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.

Afferent Pathway-Mediated Effect of α1 Adrenergic Antagonist, Tamsulosin, on the Neurogenic Bladder After Spinal Cord Injury / 대한배뇨장애요실금학회지

PURPOSE: The functions of the lower urinary tract (LUT), such as voiding and storing urine, are dependent on complex central neural networks located in the brain, spinal cord, and peripheral ganglia. Thus, the functions of the LUT are susceptible to various neurologic disorders including spinal cord injury (SCI). SCI at the cervical or thoracic levels disrupts voluntary control of voiding and the normal reflex pathways coordinating bladder and sphincter functions. In this context, it is noteworthy that α1-adrenoceptor blockers have been reported to relieve voiding symptoms and storage symptoms in elderly men with benign prostatic hyperplasia (BPH). Tamsulosin, an α1-adrenoceptor blocker, is also considered the most effective regimen for patients with LUT symptoms such as BPH and overactive bladder (OAB). METHODS: In the present study, the effects of tamsulosin on the expression of c-Fos, nerve growth factor (NGF), and nicotinamide adenine dinucleotide phosphate-diaphorase (NADPH-d) in the afferent micturition areas, including the pontine micturition center (PMC), the ventrolateral periaqueductal gray matter (vlPAG), and the spinal cord (L5), of rats with an SCI were investigated. RESULTS: SCI was found to remarkably upregulate the expression of c-Fos, NGF, and NADPH-d in the afferent pathway of micturition, the dorsal horn of L5, the vlPAG, and the PMC, resulting in the symptoms of OAB. In contrast, tamsulosin treatment significantly suppressed these neural activities and the production of nitric oxide in the afferent pathways of micturition, and consequently, attenuated the symptoms of OAB. CONCLUSIONS: Based on these results, tamsulosin, an α1-adrenoceptor antagonist, could be used to attenuate bladder dysfunction following SCI. However, further studies are needed to elucidate the exact mechanism and effects of tamsulosin on the afferent pathways of micturition.

Pharmacologic Considerations for Youth with Posttraumatic Stress Disorder

Children exposed to potentially traumatic events are at risk of developing posttraumatic stress disorder (PTSD). However, the subsequent developmental course of posttraumatic stress symptoms appears to vary considerably. In this regard, some PTSD symptoms resolve without significant interventions, while for many children and adolescents, they persist until the patient receives appropriate treatment specifically designed to address PTSD and other trauma related symptoms. Evidence-based psychotherapies represent the standard of care for children with PTSD and, while psychopharmacologic interventions are utilized for many youth with posttraumatic stress symptoms and PTSD, there is little data available to guide the use of these medications in this population. However, given the structural challenges involved in disseminating and delivering evidence-based psychotherapies in all settings, prescribing clinicians should be aware of the medications whose use in children with pediatric PTSD has been studied. Herein, we review the PTSD assessment modalities, as well as the use of pharmacologic interventions in PTSD, including antiadrenergic agents, selective serotonin reuptake inhibitors and other medications.

β3-adrenoceptor impacts apoptosis in cultured cardiomyocytes via activation of PI3K/Akt and p38MAPK / 华中科技大学学报（医学）（英德文版）

β3-adrenoceptor (β3-AR) has been shown to promote myocardial apoptosis. However, the exact physiological role and importance of this receptor in the human myocardium, and its underlying mode of action, have not been fully elucidated. The present study aimed to determine the effects of β3-AR on the promotion of myocardial apoptosis and on norepinephrine (NE) injury. We analyzed NE-induced cardiomyocyte (CM) apoptosis by using a TUNEL and an annexin V/propidium iodide apoptosis assay. Furthermore, we investigated the NE-induced expression of the apoptosis marker genes Akt and p38MAPK, their phosphorylated counterparts p-Akt and p-p38MAPK, caspase-3, Bcl-2, and Bax. In addition, we determined the effect of a 48-h treatment with a β3-AR agonist and antagonist on expression of these marker genes. β3-AR overexpression was found to increase CM apoptosis, accompanied by an increased expression of caspase-3, bax/bcl-2, and p-p38MAPK. In contrast, the β3-blocker reduced apoptosis of CMs and the associated elevated Akt expression. We identified a novel and potent anti-apoptosis mechanism via the PI3K/Akt pathway and a pro-apoptosis pathway mediated by p38MAPK.

Updated roles of adrenergic receptors in prostate cancer / 中华男科学杂志

Adrenergic receptors are members of the G-protein coupled receptor superfamily. Recent studies revealed that these adrenergic receptors are playing an important role in the growth and metastasis of prostate cancer cells. The expression of adrenergic receptors rises significantly in prostate cancer cells and tissues. Agonists of these receptors promote the growth and mobility of prostate cancer cells, while antagonists may suppress their proliferation, trigger their apoptosis, and inhibit their metastasis. Clinically, receptor antagonists can significantly reduce the risk of prostate cancer and improve its prognosis after androgen depravation therapy. This article presents an overview on the roles of adrenergic receptors in prostate cancer.

Evidence for the involvement of peripheral -adrenoceptors in delayed liquid gastric emptying induced by dipyrone, 4-aminoantipyrine, and antipyrine in rats

Dipyrone (Dp), 4-aminoantipyrine (AA), and antipyrine (At) delay liquid gastric emptying (GE) in rats. We evaluated adrenergic participation in this phenomenon in a study in male Wistar rats (250-300 g) pretreated subcutaneously with guanethidine (GUA), 100 mg·kg−1·day−1, or vehicle (V) for 2 days before experimental treatments. Other groups of animals were pretreated intravenously (iv) 15 min before treatment with V, prazosin (PRA; 1 mg/kg), yohimbine (YOH; 3 mg/kg), or propranolol (PRO; 4 mg/kg), or with intracerebroventricular (icv) administration of 25 µg PRO or V. The groups were treated iv with saline or with 240 µmol/kg Dp, AA, or At. GE was determined 10 min later by measuring the percentage of gastric retention (%GR) of saline labeled with phenol red 10 min after gavage. %GR (mean±SE, n=8) indicated that GUA abolished the effect of Dp (GUA vs V=31.7±1.6 vs 47.1±2.3%) and of At (33.2±2.3 vs 54.7±3.6%) on GE and significantly reduced the effect of AA (48.1±3.2 vs 67.2±3.1%). PRA and YOH did not modify the effect of the drugs. %GR (mean±SE, n=8) indicated that iv, but not icv, PRO abolished the effect of Dp (PRO vs V=29.1±1.7 vs 46.9±2.7%) and At (30.5±1.7 vs 49±3.2%) and significantly reduced the effect of AA (48.4±2.6 vs 59.5±3.1%). These data suggest activation of peripheral β-adrenoceptors in the delayed GE induced by phenylpyrazolone derivatives.

Effects of beta3-adrenergic receptor antagonist on myocardial UCP2 expression and energy metabolism in chronic heart failure rats / 中国应用生理学杂志

<p><b>OBJECTIVE</b>To observe the effects of beta3-adrenergic receptor(beta3-AR) antagonist on myocardial uncoupling protein 2 (UCP2) expression and energy metabolism in chronic heart failure rats.</p><p><b>METHODS</b>Seven weight-matched normal adult rats (control group), 18 isoproterenol (ISO) induced heat failure (HR) rats (ISO group) and 21 ISO induced heart failure rats but received specific beta3-AR inhibitor SR59230A (ISO+ SR59230A group) for 6 weeks were included in this research. At the end of the study, echocardiography was performed, the ratio of left ventricular weight and body weight (LVW/BW) was calculated. The expression of beta3-AR ad UCP2 mRNA in myocardium were detected by reverse transcription-polymerase chain reaction (RT-PCR), the UCP2 protein in myocardium were detected by Western blot. The myocardial contents of creatine phosphate (PCr) and adenosine triphosphate (ATP) were measured by high performance liquid chromatography (HPLC).</p><p><b>RESULTS</b>Compared with control group, the cardiac function was significantly reduced and myocardial beta3-AR mRNA significantly increased, UCP2 mRNA and protein were also significantly increased in ISO group, this change could be attenuated by the treatment with SR59230A, and the expression of myocardial UCP2 protein negatively correlated with the ratio of PCr/ATP.</p><p><b>CONCLUSION</b>In the chronic stage of HF, the expression of UCP2 increases, which causes myocardial energy shortage, SR59230A improves myocardia energy efficiency and cardiac function by means of suppressing the expression of UCP2.</p>

Biphasic anaphylaxis to gemifloxacin

Anaphylaxis have been documented as adverse effects of ciprofloxacin, ofloxacin, norfloxacin, levofloxacin, and moxifloxacin. However resistant and biphasic anaphlylactic reactions to gemifloxacin have not been reported to date. Management of severe anaphylaxis in the elderly can be complicated by concurrent medications such as beta (β) adrenergic, alpha (α) adrenergic blockers and angiotensin-converting enzyme (ACE) inhibitors. We report here in the case of a 60-year-old male who was taking on ACE inhibitor, α and β blockers and experienced a severe, resistant and biphasic anaphlylactic reaction to gemifloxacin mesylate.

The Effect of alpha1-Adrenergic Blocker on Phacoemulsification

PURPOSE: To evaluate the influence of alpha1-adrenergic blocker on phacoemulsification and the preventive effect of adrenergic blocker (AB) cessation before cataract surgery. METHODS: A prospective study was performed involving 92 eyes of 60 patients undergoing cataract surgery. Cases were divided into three groups: the use of alpha1AB with discontinuance before surgery (32 eyes), the use of alpha1AB with no discontinuance before surgery before surgery (31 eyes), and eyes not treated with alpha1AB (29 eyes). Clinical measurements and intraoperative parameters were compared among the three groups. RESULTS: Preoperative maximum pupil diameters of patients treated with alpha1AB were smaller than those of patients not administered alpha1AB (p = 0.027 and p = 0.018, respectively). The incidence of IFIS in the patients using of alpha1AB with discontinuance before surgery was 6.25%, and that in the patients using of alpha1AB with no discontinuance before surgery was 6.45%. There was no IFIS outbreak in the patients not using of alpha1AB. We noted no significant differences in absolute phaco time during phacoemulsification (p = 0.207) or in the three-month postoperative best corrected visual acuities among the three groups (p = 0.189). CONCLUSIONS: Importantly, there appears to be a significant correlation between alpha1AB and the development of IFIS. To prevent complications of IFIS, surgeons should be vigilant in identifying patients taking alpha1AB, checking the degree of preoperative pupil dilatation and anticipating intraoperative difficulties. In addition, appropriate modifications should be made to the surgical strategy. Furthermore there was no benefit to discontinuing alpha1AB treatment before cataract surgery in the prevention of IFIS.

Update on congenital glaucoma.

Congenital glaucoma is a global problem and poses a diagnostic and therapeutic challenge to the ophthalmologist. A detailed evaluation under general anesthesia is advisable to establish the diagnosis and plan for management. Medical therapy has a limited role and surgery remains the primary therapeutic modality. While goniotomy or trabeculotomy ab externo is valuable in the management of congenital glaucoma, primary combined trabeculotomy–trabeculectomy offers the best hope of success in advanced cases. Trabeculectomy with antifibrotic agent and glaucoma drainage devices has a role in the management of refractory cases, and cyclodestructive procedures should be reserved for patients where these procedures have failed. Early diagnosis, prompt therapeutic intervention and proper refractive correction are keys to success. Management of residual vision and visual rehabilitation should be an integral part of the management of children with low vision and lifelong follow-up is a must.

Neuroprotection in glaucoma.

Glaucoma is a neurodegenerative disease characterized by loss of retinal ganglion cells and their axons. Recent evidence suggests that intraocular pressure (IOP) is only one of the many risk factors for this disease. Current treatment options for this disease have been limited to the reduction of IOP; however, it is clear now that the disease progression continues in many patients despite effective lowering of IOP. In the search for newer modalities in treating this disease, much data have emerged from experimental research the world over, suggesting various pathological processes involved in this disease and newer possible strategies to treat it. This review article looks into the current understanding of the pathophysiology of glaucoma, the importance of neuroprotection, the various possible pharmacological approaches for neuroprotection and evidence of current available medications.

Avaliação dos efeitos do betabloqueador nebivolol sobre o peritônio em modelo experimental murino de diálise peritoneal / Assessment of the effects of beta-blocker nebivolol on the peritoneum in an experimental murine model of peritoneal dialysis

A falência de ultrafiltração (UFF) é uma causa importante de interrupção da diálise peritoneal (DP) enquanto terapia renal substitutiva. Além da inflamação crônica e aguda causadas à membrana peritoneal (MP) pelos produtos de degradação da glicose, produtos avançados da glicosilação, pH ácido das soluções e infecções, -bloqueadores (BB) também foram implicados na gênese da UFF. A vasoconstrição arteriolar esplâncnica é considerada a causa provável da UFF por BB. O nebivolol (NV), um bloqueador 1-adrenérgico altamente seletivo que, diferente de outros BB, possui efeito vasodilatador por aumento de óxido nítrico (NO) por ativar a via L-arginina-NO, foi testado em pacientes idosos com ICC e levou à redução na mortalidade. O objetivo desse estudo é analisar os efeitos do NV sobre a ultrafiltração (UF), MP e características do efluente em um modelo animal de DP, através do estudo de fenômenos envolvidos na degeneração da MP e UFF, como transição epitélio mesenquimal (EMT) e fibrose, além de parâmetros humorais e celulares de inflamação. 21 camundongos C57BL/6 fêmeas, não urêmicos, com 12 a 14 semanas, foram submetidos à colocação de cateter peritoneal. Após uma semana, foram divididos em 3 grupos de 7 animais: grupo controle (observação 30 dias), grupo SDP (2 mL/ dia de solução glicosada de diálise peritoneal a 4,25% através do cateter, por 30 dias) e grupo NV (além da infusão, receberam 8 mg/kg/dia de NV por gavagem, por 30 dias). Após 30 dias, comparou-se espessura submesotelial, volume de UF, velocidades de transporte de pequenos solutos, marcação submesotelial de pan-citoqueratina, para quantificar EMT, contagem de vasos, linfangiogênese diafragmática e concentração de IL-6 e IL-10 no efluente...

Ultrafiltration failure (UFF) is a major cause of peritoneal dialysis (PD) discontinuation. Besides peritoneal membrane (PM) acute and chronic inflammation caused by glucose degradation products, advanced glycation end-products, acidic pH of the solutions and peritoneal infections, also -blockers (BBs) have been implicated in UFF genesis. Splanchnic arteriolar vasoconstriction has been considered the probable cause of UFF induced by BBs. Nebivolol (NV), a highly selective 1-adrenergic blocker, unlike other BBs, has a vasodilatory effect caused by its ability to increase nitric oxide (NO) through L-arginine-NO pathway activation. NV has been tested in elderly patients with congestive heart failure and led to mortality reduction. The aim of this work is to analyze the effects of NV over ultrafiltration (UF), PM and effluent characteristics in an animal model of PD. For that end, phenomena known to be involved in PM degeneration and UFF, such as epithelial-to-mesenchymal transition (EMT), fibrosis, as well as cellular and humoral parameters of inflammation have been studied. 21 C57BL/ 6 female non uremic mice, ageing 12 to 14 weeks, underwent peritoneal catheter placement. One week later, they were divided into 3 groups of 7 animals: control group (observation for 30 day), PDF group (2 mL/ day of 4.25% dextrose peritoneal dialysis fluid injected through the catheter for 30 days) and NV group (besides the PDF infusion, this group received 8 mg/ kg/ day of NV by gavage, for 30 days). After 30 days, submesotelial thickness, UF volume, small solute transport speed, submesotelial pan-cytokeratin staining (EMT quantification), vessel count, diaphragmatic lymphangiogenesis and IL-6 and IL-10 concentrations in the effluent were compared. PM thickness was 23.14 m in the control group, 102.4 m in the PDF group and 29.04 m in the NV group, p <0.05...

Analgesic Mechanism of Electroacupuncture in an Arthritic Pain Model of Rats: A Neurotransmitter Study

PURPOSE: We investigated what kinds of neurotransmitters are related with electroacupuncture (EA) analgesia in an arthritic pain model of rats. MATERIALS AND METHODS: One hundred rats were assigned to six groups: control, EA, opioid, adrenergic, serotonin and dopamine group. A standardized model of inflammatory arthritis was produced by injecting 2% carrageenan into the knee joint cavity. EA was applied to an acupoint for 30 min in all groups except fo the control group. In the opioid, adrenergic, serotonin and dopamine groups, each receptor antagonist was injected intraperitoneally to their respective group before initiating EA. RESULTS: In the opioid receptor antagonist group, adrenergic receptor antagonist group, serotonin receptor antagonist group, dopamine receptor antagonist group and the control group weight-bearing force decreased significantly from 30 min to 180 min after EA in comparison with the EA group. CONCLUSION: The analgesic effects of EA are related to opioid, adrenergic, serotonin and dopamine receptors in an arthritic pain model of rats.

Experience of Combination Therapy with Alpha Adrenergic Receptor Antagonist and Anticholinergic Agent in Patients with Lower Urinary Tract Symptoms/Benign Prostatic Hyperplasia: 12 Month Follow-up / 대한남성과학회지

PURPOSE: Through more than 12 months of follow-up, the efficacy and safety of combination therapy with alpha adrenergic receptor antagonist and anticholinergic agent was investigated retrospectively. MATERIALS AND METHODS: This study retrospectively analyzed the data of 84 patients with lower urinary tract symptoms (LUTS)/benign prostatic hyperplasia (BPH) who were managed with an alpha adrenergic receptor antagonist and anticholinergic agent for at least 12 months between Jan 2007 and Dec 2010. On patients' first visit to our department, we obtained the patients' demographic data and information about the prostate total volume, serum prostate specific antigen (sPSA), maximum urinary flow rate (Qmax), International Prostate Symptom Score (IPSS), and postvoid residual (PVR) of each patient. After 12 months, changes in the above factors and the side-effects of anticholinergic agents were investigated. RESULTS: The mean age of the patients was 66.1 years and the total observation period after drug administration was an average 20 months; the total sPSA and prostatic volume of patients was 1.8+/-0.8 ng/dl and 37.3+/-9.5 g, respectively. Qmax in uroflowmetry was improved after 12 months of medication (changed from 9.0+/-3.4 to 13.8+/-4.5 ml/sec; p<0.001). PVR was increased from 35+/-22.2 ml to 49.3+/-37 ml (p<0.001), but the change was not clinically significant, and no acute urinary retention occurred. The total IPSS score decreased from 21.4+/-5.1 to 13.3+/-4.6 (p<0.001), the storage score of IPSS decreased from 9.8+/-2.4 to 5.6+/-2 (p<0.001), and the voiding score was decreased from 11.6+/-3.7 to 7.7+/-3.2 (p<0.001). The QoL with IPSS was improved from 4.2+/-0.8 to 2.8+/-0.7 (p<0.001). During the 12 months there were 34 patients (56 cases) of adverse events. However, no serious adverse events were reported. CONCLUSIONS: Combination therapy with alpha adrenergic receptor antagonist and anticholinergic agent was safe and made an improvement in LUTS in patients with BPH and storage symptoms.

Roles of Serotonergic and Adrenergic Receptors in the Antinociception of Selective Cyclooxygenase-2 Inhibitor in the Rat Spinal Cord

BACKGROUND: The analgesic mechanisms of cyclooxygenase (COX)-2 inhibitors have been explained mainly on the basis of the inhibition of prostaglandin biosynthesis. However, several lines of evidence suggest that their analgesic effects are mediated through serotonergic or adrenergic transmissions. We investigated the roles of these neurotransmitters in the antinociception of a selective COX-2 inhibitor at the spinal level. METHODS: DUP-697, a selective COX-2 inhibitor, was delivered through an intrathecal catheter to male Sprague-Dawley rats to examine its effect on the flinching responses evoked by formalin injection into the hindpaw. Subsequently, the effects of intrathecal pretreatment with dihydroergocristine, prazosin, and yohimbine, which are serotonergic, alpha1 adrenergic and alpha2 adrenergic receptor antagonists, respectively, on the analgesia induced by DUP-697 were assessed. RESULTS: Intrathecal DUP-697 reduced the flinching response evoked by formalin injection during phase 1 and 2. But, intrathecal dihydroergocristine, prazosin, and yohimbine had little effect on the antinociception of intrathecal DUP-697 during both phases of the formalin test. CONCLUSIONS: Intrathecal DUP-697, a selective COX-2 inhibitor, effectively relieved inflammatory pain in rats. Either the serotonergic or adrenergic transmissions might not be involved in the analgesic activity of COX-2 inhibitors at the spinal level.

Terapia de resgate com amiodarona em crianças com grave disfunção ventricular esquerda causada por veneno de escorpião / Antiadrenergic rescue therapy with amiodarone in children with severe left ventricular dysfunction secondary to scorpion envenomation / Terapia de rescate con amiodarona en niños con severa disfunción ventricular izquierda ocasionada por veneno de escorpión

Fundamentos: As crianças picadas por escorpião, pressintam ativação maciça do sistema nervoso simpática com vários graus de disfunção sistólica ventricular esquerda. Oobjetivo: Testar um protocolo de resgate em crianças com grave disfunção ventricular esquerda causada por picada de escorpião. Métodos: Quatro crianças após serem picadas por escorpião foram submetidas a: Encubação endotraqueal e suporte respiratório, eletrocardiograma, radiografia de tórax, ecocardiograma e determinação sérica da norepinefrina e troponina I. As análises foram repetidas após 12, 24 e 48 horas. As seguintes medicações intravenosas foram administradas: dobutamina 4-6 μg/kg/min; amiodarona 3 mg/kg durante duas horas, com dose de manutenção de 5 mg/kg/dia; e furosemida 0,5 mg/kg. Amiodarona, dobutamina e furosemida foram administradas durante as primeiras 48 horas. Bloqueadores beta-adrenérgicos e inibidores da enzima conversora da angiotensina foram administrados até 48 após a internação, uma vez que o estado clínico havia melhorado e a fração de ejeção ventricular esquerda encontrava-se acima de 0,35 por cento. Resultados: Na admissão, a dosagem da norepinefrina foi 1.727,50± 794,96 pg/ml, a de troponina I 24,53 ± 14,09 ng/ml e a fração de ejeção do ventrículo esquerdo foi 0,20 ± 0,056. Após 12 horas, os níveis séricos de norepinefrina e de troponina I diminuíram para a metade dos valores iniciais e a fração de ejeção aumentou para 0,32 ± 0,059. Durante as 24 e 48 horas subseqüentes, a fração de ejeção elevou-se para 0,46 ± 0,045 (p<0,01) e a norepinefrina e de troponina I diminuíram para 526,75 ± 273,73 (p< 0,02) e 2,20 ± 2,36 (p<0,02) respectivamente. Conclusão: É bem provável que a amiodarona, ao agir como neuromodulador, seja responsável pela redução rápida e progressiva dos níveis séricos de norepinefrina.

Background: Children with scorpion envenomation have massive sympathetic activation and variable degrees of left ventricular systolic dysfunction. Objective: To evaluate a rescue protocol for children with severe left ventricular dysfunction secondary to scorpion envenomation. Methods: Four children, after scorpion envenomation, were subjected to a rescue protocol for acute left ventricular dysfunction: Endotracheal intubation and respiratory assistance, electrocardiograms, chest x-Ray, echocardiograms and blood samples for norepinephrine and troponin I serum levels. Samples and echocardiograms were repeated at 12, 24 and 48 hours. Intravenous medications: Dobutamine: 4-6 μg/kg/min. Amiodarone: 3 mg/kg during a 2 hour period. Maintenance: 5 mg/kg/day. Furosemide: 0.5 mg/kg/dose. Diuretics were given when the systemic blood pressure was above percentile fifty. Amiodarone, Dobutamine and Furosemide were administered during the first 48 hours. Beta-adrenergic blockers and angiotensin converting enzyme were given, at 48 hours after admission, once the left ventricular Ejection fraction > 0.35 and the clinical status had improved. Results: On admission, norepinephrine was 1,727.50 ±794.96 pg/ml, troponin I 24.53 ± 14.09 ng/ml and left ventricular ejection fraction 0.20 ± 0.056. At twelve hours, norepinephrine and troponin I serum levels were down to half of the initial values and the ejection fraction increased to 0.32 ± 0.059. During the next 24 and 48 hours, the ejection fraction rose to 0.46 ± 0.045, (p<0.01) and norepinephrine and troponin diminished to 526.75 ± 273.73 (p < 0.02) and 2.20 ± 2.36 (p<0.02) respectively. Conclusion: Amiodarone, by acting as a neuromodulator, is very likely responsible for the early and progressive decrease of serum norepinephrine.

Fundamento: Los niños con picaduras de escorpión sufren activación masiva del sistema nervioso simpático con varios grados de disfunción sistólica ventricular izquierda. Objetivo: Probar un protocolo de rescate en niños con disfunción ventricular severa izquierda ocasionada por picadura de escorpión. Métodos: Cuatro niños tras un escorpión picarlas se sometieron a: incubación endotraqueal y soporte respiratorio, electrocardiograma, radiografía de tórax, ecocardiograma y determinación sérica de la norepinefrina y troponina I. Los análisis se repitieron tras 12, 24 y 48 horas. Las siguientes medicaciones intravenosas se administraron: dobutamina 4-6 mcg/kg/min; amiodarona 3 mg/kg durante dos horas, con dosis de mantenimiento de 5 mg/kg/día; y furosemida 0.5 mg/kg. Amiodarona, dobutamina y furosemida se administraron durante las primeras 48 horas. Bloqueante betaadrenergicos e inhibidores de la enzima convertidora de la angiotensina se administraron hasta 48 tras la internación, una vez que el estado clínico había mejorado y la fracción de eyección ventricular izquierda se hallaba superior a un 0,35 por ciento. Resultados: Al ingreso, la dosificación de la norepinefrina fue 1727,50± 794,96 pg/ml, la de troponina I 24,53 ± 14,09 ng/ml y la fracción de eyección del ventrículo izquierdo fue 0,20 ± 0,056. Tras 12 horas, los niveles séricos de norepinefrina y de troponina I disminuyeron para la mitad de los valores iniciales y la fracción de eyección aumentó para 0,32 ± 0,059. Durante las 24 y 48 horas subsiguientes, la fracción de eyección se elevó para 0,46 ± 0,045 (p<0,01) y la norepinefrina y de troponina I se redujeron para 526,75 ± 273,73 (p< 0,02) y 2,20 ± 2,36 (p<0,02) respectivamente. Conclusión: Es bien probable que la amiodarona, al actuar como neuromodulador, sea responsable de la reducción rápida y progresiva de los niveles séricos de norepinefrina.

El triple componente cromático de las experiencias: memoria, emoción y sistema nervioso autónomo / The triple chromatic component of experience: memory, emotion, and autonomic nervous system

La memoria y la emoción son temas de extenso e intenso estudio dentro de la comunidad científica mundial pues impactan directamente en la construcción del historial de las comunidades sobre el que se fundamenta la preservación de la especie, los repertorios de interacción entre individuos de una comunidad y en el caso de los humanos sirven de fundamento para la construcción de la sociedad y sus diferentes áreas de progreso. Desde hace algún tiempo surgieron dos teorías contrapuestas sobre el origen de las emociones y debido al auge histórico del momento tuvo mayor preponderancia la que daba preferencia al cerebro como el órgano que generaba las distintas experiencias que podían establecer una emoción; no obstante, experiencias recientes han demostrado que el componente periférico del sistema nervioso autónomo tiene una fuerte influencia sobre las emociones y que las intervenciones sobre dicho sistema pueden interferir de forma deletérea o no en la creación de memoria de dichos eventos, es decir en la memoria emocional. [Delgado HD. El triple componente cromático de las experiencias: memoria, emoción y sistema nervioso autónomo. MedUNAB 2009; 12:52-61].

Memory and emotion are topics of intense and widespread scientific research all over the world because they have a direct impact in communities through the construction of history which underpins vital functions like preservation of species, interaction repertories among community members and in the case of humans they serve as a fundamental pillar in the construction of society and its different areas of development. Some time ago, there emerged two conflicting theories about the origin of emotion and due to the boom of historic moment, the one proclaiming the brain as the experience-emotion generating organ had preponderancy; however, recent findings had demonstrated that peripheral components of autonomous nervous system have a strong influence on emotions and the interventions in this nervous system could interfere in the creation of memory, in other words, interfere in the emotional memory. [Delgado HD. The triple chromatic component of experience: Memory, emotion, and autonomic nervous system. MedUNAB 2009; 12:52-61].

A Case of Intraoperative Floppy Iris Syndrome in a Patient Using Tamsulosin

PURPOSE: To report a case of Intraoperative Floppy Iris Syndrome (IFIS) experienced during pars plana vitrectomy and phacoemulsification in a patient using tamsulosin, which is a selective alpha 1 adrenergic antagonist. CASE SUMMARY: A 77-year-old male who had used tamsulosin for the previous month for prostate cancer visited our clinic with left visual disturbance, that had developed a week earlier. The best-corrected visual acuity of the left eye was 0.02 and both pupils showed incomplete mydriasis. Pars plana vitrectomy and phacoemulsification with PCL implantation were performed on his left eye to correct a left cataract and retinal vein occlusion with vitreous hemorrhage. Phacoemulsification idenfied a billowing iris and progressive pupillary constriction. Therefore, we administered an intracameral epinephrine injection and applied an iris hook. The procedure was completed successfully without any complications. The best-corrected visual acuity of the left eye was good as at 0.9, and iris depigmentation and atrophy were checked two months postoperatively in the right eye, which had not had any previous surgical history. CONCLUSIONS: A detailed medical history taking is essential because IFIS may raise the risk of intraoperative complications, such as posterior capsule rupture, especially when the small pupil is small. Safe procedures must be planned with cessation of tamsulosin at least a week preoperatively.

Alpha1 and alpha2 adrenoceptor mediated melanosome aggregatory responses in vitro in Oreochromis mossambica (Peters) melanophores.

Effects of specific and non-specific adrenoceptor agonists and antagonists were examined on the isolated scale melanophores of O. mossambica in physiological Ringer solution. The responses were recorded as melanophore size index. It was observed that adrenaline, nor-adrenaline, phenylpropanolamine, clonidine and phenylepherine induced melanosome aggregation in a dose-dependent manner. Denervation of the fish melanophores increased the sensitivity of the melanophores to adrenaline but not to nor-adrenaline. Phentolamine (3.55 x 10(-5) M), prazosin (2.38 x 10(-5) M) and yohimbine (2.821 x 10(-5) M) significantly inhibited the aggregatory responses of the fish melanophores to adrenaline, nor-adrenaline, clonidine and phenylepherine. The blocking effect of yohimbine was significantly higher than that of prazosin. It is concluded that the effect of adrenaline is directly mediated through the receptors and alpha2 adrenoceptors are predominantly involved in the aggregatory responses of this fish melanophores, while alpha1 adrenoceptors presence has been indicated.