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Pharmaceuticals
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Pharmacology and Toxicology of Opioids, 2nd Edition
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Pharmacology and Toxicology of Opioids, 2nd Edition

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: 31 July 2026 | Viewed by 6448

Special Issue Editors

Dr. Juliana Faria

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Guest Editor
1. Associate Laboratory i4HB—Institute for Health and Bioeconomy, University Institute of Health Sciences—CESPU, 4585-116 Gandra, Portugal
2. UCIBIO—Applied Molecular Biosciences Unit, Translational Toxicology Research Laboratory, University Institute of Health Sciences (1H-TOXRUN, IUCS-CESPU), 4585-116 Gandra, Portugal
Interests: opioid pharmacology; prescription opioids; toxicity assays; toxicity mechanisms; in vivo models; in vitro models
Special Issues, Collections and Topics in MDPI journals
Dr. Joana Barbosa

E-Mail Website
Guest Editor
1. Associate Laboratory i4HB—Institute for Health and Bioeconomy, University Institute of Health Sciences—CESPU, 4585-116 Gandra, Portugal
2. UCIBIO—Applied Molecular Biosciences Unit, Translational Toxicology Research Laboratory, University Institute of Health Sciences (1H-TOXRUN, IUCS-CESPU), 4585-116 Gandra, Portugal
Interests: toxicology; opioid pharmacology; opioid pharmacokinetics; opioid pharmacodynamics; toxicity biomarkers; adverse outcome pathways; toxicity screening; in vitro assays; in vivo assays
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Ricardo Dinis-Oliveira

E-Mail
Guest Editor
1. Associate Laboratory i4HB, Institute for Health and Bioeconomy, University Institute of Health Sciences—CESPU, 4585-116 Gandra, Portugal
2. UCIBIO—Applied Molecular Biosciences Unit, Translational Toxicology Research Laboratory, University Institute of Health Sciences (1H-TOXRUN, IUCS-CESPU), 4585-116 Gandra, Portugal
3. Department of Public Health and Forensic Sciences and Medical Education, Faculty of Medicine, University of Porto, 4200-319 Porto, Portugal
4. FOREN—Forensic Science Experts, Dr. Mário Moutinho Avenue, No. 33-A, 1400-136 Lisbon, Portugal
Interests: toxicology; psychoactive substances; forensic sciences; drugs; opioids; biomedical research; scientometrics; scientific medical writing; pedagogical innovation; real-world evidence
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Opioids are a broad group of drugs that include both illegal drugs and medicines. In pharmacological contexts, opioids are currently used as a gold standard for the treatment of moderate to severe pain. Pain is a complex and subjective experience and a symptom associated with several pathologies, many of which are extremely frequent, leading to the widespread consumption of opioids. Despite their high analgesic efficiency, the incidence of side effects and adverse reactions; poisoning cases, including fatal intoxications; and cases of addiction are growing, along with the increase in their use and misuse. In fact, rising opioid consumption is leading to an opioid epidemic and a public health crisis.  

In this context, it is important to broaden our knowledge of opioids’ pharmacology and toxicity mechanisms to improve their therapeutic efficacy and lower the rate of adverse effects, which will ultimately improve the quality of life of many patients. Furthermore, it is also important to understand and decrease the potential for opioid dependence in addition to searching for new analgesic opioids. Therefore, in this Special Issue, authors are invited to submit original papers, (mini-)reviews, communications, perspectives, and opinion articles on all relevant aspects of opioid pharmacology and toxicology.  

Their research areas may include the following:

  • In vitro and in vivo studies on opioid toxicity;
  • In vitro and in vivo studies on opioid structure–activity relationships;
  • Pharmacokinetic and pharmacodynamic studies;
  • Behavioral studies;
  • New advancements in opioid pharmacology, including (but not limited to) new opioid drug candidates;
  • New opioid quantification methodologies.

Dr. Juliana Faria
Dr. Joana Barbosa
Prof. Dr. Ricardo Dinis-Oliveira
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 250 words) can be sent to the Editorial Office for assessment.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • opioid toxicity
  • opioid pharmacodynamics
  • opioid pharmacokinetics
  • opioid pharmacogenetics
  • prescription opioids
  • toxicity assays
  • in vivo
  • in vitro
  • abuse
  • dependence

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Related Special Issue

Published Papers (5 papers)

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Research

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19 pages, 549 KB  
Article
Pain Management in Italian Elite Athletes: Trends in the Use of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), Glucocorticoids, and Narcotics in Anti-Doping Reports (2013–2023)
by Mario Ruggiero, Stefania Santamaria, Pietro Montesano, Leopoldo Ferrante, Yuri Russo and Filomena Mazzeo
Pharmaceuticals 2026, 19(2), 298; https://doi.org/10.3390/ph19020298 - 11 Feb 2026
Cited by 1 | Viewed by 695
Abstract
Background: Analgesics are widely used in competitive sports, but their patterns of use and detection in anti-doping controls vary significantly across drug classes. This study examined a decade of Italian anti-doping reports with three aims: to describe trends involving non-steroidal anti-inflammatory drugs [...] Read more.
Background: Analgesics are widely used in competitive sports, but their patterns of use and detection in anti-doping controls vary significantly across drug classes. This study examined a decade of Italian anti-doping reports with three aims: to describe trends involving non-steroidal anti-inflammatory drugs (NSAIDs), glucocorticoids, and narcotics; to characterize the distribution of specific active ingredients; and to analyze the relative contribution of these classes to anti-doping violations, placing the findings within the regulatory framework. Methods: Data from national anti-doping reporting systems were analyzed from 2013 to the first half of 2023. Yearly data included tested athletes, athlete declarations of NSAID use, and laboratory analytical findings for prohibited substances (glucocorticoids and narcotics). NSAID prevalence was calculated relative to tested athletes, while glucocorticoid and narcotic findings were assessed as absolute counts and proportions of total violations. Temporal trends were assessed using the Cochran–Armitage test. Results: NSAIDs consistently ranked as the most frequently reported medication, with nearly half of the tested athletes reporting their use and no significant linear trend in overall prevalence. However, a significant shift was observed within the NSAID class, with a marked decrease in declarations of COX-2 selective agents over time. Glucocorticoids accounted for a significant portion of prohibited substances, with fluctuating proportions (showing no significant linear trend), betamethasone being the most common active ingredient. Narcotics appeared only sporadically, although the use of non-prohibited opioids such as tramadol and codeine—absent from official reports—remains relevant for understanding analgesic practices. Conclusions: Analgesic use in Italian elite sports shows distinct patterns driven by therapeutic needs and anti-doping regulations. NSAIDs remain the primary choice for routine pain management, though the type of NSAID reported has shifted significantly. Glucocorticoids represent a notable share of prohibited findings with a fluctuating, rather than steadily increasing, pattern. Narcotics appear only sporadically in violation data. Ongoing monitoring will be crucial to understanding how evolving clinical practices and recent regulatory changes influence future detection trends and athlete health. Full article
(This article belongs to the Special Issue Pharmacology and Toxicology of Opioids, 2nd Edition)
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19 pages, 1347 KB  
Article
Novel Synthetic Opioids (NSOs) and Their Evolving Crisis: Utilising NPSfinder® as a Real-Time Predictive Tool
by Elena Deligianni, Davide Arillotta, Alessandro Vento, John Martin Corkery, Georgios Papazisis, Antonis Goulas, Lisa Lione and Fabrizio Schifano
Pharmaceuticals 2026, 19(1), 17; https://doi.org/10.3390/ph19010017 - 21 Dec 2025
Viewed by 1064
Abstract
Background/Objectives: The rapidly evolving crisis of Novel Synthetic Opioids (NSOs) poses a serious and growing threat for global public health. NSOs include prescription/non-prescription opioids (fentanyl, non-fentanyl analogues), herbal derivatives, and other emerging analogues that are of critical concern due to their high potency, [...] Read more.
Background/Objectives: The rapidly evolving crisis of Novel Synthetic Opioids (NSOs) poses a serious and growing threat for global public health. NSOs include prescription/non-prescription opioids (fentanyl, non-fentanyl analogues), herbal derivatives, and other emerging analogues that are of critical concern due to their high potency, misuse potential, and addiction and intoxication risk. There remains an important gap in real-time, systematic monitoring of NSOs emergence, especially in online communities where these substances appear for the first time. This study aimed to employ the NPSfinder® automated web-crawling tool to detect, monitor, analyse, and evaluate the evolving NSOs scene. Methods: Data were collected during two time-periods, i.e., 2017–2019 and 2023, from selected high traffic psychonaut online platforms to better understand trends in opioids market evolution and adaptability and compare NPSfinder® findings with other well-known Early Warning Systems (EWSs) databases to assess detection overlap and early identification capacity. Results: Within the selected time-periods, a total of 446 NSOs were detected by NPSfinder®; fentanyl analogues (n = 249) were dominant, with a notable rise in non-fentanyl analogues, especially nitazene-like compounds, in 2023. Over 57% of these NSOs were not captured by any of the other EWSs, confirming the tool’s strong capacity to identify early threats. Conclusions: Overall, the low overlap across EWS databases underscores the global challenges in comprehensive opioid detection and surveillance. Future studies should integrate web-crawler findings with real-world datasets. It will be vital to combine these efforts with toxicological, mortality, and clinical outcome analyses, especially for emerging research compounds, to inform targeted harm-reduction strategies. Full article
(This article belongs to the Special Issue Pharmacology and Toxicology of Opioids, 2nd Edition)
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Review

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12 pages, 894 KB  
Review
Indole Alkaloids as Biased Opioid Receptor Modulators
by Oliver Grundmann and Allison Henderson
Pharmaceuticals 2026, 19(3), 397; https://doi.org/10.3390/ph19030397 - 28 Feb 2026
Viewed by 569
Abstract
Background: Opioid receptors are a commonly used target for treatment of pain conditions. Most opioids used in therapy are linked to adverse effects such as tolerance, dependence, and respiratory depression. Indole alkaloids acting on opioid receptors may provide a novel molecular mechanism [...] Read more.
Background: Opioid receptors are a commonly used target for treatment of pain conditions. Most opioids used in therapy are linked to adverse effects such as tolerance, dependence, and respiratory depression. Indole alkaloids acting on opioid receptors may provide a novel molecular mechanism to confer analgesic effects. Results: Indole alkaloids such as ibogaine and mitragynine act on μ-opioid receptors as biased full or partial agonists that do not, or much less strongly, recruit β-arrestin compared to non-biased agonists. The recruitment of β-arrestin has been linked to adverse effects, most notably substantial respiratory depression. The molecular mechanism of biased activation has been proposed to be associated with accommodation of the indole structure that leads to a different spatial orientation of amino acid residues in transmembrane regions 2 and 3 of the μ-opioid receptor as well as extracellular helix 8. Conclusions: Naturally occurring indole alkaloids show biased G-protein coupled activation of opioid receptors with limited recruitment of β-arrestin, thus limiting commonly observed adverse effects. Indole alkaloids may present a feasible structure to develop new biased opioid modulators with an improved risk-to-benefit ratio. Full article
(This article belongs to the Special Issue Pharmacology and Toxicology of Opioids, 2nd Edition)
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13 pages, 408 KB  
Review
Buprenorphine Oral Lyophilisate for Treatment of Opioid Use Disorder: Pharmacology and Clinical Efficacy
by Michael Soyka and Svenja Bolz
Pharmaceuticals 2026, 19(2), 270; https://doi.org/10.3390/ph19020270 - 5 Feb 2026
Viewed by 781
Abstract
Background/Objectives: Opioid use disorder (OUD) is a chronic relapsing condition associated with elevated mortality and substantial psychiatric and somatic comorbidity. Oral methadone and sublingual and depot buprenorphine are the undisputed gold standard in opioid agonist treatment (OAT). More recently, another oral buprenorphine [...] Read more.
Background/Objectives: Opioid use disorder (OUD) is a chronic relapsing condition associated with elevated mortality and substantial psychiatric and somatic comorbidity. Oral methadone and sublingual and depot buprenorphine are the undisputed gold standard in opioid agonist treatment (OAT). More recently, another oral buprenorphine formulation, buprenorphine lyophilisate (BUP-Lyo), has been introduced into clinical practice, offering potentially faster bioavailability and simplified administration. This review aims to summarize the available clinical and pharmacological data on BUP-Lyo and assess its potential role within current OAT strategies. Methods: A targeted Medline search was performed to identify publications reporting pharmacological characteristics, safety, efficacy, and clinical use of BUP-Lyo. Additional information was requested from the manufacturer. Relevant sources were reviewed narratively with a focus on OUD treatment, with particular attention to the pharmacological and clinical profile of the compound. Results: Few studies on BUP-Lyo have been published to date. As a rapid-dispersion formulation placed on the tongue, BUP-Lyo provides faster bioavailability and a quicker route of administration compared with conventional sublingual buprenorphine. These properties may reduce the need for post-administration supervision and could lessen risks of misuse or diversion. Available evidence supports its safety, efficacy, and feasibility within routine OAT, and the clinical implications of these characteristics are discussed. Conclusions: BUP-Lyo expands the range of available buprenorphine formulations and offers practical advantages through accelerated absorption and simplified administration. While initial data are encouraging, the limited evidence base underscores the need for further longitudinal and post-marketing studies to define its clinical position in the management of OUD. Full article
(This article belongs to the Special Issue Pharmacology and Toxicology of Opioids, 2nd Edition)
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Other

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14 pages, 744 KB  
Systematic Review
Harmful Effects of Prescribed Opioids in Children and Adults: A Systematic Review
by Luíza Siqueira Lima, Nayara de S. da Costa, Maria Eduarda A. Galiciolli, Quelen I. Garlet, João José Joaquim, Cláudia S. Oliveira and Cristiano Matos
Pharmaceuticals 2025, 18(10), 1429; https://doi.org/10.3390/ph18101429 - 24 Sep 2025
Cited by 2 | Viewed by 2065
Abstract
Background: Opioids are commonly used to manage both acute and chronic pain by acting on opioid receptors in the central and peripheral nervous systems. However, concerns about their increasing prescription and misuse have emerged due to adverse effects, toxicity, and the global impact [...] Read more.
Background: Opioids are commonly used to manage both acute and chronic pain by acting on opioid receptors in the central and peripheral nervous systems. However, concerns about their increasing prescription and misuse have emerged due to adverse effects, toxicity, and the global impact of opioid-related harm. Objectives: This systematic review aims to evaluate the harmful (adverse and toxic) effects of prescribed opioids on the pediatric and the general population. Methods: Following PRISMA guidelines, a systematic search was conducted for data from January 2011 to December 2024 across selected electronic databases (PubMed®, SciELO®, Web of Science®, and EMBASE®) using a specific search strategy with Boolean operators. Cross-sectional, cohort, and case–control designs published in English, analyzing and identifying the harmful effects of prescribed opioids in children and the general population, were eligible for inclusion. Three reviewers independently assessed titles and abstracts for eligibility, followed by a full-text review. A referee reviewer resolved discrepancies. Data extraction was performed for qualifying studies. The risk of bias was assessed by the ROBINS-I tool. Results: A total of 3984 papers were collected, with 1697 duplicates and 2062 non-eligible papers removed; resulting in 25 papers (112.825 patients) selected for qualitative analysis. The pediatric group experienced more harmful effects across multiple body systems (nausea and vomiting, hypotension, agitation, drowsiness/lethargy, lethargy, respiratory depression, aspiration pneumonia) compared to the general population (dominant S wave, long QTc interval, right axis deviation, seizure). Conclusions: Despite the data heterogeneity, this study highlights the importance of evaluating the harmful effects of opioids, particularly in pediatric patients, to assess the risk–benefit balance and health risks associated with their use. The lower number of effects in the general population may be attributed to increased pharmacological tolerance and tolerability. Full article
(This article belongs to the Special Issue Pharmacology and Toxicology of Opioids, 2nd Edition)
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