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Lipid composition and dynamics of cell membranes of Bacillus stearothermophilus adapted to amiodarone

Rosa, Sónia M. L. J.; Antunes-Madeira, Maria do Carmo; Matos, Manuel J.; Jurado, Amália S.; Madeira, Vítor M. C.
Fonte: Universidade de Coimbra Publicador: Universidade de Coimbra
Tipo: Artigo de Revista Científica Formato: aplication/PDF
Português
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37.62%
Bacillus stearothermophilus, a useful model to evaluate membrane interactions of lipophilic drugs, adapts to the presence of amiodarone in the growth medium. Drug concentrations in the range of 1-2 [mu]M depress growth and 3 [mu]M completely suppresses growth. Adaptation to the presence of amiodarone is reflected in lipid composition changes either in the phospholipid classes or in the acyl chain moieties. Significant changes are observed at 2 [mu]M and expressed by a decrease of phosphatidylethanolamine (relative decrease of 23.3%) and phosphatidylglycerol (17.9%) and by the increase of phosphoglycolipid (162%). The changes in phospholipid acyl chains are expressed by a decrease of straight-chain saturated fatty acids (relative decrease of 12.2%) and anteiso-acids (22%) with a parallel increase of the iso-acids (9.8%). Consequently, the ratio straight-chain/branched iso-chain fatty acids decreases from 0.38 (control cultures) to 0.30 (cultures adapted to 2 [mu]M amiodarone). The physical consequences of the lipid composition changes induced by the drug were studied by fluorescence polarization of diphenylhexatriene and diphenylhexatriene-propionic acid, and by differential scanning calorimetry. The thermotropic profiles of polar lipid dispersions of amiodarone-adapted cells are more similar to control cultures (without amiodarone) than those resulting from a direct interaction of the drug with lipids...

Investigating herb–drug interactions: the effect of Citrus aurantium fruit extract on the pharmacokinetics of amiodarone in rats

Rodrigues, Márcio; Alves, Gilberto; Falcão, Amílcar
Fonte: Elsevier Publicador: Elsevier
Tipo: Artigo de Revista Científica
Português
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37.53%
Citrus aurantium extract has been largely used in weight loss and sports performance dietary supplements. However, the safety of C. aurantium-containing products has been questioned mainly due to the association of its use with adverse events in the cardiovascular system. Therefore, this work aimed to assess the potential for herb–drug interactions among a standardized C. aurantium extract (GMP certificate) and amiodarone (narrow therapeutic index drug) in rats. In a first pharmacokinetic study, rats were simultaneously co-administered with a single-dose of C. aurantium (164 mg/kg, p.o.) and amiodarone (50 mg/kg, p.o.); in a second study, rats were pre-treated during 14 days with C. aurantium (164 mg/kg/day, p.o.) and received amiodarone (50 mg/kg, p.o.) on the 15th day. Rats of the control groups received the corresponding volume of vehicle. Overall, after analysis of the pharmacokinetic data, it deserves to be highlighted the significant increase of the peak plasma concentration of amiodarone in rats pre-treated with C. aurantium extract, while the extent of systemic exposure was comparable between both groups. This paper reports, for the first time, data on the potential of herb–drug interaction between C. aurantium extract and amiodarone. However...

How frequently should a patient taking amiodarone be screened for thyroid dysfunction?

PAZIN-FILHO, A.; DE JESUS, A.M.X.; MAGALHÃES, P.K.R.; MELATO, L.H.; CAMPOS, D.; MACIEL, B.C.; MACIEL, L.M.Z.
Fonte: Associação Brasileira de Divulgação Científica Publicador: Associação Brasileira de Divulgação Científica
Tipo: Artigo de Revista Científica
Português
Relevância na Pesquisa
37.47%
Amiodarone-induced thyroid dysfunction (AITD) is a common complication of amiodarone therapy and its prevalence varies according to iodine intake, subclinical thyroid disorders and the definition of AITD. There is no consensus about the frequency of screening for this condition. We evaluated 121 patients on chronic regular intake of amiodarone (mean intake = 248.5 ± 89 mg; duration of treatment = 5.3 ± 3.9 years, range = 0.57-17 years) and with stable baseline cardiac condition. Those with no AITD were followed up for a median period of 3.2 years (range: 0.6-6.7) and the incidence rate of AITD, defined by clinical and laboratorial findings as proposed by international guidelines, was obtained (62.8 per 1000 patients/year). We applied the Cox proportional hazard model to adjust for potential confounding factors and used sensitivity analysis to identify the best screening time for follow-up. We detected thyroid dysfunction in 59 (48.7%) of the 121 patients, amiodarone-induced hypothyroidism in 50 (41.3%) and hyperthyroidism in 9 (7.5%). Compared with patients without AITD, there was no difference regarding dosage or duration of therapy, heart rhythm disorder or baseline cardiac condition. During the follow-up of the 62 patients without AITD at baseline evaluation...

Effects of amiodarone on lung tissue mechanics and parenchyma remodeling

SANTOS, Flavia B.; GARCIA, Cristiane S. N. B.; XISTO, Debora G.; NEGRI, Elnara M.; CAPELOZZI, Vera L.; FAFFE, Debora S.; ROCCO, Patricia R. M.; ZIN, Walter A.
Fonte: ELSEVIER SCIENCE BV Publicador: ELSEVIER SCIENCE BV
Tipo: Artigo de Revista Científica
Português
Relevância na Pesquisa
37.47%
We studied the results of chronic oral administration of amiodarone on in vitro lung tissue mechanics, light and electron microscopy. Fifteen Wistar male rats were divided into three groups. In control (CTRL) group animals received saline (0.5 mL/day). In amiodarone (AMIO) groups, amiodarone was administered by gavage at a dose of 175 mg/kg 5 days per week for 6 (6AMIO) or 12 weeks (12AMIO). Lung tissue strips were analyzed 24 h after the last drug administration. Tissue resistance and elastance were higher in 6AMIO and 12AMIO than in CTRL, while hysteresivity was similar in all groups. Total amount of collagen fibers in lung parenchyma increased progressively with the time course of the lesion. However, at 6 weeks there was an increase in the amount of type III collagen fibers, while in 12AMIO mainly type I collagen fibers were found. In our study amiodarone increased lung tissue impedance that was accompanied by matrix remodeling and lesion of type II pneumocytes. (C) 2008 Elsevier B.V. All rights reserved.; PRONEX-MCT; PRONEX-FAPERJ; CNPq; FAPERJ; CAPES

Distinção entre os tipos 1 e 2 de tireotoxicose associada à amiodarona por meio de dúplex-Doppler colorido; Differentiation between types 1 and 2 of amiodarone-associated thyrotoxicosis using color duplex sonography

Macedo, Tulio Augusto Alves
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Tese de Doutorado Formato: application/pdf
Publicado em 10/11/2006 Português
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INTRODUÇÃO: A amiodarona pode causar tireotoxicose, principalmente em áreas geográficas onde a ingestão de iodo é insuficiente. Dois tipos distintos de tireotoxicose associada à amiodarona (TAA) podem ser encontrados: A) o tipo 1 - a doença é secundária à sobrecarga de iodo (fenômeno Jod-Basedow), geralmente encontrada em indivíduos com doença tireóidea preexistente, B) o tipo 2 - quando a tireotoxicose deve-se a uma tireoidite destrutiva, com ruptura folicular e liberação do conteúdo folicular. A distinção entre os dois tipos é fundamental para a conduta terapêutica. Este estudo transversal, realizado no Instituto de Radiologia do Hospital das Clínicas da Faculdade de Medicina da Universidade de São Paulo entre janeiro de 2004 a março de 2006, objetivou: A) Demonstrar a utilidade da densidade de pixéis coloridos (DPC), parâmetro objetivo obtido por meio de programa de computador, na distinção entre os dois tipos de TAA. B) Determinar os melhores critérios objetivos de distinção entre os dois tipos de TAA por meio da ultra-sonografia dúplex-Doppler colorido da tireóide. C) Conhecer o grau de concordância intra-observadores e interobservadores dos padrões subjetivos de vascularização do parênquima tireóideo. MÉTODOS: Foram examinadas 158 glândulas tireóideas por meio de dúplex-Doppler colorido. Após passagem pelos critérios de seleção...

Aplicação da catálise de trasnferência de fase na avaliação de rotas alternativas para obtenção industrial da dicicloverina caramifeno e amiodarona; The use of phase transfer catalysis, in the development of alternative routes for industrial production of dicycloverine, caramiphen and amiodarone

Polakiewicz, Bronislaw
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Tese de Doutorado Formato: application/pdf
Publicado em 20/12/1994 Português
Relevância na Pesquisa
37.12%
O emprego da catálise de transferência de fase substituindo uma ou mais etapas da síntese de um fármaco, pode ser um recurso vantajoso sob o ponto de vista tecnológico. Empregado na síntese de importantes fármacos que são a dicicloverina, caramifeno eamiodarona, a catálise de transferência de fase revelou-se muito vantajosa na síntese dos dois primeiros. A dicicloverina e o caramifeno tiveram as suas rotas de obtenção verticalizadas, com bons resultados e custos bem mais baixos quando comparados com os atualmente adquiridos no exterior. Ficou evidente que a catálise de transferência de fase pode ser aplicada com sucesso na produção destes e outros fármacos em associação com técnicas já conhecidas com ótimos resultados.; The phase transfer catalysis application replacing one or more steps in the drug synthesis, can be of advantage in the technologycal approach. Applied to the synthesis of important drugs such as diciclomine, caramiphen,and amiodarone, the phase transfer catalysis resulted in a very advantageous method in the first two drugs. The diciclomine and the caramiphen, gets their obtention routes from raw materiaIs wi th good resul ts and low coasts, when compared wi th the drugs presently purchassed in foreign countries. It is clear that the phase transfer catalysis...

Amiodarone-induced thyroid dysfunction in a tertiary center in south Brazil

Schaan,Beatriz D.; Cunha,Caroline P.; Francisconi,Alessandra; Zottis,Berenice; Brum,Graciela; Bruch,Ricardo S.; Gus,Miguel
Fonte: Sociedade Brasileira de Endocrinologia e Metabologia Publicador: Sociedade Brasileira de Endocrinologia e Metabologia
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/12/2005 Português
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37.53%
Amiodarone, used in the treatment of cardiac arrhythmias, is associated with thyroid dysfunction. No reports exist on its frequency in southern Brazil, nor studies evaluating the usefulness of clinical scores to diagnose thyroid abnormalities in these patients. This study aimed at determining the prevalence of amiodarone-induced thyroid dysfunction in a representative sample from a tertiary center, to study the conditions associated to this dysfunction and to evaluate the reliability of clinical scores of hypo and hyperthyroidism. One hundred ninety-five amiodarone users were submitted to a clinical and laboratory evaluation. Of these, 2.1% were hyperthyroid, 25.1% hypothyroid and 9.2% had only a high T4. Considering thyroid dysfunction variables researched, thyroid autoimmunity was positively associated (OR 4.8; p= 0.02), and male gender had a trend to a positive association (OR 1.86; p= 0.06). Clinical scores were highly sensitive for hyperthyroidism (100%), but not for hypothyroidism (8%). The low prevalence of amiodarone-induced hypothyroidism suggests that this specific region is iodine-sufficient. All patients receiving chronic amiodarone therapy should be checked for clinical scores for hyperthyroidism and laboratory evaluation should be performed...

Carbamazepine kinetics in cardiac patients before and during amiodarone

Leite,Silmara A.O.; Leite,Paulo J.M.; Rocha,Gilberto A.; Routledge,Philip A.; Bittencourt,Paulo Rogério M.
Fonte: Academia Brasileira de Neurologia - ABNEURO Publicador: Academia Brasileira de Neurologia - ABNEURO
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/06/1994 Português
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37.53%
Carbamazepine and amiodarone may often be used together, especially in countries where cardiomyopathies are common. In this study single doses of carbamazepine (400 mg) were given to patients with cardiac disease before and after one month of therapy with amiodarone, 400 mg daily. The kinetic profile of carbamazepine, its free fraction, and serum amiodarone, were measured at the two occasions. There was no statistically significant change in carbamazepine kinetics or free fraction, before and after the introduction of amiodarone. The concentrations of amidarone after one month of therapy were low. It is sugested that the possible interaction in the hepatic metabolism was not demonstrated because amiodarone concentrations were not enough to inhibit carbamazepine metabolism.

Acute effect of amiodarone on cardiovascular reflexes of normotensive and renal hypertensive rats

Oliveira,P.F.; Dias da Silva,V.J.; Salgado,M.C.O.; Fazan Jr.,R.; Aguiar,C.A.; Salgado,H.C.
Fonte: Associação Brasileira de Divulgação Científica Publicador: Associação Brasileira de Divulgação Científica
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/06/2005 Português
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37.58%
The aim of the present study was to evaluate the effect of amiodarone on mean arterial pressure (MAP), heart rate (HR), baroreflex, Bezold-Jarisch, and peripheral chemoreflex in normotensive and chronic one-kidney, one-clip (1K1C) hypertensive rats (N = 9 to 11 rats in each group). Amiodarone (50 mg/kg, iv) elicited hypotension and bradycardia in normotensive (-10 ± 1 mmHg, -57 ± 6 bpm) and hypertensive rats (-37 ± 7 mmHg, -39 ± 19 bpm). The baroreflex index (deltaHR/deltaMAP) was significantly attenuated by amiodarone in both normotensive (-0.61 ± 0.12 vs -1.47 ± 0.14 bpm/mmHg for reflex bradycardia and -1.15 ± 0.19 vs -2.63 ± 0.26 bpm/mmHg for reflex tachycardia) and hypertensive rats (-0.26 ± 0.05 vs -0.72 ± 0.16 bpm/mmHg for reflex bradycardia and -0.92 ± 0.19 vs -1.51 ± 0.19 bpm/mmHg for reflex tachycardia). The slope of linear regression from deltapulse interval/deltaMAP was attenuated for both reflex bradycardia and tachycardia in normotensive rats (-0.47 ± 0.13 vs -0.94 ± 0.19 ms/mmHg and -0.80 ± 0.13 vs -1.11 ± 0.13 ms/mmHg), but only for reflex bradycardia in hypertensive rats (-0.15 ± 0.02 vs -0.23 ± 0.3 ms/mmHg). In addition, the MAP and HR responses to the Bezold-Jarisch reflex were 20-30% smaller in amiodarone-treated normotensive or hypertensive rats. The bradycardic response to peripheral chemoreflex activation with intravenous potassium cyanide was also attenuated by amiodarone in both normotensive (-30 ± 6 vs -49 ± 8 bpm) and hypertensive rats (-34 ± 13 vs -42 ± 10 bpm). On the basis of the well-known electrophysiological effects of amiodarone...

How frequently should a patient taking amiodarone be screened for thyroid dysfunction?

Pazin-Filho,A.; de Jesus,A.M.X.; Magalhães,P.K.R.; Melato,L.H.; Campos,D.; Maciel,B.C.; Maciel,L.M.Z.
Fonte: Associação Brasileira de Divulgação Científica Publicador: Associação Brasileira de Divulgação Científica
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/08/2009 Português
Relevância na Pesquisa
37.47%
Amiodarone-induced thyroid dysfunction (AITD) is a common complication of amiodarone therapy and its prevalence varies according to iodine intake, subclinical thyroid disorders and the definition of AITD. There is no consensus about the frequency of screening for this condition. We evaluated 121 patients on chronic regular intake of amiodarone (mean intake = 248.5 ± 89 mg; duration of treatment = 5.3 ± 3.9 years, range = 0.57-17 years) and with stable baseline cardiac condition. Those with no AITD were followed up for a median period of 3.2 years (range: 0.6-6.7) and the incidence rate of AITD, defined by clinical and laboratorial findings as proposed by international guidelines, was obtained (62.8 per 1000 patients/year). We applied the Cox proportional hazard model to adjust for potential confounding factors and used sensitivity analysis to identify the best screening time for follow-up. We detected thyroid dysfunction in 59 (48.7%) of the 121 patients, amiodarone-induced hypothyroidism in 50 (41.3%) and hyperthyroidism in 9 (7.5%). Compared with patients without AITD, there was no difference regarding dosage or duration of therapy, heart rhythm disorder or baseline cardiac condition. During the follow-up of the 62 patients without AITD at baseline evaluation...

Use of lidocaine, propranolol, amiodarone, and verapamil in toad envenoming (genus bufo) in dogs

SAKATE,M.; OLIVEIRA,P. C. LUCAS DE
Fonte: Centro de Estudos de Venenos e Animais Peçonhentos - CEVAP, Universidade Estadual Paulista - UNESP Publicador: Centro de Estudos de Venenos e Animais Peçonhentos - CEVAP, Universidade Estadual Paulista - UNESP
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/12/2001 Português
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37.39%
Toad envenoming in dogs can cause death by cardiac fibrilation (CVF). Traditional therapy consists mainly of atropine and propranolol, the last one used to prevent the CVF, that is preceded by negative ventricular deflections (NVDs) in the QRS complex of the electrocardiogram. This study intended to verify, comparatively, the lidocaine, propranolol, amiodarone, and verapamil abilities to prevent CVF in experimentally envenomed dogs. Thirty-six dogs were divided into 6 groups (GL, GP, GA, GV, GST, and GSV) with n=6; the dogs were submitted to volatile anaesthesia. The animals of the groups GL, GP, GA, and GV received 0.38g of toad venom through oro-gastric catheter and were treated with the following drugs respectively: lidocaine (4mg/Kg), propranolol (0.1mg/Kg), amiodarone (8mg/Kg), and verapamil (2mg/Kg). These drugs were repeated if NVDs reappeared with cardiac frequency >150, GST was not treated and GSV was just anaesthetized. The following results were obtained: GL, NVDs present in 4 animals, 100% recuperation with 3.66 doses/animal; GP, NVDs present in 2 animals, 100% recuperation with 1.66 dose/animal, with bradycardia at the anaesthetic return; GA, NVDs present in 3 animals, 33.33% recuperation with 1.5 dose/animal; GV, NVDs present in 4 animals...

Amiodarone prophylaxis for tachycardias after coronary artery surgery: a randomised, double blind, placebo controlled trial.

Butler, J; Harriss, D R; Sinclair, M; Westaby, S
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /07/1993 Português
Relevância na Pesquisa
27.77%
BACKGROUND--Arrhythmias are a common cause of morbidity after cardiac surgery. This study assessed the efficacy of prophylactic amiodarone in reducing the incidence of atrial fibrillation or flutter and ventricular arrhythmias after coronary artery surgery. METHODS--A double blind, randomised, placebo controlled trial. 60 patients received a 24 hour intravenous infusion of amiodarone (15 mg/kg started after removal of the aortic cross clamp) followed by 200 mg orally three times daily for 5 days, and 60 patients received placebo. RESULTS--6 patients (10%) in the amiodarone group and 14 (23%) in the placebo group needed treatment for arrhythmias (95% confidence interval (95% CI) for the difference between groups was 0 to 26%, p = 0.05). The incidence of supraventricular tachycardia detected clinically and requiring treatment was lower in the amiodarone group (8% amiodarone v 20% placebo, 95% CI 0 to 24%, p = 0.07). The incidence detected by 24 hour Holter monitoring was similar (17% amiodarone v 20% placebo). Untreated arrhythmias in the amiodarone group were either clinically benign and undetected (n = 3) or the ventricular response rate was slow (n = 2). Age > 60 years was a positive risk factor for the development of supraventricular tachycardia in the amiodarone group but not in the placebo group. Fewer patients had episodes of ventricular tachycardia or fibrillation recorded on Holter monitoring in the amiodarone group (15% amiodarone v 33% placebo...

Parenteral magnesium sulfate versus amiodarone in the therapy of atrial tachyarhythmias: A prospective randomized study

Moran, J.; Gallagher, J.; Peake, S.; Cunningham, D.; Salagaras, M.; Leppard, P.
Fonte: Williams & Wilkins Publicador: Williams & Wilkins
Tipo: Artigo de Revista Científica
Publicado em //1995 Português
Relevância na Pesquisa
37.67%
OBJECTIVE: To compare the efficacy of parenteral magnesium sulfate vs. amiodarone in the therapy of atrial tachyarrhythmias in critically ill patients. DESIGN: Prospective, randomized study. SETTING: Multidisciplinary intensive care unit (ICU) at a university teaching hospital. PATIENTS: Forty-two patients, 21 medical and 21 surgical, of mean (SD) age 67 +/- 15 yrs and mean Acute Physiology and Chronic Health Evaluation II score of 22 +/- 6, with atrial tachyarrhythmias (ventricular response rate of > or = 120 beats/min) sustained for > or = 1 hr. INTERVENTIONS: After correction of the plasma potassium concentration to > or = 4.0 mmol/L, patients were randomly allocated to treatment with either a) magnesium sulfate 0.037 g/kg (37 mg/kg) bolus followed by 0.025 g/kg/hr (25 mg/kg/hr); or b) amiodarone 5 mg/kg bolus and 10 mg/kg/24-hr infusion. Therapeutic plasma magnesium concentration in the magnesium sulfate group was 1.4 to 2.0 mmol/L. Therapeutic end point was conversion to sinus rhythm over 24 hrs. MEASUREMENTS AND MAIN RESULTS: At study entry (time 0), initial mean ventricular response rate and systolic blood pressure were 151 +/- 16 (SD) beats/min and 127 +/- 30 mm Hg in the magnesium sulfate group vs. 153 +/- 23 beats/min and 123 +/- 23 mm Hg in the amiodarone group...

Inhibition of carnitine palmitoyltransferase-1 in rat heart and liver by perhexiline and amiodarone.

Kennedy, J.; Unger, S.; Horowitz, J.
Fonte: Universidade de Adelaide Publicador: Universidade de Adelaide
Tipo: Artigo de Revista Científica
Publicado em //1996 Português
Relevância na Pesquisa
37.39%
The mechanism of the anti-anginal effect of perhexiline is unclear but appears to involve a shift in cardiac metabolism from utilization of fatty acid to that of carbohydrate. We tested the hypothesis that perhexiline inhibits the enzyme carnitine palmitoyltransferase-1 (CPT-1), which controls access of long chain fatty acids to the mitochondrial site of beta-oxidation. Perhexiline produced a concentration-dependent inhibition of CPT-1 in rat cardiac and hepatic mitochondria in vitro, with half-maximal inhibition (IC50) at 77 and 148 mumol/L, respectively. Amiodarone, another drug with anti-anginal properties, also inhibited cardiac CPT-1 (IC50 = 228 mumol/L). The rank order of potency for inhibition was malonyl-CoA > 4-hydroxyphenylglyoxylate (HPG) = perhexiline > amiodarone = monohydroxy-perhexiline. Kinetic analysis revealed competitive inhibition of cardiac and hepatic CPT-1 by perhexiline with respect to palmitoyl-CoA but non-competitive inhibition with respect to carnitine. Curvilinear Dixon plots generated "apparent inhibitory constant (Ki)" values for perhexiline, which indicated a greater sensitivity of the cardiac than the hepatic enzyme to inhibition by perhexiline. Perhexiline inhibition of CPT-1, unlike that of malonyl-CoA and HPG...

A case series of concomitant treatment of perhexiline with Amiodarone

Gilutz, H.; Frenneaux, M.; Horowitz, J.
Fonte: Lippincott Williams & Wilkins Publicador: Lippincott Williams & Wilkins
Tipo: Artigo de Revista Científica
Publicado em //2012 Português
Relevância na Pesquisa
37.62%
Background: Concomitant treatment with amiodarone and perhsexiline has been considered to be relatively contraindicated because of the hypothetical risk of potentiated adverse effects mediated by additive inhibition of carnitine palmitoyl transferase 1. Aim: To study the prevalence of adverse effects associated with the concomitant use of perhexiline and amiodarone. Methods: A retrospective analysis of a single hospital database of patients receiving perhexiline and amiodarone between July 2009 and April 2011. Files were reviewed for short- and long-term adverse effects requiring drug cessation. Glucose concentration, gamma glutamyl transferase activity. and perhexiline blood concentrations were recorded. Results: We identified 26 patients concomitantly treated with perhexiline and amiodarone, 20 on a long-term basis. In 6 cases, amiodarone was introduced on top of preceding perhexiline. In none of the cases were drugs stopped because of adverse effects. Although blood glucose concentrations fell significantly 48 hours postadmission to hospital, this seems to reflect the resolution of "admission hyperglycemia" rather than onset of hypoglycemia; the latter was rare (5 patients), mild, and clinically silent. In 4 patients, gamma glutamyl transferase approximately doubled. Conclusions: Traditionally...

Bilateral Optic Disc Edema Secondary to Amiodarone: Manifestation of an Iatrogenic Optic Neuropathy; Edema Bilateral do Disco Óptico Secundário a Amiodarona: Manifestação de uma Neuropatia Óptica Iatrogénica

Andrade, Carlos; Serviço de Neurologia. Centro Hospitalar de São João. Porto. Portugal. Faculdade de Medicina. Universidade do Porto. Porto. Portugal.; Faria, Olinda; Serviço de Oftalmologia. Centro Hospitalar de São João. Porto. Portugal. Faculdade
Fonte: Ordem dos Médicos Publicador: Ordem dos Médicos
Tipo: info:eu-repo/semantics/article; other; info:eu-repo/semantics/publishedVersion Formato: application/pdf
Publicado em 29/05/2015 Português
Relevância na Pesquisa
37.39%
A 69-years-old male patient was treated with amiodarone 200mg/day over the passed two months for atrial fibrillation. He presented a sudden, painless and unilateral visual loss. Ophthalmologic evaluation revealed a bilateral optic disc edema. Neurological examination was otherwise unremarkable. After properly excluding increased intracranial pressure and giant cell arteritis, the main differential diagnosis was between nonarteritic anterior ischemic optic neuropathy and optic neuropathy secondary to amiodarone. The latter diagnosis was favored due to a presence of bilateral and simultaneous optic disc edema, gradual improvement of symptoms after discontinuation of the drug, and, mostly, by persistence of optic disc edema beyond 6 weeks. Of note, an acute presentation of this disorder is common. Amiodarone optic neuropathy is a rare but potentially serious cause of optic nerve dysfunction, and its discontinuation is usually warrant.; Um doente de 69 anos, sexo masculino, inicia de forma súbita uma hipovisão unilateral indolor. Encontrava-se medicado com amiodarona, 200 mg/dia, iniciada dois meses antes por fibrilação auricular. A avaliação oftalmológica inicial constatou um edema bilateral do disco óptico. O restante exame neurológico não apresentava alterações de relevo. Após a exclusão de uma etiologia arterítica ou relacionada com hipertensão intracraniana...

Is there variability in drug release and physical characteristics of amiodarone chloride from different commercially available tablets? Possible therapeutic implications

Ngo, S.; Barnes, T.
Fonte: The Royal Pharmacuetical Society of Great Britain Publicador: The Royal Pharmacuetical Society of Great Britain
Tipo: Artigo de Revista Científica
Publicado em //2010 Português
Relevância na Pesquisa
37.39%
OBJECTIVES: Amiodarone is a low-solubility, high-permeability drug with a narrow therapeutic index and reported bioavailability problems associated with switching formulations. The aim of this study was to identify whether there is variability in drug release and physical characteristics of different commercially available amiodarone hydrochloride formulations in Australia. METHODS: Four available formulations (innovator Cordarone (COR) and generic products G1, G2 and G3) were tested for drug dissolution, content uniformity, hardness, weight variation, friability and disintegration in accordance with the US Pharmacopeia specifications. KEY FINDINGS: The tested formulations exhibited variable dissolution behaviours: G1 and G3 exhibited the fastest dissolution, G2 dissolution was the slowest and Cordarone showed a medium dissolution. After 3 months' exposure to high temperature (40 +/- 2 degrees C) and relative humidity (75 +/- 5%), the products exhibited a higher degree of disparity, with drug-release profiles of the generics being markedly different from that of Cordarone. This suggests possible implications on bioequivalence for patients who live in warm/tropical regional areas. Most products met the US Pharmacopeia specifications for drug-content uniformity and other test physical characteristics. CONCLUSIONS: The results suggested that variability in drug release profiles in vitro of amiodarone formulations might be a potential indicator of compromised bioavailability...

Mechanisms of Amiodarone and Desethylamiodarone Cytotoxicity in Human Lung Cells

BLACK, JEANNE
Fonte: Quens University Publicador: Quens University
Tipo: Tese de Doutorado Formato: 558807 bytes; application/pdf
Português
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Amiodarone (AM) is a potent antidysrhythmic agent which can cause potentially life-threatening pulmonary fibrosis, and N-desethylamiodarone (DEA) is a metabolite of AM that may contribute to the toxicity of AM in vivo. Recent evidence has implicated the involvement of the renin-angiotensin system (RAS) in the initiation and progression of amiodarone-induced pulmonary toxicity. In cultured HPL1A human peripheral lung epithelial cells, we found AM to be converted to DEA minimally (< 2%) after 24 h of incubation, indicating that the HPL1A cell culture model can be used to study the effects of AM and DEA independently. Apoptotic cell death was assessed by annexin-V-FITC (ann-V) staining and by terminal deoxynucleotidyl transferase-mediated 2’-deoxyuridine 5’-triphosphate nick-end labeling (TUNEL), while necrotic cell death was determined by propidium iodide (PI) staining. The percentage of PI positive cells increased over six-fold after 24 h treatment with 20 μM AM (80.8%) compared to control (12.0%), and doubled after 24 h treatment with 3.5 μM DEA (20.4%) compared to control (10.8%). The percentage of ann-V positive cells decreased from 8.26% (control) to 1.56% following 24 h treatment with 10 μM AM and more than doubled after 24 h incubation with 3.5 μM DEA (22.0%) compared to control (9.86%) (p<0.05). Treatment for 24 h with 5.0 μM DEA caused the percentage of TUNEL positive cells to increase from 4.21% (control) to 26.7% (p<0.05). Vitamin E (5 – 20 μM) did not protect against AM or DEA cytotoxicity...

Amiodarone-induced thyroid dysfunction in a tertiary center in south Brazi; Disfunção tiroideana induzida por amiodarona em um centro terciário do sul do Brasil

Schaan, Beatriz D'Agord; Cunha, Caroline Paim da; Francisconi, Alessandra B.; Zottis, Berenice; Brum, Graciela Scalco; Brüch, Ricardo Santalucia; Gus, Miguel
Fonte: Universidade Federal do Rio Grande do Sul Publicador: Universidade Federal do Rio Grande do Sul
Tipo: Artigo de Revista Científica Formato: application/pdf
Português
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A amiodarona, usada no tratamento de arritmias cardíacas, está associada com disfunção tiroideana. Não existem relatos sobre sua freqüência no sudeste do Brasil e nem estudos avaliando a utilidade de scores clínicos para o diagnóstico de anormalidades tiroideanas nesses pacientes. Este estudo visou determinar a prevalência de disfunções tiroideanas induzidas pela amiodarona numa amostra representativa de um centro teciário, para estudar as condições associadas a esta disfunção e para avaliar a confiabilidade de scores clínicos para hipo e hipertiroidismo. Avaliação clínica e laboratorial foi realizada em 195 pacientes em uso de amiodarona; desses, 2,1% tinha hipertiroidismo, 25,1% hipotiroidismo e 9,2% tinha apenas um T4 elevado. Considerando as variáveis pesquisadas de disfunção tiroideana, a autoimunidade tiroideana estava associada positivamente (OR 4,8; p= 0,02), e o sexo masculino teve uma tendência para associação positiva (OR 1,86; p= 0,06). Os scores clínicos mostraramse altamente sensíveis para o hipertiroidismo (100%), mas não para o hipotiroidismo (8%). A baixa prevalência de hipotiroidismo induzido pela amiodarona sugere que esta região geográfica específica seja suficiente em iodeto. Todo paciente recebendo terapia crônica com amiodarona deve ser investigado pelos scores clínicos para hipertiroidismo e avaliado laboratorialmente com um screening para disfunção tiroideana...

BRONQUIOLITE OBLITERANTE E PNEUMONIA EM ORGANIZAÇÃO SECUNDÁRIA AO USO DE AMIODARONA; BRONCHIOLITIS OBLITERANS ORGANIZING PNEUMONIA SECONDARY TO AMIODARONE

Pereira da Cunha, João Pedro; Frandoloso, Gibran Avelino; Hospital de Clínicas da UFPR; Cervi Lagana, Caio Cesar; Hospital de Clínicas da UFPR; Pupo, Melissa; Hospital de Clínicas da UFPR
Fonte: Setor de Ciência da Saúde - Universidade Federal do Paraná Publicador: Setor de Ciência da Saúde - Universidade Federal do Paraná
Tipo: info:eu-repo/semantics/article; info:eu-repo/semantics/publishedVersion; Avaliado pelos pares; ; Formato: application/pdf
Publicado em 12/10/2015 Português
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A amiodarona é um antiarrítmico comumente utilizado na prática clínica e pode estar associado a diversos efeitos adversos, muitos deles com significativa morbimortalidade, como o acometimento pulmonar. O presente caso descreve uma mulher de 63 anos com toxicidade pulmonar aguda pela amiodarona, utilizada em curto período de tempo. A realização de biópsia pulmonar demonstrou bronquiolite obliterante e pneumonia em organização (BOOP). Após interrupção do uso do antiarrítmico e o início da corticoterapia, a paciente obteve expressiva melhora clínica e radiológica. ; Amiodarone is a widely used anti-arrhythmic agent in clinical practice. One of the potentially life threatening adverse effects is amiodarone-induced pulmonary toxicity (APT). We describe a case of a 63-year-old woman with APT. The diagnostic workup included pulmonary biopsy that demonstrated bronchiolitis obliterans organizing pneumonia (BOOP). Amiodarone was discontinued subsequently and corticosteroid treatment initiated, with clinical and radiological disease remission.