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1.
Pharm Dev Technol ; 26(5): 610-616, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33736577

RESUMO

Etilefrine hydrochloride (ET) is an important drug in the treatment of hypotension, and parenteral injections and oral tablets are the conventional dosage forms. However, parenteral injections may cause abnormally high plasma levels as well as pain and necrosis, and oral tablets undergo first-pass metabolism. Although fast-dissolving buccal tablets were previously reported, the initial absorption rate was a little slow and the plasma levels were varied extensively. Recently, many films have been developed as novel dosage forms. Therefore, in the present study, film dosage forms containing ET were produced using water-soluble polymers and glycerin (GLY) as excipients to obtain a practical buccal dosage form. Films composed of ET, GLY, and sodium alginate (AL) exhibited good physical characteristics and rapid release in vitro (more than 70% at 2 min). The compacted AL film containing 2 mg ET (1 × 1 cm) exhibited rapid absorption (>19 ng/mL at 0.5 h), maintained an effective plasma level (>7 ng/mL) for a long time period (0.5-4 h), and had an adequate plasma concentration-time profile with a smaller standard error (<15.3 ng/mL). These results suggest that the present compacted buccal film is a superior dosage form of ET for practical use.


Assuntos
Etilefrina/administração & dosagem , Excipientes/química , Vasoconstritores/administração & dosagem , Administração Bucal , Alginatos/química , Animais , Química Farmacêutica , Liberação Controlada de Fármacos , Etilefrina/química , Etilefrina/farmacocinética , Glicerol/química , Masculino , Polímeros/química , Ratos , Ratos Wistar , Solubilidade , Comprimidos , Vasoconstritores/química , Vasoconstritores/farmacocinética
2.
Eur Ann Otorhinolaryngol Head Neck Dis ; 138(5): 383-386, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33608232

RESUMO

BACKGROUND: Intraoperative injury of the thoracic duct is an uncommon complication of head and neck surgery, which is difficult to manage and associated with serious consequences. We report a case of lymphorrhoea of the neck refractory to all the usual treatments that resolved in response to a treatment strategy described in thoracic and visceral surgery: use of a sympathomimetic drug, etilefrine. To our knowledge and after review of the literature, this is the first reported case of lymphorrhoea of the neck treated by etilefrine. CASE REPORT: Our patient presented massive lymphatic fluid leakage following left neck dissection as part of the management of oropharyngeal cancer with lymph node metastases. The treatments usually proposed, such as intraoperative repair and appropriate dietary and drug management, were not effective, resulting in multiple, severe complications. After evaluation of the benefit-risk balance, treatment with etilefrine was introduced at the dosages proposed in the literature for the management of chylothorax. This treatment allowed complete resolution of the lymphatic fluid leak after one week. DISCUSSION: Etilefrine can therefore be added to the treatment options for the management of lymphatic fluid leaks refractory to the usual treatments.


Assuntos
Quilotórax , Etilefrina , Quilotórax/cirurgia , Humanos , Pescoço , Esvaziamento Cervical , Ducto Torácico
3.
Gac. méd. boliv ; 43(2): 162-169, dic. 2020. ilus
Artigo em Espanhol | LILACS | ID: biblio-1249997

RESUMO

Dexmedetomidina un α- agonista, de amplio uso y popular nivel mundial, que poco conocimiento se tiene sobre su uso de forma intratecal en la población boliviana, de manera especial en pacientes obstétricas. OBJETIVOS: evaluar el efecto de dexmedetomidina intratecal en anestesia obstétrica y observar los efectos secundarios del medicamento. MÉTODOS: ensayo clínico aleatorizado y simple ciego. La muestra fue de 123 pacientes, cada grupo de 41 pacientes cumpliendo ambos criterios. Grupo B (bupivacaina + fentanil); grupo D2 (bupivacaina + fentanil+ dexmedetomidina 2 µg) y grupo B3 (bupivacaina + fentanil+ dexmedetomidina 3 µg). Análisis estadístico: se utilizó el software SPSS® 25 y Excel® 2016. Con un nivel de confianza del 95 % y error muestral del 13 %. RESULTADOS: duración del bloqueo motor fue de 106,5 ± 16 minutos en el grupo B; 142,3 ± 28,2 minutos en el grupo D2 y 145,6 ± 16,7 minutos en el grupo D3. Siendo significativo entre los grupos de estudio (valor p < 0,000). PAM con significancia estadística antes y después del nacimiento. Frecuencia cardiaca significativo a los 15, 30 y 45 minutos (valor p < 0,000; 0,001; 0,004; 0,000 y 0,002). Etilefrina en el grupo B fue de 3,44 ± 1,8 ml; para el grupo D3 fue de 1,8 ± 2,7 ml y grupo D2 fue de 0,85 ± 1,6 ml. CONCLUSIONES: mejor estabilidad hemodinámica con 2 µg dexmedetomidina, menor incidencia de hipotensión, uso de vasopresores, las complicaciones escasas y un excelente estado de sedación materna


Dexmedetomidine an α-agonist, widely used and popular worldwide, with little knowledge about its use intrathecally in the Bolivian population, especially in obstetric patients. OBJECTIVES: evaluate the effect of spinal dexmedetomidine in obstetric anesthesia and observe the side effects of the medication. METHODS: randomized and simple blind clinical trial. The sample consisted of 123 patients, each group of 41 patients meeting both criteria. Group B (bupivacaine + fentanyl); group D2 (bupivacaine + fentanyl + 2 µg dexmedetomidine) and group B3 (bupivacaine + fentanyl + 3 µg dexmedetomidine). Statistical analysis: it was carried out in SPSS® 25 and Microsoft Excel® 2016. With a confidence level of 95% and sampling error of 13%. RESULTS: duration of the motor block was 106,5 ± 16 minutes in group B; 142,3 ± 28,2 minutes in group D2 and 145,6 ± 16,7 minutes in group D3. Being significant among the study groups (p value <0,000). MAP with statistical significance before and after birth. Significant heart rate at 15, 30 and 45 minutes (p value <0,000; 0,001; 0,004; 0.000 and 0,002). Ethylephrine in group B was 3,44 ± 1,8 ml; for group D3 it was 1,8 ± 2,7 ml and group D2 was 0,85 ± 1,6 ml CONCLUSIONS: better hemodynamic stability with 2 µg dexmedetomidine, lower incidence of hypotension, use of vasopressors, limited complications and an excellent state of maternal sedation.


Assuntos
Humanos , Feminino , Gravidez , Cesárea , Dexmedetomidina , Raquianestesia , Pacientes , Etilefrina , Frequência Cardíaca
4.
Pharm Dev Technol ; 25(9): 1162-1167, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32644855

RESUMO

Etilefrine hydrochloride (ET) is commonly used in the treatment of hypotension in dosage forms of oral tablets and parenteral injections. However, oral tablets only temporarily achieve high plasma levels and have low bioavailability (BA), while intravenous injections may cause pain and necrosis around administration sites. In an attempt to overcome these limitations, the buccal delivery of ET using oral droplets has been investigated. In this study, a buccal tablet as an alternative dosage form was developed for practical use. Buccal tablets were prepared by the direct compression method with sodium alginate (AL) and mannitol (MA) as excipients. Their disintegration and in vitro drug release were rapid (more than 50% being released after 3 min). Furthermore, effective plasma levels (> 5-7 ng/mL) were reached within 0.5 h of buccal administration in rats. The systemic absorption of these tablets was similar to that of buccal droplets. Therefore, the ET buccal tablets developed herein have potential as an alternative dosage form for hypotension therapy.


Assuntos
Etilefrina/química , Comprimidos/química , Administração Bucal , Alginatos/química , Animais , Disponibilidade Biológica , Liberação Controlada de Fármacos/efeitos dos fármacos , Excipientes/química , Masculino , Ratos , Ratos Wistar , Solubilidade/efeitos dos fármacos
5.
Cochrane Database Syst Rev ; 4: CD004198, 2020 04 06.
Artigo em Inglês | MEDLINE | ID: mdl-32251534

RESUMO

BACKGROUND: Sickle cell disease comprises a group of genetic haemoglobin disorders. The predominant symptom associated with sickle cell disease is pain resulting from the occlusion of small blood vessels by abnormally 'sickle-shaped' red blood cells. There are other complications, including chronic organ damage and prolonged painful erection of the penis, known as priapism. Severity of sickle cell disease is variable, and treatment is usually symptomatic. Priapism affects up to half of all men with sickle cell disease, however, there is no consistency in treatment. We therefore need to know the best way of treating this complication in order to offer an effective interventional approach to all affected individuals. This is an update of a previously published review. OBJECTIVES: To assess the benefits and risks of different treatments for stuttering (repeated short episodes) and fulminant (lasting for six hours or more) priapism in sickle cell disease. SEARCH METHODS: We searched the Cochrane Cystic Fibrosis and Genetic Disorders Group Haemoglobinopathies Trials Register, which comprises references identified from comprehensive electronic database searches and handsearches of relevant journals and abstract books of conference proceedings. We also searched trial registries. Date of the most recent search of the Group's Haemoglobinopathies Trials Register: 09 September 2019. Date of most recent search of trial registries and of Embase: 01 October 2019. SELECTION CRITERIA: All randomised or quasi-randomised controlled trials comparing non-surgical or surgical treatment with placebo or no treatment, or with another intervention for stuttering or fulminant priapism. DATA COLLECTION AND ANALYSIS: The authors independently extracted data and assessed the risk of bias of the trials. MAIN RESULTS: Three trials with 102 participants were identified and met the criteria for inclusion in this review. These trials compared stilboestrol to placebo, sildenafil to placebo and a four-arm trial which compared ephedrine or etilefrine to placebo and ranged in duration from two weeks to six months. All of the trials were conducted in an outpatient setting in Jamaica, Nigeria and the UK. None of the trials measured our first primary outcome, detumescence. However, all three trials reported on the reduction in frequency of stuttering priapism, our second primary outcome; and from the evidence included in this review, we are uncertain whether stilboestrol, etilefrine or ephedrine reduce the frequency of stuttering priapism as the certainty of the evidence has been assessed as very low. Additionally, we conclude that sildenafil may make little or no difference (low-certainty evidence). Two trials reported on immediate side effects and we are uncertain whether etilefrine or ephedrine reduce the occurrence of these (very low-certainty of evidence) and also conclude that sildenafil may make little or no difference in side effects (low-quality evidence). Given that all of the trials were at risk of bias and all had low participant numbers, we considered the certainty of the evidence to be low to very low. AUTHORS' CONCLUSIONS: There is a lack of evidence for the benefits or risks of the different treatments for both stuttering and fulminant priapism in sickle cell disease. This systematic review has clearly identified the need for well-designed, adequately-powered, multicentre randomised controlled trials assessing the effectiveness of specific interventions for priapism in sickle cell disease.


Assuntos
Anemia Falciforme/complicações , Dietilestilbestrol/uso terapêutico , Estrogênios não Esteroides/uso terapêutico , Priapismo/tratamento farmacológico , Vasoconstritores/uso terapêutico , Adrenérgicos/efeitos adversos , Adrenérgicos/uso terapêutico , Efedrina/efeitos adversos , Efedrina/uso terapêutico , Etilefrina/efeitos adversos , Etilefrina/uso terapêutico , Humanos , Masculino , Priapismo/etiologia , Ensaios Clínicos Controlados Aleatórios como Assunto , Citrato de Sildenafila/uso terapêutico , Taquicardia/induzido quimicamente , Vasoconstritores/efeitos adversos , Adulto Jovem
6.
Artigo em Inglês | MEDLINE | ID: mdl-30502391

RESUMO

INTRODUCTION: The in vivo disposition and metabolism of phenylephrine have not been establishedby previous analytical methods and there is a lack of available standards for quantitating the metabolites. METHODS: We pursued and compared the preparation of sulfation metabolites of phenylephrine and its ethyl analog etilefrine via chemical and bio-synthesis. RESULTS: Both sulfates were obtained in higher yield and purity through chemical syntheses compared to biosynthesis. DISCUSSION: A facile method for the production of phenylephrine 3-O-sulfate and etilefrine 3-O-sulfate was established. These compounds will be useful in the development of analytical assays for studying the pharmacokinetics of phenylephrine and its main route of metabolism in the presence of formulation changes and pharmacogenetic variation.


Assuntos
Etilefrina/síntese química , Descongestionantes Nasais/síntese química , Fenilefrina/síntese química , Sulfatos/síntese química , Avaliação Pré-Clínica de Medicamentos/métodos , Etilefrina/metabolismo , Etilefrina/farmacocinética , Descongestionantes Nasais/metabolismo , Descongestionantes Nasais/farmacocinética , Variantes Farmacogenômicos , Fenilefrina/metabolismo , Fenilefrina/farmacocinética , Sulfatos/metabolismo , Sulfatos/farmacocinética
7.
Biosci Trends ; 12(4): 382-388, 2018 Sep 19.
Artigo em Inglês | MEDLINE | ID: mdl-30101824

RESUMO

Hypotension commonly accompanies combined epidural and general anesthesia, and intravenous bolus ephedrine and etilefrine are widely used to correct hypotension. We have noticed that systemic vascular resistance (SVR) transiently decreases just after intravenous bolus administration of these drugs. The goal of the present study was to investigate whether bolus administration of these drugs decrease SVR just after intravenous administration in combined epidural and general anesthesia patients. We investigated 40 patients who were scheduled for elective abdominal surgery. Patients were chosen as subjects if their systolic arterial pressure decreased by 20% or to <100 mmHg at 30 min after the induction of general anesthesia. Baseline hemodynamic values were recorded, and after ephedrine 10 mg injection or etilefrine 2 mg injection (equipotent), the parameters were recorded again at 0.5 min and once each min for the next 5 min thereafter. The 40 patients were enrolled into the ephedrine (n = 20) or etilefrine (n = 20) treatment groups. Patient characteristics were comparable in both groups. After ephedrine injection, SVR decreased significantly at the 1-min time point, whereas after etilefrine injection, SVR decreased significantly at the 0.5- to 2-min time points compared with baseline values. SVR at the 0.5- to 1-min time points was lower in the etilefrine versus the ephedrine group. Both drugs transiently decreased SVR after intravenous injection, but etilefrine decreased SVR much more than ephedrine, indicating that more vasodilation occurred after the injection of etilefrine than after ephedrine. It is thus important to recognize the different characteristics of these drugs.


Assuntos
Anestesia Epidural/métodos , Anestesia Geral/métodos , Efedrina/farmacologia , Etilefrina/farmacologia , Adulto , Pressão Sanguínea/efeitos dos fármacos , Feminino , Frequência Cardíaca/efeitos dos fármacos , Hemodinâmica/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Vasodilatação/efeitos dos fármacos
8.
Int J Pharm ; 550(1-2): 14-23, 2018 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-30107221

RESUMO

Etilefrine hydrochloride (ET-HCl) is used in the treatment of hypotension. Dosage forms of orally administered tablets and parenteral injections are clinically available, but exhibit unfavorable characteristics, including cardiac toxicity, headaches, and damage at the injection site for the parenteral dosage form, and initially high plasma levels, fast elimination, and first-pass effects for its oral administration. Therefore, the buccal application of ET-HCl was herein investigated as an alternative to conventional administration routes. I.v., intragastric, and buccal administration were performed using rats, and absorption features were compared. Buccal application at open conditions for 1 h exhibited absolute bioavailability of more than 20%, while the intragastric administration gave much lower bioavailability (<10%). The drug residue and drug distribution in the oral mucosa were investigated in order to clarify drug transfer behaviors. In the application of ET-HCl solution using a cotton ball, higher plasma concentrations and their maintenance at higher levels were achieved at 10 mg/kg than at 2.5 mg/kg. In addition, absorption was greater with a longer application (4 h) than with a shorter application (1 h). Etilefrine (ET) was rapidly absorbed using aqueous buffer of pH 9.5 as the solvent. Open application was appropriate for achieving and maintaining higher plasma levels. Thus, in the buccal application of ET-HCl aqueous droplets, a wide distribution throughout the mucosal surface is important for achieving rapid absorption and the maintenance of plasma levels. These findings suggested that the buccal application should be feasible administration of ET-HCl.


Assuntos
Etilefrina/administração & dosagem , Etilefrina/farmacocinética , Absorção Intestinal , Vasoconstritores/administração & dosagem , Vasoconstritores/farmacocinética , Administração Bucal , Animais , Disponibilidade Biológica , Etilefrina/efeitos adversos , Absorção Intestinal/fisiologia , Masculino , Ratos , Ratos Wistar , Comprimidos/administração & dosagem , Comprimidos/efeitos adversos , Comprimidos/farmacocinética , Vasoconstritores/efeitos adversos
9.
Gan To Kagaku Ryoho ; 45(3): 572-574, 2018 Mar.
Artigo em Japonês | MEDLINE | ID: mdl-29650942

RESUMO

We have report a case of an 81-year-old woman who underwent distal pancreatectomy for pancreatic body cancer. Chy- lous ascites with high triglyceride(TG)level, 201mg/dL, occurred on postoperative day 2. Continuous drainage and conservative management, such as low fat diet, fasting, total parental nutrition, and octreotide monotherapy, could not resolve the problem. Successful treatment was achieved using subcutaneous octreotide injection and intravenous etilefrine infusion without any adverse side-effect. These medications were able to cause smooth muscle contraction in the thoracic duct, and also to reduce chyle flow. The amount of drainage decreased and the TG level was restored to 66mg/dL. The drainage tube was removed on postoperative day 22, 5 days after the start of both octreotide and etilefrine. This combination therapy with octreotide and etilefrine would be one of effective and safety treatment for management of postoperative intractable chylous ascites.


Assuntos
Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Ascite Quilosa/etiologia , Pancreatectomia/efeitos adversos , Neoplasias Pancreáticas/tratamento farmacológico , Complicações Pós-Operatórias , Idoso de 80 Anos ou mais , Ascite Quilosa/terapia , Drenagem , Etilefrina/administração & dosagem , Feminino , Humanos , Octreotida/administração & dosagem , Neoplasias Pancreáticas/cirurgia
10.
Pediatrics ; 141(5)2018 05.
Artigo em Inglês | MEDLINE | ID: mdl-29703801

RESUMO

Chylothorax is defined as the accumulation of chyle within the pleural space. Originally described in 1917 by Pisek, it is the most common cause of pleural effusion in the neonatal period. The leading cause of chylothorax is laceration of the thoracic duct during surgery, which occurs in 0.85% to 6.6% of children undergoing cardiothoracic surgery. Few authors of reports in the literature have looked at etilefrine, a relatively unknown sympathomimetic, as an option for the medical treatment of chylothorax. In this case report, we review the clinical course of 2 infants with type III esophageal atresia who developed chylothorax after thoracic surgery and were successfully treated with intravenous etilefrine after failing initial dietary and pharmacological management.


Assuntos
Quilotórax/tratamento farmacológico , Atresia Esofágica/cirurgia , Etilefrina/uso terapêutico , Simpatomiméticos/uso terapêutico , Procedimentos Cirúrgicos Torácicos/efeitos adversos , Fístula Traqueoesofágica/cirurgia , Quilotórax/etiologia , Etilefrina/administração & dosagem , Feminino , Humanos , Recém-Nascido , Infusões Intravenosas , Masculino , Complicações Pós-Operatórias/tratamento farmacológico , Simpatomiméticos/administração & dosagem
11.
Rev. colomb. anestesiol ; 46(4): 336-340, 2018. graf
Artigo em Inglês | LILACS, COLNAL | ID: biblio-978217

RESUMO

Abstract Introduction: In pregnancies with a diagnosis of fetal myelomeningocele (MMC), studies have shown that prenatal correction, as compared with postnatal correction, results in better outcomes in infancy, requiring less ventriculoperitoneal shunts, and resulting in improved motor function of the lower limbs. However, maternal morbidity, the risk of uterine repair dehiscence, uterine rupture secondary to hysterotomy, and the need for cesarean section are all increased. This case report is the first successful experience of intrauterine repair of a MMC in Peru. Case presentation: We describe the case of a primigravida at 25 weeks of gestation with a diagnosis of fetal malformation (MMC and Arnold Chiari II syndrome) taken to intrauterine correction of the neural tube defect under general anesthesia plus epidural analgesia. Conclusion: The use of total intravenous anesthesia associated with nitroglycerine infusion for uterine relaxation, ethylephrine infusion to maintain maternal hemodynamic stability, and adequate postoperative pain management with epidural analgesia was successful in this case.


Resumen Introducción: En los embarazos con diagnóstico de Mielomeningocele fetal, los estudios han demostrado que la corrección prenatal conlleva a mejores resultados en la infancia que la corrección postnatal, requiriendo menos derivaciones ventrículo peritoneales y mejor función motora de miembros inferiores. Sin embargo se incrementa la morbilidad materna, el riesgo de dehiscencia de histerorrafia, ruptura uterina secundaria a la histerotomía y la necesidad de parto por cesárea. El presente reporte de caso es la primera experiencia exitosa de reparación intrautero de MMC en Peru. Presentación del caso: Describimos el caso de una primigesta de 25 semanas de gestación, con diagnóstico de malformación fetal (Mielomeningocele y Síndrome de Arnold Chiari II) en quien se realizó una corrección intrautero del defecto neural y cuya técnica anestésica fue anestesia general más analgesia epidural. Conclusiones: El uso de anestesia total intravenosa asociado a la infusión de nitroglicerina para la relajación uterina, la infusión de etilefrina para mantener la estabilidad hemodinámica materna y el adecuado manejo del dolor postoperatorio vía epidural fue exitoso en este caso.


Assuntos
Humanos , Feminino , Gravidez , Adulto , Anormalidades Congênitas , Ruptura Uterina , Analgesia Epidural , Meningomielocele , Histerotomia , Anestesia Geral , Defeitos do Tubo Neural , Dor Pós-Operatória , Peru , Cesárea , Derivação Ventriculoperitoneal , Extremidade Inferior , Etilefrina , Anestesia , Anestesia Intravenosa
12.
Luminescence ; 32(5): 706-712, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27900836

RESUMO

A new, simple, sensitive and rapid spectrofluorimetric method has been developed for determination of certain adrenergic agonists such as isoxsuprine hydrochloride, ritodrine hydrochloride and etilefrine hydrochloride in their pure forms and pharmaceutical dosage forms. The method depends on micellar enhancement of the native fluorescence of investigated drugs by using 2% w/v sodium dodecyl sulfate (SDS) as an anionic surfactant. The enhanced fluorescence intensity of investigated drugs was measured at 305 nm after excitation at 278 nm. The interaction of studied drugs with SDS was studied, and the enhanced fluorescence intensity was exploited to develop an assay method for the determination of investigated drugs. The relative fluorescence intensity-concentration plots were rectilinear over the range 0.15-3.00 µg ml-1 , with low quantification limits of 0.132, 0.123 and 0.118 µg mL-1 for isoxsuprine, ritodrine and etilefrine, respectively. The proposed method was successfully applied for determination of studied drugs in their pharmaceutical formulations. Moreover, the high sensitivity of the proposed method allows performing the content uniformity testing of the studied drugs in their tablets by using the official United States Pharmacopeia (USP) guidelines. Statistical comparisons of the results with those of the reported methods revealed excellent agreement and indicated no significant difference in accuracy and precision.


Assuntos
Agonistas Adrenérgicos/análise , Espectrometria de Fluorescência/métodos , Agonistas Adrenérgicos/química , Etilefrina/análise , Etilefrina/química , Concentração de Íons de Hidrogênio , Isoxsuprina/análise , Isoxsuprina/química , Reprodutibilidade dos Testes , Ritodrina/análise , Ritodrina/química , Sensibilidade e Especificidade , Dodecilsulfato de Sódio/química , Solventes/química , Tensoativos/química , Comprimidos/análise , Comprimidos/química , Temperatura , Fatores de Tempo
13.
Medicine (Baltimore) ; 94(49): e2214, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26656358

RESUMO

Postoperative chylothorax is a rare but well-known complication of general thoracic surgery. Medical treatment of chylothorax was reported in the past, but there is still considerable controversy on the appropriate management strategies.Two patients with esophageal cancer underwent esophagectomy, 2-field lymph node dissection, and resection of thoracic duct together with ileocolic reconstruction via the retrosternal route at our hospital. Chylothorax developed on the 32nd postoperative day (POD) in 1 patient and the 12th POD in the other, manifesting as a change in the character of thoracic drainage to turbid white. Both were immediately started on octreotide (300 µg/ day) and etilefrine (120 mg/day). When the amount of pleural effusion decreased to <50 mL/day, we performed pleurodesis with Picibanil (OK432). Thereafter, the patients gradually made satisfactory progress and resumed oral food intake, and the thoracotomy tubes were eventually removed. They have remained recurrence-free at the time of writing.In this report, we demonstrated the clinical efficacy of etilefrine for the management of postesophagectomy chylothorax. New medical treatment options for this condition are now broad and the usefulness of combined therapy consisting of a sclerosing agent, etilefrine, and octreotide is underscored, regardless of the status of the thoracic duct.


Assuntos
Quilotórax/tratamento farmacológico , Quilotórax/etiologia , Neoplasias Esofágicas/cirurgia , Esofagectomia/efeitos adversos , Etilefrina/uso terapêutico , Octreotida/uso terapêutico , Adulto , Antineoplásicos/uso terapêutico , Quimioterapia Combinada , Etilefrina/administração & dosagem , Humanos , Masculino , Pessoa de Meia-Idade , Octreotida/administração & dosagem , Picibanil/uso terapêutico , Derrame Pleural/terapia , Pleurodese/métodos
14.
Prescrire Int ; 24(162): 184, 2015 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-26240886

RESUMO

The French Health Products Agency concluded that etilefrine and heptaminol have an unfavourable harm-benefit balance, and also placed restrictions on the use of midodrine.


Assuntos
Etilefrina/efeitos adversos , Heptaminol/efeitos adversos , Hipotensão/tratamento farmacológico , Humanos
15.
Artigo em Inglês | MEDLINE | ID: mdl-26001324

RESUMO

INTRODUCTION: Nonclinical safety studies are increasingly incorporating cardiac safety endpoints to discover potential cardiovascular liabilities. This trend for more thorough cardiovascular nonclinical safety evaluation is prudent given the high attrition rate of potential therapeutics due to unexpected cardiovascular liabilities discovered in late-stage clinical trials or post-market approval. In particular, the causal relationship of blood pressure changes that lead to risk of major adverse cardiac events suggests hemodynamic changes should be critically evaluated in preclinical studies of novel therapeutics. METHODS: Jacketed external telemetry with an implanted miniature blood pressure transmitter (JET-BP) was used to characterize the tolerability, functionality, and sensitivity of this study design in dogs. Thirty-six male or female beagles (n=6 dogs/sex/group) were administered vehicle control (reverse osmosis water) or etilefrine (1, 10mg/kg), sotalol (3, 30mg/kg), and hydralazine (1, 10mg/kg) on separate days. Telemetry data were evaluated for positive control article-related changes and retrospective power analysis was also completed. Animals were evaluated for instrumentation-related changes in clinical and anatomic pathology endpoints. RESULTS: All three positive controls elicited the expected pharmacologic responses that were statistically different at high and low doses. Retrospective power analysis confirmed this study design was able to statistically differentiate minor (approximately 5 to 15%) changes in electrocardiography and blood pressure values. This study also demonstrated the potential advantages of combining cardiovascular data across sex when the test article exposure and pharmacodynamics were consistent. Data collection using miniature telemetry blood pressure transmitters did not result in anatomic or clinical pathology findings that would prevent their use in general toxicology studies. DISCUSSION: This characterization study indicates that JET-BP in dogs offers a scientifically-robust method to evaluate novel therapeutics for potential cardiovascular liabilities.


Assuntos
Pressão Sanguínea/efeitos dos fármacos , Cardiotoxicidade/diagnóstico , Avaliação Pré-Clínica de Medicamentos/métodos , Telemetria/métodos , Animais , Cães , Relação Dose-Resposta a Droga , Eletrocardiografia/métodos , Etilefrina/administração & dosagem , Etilefrina/farmacologia , Feminino , Hidralazina/administração & dosagem , Hidralazina/farmacologia , Masculino , Projetos de Pesquisa , Sotalol/administração & dosagem , Sotalol/farmacologia
16.
Int J Urol ; 22(6): 609-11, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25808696

RESUMO

We describe two cases in which dynamic analysis of ejaculation using color Doppler ultrasonography was useful in diagnosis of ejaculatory dysfunction and planning of therapy. The first patient was a 32-year-old man with a diagnosis of retrograde ejaculation. A bladder neck collagen injection was carried out, as the main cause was thought to be the bladder neck remaining open during ejaculation. The patient had antegrade ejaculation 1 week later. The second patient was a 48-year-old man with a diagnosis of anorgasmia accompanied by decreased seminal emission and insufficient function of the rhythmic pelvic striated muscles. The patient was prescribed etilefrine hydrochloride 15 mg/day. The symptom improved 2 weeks after starting this drug. These cases suggest that the use of color Doppler ultrasonography during ejaculation can improve the understanding of ejaculatory dysfunction and therapy for this condition.


Assuntos
Ejaculação , Disfunções Sexuais Fisiológicas/diagnóstico por imagem , Ultrassonografia Doppler em Cores , Adulto , Colágeno/administração & dosagem , Etilefrina/administração & dosagem , Humanos , Masculino , Pessoa de Meia-Idade , Orgasmo , Disfunções Sexuais Fisiológicas/fisiopatologia , Disfunções Sexuais Fisiológicas/terapia
17.
J Pharmacol Toxicol Methods ; 70(3): 268-75, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25219539

RESUMO

INTRODUCTION: The measurement of cardiovascular endpoints in standard toxicology studies remains a challenge as the routinely used non-invasive methods require physical restraint, causing an increase of sympathetic neural activity, leading to excitement and potentially hypertension in the experimental animals. In this study, a miniature telemetry blood pressure transmitter was used to evaluate if the acute hyper- and hypotension could be detected in free moving cynomolgus monkeys as well as physically restrained animals using positive control drugs. Furthermore, as a comparator, routine high definition oscillometry (HDO) was performed in restrained animals. METHODS: Hemodynamic parameters were monitored continuously from conscious, freely moving animals following oral administration of vehicle (water) or 1 and 10mg/kg of etilefrine, and 1 and 4mg/kg of dihydralazine as positive control articles. A second dose session was performed to confirm the reproducibility of results and a third dose session combined with physical restraint procedures for blood collection and HDO measurements. RESULTS: There was a dose-dependent, statistically significant increase in the systolic blood pressure following oral doses of etilefrine at all 3 dose sessions. This effect was less apparent during session 3, probably due to the physical restraint applied for the blood sampling and HDO measurement. No differences in the blood pressure were measured using HDO. On all three dose sessions following oral doses of dihydralazine the expected statistically significant decrease in the diastolic pressure could be clearly measured even when the telemetric data recordings were combined with physical restraint. DISCUSSION: Due to the advantages of the minimally invasive telemetry technique compared to HDO and the possibility of prolonged measurement periods, it is an invaluable tool for blood pressure measurement in freely moving animals in toxicology studies.


Assuntos
Monitorização Ambulatorial da Pressão Arterial/veterinária , Pressão Sanguínea/efeitos dos fármacos , Di-Hidralazina/toxicidade , Etilefrina/toxicidade , Macaca fascicularis/fisiologia , Restrição Física/veterinária , Administração Oral , Animais , Monitores de Pressão Arterial/veterinária , Di-Hidralazina/administração & dosagem , Relação Dose-Resposta a Droga , Etilefrina/administração & dosagem , Modelos Animais
18.
J Sep Sci ; 37(21): 3015-23, 2014 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-25143252

RESUMO

A sensitive hydrophilic interaction liquid chromatography coupled with tandem mass spectrometry method was developed and validated for the simultaneous detection and quantification of etilefrine and oxilofrine in equine blood plasma and urine. The method is highly sensitive and specific with good precision and accuracy. In plasma the limit of detection and limit of quantification are 0.03 and 0.1 ng/mL, respectively, for both analytes. In urine the limit of detection and limit of quantification are 0.3 and 1 ng/mL, respectively, for both analytes. The suitability of the method for doping control analysis in equine species is demonstrated by analyzing postadministration samples collected after a single intravenous administration of 50 mg etilefrine to a standardbred mare. Etilefrine was detected up to 120 h in urine and up to 48 h in plasma. Etilefrine is highly conjugated in equine urine whereas it exists in the free form in equine plasma. Therefore, enzyme hydrolysis prior to sample preparation is recommended for the detection and quantification of etilefrine and oxilofrine in equine urine.


Assuntos
Cardiotônicos/sangue , Cardiotônicos/urina , Cromatografia Líquida de Alta Pressão/métodos , Efedrina/análogos & derivados , Etilefrina/sangue , Etilefrina/urina , Espectrometria de Massas em Tandem/métodos , Animais , Cromatografia Líquida de Alta Pressão/instrumentação , Doping nos Esportes , Efedrina/sangue , Efedrina/urina , Cavalos , Espectrometria de Massas em Tandem/veterinária
19.
Lima; s.n; 2014. 47 p. tab, graf.
Tese em Espanhol | LIPECS | ID: biblio-1113534

RESUMO

OBJETIVO: Determinar si el uso de etilefrina y fluidos intravenosos previene la hipotensión arterial secundaria a la anestesia raquídea, en pacientes sometidas a cesáreas en el INMP 2013. METODOLOGIA: Estudio de tipo observacional descriptivo, transversal, prospectivo. Realizado en un total de 320 pacientes aproximadamente, las cuales fueron sometidas a cesárea con la técnica de bloqueo subaracnoideo que cumplan con los criterios de inclusión y exclusión durante el periodo de Setiembre a Octubre del 2013. RESULTADOS: Entre las características sociodemográficas que predominaron fueron: mujer en edad reproductiva de 19-35 años (79,6 por ciento). estado civil conviviente (53,1 por ciento) y ocupación ama de casa (71,4 por ciento). Entre las principales características clínicas encontradas, la mayoría tuvo al menos sobrepeso (57,1 por ciento), fueron gestantes con embarazos a término (89,8 por ciento), en su mayoría primíparas (36,7 por ciento) y con antecedente de cesárea previa (40,8 por ciento). A la evaluación de las funciones vitales previo al bloqueo raquídeo se encontró en el 100 por ciento de casos valores normales de Saturación de oxígeno y frecuencia cardíaca, a excepción de la frecuencia respiratoria que se solo encontró normal en el 98,0 por ciento de casos y la presión arterial en un 95,9 por ciento, cuya diferencia (4,1 por ciento) tenia hipertensión; administrándose de manera paralela una dosis precarga única de 5 cc de etilefrina a 85,7 por ciento de gestantes y 1000 ml de cristaloides al 69,4 por ciento. Las cuales según monitoreo de funciones vitales, se registró una incidencia de hipotensión en 22,4 por ciento de gestantes, requiriendo de 1 a más dosis adicionales de etilefrina (14,2 por ciento) y cristaloides (30,6 por ciento) durante el procedimiento quirúrgico. Para reducirse a un 2,0 por ciento de casos de hipotensión al término de la cesárea. Finalmente, el volumen efectivo medio estimado de cristaloides administrados fue de 14,03 ml/kg...


OBJECTIVE: To determine if the use of etilefrine and intravenous f1uids prevents the hypotension secondary to spinal anesthesia, in patients who undergo to caesarean section in the INMP during the period 2013. METHODOLOGY: Was an observational, descriptive, transversal, prospective study. This study done in a total of approximately 320 patients, who were undergoing cesarean section with spinal block technique meeting the inclusion and exclusion standard in the period September to October 2013. RESULTS: Among the sociodemographic characteristics were predominant: Women in reproductive age 19-35 years (79.6 per cent), marital status: cohabiting (53.1 per cent) and occupation housewife (71.4 per cent). The main clinical features found, most had overweight (57.1 per cent) were pregnant women with term pregnancies (89.8 per cent), primiparous (36.7 per cent) with a history of previous cesarean (40.8 per cent). To the evaluation of vital functions previous to spinal block was found in 100 per cent of the cases had normal oxygen saturation and heart rate, except for respiratory rate is only found normal in 98.0 per cent of cases and arterial pressure by 95.9 per cent, the difference (4.1 per cent) had hypertension parallel administered a single dose of 5 cc preload etilefrine to 85.7 per cent of pregnant women and 1000 mi of crystalloid in the 69.4 per cent. Which as monitoring of vital functions, an incidence of hypotension in 22.4 per cent of pregnant women registered, requiring 1 to further doses of etilefrine (14.2 per cent) and crystalloid (30.6 per cent) during the surgical procedure. To be reduced to 2.0 per cent of cases of hypotension at the end of caesarean. Finally, the volume estimated average effective administered of crystalloid was 14.03 ml/kg. CONCLUSIONS: The administration of etilefrine begore subarachnoid block, previous the caesarean reduce the hypotension, evidence of this is the 22.4 per cent of cases of pregnant women with at least 1 episode...


Assuntos
Feminino , Humanos , Gravidez , Adolescente , Adulto Jovem , Adulto , Cesárea , Etilefrina/uso terapêutico , Hipotensão , Infusões Intravenosas , Raquianestesia , Estudos Observacionais como Assunto , Estudos Prospectivos , Estudos Transversais
20.
Lima; s.n; 2013. 36 p. tab, graf.
Tese em Espanhol | LILACS, LIPECS | ID: biblio-1113157

RESUMO

Introducción: El presente estudio analizó casos de gestantes sometidas a bloqueo subaracnoideo (BSA) para cesárea y que necesitaron el uso de etilefrina para la corrección de la hipotensión arterial materna. Métodos: Se incluyeron a las gestantes sometidas a cesárea bajo BSA en el periodo enero a marzo del 2013, en el Hospital Almenara de Lima Perú, se excluyeron a los neonatos inmaduros, con RCIU, hijos de madres diabéticas, con enfermedad hemolítica RH, con asfixia, sepsis, policitemia y/o hipotermia neonatal, y se compararon las glicemias de la primera y segunda hora de vida de los neonatos, agrupados según el factor de exposición (administración de etilefrina a sus madres durante la cesárea), mediante la prueba estadística del t de student y en tablas de contingencia se calculó el riesgo relativo para la exposición. Resultados: La edad promedio para ambos grupos de pacientes es 30 años, la talla promedio del grupo expuesto es 1.55m y del grupo no expuesto es 1.57m, la mediana para el peso del grupo expuesto es 69 Kg y del grupo no expuesto es 72 Kg, la mediana para la edad gestacional del grupo expuesto es 38 semanas y del grupo no expuesto es 39 semanas. El promedio del peso de los neonatos del grupo expuesto es 3318 g y del grupo no expuesto es 3444 g. El promedio de la glicemia en la primera hora de vida de los neonatos del grupo expuesto es 57 mg/dl y del grupo no expuesto es 56 mg/dl; el promedio de la glicemia en la segunda hora de vida de los neonatos del grupo expuesto es 63 mg/dl y del grupo no expuesto es 65 mg/dl. La prueba de t de student para el promedio de las glicemias a la primera y segunda hora de vida de los neonatos, no mostró diferencias significativas entre ambos grupos, pero en las tablas de contingencia se calculó un riesgo relativo para el factor de exposición de 2.68 (IC 95 por ciento 0.68 a 10.47), es decir la exposición es un factor de riesgo pero sin asociación causal. Conclusiones: Existe mayor riesgo de hipoglicemia neonatal...


Background: The present study analyzed cases of pregnant women undergoing subarachnoid block (BSA) for cesarean section and requiring the use of ethylephrine to correct maternal hypotension. Methods: We included pregnant women undergoing cesarean section under BSA in the period January to March 2013, at the Hospital Almenara in Lima Peru, were excluded immature newborns with IUGR, newborns of diabetic mothers with RH hemolytic disease, with asphyxia, sepsis, polycythemia and/or neonatal hypothermia and compared the glucose levels of the first and second hour of life for newborns, grouped according to the exposure factor (ethylephrine administration to their mothers during caesarean section), using the statistical test Student's t contingency tables and calculated the relative risk for exposure. Results: The average age for both groups of patients is 30 years, the average size of the exposed group is 1.55m the unexposed group is 1.57m, the median weight is 69 kg exposed group and the unexposed group is 72 kg, the median gestational age of 38 weeks is exposed group and the unexposed group is 39 weeks. The average weight of the newborns in the exposed group is 3318 g and the unexposed group is 3444 g. The mean blood glucose in the first hour of life of newborns exposed group is 57 mg/dI and the unexposed group is 56 mg/dI, the mean blood glucose during the second hour of life of newborns in the exposed group is 63 mg/dI. and the unexposed group is 65 mg/dI. The Student t test for average blood glucose for the first and second hour of life of newborns showed no significant differences between both groups, but in the contingency tables was calculated relative risk for the exposure factor of 2.68 (95 per cent Cl 0.68 to 10.47), the exposure is a risk factor but no causal association. Conclusions: There is increased risk of neonatal hypoglycemia associated with the use of ethylephrine to correct maternal hypotension during caesarean section under BSA.


Assuntos
Feminino , Humanos , Gravidez , Adulto , Bloqueio Neuromuscular , Cesárea , Etilefrina/administração & dosagem , Hipoglicemia/prevenção & controle , Hipotensão Controlada , Estudo Observacional , Estudos Prospectivos , Estudos Transversais
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