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1.
Medicine (Baltimore) ; 98(51): e18311, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31860981

RESUMO

BACKGROUND: Studies have shown the efficacy of norepinephrine in the treatment of maternal hypotension during cesarean section by comparing it to treatment with phenylephrine. However, few studies have compared the efficacy of norepinephrine to ephedrine. METHODS: Ninety-seven women undergoing elective cesarean section were administered norepinephrine at 4 µg/minute (group N; n = 48) or ephedrine at 4 mg/minute (group E; n = 49) immediately postspinal anesthesia, with an on-off titration to maintain systolic blood pressure (SBP) at 80% to 120% of baseline. A rescue bolus of 8 µg norepinephrine was given whenever SBP reached the predefined lower limit. Our primary outcome was the incidence of tachycardia. Secondary outcomes included the incidence of bradycardia, hypertension, hypotension, severe hypotension, hypotensive episodes, number of rescue top-ups, hemodynamic performance error including median performance error (MDPE), and median absolute performance error (MDAPE). Neonatal Apgar scores and umbilical arterial (UA) blood gas data were also collected. RESULTS: Women in group N experienced fewer cases of tachycardia (4.2% vs 30.6%, P = .002, odds ratio: 0.11 [95% confidence interval, CI: 0.02-0.47]), a lower standardized heart rate (HR) (70.3 ±â€Š11 vs 75 ±â€Š11, P = .04, difference: 4.7 ±â€Š2.2 [95% CI: 0.24-9.1]), and a lower MDPE for HR (1.3 ±â€Š9.6 vs 8.4 ±â€Š13.5 bpm, P = .003, difference: 3.1 ±â€Š1.8 [95% CI: -0.6-6.7]). In addition, the lowest or the highest HR was lower in group N compared to group E (both P < .05). Meanwhile, the standardized SBP in group N was lower than that in group E (P = .04). For neonates, the UA blood gas showed a higher base excess (BE) and a lower lactate level in group N compared to E (both P < .001). Other hemodynamic variables, maternal, and neonatal outcomes were similar. CONCLUSION: Infusion of 4 µg/minute norepinephrine presented fewer cases of tachycardia, less fluctuation and a lower HR compared to baseline values, as well as a less stressed fetal status compared to ephedrine infusion at 4 mg/minute. In addition, norepinephrine infusion presented a lower standardized SBP compared to ephedrine.


Assuntos
Raquianestesia/métodos , Cesárea/efeitos adversos , Efedrina/uso terapêutico , Hipotensão/prevenção & controle , Norepinefrina/uso terapêutico , Adulto , Raquianestesia/efeitos adversos , Pressão Sanguínea/efeitos dos fármacos , Cesárea/métodos , Método Duplo-Cego , Efedrina/efeitos adversos , Feminino , Frequência Cardíaca/efeitos dos fármacos , Humanos , Hipotensão/etiologia , Infusões Intravenosas , Norepinefrina/administração & dosagem , Gravidez
2.
Am J Case Rep ; 20: 1104-1107, 2019 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-31346152

RESUMO

BACKGROUND Denervation supersensitivity to sympathomimetic drugs has been noted in patients with Parkinson's disease (PD) whose cardiac sympathetic nerves are denervated. This phenomenon is not as well recognized as other complications of PD patients, but anesthesiologists should be aware of it because sympathomimetic drugs can sometimes be dangerous to these patients. CASE REPORT A 60-year-old woman was scheduled for total hip joint replacement under combined spinal-epidural anesthesia and sedation. She had been diagnosed as PD (stage 4 on the Hoehn and Yahr scale) with a history of orthostatic hypotension. Her ¹²³I-metaiodobenzylguanidine (MIBG) scintigraphy revealed marked reduction of ¹²³I-MIBG accumulation in the heart. In the operating room, we placed an epidural catheter through the Th12-L1 space, and spinal anesthesia (2.6 mL of 0.5% normobaric bupivacaine) was administered. During the surgery, we infused propofol at 100 mg·hr⁻¹ for sedation. When 4 mg of ephedrine was administered intravenously because of marked decrease in patient's blood pressure, we observed unexpectedly large increases in the systolic blood pressure, from 78 mmHg to 168 mmHg, and the heart rate increased from 52 to 84 beats per minute (bpm). This phenomenon recurred each time 4 mg of ephedrine was administered. CONCLUSIONS We report a case in which ephedrine induced unexpectedly large increases in blood pressure and heart rate in a patient who suffered from PD with severe cardiac sympathetic nerve denervation. We speculate that this phenomenon was caused by denervation supersensitivity of the patient's heart.


Assuntos
Efedrina/efeitos adversos , Frequência Cardíaca/efeitos dos fármacos , Hipertensão/induzido quimicamente , Doença de Parkinson/complicações , Simpatomiméticos/efeitos adversos , Raquianestesia , Efedrina/administração & dosagem , Feminino , Coração/inervação , Humanos , Pessoa de Meia-Idade , Simpatomiméticos/administração & dosagem
3.
A A Pract ; 12(11): 385-387, 2019 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-31162162

RESUMO

Acute angle-closure glaucoma is a rare complication of general anesthesia. If not treated in time, acute angle-closure glaucoma can potentially cause permanent loss of vision. Physicians should therefore be vigilant for the possibility of acute angle-closure glaucoma in patients who experience postoperative change or loss of vision. Recently, some reported a case of bilateral acute angle-closure glaucoma after general anesthesia, in which the use of ephedrine was a possible trigger. This report begins by examining a case of unilateral acute angle-closure glaucoma. The potential triggers of this complication are discussed. This article concludes with a flowchart to aid anesthesiologists to accurately diagnose postoperative ophthalmic pathology.


Assuntos
Efedrina/efeitos adversos , Glaucoma de Ângulo Fechado/induzido quimicamente , Complicações Pós-Operatórias/induzido quimicamente , Adulto , Anestesia Geral/efeitos adversos , Feminino , Humanos , Histerectomia Vaginal , Prolapso Uterino/cirurgia
4.
Am J Emerg Med ; 37(3): 494-498, 2019 03.
Artigo em Inglês | MEDLINE | ID: mdl-30553634

RESUMO

PURPOSE: Evaluate push dose vasopressor (PDP) practice patterns, efficacy, and safety in critically ill patients. METHODS: Critically ill patients receiving phenylephrine or ephedrine PDP from November 2015-March 2017 were included. Patient demographics, medication administration details, vital signs pre- and post-administration, adverse effects, and medications errors were collected. Descriptive data are presented and comparisons were made with paired samples t-test, Wilcoxon Rank Sum and Chi-squared analysis or Fisher's Exact Test as appropriate. RESULTS: A total of 146 patients (155 PDP events) were included; mean age 64.5 ±â€¯13.3 years and 66.4% males, respiratory failure (39.8%) or sepsis (24.9%) admission diagnosis. The surgical intensive care unit (ICU) (44.5%) and medical ICU (33.6%) used PDPs most often, and during the peri-intubation period (57.3%) or for other transient hypotension (38.2%). Following PDP, mean systolic blood pressure (BP), diastolic BP, and heart rate (HR) increased 32.5% (80 to 106 mmHg), 27.2% (48 to 61 mmHg), and 6.4% (93 to 99 bpm), respectively. There were 17 (11.6%) adverse events; most often related to excessive increases in BP or HR and one incidence of dysrhythmia. Thirteen patients (11.2%) had a dose related medication error (phenylephrine dose >200 µg or ephedrine dose >25 mg), nine (6.2%) received PDP with normal/elevated hemodynamics (systolic BP > 100 mmHg or HR > 160 bpm) and 15% while on a continuous infusion vasopressor. CONCLUSION: PDPs were used in a variety of patient diagnoses and for select indications. Overall, they were efficacious but associated with adverse drug events and medication errors.


Assuntos
Cuidados Críticos/métodos , Hipotensão/tratamento farmacológico , Vasoconstritores/administração & dosagem , Idoso , Arritmias Cardíacas/induzido quimicamente , Pressão Sanguínea/efeitos dos fármacos , Esquema de Medicação , Efedrina/efeitos adversos , Efedrina/uso terapêutico , Feminino , Frequência Cardíaca/efeitos dos fármacos , Humanos , Hipotensão/etiologia , Masculino , Erros de Medicação , Pessoa de Meia-Idade , Fenilefrina/efeitos adversos , Fenilefrina/uso terapêutico , Estudos Retrospectivos , Vasoconstritores/efeitos adversos
5.
Int J Surg ; 60: 48-59, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30389535

RESUMO

BACKGROUND: In the past 20 years, many studies compared phenylephrine with ephedrine to prevent or treat hypotension in elective or emergency cesarean delivery and parturients with pre-eclampsia. A meta-analysis of the abovementioned trials is needed. METHODS: Several databases (PubMed, Embase, Web of Science and Cochrane Library) were searched from inception to April 2018 for trials comparing phenylephrine with ephedrine in cesarean delivery. The primary outcome is the incidence of maternal hypotension. RESULTS: Thirty-six trials (2439 patients) with elective cesarean delivery, three trials (400 patients) with emergency cesarean delivery and three trials (192 patients) with parturients with pre-eclampsia were included and analyzed. The incidence of hypotension did not differ in the elective surgery group (relative risk 0.83, 95% CI 0.66 to 1.05), emergency surgery group (relative risk 1.02, 95% CI 0.87 to 1.19) and pre-eclamptic parturients group (relative risk 0.93, 95% CI 0.63 to 1.37). The phenylephrine group had a higher incidence of bradycardia and lower incidences of tachycardia and nausea or vomiting in all three patient groups. The phenylephrine group also had lower fetal acidosis rate, higher umbilical artery and vein pH values and less base excess in the elective surgery. The abovementioned outcomes were similar in the emergency surgery group and the pre-eclampsia group. Publication bias for hypotension was detected. However, the trim and fill method demonstrated that the publication bias had little impact on hypotension. Trial sequential analysis of hypotension in elective surgery showed that this meta-analysis lacked a sufficient cumulative sample size and that further studies should be included. CONCLUSION: Phenylephrine and ephedrine were both effective in maintaining hemodynamic balance. Newborns benefited more from phenylephrine in elective cesarean delivery, but not in emergency cesarean delivery or in parturients with pre-eclampsia. More trials should be included to achieve more conclusive results.


Assuntos
Raquianestesia/efeitos adversos , Cesárea/efeitos adversos , Efedrina/uso terapêutico , Hipotensão/epidemiologia , Fenilefrina/uso terapêutico , Vasoconstritores/uso terapêutico , Adulto , Efedrina/efeitos adversos , Feminino , Humanos , Hipotensão/etiologia , Hipotensão/prevenção & controle , Incidência , Recém-Nascido , Fenilefrina/efeitos adversos , Gravidez , Vasoconstritores/efeitos adversos
6.
Artigo em Chinês | MEDLINE | ID: mdl-29902847

RESUMO

Objective: To observe the process of nasal mucosa injury and repair induced by nasal decongestants in guinea pigs Methods: Sixty-five male guinea pigs were randomly divided into 4groups by digital random method.The guinea pigs in Group A (20 guinea pigs)were treated with 2 sprays of 0.1% Naphazoline 6 times a day for 2 weeks; Group B (20 guinea pigs)with 2 drops of 1% Ephedrine 6 times a day for 2 weeks; Group C(20 guinea pigs) with 2 sprays of Naphazolin hydrochloride and Chlorphenamine Maleate Nasal Spray 8 times a day for 2 weeks.Group D (5guinea pigs)did not do any intervention as a control group.At the end of first and second weekend, 6 guinea pigs randomly selected from each group were observed the morphological changes of the nasal cavity with nasal endoscope and pathological microscope.Two weeks after stopping use of decongestant, 24 animals were grouped.Three guinea pigs were selected randomly from each group to form Group E (n=9) and Group F (n=9)respectively. The 6 remaining guinea pigs falled into Group G. Group E received 2 sprays of Mometasone Furoate Nasal Spray once a day for 2 weeks; Group F received 1 ml 2.3% saline to wash the nasal cavities once a day for 2 weeks.Group F was used to show the natural progess without any treatment.At the end of the third and fourth weekend, nasal endoscopic and pathological microscopes were used to observe the nasal cavity structure and the pathological changes of nasal mucosa. Results: Nasal mocusa congestion and edema were observed with nasal endoscopy after 2 weeks of using nasal decongestant. Cell edema, blood vessel expansion, acute and chronic inflammatory cell infiltration, cilium lodging or loss were observed under the pathological microscope in GroupA, B, C. After using MometasoneFuroate Nasal Spray and 2.3% saline for 2 weeks, the above changes were all recovered in Group E and F. No recovery was found in Group G. Conclusions: Short-term and over dose of nasal decongestant can result in the injury of nasal mucosa in guinea pigs, and the injury is much severe as using decongestant last longer.MometasoneFuroate nasal spray and 2.3% saline can repair the injury.


Assuntos
Descongestionantes Nasais/efeitos adversos , Mucosa Nasal/efeitos dos fármacos , Animais , Clorfeniramina/efeitos adversos , Efedrina/efeitos adversos , Cobaias , Masculino , Furoato de Mometasona/uso terapêutico , Nafazolina/efeitos adversos , Mucosa Nasal/lesões , Distribuição Aleatória , Suínos
8.
Rev. esp. enferm. dig ; 110(4): 254-256, abr. 2018. ilus
Artigo em Espanhol | IBECS | ID: ibc-174602

RESUMO

This article is the first description of a spontaneous hepatic rupture in a young bodybuilder with a history of clenbuterol and ephedrine alkaloid use. The patient presented with a sudden mid-epigastric pain and vomiting. Hemoglobin levels decreased a few hours later and a computed tomography scan was performed which revealed a rupture of the right liver capsule and hemoperitoneum. Two attempts at transarterial embolization did not control the bleeding and a right hemihepatectomy was performed. The pathological report identified a hepatic adenoma, a capsular tear and diffuse peliosis hepatis. The patient was discharged in a good condition after eleven days. Spontaneous hepatic ruptures are rare and life-threatening and are usually described in association with tumors, connective tissue diseases and gestosis. This article is a review of the available literature with regard to this condition, with a focus on its relation to peliosis hepatis and banned substance used by body image fanatics. The present case highlights the challenging diagnosis of this potentially fatal liver complication in a healthy appearing male, the risk associated with the online trade of performance enhancing drugs and its relation with peliosis hepatis


No disponible


Assuntos
Humanos , Masculino , Adulto , Fígado/lesões , Peliose Hepática/induzido quimicamente , Ruptura/etiologia , Substâncias para Melhoria do Desempenho/efeitos adversos , Agonistas Adrenérgicos beta/efeitos adversos , Estimulantes do Sistema Nervoso Central/efeitos adversos , Clembuterol/efeitos adversos , Efedrina/efeitos adversos , Fígado/cirurgia , Peliose Hepática/complicações , Ruptura/cirurgia , Resultado do Tratamento
9.
Anesth Prog ; 65(1): 44-49, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29509526

RESUMO

Variant angina is caused by coronary artery spasm (CAS) with ST-segment elevation. We herein report a case of recurrent CAS during 2 operations in the same patient. An 80-year-old woman was scheduled to undergo tracheostomy, submandibular dissection, left partial maxillectomy, and coronoidectomy. We administered ephedrine and phenylephrine to manage hypotension during general anesthesia. Immediately after the administration of these drugs, the ST segment elevated. We decided to cease the operation and transport the patient to the department of cardiology. Computed tomography angiography revealed pneumomediastinum. The cardiologists considered that the electrocardiography findings had changed secondary to pneumomediastinum. About 6 weeks later, a second operation was scheduled. We administered ephedrine and phenylephrine to manage hypotension during general anesthesia. Immediately after the administration of these drugs, ST-segment elevation occurred. We discontinued use of these drugs, and the ST-segment elevation did not recur. We considered that the cause of the ST-segment elevation was vasopressor-induced CAS because the vasopressors were administered immediately before the occurrence of CAS. Vasopressors such as ephedrine or phenylephrine are frequently used to manage hypotension during general anesthesia. Therefore, anesthesiologists should consider the occurrence of CAS before using vasopressors and know how to manage CAS well.


Assuntos
Anestesia Geral/métodos , Angina Pectoris Variante/etiologia , Vasoespasmo Coronário/induzido quimicamente , Vasoconstritores/efeitos adversos , Idoso de 80 Anos ou mais , Angiografia por Tomografia Computadorizada/métodos , Efedrina/administração & dosagem , Efedrina/efeitos adversos , Feminino , Humanos , Hipotensão/tratamento farmacológico , Fenilefrina/administração & dosagem , Fenilefrina/efeitos adversos , Recidiva , Vasoconstritores/administração & dosagem
11.
Apunts, Med. esport (Internet) ; 53(197): 11-18, ene.-mar. 2018. tab, graf
Artigo em Inglês | IBECS | ID: ibc-171426

RESUMO

The presence of adverse results in doping controls is always bad news for the sport, as it reflects the moral and ethical absence of a clean competition. Its prevalence and evolution is important to know and have criteria on the relevance of this event. Method: The results of doping controls from 2003 to 2015 at the global level, offered by the World Anti-Doping Agency on its website, have been revised. Results: The presence of adverse results of the year 2015 as last reference, reached 0.83% in Olympic sports and 2.04% in the non-Olympic ones. It remains a similar level during the last 7 years, tending to decline in the Olympics and increase in the non-Olympics. The groups of predominant substances are, in order, anabolic steroids 50.3%, stimulants 15.4% and maskers 12.5%, being the rest diverse and variable. It should be noted that many treatments with therapeutic authorisation, i.e., beta agonists (3-4%), glucocorticosteroids (6-8%) or central nervous system (3-5%), are shown as adverse results, but are therefore not doping positive and in their case punishable. Similarly, the high number of anabolic positives is the result of fraud, but also the presence of repeated samples in the follow-up study of some athletes. Conclusion: The data serve as a reference to have a more accurate criterion in reference to this field of sport (AU)


La presencia de resultados adversos en los controles de dopaje son siempre una noticia nefasta para el deporte, pues refleja la ausencia moral y ética de una competición limpia. Su prevalencia y evolución es importante para conocer y disponer de criterio sobre la relevancia de este suceso. Método: Se han revisado los resultados de los controles de dopaje del 2003 al 2015 a nivel mundial, ofrecidos por la Agencia Mundial Antidopaje en su web. Se ofrecen, además, los resultados por deportes del 2015. Resultados: La presencia de resultados adversos, tomando de referencia ese año, alcanza un 0,83% de las muestras estudiadas en los deportes olímpicos y un 2,04% en los no olímpicos. Se mantiene un nivel similar en los últimos 7 años, tendiendo a disminuir en los deportes olímpicos y aumentar en los no olímpicos. Los grupos de sustancias predominantes son, por orden, anabolizantes (50,3%), estimulantes (15,4%) y enmascarantes (12,5%), siendo el resto diverso y variable. En el total de resultados debe tenerse en cuenta que muchos tratamientos con autorización terapéutica, por ejemplo para beta-agonistas (3-4%), glucocorticoides (6-8%) o del sistema nervioso central (3-5%), se muestran como resultados adversos, pero no son por tanto dopaje positivo ni en su caso sancionables. De igual manera, el elevado número de positivos en anabolizantes son fruto del fraude pero también de la presencia de muestras repetidas en los seguimientos de estudio de algunos deportistas. Conclusión: Los datos sirven de referencia para disponer de un criterio más certero en referencia a este ámbito del deporte (AU)


Assuntos
Humanos , Masculino , Feminino , Doping nos Esportes/métodos , Anabolizantes/análise , Esportes/normas , Estudos Longitudinais , Testosterona/análise , Pseudoefedrina/efeitos adversos , Efedrina/efeitos adversos , Cocaína/efeitos adversos , Cafeína/efeitos adversos , 3,4-Metilenodioxianfetamina/efeitos adversos
12.
Biol Pharm Bull ; 41(2): 247-253, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29386484

RESUMO

Ephedrine alkaloids-free Ephedra Herb extract (EFE) has been developed to eliminate the adverse effects caused by ephedrine alkaloid-induced sympathetic hyperactivation. Previously, we reported that EFE possesses analgesic, anti-influenza, and cancer metastatic inhibitory effects at comparable levels to that of Ephedra Herb extract (EHE). However, it has not yet been demonstrated that EFE is free from the known side effects of EHE, such as excitation, insomnia, and arrhythmias. In this study, the incidence of these adverse effects was compared between mice administered EHE and those administered EFE. Increased locomotor activity in an open-field test, reduced immobility times in a forced swim test, and reduced sleep times in a pentobarbital-induced sleep test were observed in EHE-treated mice, when compared to the corresponding values in vehicle-treated mice. In contrast, EFE had no obvious effects in these tests. In electrocardiograms, atrial fibrillation (i.e., irregular heart rhythm, absence of P waves, and appearance of f waves) was observed in the EHE-treated mice. It was suggested that this atrial fibrillation was induced by stimulation of adrenaline ß1 receptors, but not by hypokalemia. However, EFE did not affect cardiac electrophysiology. These results suggest that the abovementioned side effects are caused by ephedrine alkaloids in EHE, and that EFE is free from these adverse effects, such as excitation, insomnia, and arrhythmias. Thus, EFE is a promising new botanical drug with few adverse effects.


Assuntos
Ansiedade/prevenção & controle , Arritmias Cardíacas/prevenção & controle , Suplementos Nutricionais/efeitos adversos , Ephedra/química , Efedrina/efeitos adversos , Extratos Vegetais/efeitos adversos , Distúrbios do Início e da Manutenção do Sono/prevenção & controle , Alcaloides/análise , Alcaloides/toxicidade , Analgésicos não Entorpecentes/administração & dosagem , Analgésicos não Entorpecentes/efeitos adversos , Analgésicos não Entorpecentes/química , Animais , Animais não Endogâmicos , Ansiedade/sangue , Ansiedade/induzido quimicamente , Ansiedade/etiologia , Arritmias Cardíacas/sangue , Arritmias Cardíacas/induzido quimicamente , Arritmias Cardíacas/etiologia , Comportamento Animal , Cafeína/envenenamento , Estimulantes do Sistema Nervoso Central/envenenamento , Suplementos Nutricionais/análise , Efedrina/administração & dosagem , Efedrina/química , Contaminação de Alimentos , Hipnóticos e Sedativos/farmacologia , Japão , Masculino , Camundongos , Pentobarbital/farmacologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Caules de Planta/química , Potássio/sangue , Distúrbios do Início e da Manutenção do Sono/sangue , Distúrbios do Início e da Manutenção do Sono/induzido quimicamente , Distúrbios do Início e da Manutenção do Sono/etiologia
13.
Rev Esp Enferm Dig ; 110(4): 254-256, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29313696

RESUMO

This article is the first description of a spontaneous hepatic rupture in a young bodybuilder with a history of clenbuterol and ephedrine alkaloid use. The patient presented with a sudden mid-epigastric pain and vomiting. Hemoglobin levels decreased a few hours later and a computed tomography scan was performed which revealed a rupture of the right liver capsule and hemoperitoneum. Two attempts at transarterial embolization did not control the bleeding and a right hemihepatectomy was performed. The pathological report identified a hepatic adenoma, a capsular tear and diffuse peliosis hepatis. The patient was discharged in a good condition after eleven days. Spontaneous hepatic ruptures are rare and life-threatening and are usually described in association with tumors, connective tissue diseases and gestosis. This article is a review of the available literature with regard to this condition, with a focus on its relation to peliosis hepatis and banned substance used by body image fanatics. The present case highlights the challenging diagnosis of this potentially fatal liver complication in a healthy appearing male, the risk associated with the online trade of performance enhancing drugs and its relation with peliosis hepatis.


Assuntos
Fígado/lesões , Substâncias para Melhoria do Desempenho/efeitos adversos , Ruptura/etiologia , Levantamento de Peso/lesões , Agonistas Adrenérgicos beta/efeitos adversos , Adulto , Estimulantes do Sistema Nervoso Central/efeitos adversos , Clembuterol/efeitos adversos , Efedrina/efeitos adversos , Humanos , Fígado/cirurgia , Masculino , Peliose Hepática/induzido quimicamente , Peliose Hepática/complicações , Ruptura/cirurgia , Resultado do Tratamento
14.
Biomed Res Int ; 2017: 1931204, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29181387

RESUMO

Background: Drug addiction is classified as a chronic relapse nature brain disease with complicated neurobiology mechanisms. There are an increasing number of researchers that are investigating the possible mechanisms for solving the thorny problem. Methods: The model of chronic addiction of rhesus monkey ephedrine was established, where changes in body weight and behavior were monitored. The expression of cAMP response element binding protein (CREB) in the hippocampus of rhesus monkeys was identified by real-time PCR and Western blot. Results: We were successful in establishing the chronic ephedrine addiction model in the rhesus macaques. They exhibited changes in body weight and behavior. Immunofluorescence showed that CREB was expressed in the nucleus of the hippocampus, and the expression of CREB mRNA and protein in the hippocampus were increased by real-time PCR and Western blot. The CREB positive expression in the hippocampus of the modeling group was significantly higher than in the control group. Conclusions: The changes of body weight and behavior of the rhesus monkeys after ephedrine chronic addiction were significant. The changes of CREB in the hippocampus of rhesus macaques with ephedrine chronic addiction are important molecular mechanisms, and the upregulation of CREB may be involved in the physiological pathology and behavior process in individuals with chronic ephedrine addiction.


Assuntos
Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/biossíntese , Efedrina/efeitos adversos , Regulação da Expressão Gênica/efeitos dos fármacos , Hipocampo/metabolismo , Transtornos Relacionados ao Uso de Substâncias/metabolismo , Animais , Doença Crônica , Modelos Animais de Doenças , Efedrina/farmacologia , Hipocampo/patologia , Macaca mulatta , Transtornos Relacionados ao Uso de Substâncias/patologia
15.
Yakugaku Zasshi ; 137(2): 173-177, 2017.
Artigo em Japonês | MEDLINE | ID: mdl-28154328

RESUMO

Ephedra Herb is a crude drug for the treatment of headache, bronchial asthma, nasal inflammation, and the common cold. Although it has been considered that ephedrine alkaloids (EAs) are the principal active ingredients of Ephedra Herb, EAs are known to induce palpitations, hypertension, insomnia, and dysuria as major side effects. Therefore, the administration of EAs-containing drugs to patients with cardiovascular-related diseases is strongly contraindicated. Previously, we isolated herbacetin 7-O-neohesperidoside from Ephedra Herb. In addition, we found that herbacetin, a flavonoid aglycone in Ephedra Herb, had antiproliferative and analgesic effects. Therefore, the prospect of preparing safer natural medicines without the adverse effects associated with EAs was appealing. In this symposium review, to achieve the aim of producting a clinically useful Ephedra Herb extract with none of the adverse effects associated with EAs, I present an efficient preparation method of EAs-free Ephedra Herb extract, together with its chemical composition, antiproliferative effects, and a putative marker for quality control.


Assuntos
Analgésicos , Antineoplásicos Fitogênicos , Ephedra/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Extratos Vegetais/análise , Tecnologia Farmacêutica/métodos , Alcaloides/efeitos adversos , Doenças Cardiovasculares , Contraindicações , Efedrina/efeitos adversos
16.
Yakugaku Zasshi ; 137(2): 179-186, 2017.
Artigo em Japonês | MEDLINE | ID: mdl-28154329

RESUMO

Ephedra Herb is defined in the 17th edition of the Japanese Pharmacopoeia as the terrestrial stem of Ephedra sinica STAPF., Ephedra intermedia SCHRENK et C.A. MEYER, or Ephedra equisetina BUNGE (Ephedraceae) which contains more than 0.7% ephedrine alkaloids (ephedrine and pseudoephedrine). The primary effects and adverse effects of Ephedra Herb are traditionally believed to be mediated by ephedrine alkaloids. We recently reported that Ephedra Herb extract (EHE) exhibits antimetastatic and antitumor effects by suppressing the hepatocyte growth factor-c-Met signaling pathway through the inhibition of c-Met tyrosine kinase activity. We confirmed that the non-alkaloidal fraction of EHE had c-Met-inhibitory activity. Moreover, we discovered herbacetin glycosides in EHE and demonstrated that herbacetin, the aglycone of the glycosides, shows c-Met-inhibitory activity and analgesic action. These findings suggest that some pharmacological actions of EHE may be produced by its non-alkaloidal fraction, which does not cause the adverse effects of ephedrine alkaloids. Therefore, we prepared ephedrine alkaloids-free EHE (EFE) by removing ephedrine alkaloids from EHE using ion-exchange column chromatography. EFE had c-Met-inhibitory action, analgesic effects, and antiinfluenza activity similar to EHE but had no toxicity. Now, we are evaluating the safety of EFE in healthy volunteers and its efficacy in patients to obtain licensing approval for its therapeutic use in the future.


Assuntos
Ephedra/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Alcaloides/efeitos adversos , Alcaloides/isolamento & purificação , Analgésicos , Animais , Antineoplásicos Fitogênicos , Antivirais , Cromatografia por Troca Iônica , Efedrina/efeitos adversos , Efedrina/isolamento & purificação , Feminino , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Masculino , Camundongos , Extratos Vegetais/análise , Extratos Vegetais/toxicidade , Receptores Proteína Tirosina Quinases/antagonistas & inibidores , Tecnologia Farmacêutica/métodos , Células Tumorais Cultivadas
17.
Yakugaku Zasshi ; 137(2): 187-194, 2017.
Artigo em Japonês | MEDLINE | ID: mdl-28154330

RESUMO

Ephedra Herb is classified "pungent, slightly bitter, and warm" in tastes and natures, and is used to provide warmth to the body, dispel coldness, remove dampness, and reduce pain. Similar herbs are "pungent and hot" chili peppers, "pungent and hot" evodia fruit," "pungent and warm" ginger, "pungent and hot" processed ginger, "pungent and hot" Zanthoxylum fruit, etc. These herbs are prescribed to provide heat to the outer or inner body. Some pungent components such as capsaicin, evodiamine, gingerol, and shogaol are known to be activators of transient receptor potential vanilloid 1 (TRPV1). TRPV1, a pain receptor, is activated in response to irritant chemicals such as capsaicin and high heat (>43℃) and strongly acidic conditions (pH<6). The typical TRPV1 activator capsaicin has various effects such as improvement of peripheral circulation, enhancement of thermogenesis, and pain relief. These effects are commonly observed for the "pungent and hot/warm" herbs, suggesting that TRPV1 stimulation plays an important part in their pharmacological action. In this study, we demonstrated that Ephedra Herb extract (EHE) shows strong TRPV1 activation, although ephedrine didn't show such effects. Both EHE and ephedrine alkaloids-free EHE (EFE) expressed similar analgesic action following oral administration, suggesting the presence of active components other than ephedrine alkaloids. Furthermore, EFE did not show side effects such as loss of sleep and irregular heartbeat in mice. Caution needs to be exercised while prescribing Ephedra Herb because it contains ephedrine. The application of EFE in Kampo medicine might be a better alternative in some cases.


Assuntos
Analgésicos , Ephedra/química , Extratos Vegetais/farmacologia , Administração Oral , Alcaloides/efeitos adversos , Animais , Capsaicina , Células Cultivadas , Efedrina/efeitos adversos , Humanos , Camundongos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/análise , Extratos Vegetais/uso terapêutico , Canais de Cátion TRPV/metabolismo
18.
Neuromuscul Disord ; 27(3): 259-265, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-28007405

RESUMO

We studied the effect and safety of ephedrine as add-on treatment for patients with myasthenia gravis with acetylcholine receptor antibodies (AChR MG), who do not sufficiently respond to standard treatment. Four patients with AChR MG were included in a placebo-controlled, double-blind, and randomised, multiple crossover series of n-of-1 trials. Each n-of-1 trial consisted of 3 cycles, in which two 5-day intervention periods were followed by 2 days washout. In each cycle, ephedrine 50 mg daily in 2 doses was compared with placebo in the alternate treatment period. Primary outcome was a change in QMG score. Add-on treatment with ephedrine compared with placebo improved QMG score by 1.0 point (95% confidence interval 0.21-1.79), which was significant for the group of trial patients as well as for the population treatment effect. Ephedrine also showed a significant trial average treatment effect for all secondary outcomes, improving MG Composite by 2.7, MG-ADL by 1.0 and VAS score for muscle strength by 1.1. Adverse events were mild and included palpitations, tremor and restlessness. Although all ECGs were normal, ephedrine prolonged the corrected QT interval. Ephedrine as add-on treatment for myasthenia gravis resulted in a small but consistent reduction of symptoms and weakness in patients with moderate disease severity.


Assuntos
Efedrina/farmacologia , Imunossupressores/uso terapêutico , Miastenia Gravis/tratamento farmacológico , Receptores Colinérgicos/imunologia , Simpatomiméticos/farmacologia , Adulto , Autoanticorpos/sangue , Estudos Cross-Over , Método Duplo-Cego , Quimioterapia Combinada , Efedrina/administração & dosagem , Efedrina/efeitos adversos , Feminino , Humanos , Imunossupressores/administração & dosagem , Pessoa de Meia-Idade , Miastenia Gravis/imunologia , Simpatomiméticos/administração & dosagem , Simpatomiméticos/efeitos adversos
19.
J Clin Anesth ; 35: 13-19, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27871510

RESUMO

OBJECTIVE: When dexmedetomidine is used in patients undergoing spinal anesthesia, high incidence of bradycardia in response to parasympathetic activation is reported. Therefore, we aimed to evaluate the effectiveness of atropine premedication for preventing the incidence of bradycardia and the hemodynamic effect on patients undergoing spinal anesthesia with sedation by dexmedetomidine. DESIGN: Randomized, double-blind, placebo-controlled study. SETTING: Operating room. PATIENTS: One hundred fourteen patients (age range, 2-65 years; American Society of Anesthesiology class I-II) participated in this study, willing to be sedated and to undergo spinal anesthesia. INTERVENTION: The patients were divided into 2 groups: group A and group C. After performing spinal anesthesia, dexmedetomidine was infused at a loading dose of 0.6 µg/kg for 10 minutes, followed by an infusion at 0.25 µg/(kg h). Simultaneously with the loading dose of dexmedetomidine, patients in group A received an intravenous bolus of 0.5 mg atropine, whereas patients in group C received an intravenous normal saline bolus. MEASUREMENT: Data on administration of atropine and ephedrine were collected. Hemodynamic data including heart rate, systolic blood pressure, diastolic blood pressure (DBP), and mean blood pressure (MBP) were also recorded. MAIN RESULTS: The incidence of bradycardia requiring atropine treatment was significantly higher in group C than group A (P=.035). However, the incidence of hypotension needing ephedrine treatment showed no significant difference between the 2 groups (P=.7). Systolic blood pressure and heart rate showed no significant differences between the 2 groups (P=.138 and .464, respectively). However, group A showed significant increases in DBP and MBP, and group C did not (P=.014 and .008, respectively). CONCLUSION: Prophylactic atropine reduces the incidence of bradycardia in patients undergoing spinal anesthesia with dexmedetomidine sedation. However, DBP and MBP showed significant increases in patients when prophylactic atropine was administrated. Therefore, atropine premedication should be administered cautiously.


Assuntos
Raquianestesia/efeitos adversos , Bradicardia/prevenção & controle , Antagonistas Colinérgicos/uso terapêutico , Dexmedetomidina/efeitos adversos , Hipnóticos e Sedativos/efeitos adversos , Antagonistas Muscarínicos/uso terapêutico , Parassimpatomiméticos/efeitos adversos , Pré-Medicação/métodos , Adolescente , Adulto , Idoso , Raquianestesia/métodos , Atropina/administração & dosagem , Atropina/uso terapêutico , Pressão Sanguínea/efeitos dos fármacos , Bradicardia/induzido quimicamente , Bradicardia/epidemiologia , Criança , Pré-Escolar , Antagonistas Colinérgicos/administração & dosagem , Dexmedetomidina/administração & dosagem , Método Duplo-Cego , Efedrina/administração & dosagem , Efedrina/efeitos adversos , Efedrina/uso terapêutico , Feminino , Frequência Cardíaca/efeitos dos fármacos , Hemodinâmica/efeitos dos fármacos , Humanos , Hipnóticos e Sedativos/administração & dosagem , Hipotensão/induzido quimicamente , Incidência , Masculino , Pessoa de Meia-Idade , Antagonistas Muscarínicos/administração & dosagem , Antagonistas Muscarínicos/efeitos adversos , Parassimpatomiméticos/administração & dosagem , Estudos Prospectivos , Adulto Jovem
20.
J Clin Anesth ; 34: 208-15, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27687377

RESUMO

BACKGROUND: Previous evidence showed that use of phenylephrine was associated with higher umbilical artery pH (UA pH) than ephedrine after elective cesarean delivery (CD). However, the best choice of vasopressor and its effect on funic gases in cases of acute fetal compromise require additional studies. METHODS: Ninety parturients showing acute fetal compromise during intrapartum period and taken up for CD (category II) under spinal anesthesia were randomized to receive prophylactic infusion of ephedrine 2.5mg/min or phenylephrine 30µg/min. Systolic blood pressure was targeted between 90% and 110% of baseline. Incidence of fetal acidosis (UA pH <7.2 and/or base deficit >12mmol/L) was recorded. Other parameters of cord gases, Apgar score, need for immediate resuscitation, maternal hemodynamics, and adverse events were also compared. RESULTS: Number of neonates showing acidosis with ephedrine or phenylephrine was comparable (P=.22). Of these, newborns with base deficit >12mmol had low 1-minute Apgar scores (n=15/23). The ephedrine group had higher oxygen content in UA (P=.03). There was no adverse neonatal outcome during the period of observation. Incidence of maternal nausea and vomiting was higher with ephedrine than with phenylephrine (22.2% vs 4.4%; P=.02). Maternal bradycardia was observed with phenylephrine (P=.02). CONCLUSION: Our data report similar fetal acidosis with either phenylephrine or ephedrine administered during spinal anesthesia for treating maternal hypotension in cases of emergency CD.


Assuntos
Acidose/induzido quimicamente , Anestesia Obstétrica/métodos , Raquianestesia/métodos , Cesárea , Efedrina/farmacologia , Sofrimento Fetal/cirurgia , Feto/efeitos dos fármacos , Fenilefrina/farmacologia , Vasoconstritores/farmacologia , Adulto , Anestesia Obstétrica/efeitos adversos , Raquianestesia/efeitos adversos , Índice de Apgar , Bradicardia/induzido quimicamente , Método Duplo-Cego , Procedimentos Cirúrgicos Eletivos , Emergências , Efedrina/administração & dosagem , Efedrina/efeitos adversos , Feminino , Sofrimento Fetal/complicações , Sofrimento Fetal/patologia , Hemodinâmica/efeitos dos fármacos , Humanos , Concentração de Íons de Hidrogênio/efeitos dos fármacos , Hipotensão/prevenção & controle , Recém-Nascido , Fenilefrina/administração & dosagem , Fenilefrina/efeitos adversos , Gravidez , Estudos Prospectivos , Respiração Artificial , Artérias Umbilicais/química , Vasoconstritores/administração & dosagem , Vasoconstritores/efeitos adversos , Adulto Jovem
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