【异名】MDL16455

【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岁以上伴有鼻塞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。

注：以下产品是在美国本土上市，不同规格不同价格，购买时请以电话咨询为准！
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原产地英文商品名:
TELFAST FILM COATED TAB 120mg/tab 100tabs/box
原产地英文药品名:
FEXOFENADINE
中文参考商品译名:
太非薄膜衣片 120毫克/片 100片/盒
中文参考药品译名:
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 Deutschland GmbH

---------------------------------------------------------------
 原产地英文商品名:
TELFAST FILM COATED TAB 120mg/tab 20tabs/box
原产地英文药品名:
FEXOFENADINE
中文参考商品译名:
太非薄膜衣片 120毫克/片 20片/盒
中文参考药品译名:
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 Deutschland GmbH

---------------------------------------------------------------
原产地英文商品名:
TELFAST FILM COATED TAB 180mg/tab 20tabs/box
原产地英文药品名:
FEXOFENADINE
中文参考商品译名:
太非薄膜衣片 180毫克/片 20片/盒
中文参考药品译名:
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 Deutschland GmbH

---------------------------------------------------------------
原产地英文商品名:
TELFAST FILM COATED TAB 30mg/tab 100tabs/box
原产地英文药品名:
FEXOFENADINE
中文参考商品译名:
太非薄膜衣片 30毫克/片 100片/盒
中文参考药品译名:
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 Deutschland GmbH

---------------------------------------------------------------
原产地英文商品名:
TELFAST FILM COATED TAB 30mg/tab 50tabs/box
原产地英文药品名:
FEXOFENADINE
中文参考商品译名:
太非薄膜衣片 30毫克/片 50片/盒
中文参考药品译名:
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 Deutschland GmbH

---------------------------------------------------------------
原产地英文商品名:
TELFAST FILM COATED TAB 30mg/tab 50tabs/box
原产地英文药品名:
FEXOFENADINE
中文参考商品译名:
太非薄膜衣片 30毫克/片 50片/盒
中文参考药品译名:
非索非那丁
产厂家中文参考译名:
赛诺菲安万特
生产厂家英文名:
Sanofi-Aventis Deutschland GmbH

---------------------------------------------------------------
原产地英文商品名:
TELFAST FILM COATED TAB 30mg/tab 30tabs/box
原产地英文药品名:
FEXOFENADINE
中文参考商品译名:
太非薄膜衣片 30毫克/片 30片/盒
中文参考药品译名:
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 Deutschland GmbH

 
---------------------------------------------------------------

Telfast(fexofenadine)
Main use：Hayfever
Active ingredient：Fexofenadine hydrochloride
Manufacturer：Sanofi Aventis 

How does it work?
Telfast 120mg tablets contain the active ingredient fexofenadine, which is a type of medicine called a non-sedating antihistamine. It works by preventing the actions of histamine. (NB. Fexofenadine is also available without a brand name, ie as the generic medicine.)

Histamine is a substance produced by the body as part of its defence mechanisms. It is stored in cells called mast cells, in almost all tissues of the body. When the body reacts to a foreign substance (known as an allergen, eg flower pollen), the mast cells stimulated by the allergen release their stores of histamine.

The released histamine then binds to its receptors (H1 receptors), causing a chain reaction that results in allergic symptoms. It causes an increase in blood flow to the area of the allergy, and the release of other chemicals that add to the allergic response.

All this results in the symptoms of an allergic reaction. In hayfever, histamine causes inflammation of the nose, eyes, skin or airways and results in itchy watery eyes, a runny nose, sneezing and nasal congestion.

Fexofenadine works by blocking histamine H1 receptors. It does not prevent the actual release of histamine from mast cells, but prevents it binding to its receptors. This in turn prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the typical symptoms of allergies.

Fexofenadine 120mg is used to relieve the symptoms of hayfever.

Fexofenadine is called a non-sedating antihistamine as it does not enter the brain in significant amounts and is therefore unlikely to cause drowsiness. However, people react differently to medicines and extremely rarely some people may experience some drowsiness.

What is it used for?
Hayfever (seasonal allergic rhinitis).

Warning!
In the extremely unlikely event that this medicine causes drowsiness, the effect may be made worse by consuming alcohol or taking any medicines that do cause drowsiness. You should take care driving or operating machinary until you are familar with your response to this medicine.
If you are due to have any skin prick tests to diagnose allergies you should stop taking your antihistamines at least 48 hours before the tests. This is because antihistamines can prevent or lessen the skin reactions that indicate an allergy, and so can make the test results unreliable.

Use with caution in
Elderly people.
Decreased kidney function.
Decreased liver function.
History of disease involving the heart and blood vessels (cardiovascular disease).

Not to be used in
Children under 12 years of age.
Breastfeeding.

This medicine should not be used if you are allergic to one or any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy.

If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.

Pregnancy and breastfeeding
Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, before using any medicine.

The safety of this medicine during pregnancy has not been established. It should not be used by pregnant women unless considered essential by your doctor, and only if the benefits to the mother outweigh any risks to the foetus. Seek medical advice from your doctor.

This medicine may pass into breast milk. It is not recommended for use by breastfeeding mothers. Seek medical advice from your doctor.

Side effects
Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Just because a side effect is stated here does not mean that all people using this medicine will experience that or any side effect.
Headache.
Drowsiness.
Nausea.
Dizziness.
Fatigue.
Difficulty sleeping (insomnia).
Nervousness.
Awareness of your heartbeat (palpitations).
Increased heart rate (tachycardia).
Diarrhoea.

The side effects listed above may not include all of the side effects reported by the drug's manufacturer.

For more information about any other possible risks associated with this medicine, please read the information provided with the medicine or consult your doctor or pharmacist.

How can this medicine affect other medicines?
You should tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start treatment with this medicine. Similarly, check with your doctor or pharmacist before taking any new medicines while taking this one, to ensure that the combination is safe.

The manufacturer advises leaving two hours between taking fexofenadine and taking indigestion remedies (antacids) that contain aluminium or magnesium. This is because these types of antacids may decrease the absorption of fexofenadine from the gut and therefore make it less effective.