β‐2 Agonists as Misusing Drugs? Assessment of both Clenbuterol‐ and Salbutamol‐related European Medicines Agency Pharmacovigilance Database Reports

Milano, Giulia; Chiappini, Stefania; Mattioli, Francesca; Martelli, Antonietta; Schifano, Fabrizio

doi:10.1111/bcpt.12991

Cited by 31 publications

(29 citation statements)

References 43 publications

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“…Aside from the reported AAFs of beta 2 ‐agonists each year, there is a widespread abuse of these substances among bodybuilders and recreational strength athletes . Around 20% of anabolic steroid abusers have reported that beta 2 ‐agonists are part of the drugs they use for leanness .…”

Section: Antidoping Regulations Adverse Analytical Findings and Abusmentioning

confidence: 99%

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Anabolic and lipolytic actions of beta₂‐agonists in humans and antidoping challenges

Hostrup

Jacobson

Jessen

et al. 2020

Drug Testing and Analysis

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Inhaled beta 2 -adrenoceptor agonists (beta 2 -agonists) are among the most used substances in competitive sports. The 2020 Prohibited List issued by the World Anti-Doping Agency restricts use of all selective and non-selective beta 2 -agonists in-and out-of competition with few exemptions. Formoterol, salbutamol, and salmeterol are allowed by inhalation within defined dosing limits. These restrictions are in place because supratherapeutic use of beta 2 -agonist has the potential to be anabolic and to enhance performance, as well as due to potential side effects. Despite substantial documentation that beta 2 -agonists exert anabolic and lipolytic actions, these actions are not widely recognized. Furthermore, a common misconception is that the inhaled route does not exert these effects. However, given the high relative systemic bioavailability via the inhaled route, inhalation at high doses can also exert anabolic and lipolytic actions. In this review, we highlight the anabolic and lipolytic actions beta 2agonists can exert, regardless of the type of beta 2 -agonist and the route of administration. The doses needed to provide such effects are also associated with adverse effects and would in most cases be detected in routine doping control. Notwithstanding, the beta 2 -agonist regulations are associated with some challenges and given their ability to induce muscle growth and to enhance performance, it is important to continue developing effective detection strategies to prevent potential misuse of beta 2 -agonists while allowing treatment of asthmatic subjects without causing adverse side effects or ergogenic actions. K E Y W O R D Sanabolic, beta agonists, doping, hypertrophy, muscle growth

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Section: Antidoping Regulations Adverse Analytical Findings and Abusmentioning

confidence: 99%

“…Accordingly, beta 2 ‐agonist abuse is not only a problem that pertains to elite sport. While there is a high illicit use of clenbuterol among bodybuilders, occurrences of overdosing and off‐label use are actually higher for salbutamol than for clenbuterol in the European Union …”

Section: Antidoping Regulations Adverse Analytical Findings and Abusmentioning

confidence: 99%

Anabolic and lipolytic actions of beta₂‐agonists in humans and antidoping challenges

Hostrup

Jacobson

Jessen

et al. 2020

Drug Testing and Analysis

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“…Our local clinical biochemist suggested theophylline, also a methylxanthine, as a potential cause, having previously seen cases similar to this. The features of acute chest pain, palpitations and vomiting, with hypokalaemia, hypophosphataemia and hyperglycaemia on laboratory testing and the ECG demonstrating sinus tachycardia and ischaemic changes, matched reports of β-agonist toxicity 2 8. However, β-agonist toxicity was considered unlikely, given the absence of comorbidities and daily medications, plus the family denied any β-agonist medications being kept in the household.…”

Section: Differential Diagnosismentioning

confidence: 77%

“…Clenbuterol is an oral β2-agonist with anabolic and lipolytic effects, used off-licence as a ‘fat-busting’ drug 2. Adverse effects in adults are well documented, but there are limited data on effects in children or adolescents 3 4.…”

Section: Introductionmentioning

confidence: 99%

Clenbuterol: a new toxic substance in paediatrics

et al. 2020

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A 13-year-old girl presented to the emergency department with acute onset of chest pain, nausea and tremor. The patient denied drug ingestion, and urine toxicology was negative. ECG demonstrated sinus tachycardia, prolonged QTc (541 ms) and ST depression. Laboratory testing demonstrated metabolic acidosis, hypokalaemia, hypophosphataemia and hyperglycaemia. She was commenced on continuous cardiac monitoring and treated with intravenous fluids and electrolyte replacement. Presenting features and laboratory abnormalities resolved within 48 hours. The National Poisons Information Service and Clinical Biochemistry were integral to her management, advising the clinical team on the likeliest aetiology. Five weeks after discharge, urine toxicology, using mass spectrometry, identified clenbuterol. Clenbuterol is an oral β2-agonist with anabolic and lipolytic effects that is misused as a performance and image enhancing drug. Clinicians must be aware of the increasing availability of these drugs and their potential for causing harm in children and adolescents.

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“…Spontaneous reporting (SR) of adverse drug reactions (ADRs) is a critical activity for healthcare professionals, as ADRs are one of the leading causes of morbidity and mortality and a threat to public health . The identification of pharmacovigilance (PV) activities as common objectives in the global community triggered international collaborations to enhance patient safety .…”

Section: Introductionmentioning

confidence: 99%

Impact of knowledge, attitude and preceptor behaviour in pharmacovigilance education

Kim

Choi

et al. 2018

Basic Clin Pharma Tox

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This study aimed to determine the level of pharmacovigilance (PV) education in pharmacy programmes and to evaluate the predictive factors for the intent to report adverse drug reactions (ADRs) by pharmacy students in South Korea. Self‐administered questionnaires were collected from a regionally stratified nationwide convenience sample of pharmacy students in September 2017. The association between students' intent to report ADRs and their knowledge and attitude was evaluated by using multivariate logistic regression analysis. In total, 303 pharmacy students participated in the survey; the average age of students was 26.7 (standard deviation 2.9) years and 40.6% were males. Eighty‐eight students (29%) marked the degree of their intent as “strongly high.” Increased knowledge of ADR reporting methods and positive attitude towards the need for ADR reporting were significant predictors of the intent to report ADRs. Further, witnessing reporting by the preceptor (adjusted odds ratio, 2.37; 95% confidence interval, 1.26‐4.46; P < 0.01) was significantly correlated with the knowledge on and attitude towards ADR reporting of pharmacy students. The findings of our study indicated the need for improvements in PV curriculum, such as educational content focused on ADR reporting methods and demonstration of a preceptor's reporting in pharmacy practice experiential rotation, within Korean college of pharmacy curriculum.

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β‐2 Agonists as Misusing Drugs? Assessment of both Clenbuterol‐ and Salbutamol‐related European Medicines Agency Pharmacovigilance Database Reports

Cited by 31 publications

References 43 publications

Anabolic and lipolytic actions of beta₂‐agonists in humans and antidoping challenges

Anabolic and lipolytic actions of beta₂‐agonists in humans and antidoping challenges

Clenbuterol: a new toxic substance in paediatrics

Impact of knowledge, attitude and preceptor behaviour in pharmacovigilance education

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β‐2 Agonists as Misusing Drugs? Assessment of both Clenbuterol‐ and Salbutamol‐related European Medicines Agency Pharmacovigilance Database Reports

Cited by 31 publications

References 43 publications

Anabolic and lipolytic actions of beta2‐agonists in humans and antidoping challenges

Anabolic and lipolytic actions of beta2‐agonists in humans and antidoping challenges

Clenbuterol: a new toxic substance in paediatrics

Impact of knowledge, attitude and preceptor behaviour in pharmacovigilance education

Contact Info

Product

Resources

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Anabolic and lipolytic actions of beta₂‐agonists in humans and antidoping challenges

Anabolic and lipolytic actions of beta₂‐agonists in humans and antidoping challenges