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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

Related Research Articles

PubMedBMC pharmacology & toxicology2026-10-14

Correction to: In vitro comparative quality evaluation of different brands of metformin hydrochloride tablets available in Mekelle City, Tigray Regional State, Ethiopia.

Welegebrial Brhane Gebrehiwot BG, Gezae Zenawi Z, Gebrekidan Samrawit Kidanemariam SK, Gebrerufael Gebru Gebremeskel GG et al.

PubMedDrug metabolism and bioanalysis2026-10-14

Revisiting Cinacalcet HCl Hepatic Disposition: Insights from Isolated Perfused Rat Liver.

Mireskandari Katayoon K, Barazesh Ahmadreza A, Rostamnezhad Mostafa M, Darabi Majid M et al.

Hepatic drug handling determines systemic exposure, yet the balance between tissue uptake, intracellular binding, and metabolic clearance is difficult to dissect in vivo. Cinacalcet hydrochloride (CINA), a calcimimetic used to manage secondary hyperparathyroidism, has low oral bioavailability and is widely described as a high-extraction drug subject to extensive hepatic metabolism. Whether tissue sequestration rather than biotransformation underlies its rapid hepatic removal has not been tested directly in an intact ex vivo liver model. We investigated the hepatic clearance of cinacalcet hydrochloride (CINA) using the isolated perfused rat liver (IPRL) model. A validated high-performance liquid chromatography (HPLC) method was established to quantify CINA and its primary metabolite, M7, in both liver tissue and perfusate samples. To evaluate the influence of perfusate composition and protein binding, experiments were conducted under single-pass perfusion modes, in the presence and absence of bovine serum albumin (BSA). Dose recovery and mass balance analysis indicated that ~93% of the administered dose was recovered: ~63% in liver tissue and ~29% in the outlet perfusate. No metabolites were detected in any sample, pointing to tissue uptake and retention as the dominant clearance mechanism. Drug loss to plastic perfusion tubing was substantial and was only partially offset by BSA. Inclusion of BSA also shifted the apparent drug distribution between liver and perfusate. In the IPRL, hepatic tissue sequestration rather than metabolic conversion was the dominant clearance mechanism for CINA. Non-specific adsorption to plastic perfusion tubing and the protein content of the perfusion medium were important confounders that must be controlled in future ex vivo studies. CINA was extensively retained in rat liver tissue with negligible in situ metabolism over 90 min of single-pass perfusion, raising the question of whether metabolic extraction truly explains its low oral bioavailability in vivo.

PubMedRSC advances2026-10-14

CoAl2O4/Co3O4/boron and nitrogen doped biochar for round-the-clock ultra-efficient degradation of 4-nitrophenol with peroxymonosulfate.

Guo Haoran H, Xu Zixuan Z, Ding Xiaoli X, Li He H et al.

Developing a new strategy to boost the degradation efficiency of photocatalysts for toxic phenolic compounds in peroxymonosulfate (PMS)-based degradation processes was essential but remained an challenging task. Our study proposed the one-pot construction of CoAl2O4/Co3O4/boron and nitrogen doped biochar (CoAl2O4/Co3O4/BNC) to accelerate the PMS activation and enable ultra-fast degradation of 80 mg L-1 nitrophenol (4-NiP). Radical species (˙OH, SO4˙-, and h+) and non-radical (1O2) played crucial roles during the degradation process. Additionally, 4-NiP was effectively degraded across the full pH range. The catalyst's stability in simulated real aqueous environments was evaluated, demonstrating that the CoAl2O4/Co3O4/BNC exhibited excellent recyclability and anti-interference capability during degradation. Under UV-visible light irradiation, 80 mg L-1 of 4-NiP was degraded within 10 min, it has been demonstrated that illumination accelerates the activation of PMS and the photocatalytic degradation rate of 4-NiP. Furthermore, the degradation efficiency exceeded 95% for seven types of organic pollutants in different water matrices. Seven types of organic pollutants included levofloxacin (LEV), tetracycline (TC), doxycycline hydrochloride (DOX), ciprofloxacin (CIP), 2-chloro-4-nitrophenol (2C4Nip), 2-chloro-6-nitrophenol (2C6Nip), these results confirmed the capability of CoAl2O4/Co3O4/BNC to activate PMS for degrading organic pollutants in wastewater.

PubMedTalanta2026-10-14

Development of a high-throughput proteome sample preparation workflow based on efficient protein extraction to empower rational design of yeast cell factories.

Wu Yujie Y, Liu Jianhui J, Cheng Mengchun M, Yang Kaiguang K et al.

Mass spectrometry-based proteomics provides a powerful tool for the rational design of yeast cell factories. However, the rigid yeast cell wall architecture and the fast-growing scale of strain libraries present certain challenges for efficient protein extraction and high-throughput proteomic profiling. Conventional protein extraction methods either demand lengthy incubation periods or specialized equipment, leading to limited sample throughput and low efficiency. Herein, we report an efficient protein extraction strategy using a solvent combination of ionic liquid, guanidine hydrochloride, and lithium acetate under heat treatment (IGL-H). This method enables rapid protein extraction and is compatible with diverse yeast species across different growth phases. Compared with the classical glass bead grinding method, the IGL-H method affords higher protein yield and comparable or superior proteome coverage, and recovers higher proportions of integral membrane proteins of the endomembrane trafficking system. Furthermore, this method is readily amenable to liquid handling workstations for high-throughput proteome sample preparation by using magnetic solid-phase alkylation (mSPA) materials in less than 1.5 h, achieving Pearson correlation coefficients exceeding 0.97. Applying this pipeline to study proteome dynamics of Candida utilis under different nitrogen sources revealed an adaptive strategy involving carbon flux-specific allocation. These results establish the IGL-H extraction strategy as an effective solution for rapid protein extraction and high-throughput proteomic analysis of yeast strains, advancing rational cell factory design in synthetic biology.

PubMedChinese medical sciences journal = Chung-kuo i hsueh k'o hsueh tsa chih2026-10-14

Global epidemiological and indirect economic burden of neurological, mental, and substance use disorders: An analysis based on the global burden of disease data.

Tao Rong-Shan RS, Sun Zhi-Hong ZH, Long Rui-Yu RY

To evaluate the global disease burden and indirect economic costs of neurological, mental, and substance use disorders (NMSDs) from 1990 to 2023. This study analyzed data on incidence, prevalence, and disability-adjusted life years (DALYs) for NMSDs using data from the Global Burden of Disease 2023 database. Joinpoint regression analysis was used to calculate average annual percentage change. Spearman correlation was applied to examine the association between age-standardized rates and socio-demographic index (SDI). The indirect economic burden was estimated using the human capital approach, incorporating age-adjusted productivity weights and gross domestic product (GDP) per capita. From 1990 to 2023, the absolute numbers of incident cases, prevalent cases, and DALYs for NMSDs increased substantially, with DALYs for neurological and mental disorders approximately doubling. Age-standardized rates demonstrated divergent trends across disease categories. For mental disorders, the age-standardized incidence, prevalence, and DALY rates increased by 15.00%, 24.00%, and 29.00%, respectively, with the overall burden rising markedly in 2019. In contrast, while the overall burden of substance use disorders declined, a notable exception emerged in high-income North America, where rising rates were observed specifically for opioid and cocaine use disorders. The burden of neurological and mental disorders was higher in females than in males, whereas substance use disorders showed the opposite pattern. The age-standardized DALY rate for motor neuron disease exhibited a significant positive correlation with SDI (ρs = 0.82, P < 0.001). The indirect economic burden and its share of GDP increased in most countries, while the share for substance use disorders in China declined by 46.19%. The disease burden and economic costs of NMSDs increased globally from 1990 to 2023, with significant geographic, national, and demographic disparities. These findings highlight an urgent need for targeted resource allocation and integrated interventions.

PubMedDrug design, development and therapy2026-10-14

Ilioinguinal-Transversus Abdominis Plane (I-TAP) Block with Liposomal Bupivacaine for Analgesia After Cesarean Delivery: A Randomized Controlled Trial.

Pan Yun Y, Hu Xiaobing X, Fang Xin X, Zang Yu Y et al.

Cesarean delivery is frequently associated with suboptimal postoperative analgesia. While PROSPECT guidelines recommend transversus abdominis plane (TAP) block for post-cesarean analgesia, conventional TAP block may provide incomplete coverage of the L1 dermatome, potentially limiting analgesia for lower abdominal incisions. This study evaluated the efficacy and safety of ultrasound-guided ilioinguinal-transversus abdominis plane (I-TAP) block with liposomal bupivacaine after cesarean delivery. In this single-center, randomized controlled trial, 150 healthy parturients undergoing elective cesarean delivery under combined spinal-epidural anesthesia were allocated in a 1:1:1 ratio to I-TAP block, transversus abdominis plane (TAP) block, or sham block. The I-TAP and TAP blocks were performed using a mixture of 266 mg liposomal bupivacaine and 50 mg bupivacaine hydrochloride, diluted with 0.9% sodium chloride to a total volume of 60 mL. The primary outcome was the cumulative intravenous sufentanil consumption from the patient controlled intravenous analgesia (PCIA) device during the first 24 h after surgery. Secondary outcomes included 48 h PCIA sufentanil requirements, Quality of Recovery-15 (QoR-15) scores, pain scores, time to first rescue analgesia, time to ambulation, successful breastfeeding initiation, maternal satisfaction, and adverse events. At 24 h postoperatively, the I-TAP group had significantly lower sufentanil consumption than the TAP group (mean difference -11.4 μg, 95% CI: -17.6 to -5.3; 37.1% reduction) and the control group (mean difference -23.2 μg, 95% CI: -29.4 to -17.1; 54.5% reduction) (both P < 0.001). This difference persisted at 48 h. The I-TAP group also had lower postoperative pain scores, higher QoR-15 scores, longer time to first opioid rescue request, higher maternal satisfaction and higher rate of successful breastfeeding initiation. Adverse events were similar among groups. Compared with TAP block plus epidural hydromorphone and epidural hydromorphone alone, liposomal bupivacaine I-TAP block combined with epidural hydromorphone significantly reduced post-cesarean PCIA sufentanil requirements, improved postoperative analgesia and recovery quality, and increased maternal satisfaction without evidence of increased adverse events. This technique may provide a safe and effective option for implementation within multimodal analgesic strategy after cesarean delivery. ChiCTR2500112390.

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