ABSTRACT
Usage of natural substances as therapeutic agents in modern medicine has sharply declined from the predominant position held in the early decades of last century, but search for bioactive molecules from nature (plants, animals, microflora) continues to play an important role in fashioning new medicinal agents. With the advent of modern techniques, instrumentation and automation in isolation and structural characterisation, we have on hand an enormous repository of natural compounds. In parallel to this, biology has also made tremendous progress in expanding its frontiers of knowledge. An interplay of these two disciplines constitutes the modern thrust in research in the realm of compounds elaborated by nature. The purpose of this article is to underline how natural products research continues to make significant contributions in the domain of discovery and development of new medicinal products. It is proposed to present the material under several heads, each of which has made natural products research relevant in the search for new and better medication.
ABSTRACT
PURPOSE--To evaluate the tolerability and 24 hours efficacy of a new anti-hypertensive drug: cilazapril. METHODS--In an open non comparative study 20 hypertensive patients (16 females, age from 30 to 60 years, average = 49.4) were followed for 6 weeks: 2 wash out and 4 treatment (5 mg OD). Blood pressure (BP) was measured by casual and ambulatory blood pressure monitoring (ABPM) readings. RESULTS--Comparing washout and treatment periods, ABPM averages both for systolic and diastolic BP (mmHg) showed significant decrease in 24 hours, during day and night sub periods. The decrease was not significant between averages considering the early morning rising pressure sub period. Heart rate averages showed significant reduction at all sub periods except during night. Adverse effects were mild and resolved spontaneously (n = 3, 15 per cent ). CONCLUSION--Cilazapril seems to be efficacious as antihypertensive. Tolerability is excellent. It preserved circadian rhythm despite significantly reducing blood pressure at all periods evaluated except early morning. A bradycardic effect observed mostly during day period should be better evaluated
Objetivo - Avaliar a tolerabilidade e eficácia antihipertensiva nas 24h do novo inibidor da ECA: cilazapril. Métodos - Num estudo aberto e não comparativo foram avaliados 20 pacientes (16 mulheres, idade entre 30 e 60 (média 49,4) anos, durante 6 semanas (2 de wash out e 4 de tratamento: cilazapril 5mg OD). A pressão arterial (PA) foi avaliada por método casual e por monitorização ambulatorial da pressão arterial (MAPA). Resultados - As médias de MAPA, comparando as fases pré droga e com droga, mostraram que tanto para pressão arterial sistólica (PAS) como diastólica (PAD), houve significativa redução de cifras, nas 24h, no período do dia e no da noite. Não houve redução significativa no sub-período da "ascensão rápida da PA " no fim da madrugada. A freqüência cardíaca média mostrou redução quando comparadas as médias das 24h e do dia, sem significância estatística nos demais sub-períodos. Os efeitos adversos foram leves e resolveram espontaneamente (n=3,15%). Conclusão - O cilazapril parece ser um eficaz anti-hipertensivo. A tolerabilidade foi excelente. Houve preservação do rítmo circadiano apesar da significativa redução das cifras tensionais em todos os períodos avaliados exceto o início da manhã (ascensão rápida da PA). Um discreto efeito bradicárdico notado durante o dia precisa ser melhor observado.