Overdose deaths following previous non‐fatal heroin overdose: Record linkage of ambulance attendance and death registry data

Introduction and Aims. Experiencing previous non‐fatal overdoses have been identified as a predictor of subsequent non‐fatal overdoses; however, few studies have investigated the association between previous non‐fatal overdose experiences and overdose mortality. We examined overdose mortality among injecting drug users who had previously been attended by an ambulance for a non‐fatal heroin overdose. Design and Methods. Using a retrospective cohort design, we linked data on non‐fatal heroin overdose cases obtained from ambulance attendance records in Melbourne, Australia over a 5‐year period (2000–2005) with a national death register. Results. 4884 people who were attended by ambulance for a non‐fatal heroin overdose were identified. One hundred and sixty‐four overdose deaths occurred among this cohort, with an average overdose mortality rate of 1.20 per 100 person‐years (95% CI, 1.03–1.40). Mortality rate decreased 10‐fold after 2000 coinciding with widely reported declines in heroin availability. Being male, of older age (>35 years) and having been attended multiple times for previous non‐fatal overdoses were associated with increased mortality risk. Discussion and Conclusions. As the first to show a direct association between non‐fatal overdose and subsequent overdose mortality, this study has important implications for the prevention of overdose mortality. This study also shows the profound effect of macro‐level heroin market dynamics on overdose mortality.[Stoové MA, Dietze PM, Jolley D. Overdose deaths following previous non‐fatal heroin overdose: Record linkage of ambulance attendance and death registry data. Drug Alcohol Rev 2009;28:347–352]     

Availability of Paracetamol Sold Over the Counter in Europe: A Descriptive Cross‐Sectional International Survey of Pack Size Restriction

Due to the risk of hepatotoxicity when excessive amounts of paracetamol are consumed, Poisons Information Centers (PICs) frequently receive paracetamol‐related enquiries. This study examined how widely pack size restrictions of paracetamol sold over the counter have been implemented in Europe and also availability of paracetamol through non‐pharmacy outlets and their possible associations with frequency of poisoning enquiries. A cross‐sectional European multi‐centre questionnaire study was performed using a questionnaire to identify the extent and nature of paracetamol pack size restrictions, non‐pharmacy outlet sales and the frequency of paracetamol‐related enquiries to PICs. In total, 21 European countries participated. All PICs provided telephone hotline services. In 14 (67%) countries, pack size restrictions had been implemented in pharmacies (range: 8–30 g). No significant difference (median difference 0.7%, p‐value = 0.36) was found when comparing median frequencies of paracetamol‐related enquiries in countries with pack size restriction to countries without restrictions. A significantly lower median frequency of paracetamol‐related enquiries was found in countries without non‐pharmacy outlet sales compared to those with such sales (median difference 2.2%, p = 0.02). Pack size restrictions on pharmacy sales of paracetamol have been implemented in two‐thirds of examined countries. There was no difference in the proportion of paracetamol‐related enquiries to PICs among countries with and without pack size restrictions. However, a lower rate of paracetamol‐related enquiries was noted in countries where paracetamol was not available in non‐pharmacy outlets.     

Using suitability profiles to better inform consumers' choice of commonly used over‐the‐counter analgesics

Objective To quantify the impact of labelled contraindications, precautions and warnings for use on the population that may take commonly used over‐the‐counter (OTC) analgesics. Setting Primary care: data were collected from a general practitioner database in Australia. Methods Patient data were audited retrospectively (n = 107553) to determine the number of patients with contraindications, warnings or precautions to the use of OTC paracetamol and the non‐steroidal anti‐inflammatory drugs aspirin and ibuprofen. The primary outcome measure was the suitability rate (i.e. the proportion of patients with no contraindications, warnings or precautions) of these commonly used analgesics. Key findings In this Australian dataset, the proportions of patients who had no contraindications, warnings or precautions to the use of paracetamol or ibuprofen were 98.1 and 76.9%, respectively (P = 0.0001); 83.4% of patients had no contraindications, warnings or precautions to the use of aspirin (P = 0.005 compared with paracetamol). Conclusion Of the three OTC analgesics examined, paracetamol is suitable for use by a larger proportion of the general population without the need to seek medical advice.     

In vitro evaluation of the effects of anti‐fungals,benzodiazepines and non‐steroidal anti‐inflammatory drugs on the glucuronidation of 19‐norandrosterone: implications on doping control analysis

We have studied whether the phase II metabolism of 19‐norandrosterone, the most representative metabolite of 19‐nortestosterone (nandrolone), can be altered in the presence of other drugs that are not presently included on the Prohibited List of the World Anti‐Doping Agency. In detail, we have evaluated the effect of non‐prohibited drugs belonging to the classes of anti‐fungals, benzodiazepines, and non‐steroidal anti‐inflammatory drugs on the glucuronidation of 19‐norandrosterone. In vitro assays based on the use of either pooled human liver microsomes or specific recombinant isoforms of uridine diphosphoglucuronosyl‐transferase were designed and performed to monitor the formation of 19‐norandrosterone glucuronide from 19‐norandrosterone. Determination of 19‐norandrosterone (free and conjugated fraction) was performed by gas chromatography – mass spectrometry after sample pretreatment consisting of an enzymatic hydrolysis (performed only for the conjugated fraction), liquid/liquid extraction with tert‐butylmethyl ether, and derivatization to form the trimethylsilyl derivative. In parallel, a method based on reversed‐phase liquid chromatography coupled to tandem mass spectrometry in positive electrospray ionization with acquisition in selected reaction monitoring mode was also developed to identify the non‐prohibited drugs considered in this study. Incubation experiments have preliminarily shown that the glucuronidation of 19‐norandrosterone is principally carried out by UGT2B7 (39%) and UGT2B17 (31%). Inhibition studies have shown that the yield of the glucuronidation reaction is reduced in the presence of the anti‐fungals itraconazole, ketoconazole, and miconazole, of the benzodiazepine triazolam and of the non‐steroidal anti‐inflammatory drugs diclofenac and ibuprofen, while no alteration was recorded in the presence of all other compounds considered in this study. Copyright © 2015 John Wiley & Sons, Ltd.     

Non‐Fatal Suicidal Self‐Poisonings in Children and Adolescents over a 5‐Year Period (2007–2011)

The objective of this study was to analyse non‐fatal suicidal self‐poisonings in children and adolescents and to identify commonalities that might direct preventive health efforts. From the database of the Czech Toxicological Information Center, the inquiries due to non‐fatal suicidal self‐poisonings in children (9–13 years old) and adolescents (14–18 years old) in 2007–2011 were evaluated. From 10,492 calls about suicide attempts, 2393 concerned children and adolescents (13.5% and 86.5%, respectively). Most suicide attempts were committed during the spring (31.3%). Among toxic agents, drugs were used in 97.8% of the cases. 63% of cases involved monopoisonings and combinations of more than three drugs (10.3%) were rare. The most frequent ingestions appeared using drugs affecting the nervous system and anti‐inflammatory non‐steroids. The dose was evaluated as toxic in 73.4% of the cases and as severely toxic in 3.0% of the cases. The symptoms of moderate and severe intoxications were present in 10.5% of the cases. First aid was provided in 5.6%, and gastric lavage was performed in 21.9% of the cases. Antidotes were indicated in 13.3% and secondary elimination methods in 4.4% of the cases. Mostly, one or two easily accessible drugs were used in suicide attempts, with paracetamol and ibuprofen were the most common ones. Only one in 10 children applied a non‐toxic dose. One‐fifth of the patients received medical care within 60 min. and one‐third later than 4 hr after exposure. The time criterion for gastric lavages was fulfilled in less than half of the cases, and in every fourth case, the procedure was performed when it was unlikely to be beneficial.     

Drug‐Related Inadvertent Deaths in a University Hospital – A Declining Trend

We studied the incidence of fatal adverse drug reactions (ADRs) in a tertiary hospital to find out which drugs were involved. The secondary objective was to compare the data from the same hospital published 12 years earlier. All 1708 death cases in the Helsinki University Central Hospital during the year 2012 were retrospectively evaluated. All suspected drug‐related deaths, excluding suicides, were scrutinized by an expert panel using the WHO ADR probability classification. Of all cases, 52 (3.0%) were classified as certainly or probably drug related and 24 (1.4%) as possibly drug related. Together, these corresponded to 0.02% of all hospital admissions. The most commonly involved drugs in certain or probable cases were cytostatics (18 cases, 1.1% of all cases) and antithrombotics (17, 1.0%). Twelve years earlier, these caused 27 (1.8%) and 22 (1.5%) cases, respectively. Non‐steroidal anti‐inflammatory drugs (NSAIDs) and glucocorticoids caused less (2 and 0 cases) fatal ADRs than earlier (12 and 4 cases, p = 0.048 and p = 0.005, respectively). Most of the ADRs leading to death were present already in admission and affected seriously ill or elderly patients. Hospital‐born fatal ADRs occurred in 0.003% of patients. In conclusion, cytostatics and antithrombotics are still the leading causes of fatal ADRs, but NSAIDs and glucocorticoids seem to cause fatal ADRs less often than previously. The incidence of fatal ADRs in 2012 was 3.0% of all deaths, suggesting a decline compared to the 2000 value (5.0%). Improved awareness, prevention and treatment of ADRs and safer medicines may explain these declining trends.     

Patients' concerns about and problems experienced with discontinuation of antidepressants

Objective Clinical trials and epidemiological studies have shown that premature discontinuation is a major problem during antidepressant therapy. Unfortunately, there is little information on how patients perceive treatment with antidepressants in clinical practice, and it is unclear whether patients perceive discontinuation as a problem. The objective of this study is to assess whether concerns and problems experienced with drug discontinuation occur more frequently in patients using antidepressants than in patients using benzodiazepines, antipsychotics or non‐psychiatric medication. Method All calls to a national telephone medicines information service received between 1990 and 2004 were examined using retrospective examination. Calls about discontinuation were identified and classified either as a general question about discontinuation, or as a problem experienced with discontinuation. These calls were grouped into the following main classes: antidepressants, antipsychotics, benzodiazepines or non‐psychiatric medicines. Key findings Of all 39 786 registered phone calls, 6159 (15,5%) related to antidepressants, 1658 (4.2%) to antipsychotics and 3916 (9.8%) to benzodiazepines. Patients calling about antidepressants called about discontinuation three times as often (odds ratio (OR) 2.8; 95% confidence interval (CI) 2.6–3.0), and reported a problem with discontinuation five times more often (OR 5.4; 95% CI 4.6–6.3), compared to patients who called about non‐psychiatric medicines. The proportion of questions about discontinuation and problems experienced with discontinuation was also higher in patients calling about benzodiazepines and antipsychotics compared to patients calling about non‐psychiatric medication. Conclusion Patients perceive discontinuation of antidepressants, as well as discontinuation of antipsychotics and benzodiazepines, as a problem. Discontinuation seems a general problem for all psychiatric medicines, and needs more attention in the communication between patients and healthcare providers.     

Synthesis,quality control and in vivo evaluation of [123I] rhTIMP‐2, a potential tumour‐imaging agent

Matrix metalloproteinases (MMPs) are enzymes involved in the turnover of the extracellular matrix. Their overexpression in tumours may provide a target for diagnostic imaging by using labelled MMP inhibitors. MMPs are inhibited by endogenous tissue inhibitors of metalloproteinases (TIMPs). The enhanced production of MT1‐MMP, located on the surface of cells within or in the direct vicinity of the tumour, and the high affinity interaction between TIMP‐2 and MT1‐MMP suggested that TIMP‐2 could be a potential agent for non‐invasive monitoring of cancer MMP levels, diagnosis of primary and secondary tumours and tumour response to MMP inhibitor therapy. There is also evidence that ¹²⁵I‐rhTIMP‐2 internalizes, which is an important feature for its possible use as a radiotherapeuticum if labelled with ¹³¹I. Labelling of rhTIMP‐2 was performed using the iodogen method resulting in a radiochemical yield of 51.1±11.8% (n=5) and a radiochemical purity of >98%. The trichloroacetic acid (TCA) precipitability of ¹²³I rhTIMP‐2 was 95.2%. SDS‐PAGE confirmed the correct size (21 kDa) of the purified ¹²³I rhTIMP‐2 without degradation. HPLC showed one radioactive peak with a retention time corresponding to the non‐labelled rhTIMP‐2. In vivo biodistribution showed no long‐term accumulation in organs and the possibility to accumulate in the tumour. These results show the potential of ¹²³I rhTIMP‐2 as tumour‐imaging agent. Copyright © 2005 John Wiley & Sons, Ltd.     

Using ambulance attendances to recruit people who have experienced non-fatal heroin overdose

AIMS: To trial two novel methods of recruiting people who experience non-fatal heroin overdose through the ambulance service. SETTING: Melbourne and Sydney, Australia. METHODS: In Melbourne potential participants were given numbered contact cards by ambulance paramedics after revival, while in Sydney potential participants were approached after revival by a researcher who travelled with ambulance paramedics to the overdose scene. RESULTS: In Melbourne 281 cards were distributed during the period 1 June 1998-31 December 1998 and a subsequent contact rate of 24% was achieved with 14% attending a subsequent interview. In Sydney there were 170 initial contacts of which 139 (82%) answered a series of questions asked at the scene (the remainder either ineligible or incapable of answering questions) with 48 (35%) also attending for follow-up interviews. CONCLUSIONS: Recruitment through contact with ambulance services is a novel method of recruiting heroin users for research into non-fatal heroin overdose with advantages over other methods of sampling for research on non-fatal heroin overdose.     

Enhancement of Vancomycin Activity by Phenothiazines against Vancomycin‐Resistant Enterococcus Faecium in vitro

Abstract: The antimicrobial and resistance‐reversal activities of seven phenothiazine derivatives were evaluated against vancomycin‐sensitive Enterococcus faecalis ATCC 29212, vancomycin resistant E. faecalis ATCC 51299 and ten vancomycin‐resistant E. faecium strains originating from human infections. Minimum inhibitory concentrations (MIC) of the compounds were determined by agar dilution method, and synergy between phenothiazines and vancomycin was investigated using Checkerboard (microbroth dilution) technique. We found that all enterococci strains, regardless of their susceptibility to vancomycin, were inhibited by phenothiazines at concentrations varying from 8 to 256 μg/ml, with thiethylperazine being the most potent inhibitory agent. Besides, all the phenothiazines showed partial synergy with vancomycin and could lessen MIC of vancomycin from 512 to 8 μg/ml at their sub‐inhibitory concentrations. The highest reduction in MIC was observed with chlorpromazine (32 times); however, thiethylperazine and promethazine stood next (24 times). Although resistance modification was observed at concentrations higher than those that phenothiazines reach in vivo, the potential offered by non‐antibiotics justify further animal experiments as well as clinical trials to establish their clinical relevance.     

The effect of regular medication on the outcome of paracetamol poisoning

BACKGROUND: Patients admitted with paracetamol overdose frequently receive one or more types of regular medication that may affect the outcome of the paracetamol intoxication. AIM: To describe the use of regular medication in patients with paracetamol poisoning and to evaluate its effects on morbidity and mortality. METHODS: Seven hundred and thirty-seven consecutive patients admitted with paracetamol poisoning were studied and the use of regular medication was recorded. The relative risk of hepatic encephalopathy, death or liver transplantation, severe hepatic dysfunction and severe hepatocellular injury was evaluated by multivariate analysis. RESULTS: Regular medication was received by 332 patients (45%). Medication with benzodiazepines (105 cases), antidepressants (100 cases), neuroleptics (75 cases), paracetamol (58 cases), oral contraceptives (51 cases), beta-agonists (40 cases), opioid analgesics (32 cases) and anticonvulsants (27 cases) predominated. Regular medication with opioid analgesics was associated with a high incidence of hepatic dysfunction (odds ratio, 5.39; 95% confidence interval, 1.13-25.8). No significant findings were demonstrated for benzodiazepines, antidepressants, neuroleptics, paracetamol, oral contraceptives, beta-agonists or anticonvulsants in the multivariate analysis. CONCLUSIONS: Regular medication with psychotropic medication, analgesics, oral contraceptives, beta-agonists or anticonvulsants was frequent in patients admitted with paracetamol poisoning. Medication with opioid analgesics was associated with a significantly increased incidence of hepatic dysfunction, whereas the other medications did not appear to affect the outcome of the paracetamol intoxication.     

Use of antipsychotic medication and suicidality—the Northern Finland Birth Cohort 1966

In addition to psychoses, antipsychotic drugs are nowadays also prescribed for other psychiatric disturbances, such as mood disorders. We wanted to find out whether there is any association between the use of antipsychotic drugs and suicidality in cases of psychotic and non‐psychotic disorders. Our sample was the population‐based Northern Finland 1966 Birth Cohort. Information on the use of prescribed drugs was collected in 1997 from the nationwide medication register and with a postal questionnaire (N = 8218). The presence of suicidal ideation was assessed cross‐sectionally using the Symptom Check List‐25 questionnaire. We studied associations between suicidal ideation, adjusted for symptoms of depression and anxiety, and antipsychotic medication in different diagnostic groups (schizophrenia, other psychosis and no psychosis). Individuals receiving antipsychotic medication (n = 70, 0.9%) had in general more suicidal ideation regardless of diagnostic group, although the associations diminished when taking other symptoms into account. There were no statistically significant differences between those taking typical and atypical antipsychotics. In the non‐psychotic group, higher antipsychotic doses were associated with more suicidal ideation even when adjusted for symptoms of depression and anxiety (p < 0.05). In the cases of schizophrenia or other forms of psychosis, no such associations were observed. Our results suggest that one should take suicidal ideation into account when prescribing antipsychotic medication, especially for off‐label use. Copyright © 2012 John Wiley & Sons, Ltd.     

4‐amino‐6‐alkyloxy‐2‐alkylthiopyrimidine derivatives as novel non‐nucleoside agonists for the adenosine A1 receptor

Three 4‐amino‐6‐alkyloxy‐2‐alkylthiopyrimidine derivatives ( 4 – 6 ) were investigated as potential non‐nucleoside agonists at human adenosine receptors (ARs). When tested in competition binding experiments, these compounds exhibited low micromolar affinity (K_i values comprised between 1.2 and 1.9 μm ) for the A₁ AR and no appreciable affinity for the A_2A and A₃ ARs. Evaluation of their efficacy profiles by measurement of intracellular cAMP levels revealed that 4 and 5 behave as non‐nucleoside agonists of the A₁ AR with EC₅₀ values of 0.47 and 0.87 μm , respectively. No clear concentration‐response curves could be instead obtained for 6 , probably because this compound modulates one or more additional targets, thus masking the putative effects exerted by its activation of A₁ AR. The three compounds were not able to modulate A_2B AR‐mediated cAMP accumulation induced by the non‐selective AR agonist NECA, thus demonstrating no affinity toward this receptor.     

Two‐step radiosynthesis of [18F]N‐succinimidyl‐4‐fluorobenzoate ([18F]SFB)

The acylation reagent [¹⁸F]N‐succinimidyl‐4‐fluorobenzoate (¹⁸F‐SFB) has been prepared using a new two‐step approach. The starting material p‐[¹⁸F]fluorobenzaldehyde (¹⁸F‐FBA) was obtained by an improved radiosynthesis with a decay‐corrected radiochemical yield of 66±6 % (n=3). Reaction of ¹⁸F‐FBA with (diacetoxyiodine)benzene and N‐hydroxysuccinimide and preparative HPLC purification furnished ¹⁸F‐SFB in an r.c.y. of 49±6 % (n=3), based on the starting radioactivity of ¹⁸F‐FBA. The radiochemical purity of ¹⁸F‐SFB was >99%. Alternatively, purification by solid phase extraction gave ¹⁸F‐SFB with an r.c.y. of 77±9% (n=4) and a radiochemical purity of 89±5% (n=4). This radiochemical synthesis only used non‐aqueous solvents, which simplifies the method and facilitates subsequent applications of ¹⁸F‐SFB. Copyright © 2009 John Wiley & Sons, Ltd.     

Issues for sustainability of non‐government organisations in the alcohol and other drugs sector

Introduction and Aims. The study aimed to identify issues for sustainability of non‐government organisations in the alcohol and other drugs sector (AODS) in Australia within the current neoliberal context. Design and Methods. Six key‐informant group consultations were conducted in Sydney, Melbourne, Darwin (Australia). Participants were professionals working in the AODS from non‐government AOD organisations, government departments, philanthropic organisations and academic institutions (n = 40). Qualitative data were collected according to a discussion guide. Results. Issues related to problems with workforce capacity, independence, governance and funding. Factors contributing to these issues related to the competitive tendering funding model, for example: accountability requirements and tied funding. Discussion and Conclusions. Issues identified by the AODS were mostly similar to those identified by the broader non‐government organisations sector. There is much to learn from outside the AODS. Strategies to improve sustainability will include workforce development, improving governance and developing relationships within the sector and with government. These require a commitment to innovation and will entail movement of resources from service provision in the short term to organisational development for the long term.[Spooner C, Dadich A. Issues for sustainability of non‐government organisations in the alcohol and other drugs sector. Drug Alcohol Rev 2009]     

The impact of an electronic prescribing and administration system on the safety and quality of medication administration

Objective To assess the effect of an electronic prescribing and administration system on the safety and quality of medication administration in a UK hospital. Setting Surgical ward in a teaching hospital. Method Data were collected before and after introducing a closed‐loop system comprising electronic prescribing, automated dispensing, barcode patient identification and electronic medication administration records (ServeRx, MDG Medical). We observed medication administration during drug rounds and assessed medication administration error (MAE) rates for ward‐stock and non‐ward‐stock drugs, accuracy of medication administration documentation, timeliness of administration, administration of medication from unlocked areas and supervision of patients taking oral medication by nursing staff. Key findings Pre‐ and post‐intervention MAE rates were 6.4 and 2.3% respectively for ward‐stock drugs (95% confidence interval for the difference (CI) ?5.8 to ?2.4%), and 14.6 and 13.7% for non‐ward‐stock drugs (CI ?6.5 to 4.7%). Excluding omissions due to unavailability, pre‐ and post‐intervention MAE rates were 6.2 and 2.2% respectively for ward‐stock drugs (CI ?5.7 to ?2.3%), and 9.2 and 3.5% for non‐ward‐stock drugs (CI ?9.3 to ?2.1%). Pre‐intervention, 2086 doses (96.3%) were documented correctly and 1557 (95.9%) post‐intervention (CI ?1.6 to 0.8%). There were five clinically significant documentation discrepancies pre‐intervention (0.2%), and 33 (2.0%) afterwards (CI 1.1 to 2.5%). Timeliness of administration improved post‐intervention (P < 0.001; Chi‐square test), as did administration of medication from unlocked areas (CI 4.7 to 7.3%) and supervision of patients taking oral medication (CI 17 to 23%). Conclusion Reductions in MAEs, excluding omissions due to unavailability, occurred for both ward‐stock and non‐ward‐stock drugs. The system also improved timeliness and security of drug administration. However, there was an increase in potentially significant documentation discrepancies.     

Discrimination of skin sensitizers from non‐sensitizers by interleukin‐1α and interleukin‐6 production on cultured human keratinocytes

In vitro testing methods for classifying sensitizers could be valuable alternatives to in vivo sensitization testing using animal models, such as the murine local lymph node assay (LLNA) and the guinea pig maximization test (GMT), but there remains a need for in vitro methods that are more accurate and simpler to distinguish skin sensitizers from non‐sensitizers. Thus, the aim of our study was to establish an in vitro assay as a screening tool for detecting skin sensitizers using the human keratinocyte cell line, HaCaT. HaCaT cells were exposed to 16 relevant skin sensitizers and 6 skin non‐sensitizers. The highest dose used was the dose causing 75% cell viability (CV75) that we determined by an MTT [3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide] assay. The levels of extracellular production of interleukin‐1α (IL‐1α) and IL‐6 were measured. The sensitivity of IL‐1α was 63%, specificity was 83% and accuracy was 68%. In the case of IL‐6, sensitivity: 69%, specificity: 83% and accuracy: 73%. Thus, this study suggests that measuring extracellular production of pro‐inflammatory cytokines IL‐1α and IL‐6 by human HaCaT cells may potentially classify skin sensitizers from non‐sensitizers. Copyright © 2015 John Wiley & Sons, Ltd.     

Targeting misuse of 2‐amino‐N‐ethyl‐1‐phenylbutane in urine samples: in vitro–in vivo correlation of metabolic profiles and development of LC‐TOF‐MS method

A phenyethylamine derivative, 2‐amino‐N‐ethyl‐1‐phenylbutane (2‐AEPB), has recently been detected in doping control and drugs‐of‐abuse samples, and identified as a non‐labelled ingredient in a dietary supplement. To facilitate efficient control of this substance we have studied the in vitro metabolic behaviour of 2‐AEPB with human liver preparation, compared these results with in vivo pathways in human, and finally propose an analytical strategy to target the potential misuse of 2‐AEPB for toxicological, forensic and doping control purposes. The major in vitro formed metabolites originated from desethylation (M1) and monohydroxylation (M2). A minor metabolite with hydroxylation/N‐oxidation was also observed (M3). In vitro‐in vivo correlation was studied in an excretion study with a single, oral dose of 2‐AEPB‐containing supplement. An unmodified substance was the most abundant target compound and detected until the last point of sample collection (72 h), and the detection of M1 (40 h) and M2 (27 h) demonstrated good correlation to in vitro results. In the study with authentic cases (n = 6), 2‐AEPB and M1 were mainly found in free urinary fraction, whereas higher inter‐individual variability was observed for M2. It was predominantly conjugated and already within this limited number of cases, the ratio between glucuronide‐ and sulpho‐conjugated fractions varied significantly. As a conclusion, hydrolysis is not mandatory in the routine sample preparation, and as the separation can be based on either gas chromatography or liquid chromatography, this study verifies that routine mass spectrometric detection methods targeted to amphetamine derivatives can be easily extended to control the misuse of 2‐AEPB. Copyright © 2014 John Wiley & Sons, Ltd.