Local Anesthetic Activity Research Articles

A Comparative Study of Ropivacaine with and without Fentanyl for Caudal Anesthesia in Pediatric Patients

Background: One of the most prevalent regional methods in paediatric anaesthesia is the caudal epidural block. It is a safe, simple procedure that has proven to be quite beneficial in children following infra-umbilical surgery. Ropivacaine causes differential neuraxial blockade, which is associated with less motor block and lower cardiovascular damage. To extend the duration of action of local anaesthetics, several adjuvants are administered. Our goal was to see how fentanyl affected the duration of postoperative analgesia when used in conjunction with ropivacaine in a paediatric population of children aged 3 to 8 years following infraumbilical operations.
 Methods: On 100 paediatric patients receiving elective infraumbilical operations, a prospective, comparative, and randomised investigation was done. Patients were randomised into two 50-person groups at random. Caudal anaesthesia was administered once the airway was secured. 0.2 percent ropivacaine 0.5ml/kg was given to Group R, while 0.2 percent ropivacaine 0.5ml/kg with fentanyl 0.5mcg/kg was given to Group RF. Face, legs, activity, cry, and consolability pain rating scales were used to measure postoperative pain for 24 hours. The length of the motor blockage and any negative effects were recorded. Hemodynamics, post-operative analgesia duration, and the number of rescue analgesics required were all recorded and statistically evaluated.
 Results: The mean duration of analgesia in ropivacaine group was 440.60±101.29 minutes (7.25hrs) and in ropivacaine fentanyl group was 891±312.84 (14.76hrs). Statistically, the difference was highly significant.
 Conclusion: In children having infraumbilical surgery, using fentanyl as an adjuvant to ropivacaine for caudal block enhanced analgesic effectiveness and extended post-operative analgesia.

Comparison of Normal Saline and Alkalinized 2% Lignocaine to Reduce Emergence Phenomenon and Post-Intubation Morbidities: A Prospective, Double-Blind, Randomized Study.

Endotracheal intubation for airway management in general anesthesia is associated with post-intubation morbidities due to tracheal mucosa injury caused by endotracheal tube (ETT) cuff. Nitrous oxide (N2O) diffuses into tracheal tube cuffs filled with air. The rate of diffusion of N2O through the membrane is proportional to its concentration gradient. High-volume low-pressure cuffs expand with only a slight increase in pressure until fully inflated. At this point, owing to the inelasticity of the material, the cuff pressure rises rapidly. This increased pressure can damage the tracheal mucosa. This phenomenon can be avoided, if we inflate the cuff with either a liquid or a gas mixture identical to the inspired gas and monitor the cuff pressure and volume at regular intervals. When lignocaine is used to inflate the ETT cuff, it diffuses to the underlying tracheal mucosa. Thus reducing local irritation and inflammation of the airway through its local anesthetic action. Alkalinization of lignocaine increases its rate of diffusion across the ETT cuff. It also reduces the dose of local anesthetic required to achieve the desired result. We sought to determine the benefits of filling the ETT cuff with alkalinized lignocaine 2% over normal saline, to prevent ETT-induced emergence phenomenon and reduce the incidence of post-intubation morbidities like sore throat, hoarseness, and nausea. This prospective, randomized, double-blind, and comparative study was done at a multispecialty hospital. A total of 120 individuals ofAmerican Society of Anesthesiologists (ASA) physical status 1 and 2, posted for surgery under general anesthesia, were randomly selected and divided into two groups: alkalinized 2% lignocaine group (group L) and normal saline group (group S). After induction of general anesthesia, the airway was secured with appropriate-sized ETT. The ETT cuff was inflated with either of the study media. Continuous cuff pressure monitoring was done to keep cuff pressure below 30 centimeters of water (cm of H2O), at all times. At extubation, the response was evaluated in terms of percentage change in heart rate (HR) and blood pressure from baseline, coughing, bucking, and restlessness. All the surgeries lasted more than two hours. Post-operatively, the patients were evaluated for sore throat and hoarseness, at regular intervals of up to 24 hours. ETT cuff pressure was initially less in group S, which rose to a significantly higher level at extubation, compared to group L (p <0.001). At extubation, there was a significant increase in HR and systolic blood pressure (SBP) from baseline, in group S than in group L (p <0.001 and p=0.001, respectively).The incidence of cough and restlessness was less in group L, compared to group S (p<0.001 and p=0.002, respectively). Mean extubation time and emergence time was more in group S than in group L (p<0.001). Post-operatively, the incidence and severity of sore throat were significantly higher in group S than in group L (p<0.001). Meanwhile, the incidence of hoarseness and nausea was comparable in the two groups. Continuous ETT cuff pressure monitoring helps to keep cuff pressure below tracheal mucosa capillary occlusion pressure. Filling the ETT cuff with alkalinized lignocaine further reduces extubation response and post-intubation morbidities.

Evaluation of the Local Anesthetic Activity, Acute Toxicity, and Structure-Toxicity Relationship in Series of Synthesized 1-Aryltetrahydroisoquinoline Alkaloid Derivatives In Vivo and In Silico.

Isoquinoline alkaloids constitute one of the most common classes of alkaloids that have shown a pronounced role in curing various diseases. Finding ways to reduce the toxicity of these molecules and to increase their therapeutic margin is an urgent matter. Here, a one-step method for the synthesis of a series of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines was performed in 85-98% yield by the Pictet-Spengler reaction. This was accomplished using the reaction between 3,4-dimethoxyphenylethylamine and substituted benzaldehydes boiling in trifluoroacetic acid. Furthermore, 1-(3'-amino-, 4'-aminophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines were obtained in 94% and 97% yield by reduction in 1-(3'-nitro-, 4'-nitrophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines with SnCl2 × 2H2O. The structures of the substances obtained were confirmed by infrared (IR) and nuclear magnetic resonance (1H and 13C NMR) spectra. ADMET/TOPKAT in silico study concluded that the synthesized compounds exhibited acceptable pharmacodynamic and pharmacokinetic properties without carcinogenic or mutagenic potential but with variable hepatotoxicity. The acute toxicity and structure-toxicity relationship (STR) in the series of 20 derivatives of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines (3a-r, 4a, b) was studied via determination of acute toxicity and resorptive action in white mice employing intragastric step-by-step administration. The first compound, 1-phenyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (3a), showed the highest toxicity with LD50 of 280 mg/kg in contrast to 1-(3'-bromo -4'-hydroxyphenyl)-6,7-methylenedioxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (3e) which proved to be the safest of the compounds studied. Its toxicity was 13.75 times lower than that of the parent compound 3a. All compounds investigated showed high local anesthetic activity on rabbit eyes in the concentrations studied. Only 3r, 3n, and 4a caused eye irritation and redness. All investigated derivatives (except 4b) in 1% concentration were more active than lidocaine, providing longer duration of complete anesthesia. Therefore, based on the obtained results of in silico tests, local anesthesia, and acute toxicity, a conclusion can be drawn that the experimental compounds need further extensive future investigations and possible modifications so that they can act as promising drug candidates.

The dose-response relationships of the direct scavenging activity of amide-based local anesthetics against multiple free radicals.

This study aimed to illustrate the dose-response relationships of the direct scavenging activity of amide-based local anesthetics against multiple free radicals in vitro. We have demonstrated that amide-type local anesthetics selectively and directly scavenge some free radicals. Three kinds of free radicals were eliminated by all the four local anesthetics examined. Mepivacaine, lidocaine, bupivacaine, and dibucaine scavenged hydroxyl radicals in dose-dependent manners. Ascorbyl free radicals were also scavenged in dose-dependent manners, and lastly singlet oxygen was scavenged in dose-dependent manners. Three other free radicals were not scavenged by all of the four local anesthetics; tert-butoxyl radical was scavenged by all the anesthetics examined but dibucaine, nitric oxide by mepivacaine but not by the other three, and tyrosyl radical by mepivacaine and lidocaine but not by the other two. Some free radicals (superoxide anion, tert-butyl peroxyl radical, DPPH) were not scavenged by any of the four local anesthetics. The local anesthetics were also shown to inhibit lipid peroxidation by TBARS assay. These results suggest that local anesthetics have antioxidant properties through their free radical scavenging activities.

Battling Hypotension in Cesarean Section

Perhaps the greatest day in a mother's life is the birth of her child. As a father of two, I will never forget those two drastically different, yet equally beautiful moments. In each circumstance, the obstetricians, nurses, anesthesia providers, and technicians all worked seamlessly to provide a safe and enjoyable childbirth experience for our new and growing family. One key element of the childbirth experience is maternal pain control. Depending on several factors, the parturient may receive an epidural, a spinal, a combined spinal/epidural, IV analgesics or perhaps nothing at all. One key commonality after any anesthetic administration is its propensity to cause hypotension, which is usually most profound after spinal anesthesia (SA). SA is the preferred method during elective cesarean sections due to the rapid and predictable onset and duration of action of local anesthetics injected directly into the cerebrospinal fluid. Immediately after SA is administered, the patient is helped to lay supine which assists the hyperbaric local anesthetic to move with gravity and rise cephalad from the lower lumber injection site (L3-L5) towards the desired T4 vertebra. While marching up those 12 dermatome levels, the local anesthetic quickly begins to attenuate sympathetic tone at every level along the way. Depending on the health of the patient's cardiovascular system, intravascular volume status and other factors, the sympathectomy and subsequent vasodilation can result in significant and symptomatic hypotension, causing a vast array of symptoms such as maternal nausea, vomiting, dizziness, and cardiovascular collapse as well as fetal acidosis and decreased Apgar scores. Preanesthesia fluid boluses are commonly administered in hopes to increase intravascular volume and lessen the severity of hypotension, but its effectiveness is unreliable. Acute arterial vasodilation is the primary cause of hypotension after SA. Intravenous vasoactive medications such as phenylephrine and ephedrine offer the fastest and most effective means of arterial vasoconstriction and subsequent correction of blood pressure; yet healthcare providers will always continue to search for alternative and less invasive methods of preventing and/or treating hypotension after SA.

Inflammatory diseases of the external ear: place and possibilities of topical therapy

Otitis externa (NO) is manifested by inflammatory changes in the auricle, external auditory canal and epidermal layer of the eardrum. The disease is characterized by a wide prevalence and a continuing increase in morbidity, a persistent, resistant to adequate therapy course and frequent recurrence of the pathological process. For the development of NO, the presence of an etiotropic agent and a violation of the integrity of the epidermal layer of the skin of an endogenous and exogenous nature are necessary. According to the area of distribution and the type of pathological process, limited and diffuse NO are considered. Most often, bacteria act as the causative agents of NO, with diffuse forms Pseudomonas aeruginosa is the leader. The appointment of systemic antibiotics for uncomplicated forms of NO is impractical, it is optimal to use topical combined drugs that have adequate activity against the main pathogens of NO. The advantages of topical therapy in such patients are the rapid accumulation of required active substance concentration in the area of inflammation and almost complete lack of systemic action, minimal risk of development and spread of resistant strains of microorganisms. It is required to use antimicrobial agents that have been shown to be active against the main pathogens of otitis externa. The reduction of inflammation and pain is also an important component of the management of patients with OE. A good option for topical therapy of patients with inflammatory changes in the external ear is a drug with antimicrobial and local anesthetic action containing antibacterial components: aminoglycoside neomycin sulfate and cyclic polypeptide polymyxin B sulfate, and local anesthetic lidocaine hydrochloride. Such agents have a balanced antimicrobial and local anesthetic action, high safety and can be recommended for use in patients with diffuse otitis externa.

Correction to: Comparative local anaesthetic activity of lignocaine, lignocaine-adrenaline and water extracts of Annona muricata during castration in dogs

Correction to: Comparative local anaesthetic activity of lignocaine, lignocaine-adrenaline and water extracts of Annona muricata during castration in dogs

Local anesthetic, anti-inflammatory and analgesic activities of nanoparticles green-formulated by plant extract

• The results revealed a spherical morphology in the range size of 10–50 nm for AuNPs. • The IC50 of AuNPs and BHT against DPPH were 18 and 12 µg/mL, respectively. • It seems the recent nanoparticle may be use as a novel therapeutic drug in future. In the current research, we decided to formulate gold nanoparticles in aqueous medium using plant leaf aqueous extract as a new therapeutic drug for determining the local anesthetic, anti-inflammatory and analgesic activities in the in vivo condition. The common chemical tests i.e., UV–Visible Spectroscopy (UV–Vis), Transmission Electron Microscopy (TEM), and Fourier Transformed Infrared Spectroscopy (FT‐IR) were used for characterizing of nanoparticles. To survey the cytotoxicity properties of nanoparticles, MTT assay was used on the human normal cell lines. Analgesic activity was tested in mice using various doses orally. Acetic acid-induced writhing episodes were significantly and dose-dependently reduced. The local anesthetic activity were tested in frog and guinea pig models, and it was seen that in both animals, the nanoparticle produces significant local anesthetic activity. At the same dose, its anti-inflammatory activity was also tested. Carrageenin-induced paw edema in mice was significantly reduced after oral administration. It seems the recent nanoparticle may be use as a novel therapeutic drug with local anesthetic, anti-inflammatory and analgesic activities in future.

Local anesthetics and immunotherapy: a novel combination to fight cancer.

Intratumoral injection of oncolytic agents such as modified herpes simplex virus T-VEC or local administration of non-viral oncolytic therapies (such as radiofrequency, chemoembolization, cryoablation, or radiotherapy) can activate an anticancer immune response and hence trigger abscopal effects reducing secondary lesions. Preliminary data suggested that oncolytic treatments modulate tumor-infiltrating immune effectors and can be advantageously combined with the immune checkpoint inhibitors. Recent findings indicate that local anesthetics, which are usually used in the clinics to control surgical pain, also possess antineoplastic effects mimicking oncolytic treatments if they are injected into malignant lesions. Moreover, the association of local anesthetics with systemic immune checkpoint inhibition significantly improved overall survival in several preclinical tumor models. This may be explained by direct cytotoxic activity of local anesthetics and additional immune-related abscopal effects. We also summarize the molecular and cellular mechanisms by which the combination of local anesthetics and immunotherapy improves tumor control by the immune system.

Utilization of propranolol hydrochloride mucoadhesive invasomes as a locally acting contraceptive: in-vitro, ex-vivo, and in-vivo evaluation

It was found that propranolol hydrochloride (PNL), which is a beta-blocker used for hypertension treatment, has a potent spermicidal activity through local anesthetic activity or beta-blocking effect on sperm cells subsequently it could be used as a contraceptive remedy. This study aimed to entrap PNL into invasomes (INVs) and then formulate it as a locally acting contraceptive gel. PNL-loaded mucoadhesive INVs were prepared via the thin-film hydration technique. The D-optimal design was utilized to fabricate INVs employing lipid concentration (X1), terpenes concentration (X2), terpenes type (X3), and chitosan concentration (X4) as independent variables, while their impact was observed for entrapment efficiency percent (Y1; EE%), particle size (Y2; PS), zeta potential (Y3; ZP), and amount of drug released after 6 h (Y4; Q6h). Design Expert® was bestowed to nominate the desired formula. The selected INV was subjected to further studies and formulated into a mucoadhesive gel for ex-vivo and in-vivo investigations. The optimum INV showed a spherical shape with EE% of 65.01 ± 1.24%, PS of 243.75 ± 8.13 nm, PDI of 0.203 ± 0.01, ZP of 49.80 ± 0.42 mV, and Q6h of 53.16 ± 0.73%. Differential scanning calorimetry study asserted the capability of INVs to entrap PNL. Permeation studies confirmed the desired sustained effect of PNL-loaded INVs-gel compared to PNL-gel, INVs, and PNL solution. Sperm motility assay proved the potency of INVs-gel to inhibit sperm motility. Besides, the histopathological investigation verified the tolerability of the prepared INVs-gel. Taken together, the gained data justified the efficacy of PNL-loaded INVs-gel as a potential locally acting contraceptive.

Comparative local anaesthetic activity of lignocaine, lignocaine-adrenaline and water extracts of Annona muricata during castration in dogs

Comparative local anaesthetic activity of lignocaine, lignocaine-adrenaline and water extracts of Annona muricata during castration in dogs

Effect of Local Anesthetics on Dipole Potential of Different Phase Membranes: A Fluorescence Study.

The molecular mechanism behind the action of local anesthetics is not well understood. Phenylethanol (PEtOH) is an ingredient of essential oils with a rose-like odor, and it has previously been used as a local anesthetic. In this work, we explored the effect of PEtOH on dipole potential in membranes representing biologically relevant phases, employing the dual-wavelength ratiometric method utilizing the potential-sensitive probe di-8-ANEPPS. Our results show that PEtOH reduces membrane dipole potential in membranes of all biologically relevant phases (gel, liquid-ordered, and fluid) in a concentration-dependent manner. To the best of our knowledge, these results constitute one of the early reports describing reduction of membrane dipole potential induced by local anesthetics, irrespective of membrane phase.

COMPARATIVE STUDY OF INTRATHECAL HYPERBARIC BUPIVACAINE 0.5% VERSUS MIDAZOLAM PLUS HYPERBARIC BUPIVACAINE 0.5% MIXTURE FOR INFRAUMBILICAL SURGERIES.

Background: Sub arachnoid block is a commonly used anesthesia technique for all infra umbilical surgeries &amp; there is search for agents and techniques which would prolong local anesthetic action without its deleterious effects. The present study was designed to compare effect of 0.5% of hyperbaric bupivacaine intrathecal versus 0.4ml of intrathecal midazolam with 0.5% of hyperbaric bupivacaine for infra umbilical surgeries. Material And Methods: Present study was single-center, a double-blind trial, conducted in patients of age group 18-60 years with ASA grade I/II posted for elective infraumbilical surgery. 60 patients were divided into Group I received 3ml of 0.5% Bupivacaine heavy and 0.4 ml of 0.9% saline &amp; Group II received 3ml of 0.5% Bupivacaine heavy and 0.4 ml of midazolam (2mg). The meanResults: duration of maximum sensory blockade, maximum motor blockade was more in group II as compared to group I &amp; difference was statistically signicant (p&lt;0.05). Mean duration of surgery was less in group II as compared to group I &amp; difference was statistically signicant (p&lt;0.05). Duration of Motor blockade, duration of sensory blockade, time for two segment regression, time of rescue analgesia was more in group II as compared to group I &amp; difference was statistically signicant (p&lt;0.05). Patients complained of pain faster in Group I than in Group II, VAS score. Midazolam still nds a place in regularConclusion: clinical use as an intrathecal adjuvant with hyperbaric bupivacaine due to its hemodynamic stability and better post-operative analgesia with no signicant adverse effects.

ACE Question

Article| May 2022 ACE Question ASA Monitor May 2022, Vol. 86, 16. https://doi.org/10.1097/01.ASM.0000830808.15004.67 Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Peer Review Share Icon Share Facebook Twitter LinkedIn MailTo Cite Icon Cite Get Permissions Search Site Citation ACE Question. ASA Monitor 2022; 86:16 doi: https://doi.org/10.1097/01.ASM.0000830808.15004.67 Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search Dropdown Menu toolbar search search input Search input auto suggest filter your search All ContentAll PublicationsASA Monitor Search Advanced Search Topics: anesthesiology continuing education (ace) Due to national drug shortages, your facility is unable to obtain bupivacaine. You are planning a peripheral nerve block, and the only preservative-free local anesthetic available is 1.5% mepivacaine. What would be the MOST likely result of using mepivacaine in comparison to bupivacaine? Mepivacaine is an intermediate-potency amide local anesthetic that can be used for peripheral nerve blockade. It is commonly available in a 1.5% concentration. When compared to longer-duration agents such as bupivacaine, the following differences are commonly noted: The addition of epinephrine (1:200,000) will prolong the action of local anesthetics administered for a peripheral nerve block. The extent of this prolongation is greater with intermediate-acting agents such as mepivacaine than with longer-acting agents such as bupivacaine. Anesthesiology Continuing Education (ACE) is a self-study CME program that covers established medical knowledge in the field of anesthesiology. ACE can help fulfill the CME requirements of MOCA®. To learn... You do not currently have access to this content.

Clinical results of the using leucocyte interferon for the therapy of viral pathology of the oral mucous in somatic patients with combined dentistry pathology

Aim. To conduct a clinical test of the unguent form of human leukocyte interferon in somatic patients with relapsing of herpetic stomatitis.Material and methods. 98 somatic patients with viral pathology of the oral mucous at the age of 20 to 60 years and older were studied to identify the clinical efficiency of the leukocyte interferon. The order of the clinical studies was specified by a special program: preparations were decrypted, decryption was conducted after the analysis of the results of the clinical study. Preparation 1 – placebo (2% emulsion of lidocaine on vinilin), preparation 2 – interferon’s unguent, preparation 3 – 0.5% oxoline unguent. After active implementation of the complex treatment of patients with mucologic pathology were divided into 3 groups: 1st group included 31 patients who got a course of the treatment by preparation 1; 2nd - 34 persons, 2 have taken preparation; 3rd - 33 patients, 3 used preparation.Results. The most expressed clinical effect in the treatment of relapsing of herpetic stomatitis in somatic patients with combined dentistry pathology was shown by preparation 2, which had local anesthetic and anti-inflammation action. Indicators of the recovery of patients who got this preparation in contrast with patients of the third group decreased on average by 2 days, the 1st groups - by more than 1 day.Conclusion. Using oxolin’s unguent and preparation 1 in course of the treatment of herpetic stomatitis did not prevent the development of secondary elements in the oral mucous (24.0% and 44.0% accordingly) in most of the patients. Using preparation 2, new elements on oral mucous were observed only in 6.0% of cases, which shows it good antiviral effect.

Enhanced Antitumor Activity of Lidocaine Nanoparticles Encapsulated by a Self-Assembling Peptide.

Although local anesthetics (LAs) such as lidocaine have been traditionally used for pain relief, their antitumor activity has attracted more and more attentions in recent years. However, since nearly all LAs used in clinic are in their hydrochloride forms with small molecular weight and high water-solubility, their fast absorption and clearance greatly limit their antitumor activity in vivo. To better exploit the antitumor activity of LAs, lidocaine nanoparticles (LNPs) are prepared by using a self-assembling peptide to encapsulate the hydrophobic base form of lidocaine. In cultured A375 human melanoma cells, the LNPs show much higher cellular uptake level than the clinic formulation of lidocaine hydrochloride, which leads to enhanced efficacy in inhibiting the proliferation, migration and invasion of the cells, as well as in inducing cell apoptosis. Compared with lidocaine hydrochloride, LNPs can also significantly slow down the release rate of lidocaine. In nude mice, LNPs can effectively inhibit the development of solid tumors from seeded A375 cells and prevent the recurrence of tumors after surgical excision. These results indicate that by using self-assembling peptide to fabricate nanoparticle formulations of local anesthetics, their antitumor activity can be significantly enhanced, suggesting a potential postoperative treatment to prevent tumor recurrence after surgical excision.

Cocaine: An Updated Overview on Chemistry, Detection, Biokinetics, and Pharmacotoxicological Aspects including Abuse Pattern.

Cocaine is one of the most consumed stimulants throughout the world, as official sources report. It is a naturally occurring sympathomimetic tropane alkaloid derived from the leaves of Erythroxylon coca, which has been used by South American locals for millennia. Cocaine can usually be found in two forms, cocaine hydrochloride, a white powder, or ‘crack’ cocaine, the free base. While the first is commonly administered by insufflation (‘snorting’) or intravenously, the second is adapted for inhalation (smoking). Cocaine can exert local anaesthetic action by inhibiting voltage-gated sodium channels, thus halting electrical impulse propagation; cocaine also impacts neurotransmission by hindering monoamine reuptake, particularly dopamine, from the synaptic cleft. The excess of available dopamine for postsynaptic activation mediates the pleasurable effects reported by users and contributes to the addictive potential and toxic effects of the drug. Cocaine is metabolised (mostly hepatically) into two main metabolites, ecgonine methyl ester and benzoylecgonine. Other metabolites include, for example, norcocaine and cocaethylene, both displaying pharmacological action, and the last one constituting a biomarker for co-consumption of cocaine with alcohol. This review provides a brief overview of cocaine’s prevalence and patterns of use, its physical-chemical properties and methods for analysis, pharmacokinetics, pharmacodynamics, and multi-level toxicity.

PHARMACOLOGICAL ACTIVITY OF NEW COMPOSITION WITH A DIMETHYLACETAMIDE DERIVATIVE IN INFRAORBITAL ANESTHESIA IN RATS WITH PERIODONTITIS

The safety and local anesthetic activity of the pharmaceutical composition LHT-15-13 containing a dimethylacetamide derivative, an antioxidant and a vasoconstrictor in rats with chronic periodontitis was studied in the work. White laboratory mice were used to determine acute toxicity with intravenous and subcutaneous administration of a 2% aqueous solution of LHT-15-32. In rats with experimental periodontitis, the threshold of pain sensitivity of the second upper molar was determined. The activity of oxidative stress and total antioxidant activity was determined in the mucous membrane of the gums of rats by the method of induced chemiluminescence. Local changes in periodontal tissues were assessed by quantitative enzyme immunoassay. The acute toxicity of the pharmaceutical composition when administered intravenously and subcutaneously was lower than that of the dimethylacetamide derivative with succinic acid LHT-600. LHT-15-13, when administered infraorbitally, caused deep anesthesia that lasted more than 70 minutes, activated the local antioxidant defense system and reduced the level of IL-1β in the gum tissue, caused tissue repair around the impacted upper molar in rats five days after injection. Thus, the pharmaceutical composition can be considered as an effective and safe agent for pain relief of the upper molars in periodontitis.

Experimental study of the pharmacological activity of new azaheterocycles derivatives: A literature review

Diseases associated with the pathology of the cardiovascular system are one of the key causes of death all over the world. In particular, arrhythmia may entail the most severe complications, including unexpected death. With high-tech advances, antiarrhythmic drugs remain an integral part of both therapy and prevention. However, the existing arsenal of drugs often does not provide the necessary clinical effect, and therapy is associated with a high risk of severe adverse events. Another significant problem today is the administration of low-toxic drugs that provide effective anesthesia with a sufficient depth and duration of action. Currently, there is also the problem of the limited effectiveness of many drugs with antitumor, antimicrobial, antiviral, antifungal, anti-inflammatory activity and action on the central nervous system. One of the solutions to address the existing problems in these areas is the search and study of compounds that may serve as a basis for the development of new drugs. Given the membrane-stabilizing action by influencing ion channels, new derivatives of azaheterocycles- compounds of piperidine and piperazine are of particular interest in these areas of medicine. According to domestic studies, new piperidine derivatives during screening and in-depth studies showed pronounced local anesthetic activity during infiltration and conduction anesthesia. The results of a number of studies confirm the presence of antiarrhythmic activity in piperidine derivatives. Experimental data on the synthesis and study of the pharmacological activity of new derivatives of piperidine and piperazine in world practice prove their promise for the creation of drugs in various fields of medicine in the future.

Is lumbar erector spinae plane block (L-ESPB) a lumbar plexus block?: a case report of three cases

BackgroundLumbar erector spinae plane block (L-ESPB) is being used in fractured hip patients for the postoperative pain relief and as a sole anesthetic technique. Various clinical and cadaveric studies have differences of opinion about its mechanism of action and pathways of local anesthetic spread; however, the role of lumbar plexus (LP) in the mechanism of action is still not considered. In our clinical experience, we observed that the action on LP could be a pathway for the analgesic action of local anesthetic along with paravertebral spread.Case presentationWe report here three cases of the fractured hip who were given L-ESPB for postoperative pain management. The radiological examination was done after injection of non-ionic contrast to know the spread of local anesthetic. In two cases, the contrast spread was seen towards LP and in one case spread of contrast was observed towards the paravertebral area.ConclusionsEffect of local anesthetic on the lumbar plexus is one of the plausible pathways in L-ESPB for its analgesic mechanism of action.