Drug Database
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naltrexone (Exopio)

✓ Approved

Nanodaru · OPRK1 · 小分子

什么是 naltrexone?

naltrexone 是一种小分子,由Nanodaru研发。该药已获批,用于治疗相关适应症,给药途径:Injectable (Others)、Intramuscular (IM) Injection。

药物档案

商品名Exopio
公司Nanodaru
药物类别小分子
分子靶点OPRK1, OPRM1
给药途径Injectable (Others), Intramuscular (IM) Injection
状态Approved

作用机制

分子靶点

naltrexone 作用于 2 个分子靶点:

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

naltrexone 针对 2 个适应症,涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersAlcoholism✓ Approved
Psychiatric disordersDrug dependence✓ Approved

相关研究文献

PubMedCureus2026-10-25

Overlapping Post-COVID Conditions: A Case of Myalgic Encephalomyelitis and Postural Orthostatic Tachycardia Syndrome Triggered by Sequential Epstein-Barr Virus (EBV) and Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Infections.

Mayrink Magalhães Virgínia R VR, Ribeiro Oliveira Laura A LA, Lourenço Adelina J AJ, Ribeiro Camargos Isabela I et al.

The rise in post-infectious syndromes following COVID-19, such as Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS) and Postural Orthostatic Tachycardia Syndrome (POTS), has become increasingly common in clinical practice, representing an emerging clinical challenge. This case highlights a possible clinical scenario involving the interaction between sequential viral infections - such as the Epstein-Barr virus (EBV) and Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) - in triggering overlapping chronic conditions. This report presents the case of a patient who developed ME/CFS and POTS following SARS-CoV-2 infection, with a prior history of EBV mononucleosis, and discusses the diagnostic, therapeutic, and pathophysiological implications. A 48-year-old woman with a history of mononucleosis in childhood developed persistent and disabling symptoms after COVID-19 in January 2022. She presented with extreme fatigue, orthostatic intolerance, paresthesia, cognitive dysfunction, and multisystem symptoms. After extensive investigation, she was diagnosed with ME/CFS (early 2023) and POTS (later that year). Mast Cell Activation Syndrome (MCAS) was considered as a hypothesis during follow-up, but objective testing was not confirmatory. Management included pharmacological therapy (including low-dose naltrexone, duloxetine, and palmitoylethanolamide (PEA)), activity adjustments (pacing), and a multidisciplinary approach, with partial and fluctuating responses. This case illustrates how viral infections such as EBV and SARS-CoV-2 may act as sequential triggers in an individual clinical trajectory compatible with the development of ME/CFS and POTS. The symptomatic overlap, the lack of readily available objective biomarkers in this patient, and the need for a predominantly clinical and functional diagnostic approach in her evaluation highlight the complexity of these conditions. This experience also underscores the importance of continued efforts in research, clinical training, and integrated care models to improve the management of patients presenting with post-COVID conditions (PCC).

PMID 42927133
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PubMedFrontiers in psychiatry2026-10-23

Comparative efficacy of naltrexone-accelerated versus sublingual buprenorphine in opioid withdrawal management and initiating injectable naltrexone treatment: study protocol for a randomized controlled trial.

Jafari Saeede S, Rahimi-Movaghar Afarin A, Noroozi Alireza A, Malekifar Pooneh P et al.

Extended-release injectable naltrexone (XR-NTX), a long-acting opioid antagonist, is an effective relapse prevention strategy in the treatment of opioid use disorder (OUD). However, standard XR-NTX initiation requires completion of opioid withdrawal management and a 1-2 week opioid-free period. This interval is associated with heightened vulnerability to lapse and relapse, and many patients fail to initiate XR-NTX treatment successfully. Therefore, alternative strategies that enable rapid XR-NTX initiation are needed. This study aimed to compare the effectiveness and safety of naltrexone-accelerated (NA) versus sublingual buprenorphine (SB) withdrawal management in facilitating XR-NTX initiation among patients with OUD. This single-center, open-label, randomized controlled trial uses a parallel-group design. Eligible patients aged 18-60 years with moderate to severe OUD who are actively using opioids and are not receiving regular maintenance treatment with methadone or buprenorphine are randomly assigned to one of two groups: (1) NA withdrawal management, comprising one day of adjunctive non-opioid medications, one day of buprenorphine administration, one day of washout, and four days of gradual oral naltrexone titration (1, 3, 12, and 25 mg/day); or (2) SB withdrawal management, comprising one day of adjunctive non-opioid medications, six days of buprenorphine tapering (up to 8 mg on Day 2, 6 mg on Day 3, 4 mg on Days 4-5, 2 mg on Day 6, and 1 mg on Day 7), and a seven-day washout period. Adjunctive non-opioid medications in both groups comprised clonidine, clonazepam, gabapentin, and trazodone. The primary outcomes are the proportions of participants who (1) achieve a negative urine drug test for the assessed opioids and (2) receive XR-NTX at the end of the withdrawal management period. Secondary outcomes include severity of withdrawal symptoms, opioid craving intensity, and adverse effects. All analyses are conducted according to the intention-to-treat principle. The findings of this trial may provide clinically relevant evidence to support rapid initiation of XR-NTX treatment in patients with OUD and inform clinical practice. https://en.irct.ir/trial/81525, Iranian Registry of Clinical Trials IRCT20250123064499N1.

PMID 42909039
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PubMedBMJ open2026-10-23

Double-blind, placebo-controlled randomised clinical trial on flexible doses of escitalopram and naltrexone in the treatment of men with compulsive sexual behaviour disorder: study protocol presentation.

Lew-Starowicz Michał M, Draps Małgorzata M, Wilk Kacper K, Wisniewski Pawel P et al.

PMID 42919590
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PubMedSubstance abuse treatment, prevention, and policy2026-10-23

Treatment interventions for co-occurring opioid use disorder, and sleep disturbances: a scoping review.

Ruppert Elisabeth E, Rolling Julie J, Medde Alessandro A, Durpoix Amaury A et al.

Opioid use disorder (OUD) is part of the broader spectrum of substance use disorders often complicated by psychiatric symptoms such as depression, anxiety, PTSD (Post-Traumatic Stress Disorder), and sleep disturbances, with insomnia being particularly frequent. These psychiatric symptoms may act as precipitating factors and consequences of OUD, reinforcing a complex bidirectional relationship that complicates treatment and recovery. Despite the clinical importance of dual disorders, sleep impairments are particularly relevant yet understudied therapeutic targets and literature addressing sleep disturbances in the context of psychiatric symptoms or disorders in OUD remains limited. This scoping review examines pharmacological and non-pharmacological interventions of OUD and sleep disturbances in the presence of psychiatric disorders or symptoms, such as anxiety, depression, and PTSD. This review follows the Preferred Reporting Items for Systematic Reviews and Meta-analyses extension for Scoping Reviews (PRISMA-ScR) guidelines using the following keywords: ("sleep" OR "insomnia") AND ("depression" OR "anxiety" OR "PTSD" OR "post-traumatic stress disorder" OR "posttraumatic stress disorder") AND ("opioid use disorder" OR "OUD" OR "opioid addiction. Sleep disordered breathing was excluded. Participants were adults (> 18 years old) with OUD or opioid dependence undergoing withdrawal or treatment. The study focused on quantitative and qualitative study designs. Fifteen studies including 1,167 adults with OUD or opioid dependence were selected and categorized into pharmacological (targeting opioid or non-opioid receptors) and non-pharmacological interventions. Most interventions were adjunctive to opioid substitution or antagonist therapies. Naltrexone-induced insomnia was common but did not significantly affect mood and could be mitigated with lorazepam. Non-opioid pharmacotherapies yielded mixed results: guanfacine is suggested to increase insomnia risk but reduce stress and craving, while amitriptyline, prazepam, dronabinol, and neurotransmitter-precursor-supplements showed potential in improving sleep and withdrawal symptoms. Improved characterization and management of impaired sleep in individuals with OUD and psychiatric symptoms may reduce relapse risk, enhance emotional regulation, and decrease self-medication. Clinicians should consider the complex interplay between OUD, psychiatric symptoms, and sleep as part of comprehensive care. Further research is needed to clarify these interactions and support the development of integrated, evidence-based strategies for treatment and prevention. Not applicable.

PMID 42919383
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PubMedAdvances in anesthesia2026-10-22

Management of Patients on Medications for Opioid Use Disorder in the Perioperative or Peripartum Setting.

Awuku Breta B, Lai Benjamin B, Oberhelman-Eaton Sara S SS, Liu Mingchun M

There is an increasing proportion of surgical and obstetric patients on medications for the treatment of opioid use disorder (medications for opioid use disorder [MOUD]), formerly known as medication-assisted treatment, in the United States. Due to lack of institutional protocols and limited evidence-based guidelines, perioperative management of patients on MOUD has largely been varied and often provider-dependent. This article explores the current evidence and recommendations for perioperative and peripartum management of patients on buprenorphine, methadone, and naltrexone; as well as key principles for optimizing perioperative and peridelivery pain management.

PMID 42907083
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PubMedAddiction & health2026-10-20

Acute Olfactory Hypersensitivity to Opium and Cannabis Following Naltrexone Administration: A Rare Case Report.

Hosseini Seyed Hamzeh SH, Rafaiee Raheleh R

Naltrexone, a long-acting opioid receptor antagonist, is commonly utilized to avert relapse in individuals with opioid or alcohol dependence. While its efficacy in modifying cue-reactivity and lowering desire is well documented, less is known regarding its ability to elicit negative sensory-emotional reactions, particularly in response to olfactory stimulation. We present a rare case of a 16-year-old male with a history of cannabis usage who experienced acute episodes of respiratory distress after starting oral naltrexone (50 mg/day). These episodes were consistently triggered by the smell of opium or cannabis smoke, despite the patient's abstinence. The reactions were severe enough to necessitate multiple emergency medical procedures. The patient had a prior adverse reaction to morphine and a history of multiple drug allergies, suggesting a possible underlying sensitivity to opioid system modulation. The symptoms resolved after discontinuation of naltrexone. This case raises significant clinical and neurobiological concerns about the role of opioid antagonism in modifying olfactory and emotional processing. We propose that naltrexone-induced disinhibition in olfactory-limbic circuits may have contributed to heightened sensory gain and conditioned unpleasant reactions in a sensitized individual. More research is needed to understand the mechanisms driving this unusual yet important reaction.

PMID 42898469
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