Evaluación de la relajación neuromuscular y predictores de vía aérea difícil en pacientes programados para cirugía general Hospital Central Universitario Dr. Antonio María Pineda / Evaluation of muscle relaxation and predictors of difficult airway in patients programmed for general surgery Hospital Central Universitario Dr. Antonio María Pineda

Se realizó una investigación experimental tipo ensayo clínico controlado simple ciego con el fin de evaluar la relajación muscular y los predictores de vía aérea difícil en pacientes programados para cirugía general en el Hospital Central Universitario Dr. Antonio María Pineda. La muestra estuvo conformada por 100 pacientes distribuidos aleatoriamente en cuatro grupos de 25 pacientes cada uno. En los grupos Experimental-1 (E-1) y Control-1 (C-1) se utilizó una dosis del bloqueante neuromuscular Bromuro de Rocuronio de 0,6 mg/kg y en los grupos Experimental-2 (E-2) y Control-2 (C-2) de 1 mg/kg. La edad promedio de los pacientes fue de 34,8 ± 9,8 años; en los grupos E-1 y E-2, los predictores de vía aérea difícil predominantes fueron distancia esternomentoniana (32% y 42%), distancia tiromentoniana (24% y 40%), distancia interincisivos clase I (88% y 92 %), circunferencia de cuello  40 cm (16% y 8 %), Mallampati (88% y 40%), extensión atlanto-occipital (28% y 20%) y protrusión mandibular (28% y 20%). En el 72% y 80% de los pacientes de los grupos experimentales y control no hubo intento adicional de intubación orotraqueal (IOT); el tiempo invertido para alcanzar la IOT fue < 1 minuto en el grupo C-2 (64%) y E-2 (72%). Existen diferencias estadísticamente significativas entre el número de intentos para alcanzar la IOT, la presencia de predictores de vía aérea difícil y la dosis de bloqueante neuromuscular utilizada lo que evidencia de que a medida que se aumenta la dosis del medicamento hay mayor posibilidad de éxitos en la IOT, aun cuando estén presentes predictores de vía aérea difícil(AU)

An experimental simple blind controlled clinical trial was carried out to evaluate muscle relaxation and predictors of difficult airway in patients scheduled for general surgery at the Hospital Central Universitario Dr. Antonio María Pineda. The sample consisted of 100 patients randomly distributed into four groups of 25 patients each. Patients from the Experimental-1 (E-1) and Control-1 (C-1) groups received 0.6 mg/kg of the neuromuscular blocking agent Rocuronium Bromide while Experimetal-2 (E-2) and Control-2 (C-2) patients received a dosage of 1 mg/kg. Average age of participants was 34.8 ± 9.8 years. Predictors of difficult airway in E-1 and E-2 were sternomental distance (32% and 42%, thyromental distance (24% and 40%), interincisive distance class 1 (88% and 92%), neck circumference  40 cm (16% and 8%), Mallampati (88% and 40%), atlanto-occipital extension (28% and 20%) and mandibular protrusion (28% and 20%). In 72% and 80% of patients from the E and C groups there was not an additional attempt of orotracheal intubation (OTI); the time invested to reach the OTI was less than one minute in 64% of patients from the C-2 and 72% of the E-2. There are statistically significant differences between the number of attempts to reach the OTI, presence of predictors of difficult airway and the dose of Rocuronium Bromide which means that as the drug dosage increases, there is a greater possibility of success in the OTI, even when predictors of difficult airway are present(AU)

Evaluation of relaxant responses properties of cinnamon essential oil and its major component, cinnamaldehyde on human and rat corpus cavernosum

ABSTRACT Cinnamomum cassia (Cinnamon) is a well-known traditional medicine with therapeutic benefits for centuries. We evaluated the effects of cinnamon essential oil (CEO) and its main component cinnamaldehyde (CA) on human corpus cavernosum (HCC) and rat CC. The essential oil of cinnamon was analyzed for the confirmation of the oil profile. HCC specimens from patients undergoing penile prosthesis surgery (age 48-69 years) were utilized for functional studies. In addition, erectile responses in anesthetized control and diabetic rats were evaluated in vivo after intracavernosal injection of CEO and CA, and rat CC strips were placed in organ baths. After precontraction with phenylephrine (10µM), relaxant responses to CEO and CA were investigated. CA (96.9%) was found as the major component. The maximum relaxation responses to CEO and CA were 96.4±3.5% and 96.0±5.0% in HCC and 97.5±5.5% and 96.8±4.8% in rat CC, respectively. There was no difference between control and diabetic rats in relaxation responses to CEO and CA. The relaxant responses obtained with essential oil and CA were not attenuated in the presence of nitric oxide synthase (NOS) inhibitor, and soluble guanylate cyclase inhibitor (sGS) in CC. In vivo, erectile responses in diabetic rats were lower than in control rats, which was restored after intracavernosal injection of CEO and CA. CEO and CA improved erectile function and relaxation of isolated strips of rat CC and HCC by a NO/cGMP-independent mechanism. Further investigations are warranted to fully elucidate the restorative effects of CEO and CA on diabetic erectile dysfunction.

Evaluation of smooth muscle relaxant potential of Bismarckia nobilis (Hildebr. & Wendl.) in diarrhea, hypertension and asthma by ex-vivo and in-vivo method / Evaluación del potencial relajante en músculo liso de Bismarckia nobilis (Hildebr. & Wendl.) en diarrea, hipertensión y asma por métodos ex vivo e in vivo

To explore the mechanistic basis behind smooth muscle relaxant prospective of Bismarckia nobilis in gastrointestinal, respiratory and cardiovascular ailments. The methanolic extract of B. nobilis and sub-fractions have been evaluated in vitro rabbit isolated tissues, in vivo castor oil-induced diarrhea in rats and charcoal meal activity in mice. The B. nobilis extract relaxed spontaneous and K+(80 mM)- induced contractions in rabbit isolated jejunum preparations, CCh (1 µM) and K+ (80 mM)-induced contractions in tracheal and bladder preparations, PE (1 µM) and K+ (80 mM)-induced concentrations in aorta preparations, likewise verapamil. Spasmolytic activity of dichloromethane fraction is stronger as compared to aqueous fraction. In vivo castor oil-induced diarrhea in rats and charcoal meal activity in mice further supported spasmolytic activity. B. nobilis extract possess anti-spasmodic, anti-diarrheal, airway relaxant and vasodilator activities possible mediated through calcium channel blocking mechanism, justifying therapeutic utility of B. nobilis in diarrhea, asthma and hypertension.

El objetivo de trabajo fue explorar el mecanismo de acción relacionado con el efecto relajante del músculo liso inducido por Bismarckia nobilis (B. nobilis) en enfermedades gastrointestinales, respiratorias y cardiovasculares. El extracto metanólico de B. nobilis y subfracciones fue evaluado in vitro en tejidos aislados de conejos. Además se evaluó diarrea in vivo inducida con aceite de ricino en ratas y la actividad de harina de carbón vegetal en ratones. El extracto de B. nobilis relajó tanto las contracciones espontáneas como las inducidas por K+(80 mM) en preparaciones de yeyuno aisladas de conejos, las contracciones inducidas por PE (1 µM) y K+(80 mM) inducidas en preparaciones de aorta; de manera similar a verapamilo. La actividad espasmolítica de la fracción de diclorometano es más potente en comparación con la fracción acuosa. La diarrea inducida in vivo por el aceite de ricino en ratas y la actividad de la harina de carbón vegetal en ratones apoyaron aún más la actividad espasmolítica. El extracto de B. nobilis posee actividades antiespasmódicas, antidiarreicas, relajantes de las vías respiratorias y vasodilatadoras, posibles a través del mecanismo de bloqueo de los canales de calcio, lo que justifica la utilidad terapéutica de B. nobilis en la diarrea, el asma y la hipertensión.

Relaxant effects of Peperomia hispidula (Sw.) A. Dietr. on isolated rat tracheal rings / Efecto relajante de Peperomia hispidula (Sw.) A. Dietr. sobre anillos aislados de tráquea de rata

Peperomia hispidula (Sw.) A. Dietr. is used in Mexican traditional medicine for treating respiratory illnesses such as asthma. The latter disorder results from an excessive and inappropriate constriction of airway smooth muscle. The aim of the present study was to evaluate the relaxant activity of P. hispidula on isolated rat tracheal rings contracted with carbachol. The methyleugenol was identified as the main active constituent in the dichloromethane extract. To explore the possible mechanism of action, concentration-response curves were constructed in the presence and absence of propranolol (3 µM), indomethacin (10 µM), glibenclamide (1 µM), and L-NAME (300 µM), finding that neither reduced methyleugenol-induced smooth muscle relaxation. In conclusion, P. hispidula herein displayed relaxant activity on rat tracheal rings. The effect of methyleugenol, was probably not related to the activation of ß2-adrenoceptors, prostaglandins, K+ATP channels or nitric oxide.

Peperomia hispidula (Sw.) A. Dietr. es utilizada en la medicina tradicional mexicana para tratar enfermedades respiratorias como el asma. Este último trastorno es el resultado de una contracción excesiva e inapropiada del músculo liso de las vías respiratorias. El objetivo del presente estudio fue evaluar la actividad relajante de P. hispidula sobre anillos aislados de tráquea de rata contraídos con carbacol. El metileugenol fue identificado como el principal constituyente activo en el extracto de diclorometano. Para explorar el posible mecanismo de acción, se construyeron curvas concentración-respuesta en presencia y ausencia de propranolol (3 µM), indometacina (10 µM), glibenclamida (1 µM), y L-NAME (300 µM), encontrando que ninguno redujo la relajación del músculo liso inducida por metileugenol. En conclusión, P. hispidula muestra actividad relajante en anillos de tráquea de rata. El efecto de metileugenol, al parecer no está implicado con la activación de los receptores ß2-adrenérgicos, prostaglandinas, canales de K+ATP u óxido nítrico.

Long-lasting endothelium-dependent relaxation of isolated arteries caused by an extract from the bark of Combretum leprosum / Extrato das cascas de Combretum leprosum causa relaxamento dependente de endotélio de longa duração em artérias isoladas

Objective To describe and to characterize the relaxing effect of an extract of the bark of Combretum leprosum on isolated arterial rings from different animals.Methods Rings (3 to 4mm) from rabbit, rat, or porcine arteries rings were suspended in an organ bath (Krebs, 37°C, 95%O2/5%CO2) to record isometric contractions. After the stabilization period (2 to 3 hours) contractions were induced by the addition of phenylephrine (0.1 to 0.3µM) or U46619 (10 to 100nM), and Combretum leprosum extract was added on the plateau of the contractions. Experiments were performed to determine the potency, duration, reversibility, and to get insights on the potential mechanism involved in extract-induced relaxations.Results In all rings tested, Combretumleprosum extract (1.5μg/mL) was able to cause relaxations, which were strictly endothelium-dependent. In rabbit or rat thoracic aorta rings, the relaxations were reversed by vitamin B12a or L-NG-nitroarginine. In porcine right coronary arteries and rabbit abdominal aorta, extract caused both L-NG-nitroarginine-sensitive and L-NG-nitroarginine-resistant relaxations. In rabbit thoracic aorta, the extract was relatively potent (EC50=0.20µg/mL) and caused relaxations; intriguingly the endothelium continued to produce relaxing factors for a long period after removing the extract. The magnitude of extract-induced relaxations was significantly reduced in the absence of extracellular Ca2+; in addition, the TRPs channels blocker ruthenium red (10µM) was able to revert extract-induced relaxations. Phytochemical analyses indicated that the extract was rich in polyphenol-like reacting substances.ConclusionsCombretum leprosum extract contains bioactive compounds capable of promoting Ca2+-dependent stimulation of endothelial cells which results in a prolonged production of relaxing factors.

Objetivo Descrever e caracterizar os relaxamentos induzidos por um extrato das cascas de Combretum leprosum em anéis de artérias de diferentes espécies de animais.Métodos Anéis (3 a 4mm) de artérias de coelho, rato e porco foram montados em cubas para órgão isolado (Krebs, 37°C, 95%O2/5%CO2) para registro das contrações isométricas. Após um período de estabilização (2 a 3 horas), as contrações foram induzidas com fenilefrina (0,1 a 0,3µM) ou U46619 (10 a 100nM); no platô dessas contrações, adicionamos o extrato Combretum leprosum. Diferentes protocolos foram realizados para determinar potência, duração, reversibilidade e mecanismo dos relaxamentos induzidos pelo extrato.Resultados Em todas as preparações testadas, o extrato de Combretum leprosum (1,5µg/mL) provocou relaxamentos dependentes de endotélio. Em aorta torácica de coelho ou rato, os relaxamentos foram revertidos pela vitamina B12a ou L-NG-nitro-arginina. Em anéis de aorta abdominal de coelho e de artérias coronárias de porco, o extrato causou relaxamentos sensíveis e resistentes à L-NG-nitro-arginina. Em aorta torácica de coelho, o extrato foi relativamente muito potente (EC50=0,20μg/mL) e quando causou relaxamentos; intrigantemente o endotélio continuou a produzir fatores relaxantes por um longo período após remoção do extrato. A magnitude dos relaxamentos induzidos pelo extrato foi significativamente reduzida em ausência Ca2+ extracelular; ademais, o vermelho de rutênio (10μM), um bloqueador de canais TRPs, foi capaz de reverter os relaxamentos induzidos pelo extrato. Análises preliminares indicaram que o extrato continha compostos com reatividade química semelhante à polifenóis.Conclusão O extrato de Combretum leprosum contem compostos bioativos capazes de promover estimulação dependente de Ca2+ das células endoteliais a qual resulta numa produção prolongada de fatores relaxantes.

Association of acepromazine with propofol in giant amazon turtles Podocnemis expansa reared in captivity / Associação da acepromazina com propofol em tartarugas-da-amazônia Podocnemis expansa criadas em cativeiro

PURPOSE: To evaluate the effects of different concentrations of an anesthetic association in giant amazon turtles (Podocnemis expansa). METHODS: Twenty healthy P. expansa of both sexes weighing between 1.0 and 1.5kg commercially bred in the Araguaia River Valley, Goias, Brazil, were separated into two groups (G1 n=10 and G2 n=10). Each group received a respective protocol: P1= acepromazine (0.5 mg/kg IM) and propofol (5 mg/kg IV) and P2 = acepromazine (0.5 mg/kg IM) and propofol (10 mg/kg IV). The acepromazine was administered in the left thoracic member and the propofol in the cervical vertebral sinus. Assessments were made of the anesthetic parameters of locomotion, muscle relaxation, response to pain stimuli in the right thoracic and pelvic members and heartbeat. RESULTS: The anesthetic induction time was the same for both protocols (P1 and P2); however the P2 effects were of a longer duration. CONCLUSION: The sedation achieved with both protocols (P1 and P2) were satisfactory for the biological sample collection, physical examinations and minor surgeries on this species.

OBJETIVO: Avaliar os efeitos de uma associação anestésica com diferentes concentrações em tartarugas-da-amazônia (Podocnemis expansa). MÉTODOS: Vinte P. expansa, hígidas, de ambos os sexos, com massa corporal entre 1,0 e 1,5 kg, de um criatório comercial localizado no vale do rio Araguaia, Goiás, Brasil, foram distribuídas em dois grupos (G1 n=10 e G2 n=10). Cada grupo recebeu um protocolo sendo: P1 = acepromazina (0,5 mg/kg IM) e propofol (5 mg/kg IV) e P2 = acepromazina (0,5 mg/kg IM) e propofol (10 mg/kg IV), aplicados nos grupos G1 e G2, respectivamente. A acepromazina foi aplicada no membro torácico esquerdo e o propofol no seio vertebral cervical. Foram avaliados os parâmetros anestésicos: locomoção, relaxamento muscular, resposta aos estímulos dolorosos no membro torácico direito e nos membros pelvinos e frequência cardíaca. RESULTADOS: O tempo de indução anestésica foi o mesmo para ambos os protocolos (P1 e P2), porém o P2 apresentou efeitos mais duradouros. CONCLUSÃO: As sedações obtidas por esses protocolos (P1 e P2) foram satisfatórias para a colheita de amostras biológicas, exames físicos e realização de pequenos procedimentos cirúrgicos nesta espécie.

Association of midazolam with ketamine in giant Amazon river turtles Podocnemis expansa breed in captivity / Associação de midazolam com cetamina em tartarugas da Amazônia Podocnemis expansa de cativeiro

PURPOSE: Evaluate the effects of two anesthetic associations in giant Amazon river turtles (P. expansa). METHODS: Twenty P. expansa, healthy, of both sexes, with weights between 1.0 and 1.5 kg of a commercial breeding facility located in the valley of the Araguaia River, Goiás, Brazil, were divided into two groups ( G1 n = 10 and G2 n = 10). Each group received a protocol being: P1 = midazolam (2 mg/kg IM) and ketamine (20 mg/kg IM) and P2 = midazolam (2 mg/kg IM) and ketamine (60 mg/kg IM), applied on G1 and G2, respectively. The drugs were applied in the left forelimb. The clinical parameters evaluated were: locomotion, muscle relaxation, response to pain stimuli in the right thoracic and pelvic members and heart rate. These assessments were made at time 0 (immediately after injection) and times of 5, 10, 20, 30, 45, 60, 90, 120, 150 and 180 minutes after the injections. RESULTS: Group 2 showed a higher heart rate than G1 and more rapid and prolonged immobilization. CONCLUSION: The sedation scores obtained by these protocols (P1 and P2) were satisfactory, with possible pharmacological contention for collecting biological samples and physical examination in P. expansa.

OBJETIVO: Avaliar os efeitos de duas associações anestésicas em tartarugas da Amazônia em (Podocnemis expansa). MÉTODOS: Vinte P. expansa, hígidas, de ambos os sexos, com massa corporal entre 1,0 e 1,5 kg, de um criatório comercial localizado no vale do rio Araguaia, Goiás, Brasil, foram distribuídas em dois grupos (G1 n=10 e G2 n=10). Cada grupo recebeu um protocolo sendo: P1 = midazolam (2 mg/kg IM) com cetamina (20 mg/kg IM) e P2 = midazolam (2 mg/kg IM) com cetamina (60 mg/kg IM), aplicados nos grupos G1 e G2, respectivamente. Os fármacos foram aplicados no membro torácico esquerdo. Os parâmetros clínicos avaliados foram: locomoção, relaxamento muscular, resposta aos estímulos dolorosos nos membros torácico direito e pelvinos e freqüência cardíaca. Essas avaliações foram feitas no tempo 0 (imediatamente após a injeção) e nos tempos 5, 10, 20, 30, 45, 60, 90, 120, 150 e 180 minutos após as injeções. RESULTADOS: O G2 apresentou maior freqüência cardíaca que o G1 e imobilização mais rápida e prolongada. CONCLUSÃO: As sedações obtidas por esses protocolos (P1 e P2) foram satisfatórias, sendo possível a contenção farmacológica para a coleta de amostras biológicas e exame físico em P. expansa.

Relaxant effects of different fractions from Tymus vulgaris on guinea-pig tracheal chains

In previous studies, the relaxant effect of Tymus vulgaris has been demonstrated on guinea pig tracheal chains. Therefore, in the present study, the relaxant effects of n-hexane, dichloromethane, methanol and aqueous fractions of Tymus vulgaris on tracheal chains of guinea pigs were examined. The relaxant effects of four cumulative concentrations of each fraction (0.4, 0.8, 1.2 and 1.6 g%) in comparison to saline as negative control and four cumulative concentrations of theophylline (0.2, 0.4, 0.6 and 0.8 mM) were examined for their relaxant effects on precontracted tracheal chains of guinea pig by 60 mM KCl (group 1) and 10 ìÌ methacholine (group 2, n = 7 for each group). In group 1, all concentrations of the n-hexane fraction and theophylline and three last concentrations (0.8, 1.2 and 1.6 g%) of dichloromethane and two higher concentrations (1.2 and 1.6 g%) of methanol fractions showed significant relaxant effects compared to that of saline (p<0.05 to p<0.001). In group 2, all concentrations of theophylline, n-hexane and dichloromethane fractions and three concentrations (0.8, 1.2 and 1.6 g%) of methanol and two higher concentrations (1.2 and 1.6 g%) of aqueous fractions showed significant relaxant effects compared to that of saline (p<0.05 to p<0.001). In addition, with group 1, the relaxant effect of all concentrations of all fractions except the n-hexane fraction, were significantly less than those of theophylline (p<0.05 to p<0.001). The n-hexane fraction showed higher relaxant effect than theophylline. The relaxant effect of all concentrations of the n-hexane fraction and the three last concentrations (0.8, 1.2 and 1.6 g%) of dichloromethane and aqueous fractions were significantly greater in group 2 than in group 1 (p<0.05 to p<0.001). There were significant positive correlations between the relaxant effects and concentrations for theophylline and all fractions (except aqueous fraction in group 1) in both groups, but a negative correlation for the aqueous fraction in group 1 (p<0.05 to p<0.001). These results showed a potent relaxant effect for n-hexane and weaker relaxant effect for other fractions from Tymus vulgaris on tracheal chains of guinea pigs.

Effects of marmin, a compound isolated from Aegle marmelos Correa, on contraction of the guinea pig-isolated trachea

Marmin or 7-[6', 7'-dihydroxygeranyl-oxy] coumarin is a compound isolated from Aegle marmelos Correa. In the study, we examined the effects of marmin on the contraction of guinea pig-isolated trachea stimulated by several inducers, namely histamine, metacholine, compound 48/80. We also evaluated its action against contraction induced by extracellular or intracellular calcium ion. The possibility of marmin to potentiate the

elaxation effect of isoprenaline was also studied. Marmin added in the organ bath at 10 min prior to the agonist inhibited the contraction elicited by histamine and metacholine in a concentration-dependent manner. Moreover, marmin antagonized the histamine-induced contraction in competitive manner. Marmin mildly potentiated the relaxation effect of isoprenaline. In the study, marmin abrogated the contraction of tracheal smooth muscle induced by compound 48/80, an inducer of histamine release. Besides, marmin successfully inhibited CaCl[2-]-induced contraction in Ca[2+] -free Krebs solution. Marmin also inhibited two phases of contraction which were consecutively induced by metacholine and CaCl[2] in Ca[2+]-free Krebs solution. Based on the results we concluded that marmin could inhibit contraction of the guinea-pig tracheal smooth muscle, especially by interfering histamine receptor, inhibiting the histamine release from mast, inhibiting intracellular Ca[2+] release from the intracellular store and the Ca[2+] influx through voltage-dependent Ca[2+] channels

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.

Pharmacological restraint of captivity giant Amazonian turtle Podocnemis expansa (Testudines, Podocnemididae) with xylazine and propofol / Contenção farmacológica de tartaruga da Amazônia Podocnemis expansa (Testudines, Podocnemididae) de cativeiro com xilazina e propofol

PURPOSE: Identify a technique to induce brief sedation and hypnosis in Podocnemis expansa. METHODS: Twenty commercially bred P. expansa, weighing on average 1.2 ± 0.24 kg, were subjected to two protocols: G1 was given 1.5 mg/kg IM of xylazine and 5 mg/kg IV of propofol, while G2 received 1.5 mg/kg IM of xylazine and 10 mg/kg IV of propofol. The drugs were applied, respectively, in the left thoracic member and in the cervical vertebral sinus. Assessments were made of the anesthetic parameters of locomotion, muscle relaxation, response to pain stimuli in the right thoracic members, pelvic members and tail, easy handling and heartbeat, as well as ambient temperature and glycemic level. RESULTS: A consistent hypnotic effect was recorded 49.6 ± 22.1 seconds in G2 and after 58.2 ± 55.1 in G1. All the animals of G2 recovered in 198 minutes, and those of G1 in 156 minutes. CONCLUSION: The hypnosis achieved with these associations was satisfactory, and G1 was as efficient as G2, allowing for the pharmacological restraint for the collection of biological samples, physical examinations and minor surgeries on these species.

OBJETIVO: Identificar uma técnica para se induzir sedação e hipnose em Podocnemis expansa. MÉTODOS: Vinte Podocnemis expansa de criatório comercial, com média de peso 1,2 ± 0,24 kg, foram submetidas a dois protocolos: G1 recebeu xilazina 1,5 mg/kg IM e propofol 5 mg/kg IV e o G2 xilazina 1,5 mg/kg IM e propofol 10 mg/kg IV. As drogas foram aplicadas no membro torácico esquerdo e no seio vertebral cervical, respectivamente. Observaram-se os parâmetros anestésicos: locomoção, relaxamento muscular, resposta aos estímulos dolorosos no membro torácico direito, nos membros pelvinos e na cauda, facilidade de manipulação e freqüência cardíaca, além da temperatura ambiental e glicemia. RESULTADOS: Um efeito hipnótico consistente foi observado aos 49,6 ± 22,1 segundos no G2 e 58,2 ± 55,1 segundos no G1. A recuperação de todos os animais do G2 ocorreu em 198 minutos, e em 156 minutos no G1. CONCLUSÃO: A hipnose obtida por essas associações foi satisfatória e o Grupo 1 foi tão eficiente quanto o Grupo 2, o que possibilita a contenção farmacológica para coleta de amostras biológicas, exames físicos e realização de pequenas cirurgias nesta espécie.

Effects of 4-[2-Alkylthio-1-benzyl-5-imidazolyl]-dihydropyridines on the isolated rat colon and right atrium contractility

In order to provide a pharmacological profile for some newly synthesized dihydropyridines, we investigated their effects on the isolated rat colon segments and the isolated rat atrium contractility. The tested compounds include alkyl ester analogues of nifedipine, in which the ortho-nitrophenyl group at position 4 is replaced by 2-alkylthio-1-benzyl-5-imidazolyl substituent, and nifedipine as a positive control substance. Isolated rat colon and atrial tissues were prepared. Rat colon was contracted with 80 mM KC1, and maximum response was recorded [100%]. After washing tissue with Krebs solution it was preincubated with different concentrations of test compounds and again KC1 was added and percent change in contraction was calculated. Spontaneous contractions and its frequency for colon and atrium before and after addition of test compounds were also recorded and percent change was calculated. Nifedipine [10[-8]-10[-5] M] was used as positive control at all experiments. The compounds showed similar effects to that of nifedipine on the isolated rat colon. The potency of these analogues with concentration range 10[-5] to 10[-4] M was compared to potency of nifedipine which was effective at 10[-8] to 10[-5] M [P<0.01]. However, unlike nifedipine, the test compounds exerted significant positive inotropic effect on the isolated rat atrium [P < 0.01]. Our observations suggest that these analogues of nifedipine selectively enhance contractility of heart muscle while causing relaxation of intestinal smooth muscle. These compounds may serve as valuable probes to develop novel dihydropyridines with dual smooth muscle relaxant effect and positive inotropic action

contribution of nitric oxide on the relaxation effects of diethylstilbestrol

To evaluate the contribution of nitric oxide NO on the relaxation effects of diethylstilbestrol on rat uterus. Uterine rings from 8 nonpregnant Wistar Albino rats 300-350g in the pro-estrous phase were suspended in an organ bath and electrical field stimulation applied for recording isometric tension. The influence of NO on contractile responses of rat uterine rings was investigated. The effects of NO precursor L-arginine 10-7-10-4M concentration and NO synthase inhibitor L-nitro-arginine-methyl ester 10-7-10-4M concentration and a combination of them on contractile responses were studied in the presence and absence of diethylstilbestrol 2x10-4M concentration. The study was carried out at the Department of Pharmacology Laboratory, Faculty of Medicine, Dicle University, Diyarbakir, Turkey. Totally, 30 samples were investigated n=6 for each group, 5 groups. Diethylstilbestrol inhibited contractile responses 64.2 +/- 4.5% n=6, p<0.05. Contractile responses decreased in the presence of L-arginine n=6, p<0.05 and this inhibition was abolished in the presence of L-nitro-arginine-methyl ester n=6, p<0.05. The inhibition on contractile responses to diethylstilbestrol was potentiated in the presence of L-arginine under similar conditions n=6, p<0.05. The contractile responses to electrical field stimulation in the presence of diethylstilbestrol were not affected by L-nitro-arginine-methyl ester n=6, p>0.05. These data provide evidence that NO may potentiate the inhibitory effects of diethylstilbestrol by different mechanisms on the electrically induced contractions of the non-pregnant rat uterus

Lead acetate induced contraction in rat tracheal smooth muscle is independent of epithelium.

Airways are the primary target of lead exposure from atmospheric pollution, its effect on airway smooth muscle and their responsiveness to bronchoactive agents is not clearly understood. In the present investigation the effect of lead on the isolated airway smooth muscle activity was studied in organ bath set-up. Further the involvement of airway epithelium was examined and the responsiveness of airway smooth muscle to adenosine, acetylcholine (bronchoconstrictors) and isoproterenol (bronchodilator) was also investigated. Lead in concentration of 10(-12) M to 10(-4) M produced concentration-dependant contractile response in rat tracheal rings. Acetylcholine and adenosine induced concentration-dependent contractile response was slightly inhibited after lead exposure. The relaxant response to isoproterenol was also inhibited in lead exposed tissues. Epithelium removal did not significantly change the contractile response to lead suggesting that the lead induced contraction of airway smooth muscle is epithelium independent.

Involvement of potassium channels in hypoglycemic effect of sertraline.

Effect of 21 days administration of sertraline (30 mg/kg, po) in streptozotocin (55 mg/kg, ip) induced diabetic and non-diabetic rats produced hypoglycemia in diabetic and non-diabetic rats. Pinacidil (1mg/kg, po), when co-administered with sertraline or glimepiride antagonized the decrease in glucose levels in diabetic rats. Pinacidil (10(-6)-10(-3) M) produced dose dependent relaxation (EC50-1.58 x 10(-5) M). Neither sertraline nor glimepiride had any effect on the resting tension of ileum preparation. Both sertraline and glimepiride antagonized competitively the pinacidil-induced relaxation. The pA2 values of sertraline and glimepiride reversal of pinacidil-induced relaxation were 5.5 and 6.2 respectively. These studies suggest the involvement of K+ channels in hypoglyceimic effects of sertraline.

Effect of some adenosine compounds on smooth muscles of the sheep bladder Osteius ovis L.

Purines have widespread and specific extracellular signalling actions in the regulation of a variety of functions in many tissues of both invertebrates and vertebrates. The effect of some adenosine compound on sheep bladder smooth muscle contraction induced by KCI and ACh was investigated invitro. Preparations were prepreated with adenosine or ATP befor agonist exposure. It was found that adenosine inhibited K- induced contracture and enhanced Ach-induced contracture. These actions were blocked by P[1] antagonist theophylline. The results also show that ATP potentiated both KCI and ACh induced contracture. Theses actions antagonized by P[2] receptor antagonist Quinidine. These results suggest that blader smoth muscle may have A[1], A[2] and P[2x] receptors

Effects of ligustrazine on the contraction of isolated rabbit corpus cavernosum strips / 华中科技大学学报（医学）（英德文版）

To investigate the role of ligustrazine on relaxation of the isolated rabbit corpus cavernosum tissue in vitro, the effects of ligustrazine on the corpus cavernosum were observed by using experimental method of smooth muscle strips. Concentration-responses to phenylephine (PE) and KCl were recorded. The results showed that ligustrazine concentration-dependently depressed the contraction response of smooth muscle strips induced by PE. The maximum percentage relaxation of cavernosal strips by ligustrazine was 74.1% +/- 6.2% (compared with control: 21.9% +/- 5.6%, P < 0.01). Ligustrazine concentration-dependently reduced the amplitude of the contraction induced by cumulative doses of PE or KCl, shifted the cumulative concentration response curves of PE and KCI to the right and depressed their maximal responses. It was concluded that ligustrazine could significantly relax the cavernosal muscle contraction induced by PE in vitro. The results suggested that ligustrazine inhibited calcium ion influx.

The Gonyautoxin 2/3 epimers reduces anal tone when injected in the anal sphincter of healthy adults

The primary clinical symptom of Paralytic Shellfish Poisoning is acute paralytic illness produced by paralyzing toxins. Paralytic shellfish poison is formed by a mixture of phycotoxins and their toxicity is due to its reversible binding to a receptor site on the voltage-gated sodium channel on excitable cells, thus blocking neuronal transmission. We studied the effect of the gonyautoxin 2/3 epimers by local infiltration in the anal internal sphincter of healthy voluntary adults in order to reduce anal tone. The toxin was injected after prior clinical evaluation, anoscopy and anorectal manometry. Post injection clinical examination, electromyography and anorectal manometry were performed. Resting and voluntary contraction pressures were measured and the anorectal inhibitory and anocortical reflexes were tested by manometry. Blood and urine samples were obtained from each participant, and hemogram, basic metabolic panel, and urinalysis were done both before and one week after the injection. This study shows, for the first time, that gonyautoxin 2/3 reduces the anal tone by relaxing the anal sphincters in 100 % of the participants. Manometric recordings showed a significant decrease in anal maximal voluntary contraction pressure after the toxin injection, dropping to 55.2 ± 6.2 % and 47.0 ± 6.8 % (Mean Value ± Std.Dev.) of the baseline values at 2 minutes and at 24 hours respectively after the injection. Post-injection electromyography showed that activity of the muscle was abolished. We conclude that local administration of gonyautoxin 2/3 to the anal sphincter produces immediate relaxation and a statistically significant decrease in the anal tone (p <0.001)..

Could rapacuronium and rocuronium be a valid alternative to succinylcholine for rapid sequence induction of anesthesia in adults?

The intubating conditions provided by rapacuronium [Org 9487], rocuronium and succinylcholine after rapid sequence induction of anesthesia in adults undergoing surgery [elective or emergency] were assessed in this study. A total of 100 ASA I or II studied patients was randomly allocated to one of three treatment groups according to the muscle relaxant used [rapacuronium, rocuronium and succinylcholine]. Both rapacuronium and rocuronium groups were divided into two subgroups according to the dose used to rapacuronium [2 and 2.5 mg/kg] and rocuronium [0.6 and 1 mg/kg]. All patients received the same induction agents [fentanyl 1-2 ug/kg and propofol 1.5-2 mg/kg]. Fentanyl was injected intravenously four minutes before propofol injection, followed by a period of three-minute preoxygenation. The study concluded that 60 seconds after the administration of rapacuronium [2 or 2.5 mg/kg] or rocuronium [1 mg/kg], clinically acceptable intubating conditions were achieved as frequent as after succinylcholine during rapid sequence induction of anesthesia in adults given fentanyl and propofol as induction agents