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Metabolic Studies of Nandrolone Decanoate in Castrated Horses After Intramuscular Administration. 癸酸诺龙在去势马肌肉内的代谢研究。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-07-01 DOI: 10.1002/dta.3919
Yat-Ming So, Wai Him Kwok, Christina W Y Tang, Celia O L Wong, Terence S M Wan, Emmie N M Ho
{"title":"Metabolic Studies of Nandrolone Decanoate in Castrated Horses After Intramuscular Administration.","authors":"Yat-Ming So, Wai Him Kwok, Christina W Y Tang, Celia O L Wong, Terence S M Wan, Emmie N M Ho","doi":"10.1002/dta.3919","DOIUrl":"https://doi.org/10.1002/dta.3919","url":null,"abstract":"<p><p>This paper describes the studies of the in vitro biotransformation of nandrolone decanoate and its metabolic fate in equine plasma and urine after intramuscular administration to castrated thoroughbred horses. The in vitro metabolic study was performed using homogenised horse liver, and the more prominent in vitro biotransformation pathways were found to include hydrolysis, reduction, oxidation and sulfation, mainly resulting in seven Phase I metabolites and one Phase II metabolite. The administration study of nandrolone decanoate was carried out using three retired thoroughbred geldings, each of which was administered intramuscularly with 800 mg of nandrolone decanoate (Deca-Durabolin) once weekly for three consecutive weeks. Nandrolone decanoate and the majority of the identified in vitro metabolites were detectable in post-administration plasma samples for at least 20 days (last sample collected) after the last administration. Although nandrolone decanoate was not found in any post-administration urine, nandrolone (as a metabolite) and its downstream metabolites can be detected for at least 20 days post-administration (last sample collected). For doping control purpose, nandrolone decanoate itself could be a suitable target analyte in horse plasma for effectively controlling its misuse in equine sports.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144525713","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Toward a Cannabis Terroir: Untargeted Metabolomic Profiling of Authentic Samples Using Gas Chromatography-High-Resolution Mass Spectrometry (GC-HRMS) and Liquid Chromatography-High-Resolution Tandem Mass Spectrometry (LC-HRMS/MS). 走向大麻风土:使用气相色谱-高分辨率质谱(GC-HRMS)和液相色谱-高分辨率串联质谱(LC-HRMS/MS)对真实样品进行非靶向代谢组学分析。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-06-30 DOI: 10.1002/dta.3922
Sandra N Poetzsch, Michael Poetzsch, Thomas Kraemer, Andrea E Steuer
{"title":"Toward a Cannabis Terroir: Untargeted Metabolomic Profiling of Authentic Samples Using Gas Chromatography-High-Resolution Mass Spectrometry (GC-HRMS) and Liquid Chromatography-High-Resolution Tandem Mass Spectrometry (LC-HRMS/MS).","authors":"Sandra N Poetzsch, Michael Poetzsch, Thomas Kraemer, Andrea E Steuer","doi":"10.1002/dta.3922","DOIUrl":"https://doi.org/10.1002/dta.3922","url":null,"abstract":"<p><p>Cannabis sativa L. constituents, such as cannabinoids, terpenes, flavonoids, and other secondary metabolites, determine the plant's (medicinal) effects and properties in a complex interplay, a phenomenon known as the entourage effect. However, environmental influences like cultivation method, soil, light, and climate might also influence the plant's chemical composition-and thus its therapeutic profile. Much like in viticulture, the concept of a \"cannabis terroir\" might play an important role in determining the plant's chemical phenotype. The aim of this study was therefore to make these complex properties analytically accessible and develop a comprehensive metabolomics workflow using gas chromatography-high-resolution mass spectrometry (GC-HRMS) and liquid chromatography-high-resolution tandem mass spectrometry (LC-HRMS/MS) in positive and negative ionization mode, applying HILIC and reversed phase chromatography to assess multiple chemical classes. Data processing and statistical analysis were done in MS-DIAL and MetaboAnalyst, respectively. The method was applied to 35 CBD-type cannabis flowers grown under different environmental conditions, and compounds belonging to various chemical classes were successfully detected. Principal component analysis revealed distinct clustering of the samples, and key discriminative features were identified, including cannabinoids, terpenes such as β-caryophyllene and α-humulene, cuticular alkanes (e.g., pentacosane and nonacosane), and polar compounds such as choline and trigonelline. The markers enabled a discrimination of samples not only by chemical phenotype but also by cultivation environment, supporting the emerging concept of a cannabis terroir. In conclusion, this study introduces an analytical framework for the comprehensive chemical profiling of cannabis employing GC-HRMS and LC-HRMS analysis and advanced statistical techniques.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144525714","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
SARMs, Metabolic Modulators and Growth Hormone Secretagogues in Suspected Illegal Medicines, Bought as Sport Performance Enhancers: A Retro- and Prospective Study Within the GEON. SARMs,代谢调节剂和生长激素分泌剂涉嫌非法药物,作为运动成绩增强剂购买:在GEON的回顾性和前瞻性研究。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-06-23 DOI: 10.1002/dta.3918
M Mendoza Barrios, E Deconinck, C Vanhee, E K Lamme, I 't Hart-Bakker, P V Syversen, O Bøyum, G Li-Ship, S Young, A Blazewicz, M Poplawska, B Hakkarainen, N Hang Huynh, A Hackl, M J Portela, P Martinho, N Beerbaum, M C Gaudiano, M Raimondo, V Marleau, J Cloutier, J Ollerenshaw, A Hansen, J Mills, M Aha, C Luchte, M Miquel
{"title":"SARMs, Metabolic Modulators and Growth Hormone Secretagogues in Suspected Illegal Medicines, Bought as Sport Performance Enhancers: A Retro- and Prospective Study Within the GEON.","authors":"M Mendoza Barrios, E Deconinck, C Vanhee, E K Lamme, I 't Hart-Bakker, P V Syversen, O Bøyum, G Li-Ship, S Young, A Blazewicz, M Poplawska, B Hakkarainen, N Hang Huynh, A Hackl, M J Portela, P Martinho, N Beerbaum, M C Gaudiano, M Raimondo, V Marleau, J Cloutier, J Ollerenshaw, A Hansen, J Mills, M Aha, C Luchte, M Miquel","doi":"10.1002/dta.3918","DOIUrl":"https://doi.org/10.1002/dta.3918","url":null,"abstract":"<p><p>Although the abuse of muscle-building compounds in elite sports is already known for a long time, these products have become more popular in recreational sport over the past years. Although anabolic steroids are still the most popular ones in this context, the use of other molecules with anabolic properties is on the rise. Three categories of such products are the selective androgen receptor modulators (SARMs), the metabolic modulators and the growth hormone secretagogues (GHS). Based on this trend and the outcomes of a previous market surveillance study in the domain of illegal products (MSSIP), the Falsified Medicines Working Group of the General European Official Medicines Control Laboratories (OMCL) Network (GEON) decided to conduct an MSSIP with focus on SARMs, metabolic modulators and GHS over a period of 5 years. In total 324 samples and 354 results, reported by 14 laboratories in 13 countries, members of the GEON, were taken into account, for which the majority of the samples originated from illegal distribution. Sixty-five percent of the seized products were represented as medicine, though 24% as dietary supplements, which is of concern because here the (recreational) sporter is not aware he is taking an (unapproved) pharmaceutical. Eighteen different molecules, within the scope of the study, were reported with as top 5: ibutamoren, ligandrol, ostarine, cardarine and andarine. From the limited quantitative data reported, it can be assumed that the majority of the samples contain active doses and some are even overdosed, so health risks for the consumers cannot be neglected.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144473530","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Monitoring Community Use of Benzodiazepines Through Wastewater-Based Epidemiology. 通过基于废水的流行病学监测社区苯二氮卓类药物的使用。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-06-18 DOI: 10.1002/dta.3915
Maarten Quireyns, Tim Boogaerts, Natan Van Wichelen, Diāna Vanaga-Arāja, Olesia Rudminienė, Ruxanda Iliescu, Milica Georgescu, Sofie Schaerlaekens, Naomi De Roeck, Peter Delputte, Adrian Covaci, Alexander L N van Nuijs
{"title":"Monitoring Community Use of Benzodiazepines Through Wastewater-Based Epidemiology.","authors":"Maarten Quireyns, Tim Boogaerts, Natan Van Wichelen, Diāna Vanaga-Arāja, Olesia Rudminienė, Ruxanda Iliescu, Milica Georgescu, Sofie Schaerlaekens, Naomi De Roeck, Peter Delputte, Adrian Covaci, Alexander L N van Nuijs","doi":"10.1002/dta.3915","DOIUrl":"https://doi.org/10.1002/dta.3915","url":null,"abstract":"<p><p>Benzodiazepines and related z-drugs (BZDs) are widely used pharmaceuticals but require careful monitoring due to limited efficacy, tolerance development and the risk of dependence. Wastewater-based epidemiology (WBE) is a valuable approach to gather population-wide information on consumption patterns through analysis of influent wastewater. This study examines how overlapping metabolic pathways within the BZD drug class can lead to misinterpretation if not carefully considered. An analytical method is developed and validated for 26 biomarkers of prescription BZDs in influent wastewater using solid-phase extraction and liquid chromatography-tandem mass spectrometry and applied to influent wastewater samples for the first time in Belgium (13 locations), Latvia (1), Lithuania (3) and Romania (1). The countries were chosen for their differing prescription BZD market registration, allowing testing of different hypotheses. To aid in complex data interpretation, this study presents a structured categorisation of BZDs into direct biomarkers, which directly reflect consumption, and downstream biomarkers, which are influenced by multiple BZDs, and further discusses the implication this has on the interpretation. Spatial differences were noted among direct biomarkers such as higher consumption of zolpidem in Belgium and zopiclone in Riga (LVA). Downstream biomarkers had higher population-normalised mass loads but cannot be interpreted in isolation, for example, lorazepam (ranging 4-25 mg/day/1000 inhabitants over all locations), lormetazepam (8-30), oxazepam (10-50) and temazepam (1-12). These findings highlight challenges in interpreting BZD consumption trends and emphasise the need of distinguishing different biomarker classes to ensure accurate and comparable results across studies needed to guide informed decision-making.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144324004","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development of an Optimized Extraction Method to Recover Drug Material From Used Test Strips for Comprehensive Drug Checking. 综合药检用试纸中药物提取方法的优化研究。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-06-18 DOI: 10.1002/dta.3911
Meghan G Appley, Elise M Pyfrom, Rae A Elkasabany, Rick Rousch, Edward Sisco
{"title":"Development of an Optimized Extraction Method to Recover Drug Material From Used Test Strips for Comprehensive Drug Checking.","authors":"Meghan G Appley, Elise M Pyfrom, Rae A Elkasabany, Rick Rousch, Edward Sisco","doi":"10.1002/dta.3911","DOIUrl":"https://doi.org/10.1002/dta.3911","url":null,"abstract":"<p><p>Drug-checking programs use point-of-need testing (e.g., test strips) and laboratory-based analysis to rapidly identify emerging drug threats, but each has limitations. Test strips are quick but compound or class specific, whereas laboratory testing can identify more compounds but have lengthy turnaround times. To address these limitations, it was proposed that compounds could be extracted from used test strips for additional analyses allowing for rapid on-site information followed by comprehensive laboratory results. The method development process involved four parts: determining the optimal extraction approach, assessing the feasibility of performing direct analysis in real-time mass spectrometry (DART-MS) analysis on extracts, determining the limits of detection (LODs) for a range of analytes, and evaluating the method using used test strips submitted by harm reduction sites. The optimized method consisted of extracting analytes of interest from a cut test strip using 0.5-mL methanol while vortexing for 10 s. DART-MS successfully identified the compounds of interests, and the test strip chemical background was identified. LODs were found to be as low as a mass fraction of 0.005 in a mixture. For the samples submitted by harm reduction sites, concordance between extracts and test strip results was 96%, and the agreement in compound identification between used test strip extracts and authentic drug collection samples was approximately 80% regardless of test strip type and preparation. This work shows that additional analyses of extracted test strips can provide a low-barrier way for high-quality testing that can be used to increase data on the drug landscape.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144324003","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Analysis of Methyltestosterone and Testosterone Propionate in Dried Blood Spots After Transdermal Application. 经皮应用后干血斑中甲基睾酮和丙酸睾酮含量分析。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-06-05 DOI: 10.1002/dta.3914
Asami Miyamoto, Masato Okano, Masanori Ota, Mitsuhiko Sato
{"title":"Analysis of Methyltestosterone and Testosterone Propionate in Dried Blood Spots After Transdermal Application.","authors":"Asami Miyamoto, Masato Okano, Masanori Ota, Mitsuhiko Sato","doi":"10.1002/dta.3914","DOIUrl":"https://doi.org/10.1002/dta.3914","url":null,"abstract":"<p><p>In the past few years, doping tests have been performed with dried blood spots (DBS) as test samples; this sampling method is minimally invasive and requires minimal storage space. Steroid esters are stable in dried blood, allowing the direct analysis of testosterone esters. In Japan, the cream-based formulation containing 17α-methyltestosterone (MeT) and testosterone propionate (TP) is available as an over-the-counter drug for hair growth. Here, we investigated whether the transdermal uptake of this formulation could be detected using the existing method for steroid ester analysis in DBS. A method that was previously validated to detect and identify TP could also detect MeT. We developed a high throughput liquid chromatography-tandem mass spectrometry method to identify MeT in DBS. The limits of detection and identification of MeT were 0.1 ng/mL and 0.6 ng/mL, respectively. Five male human subjects received the cream-based formulation of MeT and TP transdermally. We then collected blood samples by finger pricking and made DBS on cellulose paper. Using this method, MeT was detected and identified up to 97 h after the final application. TP was also detected up to 97 h and identified up to 49 h after the final application. The developed method provides a direct confirmation of the presence of the drug. Moreover, using cream preparations could lead to contamination from MeT and TP remaining on the fingertip skin during fingertip puncture sampling.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144232782","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Detection of Transdermal Application of Testosterone to Racehorses by Analysis of Urine and Plasma. 通过尿液和血浆分析检测经皮给药赛马的睾酮。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-06-03 DOI: 10.1002/dta.3905
Marjaana Viljanto, Charlotte Cutler, Jocelyn Habershon-Butcher, Pamela Hincks, James Scarth
{"title":"Detection of Transdermal Application of Testosterone to Racehorses by Analysis of Urine and Plasma.","authors":"Marjaana Viljanto, Charlotte Cutler, Jocelyn Habershon-Butcher, Pamela Hincks, James Scarth","doi":"10.1002/dta.3905","DOIUrl":"https://doi.org/10.1002/dta.3905","url":null,"abstract":"<p><p>The use of testosterone in racehorses is predominantly monitored using international urine and plasma concentration-based thresholds and complementary steroid ratios. To date, there has been no published pharmacokinetic study on transdermally applied testosterone products in horses and whether their use could result in adverse analytical findings. Therefore, quantitative analysis of testosterone and epitestosterone in urine and testosterone in plasma samples was performed following a pilot multi-dose transdermal Testogel administration (1 mg/kg once a day for 7 days on clipped skin) to one gelding and one mare. The peak concentrations (C<sub>max</sub>) of free testosterone were 1060 and 1800 pg/mL in gelding and mare plasma, respectively. Testosterone concentrations exceeded the international plasma threshold of 100 pg/mL consistently for up to 4 h post-administration, after which detection above the threshold was sporadic up to 127 h. In urine, C<sub>max</sub> of free and conjugated (sulfate and glucuronide) testosterone were 700 and 323 ng/mL in gelding and mare urine, respectively. In the gelding, testosterone concentrations exceeded the international urine threshold of 20 ng/mL consistently for up to 47 h post-administration, but sporadically up to 143 h. In all samples, testosterone: epitestosterone ratios were greater than 5, another requirement for adverse analytical findings in geldings. In the mare, testosterone concentrations exceeded the urine threshold of 55 ng/mL consistently for up to 71 h post-administration, but sporadically up to 167 h. Therefore, these limited results for one gelding and one mare demonstrate that doping control following transdermal applications of testosterone to racehorses is possible using existing approaches.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144214492","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A "Pheraplex" Capsule Labeled as Desoxymethyltestosterone From the Market Turned Out to Be 17,17-Dimethyl-18-nor-5α-androst-13-en-3β-ol. 市场上一种标记为脱氧甲基睾酮的“Pheraplex”胶囊原来是17,17-二甲基-18-no -5α-androst-13-en-3β-醇。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-05-23 DOI: 10.1002/dta.3912
Sisi Zhu, Shan Wang, Xin Liu, Lisi Zhang
{"title":"A \"Pheraplex\" Capsule Labeled as Desoxymethyltestosterone From the Market Turned Out to Be 17,17-Dimethyl-18-nor-5α-androst-13-en-3β-ol.","authors":"Sisi Zhu, Shan Wang, Xin Liu, Lisi Zhang","doi":"10.1002/dta.3912","DOIUrl":"https://doi.org/10.1002/dta.3912","url":null,"abstract":"<p><p>In an effort to conduct a desoxymethyltestosterone (DMT) administration study to replenish excretion urine inventory of Beijing Anti-Doping Laboratory for quality assurance purpose, a product labeled as \"Pheraplex\" was purchased from the internet. The product's label indicated that each capsule contained 10 mg of 17α-methyl-etioallocholan-2-ene-17β-ol (DMT), along with medicinal corn starch and gelatin. To verify the product's contents, gas chromatography tandem quadrupole mass spectrometry (GC-MS/MS) was employed to analyze the active ingredient and compare it with the reference materials of DMT. Surprisingly, the results revealed that the product did not contain DMT or any other steroids monitored in the initial testing procedure of our laboratory. Subsequently, nuclear magnetic resonance was utilized to identify the compound's structure, which was determined to be 17,17-dimethyl-18-nor-5α-androst-13-en-3β-ol. This compound was referred to as M10 of 17α-methyltestosterone in a literature. This finding highlights the potential discrepancies between product labeling and actual contents in the supplement market, which deserves attention from the anti-doping community.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144126116","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Doping Control of Ranitidine in Horses. 马用雷尼替丁的兴奋剂控制。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-05-20 DOI: 10.1002/dta.3909
Helen S M Ho, James X Mizzi, Emmie N M Ho, Wing-Tak Wong
{"title":"Doping Control of Ranitidine in Horses.","authors":"Helen S M Ho, James X Mizzi, Emmie N M Ho, Wing-Tak Wong","doi":"10.1002/dta.3909","DOIUrl":"https://doi.org/10.1002/dta.3909","url":null,"abstract":"<p><p>Ranitidine is a histamine H<sub>2</sub>-receptor antagonist commonly used to treat gastric ulceration in horses. The author's laboratory conducted a study some years ago in the early 2000s on its metabolism as well as its urinary elimination profile in two geldings. With the technology advancement as well as popularity of blood for doping control testing, the laboratory has recently conducted another administration trials of the substance in six horses to study the in vivo metabolism of ranitidine, aiming to identify and reinvestigate the appropriate target(s) for controlling misuse of ranitidine in horses as well as to study its elimination in blood. To study the elimination and biotransformation of ranitidine, administration experiments were performed by giving six castrated horses (geldings) each 25 mL of Ulcerguard oral paste (equivalent to 9.8 g of ranitidine) in the morning and 20 mL of oral paste (equivalent to 7.9 g of ranitidine) in the afternoon daily for eight consecutive days. The postulated in vivo metabolites included ranitidine-S-oxide (M1), ranitidine-N-oxide (M2), desmethylranitidine (M3a/b) and furoic acid analogue of ranitidine (M4), resulting from oxidation, demethylation and oxidative deamination of ranitidine. To control the misuse of ranitidine in horses, elimination profiles of urinary and plasma ranitidine were established. Free ranitidine was detectable for at most 8 days and 72 h in urine and plasma, respectively. Both metabolites ranitidine-S-oxide and ranitidine-N-oxide were detected for 8 days, and therefore, they could be monitored alongside the parent drug as evidence that the substance has gone through the horse's body.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144109279","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Identification of the Novel Synthetic Opioid N-Pyrrolidino Isotonitazene at an Australian Drug Checking Service. 新型合成阿片类药物n -吡咯利迪诺异戊二烯在澳大利亚药品检验中心的鉴定。
IF 2.6 3区 医学
Drug Testing and Analysis Pub Date : 2025-05-19 DOI: 10.1002/dta.3910
Blake Curtis, Douglas J Lawes, David Caldicott, Malcolm D McLeod
{"title":"Identification of the Novel Synthetic Opioid N-Pyrrolidino Isotonitazene at an Australian Drug Checking Service.","authors":"Blake Curtis, Douglas J Lawes, David Caldicott, Malcolm D McLeod","doi":"10.1002/dta.3910","DOIUrl":"https://doi.org/10.1002/dta.3910","url":null,"abstract":"<p><p>2-Benzylbenzimidazole opioids and related derivatives, also known as 'nitazenes', present a growing threat to public health. Emerging in Europe in 2019, the nitazene group of drugs is a recent addition to the novel synthetic opioid class and has been associated internationally with adverse effects in drug users, overdose clusters and significant mortality. The high potency of many nitazene derivatives, which can in many cases exceed that of fentanyl, poses a significant challenge to the public health and early warning systems used to detect and respond to the emergence of new high-risk substances. This report describes close collaboration between an Australian drug checking service and a nearby university laboratory to identify and characterise the novel synthetic opioid N-pyrrolidino isotonitazene in an expected oxycodone sample presented by a member of the public. Though no prior publications are available describing the presence of this nitazene in the drug market, previously reported in vitro evaluation of this compound reveals it to be among the most potent nitazene opioid agonists known. The study highlights the rapid response possible though engaging drug users with drug checking services as a market monitor and early warning system to alert health services and the broader community to the presence of unexpected, high-risk substances. Integration of well-resourced and supported drug checking services provides a powerful approach to tackle the public health threats associated with novel synthetic opioids and other drugs of concern.</p>","PeriodicalId":160,"journal":{"name":"Drug Testing and Analysis","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144092377","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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