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SUMMARY: The application effect of transversus abdominis plane block (TAPB) combined with thoracic paravertebral block (TPVB) or erector spinae plane block (ESP) under ultrasound guidance in endoscopic radical resection of esophageal cancer under general anesthesia was studied. From March 2021 to February 2022, patients who underwent endoscopic radical resection of esophageal cancer in our hospital were selected as the research object, and 90 patients were selected as the samples. Patients were divided into groupA and group B according to the difference of blocking schemes. Group A received ESP and Group B received TPVB. The dosage of sufentanil, nerve block time, awakening time and extubation time of the two groups were counted. The postoperative pain, sedation effect, sleep satisfaction and analgesia satisfaction of the two groups were compared, and the complications of the two groups were observed. The nerve block time and extubation time in group A were shorter than those in group B (P0.05). At T2, T3 and T4, the visual analogue scale (VAS) scores of group A at rest and cough were significantly lower than those of group B (P0.05). The satisfaction of sleep and analgesia in group A was higher than that in group B (P0.05). The analgesic effect of ultrasound-guided TAPB combined with ESP is better than that of ultrasound-guided TAPB combined with TPVB, and it can shorten the time of nerve block and extubation, which is worth popularizing.
Se estudió el efecto de la aplicación del bloqueo del plano transverso del abdomen (TAPB) combinado con el bloqueo paravertebral torácico (TPVB) o el bloqueo del plano del erector de la columna (ESP) bajo guía ecográfica en la resección radical endoscópica del cáncer de esófago bajo anestesia general. Desde marzo de 2021 hasta febrero de 2022, en nuestro hospital, se seleccionaron como objeto de investigación pacientes sometidos a resección radical endoscópica de cáncer de esófago, y como muestra se seleccionaron 90 pacientes. Los pacientes se dividieron en el grupo A y el grupo B según la diferencia de esquemas de bloqueo. El grupo A recibió ESP y el grupo B recibió TPVB. Se contaron la dosis de sufentanilo, el tiempo de bloqueo nervioso, el tiempo de despertar y el tiempo de extubación de los dos grupos. Se compararon el dolor posoperatorio, el efecto de la sedación, la satisfacción del sueño y la satisfacción de la analgesia de los dos grupos y se observaron las complicaciones de los dos grupos. El tiempo de bloqueo nervioso y el tiempo de extubación en el grupo A fueron más cortos que los del grupo B (P0,05). En T2, T3 y T4, las puntuaciones de la escala visual analógica (EVA) del grupo A en repo- so y tos fueron significativamente más bajas que las del grupo B (P 0,05). La satisfacción del sueño y la analgesia en el grupo A fue mayor que en el grupo B (P0,05). El efecto analgésico de la TAPB guiada por ecografía combinada con ESP es mejor que el de la TAPB guiada por ecografía combinada con TPVB, y puede acortar el tiempo de bloqueo nervioso y extubación, lo que vale la pena popularizar.
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Humans , Male , Female , Middle Aged , Thoracic Vertebrae/drug effects , Esophagectomy/methods , Abdominal Muscles/drug effects , Endoscopy/methods , Paraspinal Muscles/drug effects , Nerve Block/methods , Ultrasonography , Analgesics, Opioid/administration & dosageРеферат
Objective To investigate the effect of L4 transverse process erector spinae plane block(ESPB)before general anesthesia hip surgery in elderly patients on reducing perioperative pain and stress,thus reducing opioid consumption and improving postoperative recovery quality.Methods Sixty patients aged 65 years old and above who underwent unilateral hip surgery from January to December 2023 were randomly divided into two groups(n = 30)by using the random number table method.The ESPB group received ultrasound-guided ESPB at the L4 level with 0.3%ropivacaine(0.5 ml/kg)before induction of anesthesia,while the control group did not receive ESPB.Laryngeal mask anesthesia was administered in both groups.The induction and maintenance methods were consistent in both groups.The Numerical Rating Scale(NRS)was used to evaluate the degree of pain at 8 h and 24 h after surgery.The times of pressing analgesic pump within 24 h after surgery were recorded.The hemodynamic changes at each time point during the operation were observed.The time interval from the end of the operation to the complete recovery and to remove the laryngeal mask were recorded.Intraoperative and Postanesthesia Care Unit(PACU)opioid consumption were noted.The incidence of postoperative agitation,postoperative nausea and vomiting(PONV),dizziness,and the recovery quality score were compared.Results The NRS scores of rest pain and motion pain at 8 h and 24 h after surgery were significantly lower in the ESPB group than those in the control group,and the times of pressing the analgesic pump within 24 h after surgery in the ESPB group was significantly less than that in the control group(P<0.05).The mean arterial pressure(MAP)of the ESPB group at 20 min after peeling was lower than that of the control group[(87.2±15.5)mm Hg vs.(96.7±16.9)mm Hg,P = 0.026].The sufentanil consumption,remifentanil consumption,and the number of cases using urapidil in the ESPB group were significantly lower than those in the control group[12.5(10.0,14.0)μg vs.12.5(12.5,17.5)μg,P =0.041;270(100,400)μg vs.600(448,800)μg,P<0.001;1 case vs.11 cases,P =0.001].The Steward score at30 min after entering PACU was significantly higher in the ESPB group than in the control group[6(5,6)points vs.5(4,5)points,P<0.001].There was no statistical significance in incidence of postoperative agitation,PONV,and dizziness between the two groups(P>0.05).Conclusion Preoperative ESPB at the level of the L4 transverse process can reduce the pain score within 24 h after surgery,reduce the amount of opioid used during and after hip surgery,and improve the quality of postoperative recovery in the elderly.
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ObjectiveThe mechanisms underlying therapeutic efficacies of Detumescence Analgesic Plaster was analyzed based on "effect-target" associations. MethodBased on CNKI and PubMed databases， the chemical components of Artemisia seed， bastard speedwell， and menthol in Detumescence Analgesic Plaster were collected. The capacity of transdermal absorption was predicted based on the Encyclopedia of Traditional Chinese Medicine （ETCM 2.0）. Golden Triangle of compounds with Accepted used for candidate target prediction based on the Integrative Pharmacology-based Research Platform of Traditional Chinese Medicine （TCMIP v2.0）according to the similarity of chemical structures. At the same time， the SoFDA data platform was employed to collect the symptoms related to the efficacy of Detumescence Analgesic Plaster and its related genes information. In addition， based on the interaction between the above-mentioned candidate targets and their efficacy-related genes， the "effect-target" interaction network of Detumescence Analgesic Plaster was constructed. The key targets by topological features calculation， and functional mining was carried out to explain the efficacy mechanism of Detumescence Analgesic Plaster. ResultA total of 165 candidate targets were obtained based on ETCM 2.0 and TCMIP v2.0 databases， and symptoms related to the efficacy of clearing heat， detumescence， and relieving pain， as well as 1 744 related genes were collected based on the SoFDA database. Network construction and analysis showed that the core effect targets of Detumescence Analgesic Plaster were mainly involved in regulating the "immune-inflammation" balance of the body and maintaining the homeostasis of material and energy metabolism， blood circulation， and nervous system functions， and they were closely related to the efficacy of this prescription in clearing heat， reducing detumescence， and relieving pain. Among them， the heat clearing group of Detumescence Analgesic Plaster had the functions of heat clearing， detoxifying， antibacteria， and anti-inflammation. The biological function of its key effect target group was related to correcting the imbalance of "immune-inflammation" induced by pathogens. The detumescence group of Detumescence Analgesic Plaster had the functions of reducing water and swelling and resolving hard lumps， and the biological function of its core effect target group was related to improving microcirculation disturbance. The pain relieving group of Detumescence Analgesic Plaster had the functions of removing stasis， promoting blood circulation， and relieving pain， and its core effect target group was related to correcting the nervous system and the disorder of material and energy metabolism. ConclusionThe heat clearing， swelling reducing， and pain relieving effects of Detumescence Analgesic Plaster may be closely related to its act on related candidate targets， so as to correct the imbalance of "nerve-immunity-vascular-axis"， regulate neuronal excitability and inflammatory response， and intervene in material and energy metabolism. The relevant research results lay a theoretical foundation for clarifying the advantages of Detumescence Analgesic Plaster and assisting its clinical precise positioning.
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Analgesia is an important link in the treatment of severe patients after neurosurgery and plays a vital role in improving the prognosis of the patients.Understanding the status quo and influencing fac-tors of pain in severe patients after neurosurgery helps to predict the occurrence of pain,which is crucial for determining the new pain assessment methods and auxiliary analgesic methods and developing novel analgesic drugs.This paper reviews the pain status,pain evaluation and analgesic methods of severe patients after neuro-surgery in recent years so as to understand the pain management current status of the patients with severe neurological conditions and provide reference for the medical staff to implement the analgesic programs.
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Objective To investigate the effect of intravertebral labor analgesia nursing intervened by anesthesia nurse on labor analgesia and delivery outcome.Methods Two hundreds cases of parturients who received intravertebral labor analgesia in The First Affiliated Hospital of Kunming Medical University from July to December 2022 were selected as research objects and randomly divided into observation group and control group by drawing lots,with 100 cases in each group.The control group was given routine nursing by midwives,and the observation group was given anesthesia nursing by an anesthesia nurse.The degree of labor pain,the outcome of labor,the incidence of anesthesia-related complications,and the satisfaction of labor analgesia nursing were compared between the two groups.Results The degree of labor pain in the observation group was significantly lower than that in the control group(P<0.05).The duration of labor in the observation group was longer than that in the control group(P<0.05).The incidence of anesthesia-related complications in the observation group was significantly lower than that in the control group(P<0.05).The satisfaction of parturient analgesic care in the observation group was higher than that in the control group(P<0.05).Conclusion Labor analgesia care intervened by anesthesia nurses can effectively reduce labor pain,shorten the labor process,reduce the incidence of anesthesia-related complications,improve the satisfaction of labor analgesia nursing,and provide a safe,comfortable,and effective labor process for women,which is worthy of clinical promotion.
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BACKGROUND:With the further development of minimally invasive concepts,unicompartmental knee arthroplasty has become an important treatment for osteoarthritis of the knee;however,early postoperative pain adversely affects the recovery process,so effective analgesic measures are necessary.Femoral nerve block and cocktail therapy are common analgesic methods for unicompartmental knee arthroplasty,but there is a lack of studies confirming the analgesic effect and safety of their combined application. OBJECTIVE:To investigate the analgesic effect of cocktail therapy combined with femoral nerve block in unicompartmental knee arthroplasty. METHODS:One hundred patients who received unicompartmental knee arthroplasty from October 2021 to January 2023 were selected as the study subjects.They were divided into a control group(n=50)and a study group(n=50)using a random number table method.The femoral nerve block was used in the control group,while cocktail therapy combined with femoral nerve block was used in the study group during unicompartmental knee arthroplasty.Postoperative analgesia effect,analgesic frequency of dezocine injection within 2 days after surgery,motion range of affected knee joint,KSS function scores,and the occurrence of postoperative adverse reactions were compared between the two groups. RESULTS AND CONCLUSION:(1)Visual analog scale scores in the study group were lower than those in the control group at 12,24,and 48 hours after surgery(P<0.05).(2)The analgesic frequency of dezocine in the study group was less than that in the control group within 2 days after surgery(P<0.05).(3)The motion range in the study group was higher than that in the control group 1 and 3 days after surgery(P<0.05).On day 14 after surgery,there was no significant difference in motion range between the two groups(P>0.05).(4)The knee KSS score in the study group was higher than that in the control group at 2 weeks after surgery(P<0.05).There was no statistically significant difference in knee KSS scores between the two groups from 6 weeks to 6 months after surgery(P>0.05).(5)The difference in the occurrence of adverse reactions within 14 days after surgery was not significant between the two groups(P>0.05).(6)These results show that the use of cocktail therapy combined with femoral nerve block in unicompartmental knee arthroplasty can effectively reduce postoperative pain,improve the analgesic effect,reduce the frequency of analgesic drugs,and improve motion range of the early affected knee joint of patients.
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The complex chemical composition and limited research ideas of traditional Chinese medicine （TCM） have led to the unclear material basis and mechanism of the medicinal effects， which is a common problem hindering the modernization of TCM in China. The introduction of computer virtual technology has provided a new perspective for TCM research. In this study， we established the research method of structure-activity omics to study the relationships between the structures and effects of different compounds in TCM based on the chemical structures of TCM components and to analyze and predict the material basis and multitarget synergistic mechanism of TCM. Furthermore， a structure-activity omics study was carried out with the anti-inflammatory and analgesic effects of Qizhi Weitong granules as an example. This study provides support for screening the pharmacodynamic components and analyzing the active ingredients of TCM and gives insights into the research on the material basis and mechanism of compound efficacy and the development of lead compounds of TCM， thus promoting the modern research and the innovative development of TCM.
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ObjectiveTo explain the anti-inflammatory and analgesic effects of Corydalis Rhizoma by the means of structure-activity omics. MethodOn the basis of the previous in vitro screening study， we studied the in vivo efficacy of the alkaloids in Corydalis Rhizoma. With the targets as a bridge， the structures of chemical components in Corydalis Rhizoma were connected with the efficacy. The molecular docking of the alkaloids in Corydalis Rhizoma with the targets of inflammation and pain was carried out. According to the docking scores and the differences in the structural nucleus of Corydalis Rhizoma alkaloids， a study of structure-activity omics was carried out to summarize the rules of their connection. ResultThe alkaloids in Corydalis Rhizoma had good anti-inflammatory and analgesic effects in vivo， involving 53 chemical components and 73 targets. There were 3 074 targets associated with inflammation and pain， and 42 targets of direct action were shared by the chemical components and the disease. The protein-protein interaction （PPI） and molecular docking analysis predicted that the main active components of Corydalis Rhizoma were tetrahydropalmatine and palmatine， and the core targets were prostaglandin endoperoxide synthase 2 （PTGS2）， glutamate receptor metabotropic 5 （GRM5）， estrogen receptor 1 （ESR1）， solute carrier family 6 member 4 （SLC6A4）， and fusion oncoproteins （FOS）. According to the differences of mother nucleus， the 53 alkaloid components of Corydalis Rhizoma were classified into 8 categories， including protoberberine， berberine， and aporphine， which had high binding affinities with PTGS2， GRM5 and other targets. The relationship between the structures of Corydalis Rhizoma alkaloids and docking scores in each group showed the same law. In protoberberine， appropriate substituents with hydroxyl， alkoxy or methyl groups on the A and D rings of the parent ring were conducive to enhancing the binding activities with the two targets. In berberine， the structure containing a methyl group on position 13 had strong binding affinities with the two targets. It is hypothesized that the methyl fragment changes the binding mode between the component structure and amino acid residues， which greatly improves the binding affinity. ConclusionThis study employs the method of structure-activity omics to analyze the material basis for the anti-inflammatory and analgesic effects of alkaloids in Corydalis Rhizoma， and the structure-activity omics provides new ideas for revealing the pharmacodynamic substances of traditional Chinese medicine.
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ObjectiveTo identify the pharmacodynamic substances for the anti-inflammatory and analgesic effects of Bupleuri Radix by structure-activity omics. MethodA mouse model of pain was established with formaldehyde to examine the anti-inflammatory and analgesic effects of saikosaponins in vivo. The core targets of the active components in Bupleurum Radix for the anti-inflammatory and analgesic effects were screened from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform （TCMSP）， Online Mendelian Inheritance in Man （OMIM）， and Search Tool for Recurring Instances of Neighbouring Genes （STRING）. The key core targets with high binding affinity were screened based on the comprehensive score in the molecular docking between different types of saikosaponins and core targets. The structure-activity relationship was discussed and analyzed based on the binding of compounds to pharmacodynamic targets. ResultSaikosaponins alleviated the foot swelling induced by formaldehyde and reduced the content of prostaglandin E2 （PGE2） in the mouse model， showcasing a significant inhibitory effect on the inflammatory pain caused by PGE2. Nine components and 39 targets of saikosaponins， as well as 3 074 targets of anti-inflammatory and analgesic effects were screened out， and 22 common targets shared by saikosaponins and the effects were obtained as the direct targets. The protein-protein interaction （PPI） analysis showed that the main active components of Bupleurum Radix were saikosaponins a， b1， b2， b3， c， d， e， f， and v， and the key targets were fms-related receptor tyrosine kinase 1 （FLT1）， kinase insert domain receptor （KDR）， fibroblast growth factor 2 （FGF2）， vascular endothelial growth factor A （VEGFA）， and signal transducer and activator of transcription 3 （STAT3）. Molecular docking between saikosaponins and the top 5 targets with high degrees in PPI network analysis revealed 25 highly active docks， including 6 docks with scores of 5-6 and 18 docks with scores above 6. ConclusionThis study adopted structural-activity omics to analyze the material basis for the anti-inflammatory and analgesic effects of Bupleuri Radix in vivo， providing new ideas and methods for identifying the pharmacodynamic substances in traditional Chinese medicine.
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ObjectiveTo explain the pharmacodynamic substances of Aurantii Fructus flavonoids that exert anti-inflammatory and analgesic effects using a structure-activity omics approach. MethodOn the basis of the previous in vitro pharmacological screening conducted by the research team， an in vivo pharmacological study of Aurantii Fructus flavonoids was carried out. Core targets of the anti-inflammatory and analgesic active components of flavonoids of Aurantii Fructus were identified using various network databases， including the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform （TCMSP）， the Online Mendelian Inheritance in Man （OMIM）， and the Search Tool for the Retrieval of Interacting Genes/Proteins （STRING）. Computer-aided virtual screening technology was used to dock different types of Aurantii Fructus flavonoids with core targets. The key core targets with high binding activity were selected based on the comprehensive scores of each target and the active structures. Using these targets as bridges， the structures of one or more types of chemical components in Aurantii Fructus were closely linked to pharmacological effects. The structure-activity relationship between the clear pharmacodynamic compounds and their effects was explored through the binding patterns of various structures with pharmacodynamic targets. ResultAurantii Fructus flavonoids demonstrated significant anti-inflammatory and analgesic effects on dextran sulfate sodium （DSS）-induced colitis in mice， which could improve symptoms and significantly reduce the levels of inflammatory factors interleukin-6 （IL-6） and interleukin-1β （IL-1β）（P<0.05）. Twelve active components of Aurantii Fructus flavonoids were identified and categorized into nine dihydroflavonoids and three flavonoids based on their structures of the parent nuclei. Through Venn analysis， 167 anti-inflammatory and analgesic targets for Aurantii Fructus were identified. Based on degree value and molecular docking comprehensive scores， prostaglandin-endoperoxide synthase 2（PTGS2） and mitogen-activated protein kinase 3（MAPK3） were selected for further structural analysis. Structural analysis revealed that components containing glycoside structures exhibited higher binding activity with anti-inflammatory and analgesic targets. ConclusionThis study utilized a structure-activity omics approach based on in vivo pharmacodynamic experiments to analyze the material basis of the anti-inflammatory and analgesic effects of Aurantii Fructus flavonoids. The structure-activity omics approach provides new ideas and methods for elucidating the pharmacodynamic substances of Chinese medicine.
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Introducción: La anestesia libre de opioides surge de las alternativas farmacológicas que permiten otra opción anestésica en el arsenal del anestesiólogo. Objetivo: Evaluar la efectividad y seguridad de una técnica anestésica libre de opioides en el paciente intervenido con cirugía bariátrica laparoscópica. Métodos: Se realizó un estudio observacional analítico, prospectivo y longitudinal en 23 pacientes operados con anestesia general multimodal libre de opioides. Pacientes mayores de 18 años con un índice de masa corporal mayor o igual a 35 kg/m2, con estado físico ASA II y III. Se evaluó la analgesia posoperatoria e intraoperatoria como una necesidad de la analgesia de rescate en el tiempo de recuperación y los efectos adversos. Resultados: Se demostró que la edad promedio fue 38,19 ± 8,73 con un predominio en el sexo femenino, los pacientes fueron clasificados como ASA II y obesos grados III. Hubo una estabilidad hemodinámica intraoperatoria. El 82,6 % de los pacientes no presentaron dolor posoperatorio en las primeras 24 h. No se presentaron pacientes con dolor severo. Requirieron analgesia de rescate cinco pacientes (21,7 %) en posoperatorio, y las complicaciones fueron escasas sin repercusión clínica. El tiempo promedio para la extubación fue de 6,7 ± 0,8 min y la recuperación total de 29,6 ± 0,8 min. Conclusiones: La técnica multimodal libre de opioides resultó segura y efectiva, con un adecuado estado de analgesia perioperatoria y escasas complicaciones en los pacientes intervenido con cirugía bariátrica laparoscópica.
Introduction: Opioid-free anesthesia arises from pharmacological alternatives that allow another anesthetic option in the anesthesiologist's arsenal. Objective: To evaluate the effectiveness and safety of an opioid-free anesthetic technique in patients undergoing laparoscopic bariatric surgery. Methods: An analytical, prospective and longitudinal observational study was carried out in 23 patients operated on with opioid-free multimodal general anesthesia. The patients studied were over 18 years of age, with a body mass index greater than or equal to 35 kg/m2, ASA physical status II and III. Postoperative and intraoperative analgesia were evaluated as a need for rescue analgesia in recovery time and adverse effects. Results: It was shown that the average age was 38.19 ± 8.73 with a predominance in the female sex, the patients were classified as ASA II and grade III obese. There was intraoperative hemodynamic stability. 82.6% of patients did not experience postoperative pain in the first 24 hours. There were no patients with severe pain. Five patients (21.7%) required rescue analgesia postoperatively, and complications were rare without clinical repercussions. The average time for extubation was 6.7 ± 0.8 min and total recovery was 29.6 ± 0.8 min. Conclusions: The opioid-free multimodal technique was safe and effective, with adequate state of perioperative analgesia and few complications in patients undergoing laparoscopic bariatric surgery.
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Kelussia odoratissima fruits are utilized in Persian traditional medicine as a painkiller and to prevent inflammation-based disorders. Considering the higher content of essential oil in the fruits, the oil's anti-inflammatory and analgesic activities were investigated via the paw edema triggered in mice and the writhing test and hot plate technique, respectively. It was observed that the 100, and 200 mg/Kg doses of the oil revealed an analgesic impact (p<0.001) considering the increment in the reaction time needed for the hot plate approach. Furthermore, 100 and 200 mg/Kg doses of the oil caused a reduction in the frequency of writhes in the mice (p<0.01 and p<0.001, respectively). Using all examined doses of theoil (25, 50, and 100 mg/Kg) caused inflammatory reduction (p<0.001). The findings indicated that the oil possess significant activities against acute inflammation. It had both peripheral and central pain-killing impacts. The main components 3-n-butylphthalide (28.3%) and germacrene D (17.3%) can be considered as the responsible compounds to manage the inflammation and pain.
Las frutas de Kelussia odoratissima se utilizan en la medicina tradicional persa como analgésico y para prevenir los trastornos basados en la inflamación. Teniendo en cuenta el mayor contenido de aceite esencial en las frutas, se investigaron las actividades antiinflamatorias y analgésicas del aceite a través del edema de la pata desencadenado en ratones y la prueba de contorsiones y la técnica del plato caliente, respectivamente. Se observó que las dosis de 100 y 200 mg / kg del aceite revelaron un impacto analgésico (p<0,001) considerando el incremento en el tiempo de reacción necesario para el enfoque de placa caliente. Además, dosis de 100 y 200 mg / kg del aceite provocaron una reducción en la frecuencia de retorcimientos en los ratones (p<0,01 y p<0,001, respectivamente). El uso de todas las dosis examinadas del aceite (25, 50 y 100 mg/kg) provocó una reducción inflamatoria (p<0,001). Los hallazgos indicaron que el aceite posee actividades significativas contra la inflamación aguda. Tiene impactos analgésicos tanto periféricos como centrales. Los principales componentes 3-n-butilftalida (28,3%) y germacreno D (17,3%) pueden considerarse como los compuestos responsables del manejo de la inflamación y el dolor.
Тема - темы
Animals , Male , Rats , Oils, Volatile/administration & dosage , Plant Extracts/administration & dosage , Apiaceae/chemistry , Analgesics/administration & dosage , Anti-Inflammatory Agents/administration & dosage , Benzofurans/cerebrospinal fluid , Oils, Volatile/chemistry , Rats, Wistar , Sesquiterpenes, Germacrane/analysis , Fruit , Gas Chromatography-Mass SpectrometryРеферат
Opioids are the most effective painkillers, but their benefit-risk balance often hinder their therapeutic use. WLB-73502 is a dual, bispecific compound that binds sigma-1 (S1R) and mu-opioid (MOR) receptors. WLB-73502 is an antagonist at the S1R. It behaved as a partial MOR agonist at the G-protein pathway and produced no/unsignificant β-arrestin-2 recruitment, thus demonstrating low intrinsic efficacy on MOR at both signalling pathways. Despite its partial MOR agonism, WLB-73502 exerted full antinociceptive efficacy, with potency superior to morphine and similar to oxycodone against nociceptive, inflammatory and osteoarthritis pain, and superior to both morphine and oxycodone against neuropathic pain. WLB-73502 crosses the blood-brain barrier and binds brain S1R and MOR to an extent consistent with its antinociceptive effect. Contrary to morphine and oxycodone, tolerance to its antinociceptive effect did not develop after repeated 4-week administration. Also, contrary to opioid comparators, WLB-73502 did not inhibit gastrointestinal transit or respiratory function in rats at doses inducing full efficacy, and it was devoid of proemetic effect (retching and vomiting) in ferrets at potentially effective doses. WLB-73502 benefits from its bivalent S1R antagonist and partial MOR agonist nature to provide an improved antinociceptive and safety profile respect to strong opioid therapy.
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A chemical investigation on the aqueous extract of Corydalis yanhusuo tubers led to the isolation and structural elucidation of three pairs of trace enantiomeric hetero-dimeric alkaloids, (+)/(-)-yanhusamides A-C ( 1- 3), featuring an unprecedented 3,8-diazatricylco[5.2.2.02,6]undecane-8,10-diene bridged system. Their structures were exhaustively characterized by X-ray diffraction, comprehensive spectroscopic data analysis, and computational methods. Guided by the hypothetical biosynthetic pathway for 1- 3, a gram-scale biomimetic synthesis of (±)- 1 was achieved in 3 steps using photoenolization/Diels-Alder (PEDA) [4+2] cycloaddition. Compounds 1‒3 exhibited potent inhibition of NO production induced by LPS in RAW264.7 macrophages. The in vivo assay showed that oral administration of 30 mg/kg of (±)- 1 attenuated the severity of rat adjuvant-induced arthritis (AIA). Additionally, (±)- 1 induced a dose-dependent antinociceptive effect in the acetic acid-induced mice writhing assay.
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OBJECTIVE To explore the efficacy and safety of intra-articular injection of ropivacaine combined with alfentanil for postoperative analgesia in patients who underwent knee arthroscopic surgery. METHODS A total of 60 patients who underwent knee arthroscopic surgery were collected from the Central Hospital of Enshi Tujia and Miao Autonomous Prefecture from March to September in 2022， and then divided into trial group and control group with random number table method， with 30 cases in each group. The control group received intra-articular injection of 0.25% ropivacaine 50 mg， and the trial group received intra-articular injection of 0.25% ropivacaine 50 mg+alfentanil 0.15 μg/kg.The first postoperative remedial analgesia time， the total amount of postoperative remedial drugs， numerical rating scale at rest （NRS-R） scores， numerical rating scale at movement （NRS-M） scores， heart rate， mean arterial blood pressure， and pulse oxygen saturation during exercise at different monitoring time points after surgery， the incidence of adverse drug reactions such as hypotension， respiratory depression， nausea， and vomiting after surgery were compared between 2 groups. RESULTS Compared with the control group， the first postoperative remedial analgesia time was significantly longer in the trial group， and the total amount of postoperative remedial drugs was significantly reduced （P＜0.001）. The trial group had lower NRS-R and NRS-M scores at each monitoring time point， with statistically significant differences （P＜0.001）， and there was an interactive effect between time and groups （P＜0.001）. The changes in heart rate， mean arterial blood pressure， and pulse oxygen saturation of patients in the trial group were relatively small， with no statistically significant differences （P＞0.05）， and there was no interactive effect between time and groups （P＞0.05）. There was no statistical significance in the incidence of adverse drug reactions between 2 groups， such as postoperative hypotension， respiratory depression， nausea， vomiting （P＞0.05）. CONCLUSIONS The intra- articular injection of ropivacaine combined with alfentanil shows good efficacy and safety for post-knee arthroscopic analgesia， and significantly prolongs the analgesic duration of ropivacaine.
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Establish a production line with controllable process and high intelligence, contribute to improve the quality and production efficiency of aconite processed by microwave, and promote the transformation and application of aconite processed by microwave. According to the principle of aconite detoxification and the characteristics of industrial microwave equipment, an industrial production line of aconite processed by microwave was established with diester alkaloids and monoester alkaloids as indicators, and pilot production was carried out. At the same time, the content of active constituents and efficacy were compared with that of the main processed products, such as Shengfupian, Baifupian and Heishunpian. The results showed that the industrial production of aconite processed by microwave can be divided into two stages: "Liquid seal to detoxification - drying and puffing". The content of monoester alkaloids in 10 batches of aconite processed by microwave was 0.071%-0.166% and the content of diester alkaloids was 0.004%-0.016%, which met the relevant requirements of the Chinese Pharmacopoeia in 2020. Compared with Heishunpian and Baifupian, the retention rate of the effective components of aconite processed by microwave was higher. Pharmacological experiments showed that aconite processed by microwave not only retained the anti-inflammatory and analgesic activities of Heishunpian and Baifupian, but also significantly increased the levels of leukocytes and lymphocytes in mice with liver cancer chemotherapy, enhanced the CD4/CD8 ratio in spleen cells of mice (P < 0.05), thus regulating the body's immunity. However, this effect of Baifupian was weak, while Heishunpian and Shengfupian had no such effect. Through the above research, this study established microwave processing line with controllable process and high intelligence, as well produced the aconite processed by microwave with low toxicity and stable quality. It laid a foundation for the industrialized continuous production and clinical positioning of aconite by microwave processed, and provided scientific support for the development and application of microwave technology in the field of traditional Chinese medicine. All animal experiments in this study were reviewed and approved by the Experimental Animal Ethics Committee of Chengdu University of Traditional Chinese Medicine before being carried out (Approval No. 2020-28).
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OBJECTIVE@#To observe the immediate analgesic effect of electroacupuncture (EA) combined with diclofenac sodium on acute gouty arthritis (AGA).@*METHODS@#A total of 90 patients with AGA were randomly divided into a low-dose medication (LM) group (30 cases, 1 case was eliminated, 1 case dropped off), a conventional medication (CM) group (30 cases, 1 case dropped off) and a combination of acupuncture and medication (AM) group (30 cases ). The LM group was given oral administration of 50 mg diclofenac sodium sustained-release capsule; the CM group was given oral administration of 100 mg diclofenac sodium sustained-release capsule; on the basis of the treatment of LM group, the AM group was treated with electroacupuncture at ashi points, Dadu (SP 2), Taichong (LR 3), Taibai (SP 3), Neiting (ST 44), Sanyinjiao (SP 6), Zusanli (ST 36) and Yinlingquan (SP 9) on the affected side, and Taichong (LR 3) and Zusanli (ST 36), Sanyinjiao (SP 6) and Yinlingquan (SP 9) were connected to electroacupuncture respectively, continuous wave, 2 Hz in frequency. The visual analogue scale (VAS) scores of pain before treatment and after 10 min, 2 h, 4 h and 6 h of treatment completion, joint tenderness and swelling scores before treatment and after 10 min and 6 h of treatment completion were compared, and the rate of diclofenac sodium addition within 24 h after treatment completion was recorded among the three groups.@*RESULTS@#After 10 min of treatment completion, the scores of VAS, joint tenderness and joint swelling in the AM group were lower than those before treatment (P<0.05), and the VAS score in the AM group was lower than that in the other two groups (P<0.05). After 2, 4 and 6 h of treatment completion, the VAS scores of the three groups were lower than those before treatment (P<0.05), and the scores in the AM group were lower than those in the LM group (P<0.05). After 6 h of treatment completion, the joint tenderness scores of the three groups and the joint swelling scores of the AM group and the CM group were lower than those before treatment (P<0.05), and the joint tenderness and swelling scores of the AM group were lower than those of the LM group (P<0.05). The rate of diclofenac sodium addition was 3.3 % (1/30) and 3.4 % (1/29) in the AM group and the CM group, respectively, which were lower than 17.9% (5/28) in the LM group (P<0.05).@*CONCLUSION@#Electroacupuncture combined with diclofenac sodium have a good immediate analgesic effect in the treatment of AGA, and have the advantages of small dosage of analgesic drugs and less adverse reactions.
Тема - темы
Humans , Diclofenac , Electroacupuncture , Arthritis, Gouty/drug therapy , Delayed-Action Preparations , Acupuncture Therapy , ArthralgiaРеферат
Objective To exploxe the analgesic effect of general anesthesia combined with different concentrations of ropivacaine and transverse abdominis plane block on laparoscopic appendectomy(LA).Methods LA patients from Xiamen University Affiliated Zhongshan Hospital from January 2022 to July 2023 were included.All patients underwent general anesthesia combined ropivacaine plane block of the transverse abdominis muscle.According to the different concentrations of ropivacaine,patients were divided into high concentration group(0.50％,20 mL),medium concentration group(0.375％,20 mL)and low concentration group(0.25％,20 mL).The dosage of fentanyl,postoperative bleeding,time of first press of the analgesic pump,and number of presses among three groups of patients were recorded and compared.The postoperative vital signs(mean arterial pressure and heart rate),pain level(NRS),comfort level(BCS)(1 h,6 h,12 h,and 24 h),and incidence of postoperative adverse reactions were observed and compared.Results This study included a total of 90 LA patients,with 30 cases in each group.The first press of the analgesic pump in the low concentration group was significantly shorter than that in the medium and high concentration groups(P＜0.05),while the number of presses was significantly higher than the other two groups(P＜0.05).The mean arterial pressure and heart rate significantly decreased with the increase of ropivacaine concentration at 1 hour after surgery(P＜0.05);compared with 1 hour after surgery,the average arterial pressure and heart rate of patients in the medium concentration group and low concentration group significantly increased at 6 hours after surgery(P＜0.05),and no significant changes occurred thereafter.The NRS scores of patients in the high concentration group were significantly lower than those in the medium and low concentration groups at all four postoperative time points(P＜0.05);the NRS scores of patients in the medium concentration group were significantly lower than those in the low concentration group at four postoperative time points(P＜0.05).The BCS scores of the low concentration higher than those of the medium concentration group and low concentration group an 1 h,6 h and 24 h.The incidence of adverse reactions in the high concentration group was significantly higher than that in the low concentration group and the medium concentration group(P＜0.05);there was no significant difference in the incidence of adverse reactions between the medium concentration group and the low concentration group(P＞0.05).Conclusion General anesthesia combined with 0.50％ropivacaine abdominal transverse muscle plane block has a significant analgesic effect and high comfort for patients undergoing LA,but the risk of postoperative adverse reactions is high,and the plan needs to be adjusted according to the actual situation.
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Objective To investigate the influencing factors of opioid analgesics need within 48 hours after arthroscopic rotator cuff repair.Methods Clinical data of 90 consecutive arthroscopic rotator cuff repairs by the same operator from March 2017 to July 2022 were retrospectively analyzed.The patients were divided into opioid group(62 patients)and control group(28 patients)according to whether they used opioid analgesics within 48 hours after surgery.The control group consisted of patients who did not use analgesics or who had good analgesic effects with conventional analgesic regimens(non-steroidal anti-inflammatory drugs or non-opioid central analgesics)after surgery,and the opioid group consisted of patients who required opioid analgesics as assessed by the surgeon or who need opioid analgesics because of inefficacy of conventional analgesic regimens.The following factors were selected as independent variables:gender,age(whether≥65 years old),duration of disease(whether≥4 weeks),body mass index(BMI)(whether≥25),occupation(whether employed),with or without a history of smoking and alcohol consumption,hypertension,diabetes,heart disease,and trauma,duration of surgery(whether≤180 min),number of torn tendons(whether≥2),number of screws(whether≥2),large nodular osteophyte,and whether there was moderate-to-severe impingement.Single factor analysis was used to screen the factors influencing the need for opioid analgesics within 48 hours after arthroscopic rotator cuff repair.Results The results of univariate analysis showed that among the above independent variables,only the number of torn tendons≥2 was the factor affecting the need for opioid analgesics within 48 hours after arthroscopic rotator cuff repair(OR = 5.263,P = 0.007).Conclusions Patients with rotator cuff tears with≥2 tendons had more severe pain within 48 hours after rotator cuff repair,requiring opioid analgesics.Focus should be placed on postoperative pain in such patients,and a diverse analgesic regimen should be used early.
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Tetrodotoxin (TTX) is a neurotoxin found in puffer fish and other marine organisms. It has been used as an inhibitor of voltage-gated sodium channels (VGSCs), which could selectively bind to the α-subunit on the outer vestibule of VGSCs, preventing sodium ions from entering the channel, resulting in pharmacological activities. As a typical sodium channel blocker, TTX shows a significant analgesic effect. TTX could selectively block Na+ channels without affecting other ion channels, therefore it could reduce the probability of adverse reactions caused by commonly used antiarrhythmic drugs. In addition, TTX has a significant role in detoxification and prevention of renal failure, so TTX has great potential as a medicine. The structure and physicochemical properties, mechanism of action, pharmacological activities and preparations of tetrodotoxin have been reviewed in this paper, so as to provide a general support for the evaluation of its druggability and application in the field of pharmacy.