James M A, Walker P R, Papouchado M, Wilkinson P R
Br Heart J. 1985 Jun;53(6):631-5. doi: 10.1136/hrt.53.6.631.
A study was carried out to assess the efficacy of a new transdermal preparation of glyceryl trinitrate (Transiderm-Nitro 5) in the 24 hour prophylaxis of angina and to determine the duration of effect of a single patch application. Twelve men with chronic stable angina were studied in a randomised, placebo controlled, double blind trial. By serial treadmill exercise testing a therapeutic effect was shown at three hours; the exercise time to angina and to 1 mm ST segment depression and the total exercise time were all significantly increased. At 24, 48, and 72 hours, however, no therapeutic effect was observed. Recent studies have shown a similar lack of effect at 24 hours for various forms of transdermal delivery systems. It is suggested that this lack of effect is due to the rapid onset of tolerance probably as a result of the constancy of blood concentrations obtained by this method of administration.
开展了一项研究,以评估新型硝酸甘油透皮制剂(硝酸甘油控释贴片5)在心绞痛24小时预防中的疗效,并确定单次贴片应用的作用持续时间。在一项随机、安慰剂对照、双盲试验中对12名慢性稳定型心绞痛男性患者进行了研究。通过连续跑步机运动试验,在3小时时显示出治疗效果;心绞痛发作时间、ST段压低1毫米的运动时间以及总运动时间均显著增加。然而,在24、48和72小时时,未观察到治疗效果。最近的研究表明,各种形式的透皮给药系统在24小时时也有类似的无效情况。有人认为,这种无效是由于耐受性迅速产生,这可能是由于这种给药方法所获得的血药浓度恒定所致。