英文药名: Zefix(Lamivudine Tablets)
中文药名: 拉米夫定片
生产厂家: 葛兰素史克公司
ゼフィックス錠100
治疗类别名称
抗病毒化疗药物
商標名
Zefix Tablets
一般名
ラミブジン(Lamivudine)
化学名
(-)-1-[(2R,5S)-2-hydroxymethyl-1,3-oxathiolan-5-yl]cytosine
分子式
C8H11N3O3S
分子量
229.26
構造式
性状
白色至浅黄色结晶性粉末。易溶于二甲基亚砜,微溶于水,微溶于甲醇或乙醇(99.5),并在乙醚中几乎不溶。
熔点
关于176℃
分配系数
-0.9(1-辛醇/水系统)
药效药理
1. 抗病毒作用
其中慢性HBV感染的黑猩猩为拉米夫定为0.1mg/ kg的每日两次持续14天口服给药,血清HBV-DNA的浓度降低至先前值给药的不到10%。当除了施用拉米夫定为0.3mg/ kg的每日2次,14天,血清HBV-DNA的浓度低于检测极限。
2. HBV-DNA産生阻害作用
HepG22.2.15细胞中的HBV-DNA转染孵育7天拉米夫定或12天,HBV-DNA量从HepG2细胞释放2.2.15细胞减少浓度依赖性。
培养拉米夫定和HBV-DNA的游离量(IC 50)的50%抑制的浓度为0.032μM或0.018μM。
3. 转化为通过磷酸化活性形式
与HBV转染的DNA的HepG22.2.15细胞培养[3H]标记的拉米夫定和24小时,其中,细胞内的[3H]标记的拉米夫定和磷酸化体通过HPLC法测定,细胞内拉米夫定23.56%到35.65%被转换成5'-三磷酸物的活性形式。
4. 作用机序
拉米夫定在细胞中磷酸化,它被转换为活性物质的拉米夫定5'-三磷酸。
在乙型肝炎病毒DNA复制,拉米夫定-5'-三磷酸抑制脱氧胞苷5'-三磷酸(的dCTP)的DNA链通过DNA聚合酶竞争的摄取。此外,由于尽管拉米夫定5'-三磷酸掺入病毒DNA链作为DNA聚合酶的底物,拉米夫定-5'-三磷酸具有用于下一个核苷酸的DNA结合所需无OH基团的3'位置的链延伸被停止(链终止)。
基于上述,抗拉米夫定
适应症:
病毒的肝功能的乙型肝炎病毒的乙型肝炎增殖生长抑制伴随着异常已经证实B型慢性肝病
用法与用量
成人每天一次,每次100毫克。
包装规格
片剂
100mg:70片(PTP)
生产商
葛兰素史克日本公司
完整处文资料附件:http://www.info.pmda.go.jp/go/pack/6250020F1023_1_11/
Zefix Tablets(Lamivudine)
Zefix Tablets 100(ゼフィックス錠100)
Brand name : Zefix Tablets 100
Active ingredient: Lamivudine
Dosage form: pale orange brown tablet, major axis: 11.5 mm, minor axis: 5.5 mm, thickness: 3.6 mm
Print on wrapping: (Face) Zefix 100 mg, GX CG5, (Back) ゼフィックス100 mg
Effects of this medicine
This medicine decreases the amount of virus by suppressing the growth of the hepatitis B virus and improves liver function.
It is usually used to treat chronic hepatitis B virus infection.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
•If you are pregnant or breastfeeding.
•If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
•Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>>
•In general, for adults, take one tablet (100 mg of the active ingredient) at a time once a day. Strictly follow the instructions.
•If you miss a dose, take the missed dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time.
•If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
•Do not stop taking the medicine unless your doctor instructs you to do so. In general, it is necessary to take this medicine for a long period of time. Discontinuation of this medicine without permission may lead to disease progression.
Precautions while taking this medicine
•It is important that you receive medical examination on a regular basis because symptoms of chronic hepatitis B and hepatic cirrhosis B are extremely difficult to detect on your own.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include headache and malaise. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
•nasal bleeding, gum bleeding, subcutaneous bleeding [thrombocytopenia]
•muscle pain of limbs, feeling of weakness, reddish brown urine [rhabdomyolysis]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
•Keep out of the reach of children. Store away from direct sunlight, heat and moisture.
•Discard the remainder. Do not store them. Consult with your dispensing pharmacy or medical institution on how to discard the medicine.
GlaxoSmithKline K.K.Internal
Revised: 9/2014
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.