【通用名称】非索非那丁(Fexofenadine)
【商品名称】Allegra
【性状】本品为白色结晶状粉末，无臭无味，几乎难溶于水，极易溶于氯仿，亦溶于乙醇和丙酮，几乎不溶于水，熔点为147-151℃。
【体内过程】非索非那丁口服吸收良好，吸收较为迅速，口服0.5-１小时出现抗组胺作用，1-3小时血药浓度达峰值，平均为1.3 h。半衰期为11-15小时，平均为14.4 h，蛋白结合率60%～70%(主要是α1酸性糖蛋白)。疗效可持续约18-24小时，因此可每日1次给药。吸收后非索非那丁和血浆蛋白广泛结合, 结合率高达95%。已证实非索非那丁不需通过肝脏的细胞色素P-450酶系统的CYP酶代谢。本品不透过血脑屏障。
【药理机制】初期研究发现特非那丁不仅本身有药理作用，其代谢产物仍具有药理活性，如直接用其治疗过敏反应，可免受药酶代谢而消除对人体的心脏毒性，就是根据特非那丁的这个特性，在1995年德国hoechest marion roussel 药厂最先研究开发了特非那丁的活性代谢产物——非索非那丁，并于1997年获FDA批准，由于该药没有心脏毒副作用，被某些学者认为是高效、长效、低毒特点的第三代抗组胺药物。非索非那丁在哮喘病治疗中的作用可能与以下机制有关：
１、直接拮抗H1受体的作用；
２、对粘附分子的活性：研究发现非索非那丁通过抑制粘附分子的表达和趋化因子的活性来减少气道内炎性细胞的聚集和浸润，可以显著减少体内ICAM-1的表达，从而抑制炎性细胞向炎症组织的趋化，即使药物浓度低至10～10mol/L，也可显著降低从季节性变应性鼻炎患者鼻上皮细胞释放白介素-8和可溶性ICAM-1的水平。
３、稳定炎性细胞活性：通过调节细胞膜的稳定性来抑制气道内炎性细胞的释放活性，包括稳定肥大细胞膜来减少组胺、白细胞三烯等炎性介质的产生；通过抑制嗜酸细胞活性来减少气道上皮毒性蛋白和炎性介质的释放；抑制淋巴细胞的活性来减少TH2细胞因子的活性等；
４、拮抗其他炎性介质的活性：如拮抗白细胞三烯、血小板激活因子和5-羟色胺的作用；
５、气道效应：非索非那丁可以增强β2-受体激动剂的支气管舒张作用，可抑制吸入变应原诱发的致敏豚鼠的支气管痉挛，并可以降低吸入乙酰甲胆碱引起的气道高反应性，而对气道内的嗜酸细胞没有影响。
【临床应用】
非索非那丁由Aventis公司生产，其在世界市场上的销售份额已占所有抗过敏药物的40%左右。临床研究表明非索非那丁有较强的支气管解痉效应，单次口服非索非那丁180mg可以产生比吸入色甘酸钠气雾剂大3-5倍的气道保护效应。临床研究证实，连续口服非索非那丁四周后，哮喘患者在症状评分、支气管解痉剂的用量、肺通气功能指标和气道反应性等方面均有显著改善，同时可以显著改善过敏性鼻炎的临床症状。以生活质量改善作为评价指标对1 948例季节性过敏性鼻炎服用60 mg，每日一次，结果表明非索非那丁不仅可以显著改善鼻部症状，而且还能提高患者的生活质量。目前非索非那丁已成为欧美各国治疗过敏性鼻炎、过敏性皮肤病和过敏性哮喘等过敏性疾病的主要药物。另外，由于近年来发现第二代抗组胺药物有配伍禁忌,且有一定的心脏毒副作用，而非索非那丁没有发现心脏毒性，上市后短短两年，在美国市场的使用量已上升为第二大品种并保持强劲增长势头。
【用法和剂量】有片剂、胶囊、混悬液三种剂型，用于过敏性鼻炎的临床推荐口服剂量为120mg，一日一次，或60mg每日2次；用于皮肤过敏疾病180mg一日一次；为预防夜间或清晨哮喘发作，睡前可顿服120-180mg/次。混悬液为5ml，含非索非那丁30mg。含本品60 mg和盐酸伪麻黄碱120 mg的Allegra D已在美国上市，主要用于12岁以上伴有鼻等鼻部症状的感冒患者。
【副作用】动物放射标记试验证实非索非那丁不通过血脑屏障，因而没有嗜睡和困倦等副作用。常规临床推荐剂量的常见副作用有口干、头晕，偶有头痛和恶心等，停药后可很快消失。由于非索非那丁对H1受体有较高的选择性，对H2受体影响很小，因此无抗组胺类抗过敏药物通常的影响胃酸分泌作用，也无抗胆碱作用和α1-受体阻滞作用。
【安全性】动物试验没有发现非索非那丁有心脏毒性，分别给狗和兔子高于成人常规口服剂量（60 mg,bid）的28倍和63倍,也没有延长QTc。临床试验也证实即使大剂量口服非索非那丁也不诱发心率失常，这是非索非那丁区别于其他抗组胺药物的最大特点。临床试验60 mg/次,bid，疗程6个月，或240 mg/次,qd,疗程12个月，未见QTc明显延长。对非索非那丁诱致人体的心律失常试验表明，能阻滞心脏钾通道所需的药物浓度是特非那丁的500倍以上，这是非索非那丁心脏毒性很低的主要原因。
【注意事项】
1．妊娠期和哺乳期妇女应慎用，FDA将非索那丁划为孕妇用药中较不安全的C类。
2．对本化合物或活性成分过敏者慎用。
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原产地英文商品名:
ALLEGRA SUSPENSION 30mg/5ml 300mls/bottle
原产地英文药品名:
FEXOFENADINE HCL
中文参考商品译名:
艾来混悬剂 30毫克/5毫升 300毫升/瓶
中文参考药品译名:
盐酸非索非那丁
生产厂家中文参考译名:
赛诺菲安万特
生产厂家英文名:
SANOFI AVENTIS US
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ALLEGRA®
(fexofenadine hydrochloride) Tablets, ODT (orally disintegrating tablets) and Oral Suspension
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What is Allegra?
Allegra (fexofenadine) is an antihistamine that reduces the natural chemical histamine in the body. Histamine can produce symptoms of sneezing, itching, watery eyes, and runny nose.
Allegra is used to treat the symptoms of seasonal allergies (hay fever) in adults and children.
Allegra is also used to treat skin itching and hives caused by a condition called chronic idiopathic urticaria in adults and children.
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Important information about Allegra
Before using Allegra, tell your doctor if you are allergic to any drugs, or if you have kidney disease.
Fruit juices and certain antacids can make it harder for your body to absorb Allegra. Take the disintegrating tablet on an empty stomach, at least 1 hour before or 2 hours after a meal.
There may be other drugs that can affect Allegra. 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.
Stop using this medication and get emergency medical help if you think you have used too much medicine, or if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Tell your doctor if your symptoms do not improve, or if they get worse after you start taking Allegra. Never take more of the medication than your doctor has prescribed.
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Before taking Allegra
Before using Allegra, tell your doctor if you are allergic to any drugs, or if you have kidney disease.
FDA pregnancy category C. It is not known whether Allegra is harmful to an unborn baby. Before taking Allegra, tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether fexofenadine passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.
Allegra tablets and capsules may be used to treat seasonal allergy symptoms in children who are at least 6 years old. Allegra oral suspension (liquid) may be used in children ages 2 through 11. When treating chronic idiopathic urticaria, the liquid may be used in children as young as 2 months old.
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How should I take Allegra?
Take Allegra exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
Take the regular Allegra tablets with a full glass of water. Do not use any other type of liquid. Shake the oral suspension (liquid) well just before you measure a dose. To be sure you get the correct dose, measure the liquid with a marked measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
To take fexofenadine orally disintegrating tablets (Allegra ODT):
Keep the tablet in its blister pack until you are ready to take the medicine. Open the package and peel back the foil from the tablet blister. Do not push a tablet through the foil or you may damage the tablet.
Using dry hands, remove the tablet and place it in your mouth. It will begin to dissolve right away.
Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.
Swallow several times as the tablet dissolves. If desired, you may drink liquid to help swallow the dissolved tablet.
Take the disintegrating tablet on an empty stomach, at least 1 hour before or 2 hours after a meal.
Tell your doctor if your symptoms do not improve, or if they get worse after you start taking Allegra. Never take more of the medication than your doctor has prescribed.
Store Allegra at room temperature away from moisture and heat. Keep the medicine bottle tightly closed.
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What happens if I miss a dose?
Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at your next regularly scheduled time. Do not take extra medicine to make up the missed dose.
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What happens if I overdose?
Seek emergency medical attention if you think you have used too much of this medicine.
Overdose symptoms may include dry mouth, dizziness, or drowsiness.
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What should I avoid while taking Allegra?
Avoid using antacids within 15 minutes before or after taking a medication that contains Allegra. Antacids can make it harder for your body to absorb this medication.
Do not take Allegra with fruit juice (such as apple, orange, or grapefruit).
Avoid taking any other cold or allergy medicines unless your doctor has told you to.
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Allegra side effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking Allegra and call your doctor if you have fever, chills, body aches, cough, or other flu symptoms.
Less serious Allegra side effects may include:
nausea, diarrhea, upset stomach;
menstrual cramps;
drowsiness, tired feeling;
headache; or
muscle or back pain.
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 Allegra?
Before taking Allegra, tell your doctor if you are also taking ketoconazole (Nizoral), or erythromycin (E-Mycin, E.E.S., Ery-Tab, Erythrocin).
There may be other drugs that can interact with Allegra. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.
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Where can I get more information?
Your pharmacist can provide more information about Allegra.
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication 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.