近日，美国食品和药物管理局（FDA）已批准其产品ZYFLO CR™（齐留通）缓释片用于治疗哮喘， ZYFLO CR™提供每日两次，延长释放剂量。
ZYFLO CR™和ZYFLO®（齐留通片剂）是唯一用于预防和长期治疗成人和12岁及以上儿童哮喘的白三烯合成抑制剂。 ZYFLO CR™和ZYFLO®不适用于急性哮喘发作时逆转支气管痉挛，但可在哮喘急性发作期间继续使用。
批准日期：2007年5月31日 公司：Chiesi USA, Inc
ZYFLO CR（齐留通[zileuton]）缓释片,供口服使用
最初的美国批准：1996年
作用机制
Zileuton是5-脂氧合酶的抑制剂，因此抑制白三烯（LTB4，LTC4，LTD4和LTE4）的形成。R（+）和S（ - ）对映体都在体外和体内系统中作为5-脂氧合酶抑制剂具有药理学活性。白三烯是诱导许多生物效应的物质，包括中性粒细胞和嗜酸性粒细胞迁移的增加，中性粒细胞和单核细胞聚集，白细胞粘附，毛细血管通透性增加和平滑肌收缩。这些作用导致哮喘患者气道中的炎症，水肿，粘液分泌和支气管收缩。LTB4是中性粒细胞和嗜酸性粒细胞的化学引诱物，半胱氨酰白三烯（LTC4，LTD4，LTE4）可以在许多生物液体中测量，包括来自哮喘患者的支气管肺泡灌洗液（BALF），血液，尿液和痰液。
Zileuton是几种物种中体外LTB4形成的口服活性抑制剂，包括小鼠，大鼠，兔，狗，绵羊和猴子。 Zileuton抑制花生四烯酸诱导的小鼠耳水肿，小鼠响应聚丙烯酰胺凝胶的中性粒细胞迁移，以及嗜酸性粒细胞迁移到抗原攻击的绵羊的肺中。在过敏性炎症的小鼠模型中，齐留通抑制中性粒细胞和嗜酸性粒细胞流入，降低BALF中多种细胞因子的水平，并降低血清IgE水平。Zileuton在豚鼠和人类呼吸道中抑制体外白三烯依赖性平滑肌收缩。该化合物抑制抗原和花生四烯酸激发的豚鼠中白三烯依赖性支气管痉挛。在抗原攻击的绵羊中，齐留通抑制晚期支气管收缩和气道高反应性。这些发现的临床相关性尚不清楚。
适应症和用法
ZYFLO CR是一种白三烯合成抑制剂，适用于成人和12岁及以上儿童的哮喘的预防和慢性治疗。
不要使用ZYFLO CR治疗急性哮喘发作。
剂量和给药
成人和12岁及以上的儿童：推荐剂量的ZYFLO CR是每天两次600毫克缓释片，早晨和晚餐后一小时内，每日总剂量为2400毫克。
监测：在开始ZYFLO CR之前评估肝功能酶并在治疗期间定期监测。
剂量形式和强度
延长释放片剂：600毫克。
禁忌症
活动性肝病或持续性肝功能酶升高≥正常上限的3倍。
对齐留通或ZYFLO CR任何成分的过敏反应史。
警告和注意事项
肝毒性：ZYFLO CR可能出现一种或多种肝功能酶和胆红素的升高。在开始ZYFLO CR之前评估肝功能酶，前3个月每月评估一次，第一年剩余时间每2-3个月评估一次，之后定期评估。对于摄入大量酒精和/或有肝病史的患者，请谨慎使用ZYFLO CR。
神经精神事件：ZYFLO CR可能发生神经精神事件，包括睡眠障碍和行为改变。指导患者警惕神经精神事件。如果发生此类事件，评估ZYFLO CR持续治疗的风险和益处。
不良反应
最常见的不良反应（≥5％）包括：鼻窦炎，恶心和咽喉疼痛。
要报告疑似不良反应，请致电1-888-661-9260联系Chiesi USA，Inc。或致电1-800-FDA-1088或www.fda.gov/medwatch联系FDA。
药物相互作用
齐留通增加茶碱水平。降低茶碱的剂量和监测水平。
齐留通增加华法林水平。监测凝血酶原时间并相应调整华法林剂量。
齐留通增加普萘洛尔水平和β-受体阻滞剂活性。适当监控。
用于特定人群
肝功能损害：ZYFLO CR禁用于活动性肝病患者和肝功能酶升高≥3倍正常上限的患者。
包装提供/存储和处理
ZYFLO CR（齐留通）缓释片一侧贴有“CT2”; 它们有120片（NDC 10122-902-12）和20片（NDC 10122-902-20）瓶装样品。
储存温度在20到25°C（68-77ºF）之间; 允许偏移15-30°C（59-86°F）[见USP受控室温]。 避光。
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9bc08d7b-13da-444f-ac8a-3714a05176cc 
ZYFLO CR (zileuton) helps control asthma symptoms
About ZYFLO CR (zileuton)
ZYFLO CR is a medicine that is used to prevent asthma attacks and for long-term management of asthma in adults and children 12 years of age and older. ZYFLO CR blocks the production of leukotrienes. Leukotrienes are substances that may contribute to your asthma.
ZYFLO CR is not a rescue medicine (it is not a bronchodilator) and should not be used if you need relief right away for an asthma attack.
Important Patient Safety Information
Do not take ZYFLO CR if you have active liver disease, repeated blood tests showing elevated liver enzymes (substances released by the liver) or have ever had an allergic reaction to ZYFLO CR or any of the ingredients in ZYFLO CR.
ZYFLO CR may not be right for you. Tell your health care provider if you have ever had liver problems, including hepatitis, jaundice (yellow eyes or skin), or dark urine.
Tell your health care provider how much and how often you drink alcohol.
Tell your health care provider if you are pregnant or planning to become pregnant. It is not known if ZYFLO CR will harm your unborn baby. Do not take ZYFLO CR during pregnancy unless you and your health care provider decide that taking the medicine is more important than the possible risk to your unborn baby. It is not known if ZYFLO CR passes into your breast milk. You and your health care provider should decide if you will take ZYFLO CR or breastfeed. You should not do both.
Tell your health care provider if you have difficulty swallowing pills and about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.
ZYFLO CR can cause serious side effects including liver problems. Liver function enzymes and bilirubin can increase while taking ZYFLO CR and severe liver injury can occur. Have your blood tests done as ordered to check your liver enzymes.
In addition, tell your healthcare provider if you have any sleep problems or changes in behavior while taking ZYFLO CR.
Tell your health care provider right away if you get any of the following signs or symptoms: pain on the right side of your abdomen (stomach area), nausea, tiredness, lack of energy, itching, yellow skin or yellow color in the whites of your eyes, dark urine, or “flu-like” symptoms.
Some of the most common side effects are nose and throat irritation, sinusitis, upper respiratory infection, throat pain, headache, muscle aches, nausea, and diarrhea.
Allergic reactions can happen while taking ZYFLO CR. Tell your health care provider right away if you get any of the following signs or symptoms: rash or hives.
Tell your health care provider if you have any new or unusual symptoms that bother you or do not go away while taking ZYFLO CR.
These are not all of the possible side effects of ZYFLO CR. For more information, ask your health care provider or pharmacist.
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch or call 1-800-FDA-1088.