes N-dealkylation to 1-(2,3-dichlorophenyl)-piperazine which was present as a minor metabolite in serum of eight schizophrenic outpatients taking 5-15 mg/day. As phenylpiperazines concentrate in the brain, causing serotonin receptor-related effects, the authors examined the compounds’ concentrations in brain of rats given 10 mg/kg aripiprazole dihydrochloride orally, approximately every half-life for five half-lives, and evaluated the metabolite-to-parent drug ratio at steady state. The metabolite had higher brain uptake (about 26) than aripiprazole (about 5) and therefore the metabolite-to-parent drug ratio was higher in brain (0.43 ± 0.07, on molar basis) than in blood (0.08 ± 0.01). However, assuming that the compounds concentrate in human brain to the same extent as in the rat, one can conclude that at the site of action the metabolite represents only about 6% of aripiprazole. It is therefore conceivable that the metabolite contributes to the central effects of aripiprazole for rats, but this is unlikely for patients taking therapeutic doses. Key Words: Aripiprazole; 1-(2,3-dichlorophenyl)-piperazine; brain-to-blood distribution; metabolite-to-parent drug ratio With a pharmacological profile that differs from currently marketed antipsychotics for the treatment of schizophrenia and schizoaffective disorders, aripiprazole is a first-in-class drug. -
Thioxanthene Derivates As Sole Anti-Infective Agents
(19) & (11) EP 2 114 406 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/496 (2006.01) A61P 31/04 (2006.01) 25.05.2011 Bulletin 2011/21 A61P 33/00 (2006.01) (21) Application number: 08700129.3 (86) International application number: PCT/DK2008/000005 (22) Date of filing: 07.01.2008 (87) International publication number: WO 2008/080408 (10.07.2008 Gazette 2008/28) (54) THIOXANTHENE DERIVATESAS SOLEANTI- INFECTIVEAGENTS FORUSE INT HE TREATMENT OF INFECTIOUS DISEASES THIOXANTHEN-DERIVATE ALS ALLEINVERTRETER DER ANTIINFEKTIVA ZUR VERWENDUNG IN DER BEHANDLUNG VON INFEKTIONSKRANKHEITEN DÉRIVÉS DE THIOXANTHÈNE COMME SEULS AGENTS ANTIINFECTIEUX POUR LEUR UTILISATION DANS LE TRAITEMENT DES MALADIES INFECTIEUSES (84) Designated Contracting States: • MORTENSEN I ET AL: "THE ANTIBACTERIAL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR ACTIVITY OF THE HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT PSYCHOPHARMACOLOGICAL AGENT RO SE SI SK TR CLOPENTHIXOL AND ITS TWO MAIN METABOLITES" ACTA PATHOLOGICA (30) Priority: 05.01.2007 PCT/DK2007/000006 MICROBIOLOGICASCANDINAVICA, SECTION B, XX, XX, vol. 95B, no. 6, 1987, pages 355-359, (43) Date of publication of application: XP008066133 ISSN: 0108-0180 11.11.2009 Bulletin 2009/46 • KOCISKO ET AL: "Comparison of protease- resistant prion protein inhibitors in cell cultures (60) Divisional application: infected with two strains of mouse and sheep 10181816.9 / 2 301 545 scrapie" NEUROSCIENCE LETTERS, LIMERICK, IE, vol. 388, no. 2, 11 November 2005 (2005-11-11), (73) Proprietor: BKG Pharma ApS pages 106-111, XP005042190 ISSN: 0304-3940 2920 Charlottenlund (DK) • KAISER C ET AL: "Analogs of phenothiazines. -
A Straightforward Route to Enantiopure Pyrrolizidines And
Molecules 2001, 6, 784-795 molecules ISSN 1420-3049 http://www.mdpi.org Biologically Active 1-Arylpiperazines. Synthesis of New N-(4- Aryl-1-piperazinyl)alkyl Derivatives of Quinazolidin-4(3H)-one, 2,3-Dihydrophthalazine-1,4-dione and 1,2-Dihydropyridazine- 3,6-dione as Potential Serotonin Receptor Ligands Piotr Kowalski1,*, Teresa Kowalska1, Maria J. Mokrosz2, Andrzej J. Bojarski2 and Sijka Charakchieva-Minol2 1 Institute of Organic Chemistry and Technology, Cracow University of Technology, 24 Warszawska str., 31-155 Cracow, Poland; 2 Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna str., 31-343 Cracow, Poland * Author to whom correspondence should be addressed; e-mail: [email protected] Received: 26 February 2001; in revised form: 28 August 2001 / Accepted: 28 August 2001 / Published: 31 August 2001 Abstract: The synthesis of a series of new n-propyl and n-butyl chain containing 1-aryl- piperazine derivatives of quinazolidin-4(3H)-one (7) 2-phenyl-2,3-dihydrophthalazine-1,4- dione (8) and 1-phenyl-1,2-dihydropyridazine-3,6-dione (9) as potential serotonin receptor ligands is described. Keywords: Arylpiperazines, lactams, serotonin receptor ligands. Introduction Early studies by Hibert et al. have shown that there are two basic pharmacophore groups common to all five classes of 5-HT1A receptor ligands: a basic nitrogen atom and an aromatic ring with its centre positioned at a distance of 5.2-5.7 Å [1]. Since then several attempts have been made to extend that model, but the large diversity of ligand structures made definition of general interaction modes Molecules 2001, 6 785 impossible.