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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C20H32N5O8P
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RX_link
http://www.rxlist.com/cgi/generic3/hepsera.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
No information avaliable
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Molecular Weight
501.471 g/mol
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Melting Point
No information avaliable
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H2O Solubility
19 mg/mL at pH 2.0 and 0.4 mg/mL at pH 7.2.
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State
Solid
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LogP
3.649
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Dosage Forms
Tablet (10 mg)
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Indication
For the treatment of chronic hepatitis B in adults with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease.
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Pharmacology
Adefovir dipivoxil a diester prodrug of adefovir. Adefovir is an acyclic nucleotide analog with activity against human hepatitis B virus (HBV). The concentration of adefovir that inhibited 50% of viral DNA synthesis (IC50) in vitro ranged from 0.2 to 2.5 μM in HBV transfected human hepatoma cell lines. The combination of adefovir with lamivudine showed additive anti-HBV activity.
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Absorption
Approximate oral bioavailability is 59%.
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side effects and Toxicity
Renal tubular nephropathy characterized by histological alterations and/or increases in BUN and serum creatinine was the primary dose-limiting toxicity associated with administration of adefovir dipivoxil in animals. Nephrotoxicity was observed in animals at systemic exposures approximately 3–10 times higher than those in humans at the recommended therapeutic dose of 10 mg/day.
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Patient Information
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Organisms Affected
Hepatitis B virus