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【通用名称】Montelukast孟鲁司特
【化学名称】[R-（E）-1[[[1-[3[2-（7-氯-2-喹啉基）乙烯基]苯基]-3-（1-羟基-1-甲基乙基）苯基]丙基]硫代]甲基]环丙基乙酸，单纳盐]
【理化性质】白色粉末，易溶于甲醇、乙醇和水，不溶于乙腈，对光敏感。
【药理作用】本品是一种强效的选择性的白三烯D4（LTD4，cysLT1）受体拮抗剂，是新一代非甾体抗炎药物。能选择性抑制气道平滑肌中白三烯多肽的活性，并有效预防和抑制白三烯所导致的血管通透性增加、气道嗜酸粒细胞（EOS）浸润及支气管痉挛，能减少气道因变应原刺激引起的细胞和非细胞性炎症物质，能抑制变应原激发的气道高反应。对二氧化硫、运动和冷空气等刺激及各种变应原如花粉、毛屑等引起的速发相和迟发相炎症反应均有抑制作用。本品与人类气道中的cysLT受体能高度选择性结合，从而阻断白三烯的病理作用。已经证明，吸入LTD4可引起较组胺强1000倍的剂量依赖性支气管收缩。
【药代动力学】健康成人中观察到孟鲁司特的AUC随静脉应用剂量（3.9～18mg）的增大而按比例增加。血浆清除率平均45.5ml/min（2.73L/h），稳态分布容积10.5L，血浆终点半衰期5.1h，平均残留时间3.9h。各项指标在上述研究剂量范围内基本维持恒定。口服孟鲁司特10mg后Cmax男性为385μg/L，女性为350μg/L，用药后Tmax男女分别为3.7丐3.3h。AUC值分别为2441与2270mg?h/L，半衰期为4.9与4.4h，平均吸收时间为3.4与2.6h。口服平均生物利用度为64%，健康成人的血浆清除率平均为45ml/min。口服同位素标记孟鲁司特后86%可从5d的粪便中收集到，仅0.2%出现于尿中，提示其代谢物大部分经胆汁排泄。老年志愿者（平均年龄69.4岁）口服一次孟鲁司特10mg后生物利用度为61%，与青年志愿者相似，故老年患者使用孟鲁司特无需调整剂量。肝、肾功能不全时不影响孟鲁司特的排泄。同时使用茶碱亦不产生药物相互作用。
【适应证】本品适用于成人和儿童哮喘的预防和长期治疗，包括预防白天和夜间的哮喘症状，能够改善慢性气道炎症，改善肺功能，控制哮喘症状，减少必需的β2激动剂用量，治疗对阿司匹林敏感的哮喘患者以及预防运动引起的支气管收缩。
【用法与用量】15岁及15岁以上成人剂量为10mg，qd睡前服用。6～14岁儿童剂量为5mg，qd，睡前服用。该组患者不需再按年龄调整剂量。6岁以下患儿的安全有剂量及用法尚未确定。
【不良反应】顺尔宁的一般耐受性良好，不良反应较轻微，通常不需中止治疗。最常见的不良反应是头痛、偶有腹痛、咳嗽、流感样症状，儿童与成人的发生率相似。
【注意事项】
①口服本品治疗急性哮喘发作的疗效尚未确定，所以口服本品不应该用于治疗急性哮喘发作，应劝告患者准备好必要的急救药品备用。
②虽然合用的吸入皮质类固醇制剂可在医师监督下逐渐减量，但不应骤然使用本品取代吸入或口服皮质类固醇制剂。
③尚未研究本品在妊娠妇女中的应用，只有在十分必要的情况下才在妊娠期间使用。
④尚不清楚本品是否在人体经乳汁排泄，所以在给授乳妇女使用本品时应谨慎。
⑤6岁以下患儿的安全有效剂量及用法尚未研究。
【临床评价】
对成年哮喘的治疗：
多中心研究343例（285例用孟鲁司特，58例用安慰剂）纳入双盲试验。307例（90%）完成治疗，299例（87%）完成安慰剂洗脱（Washout期）。结果表明，与安慰剂相比，孟鲁司特治疗组的FEV1明显改善，必需的β激动剂使用量减少，治疗组的哮喘急性发作次数显著减少。与安慰剂相比，孟鲁司特治疗组的周围血嗜酸粒细胞计数明显减少，又随机选择140例中度运动性哮喘作为研究对象，54例孟鲁司特10mg，qd，56例为安慰剂对照。经12周治疗，结果显示孟鲁司特具有显著的防止由运动诱发的支气管痉挛，疗程虽较长，但并不产生对孟鲁司特的耐受性。终止治疗后2周，孟鲁司特虽未能继续维持其保护作用，亦未证实有运动性支气管痉挛症状的恶化反跳。
对儿童哮喘治疗的试验：
美国及加拿大47个医学中心336例6～14岁儿童哮喘使用孟鲁司特5mg，qd治疗2周后，与对照组相比，其平均晨间FEV1显著改善，且发现孟鲁司特起效迅速（用药1d内），用药期间哮喘症状评分降低、β激动剂使用量减少。孟鲁司特不仅作用快速，且治疗效果能维持稳定。Reiss等报道的孟鲁司特临床观察包括50个医学中心681例慢性哮喘治疗12周（408例孟鲁司特治疗组，孟鲁司特10md/d；273例安慰剂对照），结果显示孟鲁司特对各项哮喘控制指标均有恒定而明显改善，亦未见发生药物耐受性。慢性哮喘治疗的另一重要目标是防止哮喘症状突发恶化，孟鲁司特具有突出的防止症状恶化的效果，可减少31%的复发天数与增加30%的哮喘控制天数。
孟鲁司特治疗哮喘的联合用药的试验：
Laviol-lette等的临床研究观察口服孟鲁司特合并吸入倍氯美松，642例慢性哮喘患者（FEV1为预计值的50%～85%），均为吸入倍氯美松200μg，bid未能完全控制者，随机双盲分成4组：
①孟鲁司特10mg+继续吸入倍氯美松。
②安慰剂片剂+继续吸入倍氯美松。
③孟鲁司特10mg+吸入安慰剂。
④安慰剂片剂+吸入安慰剂。结果显示第一组FEV1白天症状与夜间憋醒等均有明显改善。联合治疗组的哮喘症状加剧及急性发作的天数较单用吸入倍氯美松短，故联合用药可起协同作用。
【原产地英文商品名】SINGULAIR 10mg/Tablet 100Tablets/box
【原产地英文药品名】MONTELUKAST SODIUM
【中文参考商品译名】顺尔宁 10毫克/片 100片/盒
【中文参考药品译名】孟鲁司特钠
【生产厂家中文参考译名】默克
【生产厂家英文名】Merck
Singulair
Generic Name: montelukast (mon te LOO kast)
Brand Names: Singulair
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What is Singulair?
Singulair is a leukotriene (loo-koe-TRY-een) inhibitor. Leukotrienes are chemicals your body releases when you breathe in an allergen (such as pollen). These chemicals cause swelling in your lungs and tightening of the muscles around your airways, which can result in asthma symptoms.
Singulair is used to prevent asthma attacks in adults and children as young as 12 months old. It is also used to relieve runny nose and sneezing caused by allergies in adults and children as young as 6 months old.
Do not give Singulair to a child without a doctor's advice.
Singulair is also used to prevent exercise-induced bronchoconstriction (narrowing of the air passages in the lungs) in adults and teenagers who are at least 15 years old and are not already taking this medicine for other conditions.
If you already take Singulair to prevent asthma or allergy symptoms, do not use an extra dose to treat exercise-induced bronchoconstriction.
Singulair may also be used for other purposes not listed in this medication guide
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What is the most important information I should know about Singulair?
Singulair will not work fast enough to treat an asthma attack that has already begun. Use only a fast-acting inhalation medicine to treat an asthma attack. Talk with your doctor if any of your asthma medications do not seem to work as well in treating or preventing attacks.
It may take up to several weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve after several weeks of treatment.
Call your doctor right away if you feel that this medicine is not working as well as usual, or if it makes your condition worse. If it seems like you need to use more of any of your medications in a 24-hour period, talk with your doctor.
If you already take Singulair to prevent asthma or allergy symptoms, do not use it for exercise-induced bronchoconstriction.
Call your doctor at once if you have any mood or behavior changes, anxiety, depression, or thoughts about suicide or hurting yourself.
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What should I discuss with my healthcare provider before taking Singulair?
Do not use Singulair if you are allergic to montelukast.
The chewable tablet form of Singulair may contain phenylalanine. Talk to your doctor before using this form of Singulair if you have phenylketonuria (PKU).
FDA pregnancy category B. Singulair is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether Singulair passes into breast milk or if it could harm a nursing baby. Do not use Singulair without telling your doctor if you are breast-feeding a baby.
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How should I take Singulair?
Take Singulair exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Singulair is usually taken once daily in the evening for prevention of asthma or allergy symptoms. For exercise-induced bronchoconstriction, take a single dose at least 2 hours before you exercise, and do not take another dose for at least 24 hours. Follow your doctor's instructions.
If you already take Singulair to prevent asthma or allergy symptoms, do not use it for exercise-induced bronchoconstriction.
Swallow the regular tablet whole, with a glass of water.
The chewable tablet must be chewed completely before you swallow it.
The oral granules can be placed directly into the mouth and swallowed, or mixed with a spoonful of applesauce, mashed carrots, rice, or ice cream. Oral granules can also be mixed with 1 teaspoon of baby formula or breast milk. Do not use any other type of liquid for mixing the granules. Other liquids can be taken before or after taking the medicine.
After opening or mixing the oral granules, you must use them within 15 minutes. Do not save an open packet or mixed medicine for later use.
Singulair will not work fast enough to treat an asthma attack that has already begun. Use only a fast-acting inhalation medicine to treat an asthma attack. Talk with your doctor if any of your asthma medications do not seem to work as well in treating or preventing attacks.
It may take up to several weeks before your symptoms improve. Keep using Singulair as directed and tell your doctor if your symptoms do not improve after several weeks of treatment.
Asthma is usually treated with a combination of drugs. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or medication schedulewithout your doctor's advice, even if you have no asthma symptoms.
If you also take a steroid asthma medicine, do not stop using it suddenly without first talking to your doctor. You may need to use less and less before you stop the medication completely.
Call your doctor right away if you feel that this medicine is not working as well as usual, or if it makes your condition worse. If it seems like you need to use more of any of your medications in a 24-hour period, talk with your doctor.
Store Singulair at room temperature away from moisture and heat. Do not open a packet of oral granules until you are ready to use the medicine.
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What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
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What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
Symptoms of a Singulair overdose are not known.
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What should I avoid while taking Singulair?
Avoid situations or activities that may trigger an asthma attack.
If your asthma symptoms get worse when you take aspirin, avoid taking aspirin or other NSAIDs (non-steroidal anti-inflammatory drugs) while you are taking montelukast. NSAIDs include ibuprofen (Motrin, Advil), diclofenac (Cataflam, Voltaren), etodolac (Lodine), indomethacin (Indocin), meloxicam (Mobic), nabumetone (Relafen), naproxen (Aleve, Naprosyn), piroxicam (Feldene), and others.
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Singulair side effects
Get emergency medical help if you have any of these signs of an allergic reaction to Singulair: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have any of these serious side effects:
skin rash, bruising, severe tingling, numbness, pain, muscle weakness;
mood or behavior changes, anxiety, depression, or thoughts about suicide or hurting yourself;
tremors or shaking;
severe sinus pain, swelling, or irritation; or
worsening asthma symptoms.
Less serious Singulair side effects may include:
headache;
stomach pain, heartburn, upset stomach, nausea, diarrhea;
tooth pain;
tired feeling;
fever, stuffy nose, sore throat, cough, hoarseness; or
mild rash.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
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What other drugs will affect Singulair?
Before using Singulair, tell your doctor about all other medicines you use, especially:
phenobarbital (Luminal, Solfoton); or
rifampin (Rifadin, Rifater, Rifamate, Rimactane).
This list is not complete and there may be other drugs that can interact with Singulair. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor
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Where can I get more information?
Your pharmacist can provide more information about Singulair.
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What does my medication look like?
Montelukast is available with a prescription under the brand name Singulair. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about Singulair, especially if it is new to you.
Singulair 4 mg chewable tablets - pink, oval tablets
Singulair 5 mg chewable tablets - pink, round tablets
Singulair 10 mg - beige, rounded-square shaped, film-coated tablets
Singulair Oral granules 4 mg-white granules
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Singulair only for the indication prescribed.
Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist. | 
