英文药名: Lamivudine (3TC Tablets)

中文药名: 拉米夫定（3TC片）
药品名称

通用名称: 拉米夫定
常用名称: 拉咪呋定, 拉咪呋啶, 雷米夫定
英语名称: Epivir (3TC),Heptodin,Heptovir,Lamivudine Bulk,3TC
药物类别: 核苷类抗HIV药;抗感染药物;特异性药物;抗病毒药;抗生素类抗微生物药;抗HIV病毒类药物;抗肝炎病毒类药物;反-转录酶抑制剂/RNA。
 
药理作用　　

在一些不同的巨噬细胞和淋巴细胞培养基和新鲜的周围血液淋巴细胞(PBL)中，对拉米夫定(3TC)的抗人类免疫缺陷病毒-1和病毒-2(HIV-1和HIV-2)的活性进行了测试。本品用于抑制病毒复制50％的浓度为4nmol/L～0.67μmol/L。
在体外，本品与AZT有协同作用，但是与ddc和ddl有加和作用。
本品对于临床上分离的拮抗AZT的HIV也有活性。
拉米夫定在体内不管是人类免疫缺陷病毒(HIV)感染还是未感染的周围血液淋巴细胞中被磷酸化成5’-三磷酸化合物，其 t1/2为10～15小时。本品并不影响脱氧核苷在U937细胞中的代谢。
拉米夫定的5’-三磷酸化合物是人类免疫缺陷病毒逆转录酶(HIV-RT)的一个竞争性抑制剂〔相对三磷酸脱氧胞苷(dCTP)而言〕(其表观 Ki＝106±1.0～12.4±5.1μmol/L)拉米夫定5’-三磷酸化合物对于RT DNA依赖的DNA聚合酶的IC50为23.4±2.5μmol/L。相对于dCTP来说，拉米夫定5’-三磷酸化合物是哺乳动物DNA聚合酶β和γ的竞争性抑制剂，其Ki分别为18.7μmol／L和15.8±0.8μmol／L。该化合物抑制DNA聚合酶α的IC50为175±31μmol/L。拉米夫定也是HIV-RT的一条链结尾物，进一步研究表明链结尾作用是这个化合物作用的主要机理。
本品是乙肝病毒(HBV)交叉感染的HepG2细胞HBV-DNA复制的有效抑制剂(IC50为0.1μmol/L)。而且，该化合物在一日2次0.3mg/kg的剂量下对HBV慢性感染的黑猩猩的HBV-DNA复制有抑制作用，但是在治疗(大约80天)结束后2～3周复制会出现一个反弹反应。
适应症　　

本品适用在艾滋病患者病情好转的情况下与齐多夫定联合对艾滋病进行治疗；以及适用于获得性免疫缺陷综合征/AIDS;乙型肝炎;慢性侵袭性肝炎;慢性活动性肝炎/HBV。
用法用量　　

本品对成年人和青年人(12～16岁)的剂量是一天2次，每次150mg，与齐多夫定合并使用。对于体重不足50千克的成年人，剂量为每日2次，每次4mg/kg(直到最高剂量为150mg，一天2次)，也要与齐多夫定联合使用。
儿童病人剂量要加大，这是由于该药在儿童体内的平均生物利用度较低。
任何疑问，请遵医嘱！
制剂/规格

片剂：含量为150mg；300mg。
口服液：10mg/ml装在240ml获300ml塑料瓶中。
不良反应　

主要是胃肠道反应(恶心33％，腹泻18％，恶心和呕吐13％，厌食10％)；神经系统反应(神经痛12％，麻木10％，失眠11％)。另有头痛35％，困倦27％，发热或畏寒10％，鼻塞20％，咳嗽18％，骨骼肌痛12％以及中性粒细胞减少症5％～7％。

3TC™ Oral Solution 10mg/ml 240ml

3TC™ Tablets 150mg 60's

English drug name: Lamivudine (3TC Tablets)

Chinese medicine name: lamivudine (3TC tablets)
Drug Name

Common name: Lamivudine
Common name: La Mia given furosemide, lamivudine, Lei Mifu set
English name: Epivir (3TC), Heptodin, Heptovir, Lamivudine Bulk, 3TC
Drug Class: Nucleoside Anti-HIV drugs; anti-infectives; specific drugs; antiviral; antibiotic anti-microbial drugs; Anti-HIV viral drugs; anti-virus drugs; anti - transcriptase inhibitors / RNA.
 
Pharmacology

In a number of different culture media of macrophages and lymphocytes in peripheral blood lymphocytes and fresh (PBL) in lamivudine (3TC) resistance to human immunodeficiency virus HIV -1 and -2 (HIV-1 and HIV -2) activity were tested. This product is used for 50% inhibition of viral replication in the concentration of 4nmol / L ~ 0.67μmol / L.
In vitro, the product a synergistic effect with AZT, but with the ddc and ddl have additive effect.
This product is for the clinically isolated HIV have antagonized the activity of AZT.
Lamivudine in the body, whether human immunodeficiency virus (HIV) infection or uninfected peripheral blood lymphocytes is phosphorylated into 5'-triphosphate compounds, the t1 / 2 was 10 to 15 hours. This product does not affect nucleoside metabolism in U937 cells.
Lamivudine 5'-triphosphate compounds are reverse transcriptase of human immunodeficiency virus (HIV-RT), a competitive inhibitor relative 〔deoxycytidine triphosphate (dCTP) in terms of〕 (apparent Ki = 106 ± 1.0 ~ 12.4 ± 5.1μmol / L) lamivudine 5'-triphosphate compounds for the RT DNA dependent DNA polymerase of the IC50 was 23.4 ± 2.5μmol / L. Relative to dCTP, the lamivudine 5'-triphosphate compounds are mammalian DNA polymerase β and γ a competitive inhibitor, the Ki are 18.7μmol / L and 15.8 ± 0.8μmol / L. The compounds inhibit the DNA polymerase α and IC50 was 175 ± 31μmol / L. Lamivudine in HIV-RT is also the end of one strand of material, further study showed that the role of chain at the end of the main mechanism of the role of this compound.
This product is hepatitis B virus (HBV) infection in HepG2 cells cross-HBV-DNA replication effective inhibitor (IC50 = 0.1μmol / L). Furthermore, the compounds 2 times a day dose of 0.3mg/kg of HBV infection in chimpanzees with chronic HBV-DNA replication inhibition, but in the treatment (about 80 days) 2 to 3 weeks after the emergence of a rebound in replication reaction.
Indications

This product is suitable for AIDS patients got better in the case of joint and zidovudine treatment of AIDS; and for acquired immunodeficiency syndrome / AIDS; hepatitis B; chronic aggressive hepatitis; chronic active hepatitis / HBV.
Dosage

This product is for adults and young people (12 to 16 years) dose is 2 times a day, each 150mg, and zidovudine combination. For adults weighing less than 50 kg, a dose of 2 times a day, every 4mg/kg (until the maximum dose of 150mg, 2 times a day), but also in combination with AZT.
Children to increase patient dose, due to the drug in children, the average bioavailability of the body low.
Any questions, please doctor!
Preparation / Specifications

Tablet: content was 150mg; 300mg.
Oral: 10mg/ml be installed in 240ml 300ml plastic bottle.
Adverse reactions

Primarily gastrointestinal reactions (nausea 33%, 18% diarrhea, nausea and vomiting 13%, anorexia 10%); nervous system response (12% of neuropathic pain, numbness, 10%, insomnia 11%). Another 35% of headache, drowsiness 27%, 10% fever or chills, stuffy nose 20%, 18% cough, muscle pain, 12% and neutral neutropenia 5% to 7%.

3TC ™ Oral Solution 10mg/ml 240ml


3TC ™ Tablets 150mg 60's