RESUMEN
Pranlukast is a novel LTD4 antagonist under development for the treatment of asthma. To assess the effect of age, the pharmacokinetics of pranlukast were studied in healthy young (9 females, 10 males, mean 30 years) and elderly subjects (9 per sex, mean 70.4 years). After an overnight fast volunteers were given 300 mg of pranlukast orally, 30 min after a light breakfast. Serial blood samples were collected for 24 hs, and the plasma was assayed by HPLC/UV. Pranlukast was well tolerated by the volunteers. The resultant mean plasma concentration vs. time data were very similar for both age groups. The estimated geometric mean AUCO-t and Cmax ratios (95% CI in parentheses) for elderly : young were 1.00 (0.71, 1.41) and 0.93 (0.66, 1.33), respectively. Median Tmax occurred at 4.5 h in both age groups. There were no significant differences observed in the pharmacokinetics of pranlukast between healthy young and elderly subjects. On stratifying the young and elderly data with respect to gender, no marked differences were observed between male and female subjects in the mean pharmacokinetic parameters of pranlukast, and the respective plasma concentrations profiles were very similar.
Asunto(s)
Asma/metabolismo , Cromonas/farmacocinética , Adulto , Factores de Edad , Anciano , Anciano de 80 o más Años , Análisis de Varianza , Asma/tratamiento farmacológico , Cromonas/sangre , Femenino , Humanos , MasculinoRESUMEN
A single 100 mg oral dose of denbufylline was administered in an open study to ten healthy, elderly subjects in order to characterise the pharmacokinetics of parent compound and its major pharmacologically active, circulating metabolites. Plasma concentrations were determined using a combination of GC and HPLC methods. Since denbufylline plasma concentrations were close to the assay limit of reliable determination, the disposition of the compound was assessed in terms of the pharmacokinetic parameters of three active metabolites. The general pharmacokinetic behaviour of debufylline was similar to that observed in young, healthy subjects, although plasma concentrations of the metabolites were higher and half-lives tended to be longer in the elderly group. None of the subjects presented any adverse events during the study.
Asunto(s)
Xantinas/farmacocinética , Anciano , Anciano de 80 o más Años , Biotransformación , Cromatografía de Gases , Cromatografía Líquida de Alta Presión , Femenino , Semivida , Humanos , Masculino , Xantinas/sangreRESUMEN
The safety and clinical efficacy of percutaneous transluminal coronary angioplasty (PTCA) in elderly patients has not been established. Of 639 PTCAs performed between March 1980 and May 1984, 119 patients were 65 years or older (mean 70 years). On angiography, elderly patients differed only in the more frequent occurrence of visible calcific deposits (26% vs 8% in younger patients, p less than 0.01). Primary success was achieved in 81%, vs 80% in patients younger than 65 years. Major complication rates were comparable to those of younger patients: emergency coronary artery bypass surgery, 4.1% vs 4.7%; acute myocardial infarction, 2.5% vs 2.9%; and death, 0.8% vs 0. Late clinical follow-up ranging from 5 to 50 months (mean 18) showed that symptomatic improvement was achieved in 91% of patients in whom PTCA was successful, with 55% being asymptomatic. Seventy percent of patients were as active or more active (30%) than before PTCA and 47% were taking fewer medications. Four late deaths occurred, none from cardiac causes. These data support the safety and clinical effectiveness of PTCA in elderly patients and justify the extension of indications for PTCA to selected patients with multivessel disease in this age group.