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1.
Am Surg ; 86(9): 1153-1158, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32812770

RESUMO

BACKGROUND: Pain control is an important aspect of rib fracture management. With a rise in multimodal care approaches, we hypothesized that transdermal lidocaine patches reduce opioid utilization in hospitalized patients with acute rib fractures not requiring continuous opioid infusion. METHODS: We performed a retrospective analysis of adult trauma patients with acute rib fractures admitted to the Trauma Service from January 2011 to October 2018. We compared patients who received transdermal lidocaine patches to those who did not and evaluated cumulative opioid consumption, expressed in morphine milligram equivalents (MMEs). Secondary outcomes included the rate of pulmonary complications and length of hospital stay. RESULTS: Of the 21 190 trauma admissions, 3927 (18.5%) had rib fractures. Overall, 1555 patients who received continuous opioid infusion were excluded. Of the remaining 2372 patients, 725 (30.6%) patients received lidocaine patches. The mean total MME of patients who received lidocaine patches was 55.7 MME (30.7 MME on multivariate analysis) and was lower than that of patients who did not receive lidocaine patches (P ≤ .01). There was no difference in hospital length of stay (no lidocaine patches vs received lidocaine patches: 6.2 days vs 6.5 days, P = .34) or pulmonary complications (1.7% vs 2.8%, P = .08). DISCUSSION: In admitted trauma patients with acute rib fractures not requiring continuous intravenous opiates, lidocaine patch use was associated with a significant decrease in opiate utilization during the patients' hospital course.


Assuntos
Analgésicos Opioides/farmacologia , Lidocaína/farmacologia , Transtornos Relacionados ao Uso de Opioides/prevenção & controle , Manejo da Dor/métodos , Fraturas das Costelas/terapia , Anestésicos Locais/farmacologia , Feminino , Humanos , Incidência , Masculino , Transtornos Relacionados ao Uso de Opioides/epidemiologia , Estudos Retrospectivos , Estados Unidos/epidemiologia
3.
Br J Anaesth ; 125(5): 712-721, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-32616309

RESUMO

BACKGROUND: Experimental and, retrospective, clinical data indicate that anaesthetic technique might influence the risk of metastasis after cancer surgery. Neutrophil extracellular trapping (NETosis) is an immunological mechanism strongly linked with increased metastatic risk. Similarly, vascular endothelial growth factor A is linked to angiogenesis implicated in recurrence. Therefore, we investigated the effect of four anaesthetic techniques on NETosis and angiogenic factors expression in women undergoing breast cancer resection. METHODS: Women (n=120) undergoing primary breast tumour resection were randomly assigned to receive one of four anaesthetics: sevoflurane (S), sevoflurane plus i.v. lidocaine (SL), propofol (P), and propofol plus i.v. lidocaine (PL). Venous blood was collected before induction and 20-28 h after operation. Neutrophil myeloperoxidase and citrullinated histone H3, biomarkers of NETosis, and biomarkers of angiogenesis were measured by enzyme-linked immunosorbent assay. RESULTS: Patient characteristic data and perioperative management did not differ between study groups. The anaesthetic technique including lidocaine decreased expression of citrullinated histone H3 compared with no lidocaine (109 [23] vs 125 [22] ng ml-1, P=0.01 for SL and S and 98 [14] vs 130 [32] mg ml-1, P=0.007, for PL and P, respectively). Similarly, myeloperoxidase was decreased by lidocaine (8.5 [3.4] vs 10.8 [1.8] ng ml-1, P=0.03 for SL and S and 8.6 [3.1] vs 11.6 [2.5] ng ml-1, P=0.01 for PL and P, respectively). Lidocaine also decreased expression of matrix metalloproteinase 3 (MMP3) but not MMP9, whichever anaesthetic was used. Vascular endothelial growth factor A concentrations were not significantly influenced by the anaesthetic technique. CONCLUSIONS: I.V. perioperative lidocaine decreased postoperative expression of NETosis and MMP3, regardless of general anaesthetic technique. This supports the hypothesis that i.v. lidocaine during cancer surgery of curative intent might reduce recurrence. CLINICAL TRIAL REGISTRATION: NCT02839668.


Assuntos
Anestésicos Locais/farmacologia , Neoplasias da Mama/cirurgia , Armadilhas Extracelulares , Lidocaína/farmacologia , Neovascularização Patológica/sangue , Adulto , Idoso , Idoso de 80 Anos ou mais , Anestesia por Inalação , Anestesia Intravenosa , Biomarcadores/sangue , Feminino , Histonas/sangue , Humanos , Metaloproteinase 3 da Matriz/sangue , Pessoa de Meia-Idade , Recidiva Local de Neoplasia/prevenção & controle , Peroxidase/sangue , Estudos Prospectivos
4.
Br J Anaesth ; 125(4): 560-579, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32703549

RESUMO

BACKGROUND: Continuous epidural infusion (CEI) is commonly used for labour analgesia, but concerns over potential motor block, second-stage labour complications, and ineffective analgesia in late labour have prompted examining intermittent epidural bolus (IEB) as an alternative. However, evidence comparing these modalities is conflicting. The meta-analysis evaluates the analgesic efficacy of CEI vs IEB. METHODS: Databases were searched for trials comparing CEI to IEB for labour analgesia. The two co-primary outcomes were risk of breakthrough pain and difference in area under the curve (AUC) for pain scores during the first 4 h post-epidural initiation. Local anaesthetic consumption, maternal outcomes (i.e. delivery mode, labour duration, and maternal satisfaction), and side-effects of epidural analgesia were also evaluated. Results were pooled using random-effects modelling. Trial sequential analysis (TSA) was used to evaluate evidence reliability. RESULTS: Twenty-seven studies (3133 patients) were analysed. Compared with CEI, IEB decreased risk of breakthrough pain by 38% (risk ratio [95% confidence interval {CI}] of 0.62 [0.48, 0.81]; P=0.0004; I2=47%; 1164 patients) and reduced AUC of pain during the 4 h interval by 32.9% (mean difference [95% CI] of -16.7 mm h-1 [-18.9, -14.4]; P<0.0001; 1638 patients). Intermittent epidural bolus enhanced maternal satisfaction, shortened labour duration, decreased motor block, and reduced local anaesthetic consumption. The difference between the two groups was not statistically significant for epidural side-effects or mode of delivery. The TSA indicated adequate power for reliable inferences. CONCLUSIONS: Intermittent epidural bolus provides improved labour pain control during the first 4 h after epidural initiation with less breakthrough pain. Moderate- to high-quality evidence of intermittent epidural bolus superiority support its use as a safe and effective continuous epidural infusion alternative for labour analgesia.


Assuntos
Analgesia Epidural/métodos , Analgesia Obstétrica/métodos , Anestésicos Locais/administração & dosagem , Anestésicos Locais/efeitos adversos , Anestésicos Locais/farmacologia , Feminino , Humanos , Trabalho de Parto , Satisfação do Paciente , Gravidez
5.
J Neurosci ; 40(27): 5314-5326, 2020 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-32527981

RESUMO

An epileptic seizure can trigger a headache during (ictal) or after (postictal) the termination of the event. Little is known about the pathophysiology of seizure-induced headaches. In the current study, we determined whether a seizure can activate nociceptive pathways that carry pain signals from the meninges to the spinal cord, and if so, to what extent and through which classes of peripheral and central neurons. To achieve these goals, we used single-unit recording techniques and an established animal model of seizure (picrotoxin) to determine the effects of epileptic seizure on the activity of trigeminovascular Aδ-, C-, wide-dynamic range, and high-threshold neurons in male and female rats. Occurrence of seizure activated 54%, 50%, 68%, and 39% of the Aδ-, C-, wide-dynamic range, and high-threshold neurons, respectively. Regardless of their class, activated neurons exhibited a twofold to fourfold increase in their firing, which started immediately (1 min) or up to 90 min after seizure initiation, and lasted as short as 10 min or as long as 120 min. Administration of lidocaine to the dura prevented activation of all neuronal classes but not the initiation or maintenance of the seizure. These findings suggest that all neuronal classes may be involved in the initiation and maintenance of seizure-induced headache, and that their activation patterns can provide a neural substrate for explaining the timing and duration of ictal and possibly postictal headaches. By using seizure, which is evident in humans, this study bypasses controversies associated with cortical spreading depression, which is less readily observed in humans.SIGNIFICANCE STATEMENT This preclinical study provides a neural substrate for ictal and postictal headache. By studying seizure effects on the activity of peripheral (C and Aδ) and central (wide dynamic range and high-threshold) trigeminovascular neurons in intact and anesthetized dura, the findings help resolve two outstanding questions about the pathophysiology of headaches of intracranial origin. The first is that abnormal brain activity (i.e., seizure) that is evident in human (unlike cortical spreading depression) gives rise to specific and selective activation of the different components of the trigeminovascular system, and the second is that the activation of all components of the trigeminovascular pathway (i.e., peripheral and central neurons) depends on activation of the meningeal nociceptors from their receptors in the dura.


Assuntos
Cefaleia/etiologia , Cefaleia/fisiopatologia , Neurônios , Convulsões/complicações , Convulsões/fisiopatologia , Nervo Trigêmeo/fisiopatologia , Anestésicos Locais/farmacologia , Animais , Sistema Nervoso Central/fisiopatologia , Eletroencefalografia , Feminino , Lidocaína/farmacologia , Masculino , Meninges/fisiopatologia , Fibras Nervosas Mielinizadas , Fibras Nervosas Amielínicas , Vias Neurais/fisiopatologia , Nociceptores , Sistema Nervoso Periférico/fisiopatologia , Ratos , Ratos Sprague-Dawley , Medula Espinal/fisiopatologia
6.
Br J Anaesth ; 125(2): 175-183, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32593455

RESUMO

BACKGROUND: Liposomal bupivacaine (Exparel®) is a sustained-release formulation of bupivacaine for use in surgical infiltration anaesthesia. We analysed the histological nerve toxicity and clinical effectiveness of perineural Exparel® alone or with added dexamethasone in a mouse model. METHODS: We assigned 98 mice receiving a perineural sciatic nerve injection into seven groups: sham (n=14, perineural saline), B (n=14, perineural bupivacaine), BDIP (n=14, perineural bupivacaine + intraperitoneal dexamethasone), BDPN (n=14, perineural bupivacaine + perineural dexamethasone), E (n=14, perineural Exparel®), EDIP (n=14, perineural Exparel® + intraperitoneal dexamethasone), and EDPN (n=14, perineural Exparel® + perineural dexamethasone). The duration of thermoalgesic and motor block was evaluated in 49 mice (seven mice randomly selected by group) every 30 min until recovery. Mice were killed for sciatic nerve histological assessment at 14 or 28 days. RESULTS: The median duration of motor block was 90, 120, 120, 120, 180, and 180 min and the duration of thermoalgesic block was 240, 300, 360, 360, 360, and 420 min for groups B, BDIP, BDPN, E, EDIP, and EDPN, respectively. The B group mice showed mild neural inflammation at 14 days and the E group mice showed mild neural inflammation at 28 days. Addition (intraperitoneal or perineural) of dexamethasone reduced neural inflammation induced by bupivacaine, whereas only perineural dexamethasone reduced neural inflammation induced by Exparel®. CONCLUSIONS: Perineural or systemic dexamethasone had a protective effect against the neural inflammation induced by bupivacaine, and perineural dexamethasone attenuated delayed inflammation induced by perineural Exparel®.


Assuntos
Anestésicos Locais/farmacologia , Anti-Inflamatórios/farmacologia , Bupivacaína/farmacologia , Dexametasona/farmacologia , Inflamação/prevenção & controle , Animais , Modelos Animais de Doenças , Interações Medicamentosas , Inflamação/induzido quimicamente , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Tempo
7.
Jpn J Clin Oncol ; 50(8): 867-872, 2020 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-32409838

RESUMO

OBJECTIVE: To observe the antibacterial effect of adding cefazolin into anesthetics in patients with terminal cancer undergoing long-term epidural analgesia. METHODS: Patients undergoing epidural analgesia with terminal cancer were randomly divided into two groups: the conventional drug group (group C) and the cefazolin group (group G). Both groups were given levobupivacaine and morphine, while cefazolin was added to group G. The mean arterial pressure (MAP), heart rate (HR), respiratory rates (R), visual analogue scale (VAS) scores, satisfaction and complications of patients in the two groups were observed. 3 ml of the used analgesic was taken for bacterial culture when replacing the new analgesic case. RESULTS: HR, MAP, R, VAS scores, dosages of morphine, satisfaction of the analgesic and the complications were not significantly different between the two groups (P > 0.05). The overall satisfaction of patients in group G was significantly higher than that in group C (P < 0.05). One patient's anesthetics in group C were infected with colibacillus. Four patients in group C got infected in their epidural puncture sites. There was no infection in group G (P < 0.05). CONCLUSION: Adding cefazolin to local anesthetics could effectively prevent bacterial infection and ensured the safety of epidural analgesia for patients with terminal cancer.


Assuntos
Analgesia Epidural , Anestésicos Locais/farmacologia , Cefazolina/farmacologia , Infecções/etiologia , Neoplasias/complicações , Analgésicos Opioides/administração & dosagem , Anestésicos Locais/administração & dosagem , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Morfina/uso terapêutico , Satisfação do Paciente , Resultado do Tratamento , Escala Visual Analógica
8.
Arch Gynecol Obstet ; 301(5): 1153-1158, 2020 05.
Artigo em Inglês | MEDLINE | ID: mdl-32219521

RESUMO

PURPOSE: The purpose of this study was to study the impact of epidural analgesia using low-concentration local anesthetic during the entire labor on maternal and neonatal outcomes. METHODS: The authors enrolled 2310 parturient mothers who underwent vaginal delivery at their hospital since January 1, 2019. The parturients were allocated either into the analgesia or into the non-analgesia groups based on whether they received analgesia during the delivery process. To investigate the effects of epidural analgesia using low-concentration local anesthetic on maternal and neonatal outcomes, the authors assessed between-group differences in the labor duration, newborn Apgar score, and maternal and neonatal outcomes. RESULTS: Compared to the non-analgesia group, the first and second labor stage durations in the analgesia group were significantly longer. Similarly, the analgesia group had a higher frequency of oxytocin injections, Category II and III fetal heart rate tracing during labor, and intrapartum fever development. Further, the need for episiotomy and assisted vaginal delivery was higher in the analgesia group than that in the non-analgesia group. Regarding neonatal outcomes, the neonatal hospitalization rate and incidence rate of umbilical cord blood pH < 7.2 were higher in the analgesia group than those in the non-analgesia group. However, there were no significant between-group differences in the incidence rates of stained amniotic fluid, mild neonatal asphyxia, and severe perinatal asphyxia. CONCLUSION: Patient-controlled epidural analgesia using low-concentration local anesthetic during the entire labor did not increase the incidence rate of severe adverse outcomes in neonates born through vaginal delivery; however, it increased the delivery duration, and thus, the chance of possible perinatal interventions.


Assuntos
Analgesia Epidural/efeitos adversos , Analgesia Obstétrica/efeitos adversos , Anestésicos Locais/uso terapêutico , Adulto , Analgesia Epidural/métodos , Analgesia Obstétrica/métodos , Anestésicos Locais/farmacologia , Feminino , Humanos , Recém-Nascido , Masculino , Gravidez , Estudos Prospectivos , Resultado do Tratamento
9.
Niger J Clin Pract ; 23(2): 172-178, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32031091

RESUMO

Background: One of the drawbacks of subarachnoid block is the short duration of analgesia particularly when adjuvants are not added to local anesthetics agent used. However, dexmedetomidine an α2-adrenergic agent has been found to possess analgesic effect. Aims: This study seeks to determine the analgesic efficacy of intrathecal 7.5 µg of dexmedetomidine and its side effects when used for open reduction and internal fixation (ORIF) of femoral fractures. Methodology: It is a prospective randomized, double-blinded study that was carried out in a Nnamdi Azikiwe University Teaching Hospital, Nnewi in Nigeria. Seventy American Society of Anesthesiologists I or II patients were randomized into two groups of 35 each to receive 3 ml of 0.5% hyperbaric bupivacaine combined with either 7.5 µg of dexmedetomidine in 0.3 ml of normal saline (Group D) or 0.3 ml of normal saline alone (Group S). Patient's outcome measures noted (time to first request of analgesia, proportion of patients with pain score <4 postoperatively using numerical rating scale [NRS], and total analgesic consumed in 24 h.). Results: The patients in Group D had a longer time to first request of analgesia, larger proportion of patients with pain score <4 using NRS in the 2nd h postoperatively and lower amount of total analgesic consumed compared to those in Group S. These differences between the two groups were all statistically significant. Furthermore, there was no difference in the incidences of side effects between the two groups (P > 0.05). However, the patient satisfaction was better in Group D. Conclusion: The addition of 7.5 µg of dexmedetomidine to bupivacaine for subarachnoid block in the management of femoral fractures using ORIF provided better anesthetic profile, particularly prolonged duration of postoperative analgesia without significant side effects.


Assuntos
Analgésicos/administração & dosagem , Bupivacaína/administração & dosagem , Dexmedetomidina/administração & dosagem , Dor Pós-Operatória/prevenção & controle , Adulto , Analgesia/métodos , Analgésicos/farmacologia , Analgésicos não Entorpecentes/administração & dosagem , Analgésicos não Entorpecentes/farmacologia , Raquianestesia , Anestésicos Locais/administração & dosagem , Anestésicos Locais/farmacologia , Bupivacaína/farmacologia , Dexmedetomidina/farmacologia , Método Duplo-Cego , Feminino , Fraturas do Fêmur/cirurgia , Humanos , Injeções Espinhais , Masculino , Pessoa de Meia-Idade , Bloqueio Nervoso/métodos , Nigéria , Manejo da Dor , Período Pós-Operatório , Estudos Prospectivos , Adulto Jovem
10.
J Craniofac Surg ; 31(3): 791-793, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32028367

RESUMO

Plastic surgeons commonly administer subcutaneous epinephrine to reduce intraoperative blood loss. The authors hypothesized that there are safe and effective concentration of epinephrine for vasoconstriction and their durations. The aim of this study is to summarize the existing literatures for the usage of epinephrine mixed with lidocaine in plastic surgical field.In 1903, Braun reported that adrenaline prolonged the local anesthetic effects of cocaine. The Parke-Davis Company began selling cocaine with adrenaline, as well as combining adrenaline with new synthetic local anesthetics.Based on a review of the literature, concentrations between 1:50,000 and 1:400,000 are equally effective and provide superior vasoconstriction compared with more dilute solutions. If epinephrine is further diluted, its onset and time to peak serum concentration are delayed, and its duration of action is shortened. When lidocaine is used without epinephrine, duration of anesthesia is shortened reverse proportionally to the lidocaine concentration. When lidocaine is used with epinephrine, duration of anesthesia is prolonged proportionally to the lidocaine concentration. With slow injection rate in the soft tissue, the maximum safe dose of lidocaine is approximately 3 mg/kg plain and 7 mg/kg when mixed with epinephrine. Lidocaine may protect the myocardium because of its antiarrhythmic activity, which is the rationale for infiltrating lidocaine mixed with epinephrine in general anesthesia.In plastic surgery, subcutaneous infiltration of epinephrine-lidocaine solution is performed to reduce intraoperative blood loss. Even in general anesthesia, infiltrating lidocaine mixed with epinephrine may protect the myocardium because of its antiarrhythmic activity.


Assuntos
Anestésicos Locais/farmacologia , Epinefrina/farmacologia , Lidocaína/farmacologia , Humanos , Procedimentos Cirúrgicos Reconstrutivos , Cirurgia Plástica , Vasoconstrição
11.
Toxicol Appl Pharmacol ; 392: 114921, 2020 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-32061592

RESUMO

Angioedema may occur during local anesthetic (LA) injection in the perioperative period. Histaminergic angioedema is the most common form of angioedema. It has been reported that LA is a potential exogenous ligand for histamine receptor 1 (H1R). Whether H1R participates in LA-induced angioedema is still controversial. By using a constructed H1R high-expressed cell model, siRNA transfection, pharmacologic means, and genetically modified animal models, here we showed that H1R mediated LA-induced hyperpermeability. LA with uncycled N-methyl scaffold in the side chain (procaine, tetracaine and lidocaine) had a better strength of drug-H1R affinity than that for LA with cycled N atom (bupivacaine and ropivacaine) by the molecular docking assay and equilibrium dissociation constant (KD values) obtained from the cell membrane chromatography (CMC) relative standard method. Procaine, tetracaine, and lidocaine triggered big calcium mobilization in H1R-HEK293 cells and human umbilical vein endothelial cells (HUVECs) but much weaker in NC-HEK293 cells or H1R knockdown HUVECs. Besides, the results of transendothelial resistance measurement, paracellular flux assay and immunofluorescence showed that procaine induced H1R-dependent hyperpermeability, which involved in PLCγ/IP3R/PKC, ERK1/2, Akt signaling pathways, downstream vascular endothelial cadherin (VE-cad) destabilization. Furthermore, H1R gene knockout prevented paw swelling and vascular leakage caused by procaine, tetracaine, and lidocaine in vivo. This study supported a key role of H1R in LA-induced angioedema, and suggested that in the design of LA structure, the ring formation of the N-methyl scaffold on the side chain can properly avoid the angioedema.


Assuntos
Anestésicos Locais/farmacologia , Angioedema/patologia , Permeabilidade Capilar/efeitos dos fármacos , Receptores Histamínicos H1/metabolismo , Animais , Feminino , Células HEK293 , Células Endoteliais da Veia Umbilical Humana , Humanos , Masculino , Mastócitos , Camundongos , Camundongos Knockout , Distribuição Aleatória
12.
Pediatr Surg Int ; 36(4): 523-528, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32088740

RESUMO

PURPOSE: To perform a medical evaluation of penile necrosis causes and treatment approaches by examining patients who had penile necrosis after circumcision surgery. METHODS: A total of 24 patients with penile necrosis after circumcision surgery, who presented at various hospitals in Turkey between September 2003 and April 2013 and whose cases were being reviewed at the Institution of Forensic Medicine with regard to malpractice, were evaluated retrospectively. RESULTS: The mean age of the patients was 5 ± 3.7 years, and the mean time of the necrosis diagnosis after circumcision was 5.2 ± 6.3 days. In etiologic terms, the predictive factors were monopolar cautery use in ten (41.6%) patients, post-circumcision infection in eight (33.3%), compartment syndrome due to post-circumcision dressing in three (12.5%), local anesthetic agent used for dorsal nerve blockage in two (8.3%), and methemoglobinemia in one (4.1%) patient. The first approaches to necrosis treatment were surgical intervention in 15 (62.5%) patients, hyperbaric oxygen treatment (HBOT) in 6 (25%), the conservative approach in 2 (8.3%), and HBOT plus surgical intervention in 1 (4.1%) patient. CONCLUSION: Penile necrosis is a preventable complication that requires early intervention. The current study will be helpful in preventing penile necrosis and in guiding surgeons in approaches following its occurrence.


Assuntos
Anestesia Local/métodos , Anestésicos Locais/farmacologia , Circuncisão Masculina/efeitos adversos , Bloqueio Nervoso/métodos , Doenças do Pênis/cirurgia , Pênis/patologia , Complicações Pós-Operatórias/epidemiologia , Adolescente , Bandagens , Criança , Pré-Escolar , Humanos , Incidência , Lactente , Recém-Nascido , Masculino , Necrose/epidemiologia , Necrose/etiologia , Necrose/cirurgia , Doenças do Pênis/epidemiologia , Doenças do Pênis/etiologia , Pênis/cirurgia , Complicações Pós-Operatórias/etiologia , Complicações Pós-Operatórias/cirurgia , Reoperação , Estudos Retrospectivos , Turquia/epidemiologia
13.
Mater Sci Eng C Mater Biol Appl ; 108: 110373, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31924003

RESUMO

We report on the advance of freeze-dried mucoadhesive orodispersible tablets (ODTs) loaded with prilocaine (PRC) and lidocaine (LDC) hydrochlorides, aiming to promote noninvasive buccal anesthesia. The influences of combining biocompatible polymers (pullulan and HPMC K100 LV) and a blend of surfactants (oleic acid, polysorbate 80 and propylene glycol) acting as chemical enhancers on the permeation of such drugs through the esophageal porcine epithelium and in vitro mucoadhesion were investigated. The ODTs were also characterized in terms of average weight, thickness, pH, drug content, in vitro release, thermal behavior and scanning electronic microscopy. A dissolution test showed fast drug release within one hour. The drug release data for all ODTs fitted first order. No significant influence of the type of mucoadhesive polymer on release was observed, while the drug release from ODTs decreased in the presence of chemical enhancers. For the ODT containing pullulan the drug release mechanism was anomalous transport, whist for all others it was case-II transport. A remarkable synergic effect between pullulan and chemical enhancers on the permeation flux, lag time, and permeability coefficient of both drugs, but mainly for PRC was observed. Pullulan together with permeation enhancers also substantially improved the work of mucoadhesion as compared to HPMC. In contrast, HPMC improved drug retention in the epithelium. The novel drug delivery platform achieved by combining a freeze-drying technique, mucoadhesive biocompatible polymers, and chemical permeation enhancers displayed an effective strategy for the transbuccal delivery of PRC and LDC that can be used to improve needle-free buccal anesthesia.


Assuntos
Anestésicos Locais/farmacologia , Mucosa Bucal/efeitos dos fármacos , Muco/química , Polímeros/farmacologia , Tensoativos/farmacologia , Adesividade , Animais , Varredura Diferencial de Calorimetria , Liberação Controlada de Fármacos , Epitélio/efeitos dos fármacos , Esôfago/efeitos dos fármacos , Liofilização , Cinética , Lidocaína/farmacologia , Permeabilidade , Prilocaína/farmacologia , Suínos , Comprimidos , Temperatura
15.
Clin Oral Investig ; 24(1): 239-246, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31079247

RESUMO

OBJECTIVES: This study aimed to evaluate pulse pressure fluctuation on dental local anesthetic administration in diabetic patients with and without coronary heart disease undergoing tooth extraction. MATERIALS AND METHODS: This retrospective study in diabetic patients undergoing tooth extraction included 33 patients with coronary heart disease (mean age 79.3 ± 7.4, 64% male) and 49 patients without coronary heart disease (mean age 78.6 ± 6.5, 29% male). The increase in pulse pressure before and after administration of local anesthetics was compared between diabetic patients with and without coronary heart disease. RESULTS: Pulse pressure was increased in male diabetic patients with coronary heart disease compared with those without coronary heart disease following administration of 3% prilocaine hydrochloride with felypressin 0.03 IU/mL (prilocaine) (15.6 ± 15.4 mmHg in those with coronary heart disease (n = 11) versus 4.3 ± 10.9 mmHg in those without coronary heart disease (n = 13), p = 0.03). CONCLUSIONS: Prilocaine administration increased pulse pressure in male diabetic patients with coronary heart disease compared with those without coronary heart disease. Further study is needed to reveal the mechanisms involved in the increase in pulse pressure. CLINICAL RELEVANCE: This is the first study of pulse pressure fluctuation in diabetic patients with and without coronary heart disease following administration of local anesthetics. Our findings can help guide the choice of local anesthetics and serve as a predictor of coronary vascular condition in diabetic patients during dental treatment.


Assuntos
Anestesia Dentária , Pressão Sanguínea , Doença das Coronárias , Diabetes Mellitus , Idoso , Idoso de 80 Anos ou mais , Anestésicos Locais/farmacologia , Pressão Sanguínea/efeitos dos fármacos , Doença das Coronárias/complicações , Epinefrina , Felipressina/farmacologia , Feminino , Frequência Cardíaca , Humanos , Lidocaína , Masculino , Prilocaína/farmacologia , Estudos Retrospectivos , Extração Dentária , Vasoconstritores
16.
Mini Rev Med Chem ; 20(1): 3-11, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31518221

RESUMO

Benzocaine is well-known for its role as an anesthetic agent and largely used in oral ulcers, ear pain and dental complications. Along with lidocaine and other local anesthetics, benzocaine has marked it as an anesthetic agent in surgical procedures and as Na+ channels blocker, as well. Analogues of benzocaine have been found to possess biological potentials including antibacterial, antifungal and anti-cancer. Some derivatives were found to have conspicuous action against tuberculosis. The current review focuses to explore the century-long potential of the molecule and its analogs that have appeared in the literature. Furthermore, highlighting the biological potential of benzocaine and its analogues shall open-up new dimensions of future research to design more potent analogues.


Assuntos
Anestésicos Locais/química , Anestésicos Locais/farmacologia , Benzocaína/análogos & derivados , Benzocaína/farmacologia , Desenvolvimento de Medicamentos , Anestésicos Locais/uso terapêutico , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/uso terapêutico , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Benzocaína/uso terapêutico , Desenvolvimento de Medicamentos/métodos , Descoberta de Drogas/métodos , Humanos
17.
Vet Rec ; 186(16): 534, 2020 05 16.
Artigo em Inglês | MEDLINE | ID: mdl-31879322

RESUMO

BACKGROUND: The aims of this study were evaluate cardiopulmonary, sedative and antinociceptive effects of dexmedetomidine-lidocaine combination via lumbosacral epidural injection in sheep. METHODS: Six Santa Inês breed sheep, 16±6 months old and weighing 42.2 ± 5.7 kg were used. Sheep were subjected to epidural anaesthesia with three treatments: L, lidocaine (1.2 mg/kg), D, dexmedetomidine (2.5 µg/kg) or DL, dexmedetomidine plus lidocaine (2.5 µg/kg + 1.2 mg/kg). Drugs were injected via pre-placed lumbosacral epidural catheters. Cardiopulmonary, arterial blood gases, electrolytes, degree of sedation and antinociceptive aspects were measured before drug administration (T0) and then at 15, 30, 60 and 120 min after drug injection (T15-T120) in all treatments and at T0 to T240 in DL. RESULTS: There were significantly increases in PaCO2 at times T60 and T120 in D, and at T30-T120 in DL, compared to baseline. The antinociceptive effects were observed up to 240 min in DL and 60 min in L, and were more intense in DL. Treatment D provided analgesia only in the perineal region, and only at T15. CONCLUSION: The combination of DEX with lidocaine produced similar cardiopulmonary changes compared with either drug alone, but with greater and more prolonged antinociceptive effects.


Assuntos
Dexmedetomidina/administração & dosagem , Dexmedetomidina/farmacologia , Lidocaína/administração & dosagem , Lidocaína/farmacologia , Anestésicos Locais/administração & dosagem , Anestésicos Locais/farmacologia , Animais , Pressão Sanguínea/efeitos dos fármacos , Combinação de Medicamentos , Feminino , Frequência Cardíaca/efeitos dos fármacos , Hipnóticos e Sedativos/administração & dosagem , Hipnóticos e Sedativos/farmacologia , Injeções Epidurais/veterinária , Masculino , Dor/tratamento farmacológico , Dor/veterinária , Taxa Respiratória/efeitos dos fármacos , Ovinos
18.
Colloids Surf B Biointerfaces ; 185: 110632, 2020 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-31735422

RESUMO

Lidocaine is widely used as a local anaesthetic in the clinical practice to manage pre- and post-operative pain, skin burns, etc. However, the short duration of action (< 2 h) of marketed dosage forms limit their ability to meet clinical needs. Herein, we prepared a lidocaine-tPP(tri potassium phosphate)-complex loaded microemulsion to achieve greater penetration, followed by destabilization of microemulsion in the skin layer to precipitate oil-complex to produce a depot effect in the skin for prolonging the effects of anaesthesia. The lidocaine-tPP-complex-microemulsion was compared with lidocaine base loaded microemulsion, marketed ointment USP and lidocaine HCl. The pseudo ternary phase diagrams at three Smix ratios (1:2, 1:3 and 1:4; Pluronic F127: PEG 400) were constructed using Capmul MCM C8 EP as oil phase. The Smix at 1:4 ratio showed large microemulsion area in comparison to 1:2 and 1:6 ratio. The lidocaine base (LD-1:4-ME10O45SM and LD-1:4-ME20O45SM) and lidocaine-tPP-complex (LDC-1:4-ME10O45SM and LDC-1:4-ME20O45SM) loaded microemulsion batches (1:4 ratio) were thermodynamically stable. The ex vivo diffusion study showed sustained release up to 12 h with microemulsion batches, in comparison to lidocaine HCl (4 h) and ointment base (7 h). The selected LDC-1:4-ME20O45SM batch was non-irritating on the rabbit skin. In drug retention studies, LD-1:4-ME20O45SM and LDC-1:4-ME20O45SM batches showed 2.68- and 3.93-fold greater lidocaine retention in comparison to ointment USP. The radiant heat tail-flick test showed prolong local anaesthesia using LDC-1:4-ME20O45SM in comparison to ointment USP. The findings suggest that lidocaine-tPP-complex loaded microemulsion could be a potential strategy for providing prolong local anaesthesia.


Assuntos
Anestesia Local , Emulsões/química , Lidocaína/farmacologia , Polifosfatos/farmacologia , Analgésicos/farmacologia , Anestésicos Locais/farmacologia , Animais , Corantes/química , Difusão , Condutividade Elétrica , Cabras , Concentração de Íons de Hidrogênio , Masculino , Tamanho da Partícula , Transição de Fase , Coelhos , Ratos Wistar , Pele/efeitos dos fármacos , Testes de Irritação da Pele , Eletricidade Estática , Termodinâmica , Viscosidade
19.
Am J Vet Res ; 81(1): 13-16, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31887088

RESUMO

OBJECTIVE: To assess onset of analgesia for 3% chloroprocaine hydrochloride and 2% mepivacaine hydrochloride when used for median and ulnar nerve blocks in lame horses. ANIMALS: 6 naturally lame horses. PROCEDURES: A crossover experiment was conducted. Horses were assigned to 1 of 2 treatment groups (3% chloroprocaine or 2% mepivacaine first). Median and ulnar nerve blocks were performed in the lame limb with the assigned treatment. Lameness was objectively evaluated before treatment administration and at various points for 120 minutes after treatment with a wireless inertial sensor-based motion analysis system. Following a 7-day washout period, horses then received the other treatment and lameness evaluations were repeated. RESULTS: Median and ulnar nerve blocks performed with 3% chloroprocaine resulted in more consistent, rapid, and profound amelioration of lameness than did blocks performed with 2% mepivacaine. Lameness decreased more between 20 and 40 minutes after injection when 3% chloroprocaine was used than when 2% mepivacaine was used. Complete resolution of lameness was detected a mean of 9 minutes after injection when median and ulnar nerve blocks were performed with 3% chloroprocaine and a mean of 28 minutes after injection when performed with 2% mepivacaine. CONCLUSIONS AND CLINICAL RELEVANCE: 3% chloroprocaine had a more rapid onset and provided better analgesia for median and ulnar nerve blocks in horses with naturally occurring lameness, compared with 2% mepivacaine. These favorable properties suggest that 3% chloroprocaine would be useful for performance of median and ulnar regional nerve blocks during complicated lameness evaluations.


Assuntos
Marcha/efeitos dos fármacos , Doenças dos Cavalos/tratamento farmacológico , Coxeadura Animal/tratamento farmacológico , Bloqueio Nervoso/veterinária , Dor/veterinária , Procaína/análogos & derivados , Analgesia/veterinária , Anestésicos Locais/farmacologia , Anestésicos Locais/uso terapêutico , Animais , Estudos Cross-Over , Cavalos , Masculino , Mepivacaína/farmacologia , Mepivacaína/uso terapêutico , Dor/tratamento farmacológico , Procaína/farmacologia , Procaína/uso terapêutico
20.
Acta Med Okayama ; 73(6): 543-546, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31871339

RESUMO

We here report that a 71-year-old Japanese woman with a history of anaphylaxis induced by muscle relaxants had local anesthetic systemic toxicity (LAST) following an abdominal surgery under general anesthesia with combined spinal-epidural anesthesia without muscle relaxants. The total dosages of local anesthetics reached 0.67 mg/kg of ropivacaine and 11.5 mg/kg of lidocaine over 12.5 h to obtain sufficient muscle relaxation for surgery. Regional anesthesia is useful in cases in which muscle relaxants are to be avoided during a surgery. However, especially for a patient with risk factors and prolonged surgery, precautions should be taken to prevent LAST.


Assuntos
Anestesia Epidural/efeitos adversos , Raquianestesia/efeitos adversos , Anestésicos Locais/efeitos adversos , Emulsões Gordurosas Intravenosas/uso terapêutico , Lidocaína/efeitos adversos , Ropivacaina/efeitos adversos , Idoso , Anestésicos Locais/administração & dosagem , Anestésicos Locais/farmacologia , Emulsões Gordurosas Intravenosas/administração & dosagem , Feminino , Humanos , Lidocaína/administração & dosagem , Lidocaína/farmacologia , Ropivacaina/administração & dosagem , Ropivacaina/farmacologia
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