1. Chronic hepatitis B virus (HBV) in patients ≥2 y/o weighing ≥10 kg
2. HIV-1 infection in patients ≥2 y/o weighing ≥10 kg (in combination with other antiretroviral agents)
藥理
Nucleotide Reverse Transcriptase Inhibitor (Anti-HBV)
Tenofovir disoproxil fumarate (TDF) is an analog of adenosine 5'-monophosphate; it interferes with the HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication. TDF is first converted to tenofovir and subsequently phosphorylated to the active tenofovir diphosphate; nucleotide reverse transcriptase inhibitor. Tenofovir inhibits replication of HBV by inhibiting HBV polymerase.
藥動學
Absorption:
1. Bioavailability: ~25% (fasting); increases ~40% with high-fat meal
2. Time to peak: (Fasting) 36-84 minutes; (With high-fat meal) 96-144 minutes Distribution:
1. Vd: 1.2 to 1.3 L/kg
2. Protein binding: <7% to serum proteins Metabolism:
1. Tenofovir disoproxil fumarate (TDF) is converted intracellularly by hydrolysis (by non-CYP enzymes) to tenofovir, then phosphorylated to the active tenofovir diphosphate
2. Half-life elimination: (Serum) 17 hours Excretion:
Urine (70% to 80%) via filtration and active secretion, primarily as unchanged tenofovir within 72 hours
禁忌症
Hypersensitive to tenofovir
懷孕分類
B
哺乳分類
Due to the risk of postnatal transmission of HIV, breastfeeding is not recommended.
HIV infection:
300 mg once daily without food, in combination with other antiretrovirals Hepatitis B infection:
300 mg once daily without food
小兒調整劑量
腎功能調整劑量
1. ClCr 30-49 mL/min: 300 mg every 48 hr
2. ClCr 10-29 mL/min: 300 mg every 72 to 96 hr
3. ClCr <10 mL/min, not receiving hemodialysis: no recommendation available
4. Hemodialys: 300 mg every 7 days or after a total of approximately 12 hours of hemodialysis; give dose after hemodialysis session