药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201883022234010.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分TAMIFLU处方资料(仅供参考)
英文药名: TAMIFLU Dry Syrup 3%(Oseltamivir Phosphate)
中文药名: 达菲(磷酸奥司他韦干糖浆)
タミフルドライシロップ3%
治疗类别名称
抗流感病毒剂
商標名
TAMIFLU
一般名
オセルタミビルリン酸塩(Oseltamivir Phosphate)(JAN)
化学名
(-)-Ethyl(3R,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)cyclohex-1-ene-1-carboxylate monophosphate
分子式
C16H28N2O4・H3PO4
分子量
410.40
熔点
192~195℃(分解)
分配系数
在酸性至中性区域分配到水相中,它是分散在油相中在碱性区域。
操作注意事项
1.即使在到期日开幕后,将尽快用定。
2.由于有吸湿性,开口密封后,您保存,避免受潮。
3.超过4周后保存,将存放在冰箱或阴凉处(10℃以下)。此外,使用时被打开,以避免冷凝。
药效药理
1.体外抗病毒活性
磷酸奥塞米韦是一种前药,被转化为活性形式通过代谢,显示出抗病毒活性之后。
磷酸奥塞米韦的活性形式是A型和B型流感病毒在体外的低浓度的副本是由(实验室菌株的IC 50:<0.35微米:0.6-155nM,临床分离株的IC 50)抑制。
2.在体内抗病毒活性
在小鼠和雪貂的A型和B型流感病毒感染的模型,磷酸奥塞米韦(0.1-100毫克/kg/天)口服给药,增加,这取决于生存的剂量,减少症状与感染有关,观察到的治疗效果,如在病毒滴度的降低。此外,从病毒感染前24小时在鸡感染模型(10,100mg/千克,1天两次),对病毒感染的抑制作用,例如在生存增加观察到的口服给药。
3.作用机理
磷酸奥塞米韦的活性形式选择性地抑制人A型和B型流感病毒的神经氨酸苷酶:通过抑制从所述新形成的病毒感染细胞的释放(IC 500.1~为3nM),病毒抑制生长。
4. 耐性
在发病的成人和抗病毒的青少年相对于国外和国内的临床试验目前剂(例4/1245)0.32%,为4.1%,在1至12岁儿童(N =464分之19)。所有耐药病毒是由A型流感病毒来源,出现在B型进行了观察。的抗病毒韩元,在感染的小鼠和雪貂的减少进行观察,生长在感染部位,传播力被认为是低的。的抗病毒韩元,氨基酸突变的神经氨酸酶已观察。
适应病症
A型或B型流感病毒感染及其预防
用法与用量
1.在治疗中使用
(1) 成人
一般,每天75毫克,连服五天后暂停口服给药。
(2) 婴儿和儿童
通常,为2mg/kg的每日两次(66.7mg/kg的作为干糖浆),连服五天暂停口服给药。然而,最高剂量一次为75mg。
2.在预防使用
(1) 成人
每日一次,每次为75mg,为7至10天在使用时通过口服给药。
(2) 婴儿和儿童
为2mg/kg的每日一次(66.7mg/kg的作为干糖浆),连服10天口服给药。然而,最高剂量一次为75mg。
包装规格
干糖浆3%:30克
English name: TAMIFLU Dry Syrup 3% (Oseltamivir Phosphate)
Chinese medicine name: Tamiflu (oseltamivir phosphate syrup)
タミフルドライシロップ3%
Treatment category name
Anti-influenza virus
Trademark name
TAMIFLU
General Name
Oseltamivir Phosphate (JAN)
Chemical name
(-)-Ethyl(3R,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)cyclohex-1-ene-1-carboxylate monophosphate
Molecular formula
C16H28N2O4・H3PO4
Molecular weight
410.40
Melting point
192~195°C (decomposition)
Assignment coefficient
The acid to neutral zone is partitioned into the aqueous phase, which is dispersed in the oil phase in the alkaline zone.
Operational Precautions
1. Even after the opening date, it will be used as soon as possible.
2. Because of the hygroscopicity, after the opening is sealed, you save it and avoid moisture.
3. Save after 4 weeks and store in a refrigerator or in a cool place (below 10 °C). In addition, it is opened during use to avoid condensation.
Pharmacological Pharmacology
1. Antiviral activity in vitro
Oseltamivir phosphate is a prodrug that is converted to an active form by metabolism, showing antiviral activity.
The active form of oseltamivir phosphate is a low concentration copy of influenza A and B viruses in vitro is inhibited by (laboratory strain IC50: <0.35 micron: 0.6-155 nM, IC50 of clinical isolates).
2. Antiviral activity in vivo
In mice and ferrets infected with influenza A and B viruses, oral administration of oseltamivir phosphate (0.1-100 mg/kg/day) increases, depending on the dose of survival, reducing symptoms and infections Related to the observed therapeutic effects, such as a decrease in virus titer. In addition, from the chicken infection model (10, 100 mg / kg, twice a day) in the chicken infection model 24 hours before the infection, the inhibition of viral infection, for example, the oral administration observed in the increase in survival.
3. Mechanism of action
Active form of oseltamivir phosphate selectively inhibits neuraminidase of human influenza A and B viruses: by inhibiting release from the newly formed virus-infected cells (IC 500.1 to 3 nM), viral suppression Growing.
4. Patience
The incidence of adult and antiviral adolescents relative to foreign and domestic clinical trials currently (0.34%) was 0.42%, 4.1% in children between 1 and 12 years of age (N = 19/46). All resistant viruses were observed by the type A influenza virus and appeared in type B. The antiviral Won, observed in infected mice and ferrets, was grown at the site of infection and transmission was considered low. The antiviral Won, an amino acid mutant of neuraminidase has been observed.
Adapted to the disease
Type A or B influenza virus infection staining and prevention
Usage and dosage
1. Use in treatment
(1) Adult
In general, 75 mg per day, and repeated oral administration after five days of service.
(2) Infants and Children
Typically, 2 mg/kg twice daily (66.7 mg/kg as a dry syrup) was administered orally for five days. However, the highest dose was 75 mg at a time.
2. Use in prevention
(1) Adult
Once daily, 75 mg each time, for 7 to 10 days by oral administration at the time of use.
(2) Infants and Children
It was once daily at 2 mg/kg (66.7 mg/kg as a dry syrup) and was administered orally for 10 days. However, the highest dose was 75 mg at a time.
Packing specification
dry syrup 3%: 30 g
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201883022234010.pdf)的“原文Priscribing Information”为准 --------------------------------------------------------------- |