【药物名称】
通用名：塞来昔布
商品名：西乐葆
英文名：celecoxib
汉语拼音：sailaixibujiaonang
【成分】 本药为口服硬胶囊，除活性成分外，尚含有一水乳糖、十二烷基硫酸钠、聚乙烯吡咯烷酮、羟甲基纤维素钠和硬脂酸镁。
【性状】 胶囊剂，内容物为白色粉末。
【适 应 症】 急性期或慢性期骨关节炎和类风湿关节炎的症状和体征。
【规格】硬胶囊：200mg
【用法用量】 骨关节炎和类风湿关节炎，根据个体情况决定本品治疗的最低剂量。进食的时间对此使用剂量没有影响。关节炎类：本品缓解骨关节炎的症状和体征推荐剂量为200mg，每日一次口服或100mg每日两次口服。类风湿关节炎：本品缓解类风湿关节炎的症状和体征推荐剂量为100mg至200mg，每日两次。家族性腺瘤息肉（FAP）：FAP患者在接收本品治疗时，应继续其常规的治疗。用于FAP患者减少腺瘤性结直肠息肉数目治疗时，推荐剂量为400mg，每日两次，与食物同服。肝功能受损患者：中度肝功能损害患者的推荐剂量约为常规剂量的50％。
【不良反应】 过敏反应，常见的表现为皮疹、瘙痒、荨麻疹等，严重者出现皮肤-黏膜-眼综合症、中毒性表皮坏死溶解、剥落性皮炎等。消化道不良反应有腹痛、腹泻、消化不良、腹胀、恶心等，严重不良反应则包括症状性溃疡、胃肠出血、胃穿孔。神经系统反应有头痛、头晕、嗜睡；水钠潴留，可出现下肢水肿、血压升高。心血管系统发硬包括心肌梗死及脑血管病。肝损害，丙氨酸氨基转移酶、门冬氨酸氨基转移酶升高。老年病人、原有心肾肝病变和同时服用多种药物的病人易出现肾功能损害。
【禁 忌】 本品禁用于对塞来昔布过敏者。本品不可用于已知对磺胺过敏者。临床研究中哮喘病人服用西乐葆后未发生支气管痉挛。但由于未在阿司匹林或其他非甾类抗炎药诱发哮喘，荨麻疹或急性鼻炎的患者中评估西乐葆，因此，尚未有研究资料以前，此类病人应避免服用西乐葆。
【注意事项】 对本产品中任何成份过敏者，已知对磺胺过敏者禁用。塞来昔布含有磺胺基团，临床研究中哮喘病人服用西乐葆后未发生支气管痉挛。但由于未在阿司匹林或其他非甾体抗炎药诱发哮喘、荨麻疹或急性鼻炎的患者中评估西乐葆，因此，尚未有研究资料以前，此类病人应避免服用西乐葆。妊娠期：没有关于妊娠期应用西乐葆的资料，只有潜在益处大于对胎儿的危害时，妊娠期妇女才可以考虑用西乐葆治疗。哺乳期：因没有在人体中进行类似研究，故西乐葆不应用于哺乳期妇女。
【药物相互作用】 本品因主要经细胞色素P450CYP2C9代谢，故细胞色素P450 2C9抑制剂氟康唑能抑制本品代谢，而使其血药浓度增高约1倍。抗酸剂降低本品的吸收。塞来昔布可与氨甲喋呤、酮康唑、抗酸剂（铝剂和镁剂）、苯妥英、格列苯脲、甲苯磺丁脲联合使用。在西乐葆和华法令或其他类似药物联合应用的头几天，或西乐葆的剂量改变后数天内，应密切监测其抗凝血作用。
【药理毒理】 塞来昔布是一种新一代的化合物，具有独特的作用机制即特异性地抑制环氧化酶-2（COX-2）。炎症刺激可诱导COX-2生成，因而导致炎性前列腺素类物质的合成和聚积，尤其是前列腺素E2，引起炎症、水肿和疼痛。塞来昔布可通过抑制COX-2阻止炎性前列腺素类物质的产生，达到抗炎、镇痛及退热作用。
【药 动 学】 空腹给药的塞来昔布吸收良好，约2～3小时达到血浆峰浓度，胶囊口服后的生物利用度为口服混悬后生物利用度的99%(混悬液为口服利用的最佳剂型)。在整个治疗剂量范围内，塞来昔布具有线性、且与剂量成正比的药代动力学特征。本药的血浆蛋白结合率与浓度无关，在治疗血浆浓度时，血浆蛋白结合率约为97%。药物在血中并不是优先与红细胞结合。与进食(高脂食物)同时给药，则本药的延迟吸收，Tmax延至4个小时，生物利用度增加约20%。健康受试者每日1次或分2次口服400mg本品后其生物利用度相同。而在骨关节炎患者，每日1次或分2次口服200mg本品后，其临床疗效及安全性相当。代夂和要通过细胞色素P450-CYP2C9。原形药具有药理活性，循环中其主要代谢产物未测得COX-1和COX-2抑制活性。本品的清除主要通过肝脏进行，少于1%剂量的药物以原形从尿中排出。多剂服药后清除半衰期为8～12小时，清除率约为500mL/分。连续给药5天内达到其稳态分布容积均值，约为500L/70kg，表明塞来昔布在组织中的广泛分布。临床前研究表明本药可通过血脑屏障。
【批准文号】 注册证号BH20050351
【生产企业】 Pfizer Pharmaceuticals LLC(PPLLC)
【贮藏/有效期】 有效期2年。
Celebrex - a drug of choice in the treatment of osteoarthritis
Each doctor should keep in mind that all non-steroidal anti-inflammatory drugs (NSAID's) negatively affect cartilage and aggravate the course of osteoarthrosis.
That is why The European League Against Rheumatism suggests that the treatment of osteoarthrosis should be started with indication of analgesic agents, and NSAID's should be administered only in low therapeutic doses for a short period of time.
However, it is commonly known that a lot of patients with osteoarthrosis suffer from persistent pain and inflammatory syndrome which require the application of NSAID's. For this category of patients the application of selective COX-2 inhibitors are the most preferable and worthwhile.
Celebrex - a drug for treatment of osteoarthritis
Selective inhibitors of cyclooxygenase type 2 do not exert negative effects on cartilage and some of them like Celebrex (Celecoxib) contributes to increase of glycosaminoglycans synthesis as well possess a positive influence on the course of the knee joints osteoasthrosis. 2-years placebo controlled trial proved a high effectiveness of Celebrex in management of pain, stiffness and inflammation. The effects of Celebrex are comparable with glucosamine, chondroitin sulfate or their combination. Since cyclooxygenase is involved in the activation of osteoclasts, selective inhibitors of cyclooxygenase type 2 belongs to a first line treatment of patients with osteoporosis or with a risk factor for osteoporosis development.
In spite of its advantages, Celebrex may have some negative effects. Like other NSAID medication, Celebrex could increase the chance of having a heart attack or stroke, possibly resulting in death. The risk is greater if you have heart disease or use NSAIDs for a long time. It's important to discuss the risks and benefits of using Celebrex with your doctor and to use the lowest effective dose for the shortest amount of time possible.
Although Celebrex is easy on the stomach, it still poses some degree of risk-especially if you've had a stomach ulcer or gastrointestinal bleeding in the past. All NSAIDs, including Celebrex, can cause serious-and even life-threatening-ulcers and bleeding in the stomach and intestines. These side effects can happen without symptoms and may occur at any time during treatment. If you've ever had ulcers or stomach bleeding, make sure the doctor is aware of it. And be sure to alert the doctor if you develop any digestive problems or notice a change in your bowel movement (such as blood in the stool or black, sticky stools).
Celebrex may cause serious skin reactions such as Stevens-Johnson syndrome (marked by blisters of the mouth, eyes, and skin) and toxic epidermal necrolysis (marked by large patches of red, peeling skin). If you have a skin reaction, you should stop taking this drug and seek medical attention immediately.
Celebrex has been known to cause kidney or liver problems, particularly in people with an existing condition. If you have such a disorder, take Celebrex with caution. If you develop symptoms of liver poisoning stop taking the drug and see your doctor immediately. Warning signs include nausea, fatigue, itching, yellowish skin, pain in the right side of the stomach, and flu-like symptoms.