北京若生智能科技有限公司
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fentanyl (Fentanyl Dura / fentanyl, Lavipharm / fentanyl, Recordati)

✓ Approved

Lavipharm · OPRD1 · 小分子

什么是 fentanyl？

fentanyl 是一种小分子，由Lavipharm研发。该药已获批，用于治疗相关适应症，给药途径：Transdermal。

药物档案

商品名Fentanyl Dura, fentanyl, Lavipharm, fentanyl, Recordati
公司Lavipharm
药物类别小分子
分子靶点OPRD1, OPRK1, OPRM1
给药途径Transdermal
状态Approved
来源： ClinicalTrials.gov, Lavipharm

作用机制

分子靶点

fentanyl 作用于 3 个分子靶点：

OPRD1opioid receptor delta 1 (DOR, OPRD)
OPRK1opioid receptor kappa 1 (KOR1, OPRK)
OPRM1opioid receptor mu 1 (MOR1, LMOR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

fentanyl 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved

相关研究文献

PubMedCurrent addiction reports2026-09-10

A Conceptual Model of Opioid Use Pathways: Addressing the Prescription-to-Illegal Opioid "Transition".

Dash Genevieve F GF, Slutske Wendy S WS, Nguyen Carolyne L CL, Langdon Kirsten J KJ

To review risk factors shared by and unique to nonmedical use of prescription opioids (NUPO) and heroin/illegally manufactured fentanyl (IMF) use, and synthesize them into distinct conceptual pathways. Much discussion of the opioid crisis focuses on a causal "transition" from NUPO to heroin/IMF use. However, most people with NUPO do not go on to use heroin or other illegal opioids; other nonopioid substance use prior to heroin/IMF is ubiquitous; and numerous other risk factors act in concert to facilitate or inhibit heroin/IMF initiation in the context of prior NUPO. Rather than a direct and causal pathway from NUPO to heroin/IMF use, largely overlapping risk factors in biological, environmental, social-interpersonal, and psychological-behavioral domains may give rise to both NUPO and heroin/IMF use in tandem, with some degree of drug-specific influence shaping distinct trajectories. There are genetic and environmental influences shared by and unique to NUPO and heroin/IMF use. NUPO-only use is facilitated by easier access to healthcare and implied legitimacy of POs; negative attitudes toward drug use and lack of drug-involved peers to facilitate access to underground drug markets inhibit heroin/IMF initiation. Heroin/IMF-only use is facilitated by early life adversity, trauma, and social disenfranchisement that increase risk for heroin/IMF use, coupled with limited access to POs (e.g., barriers to healthcare). NUPO+heroin/IMF use is facilitated by strong latent liability for addiction, externalizing psychopathology, and a permissive drug use environment with substance-involved peers, compounded by a flooded drug marketplace. Implications for intervention and policy are discussed.

PMID 42719812
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PubMedThe journal of physical chemistry. A2026-09-10

Interplay of High-Field and Earth's Field NMR: Fluorofentanyls as a Case Study.

Altenhof Adam R AR, Kaseman Derrick C DC, Mason Harris E HE, Alvarez Marc C MC et al.

Earth's field NMR (EFNMR) is a useful modality for low-field NMR spectroscopy due to its availability, portability, and low cost. EFNMR can enable better line width resolution than at high fields primarily due to low magnetic susceptibility broadening. Unfortunately, EFNMR spectra are highly complex due to strong J-coupling effects and can be challenging to interpret without additional information. However, the spectral complexity paired with ultrahigh resolution offers a unique opportunity to fingerprint analytes. Herein, we show that high-field (e.g., 9.4 T) NMR and EFNMR have distinct complementary roles in explaining the NMR interactions that manifest in the respective spectra of complex molecules. Chemical shifts are nearly exclusive to high-field NMR and can enable facile observations of weak J-couplings for cursory spectral assignments, but EFNMR's ability to resolve high-precision magnitudes and signs of J-couplings is essential for fully and accurately assigning structures with high fidelity. We demonstrate this with an important category of materials, fluorinated fentanyl analogues (i.e., fluorofentanyls) and their precursors. These systems are well suited to study due to their relevance to the synthetic opioid crisis and their similarities to fluorinated pharmaceuticals and biomolecules. Results show assignment of the magnitudes and signs of J-couplings in several fluorinated precursors using both high-field and EFNMR. In select fluorofentanyls, EFNMR can provide information on J-couplings that would otherwise be inaccessible even with 3D experiments at 9.4 T. EFNMR spectra of fluorofentanyls show a strong dependence on J-coupling between 1H or 19F and 14N nuclei, where the effects that manifest in spectra may be used to gain insights into local molecular dynamics and information on 14N electric-field gradient tensors.

PMID 42720390
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PubMedJournal of medical Internet research2026-09-09

Natural Language Processing Identification of Nonprescribed Fentanyl Use in Electronic Health Records: Algorithm Development and Validation Study.

Trujeque Joshua J, Simonetti Joseph A JA, Ortiz Isai I, Ingraham Nicholas E NE et al.

Overdose and suicide due to nonprescribed fentanyl use have increased significantly, yet health care systems lack reliable methods to identify patients who use nonprescribed fentanyl. International Classification of Diseases codes are inconsistent and do not specify nonprescribed fentanyl use. This study aimed to develop natural language processing approaches to identifying nonprescribed fentanyl use in electronic health record (EHR) documentation. This retrospective study included Veterans Health Administration patients seen between April 5, 2023, and December 23, 2024. A term list was developed to identify fentanyl-related mentions in clinical text, and 250-character snippets surrounding identified mentions were extracted. Veterans (n=3878) were randomly sampled from 5 predefined groups based on the presence of 1 of 4 terms ("fent," "blues," "M30s," and "tranq") in their EHR documentation. Physician annotators classified snippets into "nonprescribed fentanyl use," "prescribed fentanyl use," or "other," with interannotator agreement evaluated using the mean pairwise Cohen κ. Cross-validation folds were constructed at the patient level between training and test sets. Penalized logistic regression, Bio-ClinicalBERT, Llama 3-8B, and Mistral-7B were trained on labeled data and compared. Model performance was evaluated using precision, recall, and F1-scores for each class, with a focus on the nonprescribed fentanyl use class as the primary label of clinical interest using bootstrapped 95% CIs. A fairness analysis and Shapley additive explanations analysis were performed using Bio-ClinicalBERT. External validation was performed using Bio-ClinicalBERT on an independent sample of 200 snippets, each representing a unique patient from January 2025 to June 2026, with precision reported as the primary validation metric. Of 7389 snippets, 9.6% (n=709) were classified as "nonprescribed fentanyl use," 40.3% (n=2981) were classified as "prescribed fentanyl use," and 50% (n=3699) were classified as "other." Interannotator agreement was high (κ=0.822). Llama 3-8B achieved the highest F1-score for nonprescribed fentanyl use (0.87, 95% CI 0.83-0.92), followed by Mistral-7B (0.80, 95% CI 0.75-0.84), Bio-ClinicalBERT (0.80, 95% CI 0.74-0.85), and penalized logistic regression (0.74, 95% CI 0.73-0.75). Performance was consistent across demographic subgroups, with lower performance for the nonprescribed fentanyl use class observed in female and Hispanic subgroups. Shapley additive explanations analysis revealed clinically meaningful discriminating terms for each class, although subword tokens required contextual interpretation. External validation of Bio-ClinicalBERT demonstrated a precision of 0.79 for nonprescribed fentanyl use. Natural language processing can identify nonprescribed fentanyl use in EHR documentation, although model performance for this class was lower than overall model performance, reflecting the clinical complexity of identifying nonprescribed use and the variable ways in which clinicians document this problem. This approach may support risk prediction and targeting of interventions to patients exposed to nonprescribed fentanyl.

PMID 42715406
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PubMedArchives of toxicology2026-09-09

Mitochondrial oxidative stress and ion-channel suppression reveal a distinct neurotoxic profile of fentanyl analogues in a human neuronal model.

Ratto Daniela D, Bilel Sabrine S, Sasse Francesca Dalle FD, Bassi Marta M et al.

Fentanyl analogues, including butyrylfentanyl (BUF) and 4-fluorobutyrylfentanyl (4F-BUF), are increasingly implicated in severe toxicity and fatal overdoses. While their pharmacological activity at µ-opioid receptors is well established, the cellular mechanisms underlying their neurotoxic effects remain incompletely understood, particularly with respect to mitochondrial dysfunction and its relationship with neuronal functional impairment. In this study, differentiated SH-SY5Y cells were used as a human neuronal model to evaluate the toxicodynamic effects of morphine, fentanyl, BUF, and 4F-BUF. Cell viability assays were performed to define sub-toxic concentrations, while oxidative stress was assessed by measuring cytoplasmic reactive oxygen species (ROS) and mitochondrial superoxide at early (25 min) and prolonged (24 h) time points. Functional alterations were examined using whole-cell patch-clamp recordings of voltage-gated inward and outward membrane currents. All compounds induced concentration-dependent cytotoxicity, with BUF and 4F-BUF exhibiting the lowest IC₂₅ values (8.39 ± 0.55 and 8.36 ± 0.67 µM, respectively), compared with fentanyl (37.87 ± 4.23 µM) and morphine (59.09 ± 4.72 µM). Cytoplasmic ROS levels increased similarly across all treatments, whereas mitochondrial superoxide generation displayed a time-dependent divergence, with 4F-BUF producing the highest mitochondrial superoxide levels after prolonged exposure (334.7 ± 26.1% of control), significantly exceeding fentanyl (281.6 ± 21.6% of control). Electrophysiological analysis revealed that fentanyl preferentially reduced inward currents, whereas BUF and 4F-BUF induced a broader suppression of both inward and outward membrane conductance. Importantly, mitochondrial ROS scavenging with mitoTEMPO markedly attenuated 4F-BUF-induced mitochondrial superoxide accumulation (278.6 ± 24.8% vs. 152.5 ± 7.8% of control) and prevented the associated suppression of voltage-gated membrane currents. These findings indicate that fentanyl analogues exert distinct cellular effects characterized by enhanced mitochondrial oxidative stress and associated alterations in membrane conductance. Notably, mitochondrial superoxide emerges as an indicator of fentanyl analogue toxicity, revealing differences not captured by cytoplasmic ROS measurements and highlighting mitochondrial dysfunction as a relevant target for toxicological evaluation.

PMID 42711419
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PubMedFederal practitioner : for the health care professionals of the VA, DoD, and PHS2026-09-09

Mental Health Prescribers' Perceptions of Patients With Substance Use Disorders and Harm Reduction Services.

Jubran Nadia N, Kang Kelly K, Chai Joy J, Jaume Alyssia A

The Veterans Health Administration (VHA) has published guidelines outlining the legal authority to operate syringe services programs. To aid in the implementation of harm reduction programs at VHA medical centers in Maryland; Washington, DC; and West Virginia, the perceptions of harm reduction tools by mental health prescribers were evaluated. A mixed-methods analysis examined mental health prescriber perceptions of patients with substance use disorders (SUDs) and their willingness to provide harm reduction tools. A survey was conducted followed by a voluntary postsurvey interview. A descriptive analysis was performed on responses. Notes from postsurvey interviews were analyzed using the Prosci Awareness, Desire, Knowledge, Ability, and Reinforcement (ADKAR) Model for Change Management. Prescribers felt comfortable and confident in their abilities to educate patients to reduce harm related to substance use. Survey results were mixed regarding comfort in working with people with or without SUDs. Prescribers were represented across the continuum of the ADKAR change model and were more willing to provide naloxone than fentanyl test strips or syringes. Prescribers expressed mixed opinions on the use of harm reduction tools for patients with SUDs. Some prescribers viewed harm reduction as part of a treatment plan, while others viewed a return to drug use as a failure of treatment. This study highlights the need for additional interventions to address clinician hesitancy and concerns surrounding harm reduction tools to successfully implement harm reduction programs across the VHA.

PMID 42713507
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PubMedPloS one2026-09-08

Supporting clinical guidelines for opioid conversion to methadone and tapering to prevent withdrawal in critically ill children using physiology based pharmacokinetic modeling and simulation.

de Hoop-Sommen Marika A MA, Alozai Sahar S, Gijsen Violette M G J VMGJ, van der Zanden Tjitske M TM et al.

Long-term opioid use is common in critically ill children and can cause withdrawal symptoms at discontinuation. To avoid withdrawal, short-acting opioids are usually converted into a long-acting drug, such as methadone, which is then carefully tapered. However, the exact conversion ratio and the optimal tapering protocol are unknown. This study aimed to design optimized conversion and tapering schedules of morphine and fentanyl to methadone for pediatric intensive care unit patients using physiologically-based pharmacokinetic (PBPK) modeling and expert panel decision-making. PBPK models of fentanyl, morphine, and methadone were verified with published pharmacokinetic data and opioid conversion ratios and relevant tapering protocols identified through literature review. Then, plasma concentration-time curves of opioid infusions (1 µg/kg/h fentanyl, 10 µg/kg/h morphine), several opioid-methadone conversion ratios, and different methadone tapering protocols were simulated. Predicted methadone plasma concentrations were compared to minimal therapeutic concentrations (i.e., 1 ng/mL for fentanyl, 4 ng/mL for morphine, and 60 ng/mL for methadone). These simulations were reviewed by the expert panel consisting of pediatric intensivists and hospital pharmacists to establish recommendations. Simulations showed that a conversion ratio of 1:10 for fentanyl and 1:1 for morphine resulted in therapeutic methadone concentrations. Most previously established tapering recommendations resulted in equal maximum methadone concentrations, except for the low-risk tapering schedules of two of the three protocols. The robustness of these findings is reinforced by both a target attainment analysis and a sensitivity analysis employing the therapeutic target of methadone. The panel established consensus-based Dutch recommendations for conversion and tapering. These findings demonstrate that PBPK models can support dosing decisions by simulating clinical scenarios. The resulting recommendations have been implemented in the Dutch Pediatric Formulary, ensuring that the model-informed recommendations are directly applied in clinical practice.

PMID 42709714
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