Products
Adefovir is commercially available in tablet form (Hepsera). It has been approved in the United States since 2002, in the EU since 2003, and in many countries since 2004. It was actually originally developed to treat HIV infection, but was not approved for that purpose.
Structure and properties
Adefovir is present in the drug in the form of the diester prodrug adefovirdipivoxil (C20H32N5O8P, Mr = 501.5 g/mol) is present, which is rapidly converted to adefovir by esterases in the body. Adefovir is itself also a prodrug of the active agent adefovir diphosphate. It is an analog of adenosine monophosphate.
Effects
Adefovir (ATC J05AF08) has antiviral properties. It is phosphorylated in host cells by intracellular kinases to adefovir diphosphate and inhibits viral HBV DNA polymerase (reverse transcriptase). It is incorporated into viral DNA and, as the wrong substrate, leads to chain termination.
Indications
For the treatment of chronic hepatitis B.
Dosage
According to the SmPC. The tablets are taken once daily and independently of meals. They should be administered at the same time of day.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Adefovir undergoes glomerular filtration at the kidney and is actively secreted via organic anion transporters (OAT). In contrast, adefovir does not interact with CYP450 isozymes. It should not be administered concomitantly with tenofovir.
Adverse effects
The most common potential adverse effects include weakness, headache, abdominal pain, and nausea. Adefovir has nephrotoxic properties and may cause kidney damage and even kidney failure.
