Tetradenia riparia leaves, flower buds, and stem essential oils to control of Aedes aegypti larvae

Abstract Tetradenia riparia (Hochst.) Codd (Lamiaceae) is a species native to the African continent and used as an insect repellent. The objective of the study was to evaluate the larvicidal potential of essential oils (EOs) from the leaves, flower buds, and stem of T. riparia, collected in winter against Aedes aegypti larvae. The EOs were extracted by hydrodistillation (3 h) and identified by GC/MS. The EOs were tested against larvae of A. aegypti at concentrations ranging from 12500 to 1.5 µg/mL for 24 h. The insecticide activity was evaluated by probit analysis, and the anticholinesterase activity was determined by bioautographic method. The results of the class projection indicated sesquiterpenes as the majority class, corresponding to 60.66% (leaves), 64.70% (flower buds) and 83.99% (stem), and the bioassays on A. aegypti larvae indicated LC50 of 1590, 675 and 665 µg/mL, respectively. The anticholinesterase activity indicated that the EO of the leaves inhibited the enzyme at a concentration of 780 µg/mL, and those from the flower buds and stem inhibited up to 1560 µg/mL. The results indicated weak activity of essential oils against A. aegypti larvae.

Anticholinesterase activity of ß-carboline-1, 3, 5-triazine hybrids

Abstract The ß-carboline-1,3,5-triazine hydrochlorides 8-13 were evaluated in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The analysed compounds were selective to BuChE, with IC50 values in the range from 1.0-18.8 µM being obtained. The N-{2-[(4,6-dihydrazinyl-1,3,5-triazin-2-yl)amino]ethyl}-1-phenyl-ß-carboline-3-carboxamide (12) was the most potent compound and kinetic studies indicate that it acts as a competitive inhibitor of BuChE. Molecular docking studies show that 12 strongly interacts with the residues of His438 (residue of the catalytic triad) and Trp82 (residue of catalytic anionic site), confirming that this compound competes with the same binding site of the butyrylthiocholine

Síndrome miasténico congénito por deficiencia de rapsina: reporte de caso con nueva mutación y heterocigosidad compuesta / Congenital myasthenic syndrome due to rapsyn deficiency: A case report with a new mutation and compound heterozygosity

INTRODUCCIÓN Los síndromes miasténicos congénitos son un grupo heterogéneo de desórdenes genéticos, caracterizados por una transmisión sináptica anormal en la placa neuromuscular. REPORTE Presentamos el caso de un paciente de dos años, varón, con hipotonía, ptosis palpebral y debilidad simétrica y de predominio proximal, características que aparecieron desde el nacimiento y que motivaron varias hospitalizaciones por neumonía e insuficiencia ventilatoria. Desde el inicio de la deambulación a los dos años, los padres notaron que la debilidad empeoraba por las tardes y con la actividad física repetida o prolongada. El examen físico a los dos años mostró ptosis palpebral, debilidad de predominio proximal y fatigabilidad con el esfuerzo sostenido. La electro-miografía evidenció decremento del 27% en el potencial de acción muscular compuesto. El análisis de tríos mostró heterocigosis compuesta por transmisión de dos mutaciones diferentes en el gen de rapsina, una ya conocida procedente del padre y la otra no reportada previa-mente, procedente de la madre. El paciente recibió piridostigmina obteniendo mejoría inmediata y logrando un desempeño óptimo en actividades escolares, deportivas y de la vida cotidiana. A la fecha, no ha presentado nuevos episodios de insuficiencia ventilatoria. CONCLUSIONES La debilidad de inicio neonatal y la fatigabilidad o agotamiento con el esfuerzo sostenido, con afección principalmente de los músculos con inervación troncal y con un decremento mayor al 10% en el potencial de acción muscular compuesto en la electromiografía, deben hacer sospechar en un síndrome miasténico congénito. Se revisan los puntos clínicos clave que permiten establecer el diagnóstico oportuno y las opciones de tratamiento efectivo para algunos de estos síndromes.

INTRODUCTION The congenital myasthenic syndromes are a heterogeneous group of genetic disorders characterized by an abnormal synaptic transmission in the neuromuscular plate. REPORT We present a two-year-old patient, male, with hypotonia, palpebral ptosis, and proximal symmetric weakness with a neonatal onset that motivated several and prolonged hospitalizations for pneumonia and respiratory failure. From two years of age, the parents noticed that the facial and general weakness worsened in the afternoons and with repeated or prolonged physical activity. The physical examination showed palpebral ptosis, predominantly proximal weakness, and fatigability with sustained muscular effort. The electromyography showed a 27% decrement in the Compound Muscular Action Potential and the case-parents genetic study showed compound heterozygosity with the transmission of two different mutations in the rapsyn gene from both parents. The patient received pyridostigmine with great improvement, achieving optimal performance in school, sports, and daily life activities. CONCLUSIONS Weakness and fatigability with neonatal onset, mainly affecting the muscles with brain stem innervation and the decrement greater than 10 percent in the Compound Muscular Action Potential in the electromyographic studies, should make us suspect in a congenital myasthenic syndrome. We review the literature and key clinical points to establish a timely diagnosis and effective treatment in some of these syndromes.

Effects of galantamine and galantamine combined with nimodipine on cognitive speed and quality of life in mixed dementia: a 24-week, randomized, placebo-controlled exploratory trial (the REMIX study) / Efeitos da galantamina e da galantamina combinada à nimodipina sobre a velocidade de processamento cognitivo e qualidade de vida na demência mista: ensaio clínico exploratório, randomizado e controlado com placebo (estudo REMIX)

The effects of galantamine (GAL) on quality of life (QoL) and cognitive speed, as well its effects combined with nimodipine (NIM) in Alzheimer disease (AD) with cerebrovascular disease (mixed dementia), have not been explored. Method : Double-blind, placebo-controlled, multicenter Brazilian trial, studying the effects of GAL/NIM vs. GAL/placebo (PLA) in mild to moderate mixed dementia. Patients were randomized to receive GAL/NIM or GAL/PLA for 24 weeks. Primary efficacy measures were changes on a computerized neuropsychological battery (CNTB) and QoL Scale in Alzheimer's Disease (QoL-AD) from baseline to week 24. Results : Twenty-one patients received at least one drug dose (9 GAL/NIM and 12 GAL/PLA). Groups were matched for age, sex, education, cognitive and QoL scores at baseline. No significant differences were observed between groups on primary or secondary measures. QoL and cognitive performance showed significant improvement (p<0.05) from baseline when all GAL-treated patients were analyzed. Adverse events were predominantly mild to moderate. Conclusion : GAL treatment improved QoL in mixed dementia, in addition to its previously known cognitive benefits. The combination GAL/NIM was not advantageous. However, the small sample size precludes any definitive conclusions. Trial registered at ClinicalTrials.gov: NCT00814658 .

Os efeitos da galantamina (GAL) sobre qualidade de vida (QdV) e velocidade de processamento cognitivo, bem como da combinação com nimodipina (NIM) no tratamento da doença de Alzheimer (DA) com doença cerebrovascular (demência mista) ainda não foram investigados. Método : Estudo multicêntrico brasileiro, duplo-cego, controlado com placebo, avaliando os efeitos de GAL/NIM x GAL/placebo (PLA) na demência mista leve a moderada. Pacientes receberam tratamento com GAL/NIM ou GAL/PLA por 24 semanas. Medidas de eficácia primária foram as variações no desempenho em bateria de testes neuropsicológicos computadorizados e na escala QdV-DA ao final do estudo. Resultados : Vinte um pacientes receberam pelo menos uma dose da droga (9 GAL/NIM e 12 GAL/PLA). Os grupos foram emparelhados por idade, sexo, escolaridade, escores cognitivos e de QdV na linha de base. Não foram observadas diferenças significativas entre os dois grupos nas medidas de eficácia primária e secundária. Na avaliação de todos os pacientes que receberam GAL, houve melhora significativa (p<0,05) em QdV-DA e desempenho cognitivo. Os eventos adversos foram predominantemente leves a moderados. Conclusão : O tratamento com GAL proporcionou melhora da QdV na demência mista, além dos benefícios cognitivos previamente conhecidos. A combinação GAL/NIM não foi vantajosa. O reduzido tamanho amostral impede conclusões definitivas. .

Efectividad y seguridad de donepezilo, galantamina y memantina para el tratamiento de la Enfermedad de Alzheimer / Effectiveness and safety of donepezil, galantamine and memantine for the treatment of Alzheimer's disease

Antecedentes: Descripción de la condición de salud de interés: Las demencias son un grupo de trastornos del sistema nervioso central, caracterizados por alteración de la memoria, de las funciones ejecutivas, déficit cognitivo y cambios en la personalidad. La Enfermedad de Alzheimer es un tipo de demencia de inicio insidioso y progresión lenta, que compromete la memoria, el lenguaje, la personalidad y la función ejecutiva. Descripción de la tecnología: En general los medicamentos empleados en la enfermedad de Alzheimer ayudan a controlar los síntomas y manejar la agitación, la depresión o los síntomas psicóticos (alucinaciones o delirios) que pueden ocurrir cuando la enfermedad progresa. Evaluación de efectividad y seguridad: Pregunta de investigación: ¿Cuál es la efectividad y seguridad de donepezilo, memantina y galantamina comparado con rivastigmina para el tratamiento de la demencia por enfermedad de Alzheimer? La pregunta de investigación fue refinada y validada con base en: autorización de mercadeo de la tecnología para la indicación de interés (registro sanitario INVIMA), listado de medicamentos vitales no disponibles, cobertura de las tecnologías en el Plan Obligatorio de Salud (POS) (Acuerdo 029 de 2011), revisión de grupos terapéuticos (código ATC: Anatomical, Therapeutic, Chemical classification system), recomendaciones de guías de práctica clínica actualizadas, disponibilidad de evidencia sobre efectividad y seguridad (reportes de evaluación de tecnologías, revisiones sistemáticas de la literatura), uso de las tecnologías (listas nacionales de recobro, estadísticas de prescripción, entre otros), estudios de prevalencia/incidencia y carga de enfermedad y consulta con expertos temáticos (especialistas clínicos), sociedades científicas y otros actores clave. No se identificaron otros comparadores relevantes para la evaluación. Población: Hombres y mujeres adultos con enfermedad de Alzheimer. Conclusiones: La evidencia disponible sobre la eficacia de los inhibidores de acetilcolinesterasa (donepezilo, galantamina y rivastigmina) muestra un efecto sobre la cognición y la funcionalidad de los pacientes con enfermedad de Alzheimer moderada y severa. Las comparaciones directas disponibles y las comparaciones indirectas no permiten establecer la superioridad de alguno de los inhibidores de colinesterasa. La eficacia de la memantina para el manejo de la enfermedad de Alzheimer moderada en comparación con rivastigmina no ha sido evaluada en experimentos clínicos controlados. El perfil de seguridad de las intervenciones en estudio es similar al del comprador (rivastigmina).

Acute electrophysiologic consequences of pyridostigmine inhibition of cholinesterase in humans

The cardiovascular electrophysiologic basis for the action of pyridostigmine, an acetylcholinesterase inhibitor, has not been investigated. The objective of the present study was to determine the cardiac electrophysiologic effects of a single dose of pyridostigmine bromide in an open-label, quasi-experimental protocol. Fifteen patients who had been indicated for diagnostic cardiac electrophysiologic study underwent two studies just before and 90-120 min after the oral administration of pyridostigmine (45 mg). Pyridostigmine was well tolerated by all patients. Wenckebach nodal anterograde atrioventricular point and basic cycle were not altered by pyridostigmine. Sinus recovery time (ms) was shorter during a 500-ms cycle stimulation (pre: 326 ± 45 vs post: 235 ± 47; P = 0.003) but not during 400-ms (pre: 275 ± 28 vs post: 248 ± 32; P = 0.490) or 600-ms (pre: 252 ± 42 vs post: 179 ± 26; P = 0.080) cycle stimulation. Pyridostigmine increased the ventricular refractory period (ms) during the 400-ms cycle stimulation (pre: 238 ± 7 vs post: 245 ± 9; P = 0.028) but not during the 500-ms (pre: 248 ± 7 vs post: 253 ± 9; P = 0.150) or 600-ms (pre: 254 ± 8 vs post: 259 ± 8; P = 0.255) cycle stimulation. We conclude that pyridostigmine did not produce conduction disturbances and, indeed, increased the ventricular refractory period at higher heart rates. While the effect explains previous results showing the anti-arrhythmic action of pyridostigmine, the clinical impact on long-term outcomes requires further investigation.

The use of rocuronium in giant Amazon turtle Podocnemis expansa (Schweigger, 1812) (Testudines, Podocnemididae) / Uso do rocurônio em tartaruga da Amazônia Podocnemis expansa (Schweigger, 1812) (Testudines, Podocnemididae)

PURPOSE: To determine whether rocuronium would provide safe, short-term immobilization in Podocnemis expansa. METHODS: Twenty P. expansa, weighing on average 1.59 ± 0.28 kg, were subjected to two protocols: G1 0.25 mg/kg IM of rocuronium and 0.07 mg/kg IM of neostigmine, while G2 received 0.50 mg/kg IM of rocuronium and 0.07 mg/kg IM of neostigmine. The drugs were applied, respectively, in the left and right thoracic members. Assessments were made of the anesthetic parameters of respiratory frequency, heartbeat, righting reflex, cloacal relaxation, palpebral and pupilar reflexes, easy handling, muscle relaxation, locomotion, response to pain stimuli in the right thoracic members, pelvic members and tail, ambient humidity and temperature. RESULTS: They were not found statistical differences between the dosages for the majority of the assessments. G1 was as efficient as G2. A consistent neuromuscular blockade effect was recorded 12 ± 4.21 minutes in G1 and G2. All the animals were recovered in 150 minutes. CONCLUSIONS: Administration of rocuronium at dose of 0.25 to 0.5 mg/kg IM is a safe and effective adjunct to clinical proceedings or pre-anesthetics in P. expansa. Because rocuronium does not provide any analgesic or sedative effects, the duration of neuromuscular blockade without anesthesia should be minimized to avoid undue stress.

OBJETIVO: Determinar se o rocurônio promove imobilização segura e de curta duração em Podocnemis expansa. MÉTODOS: Vinte P. expansa com média de peso 1,59 ± 0,28 kg, foram submetidas a dois protocolos: G1 recebeu rocurônio 0,25 mg/kg IM e neostigmina 0,07 mg/kg IM enquanto G2 rocurônio 0,50 mg/kg IM e neostigmina 0,07 mg/kg IM, aplicados no membro torácico esquerdo e direito, respectivamente. Observaram-se os parâmetros anestésicos: freqüência respiratória e cardíaca, reflexo de endireitamento, relaxamento do esfíncter da cloaca, reflexo palpebral e pupilar, facilidade de manipulação, relaxamento muscular, locomoção, resposta aos estímulos dolorosos no membro torácico direito, nos membros pelvinos e na cauda, temperatura e umidade ambiental. RESULTADOS: Não foram encontradas diferenças estatísticas entre as doses para a maioria dos parâmetros e o G1 foi tão eficiente quanto o G2. Um bloqueio neuromuscular consistente foi observado aos 12 ± 4,21 minutos tanto no G1 como no G2. A recuperação de todos os animais ocorreu em até 150 minutos. CONCLUSÕES: Administração de rocurônio nas doses 0,25 e 0,50 mg/kg IM é segura e efetiva para os procedimentos clínicos ou pré-anestésicos em P. expansa. Como o rocurônio não produz efeitos sedativos ou analgésicos, a duração do bloqueio neuromuscular sem anestesia deverá ser minimizado para evitar estresse.

Effects of 6 months of treatment with donepezil and rivastigmine on results of neuropsychological tests of MMSE, NPI, clock and bender in patients with Alzheimer's disease

Alzheimer's disease is the most common degenerative disease of brain. Nowadays, acetyl cholinesterase inhibitors, including donepezil, rivastigmine and galantamine, are standard treatments to slow down disease progression. Purpose of our study was to show effects of treatment with donepezil and rivastigmine and to compare these effects between two drugs. Samples selected from patients who had Alzheimer disease with DSM IV criteria and were candidate of receiving donepezil or rivastigmine for the first time. We used four neuropsychological tests including MMSE, NPI, Clock and Bender to assess patient's cognitive and behavioral changes during treatment with two drugs. Patients divided to two groups [each group 35 cases], one group taking donepezil and the other rivastigmine. The four tests were completed once before starting treatment and then, 1 month, 3 months and 6 months after treatment with Donepezil and Rivastigmine. MMSE, 6 months after treatment with Donepezil, improved from 20.63 before treatment to 21.83, which was statistically significant. Also, MMSE, 6 months after treatment with Rivastigmine, improved from 20.03 before treatment to 22.71, which was statistically significant. About Clock test, there was a significant improvement from 5.74 before treatment to 6.4 after 6 months of treatment with Rivastigmine; while this significant improvement was not seen in patients receiving Donepezil. In two other tests, no significant differences were seen before and after treatment. Also, No significant difference was detected between two groups and so no different effects on these tests between Donepezil and Rivastigmine in 6 months period of treatment

Intoxicación por amitraz: reporte de dos caso / Amitraz poisonig: report of two case

El incremento en la disponibilidad y uso de amitraz para el control de garrapatas en animales domésticos puede causar intoxicaciones accidentales en niños, con depresión severa del sistema nervioso central. Es necesario conocer el manejo correcto de esta intoxicación emergente. Reportamos los primeros casos de intoxicación aguda por amitraz en el estado Lara, en dos niñas quienes presentaron miosis pupilar y depresión del estado de conciencia. Una de ellas recibió varias dosis de atropina por los signos colinérgico similares, sin respuesta; posteriormente mejoró con el tratamiento de sostén. A la otra paciente se le administró precozmente naloxoma, observándose respuesta satisfactoria inmediata.

Increase of availability and use of amitraz for tick control in domestic animal, may cause accidental poisoning in children with severe CNS depression. It is necessary to know the right management of this emerging poisoning. We report the first cases of acute amitraz poisoning in Lara state, in two children who developed pupilar myosis and nervous central system depression. One of them received several doses of atropine for cholinergic-like signs, without response, but finally she improved with support therapy; to the other patient naloxona was administered early, being observed immediate satisfactory response.

Neostigmine does not prolong the duration of analgesia produced by caudal bupivacaine in children undergoing urethroplasty.

CONTEXT: Neostigmine extends the duration of analgesia produced by caudal bupivacaine in children. AIMS: To study the effect of different doses of caudal neostigmine on the duration of postoperative analgesia. SETTINGS AND DESIGN: A randomized, double-blind study was conducted in 120 boys aged 1-12 years undergoing urethroplasty under combined general and caudal anesthesia. MATERIALS AND METHODS: Children were administered 1.875 mg/kg bupivacaine alone (Group B) or with 2, 3 or 4 microg/kg of neostigmine (groups BN 2, BN 3 or BN 4 respectively) as caudal drug (0.75 ml/kg). Children with a pain score of 4 or more (OPS and NRS) postoperatively were administered rescue analgesic. Time to first analgesic and the number of analgesic doses administered in the 24h were recorded. STATISTICAL ANALYSIS: Parametric data were analyzed using ANOVA. Kaplan-Meier survival curves for the time to first analgesic administration were plotted and compared using log rank analysis. Chi-square test was used to analyze the incidence data. RESULTS: The median [IQR] time to first analgesic in Group B (540 [240-1441] min) was similar to that in Groups BN 2 (450 [240-720]), BN 3 (600 [360-1020]) and BN 4 (990 [420-1441]). Significantly more patients in Groups B (9 [34.6%]) and BN 4 (13 [44.8%]) required no supplemental analgesic for 24h than those in Groups BN 2 and BN 3 (4 [13.8%] and 4 [13.3%]). The number of analgesic doses required in 24h in the four groups was similar. CONCLUSION: Addition of neostigmine to 1.875 mg/kg of caudal bupivacaine did not prolong the analgesia following urethroplasty in children.

Depressão vascular no idoso: resposta ao tratamento antidepressivo associado a inibidor das colinesterases / Vascular depression in elderly: response to treatment with antidepressant associated to cholinesterase inhibitor

CONTEXTO: Entre os transtornos neuropsiquiátricos ocasionados por eventos cerebrovasculares, a depressão vascular é pouco diagnosticada por médicos não especialistas, causando aumento da morbimortalidade de pacientes idosos. CASO CLÍNICO: Trata-se de um paciente com 67 anos que apresentou resposta parcial a tratamento com inibidores da recaptura de serotonina e efeitos adversos autonômicos graves com outros antidepressivos. A adição de rivastigmina ao citalopram promoveu sucesso terapêutico, com redução de 23 para 7 pontos, na escala de Hamilton para depressão. DISCUSSÃO: O resultado obtido traz novas perspectivas para o tratamento da depressão vascular, sendo necessários ensaios clínicos controlados que evidenciem o benefício da adição dos inibidores das colinesterases aos antidepressivos no tratamento destes pacientes.

CONTEXT: Among neuropsychiatric disorders caused by cerebrovascular factors, vascular depression is diagnosed in a small degree by general practitioners, causing morbid-mortality increase in elderly. CASE REPORT: That is a case of a 67 year-old-man with partial response after treatment with a Selective Serotonin Receptors Inhibitor, and severe autonomic adverse effects with other antidepressants. The addition of rivastigmine to citalopram resulted in a therapeutic success, with a reduction of 23 to 7 points on the Hamilton Depressive Scale (HAM-D). DISCUSSION: The result obtained brings new perspectives to the treatment of vascular depression, providing that randomized controlled trials with larger sample sizes confirm the positive effect of the addition of a cholinesterase inhibitor to antidepressants in the treatment of these patients.

Effect of anticholinesterase compound phosalone on blood-brain barrier (BBB) permeability.

To elucidate the role of acetylcholinesterase (AChE) enzyme in BBB function, phosalone, an organophosphorous compound, was studied using rat brain micro vessels in vitro. Phosalone at 100 mg/kg b. wt. induced convulsions and caused a significant inhibition of AChE resulting in increased permeability as assessed by volume distribution. The anaesthetized phosalone treated group also increased permeability as compared to the control but the values were significantly (P<0.05) lower than phosalone alone treated group. The inhibition of AChE enzyme has altered the barrier function at the dose level at which it caused convulsion and had an added effect on permeability of BBB.

Reversäo do bloqueio neurosmuscular induzido pelo cisatracúrio com diferentes doses de neostigmina / Reversal of cisatracurium neuromuscular block with different doses of neostigmine

Justificativa e objetivos - A neostigmina em doses de 0,04 a 0,06mg.kg-1 antagoniza efetivamente o bloqueio neuromuscular induzido pelo cisatracúrio. Este estudo avaliou o padräo de recuperaçäo do bloqueio neuromuscular induzido pelo cisatracúrio, com três doses diferentes desses anticolinesterásico. Método - participaram do estudo 56 pacientes adultos (M/F:22/34), estado físico ASA I e II, com idade de 40,18 ñ 12,7 anos, alocados por sorteio prévio em quatro grupos. Todos os pacientes receberam cisatracúrio na dose de 0,15 mg.kg-1, por via venosa, logo, após a induçäo da anestesia. A resposta eletromiográfica foi medida em intervalos de 10 segundos. Quando T1 apresentou recuperaçäo de 10 por cento em relaçäo ao controle, neostigmina foi administrada nas doses de 0,02 (G1;n=16), 0,03 (G2;n=15) e 0,05 (G3;n=14)mg.kg-1. O grupo G4 näo recebeu neostigmina. A relaçäo T4/T1 foi anotada a intervalos de 1 minuto nos 20 minutos subsequentes. Resultados - no período entre 0 e 4 minutos, näo houve diferença significativa entre as doses, quanto à relaçäo T4/T1. Entre o 5º e o 14º minuto, o grupo G3 apresentou relaçöes T4/T1 médias maiores que o grupo G1, em todos os momentos e maiores que o grupo G2 nos minutos 5, 7, 9 e 10. A partir do 15º minuto näo houve diferença estatisticamente significativa entre os valores médios da relaçäo T4/T1 entre os grupos que receberam neostigmina. Os valores médios de T4/T1 foram significativamente menores no grupo G4, a partir do 4º minuto. O percentual de pacientes que apresentaram relaçöes T4/T1 maior ou igual 0,9 ao término do período de observaçäo (20ºminuto) no grupo G3 (92,85 por cento) foi significativamente maior do que nos grupos G1 (56,25 por cento) e G2 (46,66 por cento). No grupo G4, nenhum paciente apresentou relaçäo T4/T1 igual ou superior a 0,9, diferindo significativamente dos outros grupos. Conclusöes - embora a dose de 0,05mg.kg-1 acelere a recuperaçäo da relaçäo T4/T1 até 0,7, näo difere das doses de 0,02 e 0,03mg.kg-1. Apesar disto, um percentual significativamente maior de pacientes apresentou relaçäo T4/T1 igual ou seperior a 0,9, quando a dose de neostigmina foi de 0,05 mg.kg-1, em comparaçäo com as doses menores

Efeito antinociceptivo sinergístico entre receptores opióides espinhais e supraespinhais. Comparaçäo com a associaçäo opióide e anticolinesterásico por via central / Synergistic antinociceptive effect of spinal and supra spinal opioid receptors. Comparison with the association of spinal morphine and neostigmine

Justificativa e objetivos - A administraçäo de morfina por vias distintas resultou em potencializaçäo do efito analgésico em animais. Este estudo visou avaliar, em pacientes, o efeito analgésico da morfina por via venosa, intratecal ou sua associaçäo para analgesia pós-operatória, comparada à associaçäo morfina e anticolinesterásico por via espinhal. Método - Cinquenta pacientes submetidas a colpoperineoplastia sob anestesia subaracnóidea foram divididas em cinco grupos. Por via venosa (v), as pacientes receberam midazolam (0,05 mg.kg elevado a menos um) como medicaçäo pré-anestésica, associado à droga teste. A anestesia foi realizada com bupivacaína mais a droga teste intratecal (it). O grupo controle (GC) recebeu slina por via venosa (v) e ev e salina por via intratecal (it). O grupo morfina venosa (GMv) 100 µg de morfina venosa e salina intratecal. O grupo morfina it (GMit) salina ev e 100 µg de morfina it. O grupo morfina ev+it (GMv+it) 100 µg de morfina venosa e 100 µg de morfina intratecal; e o grupo morfina-neostigmina (GMN) salina venosa e 100 µg de morfina + 10 µg de neostigmina intratecal. Analgesia e efeitos adversos foram medidos pela escala analógica visual (EAV). As pacientes fizeram uso de analgesia controlada pelo paciente com morfina, no pós-operatório. Resultados - Os valores da EAV para as 24 horas foram semelhantes entre os grupos. O tempo (minutos) para requisiçäo do primeiro analgésico foi: GMN (982 ñ 178) = Gmv+it (1022 ñ 434) > GMit (736 ñ 218) (p < 0,03) > GMv (140 ñ 26) (p < 0,05) = GC (121 ñ 19). O consumo de morfina (mg) durante as primeiras 24 horas foi: GMN (9 ñ 4) = GMv+it (6 ñ 7) = GMit (10 ñ 3) < GMv (22 ñ 7) = GC (26 ñ 7) (p < 0,0006). Conclusöes - A administraçäo de 100 µg de morfina intratecal resultou em 12 horas de analgesia pós-operatória, a qual foi potencializada pela morfina (100 µg) por via venosa (17 horas) e pela neostigmina por via intratecal (16 horas), refletindo um efeito antinociceptivo sinergístico entre receptores opióides espinhais e supraespinhais e entre receptores opióides e colinérgicos espinhais em pacientes

Do we need anti snake venom (ASV) for management of elapid ophitoxaemia.

Twelve patients of elapid ophitoxaemia presented with neuromuscular paralytic features were given anticholinesterase (Neostigmine) in recommended dosage. In four of these patients, despite neuromuscular paralysis, no ASV was used. All these four patients survived. In eight patients, ASV was used; in three of whom it used in doses less than 50 units, yet patients survived. Of the remaining five, despite use of ASV in higher doses (more than 50 units), two succumbed to death. Eight patients required ventilatory support. Hence, in absence of any definite role of ASV in management of elapid ophitoxaemia (snake bite), use of anticholinesterase drugs alone, with good supportive care and prevention of likely complications, can result in satisfactory outcome.

La cervicomanubriotomía en la timectomía por miastenia gravis / Cervicalmanubriotomy in thymectomy for myasthenia gravis

Se presenta nuestra experiencia con la cervicomanubriotomía como vía de acceso para realizar la timectomía en los pacientes portadores de miastenia gravis. Se analiza la parte histórica, la fundamentación anatómica y se describe la técnica quirúrgica de esta vía de abordaje. Se analiza a continuación la casuística, los hallazgos y los resultados con ella obtenidos. Los pacientes operados fueron doce, con un 58,3 por ciento en la etapa grave de la enfermedad (Osserman III y IV), encontrándose un timoma en el 50 por ciento. No hubo mortalidad postoperatoria. En el seguimiento hubo 4 fallecidos tardíos, el seguimiento promedio del resto fue de 5,5 años, con dos de ellos en remisión permanente

Biochemical and behavioral effects of intraseptal microinjection of fasciculin, an irreversible acetylcholinesterase inhibitor

We examined the effect, in rats, of an intraseptal microinjection of fasciculin (FAS), an irreversible peptide acetylcholinesterase (AChE) inhibitor, on a)AChE activity measured in septum and hippocampus, b)3H-quinuclidiny benzylate (3H-QNB) and 3H-oxotremorine (3H-OXO) binding to hippocampal cholinergic muscarinic receptors, c) 3H-flunitrazepan (3H-FNZ) binding to hippocampal benzodiazepine receptors as a control for QNB and OXO binding, d) acquisition and retention in three different behavioral paradigms, i. e., water-finding (in which there is concomitant habituation to be apparatus), step-down inhibitory avoidance, and shuttle avoidance. AChE activity in septum decreased 2 days (-66%) and 5 days (-48%) after FAS microinjection; a slight reduction (-35%) occurred in the dorsal hippocampus on day 2 (P<0.05; N=6 per group); no changes in AChE activity were observed in ventral hippocampus ion day 2 or day 5. No changes in 3H-QNB, 3H-OXO, or 3H-FNZ binding constants were demonstrable in the hippocampus either 2 or 5 days after intraseptal FAS adminstration. No changes in training or test session performance in any of the three behavioral situations were observed 2-3 days after the intraseptal microinjection of FAS. The persistent inhibition of septal AChE caused by FAS microinjection into the septum is not sufficient to induce major changes either in hippocampal cholinergic muscarinic receptors, or in the learning or retention of behaviors regulated by the septum and/or hippocampus

Perfil de la colinesterasa sanguínea en la población de Panamá / Cholinesterase blood profile in the panamenian population

Presenta información sobre la actividad de en sangre total, la finalidad de conocer los niveles de esta enzima y su variación en la población panameña tomando en consideración los siguientes parámetros: exposición a plaguicidas, sexo, edad y área de trabajo. Se empleó el método de Hidroxamato, de Trunaut-Vernin para las determinaciones analíticas de la actividad de la Colinesterasa en muestras de sangre en un total de 103 varones y 52 mujeres, en algunos casos expuestos y en otros no expuestos a plaguicidas inhibidores de la colinesterasa en diferentes provincias del país (Chiriquí, Coclé, Herrera, Panamá y Veraguas)