Baraclude is a nucleoside analogue indicated for the treatment of chronic hepatitis B
virus infection in adults with evidence of active viral replication and either evidence of
persistent elevations in serum aminotransferases (ALT or AST) or histologically active
disease.
Usage and administration
• Nucleoside-treatment-naïve (≥16 years old): 0.5 mg once daily.
• Lamivudine-refractory or known lamivudine or telbivudine resistance mutations
(≥16 years old): 1 mg once daily.
•Renal impairment: Dosage adjustment is recommended if creatinine clearance
is less than 50 mL/min.
•Baraclude (entecavir) should be administered on an empty stomach.
Dosage forms and strengths
• Tablets: 0.5 mg and 1 mg
• Oral solution: 0.05 mg/mL
Controindications
• None.
Warnings and precautions
• Severe acute exacerbations of hepatitis B virus infection after discontinuation:
Monitor hepatic function closely for at least several months.
• Co-infection with HIV: Baraclude is not recommended unless the patient is
also receiving HAART.
• Lactic acidosis and severe hepatomegaly with steatosis: If suspected, treatment
should be suspended.
Advers reactions
• Most common adverse reactions (≥3%, all severity grades) are headache,
fatigue, dizziness, and nausea.
To report suspected adverse reactions, contact Bristol-Myers Squibb at
1-800-721-5072 or FDA at 1-800-FDA-1088.
Use in specific populations
• Pregnancy: Pregnancy registry available. Enroll patients by calling
1-800-258-4263.
• Nursing mothers: Discontinue nursing or Baraclude taking into consideration
the importance of Baraclude to the mother.
Adverse reactions
The following adverse reactions are discussed in other sections of the labeling:
• Exacerbations of hepatitis after discontinuation of treatment
• Lactic acidosis and severe hepatomegaly with steatosis
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详细处方信息以本药内容附件PDF文件(200912917033916.pdf)的“原文Priscribing Information”为准
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部分中文 Baraclude (Entecavir) )处方资料(仅供参考)
【药品名】恩替卡韦片
【商品名】博路定
本品主要成分为:恩替卡韦,其化学名称为2-氨基-9-[(1S,3S,4S)-4-羟基-3-羟甲基-2-亚甲戊基]-1,9-氢-6-H-嘌呤-6-酮-水合物;分子式:C12H15N5O3·H2O 分子量:295.3
【形状】本品为薄膜衣片,除去包衣后显白色。
【作用机制】本品为鸟嘌呤核苷类似物,对乙肝病毒(HBV)多聚酶具有抑制作用。它能够通过磷酸化成为具有活性的三磷酸盐,三磷酸盐在细胞内的半衰期为15小时。通过与HBV多聚酶的天然底物三磷酸脱氧鸟嘌呤核苷竞争,恩替卡韦三磷酸盐能抑制病毒多聚酶(逆转录酶)的所有三种活性:(1)HBV多聚酶的启动;(2)前基因组mRNA逆转录负链的形成;(3)HBV DNA正链的合成。恩替卡韦三磷酸盐对HBV DNA多聚酶的抑制常数(Ki)为0.0012μM。恩替卡韦三磷酸盐对细胞的α、β、δDNA多聚酶和线粒体γDNA多聚酶抑制作用较弱,Ki值为18至于160μM。
【适应症】本品适用于病毒复制活跃,血清转氨酶ALT持续升高或肝脏组织学显示有活动性病变的慢性成人乙型肝炎的治疗。
【用法用量】患者应在有经验的医生指导下服用本品。
推荐剂量:成人和16岁以上青年口服本品,每天一次,每次0.5mg。拉米夫定治疗时病毒血症或出现拉米夫定耐药突变的患者为每天一次,每次1.0mg(0.5mg 两片)。
本品应空腹服用(餐前或餐后至少2小时)。
肾功能不全的患者中,恩替卡韦的表现口服清除率随肌酐清除率的降低而降低(参见药代动力学:特殊人群)。肌酐清除率<50ml/分钟的患者(包括接受血液透析或CAPD治疗的患者)应调整用药剂量。
【警告】1.停止治疗后的病情加重:
当慢性乙肝病人停止抗乙肝治疗后,包括恩替卡韦在内,已经发现有重度急性肝炎发作的报道。对那些停止抗乙肝治疗的病人的肝功能情况应从临床和实验室检查等方面严密监察,并且至少随访数月。如必要,可重新恢复抗乙肝病毒的治疗。
2.核苷类药物在单独或与其他抗逆转录病毒药物联合使用时,已经有乳酸性酸中毒和重度的脂肪性肝肿大,包括死亡病例的报道。
【不良反应】在国外进行的研究中,本品最常见的不良反应有:头痛、疲劳、眩晕、恶心。拉米夫定治疗的患者普遍出现的不良反应有:头痛、疲劳、眩晕。
【注意事项】患者应在医生的指导下服用恩替卡韦,并告知医生任何新出现的症状及合并用药情况。应告知患者如果停药有时会出现肝脏病情加重,所以应在医生的指导下改变治疗方法。
使用恩替卡韦治疗并不能降低经性接触或污染血源传播HBV的危险性。因此,需要采取适当的防护措施。
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详细处方信息以本药内容附件PDF文件(200912917033916.pdf)的“原文Priscribing Information”为准
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于2011年2月28日更新