英文药名:Zyflo(Zileuton A-64077、Leutrol)
中文药名;齐留通片剂
药品介绍
齐留通副作用;别名:Zyflo、A-64077、Leutrol;齐留通适应症: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。;齐留通药理学作用: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。
分类名称 一级分类:呼吸系统药物 二级分类:平喘药物 三级分类:抗炎性平喘药 药品英文名 Zileuton 药品别名 Zyflo、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。 专家点评 在一多剂量的临床Ⅰ期试验中,健康者服用本品600mg/次,4次/d,共14天,可减少全血中LTB4生成并回到对照组水平。 在多中心Ⅱ期临床试验中,轻中度的溃疡性结肠炎患者口服本品800mg/次,2次/d,共4周有较好的疗效。单次口服本品800mg可保护由抗原经激发致敏的患者不出现严重充血反应。在一双盲、安慰剂对照试验中、轻度至中度哮喘患者服用本品600mg/次,4次/d,共4周,治疗组患者与安慰剂组比较有显著的改善,表现为FEV1提高13.4%,早晨呼吸量峰值提高了10%,β激动剂的用量减少了24%,总的症状改善率提高了37%。
Zyflo Generic Name: zileuton (Oral route) zye-LOO-ton Commonly used brand name(s): In the U.S. Zyflo Zyflo CR
Available Dosage Forms: Tablet Tablet, Extended Release Therapeutic Class: Anti-Inflammatory Pharmacologic Class: Leukotriene Pathway Inhibitor ------------------------------------------------------- Uses For Zyflo Zileuton is used by patients with mild-to-moderate chronic asthma to decrease the symptoms of asthma and the number of acute asthma attacks. However, this medicine should not be taken to relieve an asthma attack that has already started.
This medicine is available only with your doctor's prescription. Zileuton immediate-release tablets (Zyflo(R)) were withdrawn from the U. S. market by Critical Therapeutics on February 12, 2008. The extended-release formulation of zileuton (Zyflo CR(R)), also manufactured by Critical Therapeutics, Inc, is still available. Before Using Zyflo In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered: Allergies Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully. Pediatric Appropriate studies have not been performed on the relationship of age to the effects of zileuton in children younger than 12 years of age. Safety and efficacy have not been established. Geriatric Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of zileuton in the elderly. However, elderly patients are more likely to have age-related liver disease, and this medicine should not be used in patients with this condition. Pregnancy All Trimesters Pregnancy Category:C Explanation:Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women. Breast Feeding There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding. Interactions with Medicines Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take. Dihydroergotamine Ergoloid Mesylates Ergonovine Ergotamine Methylergonovine Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines. Astemizole Eltrombopag Pimozide Terfenadine Theophylline Tizanidine Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines. Propranolol Warfarin Interactions with Food/Tobacco/Alcohol Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
Other Medical Problems The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially: Alcohol use, severe or Liver disease, history of—Use with caution. The chance of serious side effects may be increased. Liver disease, active—This medicine should not be used with this condition. ------------------------------------------------------- Proper Use of zileuton This section provides information on the proper use of a number of products that contain zileuton. It may not be specific to Zyflo. Please read with care.
Zileuton is used to prevent asthma attacks. It is not used to relieve an attack that has already started. For relief of an asthma attack that has already started, you should use another inhaled medicine that works quickly. If you have any questions about this, check with your doctor.
Swallow the extended-release tablet whole. Do not crush, break, or chew it.
To work properly, zileuton must be taken every day at regularly spaced times, even if your asthma seems better.
Dosing The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
For oral dosage form (extended-release tablets): For asthma prevention: Adults and children 12 years of age and older—Two 600 milligram (mg) tablets two times a day, within one hour after morning and evening meals. Children up to 12 years of age—Use and dose must be determined by your doctor. Missed Dose If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing. Keep out of the reach of children. Do not keep outdated medicine or medicine no longer needed. Ask your healthcare professional how you should dispose of any medicine you do not use. ------------------------------------------------------- Precautions While Using Zyflo It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if the medicine is working properly and to check for unwanted effects. Check with your doctor if you are using more inhalations (puffs) than usual of your inhaled bronchodilator to relieve an acute asthma attack. You may be taking other medicines for asthma along with zileuton. Do not stop taking or reduce the dose of the other medicines, even if your asthma seems better, unless you are told to do so by your doctor. You should limit the amount of alcohol you drink while you are taking this medicine. This medicine may cause some people to be agitated, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed and have problems with sleep. If you or your caregiver notice any of these side effects, tell your doctor right away. ------------------------------------------------------- Zyflo Side Effects Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention. Check with your doctor immediately if any of the following side effects occur:
Rare Flu-like symptoms itching right upper stomach pain unusual tiredness or weakness yellow eyes or skin Incidence not known Attack, assault, or force attempts at killing oneself discouragement dry mouth fear or nervousness feeling sad or empty hyperventilation irregular heartbeats irritability lack of appetite loss of interest or pleasure restlessness seeing, hearing, or feeling things that are not there shakiness in the legs, arms, hands, or feet shortness of breath sleeplessness tiredness trembling or shaking of the hands or feet trouble with concentrating trouble with sleeping unable to sleep Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them: More common Cough fever headache nausea pain or tenderness around the eyes and cheekbones stuffy or runny nose tightness of the chest or wheezing troubled breathing upset stomach Less common Abdominal or stomach pain sore throat weakness Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088. The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you. The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products. --------------------------------------------------------------- 原产地英文商品名: ZYFLO 600mg/filmtab 120filmtabs/bottle 原产地英文药品名: ZILEUTON 原产地英文化合物名称: Urea, N-(1-Benzo[b]thien-2-ylethyl)-N-hydroxy- 中文参考商品译名: ZYFLO 600毫克/膜片 120片/瓶 中文参考药品译名: 齐留通 生产厂家中文参考译名: CORNERSTONE THERAPEUTICS INC. 生产厂家英文名: CORNERSTONE THERAPEUTICS INC.
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