100．仙特敏
出处：按学科分类—医药、卫生 军事医学科学出版社《临床常用进口药物手册》第559页（6234字）
【中文释文】：
(西替利嗪)盐酸西替利嗪包衣片
〔组成〕
每包衣片含10mg盐酸西替利嗪
〔剂型、用途及包装〕
每盒5片、10片、20片、100片，口服，有痕纹包衣片
〔特性〕
动物实验证明仙特敏是一种H1受体抑制剂，并完全无明显抗胆碱或抗5-羟色胺作用。在药效剂量，仙特敏不会引起困倦或行为变化，此可从仙特敏不能通过血脑屏障解释。在临床药理，仙特敏被证实可抑制一些外源性组胺作用，这抑制能力迅速产生，仙特敏也抑制体内由组胺释放剂例如48／80的组胺作用。最后，仙特敏可抑制由肠血管活性肽及P物质，神经肽所引起的皮肤反应，这些物质被认为参与了过敏反应。仙特敏明显地降低哮喘病人对组胺所起气管过敏反应，仙特敏降低由个别抗过敏原所引起的变态反应。这些作用并没有带来任何中枢神经作用，无论以心理测量测验或定量脑电图测定。
口服10mg仙特敏30～60min内，达至最高血药浓度，约为0．3μg／ml，血浆半衰期为11h。请注意在每一个病例中仙特敏被吸收是很有规律的，肾清除率为30ml／min。排泄半衰期约为9h，仙特敏与血浆蛋白紧密结合。
〔适应证〕
主要治疗季节性鼻炎及眼结膜炎，长期性过敏鼻炎，瘙痒及过敏引起的荨麻疹。
〔剂量及服用方法〕
成人或儿童超过12岁。在大多数超量情况下，推荐剂量为10mg，一次口服。从本品适应证来看，若在晚间服用，最好在晚饭时间用少许液体服用此药。若病人对副作用敏感，推荐每天早晚2次服用，每次5mg。
〔禁忌证〕
病人曾有病史对仙特敏片任何成分产生超敏反应，均禁止使用。
〔副作用〕
就副作用来讲，在推荐剂量下服用，与安慰剂无大分别(激动、口干、嗜睡、头痛)，稀有报告超敏反应的病例。
〔警戒〕
在治疗剂量下，仙特敏不会强化酒精作用(血药浓度0．8g／L)但是，必须小心。
〔怀孕及哺乳期〕
动物畸胎试验并无显示任何畸形现象，但为了预防，仙特敏不应给在器官发育期的孕妇服用，同样适用于授乳妇。
〔药物交叉作用〕
至今未有报道，但同时服用安眠药要小心。
〔驾驶或操作机械〕
在健康自愿者服用20mg／d或25mg／d试验中，并未证实对警戒性及反应时间有任何改变。建议病人服药时不要超过以上剂量。
〔过量〕
嗜睡是过量症状之一，出现于1次口服50mg。现今无特别解毒剂，在大量过量情况下，胃灌洗应尽快进行，建议一般急救支持性治疗包括经常监测维持生命必需的功能。
〔贮藏〕
保持于室温(15～25℃)
〔稳定性〕
检查在包装纸上注明的过期日子并未超过。
〔生产厂家〕
比利时布赖讷拉勒UCB公司药品部
(附本品别名：疾立静、赛特赞、Cetrizet)
【外文释文】：
Cetirizine hydrochloride
film-coated tablets
Composition
Each film-coated tablet contains cetirizine hydrochloride 10 mg．
Dosage form，route of administration and packaging
Box containing 5，10，20，or 100 film-coated tablets for oral use．
Properties
In experimental animals，Zyrtec has been shown to be an anti-H1agent devoid of any significant anticholinergic or antiserotonin effects．At pharmacologically active doses，it induces neither sedation nor behavioural changes．This may be explained by the fact that Zyrtec does not cross the blood-brain barrier．
It was shown in human pharmacology studies that Zyrtec will inhibit certain effects produced by exogenous histamine．This activity appears rapidly．Zyrtec also inhibits the effects produced by endogenous histamine released in vivo by an agent such as 48／80．Finally，it in hibits the cutaneous reaction induced by VIP(vasoactive intestinal polypeptide)and substance P，neuropeptides which are believed to take part in the allergic reaction．
Zyrtec markedly reduces bronchial hyperreactivity to histamine in the asthmatic patient．It also reduces the allergic reaction induced by specific allergens．These effects are obtained without any central effects being demonstrated either by psychometric tests or by a quantified EEG．
Peak blood levels of the order of 0．3 μg／ml are reached between thirty and sixty minutes after administration of a l0mg dose of Zyrtec．Its plasma half-life is approximately 11 hours．Absorption is very consistent from one subject to the next．Its renal clearance is 30 ml／min and the excretion half-life is approximately 9 hours．Zyrtec is strongly bound to plasma proteins．
Indications
Symptomatic treatment of seasonal rhinitis and conjunctivitis，perennial allergic rhinitis as well as pruritus and urticaria of allergic origin．
Dosage and directions for use
Adults and children of 12 years and older．
In most cases，the recommended dose is one 10 mg tablet daily．
It is advisable to take the drug with a little liquid during the evening meal since the symptoms for which the product is given usually appear during the night．
In patients affected by side effects，the dose may be taken as 5 mg in the morning and 5mg in the evening．
Contraindications
Zyrtec tablets are contraindicated in patients with a history of hypersensitivity to any of the constituents．
Side effects
When Zyrtec is administered at recommended doses any side effects that may occur，such as agitation，dry mouth，drowsiness，or headache，do not differ significantly from placebo．
Very occasionally symptoms of hypersensitivity have been reported．
Special precautions
At therapeutic doses，Zyrtec does not potentiate the effect of alcohol(at a blood level of 0．8g／L)．
Care should，however，be taken．
Pregnancy and lactation
Teratology studies in animals have not demonstrated any special adverse effects．
As a precaution，however，Zyrtec should not be administered to pregnant women during the first three months of pregnancy，nor should women who are breastfeeding take the drug．
Drug interactions
To date，there are no known interactions with other drugs．
Nevertheless，Zyrtec should be used with caution if sedatives are also being taken．
Driving or operating machinery
Studies in healthy volunteers on 20 mg／d or 25 mg／d have not revealed effects on alertness or reaction time．Patient should be advised，however，to take care not to exceed the recommended dose．
Overdosage
Drowsiness can be a symptom of overdosage，occurring from administration of 50 mg of Zyrtec as a single dose．
To date，there is no specific antidote．
In the case of massive overdosage，gastric lavage should be performed as soon as possible．Usual supportive measures should be provided and routine observations carried out regularly．
Storage
Store below 25℃ in a dry place．
Stability
The expiry date on the package，found after the mention“Exp’’should not have been exceeded．
Manufacture
UCB S．a．Pharma Sector
Braine-l Alleud，Belgium