アデホビル 化学特性,用途語,生産方法
効能
抗ウイルス薬, 逆転写酵素阻害薬
化学的特性
Pale Brown Solid
使用
Adefovir has been used to study its anti-retro viral effect on porcine endogenous retrovirus (PERV) activity.
獲得抵抗性
It has a lower propensity to induce drug resistance than lamivudine.
Clinical trials of patients receiving 48 weeks of therapy
did not identify any cases of resistance. Longer courses
yield resistant strains of HBV with mutations in the DNA
polymerase gene; other rare variants of resistant strains have
been identified. Lamivudine-resistant strains of HBV retain
susceptibility to adefovir.
応用例（製薬）
A nucleotide analog of adenosine monophosphate, administered
orally as its prodrug, adefovir dipivoxil.
薬物動態学
Oral absorption： c. 60%
C
max 10 mg/kg oral： 18.4 ng/mL
Plasma half-life： c. 7.5 h.
Volume of distribution： 392 mL/kg
Plasma protein binding： Not known
The prodrug is metabolized to adefovir, which is excreted by the kidneys and therefore requires dose adjustment in patients with impaired renal function. It does not induce cytochrome P
450 at standard doses and does not influence the metabolism or plasma concentrations of the other licensed medications used in the treatment of hepatitis B.
臨床応用
Treatment of chronic hepatitis B virus infection in patients >12 years
of age
副作用
It is generally well tolerated, with headache, pharyngitis,
abdominal pain and peripheral neuropathy being the most
common side effects. Nephrotoxicity has been observed in
some patients, with those receiving higher doses and longer
courses of therapy at greater risk. Exacerbation of hepatitis
has been reported in patients immediately following discontinuation
of treatment. Most exacerbations occur within 12
weeks of stopping therapy, and elevations of alanine aminotransferase
(ALT) up to 10 times the upper limit of normal
can be observed in over 25% of patients. Lactic acidosis has
been reported in a few patients and is an indication for immediate
discontinuation.
アデホビル 上流と下流の製品情報
原材料
準備製品