※ 引述《vic0919 (阿翔)》之铭言： : to Basmey~如果是作业我也不需要上来提问!! : 就是因为看到一篇期刊 : 但文中只提到不建议使用 : 而我想要知道其机转 : 才会发问~ : http://www.medscape.com/viewarticle/582385_print : 小朋友... : 科科 : 原来药学界也有爱嘴炮的!! 首先，要先跟原po道歉...我本来以为你真的是来问报告的 XD 再者，恕我懒惰，仅引用UpToDate ONLINE 17.2 《NSAIDs and acetaminophen: Effects on hypertension》 Last literature review version 17.2: 五月 2009 This topic last updated: 十月 8, 2008 All NSAIDs in doses adequate to reduce inflammation and pain can increase blood pressure in both normotensive and hypertensive people [1]. The average rise in blood pressure is 3/2 mmHg but varies considerably [2]. NSAID use may reduce the effect of all anti-hypertensive drugs except calcium channel blockers [3]. The pro-hypertensive effect likely involves inhibition of the cyclooxygenase-2 (COX-2) enzyme in the kidneys, which reduces sodium excretion and increases intravascular volume [3]. There is a common misconception that non-selective NSAIDs (such as naproxen) cause hypertension, but selective NSAIDs (such as refocoxib), which spare the COX-1 enzyme, do not. In fact, all NSAIDs must block COX-2 to reduce inflammation and pain; therefore, all may raise blood pressure. The pro-hypertensive effect is dose-dependent [3]. [注] Reference： 1：Warner TD; Mitchell JA. COX-2 selectivity alone does not define the cardiovascular risks associated with non-steroidal anti-inflammatory drugs. Lancet. 2008 Jan 19;371(9608):270-3. 2：Grover SA; Coupal L; Zowall H. Treating osteoarthritis with cyclooxygenase-2 -specific inhibitors: what are the benefits of avoiding blood pressure destabilization? Hypertension. 2005 Jan;45(1):92-7. Epub 2004 Nov 15. 3：White WB. Cardiovascular effects of the cyclooxygenase inhibitors. Hypertension. 2007 Mar;49(3):408-18. Epub 2007 Jan 29. 《COX-2 selective inhibitors: Adverse cardiovascular effects》 Last literature review version 17.2: 五月 2009 | This topic last updated: 一月 21, 2009 在"Hypertension"这一段 NSAIDs, both nonselective and COX-2-selective, can raise the blood pressure. A 2005 meta-analysis of 19 randomized trials of COX-2 selective agents involving 45,461 patients noted a statistically significant effect on the incidence of hypertension in clinical trials only among those who received rofecoxib when compared to placebo (RR 2.63, 95% CI 1.42-4.85) [36]. The weighted mean difference in blood pressure attributed to use of a COX-2 selective agent when compared to placebo was greatest for rofecoxib; a 5.66 mmHg increase in systolic blood pressure compared to placebo. Changes in systolic blood pressure were less for celecoxib, 2.6 mmHg. However, celecoxib was associated with an increase in diastolic blood pressure of 0.99 mmHg, whereas rofecoxib was not. The following observations from selected studies are illustrative: * The effects of celecoxib and rofecoxib were evaluated in a study of 810 elderly patients with osteoarthritis who were taking antihypertensive drugs [37]. At six weeks, rofecoxib produced a mean elevation in systolic pressure of 2.3 mmHg, whereas celecoxib was associated with no change (-0.5 mmHg). An increase in risk of worsening hypertension with rofecoxib but not celecoxib was also noted in a survey-based postmarketing study [38]. * A retrospective case-control study evaluating the frequency of new onset hypertension in elderly NSAID users [39]. The relative risk with rofecoxib was significantly increased compared to celecoxib (odds ratio [OR] 1.6), a nonselective NSAID (OR 1.4), or no NSAID (OR 1.6). Thus, patients may develop hypertension or experience worsening of established high blood pressure when treated long-term with a COX-2 selective agent. This effect appears to have occurred most frequently with rofecoxib. Monitoring of blood pressure in patients treated with coxibs is recommended. Their use in patients with poorly controlled hypertension is discouraged. ~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~ [注] Reference： 36：Aw TJ; Haas SJ; Liew D; Krum H. Meta-analysis of cyclooxygenase-2 inhibitors and their effects on blood pressure. Arch Intern Med 2005 Mar 14;165(5):490-6. Epub 2005 Feb 14. 37：Whelton A; Fort JG; Puma JA; Normandin D; Bello AE; Verburg KM Cyclooxygenase-2--specific inhibitors and cardiorenal function: a randomized, controlled trial of celecoxib and rofecoxib in older hypertensive osteoarthritis patients. Am J Ther 2001 Mar-Apr;8(2):85-95. 38：Wolfe F; Zhao S; Pettitt D. Blood pressure destabilization and edema among 8538 users of celecoxib, rofecoxib, and nonselective nonsteroidal antiinflammatory drugs (NSAID) and nonusers of NSAID receiving ordinary clinical care. Rheumatol 2004 Jun;31(6):1143-51. 39：Solomon DH; Schneeweiss S; Levin R; Avorn J. Relationship between COX-2 specific inhibitors and hypertension. Hypertension 2004 Aug;44(2):140-5. Epub 2004 Jun 28. ※ 编辑: sharkimage 来自: 122.121.156.179 (09/12 16:18) ※ 编辑: sharkimage 来自: 122.121.156.179 (09/12 16:23)