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达卡他韦

印度达卡他韦

资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-03-27 09:58:51

【药品简介】 达卡他韦(Daklinza)是一种丙型肝炎病毒NS5A抑制剂适用为与索非布韦使用为慢性HCV基因型3感染的治疗。口服,每天1次与索非布韦联用共12周

【适应症状】 达卡他韦,达卡他韦是一种丙型肝炎病毒(HCV)NS5A抑制剂适用为与索非布韦使用为慢性HCV基因型3感染的治疗

【 药品别名 】 达卡他韦 Daclatasvir Daklinza

印度达卡他韦(达卡他韦 Daclatasvir Daklinza)价格,正品图片,治疗丙肝药物, 购买达卡他韦请到印度药房官方网站进行购买 【印度药房大全目录】

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【印度达卡他韦说明书,怎么吃?】

【用法用量】

1)达卡他韦60mg 口服每天1次有或无食物与索非布韦联用。
 
2)达卡他韦推荐治疗时间:达卡他韦服用12周。
 
3)达卡他韦剂量调整:与强CYP3A抑制剂减低达卡他韦剂量至30 mg每天1次;与中度CYP3A诱导剂增加达卡他韦剂量至90mg每天1次。
 
 
 
【不良反应】
 
达卡他韦与索非布韦联用观察到达卡他韦最常见不良反应(≥10%)是头痛和疲乏。
 
 达卡他韦
 
【注意事项】
 
1)达卡他韦紧急CYP3A的强诱导剂,包括苯妥英钠,卡马西平,利福平,和圣约翰草

2)索非布韦和胺碘酮共同给药:在服用胺碘酮与索非布韦联用与另一个HCV直接作用药物患者可能发生严重症状性心动过缓,包括达卡他韦达卡他韦(达卡他韦),尤其是还接受β受体阻滞剂或那些具有潜在心脏合并症和(或)晚期肝病患者。建议胺碘酮与达卡他韦与索非布韦联用不要共同给药。建议在无另外治疗选择患者中监视心脏。
 
 
 
【特殊人群使用】
 
1)肾受损使用达卡他韦:达卡他韦是与血浆蛋白高度结合,通过透析可能不能去除达卡他韦。
 
2)在HCV-感染受试者达卡他韦群体药代动力学分析显示被分析的年龄范围(18-79岁),年龄对达卡他韦的药代动力学没有达卡他韦临床上相关影响[见达卡他韦特殊人群中使用。
 
3) 未曾在儿童患者中评价达卡他韦的药代动力学。
 
4) 在HCV-感染受试者达卡他韦群体药代动力学分析估计女性受试者与男性受试者比较有一个30%较高的达卡他韦AUC,这个达卡他韦AUC差别不认为临床上相关。
 
5) 在HCV-感染受试者达卡他韦群体药代动力学分析表明种族对达卡他韦暴露无临床相关影响。


DACLACURE TABLET SIDE EFFECTS

Common
Fatigue
Headache
Nausea
Insomnia (difficulty in sleeping)
Anemia (low number of red blood cells)

HOW TO USE DACLACURE TABLET
Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it.

HOW DACLACURE TABLET WORKS
Daclacure 30 mg Tablet is an antiviral medication. It works by lowering a load of hepatitis C virus in the body and removing the virus from the blood over a period of time.

DACLACURE TABLET RELATED WARNINGS
warnings

Alcohol
There is no data available. Please consult doctor before consuming the drug.

warnings

Pregnancy
There is no data available. Please consult doctor before consuming the drug.

warnings

Lactation
Daclacure 30 mg Tablet is probably safe to use during lactation. Limited human data suggests that the drug does not represent a significant risk to the baby.

warnings

Driving
Do not drive unless you are feeling well.
Some patients have reported dizziness, difficulty in concentrating, and vision problems while taking Daclacure 30 mg Tablet which may affect your ability to drive.

warnings

Kidney
There is no data available. Please consult doctor before consuming the drug.

warnings
Liver
There is no data available. Please consult doctor before consuming the drug.

Daclatasvir

生物活性

产品描述

Daclatasvir (BMS-790052) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

靶点活性

HCV NS5A,9pM-50pM(EC50)

体外活性

BMS-790052 is one of the most potent inhibitors of HCV replication reported so far. The mean EC50 valuses of BMS-790052 are 50 and 9 pM for HCV genotype 1a and 1b replicons, respectively. BMS-790052 displays a therapeutic index (CC50/EC50) of at least 105 and is inactive towards a panel of 10 RNA and DNA viruses, with EC50 higher than 10 μM. This confirms BMS-790052's specificity for HCV. [1] In Huh7 cells harboring the HCV genotype 1b replicons, BMS-790052 blocks both transient and stable HCV genome replication, with EC50 values raging from 1-15 pM. BMS-790052 (100 pM or 1 nM) has been shown to alter the subcellular localization and biochemical fractionation of NS5A. [2] BMS-790052 inhibits hybrid replicons containing HCV genotype-4 NS5A genes with EC50 of 7-13 pM. Residue 30 of NS5A is an important site for BMS-790052-mediated resistance in the hybrid replicons. [3]

体内活性

In a randomized, double-blind, placebo-controlled, single ascending-dose study, Daclatasvir (BMS-790052) is administered at six dose levels to healthy, non-HCV-infected subjects over a range of 1 to 200 mg as an oral solution. Daclatasvir is safe and well tolerated up to 200 mg with no clinically relevant adverse effects. After oral administration, Daclatasvir is readily absorbed, with dose-proportional exposures over the studied dose range, and all subjects have drug concentrations greater than the protein-binding-adjusted EC90 for genotypes 1a and 1b, as measured in the replicon assay, at and beyond 24 h post-dose. (The protein binding-adjusted EC90 figures are derived from an analysis of the effect of the addition of human serum on antiviral activity in replicons. In the presence of 40% human serum, the EC90 for Daclatasvir is 383 pM (0.28 ng/mL) for the genotype 1a replicon and 49 pM (0.04 ng/mL) for the genotyope 1b replicon)[1]. Mice in each group that developed persistent HCV infection are divided into two treatment groups. One group receive 4 weeks of Asunaprevir/Daclatasvir treatment and the other group received 4 weeks of Ledipasvir/GS-558093 treatment. Asunaprevir/Daclatasvir therapy and Ledipasvir/GS-558093 therapy rapidly decease serum HCV RNA levels to below the sensitivity, and they are not detected after completion of the therapy except for two mice in the Ledipasvir/GS-558093 group[5].

激酶实验

FRET assay for HCV NS5A inhibitors: The peptide (Ac-Asp-Glu-Asp [EDANS]-Glu-Glu-Abu-[COO] Ala-Ser-Lys [DABCYL]-NH2) contains a fluorescence donor {EDANS, 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid} near one end of the peptide and an acceptor {DABCYL, 4-[(4-dimethylamino)phenyl]azo)benzoic acid} near the other end. Intermolecular resonance energy transfer between the donor and the acceptor quenches the fluorescence of the peptide, but as the NS3 protease cleaves the peptide, the products are released from resonance energy transfer quenching. The fluorescence of the donor increases over time as more substrate is cleaved by the NS3 protease. The assay reagent is: 5× luciferase cell culture lysis reagent diluted to 1× with dWater, NaCl (150 mM), the FRET peptide (20 μM). HCV-Huh-7 cells are placed in a 96-well plate, and allowed to attach overnight (1×104 cells per well). The next day, BMS-790052 is added to the wells and the plate is incubated for 72 hours. The plate is then rinsed with PBS and used for the FRET assay by the addition of 30 μL of the FRET peptide assay reagent (described above) per well. Signals are obtained using the Cytofluor 4000 instrument, which has been set to 340 nm (excitation)/490 nm (emission) automatic mode, for 20 cycles or less, with the plate being read in the kinetic mode. Following FRET, 40 μL of luciferase substrate is added to each well and the luciferase is measured.

细胞实验

BMS-790052 is added to 96-well plates containing HCV replicon cells seeded approximately 12 hours before in 200 µL media.The cell plates are tested for replication activity and cytotoxicity after 72 hours of incubation. Cytotoxicity is measured with CellTiter-Blue, after which the media and dye are removed, plates are inverted and the remaining liquid is blotted with paper towels. Replication activity of the HCV genotype 1a cell lines is quantified using Renilla luciferase. 1× Renilla luciferase lysis buffer (30 µL) is added to each well and plates are incubated with gentle shaking for 15 min. Renilla luciferase substrate (40 µL) is then added and the signals are detected using a Top Count luminometer set for light emission quantification. One hundred per cent activity is calculated for each cell line for the DMSO-only wells; percentage activity is calculated for each concentration of the inhibitor by dividing the average value for wells containing compound by the average value for wells containing DMSO.(Only for Reference)

细胞系: HCV replicon cells (Huh7)

动物实验

动物模型:Mice

化学信息

分子量

738.88

分子式

C40H50N8O6

CAS

1009119-64-5

溶解度

DMSO: 136 mg/mL (184.1 mM)

Ethanol: 136 mg/mL (184.1 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

  1 mg 5 mg 10 mg
1 mM 1.353 ml 6.767 ml 13.534 ml
5 mM 0.271 ml 1.353 ml 2.707 ml
10 mM 0.135 ml 0.677 ml 1.353 ml
50 mM 0.027 ml 0.135 ml 0.271 ml

参考文献
 
1. Gao M, et al. Nature, 2010, 465(7294), 96-100.
2. Lee C, et al. Virology, 2011, 414(1), 10-18.
3. Wang C, et al. Antimicrob Agents Chemother, 2012, 56(3), 1588-1590.
4. O'Boyle DR 2nd, et al. Antimicrob Agents Chemother, 2005, 49(4), 1346-1353.
5. Kai Y, et al. Emergence of hepatitis C virus NS5A L31V plus Y93H variant upon treatment failure of daclatasvir and asunaprevir is relatively resistant to ledipasvir and NS5B polymerase nucleotide inhibitor GS-558093 in human hepatocyte chimeric mice. J Ga
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