部份中文ZYFLO资料（仅供参考）
药品英文名
Zileuton
药品别名
Zyflo、ZYFLO CR、A-64077、Leutrol
药物剂型
片剂：每片含本品600mg。
药理作用
本品为5-脂氧合酶抑制剂，在体内和体外的药理作用均与白三烯的形成有关，剂量依赖性地抑制5-脂氧合酶所催化的生物合成，IC50＝7μmol/L。在60μmol/L浓度的花生四烯酸下的IC50值为9nmol/L。本品还抑制白三烯LTB4的产生，对各种类型细胞中白三烯的产生都有抑制作用。本品对过氧化物酶、巨细胞组胺释放酶或磷脂酶A2的活性均无影响。本品在豚鼠的体内和体外实验中显示出显著的抗过敏活性。
药动学
口服吸收迅速，给药剂量600mg时，全身平均血药浓度为19.2(μg·h)/ml，tmax为1.7小时，Cmax为4.98μg/ml。绝对生物利用度尚未知。血浆浓度同剂量呈比例，稳态水平可由单剂量药动数据推知，半衰期为2.5小时。清除率为7.0ml/(min·kg)，主要代谢途径为N-羟基脲基团的葡萄糖醛酸化。
适应证
用于成人以及12周岁以上的儿童哮喘的预防和慢性哮喘的治疗。
注意事项
本品作用与白三烯受体拮抗药作用相似，但是长期使用可致肝功能改变，转氨酶升高。
不良反应
主要的不良反应有头痛、疼痛(非特异的)、腰痛、无力和意外损伤。
用法用量
口服，本品推荐剂量为600mg/次，4次/d，可在用饭时和睡时服用。使用前以及使用中需注意检测肝转氨酶活性。

Zileuton extended-release tablets
Generic Name: zileuton (zye-LOO-ton)
Brand Name: Zyflo CR
Zileuton extended-release tablets are used for:
Preventing asthma attacks. It is also used for long-term treatment of asthma. It may also be used for other conditions as determined by your doctor.
Zileuton extended-release tablets are a leukotriene synthesis inhibitor. It works by blocking the formation of a substance called leukotriene, which helps to decrease certain asthma and allergy symptoms.
Do NOT use zileuton extended-release tablets if:
•you are allergic to any ingredient in zileuton extended-release tablets
•you have liver disease or persistent abnormal liver function tests
•you are taking terfenadine
Contact your doctor or health care provider right away if any of these apply to you.
Before using zileuton extended-release tablets:
Some medical conditions may interact with zileuton extended-release tablets. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:
•if you are pregnant, planning to become pregnant, or are breast-feeding
•if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
•if you have allergies to medicines, foods, or other substances
•if you have a history of liver problems (eg, hepatitis) or symptoms of liver problems (eg, yellowing of the skin or eyes, dark urine)
•if you have a history of mental or mood problems (eg, depression) or suicidal thoughts or actions
•if you drink alcohol
•if you have trouble swallowing tablets
Some MEDICINES MAY INTERACT with zileuton extended-release tablets. Tell your health care provider if you are taking any other medicines, especially any of the following:
•Anticoagulants (eg, warfarin) because the risk of bleeding may be increased
•Azole antifungals (eg, ketoconazole) because they may increase the risk of zileuton extended-release tablets's side effects
•Astemizole, beta-blockers (eg, propranolol), calcium channel blockers (eg, amlodipine), cisapride, cyclosporine, terfenadine, or theophylline because the risk of their side effects may be increased by zileuton extended-release tablets
This may not be a complete list of all interactions that may occur. Ask your health care provider if zileuton extended-release tablets may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.
How to use zileuton extended-release tablets:
Use zileuton extended-release tablets as directed by your doctor. Check the label on the medicine for exact dosing instructions.
•An extra patient leaflet is available with zileuton extended-release tablets. Talk to your pharmacist if you have questions about this information.
•Take zileuton extended-release tablets by mouth within 1 hour after the morning and evening meals, unless your doctor tells you otherwise.
•Swallow zileuton extended-release tablets whole. Do not break, crush, or chew before swallowing.
•Take zileuton extended-release tablets on a regular schedule to get the most benefit from it. Taking zileuton extended-release tablets at the same times each day will help you remember to take it.
•Continue to take zileuton extended-release tablets even if you feel well. Do not miss any doses.
•If you miss a dose of zileuton extended-release tablets, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use zileuton extended-release tablets.
Important safety information:
•Tell your doctor or dentist that you take zileuton extended-release tablets before you receive any medical or dental care, emergency care, or surgery.
•Do NOT take more than the recommended dose or use for longer than prescribed without checking with your doctor.
•It may take a few weeks before you get the full benefit of zileuton extended-release tablets. Do not stop using zileuton extended-release tablets without checking with your doctor.
•Zileuton extended-release tablets will not stop an asthma attack once it has already started. Be sure to carry a short-acting bronchodilator with you at all times to treat any breathing problems that may occur between doses of zileuton extended-release tablets (eg, severe or sudden onset of wheezing or shortness of breath). If you have any questions about which medicines stop asthma attacks, check with your doctor or pharmacist.
•Tell your doctor at once if you notice that your short-acting bronchodilator inhaler does not work as well, if you need to use it more often, or if you have a decrease in your peak flow meter results.
•Contact your doctor or seek medical care right away if you have breathing problems that worsen quickly, or if you use your short-acting bronchodilator and do not get relief.
•Talk with your doctor or pharmacist about all your asthma medicines and how to use them. Do not start, stop, or change the dose of any asthma medicine unless your doctor tells you to.
•Some patients taking zileuton extended-release tablets have developed mental or mood changes, including sleep problems and behavior changes. Contact your doctor immediately if you experience any unusual symptoms while taking zileuton extended-release tablets.
•Lab tests, including liver function, may be performed while you use zileuton extended-release tablets. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.
•Use zileuton extended-release tablets with caution in the ELDERLY; they may be more sensitive to its effects, especially liver problems.
•Zileuton extended-release tablets should not be used in CHILDREN younger than 12 years old; safety and effectiveness in these children have not been confirmed.
•PREGNANCY AND BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using zileuton extended-release tablets while you are pregnant. It is not known if this medicine is found in breast milk. Do not breast-feed while taking zileuton extended-release tablets.
Possible side effects of zileuton extended-release tablets:
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:
Headache; nausea; nose irritation; symptoms of upper respiratory tract infection (eg, cough, mild sore throat, runny or stuffy nose, sneezing); throat pain or irritation.
Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); chest pain; fever, chills, or persistent sore throat; mental or mood changes; sleep problems; symptoms of liver problems (eg, dark urine; flu-like symptoms; pale stools; persistent loss of appetite; right upper stomach pain; unusual nausea, sluggishness, or tiredness; yellowing of the skin or eyes); unusual changes in behavior.
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.