RESUMEN
The pharmacokinetic profile of a single dose of 100 mg of (+/-)-N-[2-[[3-(o-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]- 2-(p-hydroxyphenyl) acetamide (epanolol, Visacor), has been determined in an open study of 15 elderly patients with stable angina pectoris. Haematological, biochemical and physiological measurements demonstrated that epanolol was well tolerated in this group of patients. A mean peak epanolol concentration of 18.4 ng/ml was observed at a mean time of 1.08 h. In about one third of patients, an analytically significant secondary peak was observed. Peak concentrations showed an interindividual variability of 16-fold. Following the peak, plasma concentrations declined biphasically. Epanolol was eliminated from plasma with a mean terminal half-life of 22 h. There was some evidence of a linear relationship between heart rate and logarithmic plasma concentration but this was not statistically significant. These data are consistent with the results of pharmacokinetic studies in healthy young volunteers.
Asunto(s)
Antagonistas Adrenérgicos beta/farmacocinética , Angina de Pecho/metabolismo , Bencenoacetamidas , Propanolaminas/farmacocinética , Antagonistas Adrenérgicos beta/uso terapéutico , Anciano , Anciano de 80 o más Años , Angina de Pecho/tratamiento farmacológico , Angina de Pecho/fisiopatología , Presión Sanguínea/efectos de los fármacos , Femenino , Semivida , Humanos , Masculino , Propanolaminas/uso terapéutico , RadioinmunoensayoRESUMEN
The safety and efficacy of once-daily lisinopril was assessed in an 8-week open-label study of 24 elderly patients with mild to moderate hypertension. Following withdrawal of all previous antihypertensive treatment, including diuretics, lisinopril treatment was started at a dose of 5 mg, increasing to a maximum of 40 mg once daily as required. Treatment provided effective 24-h BP control in all patients, most of whom required a daily dose of 20-40 mg, and cardiothoracic index decreased significantly, indicating a favourable effect on left ventricular volumes. There were no significant ECG alterations and no major side effects occurred. It is concluded that lisinopril 5 mg is a safe starting dose for elderly patients who are not on diuretics, and that once-daily lisinopril monotherapy reduces BP safety without affecting heart rate.