Jackson S H, Shepherd A M, Ludden T M, Jamieson M J, Woodworth J, Rogers D, Ludden L K, Muir K T
Department of Health Care of the Elderly, Kings College and Dulwich Hospital, London, England.
J Cardiovasc Pharmacol. 1990 Oct;16(4):624-8. doi: 10.1097/00005344-199010000-00014.
Hydralazine is a vasodilator antihypertensive drug that has been in use for many years. Efficacy after oral administration correlates well with the levels of the drug in blood. Factors such as food ingestion that affect blood levels of hydralazine may therefore be of importance. There is dispute regarding the effect of food intake on blood levels of hydralazine and on the antihypertensive response. This randomized cross-over study examined the effect of food (642 K calories, 25 g protein, 43 g fat, 40 g carbohydrates, 32 mEq sodium, 17 mEq potassium) ingested immediately before hydralazine (taken as Apresoline, Ciba Geigy, or as slow-release hydralazine, SRH, Pennwalt Corporation) on the blood levels of hydralazine in 16 essential hypertensive patients who were slow acetylators currently taking at least 100 mg Apresoline daily. Peak blood hydralazine levels were reduced by food after both Apresoline and SRH, by 69 and 66%, respectively. Time to peak blood hydralazine concentration was delayed significantly with SRH. We could detect a statistically significant food-related reduction of area under blood hydralazine concentration versus time curves (AUC) only with Apresoline (by 44%). The AUC for SRH was decreased only 29% by food. Hydralazine should be taken at a consistent time with respect to meals.
肼屈嗪是一种血管扩张剂类降压药，已使用多年。口服后的疗效与血液中药物水平密切相关。因此，诸如食物摄入等影响肼屈嗪血液水平的因素可能很重要。关于食物摄入对肼屈嗪血液水平和降压反应的影响存在争议。这项随机交叉研究考察了在服用肼屈嗪（以阿普利素灵，汽巴嘉基公司生产，或缓释肼屈嗪，SRH，彭瓦尔公司生产）之前立即摄入食物（642千卡热量、25克蛋白质、43克脂肪、40克碳水化合物、32毫当量钠、17毫当量钾）对16名原发性高血压患者血液中肼屈嗪水平的影响，这些患者为慢乙酰化者，目前每天至少服用100毫克阿普利素灵。服用阿普利素灵和SRH后，食物均使血液中肼屈嗪峰值水平降低，分别降低了69%和66%。服用SRH后，达到血液中肼屈嗪浓度峰值的时间显著延迟。仅服用阿普利素灵时，我们能检测到与食物相关的血液中肼屈嗪浓度-时间曲线下面积（AUC）有统计学显著降低（降低44%）。食物仅使SRH的AUC降低29%。肼屈嗪应在与进餐一致的时间服用。
