英文药名: Zaditen(Ketotifen Fumarate Tablets)

中文药名: 富马酸酮替芬片

生产品牌药厂家: Novartis

药品名称

通用名称：酮替芬
英文名：Ketotifen
其它中文名：富马酸酮替芬、甲哌噻庚酮、萨地酮、酮替酚、噻喘酮、噻哌酮
其它英文名：Ketotifen Fumarate、Zaditen、Zasten
规格

缓释片: 2mg/片; 片剂：1mg／片。糖浆剂：1mg/5ml。
药理作用　

药效学
可抗组胺和抗过敏，其抗组胺的作用持续较长而抗过敏作用持续的时间较短，以上两种作用各自独立。
本品为新的抗变态反应药物，其特点是兼有很强的组胺 H1受体拮抗作用和抑制过敏反应介质释放的作用。其抗组胺作用较马来酸氯苯那敏(扑尔敏)强约 10倍，具有长效。另一方面，不仅抑制支气管周围粘膜下肥大细胞释放组胺、慢反应过敏物质，而且也抑制血液中嗜酸性粒细胞释放组胺、慢反应物质等，产生很强的抗过敏作用。在人体，不仅能抑制Ⅰ型变态反应中肥大细胞和嗜碱性粒细胞释放组胺、慢反应过敏物质等反应介质，在 Ⅲ型变态反应中对嗜中性白细胞也有作用 。口服有效，作用持续时间较长，一日仅需给药 2次。
药动学
口服经胃肠道可迅速完全地被吸收。半衰期＜1 小时。当其血浆浓度达到100～200μg/ml时, 75％与蛋白结合。在猴试验中, 1/3～1/2药量由尿排泄,其余由粪便排出。本品为新的抗变态反应药物，其特点是兼有很强的组胺Ｈ1受体拮抗作用和抑制过敏反应介质释放的作用。其抗组胺作用较马来酸氯苯那敏（扑尔敏）强约10倍，且有长效。另一方面，不仅抑制支气管周围粘膜下肥大细胞释放组胺慢反应过敏物质，而且也抑制血液中嗜酸性粒细胞释放组胺慢反应物质等，产生很强的抗过敏作用，在人体不仅能抑制Ｉ型变态反应中肥大细胞和嗜碱性粒细胞释放组胺、慢反应过敏物质等反应介质，在Ⅲ型变态反应中对嗜中性白细胞也有作用。口服有效，作用持续时间较长，一日仅需给药２次。
适应症　　

用于支气管哮喘或其他过敏性疾病的预防。
主要用于预防或治疗过敏性哮喘、混合性哮喘、过敏性支气管炎、过敏性鼻炎、各型荨麻疹、血管性水肿、异位性皮炎、瘙痒症、皮肤划痕症等。
用法用量

口服，每次1mg，每日2次。体重40kg以下者剂量酌情减少。
嗜睡反应者剂量减半，经1～2周嗜睡减轻或消失后再增至常量。
本品并用安眠药时，后者应适当减量。
使用本品2～3周，待哮喘症状缓解后，方可逐渐减少其他平喘药物的用量。谨遵医嘱!
禁用/慎用　

服用降血糖药物的糖尿病患者忌用，孕妇、驾驶员及其他需要高度注意力的工作人员慎用。
给药说明　　

①用药初期，中枢神经活动处于抑制状态，禁止驾驶车辆或操作精密仪器；
②本品系防止过敏和抗组胺药物，不直接作用于舒张支气管，因此本药对支气管哮喘的作用在服药后的 2—3周才出现。
不良反应　

本品的副作用主要为嗜睡、倦怠、胃肠道反应等。
①嗜睡，夜间服用嗜睡反应较少；
②少见的反应有：口干、恶心、头晕目眩、头痛、体重增加。
可有嗜睡、头晕、恶心、口于、头痛及体重增加等。
过量(10～120mg，血浆药物平均浓度为1～4mg/L，有高达5～122mg/L），其临床症状为：困倦、神志不清、昏迷、呼吸异常、心动过缓或心动过速、过度兴奋、惊厥和眼球震颤。
药物相互作用　

本品能增强各种镇定、安眠药的作用。

ZADITEN
Erythropoietin
   
COMPOSITION Each tablet contains: 1 mg ketotifen (as the hydrogen fumarate)
Each 5ml syrup contains: 1 mg ketotifen (as the hydrogen fumarate): The syrup is prepared using a sugar substitute (Iycasin) and can therefore be given to diabetic children under appropriate supervision. 5 ml syrup is equivalent to 4 g carbohydrate.
   
PROPERTIES & ACTION ZADITEN is a non-bronchodilator antiasthmatic drug with marked anti-anaphylactic properties and a specific antihistaminic effect. Laboratory experiments both in vitro and in vivo have revealed the following properties of ZADITEN, which may contribute to its anti-asthmatic activity.
- Inhibition of both the acute broncho-constrictor response to PAF (Platelet Activating Factor) and PAF- induced airway hyperresponsiveness.
- Inhibition of PAF - induced accumulation of eosinophils in the airways.
- Inhibition of the release of such chemical mediators as histamine and leukotrienes.
- Antagonism of acute bronchoconstriction due to leukotrienes.
- Reversal or prevention of experimentally inducted isoprenaline tachyphylaxis.
In addition, þZADITEN exerts a powerful and sustained H1-receptor blocking activity, which can be clearly distinguished from its anti-anaphylactic properties.
   
INDICATIONS Long term prevention of :
- Bronchial asthma(all forms, including Mixed)
- Allergic bronchitis
- Asthmatic symptoms associated with hay fever.
It may take several weeks before the full therapeutic effect of ZEDITEN is achieved. Prevention and treatment of:
- Multisystemic allergies
- Allergic rhinitis
- Allergic dermatoses ZADITEN is not effective in aborting established attacks of asthma.
   
DOSAGE Adults:
1 tablet twice daily (with morning and evening meals). In patients susceptible to sedation a progressive regimen is recommended during the first week of treatment. If necessary, the dosage may be increased to 2 tablets twice daily.
Children:
Children age 6 months to 3 years: 1.5 ml syrup twice daily.
Children over 3 years of age: 1 tablet or 5 ml syrup twice daily.
   
CONTRAINDICATIONS Hypersensitivity to ketotifen.
   
PRECAUTIONS Anti-asthmatic drugs already in use should not be withdrawn abruptly at the start of ZADITEN treatment. This applies particularly to systemic conticosteroids and ACTH, since there is risk of adrenal insufficiency in steroid dependent patients. In such cases, recovery of a normal pituitary-adrenal response to stress may take as long as one year. ZEDITEN may impair the reactions. Patients should therefore be warned to exercise caution when driving a vehicle, operating machinery, etc.
   
PREGNANCY AND LACTATION Reproduction studies in animals do not suggest that the taking of ZADITEN involves any risk of fetal damage, but this has not been confirmed by controlled trials in pregnant women. Its safety during pregnancy can not therefore be regarded as established, making very careful evaluation of the risk/benefit ratio is essential. It is not known whether ZADITEN is excreted in breast milk.
   
ADVERSE EFFECTS Sedation and in isolated cases, dryness of the mouth and slight dizziness may occur at the start of treatment but normally disappear quickly and spontaneously. Weight gain has occasionally been reported. Sedation rarely occurs in children and is less severe than in adults. Increased excitability and agitation have been reported in approximately 0.2% of patients, particularly in children.
   
INTERACTIONS A reversible fall in the thrombocyte count has been reported in a few cases in which ZADITEN was being given concomitantly with an oral anti-diabetic agent. Thrombocyte count should therefore be performed in patients taking such drugs concomitantly. AZADITEN may potentiate the effects of sedatives, hypnotics, antihistamines, and alcohol.
   
OVERDOSAGE The principal signs of acute overdosage include drowsiness to sever sedation, confusion and disorientation, tachycardia and hypotension, convulsion (especially in children), hyperexcitability (in children) and reversible coma. Treat symptomatically. If the drug has been taken recently, the stomach should be emptied. Give symptomatic treatment, with cardiovascular monitoring if necessary. Short-acting barbiturates or benzodiazipines should be given in cases of excitation or convulsions.
   
PRESENTATIONS 1 mg tablet in packs of 30 tablets and hospital packs of 1000 tablets.
Syrup 100 ml bottle.