Sofosbuvir + Ledipasvir

Thông tin thuốc gốc
Chỉ định và Liều dùng
Chronic hepatitis C
Adult: Available preparation:
Sofosbuvir 400 mg and Ledipasvir 90 mg

In patients with HCV genotype 1, 4, 5, or 6 infections: 1 tab once daily, with or without ribavirin. If vomiting occurs within 5 hours of dosing, an additional tab is needed. Treatment duration: 8 or 12 weeks, or 24 weeks if necessary (varies according to HCV genotype and treatment regimen used).
Child: ≥12 years or weighing ≥35 kg: 1 tab once daily. Treatment duration varies according to HCV genotype and treatment regimen used.
Cách dùng
May be taken with or without food.
Chống chỉ định
Hypersensitivity. Lactation. Concomitant use of potent P-glycoprotein (P-gp) inducers and rosuvastatin.
Thận trọng
Patient with hepatitis B virus (HBV) co-infection; decompensated cirrhosis and/or who are awaiting liver transplant or post-liver transplant, and those at high risk of bradyarrhythmia. Children. Pregnancy.
Tác dụng không mong muốn
Gastrointestinal disorders: Nausea, diarrhoea.
General disorders and administration site conditions: Fatigue, weakness, irritability.
Immune system disorders: Rarely, angioedema.
Investigations: Increased serum lipase, bilirubin, creatine phosphokinase.
Nervous system disorders: Headache, dizziness.
Psychiatric disorders: Insomnia, depression.
Respiratory, thoracic and mediastinal disorders: Cough, dyspnoea, nasopharyngitis.
Skin and subcutaneous tissue disorders: Rash.
Potentially Fatal: Hepatitis B virus reactivation, resulting in fulminant hepatitis or hepatic failure (in patients with HBV co-infection).
Thông tin tư vấn bệnh nhân
This drug may cause fatigue, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Screen for current or previous hepatitis B infection by measuring hepatitis B surface antigen (HBsAg) and hepatitis core antibody (anti-HBc) prior to initiation. Monitor bilirubin, liver enzymes, and serum creatinine at baseline and periodically; serum HCV-RNA at baseline, during and after treatment, and when clinically indicated.
Tương tác
Reduced plasma concentration with moderate P-gp inducers (e.g. oxcarbazepine). May increase tenofovir exposure. Reduced efficacy with antacids (Al and Mg hydroxide). May increase the serum concentration of digoxin. Reduced anticoagulant effect of vitamin K antagonists.
Potentially Fatal: Significantly reduced plasma concentration with potent P-gp inducers (e.g. rifampicin, phenobarbital, phenytoin, carbamazepine), resulting in loss of efficacy. May cause significant increase in the plasma concentration of rosuvastatin, resulting in myopathy and rhabdomyolysis. Risk of severe bradycardia and cardiac arrest with amiodarone.
Tương tác với thức ăn
Significantly reduced plasma concentration with St John’s wort, avoid use.
Tác dụng
Description: Sofosbuvir and ledipasvir reduce viral load by inhibiting hepatitis C virus RNA replication.
Sofosbuvir, a nucleotide analogue, inhibits hepatitis C virus (HCV) nonstructural 5B (NS5B) RNA-dependent polymerase which is necessary for viral replication. It is a direct-acting antiviral prodrug that has broad genotypic coverage and acts as chain terminator.
Ledipasvir inhibits the HCV nonstructural 5A (NS5A) protein, which is essential for both RNA replication and the assembly of HCV virions.
Absorption: Well absorbed.
Sofosbuvir: Time to peak plasma concentration: Approx 0.8-1 hour.
Ledipasvir: Time to peak plasma concentration: 4-4.5 hours.
Distribution: Sofosbuvir: Plasma protein binding: Approx 61-65%.
Ledipasvir: Plasma protein binding: >99.8%.
Metabolism: Sofosbuvir: Extensively metabolised in the liver via hydrolysis to form pharmacologically active nucleoside (uridine) analogue triphosphate GS-461203, followed by dephosphorylation to form nucleoside inactive metabolite GS-331007.
Ledipasvir: Undergoes slow oxidative metabolism.
Excretion: Sofosbuvir: Mainly via urine (80%); faeces (14%). Elimination half-life: Approx 0.5 hour.
Ledipasvir: Mainly via faces (approx 86%); urine (1%). Elimination half-life: 47 hours.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Sovaldi, CID=45375808, (accessed on Jan. 23, 2020)

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Ledipasvir, CID=67505836, (accessed on Jan. 23, 2020)

Bảo quản
Store below 30°C.
Phân loại MIMS
Thuốc kháng virus
Phân loại ATC
J05AP51 - sofosbuvir and ledipasvir ; Belongs to the class of antivirals for treatment of HCV infections. Used in the treatment of hepatitis C viral infections.
Tài liệu tham khảo
Anon. Ledipasvir and Sofosbuvir. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 01/02/2018.

Harvoni Tablet, Film-coated (Gilead Sciences, Inc.). DailyMed. Source: U.S. National Library of Medicine. Accessed 01/02/2018.

Joint Formulary Committee. Sofosbuvir with Ledipasvir. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. Accessed 01/02/2018.

Thông báo miễn trừ trách nhiệm: Thông tin này được MIMS biên soạn một cách độc lập dựa trên thông tin của Sofosbuvir + Ledipasvir từ nhiều nguồn tài liệu tham khảo và được cung cấp chỉ cho mục đích tham khảo. Việc sử dụng điều trị và thông tin kê toa có thể khác nhau giữa các quốc gia. Vui lòng tham khảo thông tin sản phẩm trong MIMS để biết thông tin kê toa cụ thể đã qua phê duyệt ở quốc gia đó. Mặc dù đã rất nỗ lực để đảm bảo nội dung được chính xác nhưng MIMS sẽ không chịu trách nhiệm hoặc nghĩa vụ pháp lý cho bất kỳ yêu cầu bồi thường hay thiệt hại nào phát sinh do việc sử dụng hoặc sử dụng sai các thông tin ở đây, về nội dung thông tin hoặc về sự thiếu sót thông tin, hoặc về thông tin khác. © 2022 MIMS. Bản quyền thuộc về MIMS. Phát triển bởi
  • Lesovir
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Already a member? Sign in