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盐酸西替利嗪片Zyrtec(Cetirizine Hydrochloride)

2009-10-25 11:49:14 作者：新特药房来源：中国新特药网浏览次数：189 文字大小：【大】【中】【小】

简介： 【化学名】±2-［2-［4-［（4-氯苯基）苯甲基］-1-哌嗪基］乙氧基］乙酸二盐酸盐【英文名】Cetirizine Hydrochloride Tablets 【成份】本品主要成分是盐酸西替利嗪【性状】本品为白色或类白色片。 ...

关键字：盐酸西替利嗪片 Zyrtec Cetirizine Hydrochloride

部份中文Zyrtec处方（仅供参考）
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：气道扩张药
药品英文名
Cetirizine
药品别名
西替立嗪、二盐酸西替立嗪、盐酸西替利嗪、疾立静、仙特敏、赛特赞、西可韦、Zyrtec、Cetrizet、CetirizineHydrochloride
药物剂型
缓释片：10mg。
片剂：10mg。 5mg
药理作用
具有独特的抗组胺和抗其他炎症介质的双重作用，是一种强效和高度选择性的H1受体拮抗剂，可抑制活化的肥大细胞释放组胺及抑制炎性细胞的趋化作用，同时还抑制变态反应时细胞间黏附分子的释放。此外，本品还具有抗炎活性，这可能与其具有抑制5-脂肪氧化酶的作用有关。
本品在抗组胺剂量下没有抗胆碱作用和镇静作用。
本品为羟嗪的羧化代谢物，是特异性长效组胺H1受体拮抗剂。在动物模型中其抗组胺活性强于氯马斯汀(Clemastine)、羟嗪、美吡拉敏(Mepyramine)和特非那定(Terfenadine)；对特应性和非特应性过敏患者，本品每天1次10mg，与安慰剂相比，明显抑制组胺、抗原和抗体引起的突发反应，作用最强时间4～8h，持续时间达24h；其活性与苯海拉明50mg或羟嗪25mg相似，至少与阿司咪唑(Astemizole)、氨卓斯汀(Azelastine)、溴苄那敏(Brompheniramine)、氯苯那敏(Chlorphenamine)、氯马斯汀(Clemastine)、酮替芬(Ketotifen)、氯雷他定(Loratadine)、美喹他嗪(Mequitazine)、奥沙米特(Oxatomide)或特非那定的标准剂量同效。此外，与阿司咪唑10mg相比，本品起效快得多。在抗过敏作用方面，本品10mg与阿司咪唑10mg、酮替芬1mg或特非那定120mg相同，而明显强于氯苯那敏8mg或
药动学
健康成年人口服本品10～20mg后1h内达血药峰浓度(257和580μg/L)。食物延缓吸收速率，但不影响吸收程度。作用可维持24h。本品在体内基本不被代谢，大部分以原形由尿、大便、汗液、乳液等排出。经尿排出率占70%，大便占10%。2天内全部排出体外。成人t1/2为7.4～11h，儿童t1/2为6.2h，不易透过血-脑脊液屏障。
适应证
用于治疗季节性变应性鼻炎(过敏性鼻炎，花粉症)。对急性和慢性的皮肤、眼部、呼吸道等过敏反应均有较好的疗效，常用于过敏性鼻炎、皮炎、眼结膜炎、哮喘、荨麻疹等。

禁忌证
1.对本品过敏严重肝病、严重心脏病、心律失常、心电图异常（明显或可疑QT间期延长)或低钾血症者禁用。
2.孕期尤其是前3个月和哺乳期禁用。

注意事项
1.12岁以下儿童暂不推荐使用。
2.肾功能障碍者应适当减量。
3.超剂量使用可引起致死性心律失常。
4.对驾驶、高空作业、潜水等人员用药量应严格控制在安全范围内。
5.严重肝肾功能不全者、饮酒及经常服用安眠药的患者应慎用。
不良反应
最常见不良反应是镇静、头痛、口干、疲乏和恶心。镇静作用的发生率与安慰剂、阿司咪唑、氯雷他定或特非那定相似。本品每天10mg产生的镇静作用似乎比氯雷他定每天10mg、特非那定每天120mg或安慰剂强。而每天5～20mg产生的镇静作用比羟嗪每天25～75mg弱得多。本品引起的肝功能异常自行消退，且不常见。

用法用量
口服：
1.每次10mg，每天1次。
2.6～12岁儿童每次5mg，每天1次。
3.6岁以下儿童，每天0.2mg/kg。

药物相应作用
1.不能与咪唑类抗真菌药、大环内酯类抗生素（如红霉素、竹桃霉素、克拉霉素或交沙霉素)同时使用。
2.在同时使用西咪替丁、环孢素和心痛定时应特别引起注意。乙醇和安眠药可加强本药的中枢抑制作用。
专家点评
比较了本品10mg与特非那定120mg、西替利嗪10mg、氯雷他定10mg，以及安慰剂对风疹团和皮肤潮红形成的抑制作用。结果表明咪唑斯汀比氯雷他定更有效。8项双盲、安慰剂对照志愿者研究，使用标准测试表明，本品较新抗组胺药对驾驶行为影响较小。比推荐剂量高1～2倍时，本品只出现低水平的镇静作用。另有临床试验表明本品与乙醇无潜在的药学相互作用。另在16名男性健康志愿者实验中（每天10mg)。未发现本品对技能操作和记忆力有影响。在多次随机双盲临床研究中，本品每天5～20mg对季节性和长年性过敏性鼻炎、慢性自发性荨麻疹的疗效已得到证实。本品为每天10～30mg时，有使轻微过敏性哮喘某些综合征减轻的倾向；每天10～30mg/kg时对某些物理性荨麻疹有效；每天10～40mg时减轻中度至严重的特应性皮炎综合征；每天10mg时减轻蚊子叮咬引起局部反应。对季节性过敏性鼻炎，本品每天5mg、10mg或20mg减轻综合征的疗效，至少与阿司咪唑每天10mg、氯雷他定每天10mg、特非那定每天60mg（每天2次)或每天120mg相似；对长年性过敏性鼻炎，其疗效至少与阿司咪唑每天10mg、酮替芬每天2mg或特非那定每天120mg相似；对于慢性自发性荨麻疹，其疗效至少与阿司咪唑每天10mg、羟嗪每天25～75mg或特非那定每天120mg相似；对轻微过敏性哮喘或特应性皮炎，其疗效与每天60mg(2次)特非那定相似；本品每天5mg或10mg对鼻炎患儿（≤12岁)也有效；每天5～15mg（2次)减少轻度气喘患儿的发病次数。

ZyrtecGeneric name: Cetirizine hydrochlorideBrand names: Zyrtec
Why is Zyrtec prescribed?
Zyrtec is an antihistamine. It is prescribed to treat the sneezing; itchy, runny nose; and itchy, red, watery eyes caused by seasonal allergies such as hay fever. Zyrtec also relieves the symptoms of year-round allergies due to dust, mold, and animal dander. This medication is also used in the treatment of chronic itchy skin and hives.
Most important fact about Zyrtec
Zyrtec may cause drowsiness. Be especially careful driving or operating dangerous machinery or participating in any hazardous activity that requires full mental alertness until you know how you react to Zyrtec.
How should you take Zyrtec?
Take Zyrtec once a day, exactly as prescribed. This medication can be taken with or without food.
Zyrtec may make your mouth dry. Sucking hard candy, chewing a stick of gum, or melting bits of ice in your mouth can provide relief.
If you miss a dose...If you are taking Zyrtec on a regular schedule, take the forgotten dose as soon as you remember. If it is almost time for your next dose, skip the one you missed and go back to your regular schedule. Do not take 2 doses at once.
Storage instructions...Store the tablets and syrup at room temperature. The syrup may be refrigerated.
What side effects may occur?
Side effects cannot be anticipated. If any develop or change in intensity, tell your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking Zyrtec.
Side effects in adults may include:Drowsiness, dry mouth, fatigue
Side effects in children aged 6 to 11 may include:Abdominal pain, coughing, diarrhea, headache, nosebleed, sleepiness, sore throat, wheezing
Why should Zyrtec not be prescribed?
Avoid Zyrtec if it causes a reaction, or if you have ever had a reaction to similar drugs.
Special warnings about Zyrtec
If you have kidney or liver disease, be sure to tell your doctor. Your dose of Zyrtec may have to be reduced.
Possible food and drug interactions when taking Zyrtec
You should avoid drinking alcohol or taking sedatives, tranquilizers, sleeping pills, or muscle relaxants while using Zyrtec. They can lead to increased drowsiness and reduced mental alertness. Among the products to avoid are the following:
AntidepressantsMuscle relaxantsPain-relieving narcoticsSedatives such as phenobarbitalSleeping pillsHigh doses of theophylline
Special information if you are pregnant or breastfeeding
The effects of Zyrtec during pregnancy have not been adequately studied. If you are pregnant or plan to become pregnant, tell your doctor immediately. Zyrtec appears in breast milk and should not be used if you are breastfeeding.
Recommended dosage for Zyrtec
ADULTS AND CHILDREN 12 YEARS AND OLDER
The usual starting dose is 5 or 10 milligrams once a day, depending on the severity of your symptoms. If you have a kidney or liver condition, the doctor will probably prescribe 5 milligrams daily.
CHILDREN 6 TO 11 YEARS
The usual starting dose is 5 or 10milligrams (1 or 2 teaspoonfuls of syrup) once a day. If your child has a kidney or liver condition, the doctor will probably prescribe the lower dose.
CHILDREN 2 TO 5 YEARS
The usual starting dose is 2.5 milligrams (one-half teaspoonful) once a day. Dosage may be increased to a maximum of 5 milligrams (1 teaspoonful) once daily or 2.5 milligrams (one-half teaspoonful) every 12 hours. If the child has a kidney or liver condition, Zyrtec should not be given.
CHILDREN 6 TO 23 MONTHS
The usual starting dose is 2.5 milligrams (one-half teaspoonful) once a day. In children 12 to 23 months old, the dose can be increased to a maximum of 5 milligrams a day, given as 2.5 milligrams (one-half teaspoonful) every 12 hours. Zyrtec should not be used if your child has kidney or liver problems.

セチリジン塩酸塩錠５mg「サワイ」／セチリジン塩酸塩錠10mg「サワイ」

商標名
CETIRIZINE HYDROCHLORIDE
一般名
セチリジン塩酸塩(Cetirizine Hydrochloride)
化学名
2-(2-{4-[(RS)-(4-Chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid dihydrochloride
分子式
C21H25ClN2O3・2HCl
分子量
461.81
包装
セチリジン塩酸塩錠５mg「サワイ」：
PTP：100錠(10錠×10)
セチリジン塩酸塩錠10mg「サワイ」：
PTP：100錠(10錠×10)、140錠(14錠×10)、500錠(10錠×50)