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[PMID]:26065363
[Au] Autor:Eiden C; Peyrière H; Diot C; Mathieu O
[Ad] Endereço:Department of Medical Pharmacology and Toxicology, Addictovigilance centre, Montpellier University Hospital, Montpellier University.
[Ti] Título:Prevalence of levamisole and aminorex in patients tested positive for cocaine in a French University Hospital.
[So] Source:Clin Toxicol (Phila);53(7):604-8, 2015.
[Is] ISSN:1556-9519
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: The prevalence of levamisole in urine samples of subjects positive for cocaine in the US was estimated at 78% (95%confidence interval or CI: 73%-83%). However, levamisole was not quantified, and at the time of this report, aminorex was not known to be a possible metabolite of levamisole in human. Moreover no data are available in Europe. OBJECTIVE: The aim of this study was to determine the prevalence and concentration of levamisole and aminorex in positive cocaine urine toxicology tests, and in serum samples of cocaine-positive subjects driving under the influence of drugs or forensic autopsies. MATERIALS AND METHODS: Consecutive urine toxicology samples tested positive for cocaine by immunoassay (EMIT, Siemens) from April to May 2014 at the toxicology laboratory of a French University Hospital, and blood samples of cocaine-positive subjects driving under the influence of drugs or forensic autopsies from April to December 2014 were analyzed by liquid chromatography-tandem mass spectrometry or LC-MS/MS (3200 QTrap, AB Sciex) to detect and quantify the presence of levamisole and aminorex. RESULTS: Forty-two urine samples tested positive for cocaine in 39 patients (79.5% males) with a median age of 43 [range: 20-51] years. Toxicological analyses were mainly required by addictions care centers (n = 17; 40%) in the context of the routine management of addict patients. Cocaine concentrations were above the limit of quantification for 33 patients, with a median value of 228 [0-645,000] ng/ml. Levamisole was detected in 32 urine samples (76%) (median concentration: 1,430 ng/ml, range: 30-258,000). Aminorex was never detected. During the study period, levamisole was detected in 87.5% of cocaine-positive blood samples of the subjects driving under the influence of drugs or forensic autopsies. DISCUSSION: In this prospective study, the prevalence of levamisole in cocaine-positive samples was 76%. Over this period, although clinical complications related to cocaine use were reported (agitation, road accident, and cardiac arrest), no complication specifically related to levamisole or aminorex was reported. CONCLUSION: Our results show a high prevalence of levamisole in samples of subjects positive for cocaine, close to the prevalence found in the US. This high prevalence raises issues with respect to well-identified health risks associated with regular consumption of levamisole.
[Mh] Termos MeSH primário: Aminorex/urina
Cocaína/urina
Levamisol/urina
[Mh] Termos MeSH secundário: Adulto
Cromatografia Líquida
Transtornos Relacionados ao Uso de Cocaína/urina
Europa (Continente)
Feminino
Hospitais Universitários
Seres Humanos
Masculino
Meia-Idade
Estudos Prospectivos
Espectrometria de Massas em Tandem
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
2880D3468G (Levamisole); 2SH16612I9 (Aminorex); I5Y540LHVR (Cocaine)
[Em] Mês de entrada:1510
[Cu] Atualização por classe:150729
[Lr] Data última revisão:
150729
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:150613
[St] Status:MEDLINE
[do] DOI:10.3109/15563650.2015.1054499


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[PMID]:25331619
[Au] Autor:McLaughlin G; Morris N; Kavanagh PV; Power JD; Twamley B; O'Brien J; Talbot B; Dowling G; Mahony O; Brandt SD; Patrick J; Archer RP; Partilla JS; Baumann MH
[Ad] Endereço:Department of Life and Physical Sciences, School of Science, Athlone Institute of Technology, Dublin Road, Athlone, Co. Westmeath, Ireland.
[Ti] Título:Synthesis, characterization, and monoamine transporter activity of the new psychoactive substance 3',4'-methylenedioxy-4-methylaminorex (MDMAR).
[So] Source:Drug Test Anal;7(7):555-64, 2015 Jul.
[Is] ISSN:1942-7611
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The recent occurrence of deaths associated with the psychostimulant cis-4,4'-dimethylaminorex (4,4'-DMAR) in Europe indicated the presence of a newly emerged psychoactive substance on the market. Subsequently, the existence of 3,4-methylenedioxy-4-methylaminorex (MDMAR) has come to the authors' attention and this study describes the synthesis of cis- and trans-MDMAR followed by extensive characterization by chromatographic, spectroscopic, mass spectrometric platforms and crystal structure analysis. MDMAR obtained from an online vendor was subsequently identified as predominantly the cis-isomer (90%). Exposure of the cis-isomer to the mobile phase conditions (acetonitrile/water 1:1 with 0.1% formic acid) employed for high performance liquid chromatography analysis showed an artificially induced conversion to the trans-isomer, which was not observed when characterized by gas chromatography. Monoamine release activities of both MDMAR isomers were compared with the non-selective monoamine releasing agent (+)-3,4-methylenedioxymethamphetamine (MDMA) as a standard reference compound. For additional comparison, both cis- and trans-4,4'-DMAR, were assessed under identical conditions. cis-MDMAR, trans-MDMAR, cis-4,4'-DMAR and trans-4,4'-DMAR were more potent than MDMA in their ability to function as efficacious substrate-type releasers at the dopamine (DAT) and norepinephrine (NET) transporters in rat brain tissue. While cis-4,4'-DMAR, cis-MDMAR and trans-MDMAR were fully efficacious releasing agents at the serotonin transporter (SERT), trans-4,4'-DMAR acted as a fully efficacious uptake blocker. Currently, little information is available about the presence of MDMAR on the market but the high potency of ring-substituted methylaminorex analogues at all three monoamine transporters investigated here might be relevant when assessing the potential for serious side-effects after high dose exposure.
[Mh] Termos MeSH primário: Aminorex/análogos & derivados
Aminorex/síntese química
Estimulantes do Sistema Nervoso Central/síntese química
Proteínas Vesiculares de Transporte de Monoamina/efeitos dos fármacos
[Mh] Termos MeSH secundário: Aminorex/metabolismo
Animais
Estimulantes do Sistema Nervoso Central/metabolismo
Estimulantes do Sistema Nervoso Central/farmacologia
Cristalografia por Raios X
Masculino
Psicotrópicos
Ratos
Ratos Sprague-Dawley
Sinaptossomos/efeitos dos fármacos
Sinaptossomos/metabolismo
Proteínas Vesiculares de Transporte de Monoamina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Central Nervous System Stimulants); 0 (Psychotropic Drugs); 0 (Vesicular Monoamine Transport Proteins); 2SH16612I9 (Aminorex)
[Em] Mês de entrada:1605
[Cu] Atualização por classe:170302
[Lr] Data última revisão:
170302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141022
[St] Status:MEDLINE
[do] DOI:10.1002/dta.1732


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[PMID]:25167967
[Au] Autor:Nizar H; Dargan PI; Wood DM
[Ad] Endereço:Clinical Pharmacology, Charing Cross Hospital, London, UK.
[Ti] Título:Using internet snapshot surveys to enhance our understanding of the availability of the novel psychoactive substance 4-methylaminorex and 4,4'-dimethylaminorex.
[So] Source:J Med Toxicol;11(1):80-4, 2015 Mar.
[Is] ISSN:1937-6995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:4,4'-Dimethylaminorex is a stimulant novel psychoactive substance (NPS) first detected in Europe in November 2012. It is a derivative of 4-methylaminorex, a substance controlled under Schedule 1 of the 1971 United Nations Convention on Psychotropic Substances. There is currently no information on the availability or cost of these substances from Internet suppliers. An Internet snapshot study was undertaken in English using established European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) methodology to determine the availability of 4-methylaminorex and 4,4'-dimethylaminorex in April 2014. Twenty Internet sites selling 4-methylaminorex were identified, 18 selling in US dollars and two in GB Pound Sterling. Fourteen (70 %) Internet sites had a minimum purchase amount of ≥10 g (compared to user doses of 10-25 mg). For the 18 suppliers selling in US$, 9 quoted a fixed price per gram irrespective of the amount ordered and 11 had a reducing price per gram with increasing purchase quantity (US$30.8 ± 34.2/g for 1 g purchase to US$15.2 ± 20.3/g for 1 kg purchase). Only one Internet site selling 4,4'-dimethylaminorex was identified, selling in Euros. The minimum purchase quantity was 500 mg. The price per gram reduced from 36.08/g for a 500 mg purchase to 2.20/g for a 100 g purchase. This Internet snapshot demonstrated that there was a greater availability from Internet suppliers of products advertised as 4-methylaminorex than 4,4'-dimethylaminorex, despite the 4-methylaminorex being an internationally controlled substance. Whilst this may reflect misunderstanding by suppliers, it has the potential to put those purchasing at risk of contravening border control and/or local law enforcement legislation. The use of methodology such as Internet snapshot surveys is of increasing interest to clinical/medical toxicologists in their understanding of the supply, availability and cost of novel psychoactive substances.
[Mh] Termos MeSH primário: Aminorex/análogos & derivados
Drogas Desenhadas/provisão & distribuição
Tráfico de Drogas
Oxazóis/provisão & distribuição
Drogas Ilícitas/provisão & distribuição
[Mh] Termos MeSH secundário: Aminorex/economia
Aminorex/provisão & distribuição
Drogas Desenhadas/economia
Custos de Medicamentos
Tráfico de Drogas/economia
Europa (Continente)
Toxicologia Forense/métodos
Seres Humanos
Internet
Aplicação da Lei/métodos
Metilação
Oxazóis/economia
Pós
Vigilância em Saúde Pública/métodos
Ferramenta de Busca
Drogas Ilícitas/economia
Toxicologia/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Designer Drugs); 0 (Oxazoles); 0 (Powders); 0 (Street Drugs); 0 (para-methyl-4-methylaminorex); 2SH16612I9 (Aminorex); 7PK6VC94OU (4-methylaminorex)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140830
[St] Status:MEDLINE
[do] DOI:10.1007/s13181-014-0425-0


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[PMID]:24794740
[Au] Autor:Karch SB; Defraia B; Messerini L; Mari F; Vaiano F; Bertol E
[Ad] Endereço:Consultant Pathologist/Toxicologist, Berkeley, CA, USA.
[Ti] Título:Aminorex associated with possible idiopathic pulmonary hypertension in a cocaine user.
[So] Source:Forensic Sci Int;240:e7-10, 2014 Jul.
[Is] ISSN:1872-6283
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:The conversion of levamisole to aminorex in horses was first described in 2009 and, for the first time, confirmed in humans two years later by our laboratory. Aminorex and levamisole interfere with serotonin metabolism and both are proven cause of potentially fatal idiopathic pulmonary hypertension (IPH). Because most of the world's seizures of illicit cocaine is now contaminated with levamisole, this raises the possibility that users of levamisole adulterated cocaine users may be at risk for IPH. Here we describe the first case of IPH in a user of levamisole-contaminated cocaine. Levamisole and aminorex were both identified and quantified in hair and other biological specimens by means gas chromatography/mass spectrometry system (levamisole: urine, 75.05ng/mL; blood, 15.05ng/mL; brain, >0.15ng/g; liver, >0.15ng/g; hair, 12.15ngmg; aminorex: urine, 38.62ng/mL; blood, 8.92ng/mL, brain >0.15ng/g; liver, 0.15ng/g; hair 7.35ng/mg; cocaine, benzoylecgonine, morphine, 6-acetylmorphine, methadone, 2-ethylidine-1, 5-dimetil-3, 3 diphenylpyrrolidine were also detected). Moreover histological changes associated with IPH were observed in the lung. As IPH produces relatively non-specific symptoms in its early stages, this index case may serve as a harbinger of many more cases to come. It should also alert clinicians to the possibility that their patient may be suffering from this relatively rare disorder.
[Mh] Termos MeSH primário: Aminorex/efeitos adversos
Depressores do Apetite/efeitos adversos
Transtornos Relacionados ao Uso de Cocaína/complicações
Hipertensão Pulmonar/induzido quimicamente
[Mh] Termos MeSH secundário: Aminorex/análise
Depressores do Apetite/análise
Usuários de Drogas
Patologia Legal
Cabelo/química
Seres Humanos
Levamisol/análise
Pulmão/patologia
Masculino
Meia-Idade
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Appetite Depressants); 2880D3468G (Levamisole); 2SH16612I9 (Aminorex)
[Em] Mês de entrada:1510
[Cu] Atualização por classe:140604
[Lr] Data última revisão:
140604
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140506
[St] Status:MEDLINE


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[PMID]:24574157
[Au] Autor:Hess C; Ritke N; Sydow K; Mehling LM; Ruehs H; Madea B; Musshoff F
[Ad] Endereço:Institute of Forensic Medicine, University of Bonn, Stiftsplatz 12, D-53111, Bonn, Germany.
[Ti] Título:Determination of levamisole, aminorex, and pemoline in plasma by means of liquid chromatography-mass spectrometry and application to a pharmacokinetic study of levamisole.
[So] Source:Drug Test Anal;6(10):1049-54, 2014 Oct.
[Is] ISSN:1942-7611
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Levamisole is an anti-helminthic drug and gained forensic interest after it was found that it was used as a cocaine adulterant. A liquid chromatography-mass spectrometry (LC-MS) method for the determination of levamisole and its metabolite aminorex in human plasma is described. Selectivity is given; calibration curves were linear within a calibration range of 1 ng/mL-500 ng/mL. Limits of detection and quantification (LODs, LOQs) were 0.85 ng/mL for levamisole and 0.09 ng/mL, and 0.34 ng/mL for aminorex, respectively. Precision data was in accordance with the GTFCh guidelines. The validated method was successfully applied to study the pharmacokinetics of levamisole after administration of 100 mg of levamisole orally. Levamisole could be detected up to 36 h after ingestion in serum, while aminorex never exceeded the LOQ. A one-compartment model best described levamisole pharmacokinetics. The following parameters were calculated: ka = 1.2 [1/h], CL/F = 52 l/h, V/F = 347 l, f (renal) = 0.0005, t ½ = 2.0 h, AUC = 1923 ng/mL*h, cmax = 214 ng/mL, tmax = 1.98 h. Levamisole could be quantified in 42.5% of cocaine--positive plasma samples (2.2 to 224 ng/mL). Aminorex was positive in only 11.3% of the cases; however, it was never found higher than the LOQ. Pemoline, another stimulant detected in horse urine samples after administration of levamisole, was not found either in serum or in urine of this pharmacokinetic study. In post-mortem cases, levamisole and aminorex could be detected in femoral blood and the urine of cocaine users. Pemoline was not detected.
[Mh] Termos MeSH primário: Aminorex/análise
Cromatografia Líquida/métodos
Levamisol/farmacocinética
Espectrometria de Massas/métodos
[Mh] Termos MeSH secundário: Administração Oral
Adulto
Aminorex/metabolismo
Anti-Helmínticos/administração & dosagem
Anti-Helmínticos/análise
Anti-Helmínticos/farmacocinética
Área Sob a Curva
Meia-Vida
Seres Humanos
Levamisol/administração & dosagem
Levamisol/análise
Limite de Detecção
Masculino
Modelos Biológicos
Pemolina/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthelmintics); 2880D3468G (Levamisole); 2SH16612I9 (Aminorex); 7GAQ2332NK (Pemoline)
[Em] Mês de entrada:1506
[Cu] Atualização por classe:160511
[Lr] Data última revisão:
160511
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140228
[St] Status:MEDLINE
[do] DOI:10.1002/dta.1619


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[PMID]:24296074
[Au] Autor:Hofmaier T; Luf A; Seddik A; Stockner T; Holy M; Freissmuth M; Ecker GF; Schmid R; Sitte HH; Kudlacek O
[Ad] Endereço:Institute of Pharmacology, Center for Physiology and Pharmacology, Medical University of Vienna, Waehringerstrasse 13A, 1090 Vienna, Austria.
[Ti] Título:Aminorex, a metabolite of the cocaine adulterant levamisole, exerts amphetamine like actions at monoamine transporters.
[So] Source:Neurochem Int;73:32-41, 2014 Jul.
[Is] ISSN:1872-9754
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Psychostimulants such as amphetamine and cocaine are illicitly used drugs that act on neurotransmitter transporters for dopamine, serotonin or norepinephrine. These drugs can by themselves already cause severe neurotoxicity. However, an additional health threat arises from adulterant substances which are added to the illicit compound without declaration. One of the most frequently added adulterants in street drugs sold as cocaine is the anthelmintic drug levamisole. We tested the effects of levamisole on neurotransmitter transporters heterologously expressed in HEK293 cells. Levamisole was 100 and 300-fold less potent than cocaine in blocking norepinephrine and dopamine uptake, and had only very low affinity for the serotonin transporter. In addition, levamisole did not trigger any appreciable substrate efflux. Because levamisole and cocaine are frequently co-administered, we searched for possible allosteric effects; at 30µM, a concentration at which levamisole displayed already mild effects on norepinephrine transport it did not enhance the inhibitory action of cocaine. Levamisole is metabolized to aminorex, a formerly marketed anorectic drug, which is classified as an amphetamine-like substance. We examined the uptake-inhibitory and efflux-eliciting properties of aminorex and found it to exert strong effects on all three neurotransmitter transporters in a manner similar to amphetamine. We therefore conclude that while the adulterant levamisole itself has only moderate effects on neurotransmitter transporters, its metabolite aminorex may exert distinct psychostimulant effects by itself. Given that the half-time of levamisole and aminorex exceeds that of cocaine, it may be safe to conclude that after the cocaine effect "fades out" the levamisole/aminorex effect "kicks in".
[Mh] Termos MeSH primário: Aminorex/farmacologia
Anfetamina/farmacologia
Depressores do Apetite/farmacologia
Cocaína/química
Levamisol/metabolismo
Proteínas Vesiculares de Transporte de Monoamina/efeitos dos fármacos
[Mh] Termos MeSH secundário: Sítios de Ligação/efeitos dos fármacos
Proteínas da Membrana Plasmática de Transporte de Dopamina/antagonistas & inibidores
Contaminação de Medicamentos
Células HEK293
Seres Humanos
Proteínas da Membrana Plasmática de Transporte de Norepinefrina/antagonistas & inibidores
Proteínas da Membrana Plasmática de Transporte de Serotonina/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Appetite Depressants); 0 (Dopamine Plasma Membrane Transport Proteins); 0 (Norepinephrine Plasma Membrane Transport Proteins); 0 (Serotonin Plasma Membrane Transport Proteins); 0 (Vesicular Monoamine Transport Proteins); 2880D3468G (Levamisole); 2SH16612I9 (Aminorex); CK833KGX7E (Amphetamine); I5Y540LHVR (Cocaine)
[Em] Mês de entrada:1502
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131204
[St] Status:MEDLINE


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[PMID]:24037625
[Au] Autor:Souza R; Jardim C; Humbert M
[Ad] Endereço:Department of Pulmonary, Heart Institute, University of Sao Paulo Medical School, Sao Paulo, Brazil.
[Ti] Título:Idiopathic pulmonary arterial hypertension.
[So] Source:Semin Respir Crit Care Med;34(5):560-7, 2013 Oct.
[Is] ISSN:1098-9048
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Idiopathic pulmonary arterial hypertension (IPAH), formerly called primary pulmonary hypertension, is a rare disease (incidence and prevalence rates of approximately one and six cases per million inhabitants, respectively) with different clinical phenotypes. A group of diverse conditions manifest pulmonary arterial hypertension (PAH) and share similar pathological and/or clinical findings with IPAH. By definition, IPAH is diagnosed only after alternative diagnoses have been ruled out. Extensive investigation is needed to determine if PAH is associated with thyroid diseases, infectious diseases, autoimmune conditions, exposure to certain drugs (particularly anorexigens), certain genetic mutations, and so on. The presence of genetic abnormalities and risk factors (such as specific drug exposures) reinforces the "multiple hit" concept for the development of pulmonary hypertension. Fortunately, within the past two decades, therapeutic options have become available for IPAH, resulting in improved survival and clinical outcomes. At least seven different compounds have been registered for PAH treatment. However, even with aggressive PAH-specific therapy, mortality rates remain high (∼40% at 5 years). Given the high mortality rates, the use of combinations of agents that work by different pathways has been advocated (either as "add-on" therapy or initial "up front" therapy). Further, new therapeutic agents and treatment strategies are on the near horizon, aiming to further improve survival from the remarkable progress already seen.
[Mh] Termos MeSH primário: Anti-Hipertensivos/uso terapêutico
Hipertensão Pulmonar/tratamento farmacológico
Vasodilatadores/uso terapêutico
[Mh] Termos MeSH secundário: Aminorex/efeitos adversos
Depressores do Apetite/efeitos adversos
Dasatinibe
Epoprostenol/análogos & derivados
Epoprostenol/uso terapêutico
Hipertensão Pulmonar Primária Familiar
Fenfluramina/efeitos adversos
Predisposição Genética para Doença
Seres Humanos
Hipertensão Pulmonar/etiologia
Iloprosta/uso terapêutico
Fenilpropionatos/uso terapêutico
Piperazinas/uso terapêutico
Inibidores de Proteínas Quinases/efeitos adversos
Purinas/uso terapêutico
Pirazóis/uso terapêutico
Piridazinas/uso terapêutico
Pirimidinas/efeitos adversos
Pirimidinas/uso terapêutico
Fatores de Risco
Citrato de Sildenafila
Sulfonamidas/uso terapêutico
Sulfonas/uso terapêutico
Tiazóis/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antihypertensive Agents); 0 (Appetite Depressants); 0 (Phenylpropionates); 0 (Piperazines); 0 (Protein Kinase Inhibitors); 0 (Purines); 0 (Pyrazoles); 0 (Pyridazines); 0 (Pyrimidines); 0 (Sulfonamides); 0 (Sulfones); 0 (Thiazoles); 0 (Vasodilator Agents); 2DS058H2CF (Fenfluramine); 2SH16612I9 (Aminorex); BW9B0ZE037 (Sildenafil Citrate); DCR9Z582X0 (Epoprostenol); HW6NV07QEC (ambrisentan); JED5K35YGL (Iloprost); Q326023R30 (bosentan); RBZ1571X5H (Dasatinib); RU3FE2Y4XI (riociguat); RUM6K67ESG (treprostinil); Z9K9Y9WMVL (macitentan)
[Em] Mês de entrada:1404
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130917
[St] Status:MEDLINE
[do] DOI:10.1055/s-0033-1355439


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[PMID]:23436169
[Au] Autor:Hess C; Ritke N; Broecker S; Madea B; Musshoff F
[Ad] Endereço:Institute of Forensic Medicine, University of Bonn, Bonn, Germany. cohess@uni-bonn.de
[Ti] Título:Metabolism of levamisole and kinetics of levamisole and aminorex in urine by means of LC-QTOF-HRMS and LC-QqQ-MS.
[So] Source:Anal Bioanal Chem;405(12):4077-88, 2013 May.
[Is] ISSN:1618-2650
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The antihelminthic drug Levamisole can enhance cocaine effects by conversion into the amphetamine-like drug aminorex. We describe an LC-MS method for the determination of levamisole and its metabolite aminorex in human urine. Selectivity is given, calibration curves were linear within the calibration range 2.5-250 ng/mL; limits of the method were LoD 0.51 ng/mL, LoQ 1.02 ng/mL for levamisole and LoD 0.65 ng/mL, LoQ 0.76 ng/mL for aminorex. Precision data was in accordance with the guidelines (intraday precision for aminorex ranged between 5.75 and 11.0 % for levamisole between 8.36 and 10.9 %; interday precision for levamisole 10.9-16.9 % and for aminorex 7.64-12.7 %; accuracy data for levamisole -1.96 to -14.3 % and for aminorex-11.9 to-18.5 %). The validated method was successfully applied to study the urinary excretion of levamisole after the administration of 100 mg of levamisole orally. Levamisole and aminorex could be detected in post-administration urine samples. Levamisole could be detected up to 39 h after ingestion, while aminorex was detectable up to 54 h. Maximum aminorex concentrations were 45 ng/mL urine. Further metabolites of levamisole after oral ingestion by means of liquid chromatography hybrid quadrupole time-of-flight high-resolution mass spectrometry (LC-QTOF-HRMS) were identified. Only 0.5 % of the ingested drug was quantified as unchanged levamisole in urine. Besides aminorex, five isomers of aminorex and 4 hydroxy-metabolites of aminorex or its isomers were found. Furthermore, levamisole is also hydroxylated and eliminated free or conjugated with sulfate or glucuronide into urine.
[Mh] Termos MeSH primário: Aminorex/urina
Anti-Helmínticos/metabolismo
Anti-Helmínticos/urina
Levamisol/metabolismo
Levamisol/urina
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Aminorex/metabolismo
Anti-Helmínticos/administração & dosagem
Cromatografia Líquida/métodos
Seres Humanos
Levamisol/administração & dosagem
Limite de Detecção
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Anthelmintics); 2880D3468G (Levamisole); 2SH16612I9 (Aminorex)
[Em] Mês de entrada:1311
[Cu] Atualização por classe:160512
[Lr] Data última revisão:
160512
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130226
[St] Status:MEDLINE
[do] DOI:10.1007/s00216-013-6829-x


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[PMID]:21764154
[Au] Autor:Karch SB; Mari F; Bartolini V; Bertol E
[Ad] Endereço:Consultant Pathologist/Toxicologist, Berkeley, California, United States. skarch@fdaa.com
[Ti] Título:Aminorex poisoning in cocaine abusers.
[So] Source:Int J Cardiol;158(3):344-6, 2012 Jul 26.
[Is] ISSN:1874-1754
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Levamisole is found in more than 80% of illicit cocaine seized within United States borders. Percentages are somewhat lower in Europe. In 2009, controlled in vivo studies demonstrated that horses metabolize levamisole to aminorex. Earlier this year our laboratory demonstrated that the same conversion occurs in man. Levamisole itself causes aplastic anemia and numerous reports have begun to appear in the literature, but the conversion of levamisole to aminorex is of much more concern. Aminorex ingestion was responsible for a five-year epidemic (1967-1972) of idiopathic pulmonary hypertension (IPH) confined to Switzerland, Austria, and Germany, the only countries where aminorex had been marketed as an anorectic. The incidence of IPH reverted to normal levels as soon as aminorex was withdrawn. In most cases onset of symptoms in IPH began after six to nine months of aminorex use, with average dosage ranges of 10 to 40 mg per day. The outcome was almost uniformly fatal. The conversion rate of levamisole to aminorex has not been established, but given the high daily intake of cocaine by many abusers, it seems likely that many of them will have ingested enough contaminated cocaine to ultimately cause IPH. Until the disease is well established, the symptoms of IHP are vague, and existing drug registries specifically exclude drug abusers, making it difficult to track these cases. This review is intended to draw attention to what may be a slowly emerging new epidemic.
[Mh] Termos MeSH primário: Aminorex/envenenamento
Depressores do Apetite/envenenamento
Transtornos Relacionados ao Uso de Cocaína/epidemiologia
Epidemias/estatística & dados numéricos
Hipertensão Pulmonar/induzido quimicamente
[Mh] Termos MeSH secundário: Aminorex/metabolismo
Antirreumáticos/farmacocinética
Antirreumáticos/envenenamento
Depressores do Apetite/metabolismo
Contaminação de Medicamentos
Hipertensão Pulmonar Primária Familiar
Seres Humanos
Levamisol/farmacocinética
Levamisol/envenenamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antirheumatic Agents); 0 (Appetite Depressants); 2880D3468G (Levamisole); 2SH16612I9 (Aminorex)
[Em] Mês de entrada:1302
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110719
[St] Status:MEDLINE
[do] DOI:10.1016/j.ijcard.2011.06.105


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[PMID]:21531521
[Au] Autor:Bertol E; Mari F; Milia MG; Politi L; Furlanetto S; Karch SB
[Ad] Endereço:Division of Forensic Toxicology, Department of Anatomy, Histology and Legal Medicine, University of Florence, Italy. elisabetta.bertol@unifi.it
[Ti] Título:Determination of aminorex in human urine samples by GC-MS after use of levamisole.
[So] Source:J Pharm Biomed Anal;55(5):1186-9, 2011 Jul 15.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The Drug Enforcement Administration (DEA) reports that as of October 2010, 79% of all cocaine seized in the United States contained levamisole. The equine conversion of levamisole to aminorex has been demonstrated. However, the metabolic fate of levamisole in humans is unknown. Nevertheless, as aminorex is amphetamine-like and hallucinogenic, it may be used as an adulterant to increase the effects of cocaine. We report here the results of in vivo studies demonstrating for the first time that not only equine, but also canine and human metabolism all result in aminorex formation. Levamisole and aminorex were extracted from real urine samples by liquid-liquid extraction and identified and quantified by GC-MS (identification by 3 ions per substance, LLOQ at 0.15ng/ml for both).
[Mh] Termos MeSH primário: Aminorex/urina
Cromatografia Gasosa-Espectrometria de Massas/métodos
Levamisol/urina
[Mh] Termos MeSH secundário: Adulto
Animais
Cocaína/urina
Cães
Contaminação de Medicamentos
Feminino
Seres Humanos
Masculino
Meia-Idade
Modelos Químicos
Transtornos Relacionados ao Uso de Substâncias/urina
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
2880D3468G (Levamisole); 2SH16612I9 (Aminorex); I5Y540LHVR (Cocaine)
[Em] Mês de entrada:1109
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110503
[St] Status:MEDLINE
[do] DOI:10.1016/j.jpba.2011.03.039



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