Prospecção de atividade inibitória da pasta de hidróxido de cálcio e acetazolamida sobre Enterococcus faecalis e Candida albicans / Antimicrobial effect of calcium hydroxide paste and acetazolamide against the Enterococcus faecalis and Candida albicans

Introdução: A medicação intracanal é fundamental para o tratamento de um dente avulsionado, sendo a pasta de hidróxido de cálcio comumente indicada. A acetazolamida é uma substância inibidora da anidrase carbônica e da reabsorção óssea, podendo ser sugerida como medicação intracanal em dentes avulsionados. Contudo, para que uma substância seja sugerida, estudos devem comprovar sua eficácia tanto in vitro como in vivo. Objetivo: Avaliar in vitro a ação antimicrobiana da pasta de hidróxido de cálcio e da acetazolamida, associadas a diferentes veículos, contra os micro-organismos Enterococcus faecalis e Candida albicans. Materiais e métodos: As formulações selecionadas foram: acetazolamida (pó) com soro fisiológico; acetazolamida (pó) com glicerina; acetazolamida e hidróxido de cálcio (pó) em porções iguais com soro fisiológico; acetazolamida e hidróxido de cálcio (pó) em porções iguais adicionando-se glicerina; acetazolamida (líquido) e hidróxido de cálcio (pó) com soro fisiológico. Como controle positivo foram utilizadas concentrações de clorexidina de 20%, 10%, 5%, 2,5%, 1,25% e 0,65% e como controle negativo a glicerina. O experimento foi realizado por teste de difusão em ágar. Resultados: Não houve inibição do crescimento das bactérias com os medicamentos utilizados, apenas com o controle positivo.Conclusão: As formulações de hidróxido de cálcio e acetazolamida não apresentaram atividade inibitóriacontra o E. faecalis e C. albicans.

Introduction: The intracanal medication is essential for the treatment of avulsed tooth, being the calcium hydroxide paste usually indicated. The acetazolamide is an inhibiting substance of carbonic anhydrase and the bone resorption, being suggested as intracanal medication in avulsed teeth. However, for this substance became an alternative as intracanal therapeutic agent, it must be tested in vitro and in vivo. Objective: To evaluate, in vitro, the antimicrobial action of calcium hydroxide paste and acetazolamide associated with different vehicles, against the Enterococcus faecalis and Candida albicans. Materials and methods: The experimental groups were: acetazolamide (powder) with physiological serum; acetazolamide (powder) with glycerin; acetazolamide and calcium hydroxide (powder) in equal portions with physiological serum; acetazolamide and calcium hydroxide (powder) in equal portions added with glycerin; acetazolamide (liquid) and calcium hydroxide (powder) with physiological serum. Clorexidine was used for positive control in concentrations of 20%, 10%, 5%, 2.5%, 1.25% and 0.65% and glycerin was used as negative control. The study was carried through by test of diffusion in agar. Results: No experimental groups showed inhibition of the bacterial growth, only inhibited by the positive control. Conclusion: The groups with calcium hydroxide and acetazolamide did not show antimicrobial activity against the E. faecalis and C. albicans.

Purification and some properties of carbonic anhydrase from Elephas trogontherii (Steppe elephant) bone.

Four isoenzymes of carbonic anhydrase (CA) were purified from Elephas Irogontherii (steppe elephant) bone (approx 0.3-0.5 million years old) from different locations (outer peripheral, cytosolic, inner peripheral and integral) using Sepharose 4B-L-tyrosine sulphanilamide affinity chromatography and their kinetics properties were investigated and compared with known CA isoenzymes. The purification degree of CAs was monitored by SDS-PAGE. Purification fold for outer peripheral, inner peripheral, cytosolic and integral CA was 395.6, 652.8, 1091 and 429.3 and the molecular mass (as determined by gel filtration chromatography) was 37, 36, 35, and 39 kDa, respectively. The optimal temperature for isozymes was 10-20, 30, 30 and 60 degrees C and optimal pH- was between 7.5-11, 7.5-10, 7.5-10 and 7.5 respectively. K(m) values (at optimum pH and 20 degrees C) for p-nitrophenyl acetate as substrate were 4.83, 6.80, 4.525 and 3.86 mM and the Vmax values for the same substrate were 0.00097, 0.0149, 0.00249 and 0.00072 micromol/L*min, respectively. I50 values of isoenzymes for the inhibitors of CA - sulphanilamide, KSCN, acetazolamide and NaN3 were also determined.

A Korean Family of Hypokalemic Periodic Paralysis with Mutation in a Voltage-gated Calcium Channel (R1239G)

Hypokalemic periodic paralysis (HOPP) is a rare disease characterized by reversible attacks of muscle weakness accompanied by episodic hypokalemia. Recent molecular work has revealed that the majority of familial HOPP is due to mutations in a skeletal muscle voltage-dependent calcium-channel: the dihydropyridine receptor. We report a 13-yr old boy with HOPP from a family in which 6 members are affected in three generations. Genetic examination identified a nucleotide 3705 C to G mutation in exon 30 of the calcium channel gene, CACNA1S. This mutation predicts a codon change from arginine to glycine at the amino acid position #1239 (R1239G). Among the three known mutations of the CACNA1S gene, the R1239G mutation was rarely reported. This boy and the other family members who did not respond to acetazolamide, showed a marked improvement of the paralytic symptoms after spironolactone treatment.

Hypoxia and pulmonary acclimatisation at 4578 m. altitude: the role of acetazolamide and dexamethasone

To quantify the changes in ventilatory response and arterial blood gases in healthy male volunteers on acute ascent to 4578 meters altitude alongwith evaluating the role of acetazolamide and dexamethasone prophylaxis in acclimatisation. Forty four lowlander male subjects participated as two groups in the study. Twenty four lowlander healthy male adults [age mean + SE 27.8 + 1.24 years] comprised the non-acclimatised group. They were sub grouped in a double blind fashion into four. Each subgroup [n=6] received placebo [multivitamin] or acetazolamide [250 mg] or dexamethasone [4mg] or combined regimen of the two drugs twice daily for 5 days commencing 24 hours before ascent. The volunteers reached the altitude of 4578 meters within a span of one day. The second group [acclimatised] comprised of age and height matched twenty volunteers who had arrived 4 and 8 weeks earlier at the same altitude. Arterial PO2, PCO2, SO2 and minute respiratory rate pH were measured. The pulmonary functions [FVC,%FEV1 PEF, FE25-75% and MVV] were recorded by Compact Spirometer [Vitalograph]. Pre and post ascent measurements were carried out in non-acclimatised group whereas one measurement of the same parameters were made in acclimatised group. The study revealed a significant increase in respiratory rate min-1 after 24 hours of ascent alongwith reduction in PaO2 and SaO2. The gradual increase in PaO2 and SaO2 and reduction in PaCO2 was observed after 4 weeks at the same altitude. The reduction in FVC,%FEV1, PEF, FEF25-75% and MVV were recorded in our subjects after 24 hours of acute ascent. Nevertheless, all pulmonary parameters in volunteers having 8 weeks of stay at 4578 m altitude, were found equivalent to the non-acclimatised group. The greater increase in minute respiratory rate, PaO2, SaO2 and pulmonary functions was found in volunteers taking acetazolamide. It is concluded that hyperventilation and increase in lung volumes are the adaptive pulmonary responses which help in improving levels of PaO2 and SaO2. The acetazolamide-dexamethasone prophylaxis appears beneficial in promoting pulmonary acclimatisation during hypobaric hypoxia

Chachacoma ¿un tratamiento alternativo para la prevención del mal agudo de montaña? / Chachacoma, an alternative treatment to prevention od acute mountain sickness?

Chachacoma is an herbal folk remedy used by natives and tourists to avoid high altitude sickness (AMS) when mountain climbing. Chachacoma has been described as a hypotensor. Acetazolamide is presently the best treatment for prevention of AMS and it's function is diuretic. The objectives of the present study was to make a comparative analysis of the efficacy of these two treatments for AMS. A group of 22 healthy subjects (22+- 1 years) with no high altitude experience were divided into two group of 11, one of which received a cup of Chachacoma infusion and a second group of 11 received 250mg of acetazolamide the morning prior to making an ascent (2000 m+). The day prior to the ascent the following parameters were measured on all subjects: heart rate (HR), respiratory rate (RR), systolic and diastolic pressure (SAP,DAP) and oxigen saturation (SatO2). In the following days in Colchane the measurements were repeated and the Lake Louise Test was used to determine AMS symptoms. Values were expressed +- 1 std. deviation and differences were evaluated with a student test ( vs Chachacoma, p>0.05). The incidence of AMS in the Chachacoma group was 55 percent, compared to 36 percent in the acetazolamide group (p<0.05). No significant differences were observed in arterial pressure between groups. However, the point score for AMS for the acetazolamide group was lower than that for the Chachacoma group. It was concluded that acetazolamide was more effient in preventing the symptoms of AMS than Chachacoma.

Chachacoma es un tratamiento etnomedicinal para el MAM en nativos y turistas que ascienden a grandes alturas. Chachacoma es descrita como hipotensor. Acetazolamida actualmente es el mejor tratamiento para prevenir MAM, su función es de diurético. Nuestro objetivo fue comparar su eficiencia en la prevención del MAM. Un estudio fue aplicado a 22 sujetos (22+- 1 años), sanos, sin experiencia a grandes alturas (>2000 m). Un grupo (n=11) con Chachacoma (1 taza con infusión dada en la mañana del ascenso), otro grupo (n=11) con Acetazolamida (250 mg en la mañana del ascenso), El día previo al ascenso se determinaron: frecuencia cardíaca (FC) y respiratoria (FR), presiones sistólicas y diastólicas (PAS,PAD) y saturación de oxigeno (Sat=2). En los siguientes días en Colchane las mediciones fueron repetidas y se usó un test de Lake-Louise para determinar síntomas de MAM. Los valores se expresaron en promedios +- DS, la diferencia fue medida con test de Student (vs Chachacoma, p<0,05). La incidencia de MAM en el grupo de Chachacoma fue 55 por ciento, contra el 36 por ciento del grupo de Acetazolamida )p<0.05). No se observaron cambios en presión arterial en ambos grupos. Sin embargo, el puntaje de MAM para el grupo de Acetazolamida fue menor que el de Chachacoma. En conclusión, Acetazolamida es más eficiente previniendo síntomas de MAM.

Luminal acid in water-inmersion stress and the antiulcer effect of axetazolamide in the rat gastric mucosa

En ratas con píloro ligado, la secreción ácida gástrica (volumen y débito) de los animales en estrés por 10 h (inmovilización e inmersión en agua (21 grados celsius) fue significativamente menor que la de las ratas sin estrés. Acetazolomida, un potente inhibidor de la anhidrasa carbónica, administrada por vía intraperitoneal cada 5 h por un total de dos veces, dosis dependientemente (100, 50, 25 mg/kg) inhibió la secreción ácida y la formación de lesiones mucosas gástricas inducidas por el estrés (dosis antisecretoras). La acetazolamida (5 mg/kg) no tuvo efecto sobre dos parámetros (dosis noantisecretora). El incremento de las lesiones mucosas gástricas inducidas por la instilación intragástrica de 150 mM HCL (0.5 ml/h) durante el estrés, no fueinhibido por dosis antisecretoras de acetazolamida. Se concluye que: (1) la exposición de ratas por 10 h de estrés (inmovilización e inmersión en agua) disminuye la secreción ácida gástrica (2) la acetazolamida, inhibiendo la secreción ácida gástrica protégé a la mucosa de las lesiones inducidas por el estrés y (3) una mínima cantidad de ácido en el lumen gástrico es suficiente para desarrollar las lesiones inducidas por este tipo de estrés.

Análise dos efeitos colaterais provocados pelo uso da acetazolamida via oral nos primeiros 5 dias de tratamento com relaçäo aos níveis séricos de potássio / Side effects of acetazolamide per os during the first five days of treatment and relationship with seric potassium level

Os autores realizaram um estudo duplo-cego para determinar uma possível entre potássio sérico e efeitos colaterais, que aparecem nos primeiros 5 dias de tratamento com acetazolamida 500 mg, via oral. Em todos aqueles que usaram a droga produziu-se efeitos colaterais, sendo o mais comum parestesias. Näo houve diferença significativa entre os níveis de postássio sérico antes e após o tratamento

Efecto de la acetazolamida en pacientes portadores de bronquitis crónica obstructiva y alcalosis metabólica / Acetazolamide effect in patients with obstructive chronic bronchitis and metabolic alkalosis

Nueve pacientes portadores de bronquitis crónica obstructiva hipercápnica y alcalosis metabólica recibieron oralmente una dosis inicial de 500 mg de acetazolamida seguida durante 6 días de una dosis diaria de 250 mg; la serie control estuvo constituída por 7 pacientes de características similares. El grupo tratado mostró una disminución de la PaCO2 desde 59 a 45 mmHg (p<0.001) y del bicarbonato real (de 36 a 26 mEq/L;p<0.0025), con ascenso no significativo de la PaCO2 pero sí de la relación PaCO2/FiO2, que aumentó en promedio desde 212 a 266 mmHg (p<0.01). El grupo control también disminuyó significativamente la PaCO2 y el bicarbonato aunque en un nivel menor; no se modificó la PaO2 pero si aumentó la PaO2/FiO2, aunque también en nivel menor, siendo significativa sólo la diferencia de PaCO2 y relación PaO2/FiO2 entre ambos grupos desde el primer día de tratamento. Ni la ventilación minuto ni el PH se modificaron significativamente en ninguno de los grupos. Se concluye que: 1o. La acetazolamida mejora la PaO2 y PaCO2 mas rapidamente que lo que ocurre en los pacientes no tratados, 2o. No hay peligro de acidosis metabólica severa con el esquema utilizado y 3o. La dosis inicial tiene un efecto rápido apreciable en forma significativa dentro de las primeras 24 horas

Hipercapnea inducida por acetazolamida, su efecto en la circulación pulmonar: estudio experimental / Acetazolamide induced hipercapnea, its effect on the pulmonary circulation: experimental study

Se diseño un modelo de hipercapnea, sin hipoxemia ni acidosis y se evaluaron los efectos del CO2 en la circulación arterial pulmonar. Se estudiaron 6 perros a los que se administró dosis única de acetazolamida (120mg/Kg) para inhibir la acción de la anhidrasa carbónica. Con esta dosis se logró aumentar la PaCO2 de 27.mmHg a 41.mmHg y la PvCO2 de 31.mmHg a 46.mmHg (p<0.01). A lo largo de tres horas la PaCO2 y la PvO2 permanecieron estables y no ocurrió hipoxemia. El pH arterial y el venoso se mantuvieron en promedio en 7.35 ñ 02 y 7.32 ñ.03 respectivamente. Hemodinâmicamente hubo aumento de las resistencias pulmonares totales de 312 ñ 156 a 435 ñ 173 d.s.cm >- (p<0.01) y la presión media de la arteria pulmonar no se modificó. Estos hallazgos aunados a la disminución del índice latido de 20.7 ñ 8.3 a 13.2 ñ 4.8 ml/lat. (p<0.5), sin haber ocurrido cambios en la presión capilar pulmonar, ni en la presión diastólica final del ventrículo derecho nos sugieren posible vasoconstricción pulmonar, la que se atribuye a incremento de la PaCO2 y la PvCO2, en ausencia de otros factores vasoactivos o pasivos

Efectos oculares y sistémicos de la administración preoperatoria de acetézolamida en la cirugía de la catarata senil / Ocular and systemic effects preoperative administration of acetozolamide in surgery of senile cataract

Se analizam los efectos de la administración preoperatoria de acetazolamida, tanto en forma fraccionada como em dosis única, sobre la presión intraocular preoperatoria, la presión vítrea intraoperatoria, el equilibrio ácido-base y los electrolitos plasmáticos en 99 casos de catarata senil pura operados por el autor en el Servicio de Oftalmología del Hospital José Joaquím Aguirre entre los años 1980 y 1982, divididos al azar en tres grupos de estudio, a saber: grupo I, 33 pacientes que recibieron acetazolamida en dosis de 250 mgr por vía oral 18, 10 y 2 horas antes de la operación; grupo II, 33 pacientes que recibieron acetazolamida en dosis única de 500 mgr por vía oral 2 horas antes de la operación; y grupo III, 33 pacientes que no recibieron premedicación (grupo control). La disminución de la presión intraocular observada con ambos tipos de premedicación fue leve (aproximadamente 7%) y estadísticamente no significativa. La premedicación fraccionada provocó mayores alteraciones sistémicas que la premedicación en dosis única, caracterizadas por una acidosis metabólica moderada, compensada con hiperventilación. Los electrolitos plasmáticos no experimentaron modificaciones significativas. No se apreció relación entre la acidosis metabólica inducida por la droga y la cuantía del efecto hipotensor ocular, ni se evidenció una mayor efectividad de la acetazolamida en el control de la presión vítrea durante la extracción de la catarata en comparación con el grupo de pacientes que no recibió premedicación

Acetazolamida e manitol: estudo comparativo do efeito hipotensor ocular / Acetalozamide and mannitol: comparative study of ocular hypotensive effect

Estuda-se a participaçäo dos hipotensores oculares, Acetazolamida (500 mg) e o Manitol endovenoso (2 g/Kg), no pré-operatório das cirurgias oculares, para que se busque o "ótimo" de hipotensäo ocular durante o ato cirúrgico. Estudam-se 50 pacientes normotensos selecionados. Após comentários sobre o mecanismo de açäo das duas drogas hipotensoras, conclui-se que: 1 - Com Diamox em dose única (500 mg), via oral: - a queda máxima da Po obtida foi em torno de 8.50 mmHg, após 120'; - o retorno ao nível inicial (12.00 mmHg) de morou 330'. 2 - Com Manitol endovenoso a 20% (2 g/Kg de peso aproximadamente): - a queda máxima da Po obtida foi em torno de 7.60 mmHg, após 90'; - o retorno ao nível inicial (12.00 mmHg) demorou 450'. 3 - Com a associaçäo Diamox + Manitol, nas mesmas doses: - a queda máxima da Po obtida foi em torno de 7.10 mmHg, após 90'; - o retorno ao nível inicial (12.00 mmHg) demorou 450'. 4 - Os resultados favoreceram ligeiramente a associaçäo, porém sem interesse clínico: O Manitol isoladamente lhe corresponde. 5 - O início da cirurgia näo deve ser precipitado, lembrando-nos de que 90 - 120' constitui o interregno para se atingir o declínio tensional máximo

Effect of acetazolamide on insulin sensitivity in dogs with alloxan diabetes.

The effect of acetazolamide on the sensitivity to exogenous insulin in the alloxanised diabetic dogs was studied. The administration of acetazolamide caused acidosis and insulin resistance. The liver insulinase activity of diabetic dogs after acetazolamide administration was also studied to evaluate the role of this enzyme for the destruction of exogenous insulin. It was observed that insulinase did not play role for the development of insulin resistance after acetazolamide administration.