Kloner R A, Zusman R M
University of Southern California, The Heart Institute of the Hospital of the Good Samaritan, Los Angeles 90017, USA.
Am J Cardiol. 1999 Sep 9;84(5B):11N-17N. doi: 10.1016/s0002-9149(99)00114-9.
Sildenafil citrate is the first orally active therapy proved to be effective and safe treatment for erectile dysfunction (ED). Because men with cardiovascular disease are at increased risk of developing ED, and because ED and cardiovascular disease share important risk factors, attention has focused recently on the use of sildenafil in these men. When used in combination with nitroglycerin and other nitric oxide (NO) donors, sildenafil may potentiate major drops in blood pressure. Use of nitrate antianginal agents are an absolute contraindication to sildenafil use. In normotensive men and in men receiving antihypertensive medications evaluated in Phase II/III clinical trials, sildenafil use at the recommended doses (25-100 mg 1 hour before sexual intercourse and no more than once daily) was associated with modest, transient reductions in blood pressure and negligible effects on heart rate. In a more recent study, sildenafil was well tolerated in patients receiving antihypertensive medications and was not associated with major decreases in blood pressure. From the time of its approval in the United States in March 1998 through mid-November 1998, with approximately 6 million prescriptions written, 130 deaths were reported by the US Food and Drug Administration (FDA). Seventy-seven of the men who died had documented cardiovascular events. Sixteen men took or were administered nitroglycerin or an organic nitrate; 3 others had nitroglycerin in their possession. Physician prescribing guidelines issued by the American College of Cardiology/American Heart Association (ACC/AHA) recommend caution when prescribing sildenafil to men with certain cardiovascular conditions, liver or kidney disease, and to those taking medications that may prolong sildenafil's half-life (e.g., erythromycin or cimetidine). Those with known or suspected coronary artery disease may benefit from an exercise test to determine whether resumption of sexual activity with use of sildenafil is likely to be associated with an increased risk of myocardial ischemia.
枸橼酸西地那非是首个经证实对勃起功能障碍（ED）有效且安全的口服活性治疗药物。由于患有心血管疾病的男性发生ED的风险增加，且ED和心血管疾病有共同的重要危险因素，因此近来人们的注意力集中在这些男性使用西地那非的情况上。当与硝酸甘油及其他一氧化氮（NO）供体合用时，西地那非可能会使血压大幅下降。使用硝酸盐类抗心绞痛药物是使用西地那非的绝对禁忌证。在血压正常的男性以及在II/III期临床试验中接受抗高血压药物治疗的男性中，按推荐剂量（性交前1小时服用25 - 100毫克，每日不超过1次）使用西地那非会导致血压适度、短暂下降，对心率的影响可忽略不计。在最近一项研究中，接受抗高血压药物治疗的患者对西地那非耐受性良好，且与血压大幅下降无关。从1998年3月在美国获批至1998年11月中旬，开出了约600万张处方，美国食品药品监督管理局（FDA）报告了130例死亡病例。死亡的男性中有77例记录有心血管事件。16名男性服用或被给予了硝酸甘油或有机硝酸盐；另有3人身上带有硝酸甘油。美国心脏病学会/美国心脏协会（ACC/AHA）发布的医生处方指南建议，给患有某些心血管疾病、肝脏或肾脏疾病的男性以及正在服用可能延长西地那非半衰期的药物（如红霉素或西咪替丁）的男性开西地那非时要谨慎。已知或疑似患有冠状动脉疾病的患者可能会从运动试验中受益，以确定使用西地那非恢复性活动是否可能增加心肌缺血的风险。
