Effect of pupil dilation on intraocular pressure in preterm and term infants / O efeito da dilatação da pupila na pressão intraocular em bebês pré-termo e a termo

ABSTRACT Purpose: To evaluate the effect of pupil dilation on intraocular pressure in preterm and term newborns. Methods: This prospective study involved 55 eyes of 28 preterm infants and 38 eyes of 20 term infants. The infants were divided into two groups according to their gestational ages at birth as follows: preterm group, <37 weeks and term group, ≥37 weeks. Pupil dilation was attained with tropicamide 0.5% and phenylephrine 2.5%. Intraocular pressure measurements were performed with Icare PRO (Icare Finland Oy, Helsinki, Finland) before and after pupil dilation. A paired t test was used to compare the measurements before and after pupil dilation. Results: The mean intraocular pressure change was -1.04 ± 3.03 mmHg (6.20/-11.40 mmHg) in the preterm group and -0.39 ± 2.81 mmHg (4.60/-9.70 mmHg) in the term group. A statistically significant difference in intraocular pressure was observed only in the preterm group after pupil dilation (p=0.01). Conclusion: An unexpected alteration in intraocular pressure in newborns may occur after pupil dilation, especially in preterm infants.

RESUMO Objetivo: Avaliar o efeito da dilatação da pupila sobre a pressão intraocular em recém-nascidos pré-termo e a termo. Métodos: Este estudo prospectivo envolveu 55 olhos de 28 bebês pré-termo e 38 olhos de 20 bebês a termo. Os bebês foram divididos em dois grupos, pré-termo e a termo, de acordo com a idade gestacional ao nascimento: grupo pré-termo <37 semanas; grupo a termo ≥37 semanas. A dilatação da pupila foi feita com tropicamida 0,5% e fenilefrina 2,5%. As medições da pressão intraocular foram realizadas com Icare PRO (Icare Finland Oy, Helsinki, Finlândia) antes e depois da dilatação da pupila. O teste t pareado foi usado para comparar as medidas antes e depois da dilatação da pupila. Resultados: A alteração média da pressão intraocular foi de -1,04 ± 3,03 mmHg (+6,20/-11,40 mmHg) no grupo pré-termo e -0,39 ± 2,81 mmHg (+4,60/-9,70 mmHg) no grupo a termo. Uma diferença estatisticamente significativa na pressão intraocular foi observada apenas no grupo pré-termo após a dilatação da pupila (p=0,01). Conclusão: Após a dilatação da pupila, pode ocorrer alteração inesperada da pressão intraocular em recém-nascidos, principalmente em bebês pré-termo.

Queratoconjuntivitis por fenilefrina confirmada con pruebas alérgicas tras una exploración ordinaria / Phenylephrine keratoconjunctivitis confirmed by allergy testing after routine examination

Las reacciones alérgicas tras el uso de colirios oftálmicos son comunes y pueden manifestarse con queratoconjuntivitis y dermatitis periorbitaria. La introducción reciente de nuevos fármacos tópicos facilita la sospecha clínica, pero en ocasiones se trata de un uso simultáneo de varios medicamentos y la identificación del alérgeno específico se convierte en un reto. Debido a ello, en muchas ocasiones el diagnóstico es de exclusión, ya que no se llega a confirmar con estudio alergológico el agente desencadenante de la reacción. Tal es el caso de la alergia ocular a fenilefrina, dado que son pocos los cuadros clínicos descritos en la literatura donde hay una clara causa inmunológica. Presentamos un caso poco frecuente, una forma grave de queratoconjuntivitis alérgica tras un examen oftalmológico ordinario confirmada tras estudio alergológico completo

Allergic reactions after using ophthalmic eye drops are very common and frequently manifested by ketaconjuntivitis and periorbital dermatitis. Previous introduction of new topical drugs makes the clinical suspicion easier but sometimes the patient uses multiple medications simultaneously and the specific allergen identification become a challenge. That is the reason why in many occasions the diagnosis is of exclusion since the agent triggering the reaction is not confirmed with an allergologic study. Such is the case of ocular allergy to phenylephrine: there are few clinical cases where there is a clear immunologic cause. We report an uncommon case of a patient who develops a severe form of allergic keratoconjuntivitis after routine ophthalmological examination confirmed by complete allergologic study

The effect of epinephrine for the treatment of spinal-hypotension: comparison with norepinephrine and phenylephrine, clinical trial / O efeito de epinefrina, norepinefrina e fenilefrina no tratamento da hipotensão pós-raquianestesia: estudo clínico comparativo

Abstract Background and objectives: Limited data are present on safety and efficiency of epinephrine for the prophylaxis and treatment of spinal-hypotension. This study was conducted to compare the effect of epinephrine with norepinephrine and phenylephrine on the treatment of spinal-hypotension and ephedrine requirement during cesarean delivery. Methods: One hundred and sixty parturients with uncomplicated pregnancies undergoing elective cesarean delivery under spinal anesthesia were recruited. They were allocated randomly to receive norepinephrine 5 µg.mL−1 (n = 40), epinephrine 5 µg.mL−1 (n = 40), phenylephrine 100 µg.mL−1 (n = 40) or 0.9% saline infusions (n = 40) immediately after induction of spinal anesthesia. Whenever systolic blood pressure drops to less than 80% of baseline, 5 mg of intravenous ephedrine was administered as rescue vasopressor. The incidence of hypotension, total number of hypotension episodes, the number of patients requiring ephedrine, the mean amount of ephedrine consumption and side effects were recorded. Results: There was no statistically significant difference in incidence of maternal hypotension between groups. The number of patients requiring ephedrine was significantly greater in group saline than in group phenylephrine (p< 0.001). However, it was similar between phenylephrine, norepinephrine, and epinephrine groups. The mean ephedrine consumption was significantly higher in group saline than in norepinephrine, epinephrine, phenylephrine groups (p= 0.001). Conclusion: There is no statistically significant difference in incidence of hypotension and ephedrine consumption during spinal anesthesia for cesarean delivery with the use of epinephrine when compared to norepinephrine or phenylephrine. Epinephrine can be considered an alternative agent for management of spinal hypotension.

Resumo Justificativa e objetivos: Existem dados limitados sobre segurança e eficiência da epinefrina na profilaxia e tratamento da hipotensão arterial associada à raquianestesia. O presente estudo foi realizado para comparar o efeito da epinefrina com norepinefrina e fenilefrina no tratamento da hipotensão após raquianestesia e necessidade de efedrina durante o parto cesáreo. Método: Foram recrutadas 160 parturientes com gestações não complicadas, submetidas a cesariana eletiva sob raquianestesia. Elas foram alocadas aleatoriamente para receber norepinefrina 5 µg.mL-1 (n = 40), epinefrina 5 µg.mL-1 (n = 40), fenilefrina 100 µg.mL-1 (n = 40) ou infusão de solução fisiológica NaCl a 0,9% (n = 40) imediatamente após a indução da raquianestesia. Sempre que houvesse redução da pressão arterial sistólica para valor inferior a 80% da linha de base, 5 mg de efedrina iv eram administrados como vasopressor de resgate. A incidência de hipotensão, o número total de episódios de hipotensão, o número de pacientes que necessitaram de efedrina, o consumo médio de efedrina e os efeitos colaterais foram registrados. Resultados: Não houve diferença estatisticamente significante na incidência de hipotensão materna entre os grupos. O número de pacientes que necessitaram de efedrina foi significantemente maior no grupo solução fisiológica do que no grupo fenilefrina (p< 0,001). No entanto, foi semelhante entre os grupos fenilefrina, norepinefrina e epinefrina. O consumo médio de efedrina foi significantemente maior no grupo solução fisiológica do que nos grupos norepinefrina, epinefrina e fenilefrina (p = 0,001). Conclusão: Não houve diferença estatisticamente significante na incidência de hipotensão e consumo de efedrina durante raquianestesia para parto cesáreo com uso de epinefrina quando comparada à norepinefrina ou fenilefrina. A epinefrina pode ser considerada como agente alternativo para o tratamento da hipotensão após raquianestesia.

[The effect of epinephrine for the treatment of spinal-hypotension: comparison with norepinephrine and phenylephrine, clinical trial]. / O efeito de epinefrina, norepinefrina e fenilefrina no tratamento da hipotensão pós­raquianestesia: estudo clínico comparativo.

BACKGROUND AND OBJECTIVES: Limited data are present on safety and efficiency of epinephrine for the prophylaxis and treatment of spinal-hypotension. This study was conducted to compare the effect of epinephrine with norepinephrine and phenylephrine on the treatment of spinal-hypotension and ephedrine requirement during cesarean delivery. METHODS: One hundred and sixty parturients with uncomplicated pregnancies undergoing elective cesarean delivery under spinal anesthesia were recruited. They were allocated randomly to receive norepinephrine 5 µg.mL-1 (n=40), epinephrine 5 µg.mL-1 (n=40), phenylephrine 100 µg.mL-1 (n=40) or 0.9% saline infusions (n=40) immediately after induction of spinal anesthesia. Whenever systolic blood pressure drops to less than 80% of baseline, 5 mg of iv ephedrine was administered as rescue vasopressor. The incidence of hypotension, total number of hypotension episodes, the number of patients requiring ephedrine, the mean amount of ephedrine consumption and side effects were recorded. RESULTS: There was no statistically significant difference in incidence of maternal hypotension between groups. The number of patients requiring ephedrine was significantly greater in group saline than in group phenylephrine (p <0.001). However, it was similar between phenylephrine, norepinephrine, and epinephrine groups. The mean ephedrine consumption was significantly higher in group saline than in norepinephrine, epinephrine, phenylephrine groups (p=0.001). CONCLUSION: There is no statistically significant difference in incidence of hypotension and ephedrine consumption during spinal anesthesia for cesarean delivery with the use of epinephrine when compared to norepinephrine or phenylephrine. Epinephrine can be considered as an alternative agent for management of spinal hypotension.

Effect of phenylephrine on static and dynamic accommodation.

PURPOSE: We tested the hypothesis that changes in accommodation after instillation of Phenylephrine Hydrochloride (PHCl) observed in some studies could be caused by changes in optics. METHODS: We performed two experiments to test the effects of PHCl on static and on dynamic accommodation in 8 and 6 subjects, respectively. Objective wavefront measurements were recorded of the static accommodation response to a stimulus at different distances or dynamic accommodation response to a sinusoidally moving stimulus (between 1 and 3 D of accommodative demand at 0.2Hz). The responses were characterized using two methods: one that takes into account the mydriatic optical effects on the accommodation produced by higher-order aberrations of the eye and another that takes into account only power changes paraxially due to the action of the ciliary muscle and regardless of the pupil size. RESULTS: When mydriatic optical effects were taken into account, differences in responses before and after PHCl instillation were 0.51±0.53 D, and 0.12±0.15, for static and dynamic accommodation, respectively, and were statistically significant (p<0.039). When mydriatic optical effects were not taken into account, the differences in responses before and after PHCl instillation were -0.20±0.51 D, and -0.05±0.14, for static and dynamic accommodation, respectively, and were not statistically significant (p>0.313). CONCLUSIONS: The mydriatic effect of the PHCl causes optical changes in the eye that can reduce the objective and subjective measurement of accommodation.

Eficacia de fenilefrina en la prevención de hipotensión en cesárea bajo anestesia subaracnoidea / Effectiveness of phenylefrine in prevention of hypotension during spinal anesthesia for cesarean delivery

Resumen Introducción: la hipotensión es el evento adverso más incidente cuando se administra anestesia subaracnoidea para cesárea; múltiples estrategias para su prevención y manejo se han propuesto, entre ellas el uso de vasopresores profilácticos con resultados no concluyentes. Objetivo: evaluar la eficacia preventiva del uso de Fenilefrina en la hipotensión arterial inducida por la anestesia subaracnoidea en gestantes llevadas a cesárea. Materiales y Métodos: ensayo clínico controlado, doble ciego, en gestantes, mayores de 18 años, ASA 1 y 2, quienes recibieron anestesia subaracnoidea para cesárea, fueron aleatorizadas a recibir placebo o infusión profiláctica de fenilefrina 40 mcg/min, durante 5 minutos. Resultados: se incluyeron 140 pacientes en el análisis de datos. La incidencia de hipotensión fue mayor en el grupo control que en el intervenido (RA 45,71% vs 32,85%). Sin presentarse diferencias significativas entre ambos grupos (p=0,119). RR de hipotensión en el grupo intervenido fueron menores, independiente del criterio de hipotensión (tensión arterial sistólica, RR 0,72 (IC95% 0,47-1,09); tensión arterial media, RR 0.93 (IC95% 0,64-1,37); TAS o TAM RR 0.86 (IC95% 0,62-1,21)), pero sin diferencias significativas p>0,05. El uso de vasopresores en los pacientes que presentaron este evento se dio en 75.4% (n=52), con RR mayor en el grupo control y diferencias significativas al evaluar los dos grupos. (RR: 1,4 p=0,032). Conclusiones: fenilefrina profiláctica no demostró ser eficaz en disminuir la incidencia de hipotensión; sin embargo, sí se asocia con una disminución significativa en los requerimientos de vasopresores, así como en la incidencia de náuseas y vómito. MÉD.UIS. 2018;31(2):33-9.

Abstract Background: Hypotension is the most common adverse event when subarachnoid anesthesia is administered for cesarean section; multiple strategies for its prevention and management have been proposed, including the use of prophylactic vasopressors with inconclusive results. Objective: To evaluate the preventive efficacy of the use of phenylephrine in hypotension induced by subarachnoid anesthesia in pregnant women taken to caesarean section. Methods: A double-blind, controlled clinical trial in pregnant women, older than 18 years old, ASA 1 and 2, who received a subarachnoid anesthesia for cesarean section, were randomized to receive placebo or prophylactic infusion of phenylephrine 40 mcg / min, for 5 minutes. Results: 140 patients were included in data analysis. Incidence of hypotension was higher in the control group than in the intervention group (AR 45.71% vs 32.85%). There were no significant differences between the two groups (p = 0.119). RR of hypotension in the intervention group were lower, independent of the criterion of hypotension [systolic blood pressure, RR 0.72 (95% CI 0.47-1.09), mean arterial pressure, RR 0.93 (95% CI 0.64-1.37), SBP or MAP 0.86 (RR 0.86) (IC95% 0.62-1.21)], but without significant differences p> 0.05. The use of vasopressors in patients who presented this event occurred in 75.4% (n = 52), with higher RR in the control group and significant differences when evaluating the two groups. (RR 1.4 p = 0.032). Conclusions: Prophylactic phenylephrine did not prove effective in reducing the incidence of hypotension, however, it is associated with a significant decrease in vasopressor requirements, as well as in the incidence of nausea and vomiting. MÉD.UIS. 2018;31(2):33-9.

Palidez peri orbitaria post aplicación de midriaticos en neonatos con hidrocefalia asociado a efectos sistémicos / Periorbital pallor post application of mydriatic in infants with hydrocephalus associated to systemic effects

Una adecuada dilatación pupilar es necesaria para evaluar a neonatos con riesgo de desarrollar enfermedades oftalmológicas. Sin embargo, este procedimiento no está libre de efectos adversos locales o sistémicos. La vasoconstricción local posterior a la aplicación de midriáticos es una de estas complicaciones, existiendo además descritos efectos secundarios sistémicos. OBJETIVO: Presentar complicaciones asociadas al uso de midriáticos en 2 recién nacidos sometidos a evaluación oftalmológica. CASO CLINICO 1: Recién nacido de término con diagnóstico prenatal de restricción de crecimiento intrauterino e hidrocefalia. Al 5º día de vida se solicitó evaluación oftalmológica por presencia de opacidades corneales. Al realizar el procedimiento se evidenció palidez periorbitaria, al igual que taquicardia e hipertensión arterial en las siguientes 2 horas post procedimiento. Estos efectos secundarios se resolvieron espontáneamente pocas horas después del procedimiento. CASI CLINICO 2: Neonato de pretérmino de 27 semanas de gestación con antecedentes de síndrome de dificultad respiratoria, ductus arterioso persistente, hemorragia intraventricular grado III e hidrocefalia severa. Se solicitó examen oftalmológico a los 28 días de vida por sospecha de retinopatía del prematuro. A los 10 minutos post administración de midriáticos se observó palidez periorbitaria bilateral sin deterioro de signos vitales, presentando 24 horas después intolerancia a la alimentación y distensión abdominal. Se descartó enterocolitis necrotizante. CONCLUSIÓN: Es necesario establecer protocolos clínicos en relación al uso de midriáticos para reducir efectos deletéreos en neonatos de alto riesgo, como son los prematuros y aquellos con hidrocefalia. Por lo tanto, la monitoría debería realizarse durante la evaluación.

Adequate pupil dilation is needed to evaluate some neonates at risk of developing illness during this stage. However, this procedure is not free of adverse effects, either local or systemic. One of these complications is the local vasoconstriction of the preterm baby’s skin following the application of mydriatic eye drops. OBJECTIVE: To describe secondary local and systemic complications of pharmacological pupil dilation in 2 newborns. CLINICAL CASE 1: Full term baby with diagnosis of low-birth weight and hydrocephalia. An ophtalmological evaluation was performed at 5 days of age due to the presence of corneal opacities. Peri ocular pallor was observed during the procedure, as well as tachycardia and hypertension 2 hours later, spontaneosly recovered. CASE 2: Preterm newborn, 27 weeks of gestational age. Neonatal respiratory distress syndrome, patent ductus arteriosus, intraventricular hemorrhage and hydrocephalia were diagnosed at birth. At 28 days of life an ophtalmological evaluation was performed. After 10 minutes of mydriatic drops administration to evaluate preterm retinopathy, peri ocular pallor was observed, with spontaneous resolution; however, 24 hours later, the patient showed abdominal distention and feeding intolerance. Necrotizing enterocolitis was discarded, and symptoms were spontaneosly recovered. CONCLUSION: The establishment of protocols in relation to the number of drops to apply for dilation is needed to reduce deleterious effects on high risk infants, such as premature babies and those with hydrocephalus. Therefore this monitoring practice should be performed during the evaluation.

Efeito midriático da fenilefrina a 10% na comparação entre a autoinstilação de gota em olhos abertos e a vaporização em olhos fechados / Phenylephrine 10% mydriatic effect: comparison between self instillation of eye drop in open eyes and spray in closed eyes

RESUMO Objetivo: Comparar a eficácia fenilefrina a 10% aplicada pelo próprio paciente por vaporização em olho fechado em relação à instilação de gota em olho aberto em indivíduos que irão realizar exame de fundoscopia e avaliar o nível de dificuldade e a adequação técnica entre os métodos de administração. Métodos: Ensaio clínico controlado, randomizado e pareado realizado em 2014 envolvendo 100 olhos de 50 pacientes na Policlínica Ronaldo Gazolla - RJ, sem doenças oculares ou sistêmicas que comprometiam a dilatação pupilar. Os pacientes foram submetidos à instilação de 1 gota de fenilefrina a 10% e aplicação de vaporizador do mesmo midriático no olho contralateral. O olho em que se instilou o colírio permaneceu aberto, enquanto o olho vaporizado ficou fechado durante as aplicações da medicação. O diâmetro pupilar foi medido antes da aplicação, 10, 20 e 30 minutos após. O processo de instilação ou vaporização foi observado quanto a sua adequação técnica por um dos autores. Após o processo foi perguntado ao paciente questões pré-formuladas sobre a praticidade de ambos os métodos. Resultados: A diferença de midríase média entre os grupos de olhos avaliados em um determinado tempo foi no máximo 0,3 mm , o que não foi clinicamente ou estatisticamente significativo (ANOVA: F = 1,97 e p = 0,163609) . Porém, ao longo do tempo, a diferença entre o diâmetro da pupila no tempo inicial e no tempo de 30 minutos foi 1,15 mm para os olhos vaporizados e 1,58 mm para os olhos instilados com gotas (ANOVA: F = 129,22 e p ≤ 0,0001). Percentual de 60% dos pacientes tocaram a ponta do frasco de colírio nos olhos, enquanto que 12% tocaram o orifício na ponta do vaporizador com os dedos (p < 0,000001). Setenta de dois por cento (72%) consideraram a instilação de gotas fácil ou muito fácil enquanto 62% consideraram a vaporização em olho fechado fácil ou muito fácil (p = 0,238). Conclusão: A instilação de gotas em olhos abertos e a vaporização de olhos fechados da fenilefrina a 10% apresentou eficácia clínica semelhante. A vaporização foi mais segura e apresentou nível de dificuldade um pouco maior do que a instilação, apesar dos pacientes serem experientes para instilar gotas e inexperientes para vaporizar a medicação em olho fechado.

ABSTRACT Objective: To compare the effectiveness of phenylephrine 10% applied by a spray onto the eye closed over drop instillation onto an open eye on patients who will perform ophthalmoscopy and assess the level of difficulty and technical adequacy of the administration methods. Methods: The study was a clinical trial, controlled, randomized and paired, performed in 2014, involving 100 eyes of 50 patients in the Polyclinic Ronaldo Gazolla - RJ, with no ocular or systemic diseases that compromised the pupillary dilation. Patients underwent 10% phenylephrine eye drop instillation onto one open eye and spray application onto the other eye, which was closed. Pupillary diameter was measured before application and 10, 20, 30 minutes after. The process of instillation or vaporization was observed for its technical correctness by one of the authors. A questionnaire was asked to the patient about the difficulty of both methods after topical administration. Results: The average mydriasis difference between the eye groups assessed at a given time was at most 0.3 mm, which was not clinically or statistically significant (ANOVA: F = 1.97 and p = 0.163609). However, over time, the difference between the average pupil diameter before application and after 30 minutes was 1.15 mm to vaporized eyes and to 1.58 mm in eyes instilled with drops (ANOVA: F = 129, 22 and p ≤ 0.0001). Sixty per cent of patients touched the tip of the eye drop bottle onto the eye, while 12% touched the tip of the vaporizer with their fingers (p <0.000001). Seventy two percent (72%) considered the drops instillation easy or very easy, while 62% considered vaporization in a closed eye easy or very easy (p = 0.238). Conclusion: The instillation of drops phenylephrine 10% in open eyes and the vaporization onto closed eyes showed similar clinical efficacy. Vaporization was safer and a little more difficult than instillation, despite the patients being experienced for instilling drops and inexperienced to vaporize the medication in a closed eye.

Efficacy of an eye drop mixture for pupillary dilatation: A randomized comparative study.

PURPOSE: Pupillary dilatation with three types of eye drops is used regularly in the clinic; however, a mixture of these drops in a single bottle may be more beneficial in reducing workloads and resources. This study compared the efficacy in pupillary dilatation between two protocols of dilating drop instillation. METHODS: This prospective, randomized, comparative study included 30 eligible Thai patients. The patients randomly received preoperative pupillary dilatations by either the conventional protocol (1% tropicamide (T), 10% phenylephrine (P) and 0.1% diclofenac (D) in three separate bottles) or the fixed combination (TPD) protocol which had the three types of eye drops mixed in a single bottle in a ratio of 4:3:3. The chi-square test and independent t-test were used to analyze the data. RESULTS: The conventional protocol group and TPD protocol group each had 15 patients. Sixty minutes after the initial instillation, all patients in the TPD protocol and 13 patients (86.7%) in conventional protocol achieved at least 6mm in the shortest diameter. The mydriatic rate between protocols showed no difference. In patients who received the TPD protocol, the systemic effects on the mean arterial blood pressure and pulse rate decreased over time. CONCLUSION: The mixture of tropicamide, phenylephrine and diclofenac had a comparable efficacy for a pupillary dilatation to the conventional dilating drops in separate bottles. The systemic complications on blood pressure and arterial pulse of the TPD mixture were less than the conventional protocol. TRIAL REGISTRATION: TCTR20130325001.

Alpha antiadrenergic effect of Achyrocline bogotensis extract ("Vira Vira") in isolated rat aortic ring / Efecto antiadrenérgico alfa del extracto de Achyrocline bogotensis ("Vira Vira") en anillos aislados de aorta de rata

The treatment of symptoms of prostatic hyperplasia is among the traditional uses of Achyrocline bogotensis (Kunth) [N.V. "Vira Vira", Compositae] in Colombia. Pharmacological therapy for this disorder depends mainly on alpha-1 antiadrenergic agents, and the mechanism has not been studied previously using A. bogotensis. Objectives: To assess the alpha-1 antiadrenergic effect of the extract obtained from the aerial parts of A. bogotensis in isolated aortic rings from Wistar rats. Methods: The study compared the effects of the ethanol extract of A. bogotensis, prazosin (reference) and DMSO (control) in rings stimulated with phenylephrine (PE) or KCl. The capacity to reduce the PE pressor effect by the ethanol extract (pD2' value) was determined. To quantify the A. bogotensis relaxant potency, increasing concentrations of the ethanol extract (0.1 µg/mL-0.1 mg/mL), were added cumulatively to isolated aortic rings pre-contracted with PE (0.1 µM) or KCl (80 mM). To explore the possible participation of nitric oxide (NO), L-NAME (100 µM) was administered to aortic rings exposed to cumulatively increasing concentrations of PE in isolated aortic rings in the presence of the extract (10 µg/mL). Aqueous, butanol and dichloromethane fractions (10 µg/mL) obtained from the ethanol extract were assayed. Phytochemical screening was also performed. Results: Prazosin and A. bogotensis extract notably reduced the contraction induced by PE whereas their inhibitory effect in rings contracted with KCl were lower. A. bogotensis ethanol extract showed a high capacity for reducing the PE pressor response (pD´2: 5.51) as well as total efficacy for relaxing rings previously precontracted with PE. The relaxant efficacy and potency of A. bogotensis extract against rings previously contracted with KCl were notably lower. L-NAME partly reverted the inhibitory effect of A. bogotensis. Aqueous, butanol and dichloromethane fractions gave inhibitory responses lower than that obtained with the ethanol extract. Phytochemical screening of A. bogotensis extract revealed the significant presence of flavonoid and triterpene metabolites. Conclusions: These results suggest that A. bogotensis elicits a smooth muscle relaxant effect related to the alpha-1 antiadrenergic mechanism. This response is partially NO dependent and seems to be due to interactions among active metabolites likely to be of flavonoid and/or terpenoid nature.

Antecedentes: Uno de los usos tradicionales de la especie Achyrocline bogotensis (Kunth) [N.V. "Vira Vira", Compositae] en Colombia es el tratamiento de los síntomas de la hiperplasia prostática benigna. La terapia farmacológica de este trastorno se basa principalmente en el uso de agentes que ejercen efecto anti-adrenérgico alfa-1, mecanismo no estudiado previamente en esta especie. Objetivos: Evaluar el efecto anti-adrenérgico alfa-1 del extracto de la especie Achyrocline bogotensis (Kunth) en anillos aislados de aorta de ratas Wistar. Métodos: Se comparó el efecto del extracto etanólico de A. bogotensis, prazosin (patrón) y DMSO (control) en anillos aislados de aorta de ratas Wistar estimulados con fenilefrina (PE) o KCl. Se determinó la capacidad del extracto etanólico de A. bogotensis para reducir el efecto contráctil inducido por PE (pD'2 ). Se cuantificó la potencia relajante del extracto etanólico de A. bogotensis (0.1 µg/ mL - 0.1 mg/mL) en anillos de aorta previamente contraídos con PE (0.1 µM) o KCl (80 mM). Se exploró la posible participación del óxido nítrico (NO), administrando L-NAME (100 µM) en anillos de aorta expuestos a concentraciones acumulativas de PE en presencia del extracto etanólico (10 µg/mL). También se comparó el efecto de las fracciones acuosa, butanólica y diclometanólica (10 µg/mL), obtenidas del extracto etanólico, en anillos estimulados con PE. Además, se efectuó un tamizado fitoquímico del extracto. Resultados: Prazosin y el extracto de A. bogotensis redujeron notablemente el efecto de PE mientras su efecto inhibitorio sobre la contracción inducida por KCl fue menor. El extracto etanólico mostró una ostensible capacidad para reducir el efecto contráctil inducido por PE (pD2 ´: 5.51) así como una eficacia total para relajar anillos previamente contraídos con PE. La potencia y eficacia de relajación del extracto de A. bogotensis frente a anillos previamente contraídos con KCl fue notablemente menor. L-NAME revirtió parcialmente el efecto inhibitorio del extracto de A. bogotensis. Las fracciones acuosa, butanólica y diclorometanólica arrojaron respuestas inhibitorias menores que las inducidas por el extracto etanólico. El tamizado fitoquímico del extracto de A. bogotensis mostró la presencia de metabolitos de naturaleza flavonoide y terponoide. Conclusiones: Estos resultados muestran que la especie A. bogotensis ejerce efectos relajantes sobre el músculo liso vinculados con mecanismos de tipo antiadrenérgico alfa-1. Esta respuesta depende en parte de la presencia de NO y parece deberse a la interacción de metabolitos de naturaleza flavonoide y/o terpenoide.

Etilefrina vs fenilefrina en hipotensión por anestesia espinal para cesárea: ensayo clínico multicéntrico, controlado, aleatorizado y doble ciego / Etilefrine vs. phenylephrine for hypotension during spinal anesthesia for cesarean section: Multicenter, randomized, double blind controlled clinical trial

Introduction: Hypotension after spinal anesthesia in cesarean section should be minimized. The use of vasopressors is an effective measure to treat hypotension. The objective of this paper is to compare the safety and effectiveness of etilefrine vs. phenylephrine in the management of this condition. Methods: This multicenter, double-blind trial between August 2009 and November 2010 included 196 patients with hypotension during spinal anesthesia for cesarean delivery; the patients were randomized to receive etilefrine or phenylephrine as vasopressor. The primary outcome was the fetal umbilical arterial pH. The secondary outcomes were: fetal acidosis (umbilical arterial pH < 7.20), Apgar score at 1 and 5 min, need for intubation and admission to the neonatal intensive care unit for newborns, and time of hypotension, total dose of vasopressor, atropine requirement, intravenous fluids volume and incidence of nausea and vomiting in mothers. Results: 98 patients received etilefrine and 98 phenylephrine. There were no differences in umbilical arterial pH (7.27 vs. 7.28, respectively, P = 0.493). The total dose of vasopressor (5.66 vs. 6.51ml, respectively, P = 0.024) and total time of hypotension (2.78 vs. 3.25 min, respectively, P = 0.021) were lower in the etilefrine group. Other outcomes studied showed no statistically significant differences. Conclusion: Etilefrine and phenylephrine are equally effective for the treatment of hypotension during spinal anesthesia for cesarean delivery. This study found no difference in the maternal or fetal outcomes.

Introducción: La hipotensión que ocurre luego de anestesia espinal para cesárea debe minimizarse. El uso de vasopresores es una medida eficaz para su tratamiento. El objetivo de este trabajo es comparar la seguridad y efectividad de etilefrina vs fenilefrina para manejo de esta condición. Métodos: En este estudio multicéntrico y doble ciego, entre agosto de 2009 y noviembre de 2010, 196 pacientes con hipotensión durante anestesia espinal para cesárea, fueron asignadas aleatoriamente para recibir etilefrina o fenilefrina como vasopresor. El resultado primario fue el pH arterial umbilical fetal. Los resultados secundarios fueron: acidosis fetal (pH arterial umbilical < 7,20), puntaje Apgar al 1 y 5 minutos, necesidad de intubación e ingreso a la unidad de cuidados intensivos neonatal para los recién nacidos; y tiempo de hipotensión, dosis total de vasopresor, necesidad de uso de atropina, líquidos endovenosos totales e incidencia de nausea y vómito para las madres. Resultados: 98 pacientes recibieron etilefrina y 98 fenilefrina. No se encontraron diferencias en el pH arterial umbilical (7,27 vs 7,28 respectivamente; p = 0,493). La dosis total de vasopresor (5,66 vs. 6,6 ml, respectivamente; P = 0,024) y el tiempo total de hipotensión (2,78 vs. 3,25 min, respectivamente; p = 0,021), fueron menores en el grupo de etilefrina. Los demás desenlaces estudiados no presentaron diferencia estadísticamente significativa. Conclusión: La etilefrina y la fenilefrina son igualmente efectivas para el tratamiento de la hipotensión por anestesia espinal para cesárea. Este estudio no encontró diferencia en los resultados fetales ni maternos.

Palpebral position interdependence in blepharoptosis: comparison of the effect of instillation of 10% phenylephrine drop and digital lifting / Interdependência na posição palpebral em ptose palpebral: comparação do efeito de instilação de colírio de fenilefrina 10% e o teste de elevação digital da pálpebra

Purpose: To quantify and compare the effects of instillation with 10% phenylephrine and digital lifting on the contralateral upper eyelid of patients with involutional bilateral blepharoptosis. Methods: The present prospective clinical study involved patients with involutional bilateral blepharoptosis who underwent two tests: 1) digital lifting of the more ptotic eyelid and observation of the effect on the contralateral eyelid and 2) instillation of two drops of 10% phenylephrine in the more ptotic eye and observation of the effect on the contralateral eyelid. Patients were filmed before and 5, 10, and 15 min after instillation, and the resulting images were analyzed to obtain eyelid measurements. The results were tested using a linear mixed-effects model. Results: A total of 27 patients, ranging from 52 to 82 years of age (mean age 68.51 ± 8.21 years), 24 (88.88%) of whom were women, were included in the present study. In eyes that received instillation, the marginal distance reflex-1 (MDR1) values increased from baseline (1.21 ± 0.60 mm) until 10 min after instillation, then remained statistically unchanged until 15 min after instillation (2.42 ± 0.90 mm). Significant differences were observed in the contralateral eye of the group that underwent digital lifting (1.51 ± 0.53 mm - 1.63 ± 0.56 mm) and in the contralateral eye of the group that underwent 10% phenylephrine instillation (1.38 ± 0.54 mm - 1.63 ± 0.56 mm); p=0.02 and p<0.01, respectively. Conclusion: In all eyes, 10% phenylephrine elevated the upper eyelid, with improved eyelid height at 10 min after instillation. Significant differences were observed in the height of the contralateral eyelid when compared before and after each intervention in each group; however, this difference was very small and nearly undetectable by conventional clinical evaluation in the digital lifting group. However, the 10% phenylephrine eye-drop test resulted in substantial changes in MDR1 values ...

Objetivo: Quantificar e comparar o efeito da instilação do colírio de fenilefrina 10% com o levantamento manual da pálpebra superior contralateral de pacientes com ptose palpebral bilateral involucional. Métodos: Estudo clínico e prospectivo de pacientes com ptose palpebral bilateral involucional submetidos a dois testes: 1) elevação manual da pálpebra mais ptótica e observação do efeito da intervenção na pálpebra contralateral; e 2) a instilação de duas gotas de colírio de fenilefrina 10% no olho mais ptótico e observação do efeito da intervenção na pálpebra contralateral. Os pacientes foram filmados antes e 5, 10 e 15 minutos após a instilação. Os resultados foram analisados estatisticamente com o modelo linear de efeitos mistos. Resultados: O estudo incluiu 27 pacientes com idade entre 52-82 anos (68,51 ± 8,21), 24 dos quais eram do sexo feminino (88,88%). Em olhos submetidos a instilação do colírio, os valores da DMR1 (distância marginal reflexo) aumentaram da linha de base (1,21 ± 0,60 mm) até os 10 min, em seguida, manteve-se estatisticamente estável até 15 min (2,42 ± 0,90 mm). Diferenças significativas foram observadas nos olhos contralaterais, independentemente do levantamento manual da pálpebra (1,51 ± 0,53 mm - 1,63 ± 0,56 milímetros) e da instilação do colírio de fenilefrina 10% (1,38 ± 0,54 mm - 1,63 ± 0,56 mm), p=0,02 e p<0,01 respectivamente. Conclusões: Em todos os olhos, a instilação do colírio de fenilefrina 10% mostrou um aumento gradual do valor de distância marginal reflexo até os 10 min. Nos olhos contralaterais houve diminuição do valor de distância marginal reflexo, independentemente do teste realizado, porém as mudanças que ocorrem na posição da pálpebra contralateral, durante o teste da elevação manual, são muito pequenas e difíceis de serem detectadas no exame clínico convencional. Enquanto isso, o teste de colírio de fenilefrina 10% produziu mudanças substanciais nos valores distância marginal reflexo nos ...

O Wortmannin reverte a hiporreatividade de aortas à fenilefrina associada à fase final da prenhez de ratas espontaneamente hipertensas (SHR) / The wortmannin reverses the aortas of hyporeactivity to phenylephrine associated with late pregnancy in spontaneously hypertensive rats (SHR)

Ratas prenhas normotensas ou hipertensas (SHR) apresentam redução da pressão arterial nos períodos finais da prenhez, associada à redução da atividade simpática perivascular de leitos mesentéricos e redução de respostas vasoconstritoras a alguns agonistas vasoconstritores. O endotélio vascular modula a resposta contrátil estimulada por vasoconstritores e, na prenhez, uma maior modulação do óxido nítrico (NO) sobre a reatividade vascular de aortas tem sido atribuída à maior atividade da sintase de óxido nítrico endotelial (eNOS). No entanto, nenhuma alteração da reatividade de aortas à Acetilcolina, ou a o A23187, foi observada em aortas de ratas prenhas. Foi sugerido que a participação de uma via de sinalização independente de ativação de receptores e menos dependente de cálcio, estaria envolvida na modulação endotelial sobre a vasoconstrição durante a prenhez. A expressão da eNOS fosforilada está aumentada em aorta de ratas prenhas. A eNOS pode ser fosforilada em resíduos de serina e treonina pela via PI3K/AKT. No entanto, a participação da via PI3K/AKT/eNOS na hiporreatividade de aortas de ratas prenhas à fenilefrina ainda não foi demonstrada. O objetivo deste estudo foi avaliar se o Wortmannin, um inibidor da via PI3K/AKT, poderia reverter a hiporreatividade de aortas à fenilefrina associada à prenhez e alterar as concentrações citosólicas de óxido nítrico (NO), cálcio (Ca2+) e de espécies reativas de oxigênio (ERO) em células endoteliais isoladas de aortas de ratas Wistar e SHR prenhas. Inicialmente, avaliamos as possíveis alterações nos parâmetros cardiovasculares e na sensibilidade barorreflexa associadas à prenhez de ratas espontaneamente hipertensas (SHR) por estudos in vivo. O efeito do Wortmannin foi avaliado na reatividade de aortas isoladas à fenilefrina por estudos funcionais e nas concentrações citosólicas de NO, Ca2+ e ERO em células endoteliais frescas isoladas de aortas de ratas Wistar e SHR, não prenhas (em estro) e prenhas (19-20º dia de...

Normotensive or hypertensive pregnant rats (SHR) show a significant reduction in blood pressure in the final period of pregnancy, associated with reduced activity of perivascular sympathetic mesenteric beds and reduced vasoconstrictor responses to some vasoconstrictor agonists. The vascular endothelium modulates contractile response stimulated by vasoconstrictors and in pregnancy, an additional modulation of nitric oxide (NO) on vascular reactivity of aortas has been attributed to increased activity of endothelial nitric oxide synthase (eNOS). However, no change in the aortas of reactivity to acetylcholine or A23187 was observed in aortas of pregnant rats. The involvement of a signaling pathway independent of receptor activation and less dependent calcium was suggested. This pathway is involved in the modulation of endothelial vasoconstriction during pregnancy. The expression of phosphorylated eNOS is increased in the aorta of pregnant rats and this enzyme can be phosphorylated on serine and threonine residues of the PI3K/Akt pathway. However, the participation of the PI3K/AKT/eNOS pathway in hyporeactivity in the aortas of pregnant rats to phenylephrine has not been demonstrated. The aim of this study was evaluate if the PI3K/AKT pathway inhibitor (Wortmannin) could reverse the hyporeactivity of aortas to phenylephrine associated with the end of pregnancy and change the cytosolic concentrations of nitric oxide (NO), calcium (Ca2+) and reactive oxygen species (ROS) in isolated endothelial cells from aortas of pregnant Wistar rats and SHR. Initially, we evaluated the possible changes in cardiovascular parameters and baroreflex sensitivity associated with pregnancy in spontaneously hypertensive rats (SHR) by in vivo studies. The effect of Wortmannin was evaluated in the isolated aortas reactivity to phenylephrine and by functional studies through cytosolic concentrations of NO, Ca2+ and ROS in not pregnant (estrus) and pregnant (19-20th day of pregnancy) isolated…

Desarrollo y validación de un método analítico para el control de calidad y estabilidad de fenilefrina 10 por ciento colirio y tropicamida 1 por ciento / Development and validation of an analytical method for quality control and the stability of the eyedrops 10 % Phenylephrine and the 1 % Tropicamide

Se desarrolló y validó un método analítico por cromatografía líquida de alta resolución, aplicable al control de la calidad y el estudio de estabilidad de fenilefrina 10 por ciento más tropicamida 1 percent, colirio. Para cuantificar simultáneamente los 2 principios activos en el producto terminado, la separación se realizó a través de una columna cromatográfica Lichrosorb RP-18 (5 µm) (250 x 4 mm), con detección ultravioleta a 253 nm, empleando una fase móvil compuesta por metanol:agua destilada (1:1), con 1,1 g de 1-octanosulfonato de sodio por litro ajustado pH a 3,0 con ácido fosfórico y la cuantificación de este frente a una muestra de referencia con el método del estándar externo. El método analítico desarrollado resultó lineal, preciso, específico y exacto en el rango de concentraciones estudiadas, el cual se estableció para el control de la calidad y el estudio de estabilidad del producto terminado ya que no existían métodos analíticos reportados para estos fines

An analytical high-performance liquid chromatography method was developed and validated applicable to quality control and to stability study of 10 percent phenylephrine plus eyedrops 1 percent tropicamide. To quantify simultaneously both active principles in the finished product, separation was carried out through a Lichrosorb RP-18 (15 µm) (260 x 4 mm) column chromatography, with ultraviolet detection at 253 nm using the mobile phase composed of methanol: distilled water (1:1), with 1.1 g of sodium 1-octasulfanate by litre and pH fitted to 3,0 with phosphoric acid and the quantification of this front to a reference sample using the external standard method. The analytical method developed was linear, precise, specific and accurate in the rank of study concentrations, established for the quality control and stability study of the finished product since there were not analytical methods designed for these aims

Validación del método analítico para el control de la calidad y estudio de estabilidad de fenilefrina 10 por ciento colirio / Validation of an analytical method for quality control and stability study of 10 percent Phenylephrine eyedrops

La fenilefrina se emplea como midriático en exámenes de ojos y otros procedimientos oftálmicos. Se utiliza como vasoconstrictor con anestésicos locales. En este trabajo se validó un método analítico por cromatografía líquida de alta resolución para el control de la calidad y los estudios de estabilidad de la fenilefrina 10 por ciento colirio. El método se basó en la separación del principio activo a través una columna cromatográfica Lichrosorb RP-18 (5 µm) (250 x 4 mm), con detección ultravioleta a 280 nm, para lo cual se empleó una fase móvil compuesta por una mezcla desgasificada de metanol:agua destilada (1:1), con 1,1 g de 1-octanosulfonato de sodio por litro ajustado a pH 3,0 con ácido fosfórico, con una velocidad de flujo de 1,0 mL/min. El método analítico resultó lineal, preciso, específico y exacto en el intervalo de concentraciones estudiadas(AU)

Phenylephrine is used like mydiatric in eye examinations and other ophthalmic procedures. It is used as vasoconstrictor with local anesthetic agents. In present paper a high ressolution liquid chromatography analytical method was validated to quality control and stability studies of 10 percent Phenylephrine (eyedrops). Mathod was based in separation of active principle through a Lichrosorb RO-18 (5 µm) (250 x 4 mm) chromatography column with UV detection at 280 nm using a mobile phase composed by a non-gasified mixture of methanol distilled water (1:1) with 1.1 g of 1-sodium octane-sulphonate by liter adjusted to pH 3,0 with phosphoric acid at a flow speed of 1.0 mL/min. Analytical method was linear, accuracy, specific and exact in the interval of study concentrations(AU)

Validación del método analítico para el control de la calidad y estudio de estabilidad de fenilefrina 10 por ciento colirio / Validation of an analytical method for quality control and stability study of 10 percent Phenylephrine eyedrops

La fenilefrina se emplea como midriático en exámenes de ojos y otros procedimientos oftálmicos. Se utiliza como vasoconstrictor con anestésicos locales. En este trabajo se validó un método analítico por cromatografía líquida de alta resolución para el control de la calidad y los estudios de estabilidad de la fenilefrina 10 por ciento colirio. El método se basó en la separación del principio activo a través una columna cromatográfica Lichrosorb RP-18 (5 µm) (250 x 4 mm), con detección ultravioleta a 280 nm, para lo cual se empleó una fase móvil compuesta por una mezcla desgasificada de metanol:agua destilada (1:1), con 1,1 g de 1-octanosulfonato de sodio por litro ajustado a pH 3,0 con ácido fosfórico, con una velocidad de flujo de 1,0 mL/min. El método analítico resultó lineal, preciso, específico y exacto en el intervalo de concentraciones estudiadas

Phenylephrine is used like mydiatric in eye examinations and other ophthalmic procedures. It is used as vasoconstrictor with local anesthetic agents. In present paper a high ressolution liquid chromatography analytical method was validated to quality control and stability studies of 10 percent Phenylephrine (eyedrops). Mathod was based in separation of active principle through a Lichrosorb RO-18 (5 µm) (250 x 4 mm) chromatography column with UV detection at 280 nm using a mobile phase composed by a non-gasified mixture of methanol distilled water (1:1) with 1.1 g of 1-sodium octane-sulphonate by liter adjusted to pH 3,0 with phosphoric acid at a flow speed of 1.0 mL/min. Analytical method was linear, accuracy, specific and exact in the interval of study concentrations

Diseño de una formulación de fenilefrina 10 por ciento y tropicamida 1 por ciento colirio / Design of a 10 percent Phenylephrine and 1 percent Tropicamide formula: eyedrops

El colirio de fenilefrina 10 por ciento y tropicamida 1 por ciento se emplea en la pràctica médica como antihistamínico, analgésico, midriàticos y ciclopléjicos. El objetivo del presente trabajo consistió en desarrollar una formulación de fenilefrina 10 por ciento y tropicamida 1 por ciento que cumpliera con las especificaciones de calidad establecidas por el fabricante, que fuera estable física, química y microbiológicamente, para lo cual se realizó un diseño y los estudios de preformulación. Se estudió ademàs, las especificaciones de calidad de la formulación seleccionada, la estabilidad del producto y el tiempo de vigencia de este. Se desarrolló y validó un método analítico para el control de la calidad y el estudio de estabilidad del producto terminado por cromatografía líquida de alta resolución. Se realizaron los resultados analíticos del estudio de estabilidad acelerado y por vida de estante, para lo cual se emplearon 3 lotes del producto a escala piloto. El colirio resultó estable física, química y microbiológicamente envasado en frascos de polietileno de baja densidad, por un tiempo de 12 meses almacenados a temperatura ambiente(AU)

The 10 percent Phenylephrine and 1 percent Tropicamide eyedrops is used in medical practice as antihistaminic, analgesic, mydiatric and cycloplegic. The aim of present paper was to develop a 10 percent Phenylephrine and 1 percent Tropicamide formula fulfilling the quality specifications established by manufacturer physically, chemically and microbiologically stable with the performing of a design and pre-formula studies. Also, we studied the quality specifications of selected formula, the product stability and its expiry time. An analytical method was developed and validated to quality control and stability study of the finished product by high-performance liquid chromatography. Analytical results of accelerated stability study and by shelf life using 3 batches of product at pilot scale. Eyedrops was physically, chemically and microbiologically stable when it was bottling in low density polyethylene flasks during 12 months of storage at room temperature(AU)

Diseño de una formulación de fenilefrina 10 por ciento y tropicamida 1 por ciento colirio / Design of a 10 percent Phenylephrine and 1 percent Tropicamide formula: eyedrops

El colirio de fenilefrina 10 por ciento y tropicamida 1 por ciento se emplea en la pràctica médica como antihistamínico, analgésico, midriàticos y ciclopléjicos. El objetivo del presente trabajo consistió en desarrollar una formulación de fenilefrina 10 por ciento y tropicamida 1 por ciento que cumpliera con las especificaciones de calidad establecidas por el fabricante, que fuera estable física, química y microbiológicamente, para lo cual se realizó un diseño y los estudios de preformulación. Se estudió ademàs, las especificaciones de calidad de la formulación seleccionada, la estabilidad del producto y el tiempo de vigencia de este. Se desarrolló y validó un método analítico para el control de la calidad y el estudio de estabilidad del producto terminado por cromatografía líquida de alta resolución. Se realizaron los resultados analíticos del estudio de estabilidad acelerado y por vida de estante, para lo cual se emplearon 3 lotes del producto a escala piloto. El colirio resultó estable física, química y microbiológicamente envasado en frascos de polietileno de baja densidad, por un tiempo de 12 meses almacenados a temperatura ambiente.

The 10 percent Phenylephrine and 1 percent Tropicamide eyedrops is used in medical practice as antihistaminic, analgesic, mydiatric and cycloplegic. The aim of present paper was to develop a 10 percent Phenylephrine and 1 percent Tropicamide formula fulfilling the quality specifications established by manufacturer physically, chemically and microbiologically stable with the performing of a design and pre-formula studies. Also, we studied the quality specifications of selected formula, the product stability and its expiry time. An analytical method was developed and validated to quality control and stability study of the finished product by high-performance liquid chromatography. Analytical results of accelerated stability study and by shelf life using 3 batches of product at pilot scale. Eyedrops was physically, chemically and microbiologically stable when it was bottling in low density polyethylene flasks during 12 months of storage at room temperature.

Efecto de D-004, un extracto lipídico extraído de las frutas de la palma real (Roystonea regia) sobre las contracciones provocadas por la Fenilefrina sobre la próstata aislada de rata / Effect of D-004, a lipid extract from royal palm (Roystonea regia) fruits, on phenylephrine-induced contractions of isolated rat prostate

D-004, a lipid extract of Roystonea regia fruits, inhibits norepinephrine-elicited contraction in rat vas deferens. Nevertheless, the effect of D-004 on a1-adrenergic contractile responses in isolated prostate preparations had not been studied. Therefore, this study investigated the effects of D-004 on phenylephrine-induced contractions in isolated rat prostate strips. D-004 (125-500 mg/mL) was added to prostate preparations in which contractions were induced with phenylephrine (10-6-10-4 M) or with ClK (50 mM). D-004 (250-500 mg/mL) significantly (p < 0,01).and dose-dependently inhibited the phenylephrine-induced contractions through a non-competitive mechanism, since it reduced (12-60 percent) the maximal contraction to phenyle phrine with respect to control preparations. D-004 at 500 mg/mL inhibited similarly both ClK and phenylephrine-contractile responses. Tamsulosin (0.01 mg/mL) abolished (100 percent inhibition) the phenylephrine, but unaffected the ClK-induced contractions(AU)

D-004, un extracto lipídico de las frutas de Roystonea regia, inhibe la contracción provocada por la norepinefrina en el vas deferens de las ratas. No obstante, el efecto de D-004 sobre las respuestas contráctiles adrenérgicas a1 en las preparaciones aisladas de la próstata no ha sido estudiado. Por lo tanto, este estudio investigó los efectos de D-004 sobre las contracciones provocadas por la fenilefrina en las extracciones aisladas de la próstata de la rata. D-004 (125-500 mg/mL) fue adicionado a las preparaciones a partir de la próstata en la que las contracciones fueron provocadas por la fenilefrina (10-6-10-4 M) o por CIK (50 mM). D-004 (250-500 mg/mL) en forma significativa y la dosis en forma dependiente inhibieron las contracciones provocadas por la fenilefrina mediante un mecanismo no competetitivo, reduciendo así (12-60 por ciento) la contracción máxima por la fenilefrina con respecto a las preparaciones controles. D-004 a 500 µg/mL inhibieron de la misma forma tanto CIK como las respuestas contráctiles-fenilefrina. Tamsulosin (0,01 mg/mL) eliminó la acción de la fenilefrina (100 por ciento de inhibición), pero no afectó las contracciones provocadas por CIK(AU)

Efecto de D-004, un extracto lipídico extraído de las frutas de la palma real (Roystonea regia) sobre las contracciones provocadas por la Fenilefrina sobre la próstata aislada de rata / Effect of D-004, a lipid extract from royal palm (Roystonea regia) fruits, on phenylephrine-induced contractions of isolated rat prostate

D-004, a lipid extract of Roystonea regia fruits, inhibits norepinephrine-elicited contraction in rat vas deferens. Nevertheless, the effect of D-004 on a1-adrenergic contractile responses in isolated prostate preparations had not been studied. Therefore, this study investigated the effects of D-004 on phenylephrine-induced contractions in isolated rat prostate strips. D-004 (125-500 mg/mL) was added to prostate preparations in which contractions were induced with phenylephrine (10-6-10-4 M) or with ClK (50 mM). D-004 (250-500 mg/mL) significantly (p < 0,01).and dose-dependently inhibited the phenylephrine-induced contractions through a non-competitive mechanism, since it reduced (12-60 percent) the maximal contraction to phenyle phrine with respect to control preparations. D-004 at 500 mg/mL inhibited similarly both ClK and phenylephrine-contractile responses. Tamsulosin (0.01 mg/mL) abolished (100 percent inhibition) the phenylephrine, but unaffected the ClK-induced contractions.

D-004, un extracto lipídico de las frutas de Roystonea regia, inhibe la contracción provocada por la norepinefrina en el vas deferens de las ratas. No obstante, el efecto de D-004 sobre las respuestas contráctiles adrenérgicas a1 en las preparaciones aisladas de la próstata no ha sido estudiado. Por lo tanto, este estudio investigó los efectos de D-004 sobre las contracciones provocadas por la fenilefrina en las extracciones aisladas de la próstata de la rata. D-004 (125-500 mg/mL) fue adicionado a las preparaciones a partir de la próstata en la que las contracciones fueron provocadas por la fenilefrina (10-6-10-4 M) o por CIK (50 mM). D-004 (250-500 mg/mL) en forma significativa y la dosis en forma dependiente inhibieron las contracciones provocadas por la fenilefrina mediante un mecanismo no competetitivo, reduciendo así (12-60 por ciento) la contracción máxima por la fenilefrina con respecto a las preparaciones controles. D-004 a 500 µg/mL inhibieron de la misma forma tanto CIK como las respuestas contráctiles-fenilefrina. Tamsulosin (0,01 mg/mL) eliminó la acción de la fenilefrina (100 por ciento de inhibición), pero no afectó las contracciones provocadas por CIK.