DOCSLIB.ORG

Technical Commentary

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Technical Commentary TECHNICAL COMMENTARY Metiapine Introduction When multiple copies of reviews were found and/or when findings conflict, we present the First generation ‘typical’ antipsychotics are an most recent version and the most recent older class of antipsychotic than second conclusions. generation ‘atypical’ antipsychotics. They are used primarily to treat positive symptoms Evidence was graded using the Grading of including the experiences of perceptual Recommendations Assessment, Development abnormalities (hallucinations) and fixed, false, and Evaluation (GRADE) Working Group irrational beliefs (delusions). approach where high quality evidence such as that gained from RCTs may be downgraded to First generation antipsychotics may cause side moderate or low if review and study quality is effects which can differ depending on which limited, if there is inconsistency in results, antipsychotic is being administered and on indirect comparisons, imprecise or sparse data individual differences in reaction to the drug. and high probability of reporting bias. It may Reactions may include dyskinesias such as also be downgraded if risks associated with the repetitive, involuntary, and purposeless body or intervention or other matter under review are facial movements, Parkinsonism (cogwheel high. Conversely, low quality evidence such as muscle rigidity, pill-rolling tremor and reduced that gained from observational studies may be or slowed movements), akathisia (motor upgraded if effect sizes are large, there is a restlessness, especially in the legs, and dose dependent response or if results are resembling agitation) and dystonias such as reasonably consistent, precise and direct with muscle contractions causing unusual twisting of low associated risks2. The resulting table parts of the body, most often in the neck. These represents an objective summary of the effects are caused by the dopamine receptor evidence, although the conclusions are solely antagonist action of these drugs. the opinion of staff of NeuRA (Neuroscience This table summarises overall group Research Australia). effectiveness of metiapine from information gained from randomised controlled trials (RCTs). Individual treatment programs need to Results be tailored by trained clinicians as response - both in symptoms and adverse effects - can We found one review that met our inclusion 3 vary between individuals. criteria . Method Owing to the vast number of reviews on antipsychotics, we have included only information reported in the abstracts of Cochrane systematic reviews1. This is because the Cochrane internal review process ensures a high level of scientific rigor and meta-analyses are usually conducted, giving treatment effect sizes. Data from the abstracts were supplemented from the full text when clarification was required. We have included only Cochrane reviews that have been published from the year 2000 to date to ensure the latest available evidence is presented. NeuRA Metiapine October 2020 Margarete Ainsworth Building, Barker Street, Randwick NSW 2031. Phone: 02 9399 1000. Email: [email protected] Page 1 To donate, phone 1800 888 019 or visit www.neura.edu.au/donate/schizophrenia TECHNICAL COMMENTARY Metiapine Metiapine Compared to first generation antipsychotics Efficacy: Moderate to low quality evidence (small samples, consistent, imprecise, direct) suggests no differences between chlorpromazine and metiapine in clinical improvement. Adverse effects: Moderate to low quality evidence finds no differences between chlorpromazine and metiapine in rates of parkinsonism. Zare M, Bazrafshan A. Chlorpromazine versus metiapine for schizophrenia. Cochrane Database of Systematic Reviews 2017, 3: CD011655. No difference between chlorpromazine and metiapine in clinically important improvement; 2 RCTs, N = 120, RR = 1.11, 95%CI 0.84 to 1.47, I2 = 8%, p = 0.30 Risks No difference in rate of parkinsonism; 2 RCTs, n = 70, RR = 0.97, 95%CI 0.46 to 2.03, I2 = 53%, p = 0.14 Consistency in results‡ Consistent Precision in results§ Imprecise Directness of results║ Direct Explanation of acronyms CI = confidence interval, I² = the percentage of the variability in effect estimates that is due to heterogeneity rather than sampling error (chance), N = number of participants, p = statistical probability of obtaining that result (p < 0.05 generally regarded as significant, RCT = randomised controlled trial, RR = relative risk NeuRA Metiapine October 2020 Margarete Ainsworth Building, Barker Street, Randwick NSW 2031. Phone: 02 9399 1000. Email: [email protected] Page 2 To donate, phone 1800 888 019 or visit www.neura.edu.au/donate/schizophrenia TECHNICAL COMMENTARY Metiapine Explanation of technical terms prediction, but do not confirm causality due to possible and often unforseen confounding † Different effect measures are reported by variables. An r of 0.10 represents a weak different reviews. association, 0.25 a medium association and 0.40 and over represents a strong Weighted mean difference scores refer to association. Unstandardised (b) regression mean differences between treatment and coefficients indicate the average change in comparison groups after treatment (or the dependent variable associated with a 1 occasionally pre to post treatment) and in a unit change in the independent variable, randomized trial there is an assumption that statistically controlling for the other both groups are comparable on this measure independent variables. Standardised prior to treatment. Standardised mean regression coefficients represent the change differences are divided by the pooled being in units of standard deviations to allow standard deviation (or the standard deviation comparison across different scales. of one group when groups are homogenous) which allows results from different scales to be combined and compared. Each study’s mean difference is then given a weighting ‡ Inconsistency refers to differing estimates depending on the size of the sample and the of effect across studies (i.e. heterogeneity or variability in the data. 0.2 represents a small variability in results) that effect, 0.5 a medium effect, and 0.8 and over is not explained by subgroup analyses and represents a large effect1. therefore reduces confidence in the effect Odds ratio (OR) or relative risk (RR) refers to estimate. I² is the percentage of the variability the probability of a reduction (< 1) or an in effect estimates that is due to heterogeneity increase (> 1) in a particular outcome in a rather than sampling error (chance) - 0% to treatment group, or a group exposed to a risk 40%: heterogeneity might not be important, factor, relative to the comparison group. For 30% to 60%: may represent moderate example, a RR of 0.75 translates to a heterogeneity, 50% to 90%: may represent reduction in risk of an outcome of 25% considerable heterogeneity and over this is relative to those not receiving the treatment or considerable heterogeneity. I² can be not exposed to the risk factor. Conversely, a calculated from Q (chi-square) for the test of RR of 1.25 translates to an increased risk of heterogeneity with the following formula1; 25% relative to those not receiving treatment or not having been exposed to a risk factor. A RR or OR of 1.00 means there is no difference between groups. A medium effect is considered if RR > 2 or < 0.5 and a large effect if RR > 5 or < 0.24. lnOR stands for logarithmic OR where a lnOR of 0 shows no § Imprecision refers to wide confidence difference between groups. Hazard ratios intervals indicating a lack of confidence in the measure the effect of an explanatory variable effect estimate. Based on GRADE on the hazard or risk of an event. recommendations, a result for continuous data (standardised mean differences, not Correlation coefficients (eg, r) indicate the weighted mean differences) is considered strength of association or relationship imprecise if the upper or lower confidence between variables. They are an indication of limit crosses an effect size of 0.5 in either NeuRA Metiapine October 2020 Margarete Ainsworth Building, Barker Street, Randwick NSW 2031. Phone: 02 9399 1000. Email: [email protected] Page 3 To donate, phone 1800 888 019 or visit www.neura.edu.au/donate/schizophrenia TECHNICAL COMMENTARY Metiapine direction, and for binary and correlation data, an effect size of 0.25. GRADE also recommends downgrading the evidence when sample size is smaller than 300 (for binary data) and 400 (for continuous data), although for some topics, these criteria should be relaxed5. ║ Indirectness of comparison occurs when a comparison of intervention A versus B is not available but A was compared with C and B was compared with C, which allows indirect comparisons of the magnitude of effect of A versus B. Indirectness of population, comparator and/or outcome can also occur when the available evidence regarding a particular population, intervention, comparator, or outcome is not available and is therefore inferred from available evidence. These inferred treatment effect sizes are of lower quality than those gained from head-to- head comparisons of A and B. NeuRA Metiapine October 2020 Margarete Ainsworth Building, Barker Street, Randwick NSW 2031. Phone: 02 9399 1000. Email: [email protected] Page 4 To donate, phone 1800 888 019 or visit www.neura.edu.au/donate/schizophrenia TECHNICAL COMMENTARY Metiapine References 1. CochraneCollaboration (2008): Cochrane Handbook for Systematic Reviews of Interventions. Accessed 24/06/2011. 2. GRADEWorkingGroup (2004): Grading quality of evidence and strength of recommendations. British Medical Journal 328: 1490. 3. Zare M, Bazrafshan A (2017): Chlorpromazine versus metiapine for schizophrenia. Cochrane Database of Systematic Reviews 3: CD011655. 4. Rosenthal JA (1996): Qualitative Descriptors of Strength of Association and Effect Size. Journal of Social Service Research 21: 37-59. 5. GRADEpro (2008): [Computer program]. Jan Brozek, Andrew Oxman, Holger Schünemann. Version 32 for Windows NeuRA Metiapine October 2020 Margarete Ainsworth Building, Barker Street, Randwick NSW 2031. Phone: 02 9399 1000. Email: [email protected] Page 5 To donate, phone 1800 888 019 or visit www.neura.edu.au/donate/schizophrenia .
Load more

Recommended publications
  • (12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe Et Al
    US 2011 01 05536A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe et al. (43) Pub. Date: May 5, 2011 (54) DOSING REGIMENASSOCATED WITH Publication Classification LONG-ACTING INUECTABLE PALIPERDONE ESTERS (51) Int. Cl. A 6LX 3/59 (2006.01) (76) Inventors: Peter H. Lewyn-Briscoe, A6IP 25/18 (2006.01) Newtown, PA (US); Cristiana Gassmann-Mayer, Pennington, NJ (US); Srihari Gopal, Belle Meade, (52) U.S. Cl. ................................................... S14/259.41 NJ (US); David W. Hough, Wallingford, PA (US); Bart M.M. Remmerie, Gent (BE); Mahesh N. (57) ABSTRACT Samtani, Flemington, NJ (US) The present application provides a method for treating (21) Appl. No.: 12/916,910 patients in need of psychiatric treatment, wherein said patient (22) Filed: Nov. 1, 2010 misses a stabilized dose of a monthly maintenance regimen of paliperidone palmitate. The present application also provides Related U.S. Application Data a method for treating psychiatric patients in need of a Switch (60) Provisional application No. 61/256,696, filed on Oct. ing treatment to paliperidone palmitate in a Sustained release 30, 2009. formulation. Patent Application Publication May 5, 2011 Sheet 1 of 6 US 2011/O105536 A1 FIG. 1 First-Order PrOCeSS Cp V CL Central (2) Zero-Order PrOCeSS Patent Application Publication May 5, 2011 Sheet 2 of 6 US 2011/O105536 A1 FIG. 2 25mgeq 50mgeq m-100mde::::: Missed doSe On WK 4. Patient returns On WK5 Missed doSe On WK 4. Patient returns On WK 6 -8-4 O 4 8 12 16 2024 -8-4 O 4 8 12 1620 24 Missed doSe On WK 4.
    [Show full text]
  • Known Active Compounds Used in This Article
    Known active compounds used in this article As COX-2 active compounds, 12 inhibitors and 2 natural ligands were selected. The two natural ligands were arachidonic acid and prostaglandin H2. The 12 inhibitors were diclofenac, etodolac, suprofen, diflunisal, piroxicam, sulindac, indomethacin, ketoprofen, naproxen, nimesulide, rofecoxib, and 1-phenylsulfonamide-3-trifluoromethyl-5-parabromophenylpyrazole. The names of the thermolysin inhibitors used in the present study are as follows, with the PDB code in parentheses representing the complex structure from which the compound originated: l-benzylsuccinate (1hyt), phenylalanine phosphinic acid - deamino-methyl-phenylalanine (1os0), (6-methyl-3,4-dihydro-2H-chromen-2-Yl) methylphosphonate (1pe5), 2-(4-methylphenoxy) ethylphosphonate - 3-methylbutan-1-amine (1pe7), 2-ethoxyethylphosphonate - 3-methylbutan-1-amine (1pe8), (2-sulfanyl-3-phenylpropanoyl)-Phe-Tyr (1qf0), [2(R,S)-2-sulfanylheptanoyl]-Phe-Ala (1qf1), [(2S)-2-sulfanyl-3-phenylpropanoyl]-Gly-(5-phenylproline) (1qf2), n-(1-(2(R, S)-carboxy-4-phenylbutyl) cyclopentylcarbonyl)- (S)-tryptophan (1thl), (R)-retrothiorphan (1z9g), (S)-thiorphan (1zdp), hydroxamic acid (4tln), phenylalanine phosphinic acid (4tmn), Honh-benzylmalonyl-L-alanylglycine-P-nitroanilide (5tln), 1 Cbz-GlyP-Leu-Leu (ZgPLl) (5tmn), Cbz-GlyP-(O)-Leu-Leu (ZgP(O)Ll) (6tmn), CH2CO(N-OH)Leu-OCH3 (7tln), benzyloxycarbonyl-D-Ala (1kto), benzyloxycarbonyl-L-Ala (1kl6), benzyloxycarbonyl-D-Thr (1kro), benzyloxycarbonyl-L-Thr (1kj0), benzyloxycarbonyl-D-Asp (1ks7), benzyloxycarbonyl-L-Asp
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 8,138,169 B2 Oronsky Et Al
    USOO8138169B2 (12) United States Patent (10) Patent No.: US 8,138,169 B2 Oronsky et al. (45) Date of Patent: Mar. 20, 2012 (54) COMBINATION THERAPY FOR BIPOLAR 6,863,901 B2 3/2005 Hirsh et al. 7,201.920 B2 4/2007 Kumar et al. DSORDER 2007/0213394 A1 9/2007 Beguin et al. (75) Inventors: Bryan T. Oronsky, Los Altos Hills, CA FOREIGN PATENT DOCUMENTS (US); Neil C. Oronsky, Los Altos Hills, WO WO-200806691.6 A1 6, 2008 CA (US) OTHER PUBLICATIONS (73) Assignee: ComgenRx, Inc., Mountain View, CA Boothby et al. Buprenorphine for the treatment of opioid depen (US) dence. American Journal of Health-System Pharamcy, 2007, 64 (3), pp. 266-272, abstract.* (*) Notice: Subject to any disclaimer, the term of this Brown, et al., “Naltrexone in Patients with Bipolar Disorder and patent is extended or adjusted under 35 Alcohol Dependence.” Depression and Anxiety, 2006, vol. 23, No. 8, pp. 492-495. U.S.C. 154(b) by 424 days. Carlezon, et al., “Kappa-Opioid Ligands in the Study and Treatment of Mood Disorders.” Pharmacology and Therapeutics, (21) Appl. No.: 12/422,156 XP002548302, Sep. 2009, vol. 123, No. 3, pp. 334-343. International Search Report and Written Opinion mailed on Jan. 25. (22) Filed: Apr. 10, 2009 2010, for PCT Application No. PCT/US2009/040272, 17 pages. Kamin, et al., “Extrapyramidal Side Effects in the Psychiatric Emer (65) Prior Publication Data gency Service.” Psychiatric Service, Mar. 2000, vol. 51, No. 3, pp. US 2009/0311347 A1 Dec. 17, 2009 287-289. Levin, et al., "Bipolar Disorder and Substance abuse.” Biological Psychiatry, XP004649079, vol.
    [Show full text]
  • 1 PUBLICATIONS Barry Blackwell ARTICLES
    Profiles (Publications) December 4, 2014 PUBLICATIONS Barry Blackwell ARTICLES: 1. Blackwell, B.: Why Patients Come to a Casualty Department. Lancet. (1962), 1:369. 2. Blackwell, B.: Acute Leukemia Presenting as a Lump in the Breast. British Journal of Surgery. (1963), 225:769-771. 3. Lehmann, H., Liddell, J., Blackwell, B., O’Connor, D.C., Daws, A.V.: Two Further Serum Pseudocholinesterase Phenotypes as Causes of Suxamethonium Apnoea. British Medical Journal. (1963), 1:1116-1118. 4. Blackwell, B.: Hypertensive Crisis Due to MAOI. Lancet. (1963), 2:849-851. 5. Blackwell, B.: Munchausen at Guy’s. Guy’s Hospital Reports. (1963), 114 (3):257-277. 6. Blackwell, B.: The Management of Barbituate Overdose in Nonspecialized Units. British Journal of Clinical Practice. (1964), 18 (3):135-144. 7. Blackwell, B., Mallett, B.L.: Psychiatric Illness in a Casualty Department. Guy’s Hospital Reports. (1964), 113:123-130. 8. Blackwell, B., Marley, E.: Interaction Between Cheese and MAOI in Rats and Cats. Lancet. (1964), 1:530-531. 9. Blackwell, B., Davis, B.: Psychiatric Aspects of Myclonus Epilepsy. British Journal of Clinical Practice. (1964), 18 (9):513-516. 10. Palmai, G., Blackwell, B.: The Diurnal Pattern of Salivary Flow in Normal and Depressed Patients. British Journal of Psychiatry. (1965), 111:334-338. 11. Blackwell, B., Mabbitt, L.A.: Tyramine in Cheese Related to Hypertensive Crisis after MAOI. Lancet. (1965), 1:938-940. 12. Blackwell, B., Marley, E., Mabbitt, L.A.: Effects of Yeast Extract after MAOI. Lancet. (1965), 1:940-943. 13. Blackwell, B.: The Simplified Management of Barbituate Overdose. International Medical Digest. (1966), 1:41.
    [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]
  • Fluphenazine Decanoate (Timing of Administration) for People with Schizophrenia (Protocol)
    Cochrane Database of Systematic Reviews Fluphenazine decanoate (timing of administration) for people with schizophrenia (Protocol) Abbas F, Rajab T, Alsamarrai O, Alhalabi N, Zaher Addeen S, Mheish O, Aljojo A, Essali A Abbas F, Rajab T, Alsamarrai O, Alhalabi N, Zaher Addeen S, Mheish O, Aljojo A, Essali A. Fluphenazine decanoate (timing of administration) for people with schizophrenia. Cochrane Database of Systematic Reviews 2017, Issue 10. Art. No.: CD012810. DOI: 10.1002/14651858.CD012810. www.cochranelibrary.com Fluphenazine decanoate (timing of administration) for people with schizophrenia (Protocol) Copyright © 2017 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. TABLE OF CONTENTS HEADER....................................... 1 ABSTRACT ...................................... 1 BACKGROUND .................................... 1 Figure1. ..................................... 3 OBJECTIVES ..................................... 4 METHODS ...................................... 4 ACKNOWLEDGEMENTS . 11 REFERENCES ..................................... 11 CONTRIBUTIONSOFAUTHORS . 14 DECLARATIONSOFINTEREST . 14 SOURCESOFSUPPORT . 15 Fluphenazine decanoate (timing of administration) for people with schizophrenia (Protocol) i Copyright © 2017 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. [Intervention Protocol] Fluphenazine decanoate (timing of administration) for people with schizophrenia Fatima Abbas1, Tawfik Rajab1, Omar Alsamarrai1, Nawras Alhalabi2, Sarah Zaher Addeen1, Oubadah Mheish1, Aisha Aljojo3,
    [Show full text]
  • The Organic Chemistry of Drug Synthesis
    The Organic Chemistry of Drug Synthesis VOLUME 2 DANIEL LEDNICER Mead Johnson and Company Evansville, Indiana LESTER A. MITSCHER The University of Kansas School of Pharmacy Department of Medicinal Chemistry Lawrence, Kansas A WILEY-INTERSCIENCE PUBLICATION JOHN WILEY AND SONS, New York • Chichester • Brisbane • Toronto Copyright © 1980 by John Wiley & Sons, Inc. All rights reserved. Published simultaneously in Canada. Reproduction or translation of any part of this work beyond that permitted by Sections 107 or 108 of the 1976 United States Copyright Act without the permission of the copyright owner is unlawful. Requests for permission or further information should be addressed to the Permissions Department, John Wiley & Sons, Inc. Library of Congress Cataloging in Publication Data: Lednicer, Daniel, 1929- The organic chemistry of drug synthesis. "A Wiley-lnterscience publication." 1. Chemistry, Medical and pharmaceutical. 2. Drugs. 3. Chemistry, Organic. I. Mitscher, Lester A., joint author. II. Title. RS421 .L423 615M 91 76-28387 ISBN 0-471-04392-3 Printed in the United States of America 10 987654321 It is our pleasure again to dedicate a book to our helpmeets: Beryle and Betty. "Has it ever occurred to you that medicinal chemists are just like compulsive gamblers: the next compound will be the real winner." R. L. Clark at the 16th National Medicinal Chemistry Symposium, June, 1978. vii Preface The reception accorded "Organic Chemistry of Drug Synthesis11 seems to us to indicate widespread interest in the organic chemistry involved in the search for new pharmaceutical agents. We are only too aware of the fact that the book deals with a limited segment of the field; the earlier volume cannot be considered either comprehensive or completely up to date.
    [Show full text]
  • Pharmaceutical Appendix to the Tariff Schedule 2
    Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9
    [Show full text]
  • The Organic Chemistry of Drug Synthesis
    THE ORGANIC CHEMISTRY OF DRUG SYNTHESIS VOLUME 3 DANIEL LEDNICER Analytical Bio-Chemistry Laboratories, Inc. Columbia, Missouri LESTER A. MITSCHER The University of Kansas School of Pharmacy Department of Medicinal Chemistry Lawrence, Kansas A WILEY-INTERSCIENCE PUBLICATION JOHN WILEY AND SONS New York • Chlchester • Brisbane * Toronto • Singapore Copyright © 1984 by John Wiley & Sons, Inc. All rights reserved. Published simultaneously in Canada. Reproduction or translation of any part of this work beyond that permitted by Section 107 or 108 of the 1976 United States Copyright Act without the permission of the copyright owner is unlawful. Requests for permission or further information should be addressed to the Permissions Department, John Wiley & Sons, Inc. Library of Congress Cataloging In Publication Data: (Revised for volume 3) Lednicer, Daniel, 1929- The organic chemistry of drug synthesis. "A Wiley-lnterscience publication." Includes bibliographical references and index. 1. Chemistry, Pharmaceutical. 2. Drugs. 3. Chemistry, Organic—Synthesis. I. Mitscher, Lester A., joint author. II. Title. [DNLM 1. Chemistry, Organic. 2. Chemistry, Pharmaceutical. 3. Drugs—Chemical synthesis. QV 744 L473o 1977] RS403.L38 615M9 76-28387 ISBN 0-471-09250-9 (v. 3) Printed in the United States of America 10 907654321 With great pleasure we dedicate this book, too, to our wives, Beryle and Betty. The great tragedy of Science is the slaying of a beautiful hypothesis by an ugly fact. Thomas H. Huxley, "Biogenesis and Abiogenisis" Preface Ihe first volume in this series represented the launching of a trial balloon on the part of the authors. In the first place, wo were not entirely convinced that contemporary medicinal (hemistry could in fact be organized coherently on the basis of organic chemistry.
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 6,197,764 B1 Bradley Et Al
    USOO6197764B1 (12) United States Patent (10) Patent No.: US 6,197,764 B1 Bradley et al. (45) Date of Patent: *Mar. 6, 2001 (54) CLOZAPINE COMPOSITIONS AND USES FOREIGN PATENT DOCUMENTS THEREOF 0599 576A1 1/1994 (EP). (75) Inventors: Matthews O. Bradley, Laytonsville, 693498 1/1996 (EP). MD (US); Victor E. Shashoua, 61204136 11/1984 (JP). Belmont, MA (US); Charles S. 06-072868 3/1994 (JP). Swindell, Merion; Nigel L. Webb, 6072868 3/1994 (JP). Bryn Mawr, both of PA (US) 7082146 3/1996 (JP). 8151334 6/1996 (JP). (73) Assignee: Protarga, Inc., Conshohocken, PA (US) 9030963 2/1997 (JP). (*) Notice: Subject to any disclaimer, the term of this WO 89/07938 9/1989 (WO). patent is extended or adjusted under 35 WO 96/04001 2/1996 (WO). U.S.C. 154(b) by 0 days. WO 96/22303 7/1996 (WO). WO 96/27380 9/1996 (WO). This patent is Subject to a terminal dis WO98/17325 4/1998 (WO). claimer. OTHER PUBLICATIONS (21) Appl. No.: 08/978,541 (22) Filed: Nov. 26, 1997 Bourat, et al., "Long Chain Esters of Pipotiazine as Lon g-Acting Psychotropic Pro-Drug, Med. Chem. Proc. Int. (51) Int. Cl. .............................................. A61K 31/00 Symp. 5th (1976) pp. 105-114. (52) U.S. Cl. ........................... 514/218; 514/219; 514/220 Lohr, et al., “Neuroleptic-Induced Movement Disorders . (58) Field of Search ..................................... 514/218, 219, ..", Psychiatry, vol. 3, (1989). 514/220 Makino, et al., Chemical Abstracts, vol. 106, No. 12, (56) References Cited (90.177x) issued Mar. 23, 1987, “Pharmaceuticals Permeable to Blood-Brain Barrier'.
    [Show full text]
  • Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
    20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0
    [Show full text]
  • Stembook 2018.Pdf
    The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data.
    [Show full text]