Made available in DSpace on 2014-06-12T22:56:53Z (GMT). No. of bitstreams: 2 arquivo3997_1.pdf: 6103896 bytes, checksum: 87a0c6ec2df89ef5617003ab039ab96f (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2008 / A Dioclea grandiflora é conhecida popularmente como mucunã , mucunãde- caroço e olho-de-boi e encontra-se no Brasil, distribuída nas regiões da caatinga e do cerrado. Este trabalho, através de um estudo experimental, objetivou identificar um possível efeito analgésico central dos extratos hidroalcoólico e aquoso da casca do caule da Dioclea grandiflora administrados por via intraperitonial em camundongos, nas doses de 30, 60 e 120 mg/kg, além do efeito de tolerância na dose de 30 mg/kg, através do tratamento crônico por 21 dias consecutivos. Foram utilizados os testes da placa quente, da imersão da cauda e das contorções abdominais induzidas pelo ácido acético. Nos resultados dos tratamentos agudos, observou-se um efeito antinoceptivo significante (p<0.05). Efeito este inibido pela naloxona, antagonista morfinomimético específico do receptor opióide. Enquanto que, no teste da imersão da cauda, no tratamento crônico, apenas o extrato hidroalcoólico, na dose de 30 mg/kg apresentou tolerância. Conclui-se que os extratos hidroalcoólico e aquoso apresentam ação analgésica central e apenas o hidroalcoólico apresenta tolerância, quando administrado cronicamente, que é típico dos opióides

Exposure to abnormal motion produces a variety of behavioural effects in both human and non-human species. The general purpose of the present studies was to produce and investigate some of these effects in the laboratory rat. In the first series of experiments, rats displayed appreciable decreases in reactivity to noxious stimuli presented after exposure to brief periods of different types of motion. This motion-induced antinociception was found to persist for periods of up to 15 min. A second series of experiments examined the role of the vestibular system in this motion-induced antinociception phenomenon. Rats whose peripheral vestibular apparatus had been rendered insensitive to accelerative stimuli did not exhibit motion-induced antinociception. Subsequent experiments attempted to delineate the role of some individual components of the central vestibular system but no single component investigated was found to play a major role in the production of antinociception. Experiments in this and the preceding series of experiments also demonstrated that the antinociceptive effect could be dissociated from dizziness or acute vestibular dysfunction. In the third series of experiments, the physiological mechanisms by which vestibular stimulation produces antinociception were investigated. Experiments in this series demonstrated that motion-induced antinociception could be blocked by opiate antagonists and that the motion-induced antinociceptive effect showed cross-tolerance with chronic morphine administration. These two findings strongly implicate an endogenous opiate peptide (endorphin) system as the underlying mechanism for mot ion-induced antinociception. The brief duration of the antinociceptive effect and the fact that disruption of the pituitary-adrenal axis did not affect motion-induced antinociception suggested that the opiate peptides involved were the enkephalins rather than B-endorphin. Other behavioural effects of abnormal motion were reported in the the fourth series of experiments. The resemblance between the symptoms of motion sickness and those of opiate administration suggested that endogenous opiate peptides may mediate motion sickness. Although exposure to abnormal motion did produce a substantial conditioned taste aversion (a behavioural assay for motion sickness in the rat), attempts to attenuate the aversion with two different opiate antagonists were unsuccessful. These results suggested that abnormal motion exerts its illness-producing effects through some mechanism other than an endogenous opiate system. In the final experiment, rats that were exposed to a brief period of abnormal motion subsequently exhibited a suppression of defensive burying behaviour that was similar to that produced by anxiolytic drugs. The results of this study indicate that abnormal vestibular stimulation may have a variety of different behavioural effects in rats. However, it appears that no single mechanism can account for all of these effects. / Arts, Faculty of / Psychology, Department of / Graduate

This study was designed to describe the use of analgesics ordered pro re nata (PRN) in the management of acute post-operative pain. Specifically, the study purpose was to answer the following questions. What amounts and frequencies of analgesic are ordered PRN by physicians for patients in the first 48 hours following a cholecystectomy? What amounts and frequencies of analgesic are given by nurses to patients in the first 48 hours following a cholecystectomy? What is the patient's summational description of his/her pain at 24 and 48 hours following a cholecystectomy? A descriptive survey design was used. A convenience sample of 22 subjects participated in the study. These subjects met the study criteria and were scheduled for elective cholecystectomy at one of the two hospitals used. Data were gathered by auditing the charts for information pertinent to the prescriptions and administration of the analgesics and by interviewing the subjects. There was considerable variability in the amounts and frequencies of analgesics prescribed and in those given to the post-operative subjects. No routine patterns were identified. There was a significant difference in the amounts of analgesics prescribed and given between the two hospitals, the reasons for which were not explored. The decision to use the PRN-prescribed analgesics appeared to be made by the nurses but evidence of accountability taken by nurses for their role in assessing pain and evaluating the effectiveness of the analgesics was not reflected in the reviewed records. Analgesics for use in the Post-Anaesthetic Recovery Room in the immediate post-operative period were prescribed by the anaesthetists. All initial analgesics were given by the intravenous route in this setting. Subjects at Hospital B were prescribed and received considerably more analgesics (83%) than those at Hospital A. Analgesics for use on the ward were prescribed by the surgeons. All orders were for meperidine hydrochloride to be given PRN and all orders were unchanged for the 48-hour period studied. The amount of meperidine prescribed and given per intramuscular dose was usually within the 75 to 100 milligrams optimal dosage range for the drug. The meperidine was usually prescribed with a four hour interval between doses. Doses of meperidine were given with considerably longer intervals between doses than the duration of action of the drug. For the 48-hour period, the mean total amount prescribed, based on the maximum possible dosage was 1154 milligrams. The median total amount prescribed was 1050 milligrams. The mean total amount given was 625 milligrams or 54% of the prescribed amount and the median total amount given was 587 milligrams or 56% of the prescribed amount. Subjects on the ward at Hospital A were prescribed and given significantly more meperidine than those at Hospital B. The patients' summational descriptions of their pain emphasized the individuality of the pain experience. The physical sensations described were consistent with previous literature descriptions of postoperative pain. The subjective data collected reflected the difficulties and complexities of pain management. An often-stated assumption in the literature is that nurses use PRN-prescribed analgesics inappropriately in managing post-operative pain; that is, patients are uncomfortable because the analgesics are not given in adequate amounts or frequently enough. In this study, a relationship was not identified between the amounts of meperidine received by subjects and how they reported their post-operative pain. This finding suggests that the assumption, that increasing the analgesics used would increase patient comfort, requires further investigation. Based on the findings of this study, implications for postoperative pain management and nursing practice, and suggestions for further research were made. / Applied Science, Faculty of / Nursing, School of / Graduate

Orientador: Eneida de Paula / Dissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Biologia / Made available in DSpace on 2018-07-31T21:50:48Z (GMT). No. of bitstreams: 1 Araujo_DanieleRibeirode_M.pdf: 5040962 bytes, checksum: a792ef89e3934d5414e2de392da2a716 (MD5) Previous issue date: 2002 / Resumo: Entre as várias classes de fármacos utilizados no tratamento da dor encontram-se os anestésicos locais (AL). Com a finalidade de prolongar a duração de ação e reduzir a toxicidade sistêmica desses fármacos, pesquisas têm sido desenvolvidas utilizando diferentes carreadores como lipossomas e ciclodextrinas que possibilitam a liberação controlada (prolongando o efeito anestésico) e evitam picos plasmáticos das drogas (reduzindo a toxicidade). Assim, este trabalho teve por finalidades preparar, caracterizar e avaliar in vivo a eficácia de formulações contendo os AL bupivacaína (aVC) e mepivacaína (MVC) encapsulados em lipossomas ou complexados com ciclodextrinas para, posteriormente, compará-Ias com as preparações disponíveis na clínica. Análises do diâmetro médio dos lipossomas revelaram a presença de duas populações de vesículas distintas (400 nm e 150 nm) sendo observada uma maior percentagem de encapsulação para ave do que para MVC. Com relação aos sistemas de AL em ciclodextrinas, foram observadas diferenças nas temperaturas de transição de fases e na morfologia dos cristais dos compostos puros (AL e ciclodextrinas) evidenciando a complexação. A avaliação do bloqueio motor em camundongos mostrou que os AL livres, as formulações lipossomais e as complexadas induziram um aumento dose - dependente na intensidade e na duração do mesmo. Porém, esses parâmetros não foram alterados quando comparou-se as preparações entre si, nas mesmas concentrações. Também, os efeitos antinociceptivos sistêmicos foram similares para todas as formulações testadas. Já a potência e a duração do bloqueio sensorial foram aumentadas pela complexação de BVC com ciclodextrinas e pela encapsulação de MVC em lipossomas, em relação às drogas livres (p < 0,001). Esses resultados podem ser explicados pela liberação controlada das drogas e pelo aumento da disponibilidade das mesmas no sítio de injeção. A encapsulação de MVC em lipossomas possibilitou o transporte da fração da droga disponível no interior da bicamada lipídica e a complexação de avc com ciclodextrinas aumentou a quantidade de droga solubilizada (na fase aquosa) conferindo-Ihes maior potência anestésica em relação às preparações comerciais. Desta forma, as formulações de MVC em lipossomas e BVC em ciclodextrinas apresentam-se como novas alternativas no tratamento da dor aguda e crônica / Abstract: Local anesthetics (LA) belong to the class of drugs used for the treatrnent of pain. In order to prolong the duration of action and to reduce their systemic toxicity of LA, many studies have been developed using carriers such as liposomes and cyclodextrins; these vehicles allow controlled release (improving anesthetic effect) and avoid high plasmatic levels of the anesthetics to be reached (reducing the toxicity). This work aimed to prepare, to characterize and to evaluate in vivo drug - delivery systems for bupivacaine (BVC) and mepivacaine (MVC) in liposomes or cyclodextrins, comparing them with the clinically used LA solutions. Mean size diameter analysis showed that the liposomes have diameters of 400 nm and 150 nm, with encapsulation efficiencies higher for BVC than MVC. Regarding to LA systems in cyclodextrins, differences on phase transition temperature and structural changes in the crystal's pattems evidenced LA : J3-CD complexation. Liposomal and ciclodextrin formulations increased the intensity and duration of the motor blockade showing dose-dependent relationships although these parameters did not change, if compared at the sarne concentrations. AIso the systemic antinociceptive effects were similar for ali the formulations tested. Potency and duration of sensory blockade were improved afier injection of complexed BVC and liposomal MVC in relation to the free drug injection (p < 0.001). These results can be explained by the controlled release of the LA and increased availability of the LA in their site of injection. Encapsulation of MVC in liposomes increased the amount of available drug for membrane partition while complexation into cyclodextrin increased BVC concentration in the aqueous phase, improving their anesthetic potency in relation to the commercial solutions and these LA. These drug-delivery systems offer a potential new therapeutic option for the treatments of acute and chronic pain using LA / Mestrado / Bioquimica / Mestre em Biologia Funcional e Molecular

Memoria para optar al título de Químico Farmacéutico

Despite the fact that many Nigerian women have limited access to pharmacologic methods for pain management during labor,1,2 previous studies have indicated a demand for such options.3–5 Opioids are a frequently offered analgesic method,5,6 but there are associated risks to the fetus with this type of pain management.7 The use of epidurals, another common method of labor analgesia, has not become prevalent in Nigeria due to lack of awareness, lack of resources, expense, and women’s beliefs that it is not necessary and/or it is harmful.3 Nitrous oxide is an alternative labor analgesic that has reduced side effects compared to opioids and offers pain reduction without the loss of body movement and positioning as is seen with epidurals.7 Because Nigerian women have expressed an interest in increased options for labor analgesics, and nitrous oxide aligns with some of their cultural desires,8 offering nitrous oxide could increase maternal satisfaction.9–12 The literature review examines epidurals, opioids, and nitrous oxide for use as labor analgesics, including their mechanisms of action, benefits, and side effects. It also reviews Nigerian cultural beliefs, the advantages and disadvantages of using nitrous oxide in Nigeria, current practice in Nigeria regarding labor analgesia, Nigerian women’s and healthcare providers opinions on analgesia, additional maternal advantages of labor analgesia outside of pain relief, and birthing locations in Nigeria. The study will be an exploratory, descriptive cross-sectional study that will use a questionnaire to obtain data regarding pregnant women’s knowledge of, and attitudes toward, nitrous oxide as an analgesic during childbirth. It will be administered to 270 pregnant women who visit an antenatal clinic at the Primary Health Care facilities in Mushin Local Government Area located in the state of Lagos, Nigeria. Descriptive statistics of the participants will be reported, and the chi-squared test will be used to determine the associations between the demographics and awareness of various analgesic options, cultural acceptability of using nitrous oxide for labor pain management, and the desirability to use nitrous oxide as a labor analgesic. The use of nitrous oxide for labor analgesia could provide Nigerian women with an important option apart from only opioids or epidurals. It could decrease the use of opioids, thus decreasing their associated health risks during labor.3 Additionally, because vaginal deliveries are an important cultural desire of Nigerian women, nitrous oxide could provide a method for pain management during labor that does not lead to increased risk of cesarean section.13,14

Background The lack of methadone pharmacokinetic data in children and neonates restrains dosing to achieve the target concentration in these populations. A minimum effective analgesic concentration of methadone in opioid naïve adults is 0.058 mg·l-1, while no withdrawal symptoms were observed in neonates suffering opioid withdrawal if plasma concentrations of methadone were above 0.06 mg·l-1. The racemate of methadone which is commonly used in pediatric and anesthetic care is metabolized to 2-ethylidine-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP) and 2-ethyl-5-methyl-3,3-diphenylpyrroline (EMDP). Methods Data from four studies (age 33-week PMA-15 years) were pooled (n = 56) for compartment analysis using nonlinear mixed effects modeling. Parameter estimates were standardized to a 70-kg person using an allometric model approach. Investigation was made of the racemate and metabolite (EDDP and EMDP) dispositions. In addition, neonatal data (n = 7) allowed further study of R- and S-enantiomer pharmacokinetics. Results A three-compartment linear disposition model best described the observed time-concentration profiles with additional compartments for metabolites. Population parameter estimates (between-subject variability) were central volume (V1) 21.5 (29%) l·70 kg-1, peripheral volumes of distribution V2 75.1 (23%) l·70 kg-1 and V3 484 (8%) l·70 kg -1, clearance (CL) 9.45 (11%)l·h-1·70 kg-1, and intercompartment clearances Q2 325 (21%) l·h -1·70 kg-1 and Q3 136 (14%) l·h -1·70 kg-1. EDDP formation clearance was 9.1 (11%) l·h-1·70 kg-1, formation clearance of EMDP from EDDP 7.4 (63%)l·h-1·70 kg-1, elimination clearance of EDDP was 40.9 (26%) l·h-1·70 kg-1 and the rate constant for intermediate compartments 2.17 (43%) h-1. Conclusions Current pharmacokinetic parameter estimates in children and neonates are similar to those reported in adults. There was no clearance maturation with age. Neonatal enantiomer clearances were similar to those described in adults. A regimen of 0.2 mg·kg-1 per 8 h in neonates achieves a target concentration of 0.06 mg·l-1 within 36 h. Infusion, rather than intermittent dosing, should be considered if this target is to be achieved in older children after cardiac surgery.

OBJETIVO: Describir el uso de sedantes, analgésicos y bloqueantes neuromusculares en infantes y niños críticamente enfermos en la Unidad de Cuidados Intensivos Pediátricos(PICU).MÉTODO: Estudio descriptivo, transversal y observacional realizado en niños críticamente enfermos de la PICU del Hospital E. Rebagliati Martins durante enero a diciembre del 2002. De un total de 249 infantes y niños hospitalizados en la PICU, se seleccionó una muestra representativa de 78 casos, de los cuales se revisó los datos de la historia clínica, sobre el registro de las características del uso de agentes sedantes, analgésicos y bloqueantes neuromusculares a corto plazo(menor de 6 horas), y largo plazo( mayor a 6 horas). RESULTADOS: El 62% fué de sexo masculino, 32% sexo femenino, con un promedio de edad de 5.3 años, +- 4.1 DS, 65% fueron de categoría quirúrgica; tuvieron un promedio de: Ventilación Mecanica de 2.7 dias, estancia en PICU de 6.3 dias, y Score de Glasgow de 9.8. Se usó el vecuronio en 5%, como agente bloqueante neuromuscular (NMBA) a corto plazo, la sedación y analgesia con midazolan(22%), metamizol(49%)y fentanilo(10%) respectivamente. La sedación, analgesia y relajación a largo plazo con midazolam(50%), fentanilo(50%) , metamizol(25%), y vecuronio(0.02%). Fueron usados simultáneamente midazolam y fentanilo en 23%, midazolam, fentanilo y metamizol en 5% de casos. No se encontró en ningun caso el registro de complicaciones y escalas de evaluación específicas, por el uso de estos agentes. CONCLUSIONES: La sedación y analgesia a corto plazo, es una práctica poco frecuente en la PICU del Hospital E. Rebagliatti Martins, asi mismo el bloqueo neuromuscular es casi inusual. Sin embargo la sedación y analgesia a largo plazo es de práctica relativamente frecuente(50%); no asi el bloqueo neuromuscular que es casi inusual. -- Palabras Claves: PICU: Unidad de Cuidados Intensivos Pediátricos, NMBA: agente de bloqueo neuromuscular; sedación, analgesia, relajación neuroromuscular, infantes, niños. / Tesis de segunda especialidad

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