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lidocaine hydrochloride (3268 / lignocaine, Anesiva / ALGRX 3268)

✓ Approved

Marathon Pharmaceuticals · SCN9A · Small Molecule

What is lidocaine hydrochloride?

lidocaine hydrochloride is a small molecule developed by Marathon Pharmaceuticals. It is approved for therapeutic indications via injectable (others) or intradermal injection.

Drug Profile

Brand Names3268, lignocaine, Anesiva, ALGRX 3268
CompanyMarathon Pharmaceuticals
Drug ClassSmall Molecule
Molecular TargetSCN9A
RouteInjectable (Others), Intradermal Injection
StatusApproved

Mechanism of Action

Molecular Targets

lidocaine hydrochloride acts on 1 molecular target:

SCN9Asodium voltage-gated channel alpha subunit 9 (SFNP, GEFSP7)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

lidocaine hydrochloride is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Nervous system disordersAnaesthesia✓ Approved
Nervous system disordersSensory loss✓ Approved

Related Research Articles

PubMedBehavioural brain research2026-07-25

Activation of Mitophagy by Lidocaine Limits mROS and Prevents Microglial M1 Polarization to Alleviate Postoperative Delirium.

Wang Qingfu Q, Du Qiang Q, Chen Xilin X, Ni Lifeng L et al.

Postoperative delirium (POD) is a common complication in elderly patients, yet effective interventions remain limited. Mitochondrial dysfunction and microglial M1 polarization contribute to POD pathogenesis, but the underlying mechanisms are incompletely understood. This study aimed to investigate whether lidocaine (LID) ameliorates POD by activating mitophagy to suppress mitochondrial reactive oxygen species (mROS) and inhibit M1 microglial polarization. A mouse model of POD was established by laparotomy in male C57BL/6J mice, which were randomly divided into four groups (n=6 each): sham, POD, POD+LID (8mg/kg, i.v.), and POD+LID+Mdivi‑1 (25mg/kg, i.p.). Behavioral tests (open field and Y‑maze), serum inflammatory and oxidative markers, hippocampal histology, mitophagy-related proteins, microglial polarization markers, mROS, and ATP were assessed. In vitro, LPS-stimulated BV2 cells were treated with LID (10μg/mL), Mdivi‑1 (5μM), or the mROS scavenger Mito‑TEMPO (1.5mM) to evaluate mitochondrial function, mROS, and polarization. LID treatment significantly improved behavioral performance, as evidenced by increased central zone exploration and Y‑maze alternation rate, reduced serum TNF‑α and IL‑1β, elevated IL‑10, and attenuated oxidative stress (decreased MDA, increased SOD) in POD mice. LID also restored hippocampal mitochondrial morphology, enhanced mitophagy (reduced p62, increased PINK1, Parkin, and LC3‑II/LC3‑I ratio), and shifted microglial polarization from M1 (decreased CD86/iNOS) to M2 (increased CD206/Arg‑1). All these effects were reversed by Mdivi‑1. In BV2 cells, LID reduced pro‑inflammatory cytokines (TNF‑α, IL‑1β), increased IL‑10, restored mitochondrial membrane potential, decreased mROS, and promoted M2 polarization; these effects were blocked by Mdivi‑1 and rescued by Mito‑TEMPO. LID activates mitophagy, reduces mROS, and promotes M2 microglial polarization, thereby alleviating POD, highlighting its therapeutic potential.

PubMedCanadian journal of ophthalmology. Journal canadien d'ophtalmologie2026-07-25

A case of bupivacaine-induced cardiotoxicity during a blepharoplasty.

Becker Bruce B BB, Goodyear Kendall K

Bupivacaine is the most cardiotoxic local anesthetic. We present a case of a healthy 63-year-old female with no history of arrhythmias, ischemia, or other cardiac disease who had a cardiac arrest caused by bupivacaine during a blepharoplasty. A 63-year-old healthy female with no history of arrhythmias, ischemia or other cardiac disease presented for an upper and lower blepharoplasty. Intraoperatively a total of 12 ccs of 1:1 lidocaine 2% with 1:100,000 epinephrine and bupivacaine 0.50% with 1:100,000 epinephrine was given subcutaneously and subconjunctivally in the lower eyelids. The patient developed ventricular tachycardia progressing to asystole 5 minutes after the injections. Cardiopulmonary resuscitation led to a return of circulation. Extensive investigations, including consultations with cardiologists and electrophysiologists, ruled out underlying cardiac pathology, and the cardiac arrest was determined to result from bupivacaine cardiotoxicity. This case highlights the potential for cardiac complications from the local administration of bupivacaine. It emphasizes the need for cardiac monitoring and the resources for cardiopulmonary resuscitation when using bupivacaine in periorbital anesthesia.

PubMedInternational journal of pharmaceutics2026-07-25

Development of propranolol hydrochloride extended-release lipid matrix tablets for pediatric use.

Broocks Stefanie S, Gebhardt Melanie M, Klein Sandra S

Although solid oral dosage forms are widely used in adult drug therapy, age-appropriate formulations for pediatric patients remain limited. The development of suitable dosage forms is challenged by specific requirements regarding excipient safety, tablet size, and dose flexibility, as well as the need to improve therapy adherence in the context of frequent dosing. This study aimed to develop a pediatric-appropriate extended-release matrix tablet based on lipid matrix formers, with particular attention to the use of safe excipients and the selection of excipients based on sustainability considerations. Lipid-based excipients, selected due to their natural origin and similarity to dietary fats, were investigated and compared with conventional matrix formers. A formulation screening approach was applied to identify promising candidates based on drug release after one hour, followed by further evaluation of manufacturability, tablet hardness, and extended-release performance. In addition, the influence of a physiological pH-gradient, bile salts, and long-term storage on drug release was assessed. The selected formulations showed good manufacturability, uniformity, and sustained drug release. Overall, several lipid-based matrix formulations suitable for pediatric use were identified, providing a promising basis for the development of solid oral extended-release dosage forms for children.

PubMedFrontiers in immunology2026-07-25

Multifunctional antimicrobial effects of Lactobacillus johnsonii against A/E pathogens Enteropathogenic E. coli and Citrobacter rodentium.

Vasamsetti Sai Madhuri SM, Khaderbad Yasaswi Y, Sarmah Novelina N, Atham Hari Naga Papa Rao HNPR et al.

Enteropathogenic Escherichia coli (EPEC) remains a leading cause of childhood diarrhea in low-resource settings, and escalating antimicrobial resistance necessitates non-antibiotic therapeutic approaches. This study investigates Lactobacillus johnsonii as a probiotic candidate capable of limiting A/E-pathogen colonization and attenuating infection-associated intestinal inflammation. The probiotic properties of L. johnsonii were evaluated through assays of gastrointestinal tolerance, epithelial adhesion, antimicrobial activity, biofilm inhibition, and pathogen exclusion. Secreted antimicrobial activity was investigated by fractionation and untargeted metabolomic profiling. Therapeutic efficacy was further assessed in an antibiotic-perturbed Citrobacter rodentium mouse infection. L. johnsonii exhibited robust gastrointestinal resilience (acid pH 1.5-2.5; 0.3% bile) and strong adhesion to human intestinal epithelial cells. In vitro, live L. johnsonii markedly inhibited EPEC growth, disrupted pre-formed biofilms, and displaced adherent pathogens from epithelial surfaces. In an antibiotic-perturbed Citrobacter rodentium infection model, oral L. johnsonii administration reduced pathogen loads in feces and colonic tissues by 3-4 log units, restored colon length, and alleviated epithelial ulceration and inflammatory infiltration. Mechanistic analyses revealed dual antimicrobial actions: nutrient competition and secretion of low-molecular-weight (<75 kDa) bactericidal factors active at ~30 µg mL-1. Untargeted metabolomic profiling of the active fraction generated putative annotations of chemically diverse small molecules, including fatty-acid and hydroxy-acid class compounds, as well as candidate metabolites such as quinine hydrochloride, aloperine, and γ-glutamylglutamine, thereby providing a foundation for future targeted validation of individual antimicrobial components. Notably, probiotic treatment reduced mucosal neutrophil infiltration and preserved epithelial architecture, suggesting attenuation of infection-associated inflammation. Collectively, these findings support L. johnsonii as a multifunctional probiotic that integrates biofilm disruption, metabolic competition, and immune-protective activity. The study highlights its translational potential as a probiotic-based intervention to manage attaching-and-effacing enteric infections and mitigate antibiotic reliance in vulnerable populations.

PubMedHospital pharmacy2026-07-25

Artificial Intelligence and Large Language Models as Decision-Support Tools in Hospital Compounding Pharmacy: A Proof-of-Concept Study.

Castellana Eleonora E, Chiappetta Maria Rachele MR

To evaluate the efficiency and reliability of a large language model (LLM) as a decision-support tool in hospital compounding pharmacy for pediatric extemporaneous preparations requiring assessment of drug crushability, regulatory compliance, and formulation feasibility. A proof-of-concept study compared a structured LLM-assisted workflow with the traditional manual information retrieval process in a hospital pharmacy setting. The LLM (Claude Sonnet 4.6) was configured with a standardized prompt to extract and consolidate data from multiple authoritative sources: the Friuli Venezia Giulia "Do Not Crush" list, the Italian Medicines Agency (AIFA) database for Summary of Product Characteristics (SmPC), AIFA Law 648/96 off-label use lists, and the Stabilis database for oral liquid formulation stability. Two representative drugs, propranolol hydrochloride and imatinib mesylate, were analyzed. For each drug, the model generated a structured output including crushability, regulatory information, off-label status, and extemporaneous formulation data. The same queries were manually performed by an experienced hospital pharmacist. Primary outcome was information retrieval time; secondary outcomes included completeness and accuracy. The LLM-assisted workflow reduced retrieval time to less than 2 minutes per drug (mean 1 minute 45 seconds), compared with a mean of 20 minutes (range 15-25 minutes) for the manual process, plus an additional 5 to 10 minutes for transcription. Output completeness was 100%, with all predefined fields correctly populated. The model accurately classified drug crushability and correctly identified Law 648/96 regulatory status. For propranolol, the system identified crushability, pediatric off-label authorization, and SyrSpend-based formulations with stability data of up to 146 days at room temperature. For imatinib, the model highlighted cytotoxic handling precautions, identified the absence of SyrSpend formulations, and retrieved alternative formulation stability data (30 days refrigerated). A properly configured LLM can function as an effective decision-support tool in hospital compounding pharmacy, improving efficiency while maintaining high standards of completeness, accuracy, and regulatory compliance. These preliminary results support further investigation into the integration of the LLM system into routine pediatric galenical preparation practice.

PubMedCutis2026-07-24

Predictors of Lidocaine Volume Used During Mohs Micrographic Surgery.

Varghese Kevin K, Kuckelman Dreah D, McClure Spencer S, Jibbe Atieh A

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