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A Simple Toxicological Analysis of Anabolic Steroid Preparations from the Black Market
Ann Toxicol Anal. 2012; 24(2): 67-72 Available online at: c Société Française de Toxicologie Analytique 2012 www.ata-journal.org DOI: 10.1051/ata/2012011 Original article / Article original A simple toxicological analysis of anabolic steroid preparations from the black market Analyse toxicologique simple de stéroïdiens anabolisants provenant de marchés parallèles Manuela Pellegrini, Maria Concetta Rotolo, Rita Di Giovannadrea, Roberta Pacifici, Simona Pichini Department of Therapeutic Research and Medicine Evaluation, Istituto Superiore di Sanità, Via le Regina Elena 299, 00161 Rome, Italy Abstract – Objectives: A simple and rapid gas chromatography (GC) method with mass spectrometry (MS) detection was developed for the identification and quantification of anabolic steroids in pharmaceutical preparations from the black market. Material and Methods: After a liquid-liquid extraction of pharmaceutical products at acidic, neutral and basic pH with chloroform-isopropanol (9:1, v/v), the different steroids were separated by fused silica capillary column and detected by electron impact (EI)-MS in positive ionization mode. Results and Conclusion: The assay was validated in the range from 10 mg to 250 mg/g powder preparations and 0.02 mg to 200 mg/mL liquid preparations with good determination coefficients (r2 0.99) for the calibration curves. At three concentrations spanning the linear dynamic ranges of the calibration curves, mean recoveries were always higher than 90% and intra-assay and inter-assay precision and accuracy were always better than 15%. This method was successfully applied to the analysis of 15 pharmaceutical preparations sold by illegal sources. In only two cases the content was the one reported on the labels.
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Effects of Androgenic-Anabolic Steroids on Apolipoproteins and Lipoprotein (A) F Hartgens, G Rietjens, H a Keizer, H Kuipers, B H R Wolffenbuttel
253 Br J Sports Med: first published as 10.1136/bjsm.2003.000199 on 21 May 2004. Downloaded from ORIGINAL ARTICLE Effects of androgenic-anabolic steroids on apolipoproteins and lipoprotein (a) F Hartgens, G Rietjens, H A Keizer, H Kuipers, B H R Wolffenbuttel ............................................................................................................................... Br J Sports Med 2004;38:253–259. doi: 10.1136/bjsm.2003.000199 Objectives: To investigate the effects of two different regimens of androgenic-anabolic steroid (AAS) administration on serum lipid and lipoproteins, and recovery of these variables after drug cessation, as indicators of the risk for cardiovascular disease in healthy male strength athletes. Methods: In a non-blinded study (study 1) serum lipoproteins and lipids were assessed in 19 subjects who self administered AASs for eight or 14 weeks, and in 16 non-using volunteers. In a randomised double blind, placebo controlled design, the effects of intramuscular administration of nandrolone decanoate (200 mg/week) for eight weeks on the same variables in 16 bodybuilders were studied (study 2). Fasting serum concentrations of total cholesterol, triglycerides, HDL-cholesterol (HDL-C), HDL2-cholesterol (HDL2- C), HDL3-cholesterol (HDL3-C), apolipoprotein A1 (Apo-A1), apolipoprotein B (Apo-B), and lipoprotein (a) (Lp(a)) were determined. Results: In study 1 AAS administration led to decreases in serum concentrations of HDL-C (from 1.08 (0.30) to 0.43 (0.22) mmol/l), HDL2-C (from 0.21 (0.18) to 0.05 (0.03) mmol/l), HDL3-C (from 0.87 (0.24) to 0.40 (0.20) mmol/l, and Apo-A1 (from 1.41 (0.27) to 0.71 (0.34) g/l), whereas Apo-B increased from 0.96 (0.13) to 1.32 (0.28) g/l.
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Part I Biopharmaceuticals
1 Part I Biopharmaceuticals Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 3 1 Analogs and Antagonists of Male Sex Hormones Robert W. Brueggemeier The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus, Ohio 43210, USA 1Introduction6 2 Historical 6 3 Endogenous Male Sex Hormones 7 3.1 Occurrence and Physiological Roles 7 3.2 Biosynthesis 8 3.3 Absorption and Distribution 12 3.4 Metabolism 13 3.4.1 Reductive Metabolism 14 3.4.2 Oxidative Metabolism 17 3.5 Mechanism of Action 19 4 Synthetic Androgens 24 4.1 Current Drugs on the Market 24 4.2 Therapeutic Uses and Bioassays 25 4.3 Structure–Activity Relationships for Steroidal Androgens 26 4.3.1 Early Modiﬁcations 26 4.3.2 Methylated Derivatives 26 4.3.3 Ester Derivatives 27 4.3.4 Halo Derivatives 27 4.3.5 Other Androgen Derivatives 28 4.3.6 Summary of Structure–Activity Relationships of Steroidal Androgens 28 4.4 Nonsteroidal Androgens, Selective Androgen Receptor Modulators (SARMs) 30 4.5 Absorption, Distribution, and Metabolism 31 4.6 Toxicities 32 Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 4 Analogs and Antagonists of Male Sex Hormones 5 Anabolic Agents 32 5.1 Current Drugs on the Market 32 5.2 Therapeutic Uses and Bioassays
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(12) Patent Application Publication (10) Pub. No.: US 2014/0296.191 A1 PATEL Et Al
US 20140296.191A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0296.191 A1 PATEL et al. (43) Pub. Date: Oct. 2, 2014 (54) COMPOSITIONS OF PHARMACEUTICAL (52) U.S. Cl. ACTIVES CONTAINING DETHYLENE CPC ............... A61K 47/10 (2013.01); A61 K9/0019 GLYCOL MONOETHYLETHER OR OTHER (2013.01); A61 K9/0048 (2013.01); A61 K ALKYL DERVATIVES 45/06 (2013.01) USPC ........... 514/167: 514/177; 514/178: 514/450; (71) Applicant: THEMIS MEDICARE LIMITED, 514/334: 514/226.5: 514/449; 514/338; Mumbai (IN) 514/256; 514/570; 514/179; 514/174: 514/533; (72) Inventors: Dinesh Shantilal PATEL, Mumbai (IN); 514/629; 514/619 Sachin Dinesh PATEL, Mumbai (IN); Shashikant Prabhudas KURANI, Mumbai (IN); Madhavlal Govindlal (57) ABSTRACT PATEL, Mumbai (IN) (73) Assignee: THEMIS MEDICARE LIMITED, The present invention relates to pharmaceutical compositions Mumbai (IN) of various pharmaceutical actives, especially lyophilic and hydrophilic actives containing Diethylene glycol monoethyl (21) Appl. No.: 14/242,973 ether or other alkyl derivatives thereofas a primary vehicle and/or to pharmaceutical compositions utilizing Diethylene (22) Filed: Apr. 2, 2014 glycol monoethyl ether or other alkyl derivatives thereofas a primary vehicle or as a solvent system in preparation of Such (30) Foreign Application Priority Data pharmaceutical compositions. The pharmaceutical composi Apr. 2, 2013 (IN) ......................... 1287/MUMA2013 tions of the present invention are safe, non-toxic, exhibits enhanced physical stability compared to conventional formu Publication Classification lations containing such pharmaceutical actives and are Suit able for use as injectables for intravenous and intramuscular (51) Int. Cl. administration, as well as for use as a preformed solution/ A647/ (2006.01) liquid for filling in and preparation of capsules, tablets, nasal A6 IK 45/06 (2006.01) sprays, gargles, dermal applications, gels, topicals, liquid oral A6 IK9/00 (2006.01) dosage forms and other dosage forms.
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Influence of the Anabolic-Androgenic Steroid Nandrolone on Cannabinoid
Neuropharmacology 50 (2006) 788e806 www.elsevier.com/locate/neuropharm Influence of the anabolic-androgenic steroid nandrolone on cannabinoid dependence Evelyne Ce´le´rier a, Therese Ahdepil b, Helena Wikander b, Fernando Berrendero a, Fred Nyberg b, Rafael Maldonado a,* a Laboratori of Neurofarmacologia, Facultat de Cieńcies de la Salut i de la Vida, Universitat Pompeu Fabra, C/Doctor Aiguader 80, 08003 Barcelona, Spain b Department of Pharmaceutical Biosciences, University of Uppsala, Box 591 Biomedicum, S751 24 Uppsala, Sweden Received 8 April 2005; received in revised form 29 November 2005; accepted 29 November 2005 Abstract The identification of the possible factors that might enhance the risk of developing drug addiction and related motivational disorders is crucial to reduce the prevalence of these problems. Here, we examined in mice whether the exposure to the anabolic-androgenic steroid nandrolone would affect the pharmacological and motivational effects induced by D9-tetrahydrocannabinol (THC), the principal psychoactive component of Cannabis sativa. Mice received nandrolone using pre-exposure (during 14 days before THC treatment) or co-administration (1 h before each THC injection) procedures. Both nandrolone treatments did not modify the acute antinociceptive, hypothermic and hypolocomotor effects of THC or the development of tolerance after chronic THC administration. Nandrolone pre-exposure blocked THC- and food-induced condi- tioned place preference and increased the somatic manifestations of THC withdrawal precipitated by the CB1 cannabinoid antagonist rimona- bant (SR141617A). The aversive effects of THC were not changed by nandrolone. Furthermore, nandrolone pre-exposure attenuated the anxiolytic-like effects of a low dose of THC without altering the anxiogenic-like effects of a high dose in the lit/dark box, open field and elevated plus-maze.
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Chemical Muscle Enhancement (The BDR) by Author L
Chemical Muscle Enhancement (The BDR) By Author L. Rea TABLE OF CONTENTS 1. AAS INTRODUCTION ..PG’S 1-12 WARNING: READ FIRST OVER 20 YEARS AGO... WHY STEROIDS AND WHAT IS POSSIBLE? WHAT ARE STEROIDS? FEMALE HORMONE SYNTHESIS MALE HORMONE SYNTHESIS TESTOSTERONE... WHAT DOES IT DO? STEROIDS INCREASE PC SYNTHESIS STEROIDS EFFECT BLOOD VOLUME WHAT HAPPENS AFTER TESTOSTERONE MOLECULES LEAVE RECEPTORS? STEROIDS...GROWTH ON THE CELULAR LEVEL 2. DRUG REFERENCES AND DESCRIPTIONS..PG 12 ORAL ANABOLIC / ANDROGENIC STEROIDS..PG’S 13-30 INJECTABLE ANABOLIC / ANDROGENIC STEROIDS..PG’S 31-45 TESTOSTERONE AND ITS ESTERS..PG’S 45-61 NORTESTOSTERONE (NANDROLONE) AND ITS ESTER..PG’S 62-70 TRENBOLONE AND DERIVATIVES..PG’S 71-78 ESTROGEN CONTROL AND HPTA REGENERATION DRUGS..PG’S 79-94 DIURETICS..PG’S 95-102 THYROID HORMONES ..PG’S 103-116 NON-AAS GROWTH FACTORS AND RELATED SUBSTANCES..PG’S 117-141 OTHER SUBSTANCES..PG’S 142-152 3. REPORTED CYCLES AND EFFECTS.. (Introduction) PG’S 153-159 REPORTED CYCLES AND EFFECTS EXAMPLES (MALE)...PG’S 160-169 REPORTED CYCLES AND EFFECTS EXAMPLES (FEMALE)...PG’S 170-174 REPORTED ADVANCED CYCLES AND EFFECTS-BLITZ CYCLES..PG’S 175-200 (More Reported Cycles and Effects) 4. NUTRITION..PG’S..201-211 5. SUPPLEMENTAL CREATINE..PG’S 212-216 6. REFERENCES AND AVAILABLE LITERATURE..PG’S 217-223 All Rights Reserved CHEMICAL MUSCLE ENHANCEMENT (The Report) and BODYBUILDERS DESK REFERENCE COPYRIGHT ©2002 by AUTHOR L. REA No part of this book may be reproduced or transmitted in any form or by any means, electronic or mechanical including photocopy, recording, or by any information storage and retrieval system, without the permission in writing of the author and publisher.
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A20-0767), As Follows:
05/05/20 03:02 pm HOUSE RESEARCH JD/RK H2711A8 1.1 .................... moves to amend H.F. No. 2711, the delete everything amendment 1.2 (A20-0767), as follows: 1.3 Page 21, delete section 1 1.4 Page 36, delete section 2 1.5 Page 40, delete section 3 and insert: 1.6 "Section 1. Minnesota Statutes 2018, section 152.02, subdivision 2, is amended to read: 1.7 Subd. 2. Schedule I. (a) Schedule I consists of the substances listed in this subdivision. 1.8 (b) Opiates. Unless specifically excepted or unless listed in another schedule, any of the 1.9 following substances, including their analogs, isomers, esters, ethers, salts, and salts of 1.10 isomers, esters, and ethers, whenever the existence of the analogs, isomers, esters, ethers, 1.11 and salts is possible: 1.12 (1) acetylmethadol; 1.13 (2) allylprodine; 1.14 (3) alphacetylmethadol (except levo-alphacetylmethadol, also known as levomethadyl 1.15 acetate); 1.16 (4) alphameprodine; 1.17 (5) alphamethadol; 1.18 (6) alpha-methylfentanyl benzethidine; 1.19 (7) betacetylmethadol; 1.20 (8) betameprodine; 1.21 (9) betamethadol; Section 1. 1 05/05/20 03:02 pm HOUSE RESEARCH JD/RK H2711A8 2.1 (10) betaprodine; 2.2 (11) clonitazene; 2.3 (12) dextromoramide; 2.4 (13) diampromide; 2.5 (14) diethyliambutene; 2.6 (15) difenoxin; 2.7 (16) dimenoxadol; 2.8 (17) dimepheptanol; 2.9 (18) dimethyliambutene; 2.10 (19) dioxaphetyl butyrate; 2.11 (20) dipipanone; 2.12 (21) ethylmethylthiambutene; 2.13 (22) etonitazene; 2.14 (23) etoxeridine; 2.15 (24) furethidine;
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Steroids and Other Appearance and Performance Enhancing Drugs (Apeds) Research Report
Research Report Revised Febrero 2018 Steroids and Other Appearance and Performance Enhancing Drugs (APEDs) Research Report Table of Contents Steroids and Other Appearance and Performance Enhancing Drugs (APEDs) Research Report Introduction What are the different types of APEDs? What is the history of anabolic steroid use? Who uses anabolic steroids? Why are anabolic steroids misused? How are anabolic steroids used? What are the side effects of anabolic steroid misuse? How does anabolic steroid misuse affect behavior? What are the risks of anabolic steroid use in teens? How do anabolic steroids work in the brain? Are anabolic steroids addictive? How are anabolic steroids tested in athletes? What can be done to prevent steroid misuse? What treatments are effective for anabolic steroid misuse? Where can I get further information about steroids? References Page 1 Steroids and Other Appearance and Performance Enhancing Drugs (APEDs) Research Report Esta publicación está disponible para su uso y puede ser reproducida, en su totalidad, sin pedir autorización al NIDA. Se agradece la citación de la fuente, de la siguiente manera: Fuente: Instituto Nacional sobre el Abuso de Drogas; Institutos Nacionales de la Salud; Departamento de Salud y Servicios Humanos de los Estados Unidos. Introduction Appearance and performance enhancing drugs (APEDs) are most often used by males to improve appearance by building muscle mass or to enhance athletic performance. Although they may directly and indirectly have effects on a user’s mood, they do not produce a euphoric high, which makes APEDs distinct from other drugs such as cocaine, heroin, and marijuana. However, users may develop a substance use disorder, defined as continued use despite adverse consequences.
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Control Be Implemented. the First Large-Scale Systematic Olympic Games
Br J Sports Med: first published as 10.1136/bjsm.11.4.162 on 1 December 1977. Downloaded from 162 Brit. J. Sports Med. - Vol. 1 1, No. 4, December 1977, pp. 162-169 RADIOIMMUNOASSAY OF ANABOLIC STEROIDS: AN EVALUATION OF THREE ANTISERA FOR THE DETECTION OF ANABOLIC STEROIDS IN BIOLOGICAL FLUIDS Robert DUGAL, Ph.D., Claire DUPUIS, Ph.D. and Michel J. BERTRAND, Ph.D. Centre de Recherches en Sciences de la Sante, Institut National de la Recherche Scientifique, Centre Hospitalier Louis-H. Lafontaine, Montrdal, Quebec, Canada ABSTRACT Recently developped radioimmunoassays (RIA) for the analysis of anabolic steroids and their metabolites in biological fluids were tested for cross-reactivity with other types of steroids. Results show that the degree of desirable cross-reactivity within the two classes of orally active anabolic steroids vary widely and that the antiserum for 19-Nortestosterone (the active principle of intramuscular, preparations) has a very high degree of undesirable cross- reactivity with components of oral contraceptives. Single and multiple dose studies in human volunteers demonstrate that the detection level and degree of retrospectivity are likewise variable but that the test easily detects most anabolic steroids during treatment. At the present time, the combination of the three antisera for the assay of a sample appears to be a relatively rapid and economic method for screening large numbers of samples in situations where doping control of anabolic steroids is required. The importance of utilizing physico-chemical means for identification of RIA potential positives is emphasized. INTRODUCTION (Sumner, 1974: Brooks et al, 1975) and identification procedures for a limited number of them have also been copyright.
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Permanent Ban on Anabolic Androgenic Steroids From
Permanent Ban on Anabolic Androgenic Steroids to be introduced into the Greyhounds Australasia Rules Warning to trainers – Anabolic Androgenic Steroids (AAS) usage in greyhounds On 1 January 2016, Greyhounds Australasia will introduce Anabolic Androgenic Steroids to the list of Permanently Banned Prohibited Substances within GAR 79A (2) xx. as follows: “Anabolic androgenic steroids excluding those that are defined as an exempted substance pursuant to GAR 1.” The relevant exempted substance listed within GAR 1 is as follows: “Ethyloestrenol when administered orally to a greyhound bitch and where it has been prescribed by a veterinary surgeon for the sole purpose of regulating or preventing oestrus in that bitch.” Participants are advised that in accordance with GAR 79A they must never possess, acquire, attempt to acquire, administer or allow to be administered to any greyhound from birth until retirement, any anabolic androgenic steroid, excluding ethyloestrenol where it is appropriately prescribed for use as an oestrous suppressant in females. “Anabolic androgenic steroids” include those that are currently registered in Australia by the APVMA such as boldenone, ethyloestrenol, methandriol, nandrolone, stanozolol and testosterone. Others include but are not limited to 1- androstenediol; 1-androstenedione; bolandiol; bolasterone; boldione; calusterone; clostebol; danazol; dehydrochlormethyltestosterone; desoxymethyltestosterone; drostanolone; fluoxymesterone; formebolone; furazabol; gestrinone; 4-hydroxytestosterone; mestanolone; mesterolone;
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Controlled Substances Listed in This Section from Schedule VI
Page 1 of 15 ARTICLE II Schedule I (a) Schedule I shall consist of the drugs and other substances, by whatever official name, common or usual name, chemical name, or brand name designated, listed in this section. Each drug or substance has been assigned the DEA Controlled Substances Code Number set forth opposite it. (b) Opiates: (Narcotic Drugs) Unless specifically excepted or unless listed in another schedule, any of the following opiates, including their isomers, esters, ethers, salts, and salts of isomers, esters, and ethers, whenever the existence of such isomers, esters, ethers, salts is possible within the specific chemical designation (for purposes of paragraph (b)(34) only, the term isomer includes the optical and geometric isomers): (1) Acetyl-alpha-methylfentanyl(N-[1-[1-methyl-2- phenethyl)-4-piperidinyl]-N-phenylacetamide) ----- 9815-(2-86) (2) Acetylmethadol ----------------------------------- 9601* (3) Allylprodine ------------------------------------- 9602* (4) Alphacetylmethadol (except Levo-alphacetylmethadol (LAAM)------------------------------- 9603* (5) Alphameprodine ----------------------------------- 9604* (6) Alphamethadol ------------------------------------ 9605* (7) Alpha-methylfentanyl (N-[1-(alpha-methyl-beta-phenyl) ethyl-4-piperidyl]propronanilide; 1-(1-methyl- 2-phenylethyl)-4(N-propanilido)piperidine) ------- 9814-(6-82) (8) Alpha-methylthiofentanyl(N-[1-methyl-2-(2thienyl) ethyl-4-piperidinyl]-N-phenylpropanamide) -------- 9832-(2-86) (9) Benzethidine ------------------------------------- 9606* (10)
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Other Data Relevant to an Evaluation of Carcinogenicity and Its Mechanisms
COMBINED ESTROGEN−PROGESTOGEN CONTRACEPTIVES 143 4. Other Data Relevant to an Evaluation of Carcinogenicity and its Mechanisms 4.1 Absorption, distribution, metabolism and excretion in humans The metabolism and disposition of various formulations of oral contraceptives used in humans differ. After entering the small intestine, estrogenic and progestogenic compounds in combined oral contraceptives undergo metabolism by bacterial enzymes and enzymes in the intestinal mucosa to varying extents. The mixture of metabolized and unmetabolized compounds then undergoes intestinal absorption, and thus enters the portal vein blood, which perfuses the liver. In the liver, the compounds can be metabolized extensively, which leads to variations in the amount of active drug. A fraction of the absorbed dose of ethinyl- estradiol and some progestogens is also excreted in the bile during its first transit through the liver. Although some of these compounds are partially reabsorbed via the enterohepatic circulation, a fraction may also be excreted in this ‘first pass’, which reduces overall bio- availability. Since steroids penetrate normal skin easily, various systems have also been developed that deliver estrogens and progestogens parenterally, e.g. transdermal patches, nasal sprays, subcutaneous implants, vaginal rings and intrauterine devices (Fanchin et al., 1997; Dezarnaulds & Fraser, 2002; Meirik et al., 2003; Sarkar, 2003; Wildemeersch et al., 2003; Sturdee et al., 2004). These different modes of administration have been described previously (IARC, 1999). In general, all parenteral routes avoid loss of the drug by hepatic first-pass metabolism and minimally affect hepatic protein metabolism. The absorption rates of orally administered estrogens and progestogens are usually rapid; peak serum values are observed between 0.5 and 4 h after intake.
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