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近日，由Shire Pharmac公司研发的LIALDA(mesalamine tablets)已获FDA的批准，作为第一种诱导成人轻中度溃疡性结肠炎（UC）缓解的每日一次治疗。
Lialda每日一次给药是片剂MMX技术的结果。这种递送系统使用pH依赖性、抗胃的涂层来延迟药物的释放，直到片剂到达结肠。
UC是一种慢性炎症性自身免疫性疾病，在大肠内产生溃疡或溃疡。这种疾病通常在15到30岁之间被诊断出来，并且经常表现出严重的腹痛、经常或不可控制的血性腹泻、疲劳和体重减轻等症状。情况是这样的。
批准日期：2017年5月12日 公司：Shire US Inc
LIALDA（美沙拉[mesalamine]）缓释片，口服使用
首次美国批准：1987
近期重大变化
警告和注意事项：05／2018
作用机理
美沙拉明的作用机制尚不完全清楚，但似乎对结肠上皮细胞有局部抗炎作用。慢性炎症性肠病患者通过环氧合酶和脂氧合酶途径产生花生四烯酸代谢产物的粘膜量增加，而甲胺嘧啶可能通过阻断环氧合酶和抑制前列腺素产物来减轻炎症。结肠中的离子。
三聚氰胺具有抑制核因子κB（NFκB）的激活，从而抑制关键促炎细胞因子的生产的潜力。已经提出PPARγ核受体（过氧化物酶体增殖物激活受体的γ形式）表达降低可能与溃疡性结肠炎有关。有证据表明，美沙拉明通过直接激活结肠/直肠上皮中的PPARγ受体产生药效学作用。
适应症及用法
LIALDA是一种局部起作用的5-氨基水杨酸（5-ASA），用于诱导有活动、轻度到中度溃疡性结肠炎的成人缓解，并维持溃疡性结肠炎的缓解。
剂量与给药
为了诱导缓解活动，轻度至中度溃疡性结肠炎，两到四个1.2克片每天服用一次食物。
为了维持溃疡性结肠炎的缓解，两片1.2克片每天服用一次。
剂型和强度
缓释片：1.2g
禁忌症
已知对水杨酸盐或氨基水杨酸盐或利拉达片的任何成分过敏的患者。
警告和注意事项
肾损害可能发生。在治疗开始时评估肾功能，并在治疗期间定期评估肾功能。
报道了美沙拉胺引起的急性不耐受综合征。密切观察患者在治疗过程中的症状恶化。
在治疗柳氮磺吡啶过敏患者时要慎重。
报道了美沙拉胺引起的心脏超敏反应（心肌炎和心包炎）。
肝衰竭已报告在预先存在的肝脏疾病的患者。治疗肝病时要慎重。
上消化道梗阻可能延迟行动的开始。
预先存在皮肤状况的患者报告了更严重的光敏反应。
采用液相色谱-电化学检测法检测尿中正常肾上腺素时，使用美沙拉明可能导致检测结果虚假升高。
不良反应
最常见的不良反应（发生率≥2%）是溃疡性结肠炎、头痛、肠胃胀气、肝功能异常和腹痛。
为了报告可疑的不良反应，联系SHIRAE美国公司在1-800至823-2088或FDA在1-800 -FDA-1088或www. FDA.GOV/MeWAT
药物相互作用
肾毒性药物包括非甾体抗炎药：肾反应已被报道。
硫唑嘌呤或6-巯基嘌呤：血液病已有报道。
在特定人群中的使用
肾损害：使用LalalDA谨慎的肾脏病史患者。
护理妇女：在给护理妇女时应谨慎。
老年患者：监测老年患者的血细胞计数。
包装供应/储存和搬运
LIALDA可用作红棕色椭球膜包衣的含有1.2克美沙拉明的延迟释放片，并在一侧用S476压印去压片。
NDC54092-76－12 HDPE瓶，具有防儿童关闭的120种延迟释放片。
在室温下储存15°C至25°C（59°F至77°F）；准许漂移到30°C（86°F）。
参见USP控制的室温。
完整资料附件：https://www.dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3098a080-be86-4265-9818-7fc4beab77b7
LIALDA(mesalamine) delayed-release tablets, for oral use
Important Safety Information
Lialda is contraindicated in patients with known hypersensitivity to salicylates or aminosalicylates or to any of the ingredients of Lialda.
Renal impairment, including minimal change nephropathy, acute and chronic interstitial nephritis, and, rarely, renal failure, has been reported with products such as Lialda that contain mesalamine or are converted to mesalamine. It is recommended that patients have an eva luation of renal function prior to initiating use of Lialda and periodically while on therapy. Exercise caution when using Lialda in patients with known renal dysfunction or a history of renal disease.
Mesalamine has been associated with an acute intolerance syndrome (3% of patients in clinical trials with mesalamine or sulfasalazine) that may be difficult to distinguish from an exacerbation of ulcerative colitis. Symptoms include cramping, acute abdominal pain and bloody diarrhea, and sometimes fever, headache, and rash. Observe patients closely for worsening of these symptoms while on treatment. If acute intolerance syndrome is suspected, promptly discontinue treatment with Lialda.
Some patients who have experienced a hypersensitivity reaction to sulfasalazine may have a similar reaction to Lialda or compounds that contain or are converted to mesalamine. Mesalamine-induced cardiac hypersensitivity reactions (myocarditis and pericarditis) have been reported with Lialda and other mesalamine-containing medications. Caution should be taken when prescribing Lialda to patients with conditions predisposing them to the development of myocarditis or pericarditis.
There have been reports of hepatic failure in patients with pre-existing liver disease who have been administered mesalamine. Caution should be exercised when administering Lialda to patients with liver disease.
Pyloric stenosis or other organic or functional obstruction in the upper gastrointestinal tract may cause prolonged gastric retention of Lialda, which would delay mesalamine release in the colon.
Use of mesalamine may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection because of the similarity in the chromatograms of normetanephrine and mesalamine's main metabolite, N-acetylaminosalicylic acid (N-Ac-5-ASA). An alternative, selective assay for normetanephrine should be considered.
In clinical trials, the most common adverse reactions (incidence ≥2%) were ulcerative colitis, headache, flatulence, liver function test abnormality, and abdominal pain. Pancreatitis occurred in <1% of patients and resulted in discontinuation of therapy with Lialda.
The concurrent use of mesalamine with known nephrotoxic agents, including non-steroidal anti-inflammatory drugs (NSAIDs) may increase the risk of renal reactions. The concurrent use of mesalamine with azathioprine or 6-mercaptopurine can increase the potential for blood disorders.
Safety and effectiveness of Lialda in pediatric patients have not been established.
Indication
Lialda is indicated for the induction of remission in patients with active, mild to moderate ulcerative colitis (UC) and for the maintenance of remission of UC.
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