51．立复汀
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284页（6031字）
【中文释文】：
鼻喷剂
〔概述〕
立复汀鼻喷剂含有左卡巴斯汀，即(-)-[3S-[1(顺式)，3α，4β]]-1-[4-氰基-4-(4-氟苯)环已基]-3-甲基-4-苯基-4-哌啶-羧酸-单盐酸，是一种局部应用的、高选择性的组胺H1受体拮抗剂。
立复汀鼻喷剂是微混悬液(pH6～8)。
每毫升含0．5mg左卡巴斯汀(活性成分)，0．15mg氯苄烷铵(防腐剂)及丙二醇，吐温-80、磷酸二钠、磷酸一钠、EDTA二钠盐、羟丙基甲基纤维素和水等无活性赋形剂。
〔药理学和药代动力学特性〕
立复汀鼻喷剂含有左卡巴斯汀，一种强效、速效、长效、具有高度选择性的组胺H1受体拮抗剂。局部应用于鼻部，几乎即刻起效，消除过敏性鼻炎的典型症状(打喷嚏、鼻痒、流鼻涕)，作用可维持数h。鼻内每喷一次，大约有30～40μg的左卡巴斯汀被吸收，并主要以原型药的形式由尿排出(约为吸收量的70%)。左卡巴斯汀的血浆半衰期约为35～40h。
〔适应证〕
过敏性鼻炎的症状。
〔禁忌证〕
对其中所含成分过敏者禁用。
〔特别注意〕
由于左卡巴斯汀由肾脏排泄，故肾损伤病人使用时应特别注意。
〔妊娠期和哺乳期妇女的应用〕
小鼠、大鼠和家兔全身应用高达临床局部用量1250倍的立复汀，未显示对胎儿的毒性或形成畸胎，啮齿动物服用2500倍或更大的剂量，则可见形成畸胎和(或)胎儿的吸收增加。
由于缺少孕妇应用立复汀鼻喷剂的充分资料，除非潜在的利益与对胎儿可能发生的危害相比是值得的，妊娠期不应使用本品。
根据对哺乳期妇女的唾液和乳汁中左卡巴斯汀浓度测定计算表明，母亲鼻部用药后，婴儿每天接受到的左卡巴斯汀不超过3．5μg。故哺乳期妇女应用左卡巴斯汀鼻喷剂是安全的。
〔药物相互作用〕
临床试验中未见有本品与酒精或任何其他药物产生相互作用的报告。在特殊设计的精神活动作用研究中，未见本品与安定有相互作用。但不能排除与酒精有轻微的相互作用。
〔不良反应〕
偶有应用本品后即刻出现暂时而轻微的局部刺激(鼻刺痛和烧灼感)的报告。
〔剂量和用法〕
立复汀鼻喷剂为微混悬液，用前必须摇匀。
成人和儿童：常用量为每个鼻孔喷两下，每日2次。剂量可增加到每次喷两下，每日3～4次。连续用药直至症状消除。
病人应在用药前清洗鼻道，喷药时将药物吸入。第一次喷药前使气雾泵源充满，直至能很好地喷出气雾，然后再开始使用。
〔对驾驶能力和操纵机器的影响〕
立复汀鼻喷剂无镇静作用，对精神运动性活动亦无影响。故驾驶汽车和操纵机器的病人可以应用本品。
〔规格及包装〕
15ml塑料瓶内装10ml白色微悬浮液。含左卡巴斯汀0．5mg／ml。
〔贮存〕
室温保存。
〔使用期限〕
3年。
〔生产厂家〕
比利时杨森制药公司
(附本品别名：左卡巴斯汀，Levocabastine)
【外文释文】：
Description
Livostin nasal spray contains levocabastine(-)-[3S-[1(Cis)，3α，4β]]-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidine-carboxylic acid-monohydrochloride，a highly selective histamine H1-antagonist for topical use．Livostin nasal spray is available as a microsuspension(pH 6-8)．
Each ml contains 0．5mg levocabastine as active ingredient；benzalkonium chloride 0．15 mg as preservative；and propylene glycol，polysorbate 80，disodium phosphate，monosodium phosphate，disodium edetate，HPMC and water as inactive excipients．
Pharmacological and pharmacokinetic properties
Livostin nasal spray contains levocabastine，a very potent，fast-acting and highly selective histamine H1-antagonist with a sustained duration of action．After topical application to the nose，it almost immediately and for several hours relieves the typical symptoms of allergic rhinitis(sneezing，itchy nose，rhinorrhoea)．
After intranasal application，about 30-40μg of levocabastine per puff is absorbed and predominantly excreted in the urine as unchanged drug(about 70% of the absorbed dose)．The plasma half-life of levocabastine is approximately 35-40 hours．
Indications
Symptoms of allergic rhinitis．
Contraindications
Hypersensitivity to any of the ingredients．
Special precautions for use
Considering the renal route of excretion for levocabastine，caution should be exercised when administering Livostin nasal spray to patients with renal impairment．
Use during pregnancy and lactiation
In mice，rats and rabbits，Livostin，at systemic doses up to 1 250 times the recommended topical clinical dose，did not reveal any embryotoxic or teratogenic effect．In rodents，at 2 500 times this dose and higher，teratogenicity and／or increased embryonal resorption were observed．
There are no adequate data on the use of Livostin nasal spray in pregnant women．Therefore，Livostin nasal spray should not be used during pregnancy，except if the potential benefit justifies the potential risk to the fetus．
Based on determinations of levocabastine concentrations in saliva and breast milk in a nursing woman，it was calculated that the daily dose of levocabastine in the infant would not exceed 3．5μg after nasal treatment of the mother．Therefore，levocabastine nasal spray can be given safely to nursing mothers．
Interactions
Interaction with alcohol or any other drug was never reported in clinical trials．In specially designed psychoperformance study，an interaction with diazepam was not observed but a slight interaction with alcohol could not be excluded．
Adverse reactions
Transient slight local irritation(nasal stinging and burning)immediately after the application of Livostin nasal spray has been reported occasion-ally．
Dosage and administration
As Livostin nasal spray is available as a microsuspension，the bottle should be shaken before each application．
Adults and children：the usual dose is 2 puffs of Livostin nasal spray per nostril，twice daily．The dose may be increased to 2 puffs 3 to 4 times daily．Treatment should be continued as long as required for symptom relief．
Patients should be instructed to clear the nasal passaes prior to administering the spray and to inhale through the nose during spraying．Before using the pump delivery system for the first time，the pump reservoir should be filled up by priming until a fine spray is delivered．
Effects on driving ability and use of machinery
Livostin nasal spray does not produce sedation，nor does it impair psychomotor performance；therefore，it can be used by patients driving cars or operating machinery．
How supplied
Livostin nasal spray is available in 15-ml plastic bottles containing l0ml of a white microsuspension containing 0．5mg of levocabastine per ml．
Store at room temperature
Valid period
Three years
Manufacturer
Janssen Pharmaceutical／Belgium