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cocaine hydrochloride (Numbrino)

✓ Approved

Lannett · SCN5A · 小分子

什么是 cocaine hydrochloride？

cocaine hydrochloride 是一种小分子，由Lannett研发。该药已获批，用于治疗相关适应症，给药途径：Topical。

药物档案

商品名Numbrino
公司Lannett
药物类别小分子
分子靶点SCN5A
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Lannett

作用机制

分子靶点

cocaine hydrochloride 作用于 1 个分子靶点：

SCN5Asodium voltage-gated channel alpha subunit 5 (CMD1E, SSS1)
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

cocaine hydrochloride 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
Nervous system disordersAnaesthesia✓ Approved
Nervous system disordersSensory loss✓ Approved

相关研究文献

PubMedDrug and alcohol dependence2026-06-13

Efficacy signals in a 12-week trial of clavulanic acid to decrease cocaine use.

Maser Joya J, Callans Linda L, Yu Daohai D, Kampman Kyle K et al.

There is urgent need for effective medication to treat cocaine use disorder (CUD). Clavulanic acid (CLAV) is a clinical stage medication that has potential for treating CUD. Sixty-four participants with CUD were randomized and received either 500mg/day CLAV or matched placebo in a 12-week outpatient study, with dose escalation to 750mg/day in week 5 with continued use. There was no statistically significant improvement in the CLAV treatment group compared to the placebo group. However, women taking CLAV reduced use. Starting at week 4, women reported significantly more days without cocaine use relative to baseline than women taking placebo. During the last 3 weeks of the study, women taking CLAV had a median of 4.0 more days without cocaine per week relative to baseline compared to 0.6 days in the placebo group. CLAV treatment also reduced cocaine withdrawal symptoms in women relative to baseline compared to the placebo over the first 3 weeks of the study. No such trends were identifiable in men. At the 500-750mg/day dose there is a signal that CLAV is associated with a reduction in the number of days of cocaine use in women with CUD. Men with CUD did not benefit from CLAV treatment at these doses. CLAV for 12 weeks was safe and reasonably well tolerated in people with CUD. Future studies should refine a therapeutic dose for men with CUD and further elucidate the effect of CLAV on the observed effects in women.

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PubMedBMJ open2026-06-13

Minocycline hydrochloride ointment-assisted periodontal treatment of stage III/IV periodontitis associated with type 2 diabetes mellitus targeting Chinese people: study protocol for a randomised controlled trial.

Zhao Hongqiao H, Lin Sichi S, He Lu L, Zhen Min M et al.

Scaling and root planing (SRP) combined with adjunctive antibiotic therapy is widely adopted in the management of periodontitis in patients with type 2 diabetes mellitus (T2DM), with the aims of ameliorating glycaemic control, alleviating local inflammation and facilitating periodontal tissue regeneration. As a topically administered adjunctive antibiotic for periodontal treatment, minocycline hydrochloride (MH) ointment has shown favourable clinical efficacy in systemically healthy patients with periodontitis. However, robust evidence supporting its clinical efficacy and potential glycaemic-improving effects in patients with periodontitis complicated by T2DM remains limited. The present study is designed to test the null hypothesis that no significant differences in clinical outcomes exist between SRP combined with MH and SRP alone in the management of periodontitis among patients with T2DM, with its primary objective to investigate whether MH as an SRP adjunct confers superior clinical benefits to SRP alone. We will conduct a randomised, single-blind, placebo-controlled clinical trial. 56 patients with T2DM-associated stage III/IV periodontitis will be recruited from the Department of Periodontology, Peking University School and Hospital of Stomatology, Beijing, China. Eligible participants will be randomised into two groups: the experimental group will undergo SRP combined with topically administered MH ointment and the control group will undergo SRP with a matched placebo. The primary outcomes will include probing depth (PD) changes at periodontal pocket sites with a baseline PD ≥6 mm at 6 months post-baseline, with a specific focus on the percentage of such sites with PD reduced to ≤5 mm. The secondary outcomes will comprise PD changes at pocket sites with a baseline PD ≥5 mm at 6 months post-baseline, as well as clinical attachment loss, the plaque index, bleeding index, the levels of IL-1β, IL-17, calprotectin and insulin levels in gingival crevicular fluid and serum, complete blood count, blood biochemistry, including glycated haemoglobin levels, and the composition of subgingival plaques at baseline, and 2 and 6 months post-baseline. This study was approved by the Ethics Committee of Peking University School and Hospital of Stomatology (PKUSSIRB-2024102139b). Results will be published in a peer-reviewed scientific journal. ChiCTR2400092305. V.3.1 (date: 6 January 2026).

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In situ NMR investigation of the native chemical ligation (NCL) of N-terminal cysteines to alginate.

Bučak Gasser David D, Steindorfer Tobias T, Neshchadin Dmytro D, Gescheidt Georg G et al.

Polysaccharide-peptide conjugates constitute an important class of biomaterials for tissue engineering scaffolds and glycoconjugate vaccines. Yet, benign and chemoselective synthetic strategies that operate under aqueous, physiologically relevant conditions remain scarce. Herein, we present a proof-of-concept approach for the traceless conjugation of N-terminal l-cysteines to alginate. A glycine-derived thioester functionality was synthesized and covalently introduced onto the uronic acid residues of alginate (DS = 0.47), as confirmed by 1H and 13C NMR and ATR-IR spectroscopy. The resulting alginate-thioester derivative served as a hydrolytically stable and chemoselective reactive handle for the native chemical ligation (NCL) of l-cysteine hydrochloride (l-cys·HCl) and the dipeptide l-cysteinylglycine (l-cys-gly). The ligation reactions were monitored in situ by kinetic 1H NMR spectroscopy. Control experiments of the alginate-thioester derivative with alternative biological nucleophiles glycine and l-lysine showed no reactivity (1H NMR), thus confirming the selectivity toward the thiol functionality of N-terminal l-cysteines under the provided conditions (0.1 M PO43- buffer, pH 7, 25 °C). This work establishes a convenient aqueous method to prepare peptide-polysaccharide conjugates in which the peptide is linked to the polysaccharide exclusively through stable amide bonds, without the incorporation of exogenous linker molecules or the use of conventional coupling agents or protecting groups.

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Clinical Phenomenology of Bipolar Disorder With Substance Use Disorders: A Systematic Review.

Garvie Shivahn S, Sorkhou Maryam M, George Tony P TP

Bipolar disorder (BD) frequently co-occurs with substance use disorders (SUDs), including alcohol, cannabis, tobacco, stimulants, and opioids. Comorbid SUDs can worsen the clinical presentation of BD, contributing to more severe mood episodes, rapid cycling, and poorer recovery outcomes. However, the unique impacts of different SUDs on the BD clinical profile are less studied, potentially obscuring substance-specific effects on the course of illness and prognosis in BD. We conducted a systematic review of the literature (PubMed, PsycINFO) and identified N = 48 clinical studies exploring the clinical effects of specific SUDs on BD symptomatology, course of illness, and treatment outcomes. Our findings revealed that cannabis use disorder (CUD) and alcohol use disorder (AUD) are the most studied SUDs in BD. Concurrent CUD is frequently associated with increased manic episodes, rapid cycling, psychosis, and earlier BD onset, with mixed findings for depressive episodes, suicidality, and treatment outcomes. AUD is frequently linked with worse depression outcomes and increased suicidality, with mixed findings for manic symptoms, rapid cycling, age of onset, psychosis, and treatment outcomes. Other SUDs, including cocaine, tobacco, opioids, and methamphetamine, were underexplored but were linked to increased suicidality, hospitalizations, and medication nonadherence. Specific clinical profiles were associated with different SUDs, which underscores the need for more research to improve our understanding and treatment of comorbid BD-SUDs. Further research exploring non-alcohol and non-cannabis SUDs and utilizing more rigorous methodological designs is needed to clearly elucidate these associations and advance substance-specific interventions in BD patients.

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PubMedSeminars in vascular surgery2026-06-13

Role of illicit drug use in Type B aortic dissection and trial participation.

Matabele Mario M, Newhall Karina K, Drudi Laura M LM, Curi Michael A MA et al.

Cocaine and amphetamine use is strongly associated with Type B aortic dissection (TBAD). This disproportionately affects younger patients, who are more likely to present with complicated disease and experience greater postoperative morbidity. Stimulant-positive patients are often underrepresented or excluded from prospective trials evaluating optimal medical therapy, thoracic endovascular aortic repair, and perioperative management. Ethical concerns, medicolegal risk, stigma, and barriers to follow-up have further constrained trial participation, resulting in reliance on retrospective data and an absence of standardized management guidance. A literature review was conducted investigating the clinical presentation, medical and surgical management of stimulant-positive patients presenting with uncomplicated TBAD. We focused on anesthetic and ethical challenges unique to this population and explored the role of multidisciplinary care teams in perioperative care. Stimulant use precipitates acute sympathetic activation, labile hypertension, and increased aortic wall stress, complicating medical and procedural management. Routine stimulant screening may improve risk stratification and guide antihypertensive selection. Perioperative management should be guided by clinical evidence of intoxication rather than toxicology results. Nonurgent procedures should be deferred only in cases of active intoxication. Early multidisciplinary involvement-including addiction medicine, social work, and case management-may address barriers to medication adherence, reduce recurrence risk, and improve continuity of care. Stimulant-associated TBAD represents a distinct clinical entity requiring tailored medical, surgical, anesthetic, and psychosocial strategies. Standardized screening practices, evidence-based perioperative management, and integrated multidisciplinary care pathways may improve outcomes. Prospective studies and professional society guidance are needed to define best practices for this high-risk population.

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Negative impact of nasal septal perforation on quality of life: insights from 153 patients in a Spanish study.

Edo Berta Alegre BA, Rojas-Lechuga María Jesús MJ, Arenas Trinidad T, Cabezas Natalia Arango NA et al.

To evaluate the impact of nasal septal perforation (NSP) on sinonasal symptoms and quality of life (QoL) using patient-reported outcome measures. A prospective observational study was conducted between 2018 and 2024 in two referral centres. Clinical, demographic, symptom-related, and QoL data were collected for all included patients. A total of 153 patients with NSP were included. The main aetiologies were intranasal cocaine abuse (n = 57; 37.3%), post-sinonasal surgery (n = 47; 30.7%), and rhinotillexomania (n = 31; 20.3%). The mean age was 47.8 years (SD 12.9; range 18.2-82.3), and 60.8% of patients were male. Anterior perforations were the most frequent location (n = 88; 57.5%). Mean perforation dimensions were 15.8 mm (SD 6.7) in height and 22.0 mm (SD 10.6) in length, with an estimated elliptic area of 312.9 mm² (SD 265.1; range 14.1-1272.3 mm²). The most frequent and severe symptoms reported on visual analogue scales were nasal obstruction (mean 58.3; SD 28.7), crusting (55.3; SD 34.9), and rhinorrhoea (44.8; SD 34.6). Quality of life was markedly impaired, with mean scores of 46.9 (SD 23.1) on the SNOT-22, 25.3 (SD 10.1) on the NOSE-Perf, and 24.1 (SD 10.1) on the SEPEQOL. The SF-36 physical and mental component summary scores were 45.0 (SD 10.5) and 40.5 (SD 14.2), respectively. NSP is associated with a significant burden of sinonasal symptoms and a substantial impairment in quality of life. Patient-reported outcome measures demonstrate an impact on both physical and mental health domains, underscoring the importance of a comprehensive and multidisciplinary approach to the evaluation and management of patients with NSP.

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