ABSTRACT
Background: Atrial fibrillation (AF) is the most common arrhythmia requiring treatment. High-dose oral anti-arrhythmics (mainly class 1C or quinidine) are used as “pill in the pocket” approach to convert recent onset AF. However pro-arrhythmic risk has limited the application of this approach in many patients. Ranolazine, an antianginal agent, which inhibits abnormal late Na+ channel currents, decreases sodium-calcium overload, potentially inhibits after-depolarisations which have been implicated in the initiation and propagation of AF. Methods: Two gramme ranolazine was given orally to 40 patients with new (first detected episode of AF, 16 patients) or paroxysmal (3 hours to 72 hours duration, 24 patients) AF. Twenty-four patients were in hospital, 6 in office, and 10 at home at the time of ranolazine administration. Age, sex, associated health condition, structural heart disease (SHD) and echocardiographic criteria were recorded. Treatment for other related conditions was also given. Successful conversion was defined as restoration of sinus rhythm within 6 hours of ranolazine administration. Results: Twenty-six of 40 patients (65%) converted to sinus rhythm. No pro-arrhythmic effects, haemodynamic instability, adverse effects, or perceived intolerance were noted. Conclusion: High-dose oral ranolazine shows utility as a possible safe agent to convert new or paroxysmal AF.
Subject(s)
ACETANILIDES --A ADMINISTRATION & , Acetanilides/analogs & derivatives , Administration, Oral , Adolescent , Adult , Aged , Atrial Fibrillation/drug therapy , Atrial Fibrillation/prevention & control , Female , Humans , Male , Middle Aged , Piperazines/administration & dosage , Piperazines/analogs & derivativesABSTRACT
En este trabajo se presenta el estudio químico radiofarmacológico y el uso en seres humanos realizado con el "mebrofeini-Tc-99m". La finalidad del trabajo fue determinar el uso potencial de este radiofármaco en seres humanos portadores de distintas entidades clínico patológicas. Para esto, se sintetizó el producto mejorando el rendimiento de reacción, mediante una modificación en la segunda etapa del camino de síntesis, lo que condujo a elevarlo del 70 al 90%. Se determinó la cinética plasmática mediante la circulación extracorpórea realizada en ratas wistar, mientras que la hepática y renal se llevó a cabo en ratones endocriados. Todos los resultados fueron analizados mediante un procesador, obteniéndose las vidas medias plasmáticas y los máximos tiempos de captación
Subject(s)
Mice , Rats , Animals , Humans , Liver , Sodium Pertechnetate Tc 99m , Acetanilides/analogs & derivatives , Bromine , Cholecystography , Quality Control , Sodium Pertechnetate Tc 99m/chemical synthesisABSTRACT
Six new substituted acylamides, chemically related to lignocaine were studied for local anaesthetic activity and toxicity in mice, frogs and guinea pigs. Only one of these compounds, w-pyrrolidino 2, 3, 5, 6 tetramethyl acetanilide was found to possess potency comparable to lignocaine with a slightly higher therapeutic index. Study of the S.A.R. of this group indicated that by removal of two methyl groups at position 3 and 5 in the above compound, a local anaesthetic with greater potency than lignocaine may be obtained. Further exploration of the potentialities of a compound having pyrrolidine group as a part of basic side chain is indicated.