Lidocaine Research Articles

Clinical observation of sinus tarsi syndrome after lateral ankle sprain

To study the incidence rate of sinus tarsi syndrome after lateral ankle sprain and observe the clinical efficacy of sinus tarsal corticosteroid injections. From January 2021 to Janury 2022, 391 patients with lateral ankle sprain and 88 patients with sinus tarsi syndrome using corticosteroid injections (compound betamethasone 1 ml+ lidocaine hydrochloride 4 ml) were retrospectively analyzed. There were 22 males and 66 females, aged from 29 to 60 years old with an average of (41.00±7.52) years old, duration of the disease from 1 to 12 months with an average of (5.6±4.2) months. The visual analogue scale(VAS) and American Orthopedic Foot and Ankle Society(AOFAS) scores were collected before, 1 month, 3 months, 6 months, and 12 months after treatment. All 88 patients completed a 12-month follow-up. The incidence rate of sinus tarsi syndrome after lateral ankle sprain was 22.5%. One month after treatment, VAS was 1.20±0.89, AOFAS score was 88.70±7.04. Three months after treatment, VAS was 1.60±1.35, AOFAS score was 85.20±10.95. Six months after treatment, VAS 2.35±1.39, AOFAS 80.30±9.75. Twelve months after treatment, VAS was 2.80±1.51, AOFAS score was 79.1±9.94. Significant differences were found before and after treatment at all four time points of follow-up(P<0.05). The results of this study showed that the incidence rate of sinus tarsi syndrome after lateral ankle sprain was 22.5%. Corticosteroid injections were effective in the short term with a 65% recurrence rate of symptoms within 1 year. For patients with no significant long-term effect of conservative treatment, clinicians may explore alternative approaches, including options like ankle arthroscopy.

One-pot RPA/CRISPR-Cas12a assay with photomodulated aptamer-based inhibitors

CRISPR diagnostic methods are attracting attention in nucleic acid testing (NAT) due to their sensitivity, specificity, and simplicity. To enhance the sensitivity and eliminate the risk of contamination associated with lid opening, a one-pot reaction combining the CRISPR system with recombinase polymerase amplification (RPA), a compatible amplification method, is used. However, the cleavage activity of the CRISPR system affects the efficiency of RPA, thereby limiting its effectiveness. In this study, we propose a one-pot RPA/CRISPR-Cas12a system that achieves high sensitivity through photomodulation. By utilizing a Cas12a inhibitory aptamer with a photocleavable (PC) linker, the Cas12a ribonucleoprotein can be temporarily inactivated, preventing it from degrading the RPA component during nucleic acid amplification. Upon completion of the amplification, brief UV irradiation can cleave the PC linker, allowing the Cas12a reaction to proceed and generate a fluorescence signal. This approach effectively eliminates the risk of contamination, achieves high specificity, and mitigates factors contributing to a reduction in sensitivity. Using this photomodulated one-pot RPA/CRISPR-Cas12a assay, we successfully detected the p72 gene of African swine fever virus at a concentration of 50 copies (2.5 copies/µL). This efficient one-pot assay exhibits high sensitivity, cost-effectiveness, simplicity, and a stable design, making it a highly promising technique for field diagnostics in NAT applications.

Global facial rejuvenation with hyaluronic acid: a safe set of directives to whole-approach of the aging-changes evaluated by magnetic resonance imaging

Background: Face rejuvenation with hyaluronic acid (FR-HA) through a global approach was performed in a single session, by using a safe set of directives targeted for each facial zone. Methods: FR-HA was performed with products of the QTFill Signature® range all of them with same HA-concentration and molecular-weight, with two crosslinking technologies, the own Ultra-High-Density™ crosslinking and BDDE-crosslinking with tree degrees of BDDE, resulting in high-, medium- and low-G', and 3.0% of lidocaine hydrochloride. Bolus injection with needle and retrograde-backflow injection with microcannula or needle were directed to specific facial zones. A safe FR-HA protocol based on HA-products, fat layers and vasculature, and points and techniques of injection recovered the face youthful appearance. Results: FR-HA was made for eleven facial zones, patient average of 6.95±1.30, average of 30.55±0.74 injections-points per facial-zone and of 16.80±0.83 injections-points per patient. The volume of HA injected was 49.50 ml, average of 4.50±0.37 ml per facial zone and 2.48±0.12 ml per patient. From one-month to twelve-months there was no significant differences on the face appearance and on density of the gel-diffusion displayed by MRI in T2-weighted with fat suppression on axial and coronal planes, which were endorsed by the Facelift Outcomes Evaluation questionnaire scores. Conclusions: Minimal changes on clinical outcomes and slow degradation of gel-diffusion on MRI in T2-weighted with fat suppression on axial and coronal planes from one-month to twelve-months showed that the HA-products remained stable in the injection site without evidence of significant resorption or loss of correction, indicating FR-HA efficacy and long-lasting.

Comparative Study on the Efficacy of Lignocaine Nebulisation Vs Topical Lignocaine Spray in Attenuation of Haemodynamic Surge in Patients Undergoing Surgery Under General Anaesthesia - A Single Blinded Randomized Controlled Study

Introduction: Laryngoscopy and tracheal intubation are powerful noxious stimuli that should be attenuated. The present study is to compare the efficacy of lignocaine nebulisation vs topical lignocaine spray in attenuation of haemodynamic surge in patients undergoing surgery under general anaesthesia. Methodology: After ethical committee clearance, a single blind randomized control study was done on sixty patients of either sex aged between 18-55 years of ASA status I undergoing elective surgery under general anaesthesia with endotracheal intubation. Patients were randomly allocated into 2 groups: GROUP A:received nebulised Lignocaine Hydrochloride 4% at 2 mg/kg. GROUP B: received Topical Lignocaine spray 10% at 2mg/kg. Heart rate, Systolic, diastolic and mean blood pressure was documented before administering premedication (T0), at the time of intubation (TI) and at 1min (T-1), 2min (T-2) &amp; 5min (T-5) after intubation. Attenuation in HR, SBP, DBP and MBP were found statistically significant (p&lt;0.05) in group A in comparison to group B. Thus in conclusion Lignocaine nebulisation is far more effective in comparison to topical lignocaine spray in attenuation of the laryngoscopic surge. Results: After conducting the study on a total of sixty patients it was found that there was statistically significant reduction in SBP, DBP, MBP and HR in GROUP A receiving lignocaine nebulisation compared to GROUP B receiving topical lignocaine spray. Conclusion: Lignocaine nebulisation is more effective than topical lignocaine spray in attenuation of haemodynamic surge following laryngoscopy and intubation in patients undergoing surgery under general anaesthesia. Keywords: Laryngoscopy, Tracheal Intubation, Lignocaine Nebulisation, Lignocaine Spray, Heamodynamic Surge

Polymeric Nanocapsules Loaded with Lidocaine: A Promising Formulation for Topical Dental Anesthesia.

Lidocaine is the most commonly used local anesthetic worldwide, known for its rapid onset and moderate duration of anesthesia. However, it is short-lived and does not effectively promote effective topical anesthesia in the oral cavity when used alone. Our aim was to investigate whether an approximate 50% encapsulation of lidocaine in poly(ε-caprolactone) nanocapsules (LDC-Nano) would be able to increase its permeation and analgesic efficacy and reduce cytotoxicity. In this study, we characterized LDC-Nano and conducted MTT tests with HaCaT cells to assess their in vitro cytotoxicity. Additionally, in vitro permeation assays across the pig esophageal epithelium and the anesthetic efficacy of the hind paw incision model in rats were performed. Plain lidocaine (LDC) was compared with LDC-Nano and lidocaine hydrochloride plus epinephrine (LDC-Epi). The physicochemical characteristics of LDC-Nano were satisfactory (pH: 8.1 ± 0.21; polydispersity index: 0.08 ± 0.01; mean diameter (nm): 557.8 ± 22.7; and encapsulation efficiency (%): 51.8 ± 1.87) and remained stable for up to 4 months. LDC-Nano presented similar in vitro cytotoxicity to LDC but was higher than LDC-Epi (LD50: LDC = 0.48%; LDC-Nano = 0.47%; and LDC-Epi = 0.58%; p < 0.0001). Encapsulation increased the permeability coefficient about 6.6 times and about 7.5 the steady-state flux of lidocaine across the mucosal epithelium. Both encapsulation and epinephrine improved anesthesia duration, with epinephrine demonstrating superior efficacy (100% of animals were anesthetized up to 100, 30, and 20 min when LDC-Epi, LDC-nano, and LDC were used, respectively). Although LDC-Epi demonstrated superior in vivo anesthetic efficacy, the in vitro permeation and cytotoxicity of LDC-Nano indicate promising avenues for future research, particularly in exploring its potential application as a topical anesthetic in the oral cavity.

WITHDRAWN: [Translated article] In vitro elution of local anaesthetics from PMMA bone cement

Background and aimCurrently, we do not have a gold standard for pain management after total knee arthroplasty. We may use one of more drug delivery systems, none of which are ideal.An ideal depot delivery system would provide therapeutic, nontoxic, doses of drug at the surgical side, especially during 72h postoperatively.The bone cement used in arthroplasties has been used as a drug delivery system, especially antibiotics, since 1970. Based on this principle, we developed this study with the aim to characterize the elution profile of two local anaesthetics (lidocaine hydrochloride and bupivacaine hydrochloride) from PMMA (polymethilmethacrylate) bone cement. Material and methodsPalacos® R+G bone cement and lidocaine hydrochloride or bupivacaine hydrochloride specimens were obtained depending on the study group. These specimens were immersed in PBS (phosphate buffered saline) and removed from the solution at different set times.Subsequently, the concentration of local anaesthetic in the liquid was analyzed by liquid chromatography. ResultsThe percentage of lidocaine eluted from PMMA bone cement in this study was 9.74% of the total lidocaine content per specimen at 72h and 18.73% at 336h (14 days). In case of bupivacaine, the elution percentage was 2.71% of the total bupivacaine content per specimen at 72h and 2.70% at 336h (14 days). ConclusionsLocal anaesthetics elute in vitro from PMMA bone cement, reaching doses at 72h close to the doses used in anaesthetic blocks.

Physiological responses of jundiá Rhamdia quelen juveniles anesthetized with different concentrations of lidocaine hydrochloride (Lidostesim® 3%)

The aim of this trial was to determine the effect of lidocaine hydrochloride-based immersion anesthesia in concentrations of 1,000, 1,500, 2,000 and 2,500 mg L-1 on physiological responses of jundiá Rhamdia quelen, with the control group anesthetized with clove oil (50 mg L-1) bath anesthesia. Ten jundiá juveniles were used in each experimental and control groups in order to analyze the hematocrit, blood glucose levels and induction and recovery times. Jundiás anesthetized in 2,000 and 2,500 mg L-1 solutions showed percentual hematocrit increase (42.7 ± 0.9% and 43.7 ± 0.7 %, P &lt; 0.05). It was observed inverse association between blood glucose levels and lidocaine concentration, with values ranging from 57.3 ± 14.7 mg dL-1 to jundiá anesthetized in 1,000 mg L-1 and 39.5 ± 12.5 mg dL-1 in 2,500 mg L-1 anesthetic baths, with higher values detected in the control group (78.1 ± 12.5 mg dL-1, P &lt; 0.001). Likewise, it was observed inverse relationship between lidocaine hydrochloride concentration and induction times, but direct association with recovery times. Higher concentrations were the most effective as blood glucose reduction and maintenance of hematocrit levels, with promising induction and recovery times for future anesthetic trials.

Determination of chromatographic conditions for quantitative assessment of active components in complex nasal spray after manufacturing and expiry date

The aim of the work is the development of chromatographic conditions, the study of the validation characteristics of the method of quantitative determination of phenylephrine hydrochloride, nitrofural, lidocaine hydrochloride and diphenhydramine hydrochloride, panthenol, povidone in the joint presence in the nasal spray by a complex method of liquid chromatography with UV detection. Evaluation of the quantitative content of active components after manufacturing and during the shelf life.&#x0D; Materials and methods. Agilent 1260 liquid chromatographs, equipped with a diode-matrix detector from the company "Agilent technologies", USA. Chromatographic columns 250×4.6 mm in size, filled with octadecylsilyl silica gel for chromatography (Zorbax StableBond SB-Aq, Agilent company), mobile phase A - phosphate buffer solution pH 7.0 - acetonitrile P (1650:350), mobile phase B – acetonitrile P; elution mode – gradient; mobile phase flow rate – 1.0 ml/min; detection wavelengths – 220 nm (for panthenol, phenylephrine, povidone, diphenhydramine) and 235 nm (for nitrofural and lidocaine).&#x0D; Results. Chromatographic separation conditions were developed for the co-presence determination of six target substances: panthenol, phenylephrine hydrochloride, nitrofural, povidone, lidocaine hydrochloride and diphenhydramine hydrochloride. The suitability of the technique for this task was confirmed by determining the validation characteristics. The methodology at the appropriate level is characterized by specificity, linearity, correctness and convergence in the range of application for panthenol (range 20.33-38.26 mg/ml, ΔZ=0.93 ≤ max ΔZ=3.20, a=0.63 max a=5.12, r = 0.9978 min r= 0.9924), phenylephrine hydrochloride (range 1,70-3,21 mg/ml, ΔZ=0.51 ≤ max ΔZ=3.20, a=0.15 max a=5.12, r = 0.9984 min r= 0.9924), nitrofural (range 0.137-0.257 mg/ml, ΔZ=0.91 ≤ max ΔZ=3.20, a=0.032 max a=5.12, r = 0.9987 min r= 0.9924) povidone (range 20,44-38,50 mg/ml, ΔZ=0.23 ≤ max ΔZ=3.20, a=2,33 max a=5.12, r = 0.9942 min r= 0.9924), lidocaine hydrochloride (range 6,80-12,81 mg/ml, ΔZ=0.34 ≤ max ΔZ=3.20, a=0.66 max a=5.12, r = 0.9988 min r= 0.9924), diphenhydramine hydrochloride (range 1,36-2,56 mg/ml, ΔZ=0.20 ≤ max ΔZ=3.20, a=0.15 max a=5.12, r = 0.9980 min r= 0.9924). There are no significant changes when stored at 25 °C for 6 months.&#x0D; Conclusions. An analytical method of quantitative determination of the component composition in an extemporaneous nasal spray by a complex method of high-performance liquid chromatography has been developed. The determined validation parameters confirm the correctness of the methodology. The chemical stability of the dosage form is observed for 6 months

Molecular dynamics simulations shows real-time lid opening in Hsp70 chaperone

The stress-inducible mammalian heat shock protein Hsp70 and its bacterial orthologue DnaK are highly conserved molecular chaperones and a crucial part of the machinery responsible for protein folding and homeostasis. Hsp70 is a three-domain, 70 kDa protein that cycles between an ATP-bound state in which all three domains are securely coupled into one unit and an ADP-bound state in which they are loosely attached via a flexible interdomain linker. The Hsp70 presents an alluring novel therapeutic target since it is crucial for maintaining cellular proteostasis and is particularly crucial to cancer cells. We have performed molecular dynamics simulations of the SBD (substrate binding domain) along with the Lid domain in response to experimental efforts to identify small molecule inhibitors that impair the functioning of Hsp70. Our intent has been to characterize the motion of the SBD/Lid allosteric machinery and in, addition, to identify the effect of the PET16 molecule on this motion. Interestingly, we noticed the opening of the entire Lid domain in the apo-form of the dimer. The configuration of the open structure was very different from previously published structures (PDB 4JN4) of the open and docked conformation of the ATP bound form. MD simulations revealed the Lid to be capable of far greater dynamical excursions than has been anticipated by experimental structural biology. This is of value in future drug discovery efforts targeted to modulating Hsp70 activity. The PET16 molecule appears to be weakly bound and its effect on the dynamics of the complex is yet to be elucidated.

Stress response and safety of lidocaine combined with dexmedetomidine in patients undergoing laparoscopic hysterectomy

Purpose: To investigate the anesthetic effect and safety issues when lidocaine is combined with dexmedetomidine in laparoscopic hysterectomy.&#x0D; Methods: The data for 100 patients from the Anesthesiology Department of Changzhou Second People's Hospital Affiliated to Nanjing Medical University who underwent laparoscopic total hysterectomy were randomly but equally divided into a control group and a combination group. Lidocaine hydrochloride was administered by infusion in the control group, while dexmedetomidine and lidocaine were administered together in the combination group. Inflammatory factors and stress hormone levels before and after the operation, as well as the incidence of adverse reactions following the operation, hemodynamic index, visual pain simulation (VAS) score, and sedation score at various times after the operation were evaluated in the two groups. Furthermore, the incidence of postoperative adverse reactions were also recorded and compared between the two groups.&#x0D; Results: The combination group's recovery time was significantly longer than that of the control group (p &lt; 0.05). At the point of extubation and 10 min after, mean arterial pressure (MAP) and heart rate (HR) in the combination group were significantly lower than those of the control group, respectively (p &lt; 0.05), while the combination group's VAS and Ramsay scores were statistically lower than those of the control group at 30 min, 24 h, and 48 h following surgery, respectively (p &lt; 0.05). The incidence of nausea and vomiting in the combination group was significantly lower than that in the control group (28.0% vs 58.0%, p &lt; 0.05).&#x0D; Conclusion: Lidocaine and dexmedetomidine, when combined, enhance hemodynamics, postoperative analgesia, and sedation in laparoscopic hysterectomy patients. The combination also lowers inflammatory stress and stress hormone levels, as well as the risk of nausea and vomiting, leading to better safety in the patients. However, multicenter trials are recommended to validate these findings prior to its use clinical practice.

Mechanical Characterization of Dissolving Microneedles: Factors Affecting Physical Strength of Needles.

Dissolving microneedles (MNs) are novel transdermal drug delivery systems that can be painlessly self-administered. This study investigated the effects of experimental conditions on the mechanical characterization of dissolving MNs for quality evaluation. Micromolding was used to fabricate polyvinyl alcohol (PVA)-based dissolving MN patches with eight different cone-shaped geometries. Axial force mechanical characterization test conditions, in terms of compression speed and the number of compression needles per test, significantly affected the needle fracture force of dissolving MNs. Characterization using selected test conditions clearly showed differences in the needle fracture force of dissolving MNs prepared under various conditions. PVA-based MNs were divided into two groups that showed buckling and unbuckling deformation, which occurred at aspect ratios (needle height/base diameter) of 2.8 and 1.8, respectively. The needle fracture force of PVA-based MNs was negatively correlated with an increase in the needle's aspect ratio. Higher residual water or higher loading of lidocaine hydrochloride significantly decreased the needle fracture force. Therefore, setting appropriate methods and parameters for characterizing the mechanical properties of dissolving MNs should contribute to the development and supply of appropriate products.

Mice Recognise Mice in Neighbouring Rearing Cages and Change Their Social Behaviour.

Mice are social animals that change their behaviour primarily in response to visual, olfactory, and auditory information from conspecifics. Rearing conditions such as cage size and colour are important factors influencing mouse behaviour. In recent years, transparent plastic cages have become standard breeding cages. The advantage of using a transparent cage is that the experimenter can observe the mouse from outside the cage without touching the cage. However, mice may recognise the environment outside the cage and change their behaviour. We speculated that mice housed in transparent cages might recognise mice in neighbouring cages. We used only male mice in this experiment. C57BL/6 mice were kept in transparent rearing cages with open lids, and the cage positions were maintained for 3 weeks. Subsequently, we examined how mice behaved toward cagemate mice, mice from neighbouring cages, and mice from distant cages. We compared the level of interest in mice using a social preference test. Similar to previous reports, subject mice showed a high degree of interest in unfamiliar mice from distant cages. By contrast, subject mice reacted to mice from neighbouring cages as familiar mice, similar to cagemate mice. This suggests that mice housed in transparent cages with open lids perceive the external environment and identify mice in neighbouring cages. Researchers should pay attention to the environment outside the mouse cage, especially for the social preference test.

Molecular interactions of hydrated co-amorphous systems of prilocaine and lidocaine

It is generally accepted that water as a plasticizer can decrease the glass transition temperatures (Tgs) of amorphous drugs and drug excipient systems. However, previous studies suggest that water, as an anti-plasticizer, can increase the Tgs of co-amorphous systems of prilocaine (PRL) and lidocaine (LID). In order to investigate the intermolecular interactions between water and co-amorphous PRL-LID systems, Fourier transform infrared spectroscopy (FTIR) and principal component analysis (PCA) were conducted. Water was found to bind with the carbonyl groups of PRL and LID molecularly evenly in the hydrated co-amorphous PRL-LID systems. Quantum chemical simulations visually confirmed the interactions between water and co-amorphous PRL-LID systems. Furthermore, the physical stability of hydrated co-amorphous PRL-LID systems was improved due to the anti-plasticizing effect of water, compared with the anhydrous samples. The preference of water to interact with the carbonyl groups of PRL and LID as binding sites could be associated with the anti-plasticizing effect of water on the co-amorphous PRL-LID systems.

Polymorphism of Bis(benzimidazole)bis(thiocyanato-N)cobalt(II) and Its Relevance to Studies of the Chief Color Test for Cocaine

Cobalt(II) thiocyanate-based tests are routinely used to screen cocaine products, with the formation of a blue species interpreted as a positive response. Two popular candidates for the origin of the blue color are an ionic coordination compound, frequently referred to as an ion pair, of the general form (HL)2[Co(SCN)4] or the coordination compound [CoL2(SCN)2], where L represents select nitrogenous bases. Given the high number of nitrogenous bases documented to yield false positives for cobalt(II) thiocyanate-based tests, a reasonable hypothesis is that both candidates are possible but their preferential formation depends on the specific nitrogenous bases screened. This hypothesis was tested through the crystallographic and spectroscopic analysis of reaction products of cocaine hydrochloride, lidocaine monohydrate hydrochloride, and benzimidazole exposed to a classic cobalt(II) thiocyanate reagent. Single-crystal X-ray diffraction revealed that the blue product isolated from benzimidazole test vessels is a coordination compound, with comparative ultraviolet–visible and Raman spectroscopy validating that blue precipitates collected from cocaine hydrochloride and lidocaine monohydrate hydrochloride reaction containers are ionic coordination compounds. Peaks corresponding to π-π* transitions in UV-vis at around 320 nm (cocaine hydrochloride: 320 nm, lidocaine hydrochloride: 323 nm) shift to a higher wavelength of 332 nm for the coordinated benzimidazole, and the broader d-d transitions at 550–630 nm show both a shift and change in envelope for benzimidazole coordinated with cobalt(II). The compound is a new polymorph of bis(benzimidazole)bis(thiocyanato-N)Cobalt(II), γ-[Co(Hbzim)2(SCN)2] (Hbzim = benzimidazole), and the differences in the intermolecular interactions to the two previous polymorphs were clarified by graph set analysis and Hirshfeld surface analysis. Furthermore, the coordination of aromatic nitrogen bases (such as benzimidazole) with Co(II) and aliphatic bases was compared by analyzing the Cambridge Structural Database, and the aromatic bases were found to have a shorter Co-N bond length compared to the aliphatic bases by around 0.02 Å.

Adhesive polydopamine-based photothermal hybrid hydrogel for on-demand lidocaine delivery, effective anti-bacteria, and prolonged local long-lasting analgesia

Considering the astonishing prevalence of localized pain affecting billions of patients worldwide, the development of advanced analgesic formulations or delivery systems to achieve clinical applicability is of great significance. In this study, an integrated PDA-based LiH@PDA@Ag@PAA@Gelatin system was designed for sustained delivery of lidocaine hydrochloride (LiH). By optimizing the preparation process and formulation of the hydrogel, the hydrogel exhibited superior mechanical properties, reversibility, adhesion strength, and self-healing attributes. Moreover, PDA@Ag nanoparticles were evenly dispersed within the hydrogel, and the optimized PDA@Ag@PAA@Gelatin showed a higher photothermal conversion efficiency than that of pure PDA. Importantly, LiH@PDA@Ag@PAA@Gelatin could effectively capture and eradicate bacteria through the synergistic interaction between near-infrared (NIR), PDA, Ag and LiH. In vitro and in vivo tests demonstrated that LiH@PDA@Ag@PAA@Gelatin exhibited higher drug delivery efficiency compared to commercial lidocaine patches. By evaluating the mechanical pain withdrawal threshold of the spared nerve injury (SNI) model in rats, it was proven that LiH@PDA@Ag@PAA@Gelatin enhanced and prolonged the analgesic effect of LiH. Furthermore, LiH@PDA@Ag@PAA@Gelatin induced by NIR possessed excellent on-demand photothermal analgesic ability. Therefore, this study develops a convenient method for preparing localized analgesic hydrogel patches, providing an important step towards advancing PDA-based on-demand pain relief applications.

Topical anesthetics for needle-related pain in adults and children (TOPIC): a mini-review.

Healthcare professionals (HCP) perform various needle procedures that can be distressing and painful for children and adults. Even though many strategies have been proven effective in reducing distress and pain, topical anesthetic use before needle procedures is uncommon. However, there are limited studies in the existing literature comparing specifically liposomal lidocaine and tetracaine hydrochloride topical creams. This systematic review analyzed studies on the use of two anesthetic creams, Liposomal Lidocaine (Maxilene®) and Tetracaine hydrochloride (Ametop™), in children and adults undergoing a needle-related procedure. Databases searched: PubMed, CINAHL, ClinicalTrials. Only randomized controlled trials (RCT) and Controlled Clinical Trials (CCT) studies were included. Cochrane Collaboration's Risk of Bias assessment tool was used. Strictly minimally invasive procedures were included to standardize different skin needle interventions. Only one study with 60 participants was available to be included in this review. No statistically significant difference was found in the mean pain score among both interventions. The outcomes of self-reported distress during cannulation and on HCP satisfaction were not reported. However, physiological characteristics associated with stress/anxiety and on cannulation success rate were reported and did not show statistical significance. Little to no evidence regarding the most efficient cream between liposomal lidocaine and tetracaine hydrochloride for pain management during needle-related procedures was found. Further studies, particularly RCT with larger sample sizes and standardized outcome measures, are needed to confirm the relative efficacy of either anesthetic cream.

Fabrication of lidocaine-loaded polymer dissolving microneedles for rapid and prolonged local anesthesia.

There is an urgent need for research into effective interventions for pain management to improve patients' life quality. Traditional needle and syringe injection were used to administer the local anesthesia. However, it causes various discomforts, ranging from brief stings to trypanophobia and denial of medical operations. In this study, a dissolving microneedles (MNs) system made of composite matrix materials of polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), and sodium hyaluronate (HA) was successfully developed for the loading of lidocaine hydrochloride (LidH). The morphology, size and mechanical properties of the MNs were also investigated. After the insertion of MNs into the skin, the matrix at the tip of the MNs was swelled and dissolved by absorption of interstitial fluid, leading to a rapid release of loaded LidH from MNs' tips. And the LidH in the back patching was diffused into deeper skin tissue through microchannels created by MNs insertion, forming a prolonged anesthesia effect. In addition, the back patching of MNs could be acted as a drug reservoir to form a prolonged local anesthesia effect. The results showed that LidH MNs provided a superior analgesia up to 8h, exhibiting a rapid and long-lasting analgesic effects. Additionally, tissue sectioning and in vitro cytotoxicity tests indicated that the MNs patch we developed had a favorable biosafety profile.

Inflammatory biomarker concentrations in dogs with gastric dilatation volvulus with and without 24-h intravenous lidocaine.

Canine gastric dilatation volvulus (GDV) is characterized by tissue ischemia, reperfusion, and systemic inflammation. Evidence exists that lidocaine exerts anti-inflammatory properties and potentially improves outcome. Prospective, randomized observational cohort study in client-owned dogs with GDV. The primary objective of the study was the determination of pro- and anti-inflammatory biomarker concentrations in dogs with GDV with and without intravenous (IV) lidocaine therapy. The second objective was the evaluation of side effects of lidocaine. Of 35 dogs included in the study, 20 dogs were assigned to receive lidocaine (LIDO) (2 mg/kg initially, followed by a continuous infusion at a rate of 50 μg/kg/min over 24 h) and 15 dogs not to receive lidocaine (NO-LIDO). Plasma concentrations of cytokines interleukin (IL)-6, IL-7, IL-8, IL-10, IL-15, IL-18, interferon gamma, keratinocyte chemotactic-like, monocyte chemotactic protein, and C-reactive protein (CRP) were measured at admission (prior any therapeutic intervention, T0), immediately after surgery (T1), at 24 h (T24), and at 48 h (T48) post-surgery. No significant differences in concentrations of any cytokines were found between the LIDO- and the NO-LIDO group. Significant lower CRP concentrations (median [range]) were found in dogs with lidocaine compared to dogs without at T24 (97.5 pg/mL [46.3-161.7] vs. 127.9 pg/mL [26.9-182.0]; p = 0.046) and T48 (73.7 pg/mL [18.4-169.4] vs. 116.3 pg/mL [71.4-176.8]; p = 0.002). Dogs receiving lidocaine exhibited significantly impaired mentation, a prolonged period of anorexia, and longer hospitalization compared to dogs without lidocaine. Lidocaine administration had no impact on the plasma levels of cytokines during the 48-h study period, but significantly lower CRP concentrations were found at T24 and T48. Lidocaine's potential side effects require careful decision making regarding its use.

Anti-plasticizing effect of water on prilocaine and lidocaine - the role of the hydrogen bonding pattern.

It is generally accepted that water, as an effective plasticizer, decreases the glass transition temperatures (Tgs) of amorphous drugs, potentially resulting in physical instabilities. However, recent studies suggest that water can also increase the Tgs of the amorphous forms of the drugs prilocaine (PRL) and lidocaine (LID), thus acting as an anti-plasticizer. To further understand the nature of the anti-plasticizing effect of water, interactions with different solvents and the resulting structural features of PRL and LID were investigated by Fourier transform infrared spectroscopy (FTIR) and quantum chemical simulations. Heavy water (deuterium oxides) was chosen as a solvent, as the deuterium and hydrogen atoms are electronically identical. It was found that substituting hydrogen with deuterium showed a minimal impact on the anti-plasticization of water on PRL. Ethanol and ethylene glycol were chosen as solvents to compare the hydrogen bonding patterns occurring between the hydroxyl groups of the solvents and PRL and LID. Comparison of the various Tgs showed a weaker anti-plasticizing potential of these two solvents on PRL and LID. The frequency shifts of the amide CO groups of PRL and LID due to the interactions with water, heavy water, ethanol, and ethylene glycol as observed in the FTIR spectra showed a correlation with the binding energies calculated by quantum chemical simulations. Overall, this study showed that the combination of weak hydrogen bonding and strong electrostatic contributions in hydrated PRL and LID could play an important role in inducing the anti-plasticizing effect of water on those drugs.

Evaluation of pharmacological alternatives to reduce the pain and discomfort produced by electroejaculation in rams

AbstractElectroejaculation (EE) represents the main technique for semen collection from domestic and wild animals independently of libido. However, the technique is associated with intense involuntary muscle contractions, vocalization, ataxia and lying down, caused by the electric stimulation of the nerves in the caudal epigastric region. These clinical manifestations represent important indicators of discomfort. In this context, the objective of this study was to evaluate two protocols of local anaesthetic blockade and two anatomical access for pharmacological desensitization of the caudal epigastric innervation as alternatives to promote comfort and reduce stress associated with EE in rams. For the study, four clinically healthy Dorper rams were selected. All animals were subjected to a design consisting of five semen collection treatments (n = 3 collections per treatment): T1—control, conventional EE without local anaesthetic blockade; T2, EE with ventral blockade (VB) of epigastric innervation using lidocaine hydrochloride 2%; T3, EE with VB of epigastric innervation using a combination of lidocaine hydrochloride 2% and fentanyl citrate; T4, EE with blockade of epigastric innervation through the perineal access using lidocaine hydrochloride 2%; T5, EE with blockade of epigastric innervation through the perineal access using a combination of lidocaine hydrochloride and fentanyl citrate. Seminal samples resulting from EE were subjectively evaluated for sperm motility and concentration, vigour and volume. Additionally, blood serum samples were collected for quantification of cortisol and creatine kinase (CK) enzyme. Assessments of stress and discomfort were conducted by measuring blood pressure, heart rate (HR) and respiratory rate (RR), as well as observing involuntary muscle contractions, ataxia and animal vocalization. No variations in blood pressure, sperm motility, vigour, CK, and cortisol were observed among the treatments. Individual variations were observed for the occurrence of vocalization (p = .0066), but there were no differences between the groups. Anaesthetic blockades conducted using the combination of lidocaine and fentanyl resulted in a lower incidence of ataxia during EE (p &lt; .0001). It is concluded that the combination of fentanyl citrate and lidocaine hydrochloride results in less discomfort for animals undergoing EE, regardless of the anatomical access used for local anaesthetic blockades.