Адефовир

Химические свойства

Pale Brown Solid

Использование

Adefovir has been used to study its anti-retro viral effect on porcine endogenous retrovirus (PERV) activity.

Приобретенная устойчивость

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.

Фармацевтические приложения

A nucleotide analog of adenosine monophosphate, administered orally as its prodrug, adefovir dipivoxil.

Фармакокине?тика

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 P₄₅₀ at standard doses and does not influence the metabolism or plasma concentrations of the other licensed medications used in the treatment of hepatitis B.

Клиническое использование

Treatment of chronic hepatitis B virus infection in patients >12 years of age

Побочные эффекты

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.