DOCSLIB.ORG

Rapid Identification of Sibutramine in Dietary Supplements Using A

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Rapid Identification of Sibutramine in Dietary Supplements Using A ORIGINAL ARTICLES Department of Pharmacognosy, University of Szeged, Szeged, Hungary Rapid identification of sibutramine in dietary supplements using a stepwise approach D. Csupor, K. Boros, B. Dankó, K. Veres, K. Szendrei, J. Hohmann Received March 20, 2012, accepted June 29, 2012 Deszo Csupor, Department of Pharmacognosy, University of Szeged, H-6720 Szeged, Eötvös u. 6, Hungary [email protected] Pharmazie 68: 15–18 (2013) doi: 10.1691/ph.2013.2069 Adulteration of botanical food supplements with undeclared synthetic drugs is a common problem. One of the most affected product groups are the slimming agents. There are no analytical protocols for the detection of synthetic adulterants from these products. The present study aimed at the development of a multistep analytical method for the quick and reliable determination of sibutramine, one of the most common adulterants among botanical food supplements. The extract of a sibutramine-containing slimming formula was analysed by colour tests, TLC, HPLC-DAD, MS and NMR. The multistep method proposed by the authors allows the quick identification of sibutramine in counterfeit samples in laboratories with different instrumentation. 1. Introduction In the developed countries there is an increasing demand for slimming medicines. One major group of compounds applied in the treatment of obesity act through the stimulation of the central nervous system, enhancement of metabolism and suppression of appetite. The ATC group A08AA “centrally acting antiobesity products” consists of several active agents (e.g. phentermine, fenfluramine, amfepramone, dexfenfluramine, mazindol, ethy- lamphetamine, cathine, clobenzorex, mefenorex, sibutramine) (WHO 2011), however, many of these molecules have been Fig. 1: Chemical structure of sibutramine removed from the market because of their undesirable effects (Ioannides-Demos et al. 2011). Their side effect profiles are related to the chemical and pharmacological similarities of tional foods and traditional Chinese medicines, the majority of these compounds to amphetamine. The number of anorectic the counterfeit products are registered or unregistered dietary agents available in the European Union and USA has nar- supplements. One of the most frequently applied compounds rowed to very few compounds. The European Medicines Agency as adulterant is sibutramine. In 2009 one article reported that recommended the withdrawal of phentermine, fenfluramine, 35 positive samples were found out of a total of 105 botanical amfepramone and clobenzorex from the market because of their dietary supplements, and the most common adulterant was sibu- unacceptable safety profile under normal conditions of use and tramine in slimming agents (Chen et al. 2009). In some cases limited therapeutic efficacy (EMA 2009). sibutramine was detected in Chinese herbal medicines after One of the most popular compounds, sibutramine (Fig. 1) has observing side effects characteristic of sibutramine (Jung et al. recently been withdrawn from the market of Western countries. 2006). The compound was withdrawn voluntarily by the manufacturer There are several, sophisticated methods (including HPLC- from the U.S. market in 2010 because of clinical trial data indi- DAD, HPLC-MS and NMR) described in the literature for the cating an increased risk of heart attacks and strokes. Based on reliable determination of sibutramine in medicinal produtcs and the evaluation of the currently available scientific data, the EMA biological samples. However, in developing countries, where concluded that the benefits of sibutramine-containing medicines the percentage of counterfeit products on the market is rather do not outweigh their risks, and therefore recommended that the high, a major limiting factor of the quality analysis of these marketing authorisations for sibutramine-containing medicines products is the lack of proper instrumentation. The aim of our be suspended across the EU (EMA 2010). study was the development of a rapid, multistep analytical proto- Parallelly to their withdrawal from the legal market, some col for the detection of sibutramine in dietary supplements. For of the above mentioned anorexiants reappeared in illegally this purpose we carried out the extensive analysis of a coun- adulterated products. Generally, counterfeit anorectic prepa- terfeit. Our experiments were actuated by multiple cases of rations are claimed to contain only herbal drugs or extracts, development of side effects characteristic to sibutramine after however, their efficacy is in fact based on the presence of the consumption of a food supplement (Super Slim capsules) in marked amounts of synthetic compounds. Beside some func- Hungary. Pharmazie 68 (2013) 15 ORIGINAL ARTICLES 2. Investigations and results At 222 nm, sibutramine could be unambiguously identified and its UV spectrum could be recorded. The retention time of 2.1. Sample preparation 2 min and the UV spectra with the absorption maximum at The purification of sibutramine using SPE allowed the quick 221.9 nm allows the identification of the compound (Fig. 2). separation of the compound in the fraction eluted from the col- The mean sibutramine content of the analyzed food supplement umn with CHCl3. The fraction eluted with MeOH also contained was 21.32 mg/capsule. sibutramine along with herbal constituents. 2.5. Mass spectrometry 2.2. Presumptive colour tests Full-scan ESI-positive mass spectra of the extract of the capsule In Simon’s test which is generally used as a test for sec- content and crystallized sibutramine revealed the presence of ondary amines, sibutramine, as a tertiary amine, gave a purple a pseudo-molecular ion [M + H]+ at m/z 280. The product ion coloured reaction. In Chen’s test, which is used to distinguish spectra of this showed a predominant fragment ion at m/z 125 ephedrine and its derivatives from amphetamine and metham- and a characteristic product ion at m/z 139 (Bogusz et al. 2006.) phetamine, sibutramine did not react, similarly to amphetamine (Fig. 3). The intensity of the latter peak decreased in case of derivatives. Marquis test, which allows the distinction between application of higher collision energy. These data, together with amphetamine and its ring-substituted analogues, resulted in a the previous steps of the analysis, allow the identification of light yellow reaction mixture. The low amount of other compo- sibutramine even from impure samples. nents than sibutramine in the examined sample did not influence the reaction results; accordingly the analyses of the extract of the food supplement and the solution of the reference compound 2.6. NMR gave the same results. As the result of 1D (1H and 13C) and 2D (COSY, HMBC, HSQC and NOESY) NMR experiments, complete chemical- 2.3. Thin layer chromatography shift assignements for all 1H and 13C resonances of sibutramine were achieved (Table). The Rf values of the tertiary amine sibutramine in the applied TLC systems were as follows: A: 0.81; B: 0.95; C: 0.93; D: 0.53. Since the most common amphetamine derivatives are 3. Discussion primary and secondary amines, their Rf values of the in TLC systems A, B and C (INCB 2005) are below 0.66, 0.56 and 0.47, The majority of the publications on the analysis of sibu- respectively, chromatographic analyses in these systems allow tramine concern the qualitative or quantitative determination the differentiation of sibutramine. However, due to the high Rf of the compound in medicinal products or biological samples. values of sibutramine in these systems, system D, proposed by Several HPLC, HPLC-MS, UV-spectrophotometric, capillary us, is more suitable for the analysis of the compound. System electrophoretic and infrared spectroscopic methods have been D allowed a good separation of sibutramine from the herbal developed for the analysis of sibutramine in pharmaceutical components of the examined sample, which were detected preparations or plant-based dietary supplements (de Carvalho below 0.5 Rf values. Among the applied visualization reagents, et al. 2011). concentrated (conc.) H2SO4 was not suitable for the detection The stepwise approach proposed by us, including sample of sibutramine. The compound was not detectable in UV pretreatment allows quick determination of undeclared sibu- light. Dragendorff reagent resulted in intensive orange spots tramine from adulterated herbal preparations. Colour tests, on yellow background; with acidified potassium iodoplatinate TLC, HPLC-DAD and mass spectrometric analyses of pure reagent sibutramine gave dark blue spots. sibutramine and the purified food supplement extract have shown identical results. The listed methods can be applied according to the instrumentation of the laboratory. Since these 2.4. HPLC-DAD methods rely upon independent principles, the unambiguous The HPLC-DAD analysis applied by us allows suitable detection positive results of the listed methods (colour tests, TLC, and quantification of sibutramine from the herbal constituents. HPLC-DAD, MS and NMR experiments) lead to the reliable Fig. 2: HPLC chromatogram of the purified extract of the sibutramine-containing food supplement and the UV spectrum of sibutramine 16 Pharmazie 68 (2013) ORIGINAL ARTICLES Table: NMR spectroscopic data of sibutramine [500 MHz (1H), 13 125 MHz ( C), CDCl3, ␦ (ppm) (J = Hz)] Position 1H 13C 1 – 49.4 2a 2.96 m 34.4 2b 2.77 ddd (12.3, 8.4, 3.9) 3a 1.98 m 15.8 3b 1.87 m 4a 2.38 m 35.0 4b 2.30 dd (11.2, 8.6) 5 – 139.5 6, 10 7.64 d (8.5) 130.1 7, 9 7.39 d (8.5) 128.5 8 – 133.3 11 3.60 dd (7.9, 5.0) 71.9 12 2.95 brs 47.4 13 2.21 brs 39.4 14a 1.47 ddd (15.0, 8.8, 5.0) 34.7 14b 1.34 ddd (15.0, 7.9, 6.0) 15 1.82 m 25.3 17 1.08 d (6.5) 21.7 16 1.05 d (6.5) 23.0 of origin: China) was purchased in a drug store in Szeged (Hungary). Each capule contained ∼275 mg of a greyish powder. Capsule content (100 mg) was extracted with 5 ml 50% MeOH in an ultrasonic bath for 10 min.
Load more

Recommended publications
  • WELLBUTRIN SR Safely and Effectively
    HIGHLIGHTS OF PRESCRIBING INFORMATION psychosis, hallucinations, paranoia, delusions, homicidal ideation, These highlights do not include all the information needed to use aggression, hostility, agitation, anxiety, and panic, as well as suicidal WELLBUTRIN SR safely and effectively. See full prescribing ideation, suicide attempt, and completed suicide. Observe patients information for WELLBUTRIN SR. attempting to quit smoking with bupropion for the occurrence of such symptoms and instruct them to discontinue bupropion and contact a WELLBUTRIN SR (bupropion hydrochloride) sustained-release tablets, healthcare provider if they experience such adverse events. (5.2) for oral use • Initial U.S. Approval: 1985 Seizure risk: The risk is dose-related. Can minimize risk by gradually increasing the dose and limiting daily dose to 400 mg. Discontinue if WARNING: SUICIDAL THOUGHTS AND BEHAVIORS seizure occurs. (4, 5.3, 7.3) See full prescribing information for complete boxed warning. • Hypertension: WELLBUTRIN SR can increase blood pressure. Monitor blood pressure before initiating treatment and periodically during • Increased risk of suicidal thinking and behavior in children, treatment. (5.4) adolescents and young adults taking antidepressants. (5.1) • Activation of mania/hypomania: Screen patients for bipolar disorder and • Monitor for worsening and emergence of suicidal thoughts and monitor for these symptoms. (5.5) behaviors. (5.1) • Psychosis and other neuropsychiatric reactions: Instruct patients to contact a healthcare professional if such reactions occur. (5.6) --------------------------- INDICATIONS AND USAGE ---------------------------- • Angle-closure glaucoma: Angle-closure glaucoma has occurred in WELLBUTRIN SR is an aminoketone antidepressant, indicated for the patients with untreated anatomically narrow angles treated with treatment of major depressive disorder (MDD). (1) antidepressants.
    [Show full text]
  • Clarifying the Ghrelin System's Ability to Regulate Feeding Behaviours
    International Journal of Molecular Sciences Review Clarifying the Ghrelin System’s Ability to Regulate Feeding Behaviours Despite Enigmatic Spatial Separation of the GHSR and Its Endogenous Ligand Alexander Edwards and Alfonso Abizaid * Department of Neuroscience, Carleton University, 1125 Colonel By Drive, Ottawa, ON K1S 5B6, Canada; [email protected] * Correspondence: [email protected]; Tel.: +1-613-520-2600 (ext. 1544) Academic Editor: Suzanne L. Dickson Received: 27 February 2017; Accepted: 11 April 2017; Published: 19 April 2017 Abstract: Ghrelin is a hormone predominantly produced in and secreted from the stomach. Ghrelin is involved in many physiological processes including feeding, the stress response, and in modulating learning, memory and motivational processes. Ghrelin does this by binding to its receptor, the growth hormone secretagogue receptor (GHSR), a receptor found in relatively high concentrations in hypothalamic and mesolimbic brain regions. While the feeding and metabolic effects of ghrelin can be explained by the effects of this hormone on regions of the brain that have a more permeable blood brain barrier (BBB), ghrelin produced within the periphery demonstrates a limited ability to reach extrahypothalamic regions where GHSRs are expressed. Therefore, one of the most pressing unanswered questions plaguing ghrelin research is how GHSRs, distributed in brain regions protected by the BBB, are activated despite ghrelin’s predominant peripheral production and poor ability to transverse the BBB. This manuscript will describe how peripheral ghrelin activates central GHSRs to encourage feeding, and how central ghrelin synthesis and ghrelin independent activation of GHSRs may also contribute to the modulation of feeding behaviours. Keywords: feeding; ghrelin; GHSR; blood brain barrier; vagal afferents; circumventricular organs; central ghrelin synthesis; GHSR heterodimerization; GHSR constitutive activity 1.
    [Show full text]
  • WHO Drug Information Vol. 12, No. 3, 1998
    WHO DRUG INFORMATION VOLUME 12 NUMBER 3 • 1998 RECOMMENDED INN LIST 40 INTERNATIONAL NONPROPRIETARY NAMES FOR PHARMACEUTICAL SUBSTANCES WORLD HEALTH ORGANIZATION • GENEVA Volume 12, Number 3, 1998 World Health Organization, Geneva WHO Drug Information Contents Seratrodast and hepatic dysfunction 146 Meloxicam safety similar to other NSAIDs 147 Proxibarbal withdrawn from the market 147 General Policy Issues Cholestin an unapproved drug 147 Vigabatrin and visual defects 147 Starting materials for pharmaceutical products: safety concerns 129 Glycerol contaminated with diethylene glycol 129 ATC/DDD Classification (final) 148 Pharmaceutical excipients: certificates of analysis and vendor qualification 130 ATC/DDD Classification Quality assurance and supply of starting (temporary) 150 materials 132 Implementation of vendor certification 134 Control and safe trade in starting materials Essential Drugs for pharmaceuticals: recommendations 134 WHO Model Formulary: Immunosuppressives, antineoplastics and drugs used in palliative care Reports on Individual Drugs Immunosuppresive drugs 153 Tamoxifen in the prevention and treatment Azathioprine 153 of breast cancer 136 Ciclosporin 154 Selective serotonin re-uptake inhibitors and Cytotoxic drugs 154 withdrawal reactions 136 Asparaginase 157 Triclabendazole and fascioliasis 138 Bleomycin 157 Calcium folinate 157 Chlormethine 158 Current Topics Cisplatin 158 Reverse transcriptase activity in vaccines 140 Cyclophosphamide 158 Consumer protection and herbal remedies 141 Cytarabine 159 Indiscriminate antibiotic
    [Show full text]
  • FSI-D-16-00226R1 Title
    Elsevier Editorial System(tm) for Forensic Science International Manuscript Draft Manuscript Number: FSI-D-16-00226R1 Title: An overview of Emerging and New Psychoactive Substances in the United Kingdom Article Type: Review Article Keywords: New Psychoactive Substances Psychostimulants Lefetamine Hallucinogens LSD Derivatives Benzodiazepines Corresponding Author: Prof. Simon Gibbons, Corresponding Author's Institution: UCL School of Pharmacy First Author: Simon Gibbons Order of Authors: Simon Gibbons; Shruti Beharry Abstract: The purpose of this review is to identify emerging or new psychoactive substances (NPS) by undertaking an online survey of the UK NPS market and to gather any data from online drug fora and published literature. Drugs from four main classes of NPS were identified: psychostimulants, dissociative anaesthetics, hallucinogens (phenylalkylamine-based and lysergamide-based materials) and finally benzodiazepines. For inclusion in the review the 'user reviews' on drugs fora were selected based on whether or not the particular NPS of interest was used alone or in combination. NPS that were use alone were considered. Each of the classes contained drugs that are modelled on existing illegal materials and are now covered by the UK New Psychoactive Substances Bill in 2016. Suggested Reviewers: Title Page (with authors and addresses) An overview of Emerging and New Psychoactive Substances in the United Kingdom Shruti Beharry and Simon Gibbons1 Research Department of Pharmaceutical and Biological Chemistry UCL School of Pharmacy
    [Show full text]
  • The Stimulants and Hallucinogens Under Consideration: a Brief Overview of Their Chemistry and Pharmacology
    Drug and Alcohol Dependence, 17 (1986) 107-118 107 Elsevier Scientific Publishers Ireland Ltd. THE STIMULANTS AND HALLUCINOGENS UNDER CONSIDERATION: A BRIEF OVERVIEW OF THEIR CHEMISTRY AND PHARMACOLOGY LOUIS S. HARRIS Dcparlmcnl of Pharmacology, Medical College of Virginia, Virginia Commonwealth Unwersity, Richmond, VA 23298 (U.S.A.) SUMMARY The substances under review are a heterogenous set of compounds from a pharmacological point of view, though many have a common phenylethyl- amine structure. Variations in structure lead to marked changes in potency and characteristic action. The introductory material presented here is meant to provide a set of chemical and pharmacological highlights of the 28 substances under con- sideration. The most commonly used names or INN names, Chemical Abstract (CA) names and numbers, and elemental formulae are provided in the accompanying figures. This provides both some basic information on the substances and a starting point for the more detailed information that follows in the individual papers by contributors to the symposium. Key words: Stimulants, their chemistry and pharmacology - Hallucinogens, their chemistry and pharmacology INTRODUCTION Cathine (Fig. 1) is one of the active principles of khat (Catha edulis). The structure has two asymmetric centers and exists as two geometric isomers, each of which has been resolved into its optical isomers. In the plant it exists as d-nor-pseudoephedrine. It is a typical sympathomimetic amine with a strong component of amphetamine-like activity. The racemic mixture is known generically in this country and others as phenylpropanolamine (dl- norephedrine). It is widely available as an over-the-counter (OTC) anti- appetite agent and nasal decongestant.
    [Show full text]
  • KHAT Latest Revision: June 11, 2005
    KHAT Latest Revision: June 11, 2005 O CH3 NH2 Cathinone OH CH3 NH2 Cathine N CH3 H3C N 3,6-dimethyl-2,5-diphenylpyrazine (dimer of Cathinone) 1. SYNONYMS CFR: Cathinone Cathine CAS #: Cathinone Hydrochloride: 71031-15-7 Cathine Hydrochloride: 2153-98-2 Cathine Base: 492-39-7 Other Names: Catha edulis Kat Mutsawhari Mutsawari Mdimamadzi Musitate Mirungi Miraa Ol meraa Tumayot Liruti Ikwa Arabian Tea 2. CHEMICAL AND PHYSICAL DATA Khat is used as a stimulant or as a medicine in parts of Africa and the Arabian Peninsula. The plant is thought to have been in cultivation before the coffee plant; historical references date the use of the plant to the fourteenth century. Peter Forsskal, a physician and botanist, collected khat specimens in an expedition organized by the King of Denmark in the eighteenth century. Forsskal assigned the name Catha edulis to the plant. The effects produced by the drug include excitation, hypersensitivity, anorexia, insomnia, euphoria, increased respiration, and hyperthermia. These effects closely parallel the effects of d-amphetamine. Khat is a bush or tree that grows naturally in the humid mountainous regions (elevations of 5000 to 6500 feet) of East and South Africa. The trees can grow naturally to over 60 ft; however, cultivated khat trees are pruned and their height to kept to approximately 16 feet. Khat also grows to a height of 3 feet as a small bush in arid regions. Like opium, the alkaloid content of khat will vary with the soil, climatic conditions, and cultivation. Khat belongs to the genus Catha edulis. It is recognized that the genus consists of only one species; however, the plant exhibits extreme polymorphism.
    [Show full text]
  • The 2014 Prohibited List International Standard
    The World Anti-Doping Code THE 2014 PROHIBITED LIST INTERNATIONAL STANDARD Version 2.0 (revised 2014 version) The official text of the Prohibited List shall be maintained by WADA and shall be published in English and French. In the event of any conflict between the English and French versions, the English version shall prevail. This List shall come into effect on 1 September 2014 The revised 2014 Prohibited List 17 May 2014 THE 2014 PROHIBITED LIST WORLD ANTI-DOPING CODE Valid 1 September 2014 In accordance with Article 4.2.2 of the World Anti-Doping Code, all Prohibited Substances shall be considered as “Specified Substances” except Substances in classes S1, S2, S4.4, S4.5, S6.a, and Prohibited Methods M1, M2 and M3. SUBSTANCES AND METHODS PROHIBITED AT ALL TIMES (IN- AND OUT-OF-COMPETITION) PROHIBITED SUBSTANCES S0. NON-APPROVED SUBSTANCES Any pharmacological substance which is not addressed by any of the subsequent sections of the List and with no current approval by any governmental regulatory health authority for human therapeutic use (e.g drugs under pre-clinical or clinical development or discontinued, designer drugs, substances approved only for veterinary use) is prohibited at all times. S1. ANABOLIC AGENTS Anabolic agents are prohibited. 1. Anabolic Androgenic Steroids (AAS) a. Exogenous* AAS, including: 1-androstenediol (5α-androst-1-ene-3β,17β-diol ); 1-androstenedione (5α- androst-1-ene-3,17-dione); bolandiol (estr-4-ene-3β,17β-diol ); bolasterone; boldenone; boldione (androsta-1,4-diene-3,17-dione); calusterone; clostebol;
    [Show full text]
  • (19) United States (12) Patent Application Publication (10) Pub
    US 20130289061A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0289061 A1 Bhide et al. (43) Pub. Date: Oct. 31, 2013 (54) METHODS AND COMPOSITIONS TO Publication Classi?cation PREVENT ADDICTION (51) Int. Cl. (71) Applicant: The General Hospital Corporation, A61K 31/485 (2006-01) Boston’ MA (Us) A61K 31/4458 (2006.01) (52) U.S. Cl. (72) Inventors: Pradeep G. Bhide; Peabody, MA (US); CPC """"" " A61K31/485 (201301); ‘4161223011? Jmm‘“ Zhu’ Ansm’ MA. (Us); USPC ......... .. 514/282; 514/317; 514/654; 514/618; Thomas J. Spencer; Carhsle; MA (US); 514/279 Joseph Biederman; Brookline; MA (Us) (57) ABSTRACT Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject (21) App1_ NO_; 13/924,815 comprising; administering a therapeutic amount of the neu rological stimulant and administering an antagonist of the kappa opioid receptor; to thereby reduce or prevent the devel - . opment of aversion to the CNS stimulant in the subject. Also (22) Flled' Jun‘ 24’ 2013 disclosed is a method of reducing or preventing the develop ment of addiction to a CNS stimulant in a subj ect; comprising; _ _ administering the CNS stimulant and administering a mu Related U‘s‘ Apphcatlon Data opioid receptor antagonist to thereby reduce or prevent the (63) Continuation of application NO 13/389,959, ?led on development of addiction to the CNS stimulant in the subject. Apt 27’ 2012’ ?led as application NO_ PCT/US2010/ Also disclosed are pharmaceutical compositions comprising 045486 on Aug' 13 2010' a central nervous system stimulant and an opioid receptor ’ antagonist.
    [Show full text]
  • Full Prescribing Information Warning: Suicidal Thoughts
    tablets (SR) BUPROPION hydrochloride extended-release HIGHLIGHTS OF PRESCRIBING INFORMATION anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide. Observe hydrochloride extended-release tablets (SR) was reported. However, the symptoms persisted in some Table 3. Adverse Reactions Reported by at Least 1% of Subjects on Active Treatment and at a tablets (SR) may be necessary when coadministered with ritonavir, lopinavir, or efavirenz [see Clinical These highlights do not include all the information needed to use bupropion hydrochloride patients attempting to quit smoking with Bupropion hydrochloride extended-release tablets, USP cases; therefore, ongoing monitoring and supportive care should be provided until symptoms resolve. Greater Frequency than Placebo in the Comparator Trial Pharmacology (12.3)] but should not exceed the maximum recommended dose. extended-release tablets (SR) safely and effectively. See full prescribing information for (SR) for the occurrence of such symptoms and instruct them to discontinue Bupropion hydrochloride Carbamazepine, Phenobarbital, Phenytoin: While not systematically studied, these drugs extended-release tablets, USP (SR) and contact a healthcare provider if they experience such adverse The neuropsychiatric safety of Bupropion hydrochloride extended-release tablets (SR) was evaluated in Bupropion Bupropion may induce the metabolism of bupropion and may decrease bupropion exposure [see Clinical bupropion hydrochloride extended-release tablets (SR). Nicotine events. (5.2) a randomized, double-blind, active-and placebo-controlled study that included patients without a history Hydrochloride Hydrochloride Pharmacology (12.3)]. If bupropion is used concomitantly with a CYP inducer, it may be necessary Transdermal BUPROPION hydrochloride extended-release tablets (SR), for oral use • Seizure risk: The risk is dose-related.
    [Show full text]
  • Street Names: Khat, Qat, Kat, Chat, Miraa, Quaadka) September 2019
    Drug Enforcement Administration Diversion Control Division Drug & Chemical Evaluation Section KHAT (Street Names: Khat, Qat, Kat, Chat, Miraa, Quaadka) September 2019 Introduction: User Population: Khat, Catha edulis, is a flowering shrub native to East Abuse of khat in the United States is most prevalent among Africa and the Arabian-Peninsula. Khat often refers to the immigrants from Somalia, Ethiopia, and Yemen. Abuse of khat is leaves and young shoot of Catha edulis. It has been widely highest in cities with a substantial population of these immigrants. used since the thirteenth century as a recreational drug by the These cities include Boston (MA), Columbus (OH), Dallas (TX), indigenous people of East Africa, the Arabian Peninsula and Detroit (MI), Kansas City (MO), Los Angeles (CA), Minneapolis (MN), throughout the Middle East. Nashville (TN), New York (NY), and Washington D.C. Licit Uses: Illicit Distribution: There is no accepted medical use in treatment for khat in Individuals of Somali, Ethiopian, and Yemeni descent are the the United States. primary transporters and distributors of khat in the United States. The khat is transported from Somalia into the United States and distributed Chemistry and Pharmacology: in the Midwest, West and Southeast (Nashville, Tennessee) regions Khat contains two central nervous system (CNS) of the United States. According to the National Drug Intelligence stimulants, namely cathinone and cathine. Cathinone (alpha- Center, Somali and Yemen independent dealers are distributing khat aminopriopiophenone), which is considered to be the principal in Ann Arbor, Detroit, Lansing and Ypsilanti, Michigan; Columbus, active stimulant, is structurally similar to d-amphetamine and Ohio; Kansas City, Missouri; and Minneapolis/St.
    [Show full text]
  • Toxicology Times
    TOXICOLOGY (800) 677-7995 TIMES www.sdrl.com A FREE Monthly Newsletter for Substance Abuse and Opioid Treatment Volume 5, Issue 7 Programs from San Diego Reference Laboratory July, 2015 Amphetamines (Part 1) Dr. Joseph E. Graas, Scientific Director most often used in inhalers and does not tite, increased stamina and physical energy, Dr. Edward Moore, Medical Director have the central nervous system activity nor increased sexual response/drive, involuntary any addictive properties. All of the com- body movements, increased perspiration, The term “amphetamines” has come to mean pounds that have the structure of hyperactivity, nausea and increased heart rate. a class of endogenous neurotransmitters that phenylethylamine will have this mixture of d This drug is highly addictive and tolerance stimulate the sympathetic nervous system. and l molecules. In the production of these develops quickly. Withdrawal is an extremely This is a broad class of various substituted drugs they are usually noted as a racemic unpleasant experience. A few street names derivatives of phenylethylamine. This grow- mixture, or specifically, as the d or l com- for the drug are amp, speed, crank, dolls and ing class of structurally related molecules may pound. To properly evaluate this family of crystal. also stimulate the sympathetic nervous sys- compounds known as sympathomimetic tem in many different ways, such as affecting amines, amphetamines or phenylethylamine, Methamphetamine was developed by the the re-release of neurotransmitters or pre- it is best done by describing each member of Japanese in 1919 and used during World War venting the re-uptake of neurotransmitters, the class: amphetamine , methampheta- II to help soldiers stay alert and energize hallucinogens, anorectics, bronchodilators mine , phentermine , phenylpropanola- factory workers.
    [Show full text]
  • Cross-Sectional Study of the Dispensation of Synthetic Anorectic Drugs in Community Pharmacies in the City of Cruz Alta – State of Rio Grande Do Sul
    Brazilian Journal of Pharmaceutical Sciences vol. 50, n. 4, oct./dec., 2014 Article http://dx.doi.org/10.1590/S1984-82502014000400008 Cross-sectional study of the dispensation of synthetic anorectic drugs in community pharmacies in the city of Cruz Alta – State of Rio Grande do Sul Marcieli Maria Navarini1, Viviane Cecilia Kessler Nunes Deuschle2,*, Regis Augusto Norbert Deuschle3 1Faculty of Pharmacy, University of Cruz Alta, Rio Grande do Sul, Brazil,2,3Postgraduate Program in Pharmaceutical Sciences, Federal University of Santa Maria, Brazil Obesity is defined as the excess adipose tissue in the body. Drugs responsible for inhibiting the appetite are called anorectics or appetite suppressants. Sibutramine, fenproporex and amfepramone belongs to this class, and are capable of causing physical or psychological dependence. The aim of this study was to evaluate the frequency of prescriptions for appetite suppressants in community pharmacies at Cruz Alta, State of Rio Grande do Sul, Brazil. The sales of fenproporex, amfepramone and sibutramine in the months of September, October and November 2010 and April, May and June 2011 were compared. It was observed that the most commonly dispensed anorectic in the three community pharmacies analyzed was sibutramine. In the months of September, October and November 2010, consumption was higher, with sibutramine achieving 40.3% of overall sales, amfepramone 21% and, finally, fenproporex, 7.9%. The consumption of appetite suppressants was more prevalent in females, who represented 82% of total. The results suggested the existence of high consumption of anorectics, possibly related to the current concern with aesthetic standards, which emphasizes the importance of strict control over the marketing of these substances.
    [Show full text]