Akhras F, Jefferies S, Jackson G
Z Kardiol. 1985;74 Suppl 4:16-20.
Isosorbide-5-mononitrate (ISMN) is not subject to first-pass metabolism and has more predictable blood concentrations than isosorbide dinitrate. In order to evaluate its efficacy as monotherapy in patients with chronic stable angina, 14 patients were studied. All had angiographically proven coronary artery disease and were limited by angina on a treadmill exercise test. After a 2-week placebo period ISMN was administered in a single-blind fashion with the dosage being titrated at 2-week intervals. The dosage increments were 20 mg once daily, 20 mg twice daily, 40 mg once daily and 40 mg twice daily. Patients were assessed subjectively by anginal attack rate and glyceryl trinitrate (GTN) consumption and objectively by treadmill exercise testing at 12 hours post dosage. ISMN increased the exercise ability significantly on all dosage regimes. However, a significant reduction in ST depression occurred only with the twice-daily regime. The increased exercise performance was associated with a significant decrease in anginal attack rate and GTN consumption from the 20 mg b.i.d. increment. ISMN is an effective antianginal agent with a more favourable profile in twice-daily dosage. Whilst no significant differences emerged between 20 mg and 40 mg twice daily, individual variation occurred, indicating a need for dosage flexibility.
5-单硝酸异山梨酯（ISMN）不存在首过代谢，且与硝酸异山梨酯相比，其血药浓度更具可预测性。为评估其作为慢性稳定型心绞痛患者单一疗法的疗效，对14例患者进行了研究。所有患者均经血管造影证实患有冠状动脉疾病，且在平板运动试验中受心绞痛限制。经过2周的安慰剂期后，以单盲方式给予ISMN，剂量每2周滴定一次。剂量递增依次为每日1次20mg、每日2次20mg、每日1次40mg和每日2次40mg。在给药后12小时，通过心绞痛发作率和硝酸甘油（GTN）消耗量对患者进行主观评估，并通过平板运动试验进行客观评估。在所有剂量方案下，ISMN均显著提高了运动能力。然而，仅在每日2次给药方案下，ST段压低有显著降低。从每日2次20mg剂量递增开始，运动能力的提高与心绞痛发作率和GTN消耗量的显著降低相关。ISMN是一种有效的抗心绞痛药物，每日2次给药时疗效更佳。虽然每日2次20mg和40mg之间未出现显著差异，但存在个体差异，表明需要灵活调整剂量。
