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           Search results for: Amiodarone Hydrochloride C25H30ClI2NO3 CAS: 19774-82-4   

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Do antibacterial and antifungal combinations have better activity against clinically relevant fusarium species? in vitro synergism.

The objective of this study was to evaluate the susceptibility of 20 clinical isolates of Fusarium spp. against classic antifungals (amphotericin B [AMB], itraconazole [ITC], voriconazole [VRC] and caspofungin [CAS]) and to nonantifungal agents (amiodarone [AMD], doxycycline [DOX] and moxifloxacin [MXF]) using broth microdilution method. The combinations between these antifungal plus nonantifungal agents were also evaluated for the determination of FICI (fractional inhibitory concentration index) using the checkerboard technique. Synergistic interactions were observed for the following combinations (% of synergisms): AMD + VRC (80%), MXF + AMB (75%), AMD + AMB (65%), MXF + VRC (60%), DOX + VRC (55%), DOX + AMB (50%) and AMD + CAS (30%). Synergisms were not observed for associations with itraconazole. Antagonism was not seen in any combination. Our findings suggest that the combinations of AMD, DOX or MXF with AMB or VRC to have potential for future in vivo investigations.

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Widely used pharmaceuticals present in the environment revealed as in vitro antagonists for human estrogen and androgen receptors.

A considerable amount of scientific evidence indicates that a number of pharmaceuticals that could be detected in the environment can contribute towards the development of problems associated with human reproductive systems, as well as those of wildlife. We investigated the estrogenic and androgenic effects of select pharmaceuticals with high production volume and environmental relevance. We examined the receptor-binding activities of these pharmaceuticals in the T47D human cell line using altered secretion of cytokine CXCL12. Functional yeast-luciferase reporter gene assays were also employed to confirm the mechanism of receptor binding by estrogen and androgen. Non-steroidal anti-inflammatory drugs, namely ibuprofen, diclofenac and antiarrhythmic agent amiodarone showed strong anti-estrogenic effects in the T47D cell line. In the yeast-luciferase assay, these anti-inflammatory drugs also demonstrated anti-estrogenic potency and inhibited the E2 response in a concentration-dependent manner. Amiodarone did not exhibit any response in the yeast-luciferase assay; therefore, the endocrine disruption presumably occurred at a different level without directly involving the receptor. All the anti-inflammatory drugs considered in this study, including ketoprofen, naproxen and clofibrate, exhibited a dose-dependent antagonism towards the androgen receptor in the yeast-luciferase assays. Several other drugs, including the stimulant caffeine, did not show any response in the tests that were employed. A risk assessment analysis using 'Hazard Quotient' suggested a potential risk, especially in the cases of ibuprofen, ketoprofen, diclofenac and clofibrate. The results reveal the intrinsic endocrine disrupting nature of several pharmaceuticals and thus could contribute towards explaining a number of adverse health effects on humans and wildlife.

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Comparative bioavailability study with two amiodarone tablet formulations administered with and without food in healthy subjects.

The aim was to assess the comparative bioavailability of two formulations (200 mg tablet) of amiodarone (CAS 19774-82-4) in healthy volunteers of both sexes, with and without food.

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[Long-term drug interaction of warfarin with amiodarone].

Authors describe a case of drug interaction between amiodarone and warfarin in 66-year-old man with recurrent atrial fibrillation. In spite of a relatively low dose of warfarin, prothrombin time became extremely prolonged and bleeding manifestations occurred. Effects of the interaction persisted for a long time after the withdrawal of both drugs. Various approaches to oral anticoagulant reversal are discussed. Pharmacokinetics of both drugs is explained, as well as the mechanism of their interaction through cytochrome P450 inhibition in the liver. Authors emphasize the great interindividual variability and long persistence of this interaction. It is necessary to consider carefully the indication of using these drugs together and when the use is inevitable, it is recommended to lower the warfarin dose to 50-70% and to perform thorough and frequent INR monitoring.

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[Myocardial revascularization in malignant ventricular tachyarrhythmia--prognostic significance].

The survival of patients with chronic ischaemic heart disease and malignant ventricular tachyarrhythmia is influenced positively in some instances by revascularization of the heart muscle and implantation of a cardioverter-defibrillator. The objective of the submitted work was to evaluate by perspective follow-up of subjects with chronic ischaemic heart disease and malignant ventricular tachyarrhythmia: a) the effect of revascularization of the heart muscle on the prognosis, making use of programmed stimulation of the ventricles and testing the effectiveness of antiarrhythmic treatment; b) the importance of implantation of a cardioverter-defibrillator in revascularized and non-revascularized subjects for the prevention of sudden "arrhythmic" deaths.

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[Electric programmed ventricular stimulation using a permanent cardiac pacing system--a noninvasive method in arrhythmia].

Complex forms of ventricular arrhythmias often occur in patients with an implanted permanent cardiac pacing system. Some of the pacemakers are provided with software which allows electrophysiological testing of the cardiac conduction system by coupling with an external diagnostic pacemaker via their programmer. This method is non-invasive.

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Stability of amiodarone in serum samples under various storage conditions.

The present study was intended to examine the stability of amiodarone (Cordarex, CAS 1951-25-3) and its metabolite desethylamiodarone. For this purpose 20 ml of blood were taken from each of 12 patients treated with amiodarone and were stored, after centrifuging, at room temperature, +5 degrees C, -18 degrees C and -38 degrees C. The amiodarone and desethylamiodarone concentrations were determined by the HPLC method 30 min, 24 h, 48 h, 72 h, one and two weeks after blood-taking. It turned out that the serum levels decreased continuously as of the first day regardless of the storage temperature. Correction factors were therefore calculated for the amiodarone concentration: if the blood level determination takes place after 24 h one should add 8% to the obtained value, after 48 h 16%, after 72 h 19%, after one week 23% and after two weeks 32%.

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Antiarrhythmic properties of benzyl-triamterene derivatives in the coronary artery ligated and reperfused rat.

Triamterene (CAS 396-01-0) and a series of benzyl-triamterene derivatives were evaluated for their antiarrhythmic properties in the coronary artery ligated and reperfused (CAL-R) rat. The effects were compared with the antiarrhythmic activity of the potassium sparing diuretic amiloride and drugs out of the class-I (lidocaine) and class-III (amiodarone and sotalol). Triamterene and sotalol revealed at high doses antifibrillator activity, while the benzyl-triamterenes 2, 3, 5 and 6 could also depress ventricular extrasystoles (VES) and ventricular tachycardia (VT). At low doses the most benzyltriamterenes protected significantly against ventricular fibrillation (VF) and so they were equieffective or more effective than amiodarone or lidocaine. Amiloride showed in the CAL-R rat no antiarrhythmic activity, so that we conclude different mechanisms responsible for antikaliuretic and antiarrhythmic properties of amiloride and triamterenes. Taking into account the results of recently reported in vitro studies, where we could demonstrate antiarrhythmic activity combined with positive inotropic properties for triamterenes, the antiarrhythmic profile of these compounds may offer new possibilities for the treatment of ventricular arrhythmias.

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[Monitoring the effectiveness of amiodarone in the treatment of ventricular ectopic arrhythmias].

The authors included in their investigation a total of 18 patients (15 men and 3 women) with electric instability of the ventricular heart muscle during programmed stimulation of the ventricles. They administered amiodarone to the patients by the oral route, 200 or 400 mg per day for a period of 3 to 13 months. They compared the subjective symptomatology, the finding on monitoring of the ECG with the patient in bed or by means of Holter's system and the results of programmed stimulation of the ventricles before and after amiodarone administration. There was a marked decline in the frequency of subjective symptoms reported by the patients (above all syncopes disappeared completely) and there was a marked decline or complete disappearance of serious ventricular ectopic dysrhythmias. Amiodarone eliminated electric instability of the ventricles as proved by programmed stimulation of the ventricles completely in 39% and partly in 11% of the subjects.

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