Drug Database
CO

cocaine hydrochloride (Numbrino)

✓ Approved

Lannett · SCN5A · Small Molecule

What is cocaine hydrochloride?

cocaine hydrochloride is a small molecule developed by Lannett. It is approved for therapeutic indications via topical.

Drug Profile

Brand NamesNumbrino
CompanyLannett
Drug ClassSmall Molecule
Molecular TargetSCN5A
RouteTopical
StatusApproved

Mechanism of Action

Molecular Targets

cocaine hydrochloride acts on 1 molecular target:

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

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

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

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Multicenter toxicological analysis of psychoactive substances in suicide victims in Brazil.

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To assess the prevalence and toxicological profile of psychoactive substance use among coroner-certified suicide cases in Brazil. We conducted a multicenter cross-sectional study using probabilistic post-mortem blood sampling of suicide victims autopsied at the Institutes of Forensic Medicine between March 2022 and June 2024. Data were collected from forensic units covering metropolitan areas of the state capitals of Pará, Pernambuco, Espírito Santo, and Paraná. Alcohol and other psychoactive substances were analyzed using headspace-gas chromatography and liquid chromatography-tandem mass spectrometry. Among 330 suicide victims, 54.4% tested positive for at least one psychoactive substance. Alcohol was the most detected substance (29.4%), followed by cocaine (21.2%) and benzodiazepines (20.3%). Polysubstance use occurred in 14.5% of cases, most involving simultaneous use of alcohol and cocaine. Substance-positive victims were younger than those without detectable substances (median age: 38 vs. 44 years, p = 0.04). Cocaine use was associated with concurrent alcohol use (OR: 4.05; 95% CI: 2.33-7.03) and death by asphyxia (OR: 2.65; 95% CI: 1.25-5.60). This multicenter toxicological study, the first in Brazil, shows that psychoactive substances are prevalent among suicide victims, with alcohol, cocaine, and benzodiazepines most often detected. The co-use of alcohol and cocaine, especially among younger victims, underscores a risk profile that may intensify lethality. Broader surveillance and longitudinal designs are needed to clarify causal links and strengthen suicide prevention strategies that integrate toxicological evidence with mental health and substance use care.

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Investigation of the Mechanism of Cinnamaldehyde in Irritable Bowel Syndrome Based via Network Pharmacology, Molecular Docking, and Animal Experiments.

Yu Qingyang Q, Xu Boqing B, Dai Chunfang C, Pang Yayan Y et al.

Irritable bowel syndrome (IBS) is a prevalent functional gastrointestinal disorder characterized by abdominal pain and changes in bowel habits. Cinnamaldehyde (CA) possesses anti-inflammatory, antibacterial, and digestive-regulatory properties. However, its therapeutic potential for IBS and mechanisms are not understood. We employed network pharmacology to identify potential targets and pathways of CA against IBS. Core targets were validated through molecular docking, and further verified in an IBS rat model induced by neonatal maternal separation (NMS) and water avoidance stress (WAS). Network pharmacology identified 139 potential targets of CA related to IBS. Gene Ontology (GO) enrichment analysis highlighted key biological processes, cellular components, and molecular functions. Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis suggested involvement of pathways such as nitrogen metabolism, tyrosine metabolism, and cocaine addiction. A protein-protein interaction (PPI) network revealed 11 major targets, and molecular docking demonstrated strong binding affinities between CA and several targets, particularly MAOB, PARP1, HDAC1, JAK2, and MMP2. Animal experiments confirmed that CA significantly reduces MAOB, as well as TNF-α, IL-6, and IL-1β levels, thereby alleviating visceral hypersensitivity and anxiety and depression-like behaviors in IBS rats. These findings provide a scientific basis for developing CA as a potential natural therapeutic agent for IBS.

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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.

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The Epidemiology of HIV and Injection Practices Among People Who Inject Drugs in Nigeria: Results from the 2020 Integrated Biological and Behavioural Surveillance Survey.

Shaw Souradet Y SY, Green Kalada K, Ejeckam Chukwuebuka C, Adesina Adediran A et al.

People who inject drugs (PWID) are an important driver of the HIV epidemic in Nigeria. This study describes the HIV, demographic, and injection characteristics of PWID. Cross-sectional integrated biological and behavioural survey conducted in 2020 across 12 states in Nigeria. HIV seroprevalence based on screening and confirmatory tests, and self-reported data on socio-demographic and injection/sharing practices. Multivariable logistic regression models estimated crude and adjusted odds ratios (A/ORs) and 95% confidence intervals (95% CIs) of factors associated with HIV prevalence, and injection and sharing practices. Among 4,358 participants, weighted HIV prevalence was 10.9%. Median age was 30 years (IQR: 25-35) with two-thirds reporting less than 75 months of injection drug use. 80% of participants reported injecting in the last month. Of those injecting in the last month, 21% reported injecting at least once a day, 15% reported "almost/every time" to sharing or lending syringes/needles, while 9% reported back/front-loading, sharing paraphernalia, or drawing up from a common container "almost/every time". In multivariable models, female sex (AOR: 1.6, 95% CI: 1.2-2.1) and less than secondary education (AOR: 1.4, 95% CI: 1.1-2.0) was associated with HIV. Riskier injection practices were associated with pentazocine (AOR: 1.7, 95% CI: 1.2-2.4) and crack cocaine (AOR: 2.0, 95% CI: 1.4-2.8) injection. HIV prevalence was high amongst study participants, as were riskier injection and sharing practices, with structural determinants like education being associated with both.

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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.

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