An Update the Increasing Popularity of Anabolic Androgenic Steroids
Total Page:16
File Type:pdf, Size:1020Kb
Load more
Recommended publications
-
The Use of Capillary Electrophoresis (CE) in Drug Analysis
Florida International University FIU Digital Commons FIU Electronic Theses and Dissertations University Graduate School 3-28-2005 The use of capillary electrophoresis (CE) in drug analysis Agnes D. Garcia Follow this and additional works at: https://digitalcommons.fiu.edu/etd Part of the Other Life Sciences Commons Recommended Citation Garcia, Agnes D., "The use of capillary electrophoresis (CE) in drug analysis" (2005). FIU Electronic Theses and Dissertations. 3928. https://digitalcommons.fiu.edu/etd/3928 This work is brought to you for free and open access by the University Graduate School at FIU Digital Commons. It has been accepted for inclusion in FIU Electronic Theses and Dissertations by an authorized administrator of FIU Digital Commons. For more information, please contact [email protected]. FLORIDA INTERNATIONAL UNIVERSITY Miami, Florida THE USE OF CAPILLARY ELECTROPHORESIS (CE) IN DRUG ANALYSIS A thesis submitted in partial fulfillment of the requirements for the degree of MASTER OF SCIENCE in FORENSIC SCIENCE by Agnes D. Garcia 2005 To: Dean R. Bruce Dunlap College of Arts and Sciences This thesis, written by Agnes D. Garcia, and entitled The Use of Capillary Electrophoresis (CE) in Drug Analysis, having been approved in respect to style and intellectual content, is referred to you for judgment. We have read this thesis and recommend that it be approved. Kenneth Furton Bruce McCord Jose R. Almirall, Major Professor Date of Defense: March 28,2005 The thesis of Agnes D. Garcia is approved. Dean R. Bruce Dunlap College of Arts and Sciences Dean Douglas Wartzok University Graduate School Florida International University, 2005 ii © Copyright 2005 by Agnes D. -
Download (PDF 277.63
PROJECT REVIEW “Characterization of the main metabolites of 17-methylstenblone and 17 methylmethenolone produced by human hepatocytes and liver fractions” Prof C. Ayotte, (INRS-Institut Armand-Frappier, Canada) New steroids openly appear on the market in products labelled with a rather confusing nomenclature. Once characterized, pharmaceutical grade products not being available, knowledge of the biotransformation pathways essential to an efficient detection of utilization by athletes is difficult to gain since administration to human volunteers should be restricted to the minimum. The alternative is a reliable in vitro model. Human hepatocytes, fresh or cryopreserved are now available commercially. We have successfully produced and identified phase I metabolites from incubations of human hepatocytes with different steroids, such as 17-methyldrostanolone and desoxymethyltestosterone (DMT). The aim of this project is to produce in vitro from human hepatocytes and liver fractions the metabolites of two steroids, the 17-methylated derivatives of stenbolone and its isomer methenolone. The principal metabolites will be synthesized and characterized by NMR and mass spectrometry. The characterization of metabolites will enable the identification of markers of utilization to be incorporated in routine testing methods. The approach for the chemical synthesis of metabolites will be shared with NMI insuring the distribution to other doping control laboratories. Improving the knowledge of steroid biotransformation is a further benefit from these studies. Characterization of 17-Methylstenbolone and 17-Methylmethenolone and Identification of Metabolites Produced by Human Hepatocytes and Liver Fractions WADA Project no. 11A16CA Christiane Ayotte, Philippe Räss, Alexandre Sylvestre, INRS-Institut Armand-Frappier Summary We have synthesized and characterized two designer steroids, 17α-methylmethenolone and 17α- methylstenbolone; the latter is proposed on the internet and two groups have reported different and contradictory results. -
(12) United States Patent (10) Patent No.: US 9,642,912 B2 Kisak Et Al
USOO9642912B2 (12) United States Patent (10) Patent No.: US 9,642,912 B2 Kisak et al. (45) Date of Patent: *May 9, 2017 (54) TOPICAL FORMULATIONS FOR TREATING (58) Field of Classification Search SKIN CONDITIONS CPC ...................................................... A61K 31f S7 (71) Applicant: Crescita Therapeutics Inc., USPC .......................................................... 514/171 Mississauga (CA) See application file for complete search history. (72) Inventors: Edward T. Kisak, San Diego, CA (56) References Cited (US); John M. Newsam, La Jolla, CA (US); Dominic King-Smith, San Diego, U.S. PATENT DOCUMENTS CA (US); Pankaj Karande, Troy, NY (US); Samir Mitragotri, Santa Barbara, 5,602,183 A 2f1997 Martin et al. CA (US); Wade A. Hull, Kaysville, UT 5,648,380 A 7, 1997 Martin 5,874.479 A 2, 1999 Martin (US); Ngoc Truc-ChiVo, Longueuil 6,328,979 B1 12/2001 Yamashita et al. (CA) 7,001,592 B1 2/2006 Traynor et al. 7,795,309 B2 9/2010 Kisak et al. (73) Assignee: Crescita Therapeutics Inc., 8,343,962 B2 1/2013 Kisak et al. Mississauga (CA) 8,513,304 B2 8, 2013 Kisak et al. 8,535,692 B2 9/2013 Pongpeerapat et al. (*) Notice: Subject to any disclaimer, the term of this 9,308,181 B2* 4/2016 Kisak ..................... A61K 47/12 patent is extended or adjusted under 35 2002fOOO6435 A1 1/2002 Samuels et al. 2002fOO64524 A1 5, 2002 Cevc U.S.C. 154(b) by 204 days. 2005, OO 14823 A1 1/2005 Soderlund et al. This patent is Subject to a terminal dis 2005.00754O7 A1 4/2005 Tamarkin et al. -
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. -
Testosterone Art. 31
Annex I List of the names, pharmaceutical forms, strengths of the medicinal products, routes of administration, and marketing authorisation holders in the Member States 1 Member Marketing authorisation INN Invented name Strength Pharmaceutical Route of State holder form administration (in EEA) Austria Bayer Austria GmbH testosterone undecanoat Nebido 1000 mg/4 ml 1000 mg/4ml solution for intramuscular use Herbststrasse 6-10 Injektionslösung injection 1160 Wien Austria Austria Eli Lilly GmbH testosterone Axiron 30 mg/1,5 ml 30 mg/1,5ml gel cutaneous use Kölblgasse 8-10 Lösung zur 1030 Wien Anwendung auf der Austria Haut Austria Laboratoires Besins testosterone Testogel 25 mg - Gel 25 mg gel cutaneous use International SA im Beutel Rue de Bourg lÀbbè 3 75003 Paris France Austria Laboratoires Besins testosterone Testogel 50 mg - Gel 50 mg gel cutaneous use International SA im Beutel Rue de Bourg lÀbbè 3 75003 Paris France Austria ProStrakan Ltd. testosterone Tostran 2% - Gel 0.02 gel cutaneous use Galabank Business Park TD1 1QH Galashiels United Kingdom Austria Laboratoires Besins testosterone Androgel 25 mg - Gel 25 mg gel cutaneous use International SA im Beutel Rue de Bourg lÀbbè 3 75003 Paris France Austria Laboratoires Besins testosterone Androgel 50 mg - Gel 50 mg gel cutaneous use International SA im Beutel Rue de Bourg lÀbbè 3 75003 Paris France Austria N.V. Organon testosterone undecanoat Andriol Testocaps 40 40 mg capsule, soft oral use Kloosterstraat 6 mg - Kapseln 5349 AB Oss The Netherlands 2 Member Marketing authorisation INN Invented name Strength Pharmaceutical Route of State holder form administration (in EEA) Belgium Besins Healthcare testosterone Androgel 25 mg gel transdermal use Avenue Louise 287 1050 Brussels Belgium Belgium Besins Healthcare testosterone Androgel 50 mg gel transdermal use Avenue Louise 287 1050 Brussels Belgium Belgium Eli Lilly Benelux S.A.-N.V. -
New Long-Acting Androgens
World J Urol (2003) 21: 306–310 DOI 10.1007/s00345-003-0364-x TOPIC PAPER Louis J. Gooren New long-acting androgens Received: 16 September 2003 / Accepted: 17 September 2003 / Published online: 9 October 2003 Ó Springer-Verlag 2003 Abstract Testosterone substitution treatment aims to are usually irreversible. The consequence is that life-long replace physiological actions of endogenous testosterone androgen replacement is required. Patient compliance by steadily maintaining physiological blood levels of with life-long androgen replacement depends on conve- testosterone. The underlying conditions rendering nient pharmaceutical formulations ensuring continuity androgen replacement necessary are usually irreversible. of androgen replacement. The benefits of androgen The consequence is that almost life-long androgen replacement therapy are clear, but the delivery of tes- replacement is required. Patient compliance with life- tosterone to hypogonadal men in a way that approxi- long androgen replacement depends on convenient mates normal levels and patterns still poses a therapeutic pharmaceutical formulations ensuring continuity of challenge. Among experts, there is consensus that the androgen replacement. Therefore, they must be conve- major goal of testosterone substitution is ‘‘to replace nient in usage with a relative independence of medical testosterone levels at as close to physiological concen- services. In elderly man, safety of androgen replacement trations as is possible’’ [18]. General agreements about therapy is a concern but in younger subjects (below the such an androgen replacement therapy are (1) a delivery age of 50 years) side effects of androgens are usually of the physiological amount of testosterone (3-10 mg/d); minimal. For them, long-acting testosterone prepara- (2) consistent levels of testosterone, 5a-dihydrotestos- tions are well suited. -
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. -
(19) United States (12) Patent Application Publication (10) Pub
US 20060018934A1 (19) United States (12) Patent Application Publication (10) Pub. N0.: US 2006/0018934 A1 Vaya et al. (43) Pub. Date: Jan. 26, 2006 (54) NOVEL DRUG DELIVERY SYSTEM (30) Foreign Application Priority Data (76) Inventors; Navin Vaya, Gujarat (IN); Rajesh Aug. 5, 2002 (IN) ............................... .. 698/MUM/2002 Singh Karan, Gujarat (IN); Suni] Aug. 5, 2002 (IN) .... .. 696/MUM/2003 Sadanand Nadkarni, Gujarat (IN); Jan. 22, 2003 (IN) ................................. .. 81/MUM/2003 Vinod Kumar Gupta, Gujarat (IN) Publication Classi?cation Correspondence Address: HEDMAN & COSTIGAN RC. (51) Int. Cl. 1185 AVENUE OF THE AMERICAS A61K 9/00 (2006.01) NEW YORK, NY 10036 (US) A61K 9/24 (2006.01) (52) US. Cl. .......................................... .. 424/400; 424/472 (57) ABSTRACT (21) Appl. No.: 11/134,632 A novel modi?ed release dosage form comprising of a high (22) Filed: May 19, 2005 solubility active ingredient, Which utilizes dual retard tech nique to effectively reduce the quantity of release controlling Related US. Application Data agents. Present invention can optionally comprise addition ally another active ingredient as an immediate release form (63) Continuation-in-part of application No. 10/630,348, or modi?ed release form. Present invention also relates to a ?led on Jul. 29, 2003. process for preparing the said formulation. Patent Application Publication Jan. 26, 2006 Sheet 1 0f 5 US 2006/0018934 A1 FIGURE 1 (a) FIGURE 1 (b) Patent Application Publication Jan. 26, 2006 Sheet 2 0f 5 US 2006/0018934 A1 FIGURE 2 120 — (95) 100 80 60 ActiveIngredientRelease 4O - 2O - 0 2 4 6 8 10 12 14 16 18 2O 22 24 Q 26 Time (hour) Patent Application Publication Jan. -
Molecular and Preclinical Pharmacology of Nonsteroidal Androgen Receptor Ligands
Molecular and Preclinical Pharmacology of Nonsteroidal Androgen Receptor Ligands Dissertation Presented in Partial Fulfillment of the Requirements for the Degree Doctor of Philosophy in the Graduate School of The Ohio State University By Amanda Jones, M.S. Graduate Program in Pharmacy The Ohio State University 2010 Dissertation Committee: James T. Dalton, Advisor Thomas D. Schmittgen William L. Hayton Robert W. Brueggemeier Copyright by Amanda Jones 2010 Abstract The androgen receptor (AR) is critical for the growth and development of secondary sexual organs, muscle, bone and other tissues, making it an excellent therapeutic target. Ubiquitous expression of AR impedes the ability of endogenous steroids to function tissue selectively. In addition to the lack of tissue selectivity, clinical use of testosterone is limited due to poor bioavailability and pharmacokinetic problems. Our lab, in the last decade, discovered and developed tissue selective AR modulators (SARMs) that spare androgenic effects in secondary sexual organs, but demonstrate potential to treat muscle wasting diseases. This work reveals the discovery of next generation SARMs to treat prostate cancer and mechanistically characterize a prospective SARM in muscle and central nervous system (CNS). Prostate cancer relies on the AR for its growth, making it the primary therapeutic target in this disease. However, prolonged inhibition, with commercially available AR antagonists, leads to the development of mutations in its ligand binding domain resulting in resistance. Utilizing the crystal structure of AR-wild-type and AR-W741L mutant, we synthesized a series of AR pan- antagonists (that inhibit both wild-type and mutant ARs). Structure activity relationship studies indicate that sulfonyl and amine linkages of the aryl propionamide pharmacophore are important for the antagonist activity. -
(12) Patent Application Publication (10) Pub. No.: US 2007/0078091 A1 Hubler Et Al
US 20070078091A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2007/0078091 A1 Hubler et al. (43) Pub. Date: Apr. 5, 2007 (54) PHARMACEUTICAL COMBINATIONS FOR (30) Foreign Application Priority Data COMPENSATING FORATESTOSTERONE DEFICIENCY IN MEN WHILE Sep. 6, 1998 (DE)..................................... 198 2.55918 SMULTANEOUSLY PROTECTING THE PROSTATE Publication Classification (76) Inventors: Doris Hubler, Schmieden (DE): (51) Int. Cl. Michael Oettel, Jena (DE); Lothar A6II 38/09 (2007.01) Sobek, Jena (DE); Walter Elger, Berlin A 6LX 3/57 (2007.01) (DE); Abdul-Abbas Al-Mudhaffar, A6II 3/56 (2006.01) Jena (DE) A 6LX 3/59 (2007.01) A 6LX 3/57 (2007.01) A61K 31/4709 (2007.01) Correspondence Address: A6II 3L/38 (2007.01) MILLEN, WHITE, ZELANO & BRANGAN, (52) U.S. Cl. ............................ 514/15: 514/171; 514/170; P.C. 514/651; 514/252.16; 514/252.17; 22OO CLARENDON BLVD. 514/3O8 SUTE 14OO ARLINGTON, VA 22201 (US) (57) ABSTRACT This invention relates to pharmaceutical combinations for (21) Appl. No.: 11/517,301 compensating for an absolute and relative testosterone defi ciency in men with simultaneous prophylaxis for the devel opment of a benign prostatic hyperplasia (BPH) or prostate (22) Filed: Sep. 8, 2006 cancer. The combinations according to the invention contain a natural or synthetic androgen in combination with a Related U.S. Application Data gestagen, an antigestagen, an antiestrogen, a GnRH analog. a testosterone-5C.-reductase inhibitor, an O-andreno-receptor (63) Continuation of application No. 09/719,221, filed on blocker or a phosphodiesterase inhibitor. In comparison to Feb. 16, 2001, filed as 371 of international application the combinations according to the invention, any active No. -
Use of High-Temperature Liquid Chromatography with Sub
This article was downloaded by: [Moskow State Univ Bibliote] On: 15 November 2013, At: 02:15 Publisher: Taylor & Francis Informa Ltd Registered in England and Wales Registered Number: 1072954 Registered office: Mortimer House, 37-41 Mortimer Street, London W1T 3JH, UK Journal of Liquid Chromatography & Related Technologies Publication details, including instructions for authors and subscription information: http://www.tandfonline.com/loi/ljlc20 Use of High-Temperature Liquid Chromatography with Sub-2 µm Particle C18 Columns for the Analysis of Seized Drugs Ira Lurie a & Li Li a a Special Testing and Research Laboratory, U.S. Drug Enforcement Administration , Dulles, Virginia, USA Published online: 05 Oct 2009. To cite this article: Ira Lurie & Li Li (2009) Use of High-Temperature Liquid Chromatography with Sub-2 µm Particle C18 Columns for the Analysis of Seized Drugs, Journal of Liquid Chromatography & Related Technologies, 32:18, 2615-2626, DOI: 10.1080/10826070903245516 To link to this article: http://dx.doi.org/10.1080/10826070903245516 PLEASE SCROLL DOWN FOR ARTICLE Taylor & Francis makes every effort to ensure the accuracy of all the information (the “Content”) contained in the publications on our platform. However, Taylor & Francis, our agents, and our licensors make no representations or warranties whatsoever as to the accuracy, completeness, or suitability for any purpose of the Content. Any opinions and views expressed in this publication are the opinions and views of the authors, and are not the views of or endorsed by Taylor & Francis. The accuracy of the Content should not be relied upon and should be independently verified with primary sources of information. -
Chapter 246-883 WAC PHARMACEUTICAL—SALES REQUIRING PRESCRIPTIONS
Chapter 246-883 Chapter 246-883 WAC PHARMACEUTICAL—SALES REQUIRING PRESCRIPTIONS WAC Authority: 1979 1st ex. s. c 139. 79-09-138 (Order 149, Resolution No. 246-883-020 Identification of legend drugs for purposes of chapter 9/79), § 360-32-050, filed 9/5/79.] 69.41 RCW. 246-883-025 Introductory trade or stock packages. 246-883-030 Ephedrine prescription restrictions. WAC246-883-025 246-883-025 Introductory trade or stock pack- 246-883-040 Regulated steroids. 246-883-050 Theophylline prescription restrictions. ages. Introductory trade or stock packages may be distributed by registered drug manufacturers to licensed pharmacies 246-883-020 under the following conditions: WAC 246-883-020 Identification of legend drugs for purposes of chapter 69.41 RCW. (1) In accordance with (1) The package shall be invoiced by the drug manufac- chapter 69.41 RCW, the board of pharmacy finds that those turer as a no charge sale. drugs which have been determined by the Food and Drug (2) The product shall be distributed by the manufacturer Administration, under the Federal Food, Drug and Cosmetic to the pharmacy by mail or common carrier. Act, to require a prescription under federal law should also be (3) The drug's package shall not be marked as a sample classified as legend drugs under state law because of their or with any other labeling that is inconsistent with the claim toxicity or potential for harmful effect, the methods of their that the manufacturer intended the package for sale. use and the collateral safeguards necessary to their use, indi- (4) The manufacturer shall be limited to distributing one cate that they are only safe for use under the supervision of a introductory package of each dosage strength of a product on practitioner.