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Braz. j. med. biol. res ; 53(2): e8793, 2020. tab, graf
Article in English | LILACS | ID: biblio-1055493


Aliskiren (ALS) is well known for its antihypertensive properties. However, the potential underlying the molecular mechanism and the anti-hypertrophic effect of ALS have not yet been fully elucidated. The aim of the present study was to investigate the role of ALS in mammalian target of rapamycin (mTOR) and apoptosis signaling using in vivo and in vitro models of cardiac hypertrophy. A rat model of cardiac hypertrophy was induced by isoproterenol treatment (5 mg·kg-1·day-1) for 4 weeks, with or without ALS treatment at 20 mg·kg-1·day-1. The expression of hypertrophic, fibrotic, and apoptotic markers was determined by RT-qPCR. The protein expression of apoptotic markers mTOR and p-mTOR was assessed by western blot analysis. The proliferation of H9C2 cells was monitored using the MTS assay. Cell apoptosis was analyzed using flow cytometry. In vivo, isoproterenol-treated rats exhibited worse cardiac function, whereas ALS treatment reversed these dysfunctions, which were associated with changes in p-mTOR, Bcl-2, Bax, and cleaved caspase-3 expression, as well as the number of apoptotic cells. In vitro, H9C2 cardiomyocyte viability was significantly inhibited and cardiac hypertrophy was induced by Ang II administration, but ALS reversed Ang II-induced H9C2 cardiomyocyte hypertrophy and death. Furthermore, Ang II triggered the activation of the mTOR and apoptosis pathways in hypertrophic cardiomyocytes that were inhibited by ALS treatment. These results indicated that ALS alleviated cardiac hypertrophy through inhibition of the mTOR and apoptosis pathways in cardiomyocytes.

Animals , Male , Rats , Apoptosis/drug effects , Cardiomegaly/prevention & control , TOR Serine-Threonine Kinases/metabolism , Fumarates/administration & dosage , Amides/administration & dosage , Fibrosis/chemically induced , Fibrosis/prevention & control , Angiotensin II/pharmacology , Signal Transduction/drug effects , Blotting, Western , Rats, Sprague-Dawley , Cardiomegaly/chemically induced , Cardiomegaly/metabolism , Reverse Transcriptase Polymerase Chain Reaction , Disease Models, Animal , TOR Serine-Threonine Kinases/drug effects , Flow Cytometry , Isoproterenol/pharmacology
Article in Chinese | WPRIM | ID: wpr-827933


Two new phenylpropanoid amide glycosides and ten analogues were isolated from the CH_2Cl_2 layer of 95% ethanol extract of the whole plants of Corydalis racemosa by using various chromatographic techniques, including silica gel, Sephadex LH-20, ODS column chromatographies, and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties, MS, NMR, and IR spectroscopic data as N-cis-sinapoyltyramine-4'-O-β-glucoside(1), N-cis-sinapoyl-3-methoxytyramine-4'-O-β-glucoside(2), N-cis-sinapoyltyramine(3), N-cis-feruloyltyramine(4), N-trans-cinnamoyltyramine(5), N-trans-feruloylphenethylamine(6), N-trans-p-methoxycinnamoyl-3-hydoxyoctopamine(7), N-cis-feruloyl-3-methoxytyramine(8), N-trans-feruloyltyramine(9), N-trans-feruloyl-3-methoxytyramine(10), N-trans-sinapoyltyramine(11), and N-trans-p-coumaroyltyramine(12). Compounds 1 and 2 are new compounds. Compounds 3-7 are obtained from the plants of Papaveraceae for the first time, and compounds 8-12 are firstly isolated from C. racemosa.

Amides , Chromatography, High Pressure Liquid , Corydalis , Glucosides , Glycosides
Rev Assoc Med Bras (1992) ; 66(Suppl 2): 65-70, 2020. tab, graf
Article in English | SES-SP, LILACS, SES-SP | ID: biblio-1136391


SUMMARY INTRODUCTION This study aims to evaluate changes in hematological parameters after the follow-up of patients who received treatment with favipiravir due to COVID-19 infections. METHODS Sixty-two cases receiving favipiravir treatment for at least five days due to COVID-19 infection were evaluated retrospectively. Parameters including age, gender, nasopharyngeal swab positivity, and chronic diseases were analyzed. Hematologic parameters were analyzed before and after the treatment. RESULTS The mean age of the patients receiving treatment with favipiravir was 63.7±12.3 years. Nasopharyngeal swab positivity was detected in 67.7%. The most common comorbid conditions detected in patients were hypertension in 25 cases (40.3%) and diabetes in 16 cases (25.8%). In the statistical analysis of the hematological parameters before and after treatment with favipiravir, WBC, PT-PTT-INR levels were found to be unaffected; the mean RBC was found to have decreased from 4.33 ± 0.58 M/uL to 4.16 ± 0.54 M/uL (p:0.003); the median hemoglobin level was found to have decreased from 12.3 g/dl to 11.9 g/dl (p:0.041); the hematocrit level decreased from 38.1% ± 4.8 to 36.9% ± 4.2 (p:0.026); the median neutrophil count decreased from 4.57 K/uL to 3.85 K/uL (p:0.001); the mean lymphocyte count increased from 1.22 ± 0.53 K/uL to 1.84 ± 1.19 K/uL (p:0.000); and the mean platelet count increased from 244.1 ± 85.1 K/uL to 281.9 ± 103.3 K/uL (p:0.005). CONCLUSION We concluded that the pathological effect of treatment with favipiravir on the hematologic system was the suppression in the erythrocyte series, and there were no adverse effects in other hematologic parameters.

RESUMO INTRODUÇÃO Este estudo tem como objetivo avaliar as alterações nos parâmetros hematológicos após o acompanhamento de pacientes que receberam tratamento com favipiravir devido à infecção por Covid-19. MÉTODOS Sessenta e dois casos em tratamento com favipiravir por pelo menos cinco dias devido à infecção por Covid-19 foram avaliados retrospectivamente. Parâmetros como idade, sexo, positividade do swab nasofaríngeo e doenças crônicas foram analisados. Os parâmetros hematológicos foram analisados antes e após o tratamento. RESULTADOS A idade média dos pacientes que receberam tratamento com favipiravir foi de 63,7±12,3 anos. A positividade do swab nasofaríngeo foi detectada em 67,7%. As condições comórbidas mais comuns detectadas nos pacientes foram hipertensão em 25 casos (40,3%) e diabetes em 16 casos (25,8%). Na análise estatística dos parâmetros hematológicos antes e após o tratamento com favipiravir, os níveis de leucócitos, PT-PTT-INR não foram afetados. Verificou-se que o RBC médio diminuiu de 4,33±0,58 M/uL para 4,16±0,54 M/uL (p=0,003); o nível médio de hemoglobina foi reduzido de 12,3 g/dl para 11,9 g/dl (p=0,041); o nível de hematócrito diminuiu de 38,1%±4,8 para 36,9%±4,2 (p=0,026); a contagem mediana de neutrófilos diminuiu de 4,57 K/uL para 3,85 K/uL (p=0,001); a contagem média de linfócitos aumentou de 1,22±0,53 K/uL para 1,84±1,19 K/uL (p=0,000); a contagem média de plaquetas aumentou de 244,1±85,1 K/uL para 281,9±103,3 K/uL (p=0,005). CONCLUSÃO Concluiu-se que o efeito patológico do tratamento com favipiravir no sistema hematológico foi a supressão na série eritrocitária e que não houve efeitos adversos em outros parâmetros hematológicos.

Humans , Male , Female , Adolescent , Aged , Aged, 80 and over , Pneumonia, Viral/drug therapy , Pyrazines/therapeutic use , Coronavirus Infections/drug therapy , Pandemics , Betacoronavirus , Amides/therapeutic use , Platelet Count , Pneumonia, Viral/epidemiology , Hemoglobins/analysis , Retrospective Studies , Coronavirus Infections , Coronavirus Infections/epidemiology , CD4 Lymphocyte Count , Leukocyte Count , Middle Aged
Article in Korean | WPRIM | ID: wpr-716212


PURPOSE: Our previous study demonstrated that persimmon (Diospyros kaki Thumb.) at different stages of ripening provided different protective effects against high-fat/cholesterol diet (HFD)-induced dyslipidemia in rats. In this study, we compared the metabolites profile and gene expressions related to triglyceride (TG)/cholesterol metabolism in vitro and in vivo after treating with persimmon water extracts (PWE) or tannin-enriched persimmon concentrate (TEP). METHODS: Primary and secondary metabolites in test materials were determined by GC-TOF/MS, UHPLC-LTQ-ESI-IT-MS/MS, and UPLC-Q-TOF-MS. The expression of genes related to TG and cholesterol metabolism were determined by RT-PCR both in HepG2 cells stimulated by oleic acid/palmitic acid and in liver tissues obtained from Wistar rats fed with HFD and PWE at 0, 150, 300, and 600 mg/d (experiment I) or TEP at 0, 7, 14, and 28 mg/d (experiment II) by oral gavage for 9 weeks. RESULTS: PLS-DA analysis and heatmap analysis demonstrated significantly differential profiling of metabolites of PWE and TEP according to processing of persimmon powder. In vitro, TEP showed similar hypolipidemic effects as PWE, but significantly enhanced hypocholesterolemic effects compared to PWE in sterol regulatory element-binding protein 2 (SREBP2), HMG-CoA reductase (HMGCR), proprotein convertase subtilisin/kexin type 9 (PCSK9), cholesterol 7α-hydroxylase (CYP7A1), and low density lipoprotein receptor (LDLR) gene expression. Consistently, TEP and PWE showed similar hypolipidemic capacity in vivo, but significantly enhanced hypocholesterolemic capacity in terms of SREBP2, HMGCR, and bile salt export pump (BSEP) gene expression. CONCLUSION: These results suggest that column extraction after hot water extraction may be a good strategy to enhance tannins and long-chain fatty acid amides, which might cause stimulation of hypocholesterolemic actions through downregulation of cholesterol biosynthesis gene expression and upregulation of LDL receptor gene expression.

Amides , Animals , Bile , Cholesterol , Diet , Diospyros , Down-Regulation , Dyslipidemias , Gene Expression , Hep G2 Cells , In Vitro Techniques , Liver , Metabolism , Oxidoreductases , Proprotein Convertases , Rats , Rats, Wistar , Receptors, LDL , Tannins , Triglycerides , Up-Regulation , Water
Article in English | WPRIM | ID: wpr-739991


The objective of this review was to investigate the efficacy of dental local anesthetics, as it is well known among clinicians that local anesthesia may be challenging in some circumstances. Therefore, the focus of this review was on the efficacy of the products used in dental local anesthesia. In a Pubmed database literature search conducted, a total of 8646 articles were found to be related to dental local anesthetics. After having applied the inclusion criteria (human research, performed in the last 10 years, written in English language, and focus on dental local anesthetics) and having assessed the quality of the papers, 30 were deemed eligible for inclusion in this review. The conclusion of this review is that none of the dental local anesthetic amides provide 100% anesthesia. The problem appears to be more pronounced when mandibular teeth are attempted to be anaesthetized and especially if there is irreversible pulpitis involved. The authors conclude that this finding suggest exploration of more efficient techniques to administer dental local anesthesia, especially in the mandible, to establish a 100% efficacy, is needed.

Amides , Anesthesia , Anesthesia, Local , Anesthetics, Local , Mandible , Pulpitis , Tooth
Article in Chinese | WPRIM | ID: wpr-776416


Ten phenylpropanoid amides were isolated from the whole plants of Corydalis edulis Maxim. by various of column chromatographies including silica gel, Sephadex LH-20, and ODS. Their structures were identified on the basis of physicochemical properties, MS, NMR, and IR spectroscopic data. These compounds were identified as N-trans-sinapoyl-3-methoxytyramine-4'-O-β-glucoside(1), N-trans-sinapoyl-3-methoxytyramine(2), N-trans-sinapoyltyramine(3), N-trans-p-coumaroyltyramine(4), N-trans-sinapoyl-7-hydroxytyramine(5), N-cis-feruloyltyramine(6), N-cis-p-coumaroyltyramine(7), N-trans-feruloyltyramine(8), N-trans-feruloyl-3-methoxytyramine(9), and N-trans-feruloyl-7-hydroxytyramine(10). Compound 1 is a new compound. Compounds 2-7 are obtained from the plants of Papaveraceae for the first time, while compounds 8-10 are firstly isolated from C. edulis.

Amides , Corydalis , Chemistry , Glucosides , Phytochemicals , Tyramine
J. bras. nefrol ; 39(2): 108-118, Apr.-June 2017. tab, graf
Article in English | LILACS | ID: biblio-893744


Abstract Introduction: It is still unknown how the pharmacological inhibition of the Renin Angiotensin System (RAS) impacts the levels of inflammation and fibrosis biomarkers. Objective: This study sought to evaluate the effect of enalapril, candesartan and aliskiren on urinary levels of cytokines in a model of chronic kidney disease (CKD). Methods: Male Wistar rats were submitted to surgical removal of ¾ of renal parenchyma to induce CKD (¾ nephrectomy), or subjected to sham surgery (control). Animals were then randomized into five groups: Sham surgery receiving vehicle; ¾ Nephrectomy receiving vehicle; ¾ Nephrectomy receiving enalapril (10 mg/kg); ¾ Nephrectomy receiving candesartan (10 mg/kg) and ¾ Nephrectomy receiving aliskiren (10 mg/kg). Urine output, water intake, mean arterial pressure (MAP) and urinary concentrations of creatinine, urea, albuminuria, Na+, K+, interleukin (IL) -1β, IL-6, IL-10 and transforming growth factor beta (TGF-β) were measured. Results: Nephrectomy significantly impaired renal function, increased MAP and altered the levels of all evaluated cytokines in urine. Enalapril, candesartan and aliskiren improved renal function and decreased MAP and IL-6 when compared to vehicle-treated nephrectomized group. Candesartan and aliskiren decreased IL-1β, while only candesartan reduced TGF-β and only aliskiren increased IL-10. Conclusion: Enalapril, candesartan and aliskiren presented similar effects on improving renal function and reducing MAP and urinary levels of IL-6 in rats with CKD. On the other hand, cytokine profile differed according to the treatment, suggesting that differential mechanisms were triggered in response to the site of RAS blockade.

Resumo Introdução: Ainda não se sabe como a inibição farmacológica do Sistema Renina Angiotensina (SRA) afeta os níveis de biomarcadores de inflamação e fibrose. Objetivo: Este estudo pretendeu avaliar o efeito de enalapril, candesartan e alisquireno sobre os níveis urinários de citocinas em um modelo de doença renal crônica (DRC). Métodos: Ratos Wistar machos foram submetidos à remoção cirúrgica de ¾ do parênquima renal para induzir DRC (nefrectomia), ou submetidos à cirurgia fictícia (controle). Animais foram então randomizados em cinco grupos: Cirurgia fictícia recebendo veículo; Nefrectomia recebendo veículo; Nefrectomia recebendo enalapril (10 mg/kg); Nefrectomia recebendo candesartan (10 mg/kg) e Nefrectomia recebendo alisquireno (10 mg/kg). Débito urinário, ingesta hídrica, pressão arterial media (PAM) e concentrações urinárias de creatinina, ureia, albumina, Na+, K+, interleucina (IL) -1β, IL-6, IL-10 e fator de transformação e crescimento beta (TGF-β) foram medidas. Resultados: A nefrectomia comprometeu significativamente a função renal, aumentou a PAM e alterou os níveis de todas as citocinas avaliadas na urina. Enalapril, candesartan e alisquireno melhoraram a função renal e diminuíram a PAM e a IL-6 quando comparado aos grupo de animais nefrectomizados tratados com veículo. Candesartan e alisquireno reduziram IL-1β, enquanto somente candesartan diminuiu o TGF-β e somente alisquireno aumentou a IL-10. Conclusão: Enalapril, candesartan e alisquireno apresentaram efeitos similares em relação à melhora da função renal e redução da PAM e dos níveis urinários de IL-6 em ratos com DRC. Por outro lado, o perfil de citocinas diferiu de acordo com o tratamento, sugerindo que diferentes mecanismos sejam desencadeados em resposta ao local de bloqueio do SRA.

Animals , Male , Rats , Benzimidazoles/pharmacology , Angiotensin-Converting Enzyme Inhibitors/pharmacology , Enalapril/pharmacology , Cytokines/urine , Angiotensin II Type 1 Receptor Blockers/pharmacology , Amides/pharmacology , Renin-Angiotensin System/drug effects , Tetrazoles/pharmacology , Random Allocation , Rats, Wistar , Fumarates/pharmacology , Nephrectomy
Rev. bras. anestesiol ; 67(2): 131-138, Mar.-Apr. 2017. tab, graf
Article in English | LILACS | ID: biblio-843375


Abstract Objectives: The increase in the prevalence of obesity presents a significant health and economic problem. Obesity has been reported to be a major contributor to variety of chronic diseases. Childhood obesity has been rising over the past decades leading to various complications in health. Millions of infants and children undergo surgery every year on various health grounds. The present investigation was undertaken to evaluate the effect of spinal anesthesia of equipotent doses of ropivacaine and bupivacaine on over-weight neonatal rats. Methods: The Sprague-Dawley rat pups were overfed on high fat diet to induce obesity. Behavioral assessments for sensory and motor blockade was made by evaluating thermal and mechanical withdrawal latencies at various time intervals following intrathecal injections of bupivacaine (5.0 mg·kg-1) and ropivacaine (7.5 mg·kg-1) in P14 rats. Spinal tissue was analyzed for apoptosis by determination of activated caspase-3 using monoclonal anti-activated caspase-3 and Fluoro-Jade C staining. Long-term spinal function in P30 rat pups was evaluated. Results: Exposure to intrathecal anesthesia in P14 increased thermal and mechanical latencies and was observed to increase apoptosis as presented by increase in activated caspase-3 and Fluro-Jade C positive cells. Significant alterations in spinal function were observed in high fat diet-fed pups as against non-obese control pups that were on standard diet. Bupivacaine produced more pronounced apoptotic effects on P14 pups; ropivacaine however produced long lasting effects as evidenced in motor function tests at P30. Conclusion: Ropivacaine and bupivacaine induced spinal toxicity that was more pronounced in over-fed rat pups as against normal controls.

Resumo Objetivos: O aumento da prevalência da obesidade é um problema sério de saúde e econômico. A obesidade tem sido relatada como um dos principais contribuintes para uma variedade de doenças crônicas. A obesidade infantil tem aumentado nas últimas décadas e levado a complicações de saúde. Milhões de bebês e crianças são submetidos a cirurgia todos os anos por diversos motivos de saúde. O presente estudo foi feito para avaliar o efeito da raquianestesia com doses equipotentes de ropivacaína e bupivacaína em ratos recém-nascidos com sobrepeso. Métodos: As crias de ratos Sprague-Dawley foram alimentadas em excesso com dieta rica em gordura para induzir obesidade. Avaliações comportamentais para bloqueio sensorial e motor foram feitas por meio da avaliação das latências de retirada térmicas e mecânicas em vários intervalos de tempo após injeções por via intratecal de bupivacaína (5,0 mg·kg-1) e ropivacaína (7,5 mg·kg-1) em ratos P14. Tecido medular foi analisado para apoptose por determinação da caspase-3 ativada, com o uso de anticorpo monoclonal anti-caspase 3 ativada e ecoloração com Fluoro-Jade C. A função da coluna vertebral em longo prazo em filhotes de ratos P30 foi avaliada. Resultados: A exposição à anestesia intratecal em P14 aumentou as latências térmicas e mecânicas e observamos aumento da apoptose, como apresentado pelo aumento da caspase-3 ativada e células positivas para Fluro-Jade C. Alterações significativas da função da coluna vertebral foram observadas em filhotes alimentados com dieta rica em gordura versus filhotes controles não obesos em dieta padrão. Bupivacaína produziu efeitos apoptóticos mais pronunciados sobre os filhotes P14; ropivacaína, entretanto, produziu efeitos duradouros, como evidenciado nos testes de função motora em P30. Conclusão: Ropivacaína e bupivacaína induziram toxicidade medular mais pronunciada nos filhotes de ratos sobrealimentados do que nos controles normais.

Animals , Male , Female , Rats , Bupivacaine/administration & dosage , Amides/administration & dosage , Anesthetics, Local/administration & dosage , Obesity/complications , Time Factors , Injections, Spinal , Bupivacaine/toxicity , Rats, Sprague-Dawley , Apoptosis/drug effects , Disease Models, Animal , Overweight/complications , Caspase 3/metabolism , Diet, High-Fat , Ropivacaine , Amides/toxicity , Anesthesia, Spinal/adverse effects , Anesthesia, Spinal/methods , Anesthetics, Local/toxicity , Animals, Newborn
Rev. bras. anestesiol ; 67(1): 85-88, Jan.-Feb. 2017. graf
Article in English | LILACS | ID: biblio-843359


Abstract Background and objectives: Congenital unilateral absence of a pulmonary artery (UAPA) is a rare anomaly. Although there are several reports regarding pregnancy in patients with unilateral absence of a pulmonary artery, there are no case reports describing anesthesia for Cesarean section in a patient with unilateral absence of a pulmonary artery. Case report: We present a patient with unilateral absence of a pulmonary artery who underwent Cesarean sections twice at the ages of 24 and 26 years under spinal anesthesia for surgery and epidural analgesia for postoperative pain relief. Both times, spinal anesthesia and epidural analgesia enabled successful anesthesia management without the development of either pulmonary hypertension or right heart failure. Conclusion: Spinal anesthesia combined with epidural analgesia is a useful anesthetic method for a Cesarean section in patients with unilateral absence of a pulmonary artery.

Resumo Justificativa e objetivos: A ausência congênita unilateral de uma artéria pulmonar (ACAP) é uma anomalia rara. Embora existam vários relatos sobre pacientes grávidas com ACAP, não há relatos de casos que descrevam anestesia para cesariana em pacientes com ACAP. Relato de caso: Apresentamos uma paciente com ACAP que foi submetida a duas cesarianas, aos 24 e 26 anos, sob raquianestesia para a cirurgia e analgesia epidural para a dor no pós-operatório. Nas duas cesarianas, a raquianestesia e a analgesia epidural possibilitaram o manejo bem-sucedido da anestesia, sem a ocorrência de qualquer hipertensão pulmonar ou insuficiência cardíaca direita. Conclusão: Raquianestesia combinada com analgesia epidural é um método anestésico útil para cesarianas em pacientes com ACAP.

Humans , Female , Pregnancy , Adult , Young Adult , Pulmonary Artery/abnormalities , Cesarean Section/methods , Pain, Postoperative/prevention & control , Pregnancy Complications, Cardiovascular , Infusions, Intravenous , Midazolam/administration & dosage , Bupivacaine/administration & dosage , Analgesia, Epidural/methods , Cesarean Section, Repeat/methods , Ropivacaine , Amides , Hypnotics and Sedatives , Anesthesia, Epidural , Anesthesia, Obstetrical/methods , Anesthesia, Spinal/methods , Anesthetics, Local/administration & dosage
Anaesthesia, Pain and Intensive Care. 2017; 21 (2): 141-146
in English | IMEMR | ID: emr-189137


Objective: To compare the effect of adding two different doses of dexmedetomidine to ropivacaine, on onset and duration of analgesia for supraclavicular brachial plexus block in patients scheduled for upper limb orthopedic surgery

Methodology: This prospective randomized double blind comparative study was conducted at our institution. After ethical committee approval and informed patient consents, 50 patients of ASA I, II and aged 21-60 years, who were scheduled for elective upper limb surgery and were enrolled in the study and randomly divided into two equal groups. They received either 30 ml of 0.75% ropivacaine plus dexmedetomidine [1 micro g/kg] diluted with normal saline up to 5 ml [total volume = 35 ml] in Group 1 or 30 ml of 0.75% ropivacaine plus dexmedetomidine [2 micro g/kg] diluted with normal saline up to 5 ml [total volume = 35 ml] in Group 2. The onset and duration of sensory and motor block, duration of analgesia, hemodynamic parameters, sedation score, VAS and side effects were recorded

Results: Onset time of sensory and motor block were earlier in Group 2 than in Group 1 [p < 0.001]. Duration of sensory and motor block and duration of analgesia were longer in Group 2 than in Group 1 [p < 0.001]. There was no significant difference in the incidence of hypotension and bradycardia between both the groups [p > 0.05]. There was a statistically significant reduction in number of rescue analgesic doses and total dose consumption in 24 hours in Group 2 than in Group 1. Quantitative data are represented as arithmetic mean and standard deviation and analyzed using Student's t test or ANOVA as per need. Qualitative data are represented as number [proportion or percentage] and analyzed using Chi square test. The levels of significance and alpha-error were kept 95% and 5% respectively for all statistical analyses. P values < 0.05 were considered significant

Humans , Male , Female , Adult , Middle Aged , Upper Extremity/surgery , Brachial Plexus Block , Clavicle , Prospective Studies , Double-Blind Method , Analgesia , Amides
Anaesthesia, Pain and Intensive Care. 2017; 21 (1): 59-64
in English | IMEMR | ID: emr-187464


Aims and Background: To prolong postoperative analgesia many adjuvants has been used opioids and alpha-2 agonists are very popular among them. This study was aimed at comparing the sensory, motor, hemodynamic, sedative and analgesic properties of epidural administration of fentanyl and dexmedetomidine as an adjuvant to ropivacaine

Methodology: With Institutional ethical committee clearance this study was conducted at our hospital. After obtaining informed and written consent, a total of 60 patients scheduled for elective percutaneous nephrolithotomy [PCNL] were randomly allocated into two groups of 30 each. Patients of both genders, aged 21-60 y, ASA physical status I and II were enrolled. Group RD received 28 ml of inj ropivacaine 0.5% + dexmedetomidine 1 ng/kg and Group RF received 28 ml of ropivacaine 0.5% + inj fentanyl 1 pig/kg epidurally. Hemodynamic parameters, sedation scores, and time to onset of sensory loss, complete motor blockade, two segmental dermatomal regression and time of first rescue analgesic were recorded. Data were compiled systematically and analyzed using unpaired t-test, Chi-square and Mann-Whitney U test. P < 0.05 was considered significant

Results: The demographic profile of patients was comparable in both groups. Onset of sensory analgesia up to T10 was 6.8 +/- 2.8 min vs. 8.7 +/- 2.7 min and time to reach maximum motor block was 19.8 +/- 5.8 min vs. 23.9 +/- 4.9 min in Group RD and Group RF respectively, which was significantly less in the Group RD. Postoperative analgesia was significantly prolonged in the Group RF as compared to Group RD, e.g. 394.5 +/- 36.5 vs. 268.5 +/- 28.3 min respectively. Sedation scores were better in the Group RD and highly significant on statistical comparison [P < 0.001]. Incidence of hypotension, nausea and vomiting was high in the Group RF, while incidence of dry mouth was higher in the Group RD

Conclusion: Dexmedetomidine is a better adjuvant than fentanyl when added to epidural ropivacaine in terms of early onset of sensory and motor block, prolonged postoperative analgesia and better sedation with less side effects

Adult , Female , Humans , Male , Middle Aged , Young Adult , Fentanyl/therapeutic use , Amides/therapeutic use , Adjuvants, Anesthesia , Anesthesia, Epidural , Nephrolithotomy, Percutaneous
Mycobiology ; : 73-83, 2017.
Article in English | WPRIM | ID: wpr-729884


The ability of dead cells of endophytic Drechslera hawaiiensis of Morus alba L. grown in heavy metals habitats for bioremoval of cadmium (Cd²⁺), copper (Cu²⁺), and lead (Pb²⁺) in aqueous solution was evaluated under different conditions. Whereas the highest extent of Cd²⁺ and Cu²⁺ removal and uptake occurred at pH 8 as well as Pb²⁺ occurred at neutral pH (6–7) after equilibrium time 10 min. Initial concentration 30 mg/L of Cd²⁺ for 10 min contact time and 50 to 90 mg/L of Pb²⁺ and Cu²⁺ supported the highest biosorption after optimal contact time of 30 min achieved with biomass dose equal to 5 mg of dried died biomass of D. hawaiiensis. The maximum removal of Cd²⁺, Cu²⁺, and Pb²⁺ equal to 100%, 100%, and 99.6% with uptake capacity estimated to be 0.28, 2.33, and 9.63 mg/g from real industrial wastewater, respectively were achieved within 3 hr contact time at pH 7.0, 7.0, and 6.0, respectively by using the dead biomass of D. hawaiiensis compared to 94.7%, 98%, and 99.26% removal with uptake equal to 0.264, 2.3, and 9.58 mg/g of Cd²⁺, Cu²⁺, and Pb²⁺, respectively with the living cells of the strain under the same conditions. The biosorbent was analyzed by Fourier Transformer Infrared Spectroscopy (FT-IR) analysis to identify the various functional groups contributing in the sorption process. From FT-IR spectra analysis, hydroxyl and amides were the major functional groups contributed in biosorption process. It was concluded that endophytic D. hawaiiensis biomass can be used potentially as biosorbent for removing Cd²⁺, Cu²⁺, and Pb²⁺ in aqueous solutions.

Amides , Biomass , Cadmium , Copper , Ecosystem , Fourier Analysis , Hydrogen-Ion Concentration , Metals, Heavy , Morus , Spectrum Analysis , Waste Water
Article in Chinese | WPRIM | ID: wpr-303876


<p><b>OBJECTIVE</b>To compare the postoperative analgesia efficacy, rehabilitation parameters and complication between multimodal analgesia and traditional analgesia after radical gastrectomy for gastric cancer patients.</p><p><b>METHODS</b>Patients with gastric cancer who underwent surgery in our hospital from October 2016 to December 2016 were enrolled in this prospective study. According to the non-randomized method, patients were assigned to multimodal analgesia group(n=32) and traditional analgesia group(n=33) in gastric cancer treatment team A and B in Department of Gastrointestinal Surgery, West China Hospital, Sichuan University. The treatment measures of group A were as follows: (1) The ratio of 1/1 diluted ropivacaine (100 mg, 10 ml) was infiltrated around the incision before abdomen closure, with incision sutured layer by layer. (2) Parecoxib sodium (40 mg) was injected intravenously every 12 hours after operation for 5 days. (3) Oxycodone-acetaminophen tablet was given orally on the first day or the second day after operation, 50 mg twice a day. (4) Patient-controlled analgesia was not used after operation. Patients in group B received direct suture of incision and patient-controlled analgesia. The pain score, postoperative rehabilitation and 30-day postoperative complications were collected and analyzed.</p><p><b>RESULTS</b>Multimodal analgesia group had lower pain scores at 1 d (4.8±0.9), 2 d (4.3±1.0), 3 d (2.9±0.8), 4 d (2.4±0.7) and 5 d (1.7±0.7) after surgery, as compared to traditional analgesia group (5.9±0.9, P=0.000), (5.1±0.7, P=0.001), (3.9±0.8, P=0.000), (3.0±0.6, P=0.000), (2.6±0.7, P=0.000), with significant difference. Postoperative hospital stay [(8.2±1.6) days vs. (10.6±2.2) days, P=0.000], time to ambulation [(47.5±13.8) days vs. (66.2±16.8) days, P=0.000], time to first flatus [(76.4±25.2) days vs. (120.0±29.9) days, P=0.000], time to first defecate [(117.3±42.2) days vs. (159.7±30.7) days, P=0.000] and time to first fluid diet [(83.8±21.6) days vs. (141.9±33.9) days, P=0.000] in the multimodal analgesia group were significantly shorter than those in the traditional analgesia group. There was no significant difference between the two groups with respect to 30-day postoperative complication rate(9.4% vs. 9.1%, P=1.000).</p><p><b>CONCLUSIONS</b>Multimodal analgesia can significantly reduce the postoperative pain and is beneficial to rehabilitation, meanwhile it does not increase the risk of postoperative complications. Multimodal analgesia is safe and effective for gastric cancer patients undergoing radical gastrectomy.</p>

Acetaminophen , Therapeutic Uses , Amides , Therapeutic Uses , Analgesia, Patient-Controlled , China , Comparative Effectiveness Research , Defecation , Drug Combinations , Eating , Flatulence , Gastrectomy , Rehabilitation , Humans , Isoxazoles , Therapeutic Uses , Length of Stay , Oxycodone , Therapeutic Uses , Pain Management , Methods , Pain, Postoperative , Drug Therapy , Postoperative Complications , Prospective Studies , Recovery of Function , Stomach Neoplasms , General Surgery , Surgical Wound , Rehabilitation , Therapeutics , Suture Techniques , Treatment Outcome , Walking
Int. j. morphol ; 34(4): 1191-1196, Dec. 2016. ilus
Article in Spanish | LILACS | ID: biblio-840865


La acción antiangiogénica de los inhibidores del receptor de angiotensina II (ARA II), ha sido documentada previamente, sin embargo, no ha sido descrita la relación entre angiogénesis e inhibidores directos de la renina (DRIs), los cuales participan regulando el sistema renina-angiotensina-aldosterona (SRAA). El objetivo fue demostrar el efecto antiangiogénico de aliskireno, un DRI, en membranas alantocoriónicas (MAC) de pollo, para lo cual fueron instilados aliskireno y enalapril sobre MAC en distintas concentraciones para realizar su comparación posterior. En secciones histológicas seriadas se registró el número de vasos sanguíneos presentes en 9000 µm2 bajo microscopio de luz a máximo aumento, y se realizó análisis estadístico utilizando ANOVA y el test de Tukey para demostrar posibles diferencias. Los receptores tratados con aliskireno, en ambas concentraciones utilizadas, presentaron menor densidad vascular, en comparación con los controles, siendo ésta estadísticamente significativa a mayor concentración. Aliskireno en concentraciones altas tiene un efecto antiangiogénico en un modelo experimental de MAC. Este hallazgo plantea la necesidad de estudios posteriores, dada la proyección que podría tener el uso inhibidores directos de la renina. A partir de estos resultados, se podría pensar en la factibilidad del uso de aliskireno para la modulación de la angiogénesis en diversas enfermedades crónicas no transmisibles.

Angiogenesis is the formation of new blood vessels from pre-existing ones. Antiangiogenic effect of angiotensin receptor blockers has been reported, however, the relationship between direct renin inhibitors and angiogenesis has not been well described. To assess the antiangiogenic effect of aliskiren, a direct renin inhibitor, on chick embryo chorioallantoic membrane (CAM) assay. Aliskiren and enalapril were instilled in different concentrations and compared. In serial histological sections, the number of blood vessels per 9000 µm2 area under observation through optical microscope using maximum zoom, was registered. Statistical analysis using Anova and Tukey test in order to show possible differences, was performed. Receptors treated with aliskiren presented lower vascular density, which was statistically significant when a higher concentration was administered. High concentrations of aliskiren have an antiangiogenic effect on CAM assay. This finding means further studies are needed, because of the usefulness direct renin inhibitors could have. These results, also, might enhance the possibility of using aliskiren for regulating angiogenesis in the context of non-transmissible chronic diseases.

Animals , Amides/pharmacology , Chorioallantoic Membrane/drug effects , Fumarates/pharmacology , Neovascularization, Physiologic/drug effects , Analysis of Variance , Chick Embryo , Enalapril/pharmacology , Models, Animal , Renin/antagonists & inhibitors
Rev. bras. anestesiol ; 66(6): 603-612, Nov.-Dec. 2016. graf
Article in English | LILACS | ID: biblio-829719


Abstract Background and objectives: To evaluate the thermographic predictive value of local anesthetic poisoning in rats that indicates the early recognition of thermal signs of intoxication and enable the immediate start of advanced life support. Methods: Wistar rats underwent intraperitoneal injection of saline and ropivacaine; they were allocated into pairs, and experiments performed at baseline and experimental times. For thermography, central and peripheral compartment were analyzed, checking the maximum and average differences of temperatures between groups. Thermographic and clinical observations were performed for each experiment, and the times in which the signs of intoxication occurred were recorded. In the thermal analysis, the thermograms corresponding to the times of interest were sought and relevant data sheets extracted for statistical analysis. Results: Basal and experimental: the display of the thermal images at times was possible. It was possible to calculate the heat transfer rate in all cases. At baseline it was possible to see the physiology of microcirculation, characterized by thermal distribution in the craniocaudal direction. It was possible to visualize the pathophysiological changes or thermal dysautonomias caused by intoxication before clinical signs occur, characterized by areas of hyper-radiation, translating autonomic nervous system pathophysiological disorders. In animals poisoned by ropivacaine, there was no statistically significant difference in heat transfer rate at the experimental time. Conclusions: The maximum temperature, medium temperature, and heat transfer rate were different from the statistical point of view between groups at the experimental time, thus confirming the systemic thermographic predictive value.

Resumo Justificativa e objetivos: Estudar o valor preditivo termográfico na intoxicação por anestésico local em ratos que efetue o reconhecimento precoce dos sinais térmicos de intoxicação e possibilite o início imediato do suporte avançado de vida. Método: Ratos Wistar foram submetidos à injeção intraperitoneal de soro fisiológico e ropivacaína, alocados aos pares, e foram feitos experimentos em tempos basal e experimental. Para o estudo termodinâmico foram analisados o compartimento central e o periférico, verificaram-se as diferenças das temperaturas máximas e médias entre os grupos. Foram feitas observações clínicas e termográficas para cada experimento e anotados os tempos em que os sinais de intoxicação ocorriam. Foram buscados na análise termográfica os termogramas correspondentes aos tempos de interesse e extraídas as planilhas de dados correspondentes, para análise estatística. Resultados: Foi possível a visibilização das imagens térmicas nos momentos basal e experimental. Foi possível calcular a taxa de transferência de calor em todos os casos. No momento basal foi possível observar a fisiologia da microcirculação, caracterizada por distribuição térmica no sentido craniocaudal. Foi possível visibilizar as alterações fisiopatológicas ou disautonomias térmicas causadas pela intoxicação antes que os sinais clínicos ocorressem, caracterizadas por áreas de hiperradiação e traduziram perturbações fisiopatológicas do Sistema Nervoso Autônomo. Nos animais intoxicados por ropivacaína houve diferença estatisticamente significativa na taxa de transferência de calor no momento experimental. Conclusões: Constatou-se que a temperatura máxima, a temperatura média e a taxa de transferência de calor foram diferentes do ponto de vista estatístico entre os grupos no momento experimental, o que corrobora o valor preditivo termográfico sistêmico.

Animals , Male , Rats , Poisoning/diagnostic imaging , Anesthetics, Local/poisoning , Thermography , Rats, Wistar , Ropivacaine , Amides/poisoning , Infrared Rays
Rev. bras. anestesiol ; 66(6): 594-602, Nov.-Dec. 2016. graf
Article in English | LILACS | ID: biblio-829706


Abstract Background: Local anesthetics (LAs) are generally considered as safe, but cytotoxicity has been reported for several local anesthetics used in humans, which is not well investigated. In the present study, the cytotoxicity of lidocaine, ropivacaine and the combination of lidocaine and ropivacaine were evaluated on human melanoma cell lines. Melphalan, a nitrogen mustard alkylating agent, was used as a control agent for comparison of cytotoxic activity. Methods: Melanoma cell lines, A375 and Hs294T, were exposed to 1 h to different concentrations of above agents. Cell-viability after exposure was determined by flow cytometry. Results: Investigated LAs showed detrimental cytotoxicity on studied melanoma cell lines in time- (p < 0.001), concentration- (p < 0.001), and agent dependant. In both A375 and Hs294T cell lines, minimum cell viability rates were found after 72 h of exposure to these agents. Lidocaine 2% caused a reduction of vital cells to 10% ± 2% and 14% ± 2% in A375 and Hs294T, respectively after 72 h of exposure. Ropivacaine 0.75% after 72 h reduced viable cells to 15% ± 3% and 25% ± 3% in A375 and Hs294T, respectively. Minimum cell viability after 72 h exposure to the combination was 10% ± 2% and 18% ± 2% in A375 and Hs294T, respectively. Minimum cell viability after 72 h exposure to melphalan was 8% ± 1% and 12% ± 2%, in A375 and Hs294T, respectively. Conclusion: LAs have cytotoxic activity on human melanoma cell lines in a time-, concentration- and agent-dependant manner. Apoptosis in the cell lines was mediated through activity of caspases-3 and caspases-8.

Resumo Justificativa: Os anestésicos locais (ALs) são geralmente considerados como seguros, mas citotoxicidade foi relatada em vários anestésicos locais usados em seres humanos, a qual não é bem investigada. No presente estudo, a citotoxicidade de lidocaína e ropivacaína e da combinação de lidocaína e ropivacaína foi avaliada em linhagens celulares de melanoma humano. Melfalano, um agente alquilante de mostarda nitrogenada, foi usado como um agente de controle para a comparação da atividade citotóxica. Métodos: Linhagens celulares de melanoma, A375 e Hs294T foram expostas por uma hora a concentrações diferentes dos agentes mencionados acima. A viabilidade celular após a exposição foi determinada por citometria de fluxo. Resultados: Os ALs investigados mostraram citotoxicidade prejudicial nas linhagens celulares de melanoma estudadas dependente do tempo (p < 0,001), da concentração (p < 0,001) e do agente. Em ambas as linhagens de células A375 e Hs294T, níveis mínimos de viabilidade celular foram encontrados após 72 horas de exposição a esses agentes. Lidocaína a 2% provocou uma redução das células vitais para 10% ± 2% e 14% ± 2% em A375 e Hs294T, respectivamente, após 72 horas de exposição. Ropivacaína a 0,75% após 72 horas reduziu as células viáveis para 15% ± 3% e 25% ± 3%, em A375 e Hs294T, respectivamente. A viabilidade celular mínima após exposição de 72 horas para a combinação foi de 10% ± 2% e 18% ± 2% em A375 e Hs294T, respectivamente. A viabilidade celular mínima após exposição de 72 horas ao melfalano foi de 8% ± 1% e 12 ± 2, em A375 e Hs294T, respectivamente. Conclusão: Os ALs têm atividade citotóxica em linhagens de celulares de melanoma humano de modo dependente do tempo, da concentração e do agente. A apoptose nas linhagens celulares foi mediada por meio da atividade das caspases-3 e caspases-8.

Humans , Cell Survival/drug effects , Amides/toxicity , Anesthetics, Local/toxicity , Lidocaine/toxicity , Apoptosis/drug effects , Caspases/metabolism , Cell Line, Tumor , Dose-Response Relationship, Drug , Flow Cytometry , Ropivacaine
Rev. bras. anestesiol ; 66(4): 341-345, tab, graf
Article in English | LILACS | ID: lil-787625


Abstract Background and objectives: A high sodium concentration is known to antagonize local anesthetics when infiltrated around neural tissue. Thus, we hypothesized that the onset time for sensory and motor blockade, in supraclavicular brachial plexus block using ropivacaine diluted with dextrose would be shorter than with saline. Methods: Patients scheduled for upper limb surgery were randomized to receive ultrasound guided supraclavicular brachial plexus block with 0.5% ropivacaine. Evaluation of sensory and motor blockade was performed every 5 min for 60 min. Patients were followed-up on postoperative day 1, and between days 7 and 10 for the presence of any complications. Twenty-five patients in each group were analyzed. Results: Mean time for onset of analgesia for the dextrose group was 37.6 ± 12.9 min while the mean time for the saline group was 45.2 ± 13.9 min with a p-value of 0.05. The effect size was 0.567, which was moderate to large. No major complications were observed. Conclusion: We conclude that there was a decrease in onset time of analgesia when dextrose was used as a diluent instead of saline for ultrasound guided supraclavicular block.

Resumo Justificativa e objetivos: A alta concentração de sódio é conhecida por antagonizar anestésicos locais quando infiltrado em torno de tecido neural. Portanto, a nossa hipótese foi a de que o tempo de início para os bloqueios sensorial e motor, em bloqueio do plexo braquial supraclavicular com ropivacaína diluída com dextrose, seria menor do que com solução salina. Métodos: Os pacientes agendados para cirurgia em membro superior foram randomizados para receber bloqueio do plexo braquial supraclavicular com ropivacaína a 0,5%g guiado por ultrassom. A avaliação dos bloqueios sensorial e motor foi feita a cada cinco minutos durante 60 minutos. Os pacientes foram acompanhados no pós-operatório no primeiro dia e entre os dias 7-10 para presença de qualquer complicação. Foram analisados 25 pacientes em cada grupo. Resultados: A média do tempo para o início da analgesia no grupo dextrose foi de 37,6 ± 12,9 minutos, enquanto que no grupo solução salina foi de 45,2 ± 13,9 minutos, com um valor-p de 0,05. O tamanho do efeito foi 0,567, o que foi de moderado a grande. Complicações maiores não foram observadas. Conclusão: Concluímos que houve uma redução do tempo de início da analgesia quando dextrose em vez de solução salina foi usada como diluente para bloqueio supraclavicular guiado por ultrassom.

Humans , Male , Female , Adolescent , Adult , Aged , Aged, 80 and over , Young Adult , Brachial Plexus Block/methods , Amides/therapeutic use , Glucose/administration & dosage , Anesthetics, Local/therapeutic use , Time Factors , Sodium Chloride/administration & dosage , Single-Blind Method , Follow-Up Studies , Ropivacaine , Middle Aged
Rev. bras. anestesiol ; 66(4): 335-340, tab, graf
Article in English | LILACS | ID: lil-787614


Abstract Background and objectives: Arthroscopy for shoulder disorders is associated with severe and difficult to control pain, postoperatively. The addition of clonidine to local anesthetics for peripheral nerve block has become increasingly common, thanks to the potential ability of this drug to reduce the mass of local anesthetic required and to prolonging analgesia postoperatively. The present study aimed to evaluate the success of brachial plexus block for arthroscopic rotator cuff surgery using local anesthetic with or without clonidine. Method: 53 patients of both genders, between 18 and 70 years old, American Society of Anesthesiologists I or II, who were scheduled to undergo arthroscopic shoulder surgery were selected. Patients were then randomized into two groups. The verbal numerical pain scale and the presence of motor block were obtained in the post-anesthetic recovery room and 6, 12, 18 and 24 h postoperatively. Results: The association of clonidine (0.15 mg) to a solution of 0.33% ropivacaine (30 mL) in brachial plexus block for shoulder arthroscopy has not diminished the visual numeric pain scale values, nor the need for opioid rescue postoperatively. There was a lower incidence of nausea/vomiting postoperatively and a significant motor block time prolongation in the group of patients who received clonidine as adjuvant. Conclusions: The use of brachial plexus block with local anesthetic for analgesic postoperative control is well established in the literature. The addition of clonidine in the dose proposed for prolongation of the analgesic effect and reduction of opioid rescue proved unhelpful.

Resumo Justificativa e objetivos: A artroscopia para afecções do ombro associa-se a dor de forte intensidade no pós-operatório, de difícil manejo. A adição de clonidina ao anestésico local em bloqueios periféricos tornou-se progressivamente maior graças à potencial habilidade dessa droga em reduzir a massa de anestésicos locais necessários e prolongar a analgesia no pós-operatório. O presente estudo teve como objetivo avaliar o sucesso do bloqueio de plexo braquial para a cirurgia artroscópica de manguito rotador com o uso de anestésico local associado ou não à clonidina. Método: Foram selecionados 53 pacientes de ambos os sexos, entre 18 e 70 anos, ASA I ou II, que seriam submetidos à cirurgia de ombro por artroscopia. Os pacientes foram então randomizados em dois grupos. A escala numérica verbal de dor e a presença de bloqueio motor eram obtidas na sala de recuperação pós-anestésica (SRPA) e com seis, 12, 18 e 24 horas de pós-operatório. Resultados: A associação de clonidina (0,15 mg) à solução de ropivacaína 0,33% (30 mL) no bloqueio de plexo braquial para artroscopia de ombro não diminuiu os valores da escala visual numérica de dor, nem a necessidade de resgate com opioides no pós-operatório. Houve uma menor incidência de náuseas e vômitos no pós-operatório (NVPO) e aumento considerável do tempo de bloqueio motor no grupo de pacientes que recebeu clonidina como adjuvante. Conclusões: O uso do bloqueio de plexo braquial com anestésico local para controle analgésico pós-operatório está consolidado na literatura. A adição de clonidina na dose proposta para prolongamento do efeito analgésico e redução de resgate com opioides mostrou-se pouco útil.

Humans , Male , Female , Adolescent , Adult , Aged , Young Adult , Pain, Postoperative/drug therapy , Arthroscopy/methods , Shoulder Joint/surgery , Clonidine/therapeutic use , Brachial Plexus Block/methods , Amides/therapeutic use , Rotator Cuff/surgery , Drug Therapy, Combination/methods , Ropivacaine , Analgesics/therapeutic use , Anesthetics, Local/therapeutic use , Length of Stay/statistics & numerical data , Middle Aged
Rev. bras. anestesiol ; 66(1): 29-36, Jan.-Feb. 2016. graf
Article in Portuguese | LILACS | ID: lil-773481


BACKGROUND: Intra-articular injections of local anesthetics are commonly used to enhance post-operative analgesia following orthopedic surgery as arthroscopic surgeries. Nevertheless, recent reports of severe complications due to the use of intra-articular local anesthetic have raised concerns. OBJECTIVES: The study aims to assess use of vitamin C in reducing adverse effects of the most commonly employed anesthetics - ropivacaine, bupivacaine and lidocaine - on human chondrocytes. METHODS: The chondrocyte viability following exposure to 0.5% bupivacaine or 0.75% ropivacaine or 1.0% lidocaine and/or vitamin C at doses 125, 250 and 500 µM was determined by LIVE/DEAD assay and annexin V staining. Expression levels of caspases 3 and 9 were assessed using antibodies by Western blotting. Flow cytometry was performed to analyze the generation of reactive oxygen species. RESULTS: On exposure to the local anesthetics, chondrotoxicity was found in the order ropivacaine < bupivacaine < lidocaine. Vitamin C effectively improved the reduced chondrocyte viability and decreased the raised apoptosis levels following exposure to anesthesia. At higher doses, vitamin C was found efficient in reducing the generation of reactive oxygen species and as well down-regulate the expressions of caspases 3 and 9. CONCLUSIONS: Vitamin C was observed to effectively protect chondrocytes against the toxic insult of local anesthetics ropivacaine, bupivacaine and lidocaine.

JUSTIFICATIVA: Injeções de anestésicos locais por via intra-articular são comumente usadas para melhorar a analgesia no período pós-operatório de cirurgia ortopédica como artroscopia. No entanto, relatos recentes de complicações graves devido ao uso de anestésico local por via intra-articular causou preocupações. OBJETIVOS: O objetivo do estudo foi avaliar o uso de vitamina C para reduzir os efeitos adversos dos anestésicos mais comumente usados (ropivocaína, bupivacaína e lidocaína) sobre condrócitos humanos. MÉTODOS: A viabilidade dos condrócitos após a exposição à bupivacaína a 0,5% ou ropivacaína a 0,75% ou lidocaína a 1,0% e/ou vitamina C em doses de 125, 250 e 500 µM foi determinada pelo ensaio Vivo/Morto e coloração com anexina V. Os níveis de expressão das caspases 3 e 9 foram avaliados com o uso de anticorpos pela técnica Western blotting. Citometria de fluxo foi feita para analisar a geração de espécies reativas ao oxigênio. RESULTADOS: Na exposição aos anestésicos locais, condrotoxicidade foi encontrada na seguinte ordem: ropivacaína < bupivacaína < lidocaína. A vitamina C efetivamente melhorou a redução da viabilidade dos condrócitos e diminuiu os níveis elevados de apoptose após a exposição à anestesia. Em doses mais altas, a vitamina C foi eficiente para reduzir a geração de espécies reativas ao oxigênio e assim regular negativamente a expressão das caspases 3 e 9. CONCLUSÕES: Observamos que a vitamina C foi eficaz na proteção dos condrócitos contra a agressão tóxica dos anestésicos locais ropivacaína, bupivacaína e lidocaína.

Humans , Ascorbic Acid/pharmacology , Reactive Oxygen Species/metabolism , Chondrocytes/drug effects , Anesthetics, Local/toxicity , Ascorbic Acid/administration & dosage , Bupivacaine/toxicity , Down-Regulation/drug effects , Cells, Cultured , Apoptosis/drug effects , Chondrocytes/pathology , Dose-Response Relationship, Drug , Caspase 3/genetics , Caspase 9/genetics , Flow Cytometry , Ropivacaine , Amides/toxicity , Lidocaine/toxicity , Antioxidants/administration & dosage , Antioxidants/pharmacology