化合物详情

CAS106941-25-7

分子式C8H12N5O4P

分子量273.19 g/mol g/mol

危化品

Adefovir is a member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection. It has a role as an antiviral drug, a drug metabolite, a nephrotoxic agent, a HIV-1 reverse transcriptase inhibitor and a DNA synthesis inhibitor. It is a member of 6-aminopurines, an ether and a member of phosphonic acids. It is functionally related to an adenine. It is a conjugate acid of an adefovir(1-).

科学粮草官-词典编辑部，修订于：2026-07-06

Toxicity

Interactions

Adefovir should not be used concurrently with VIREAD (tenofovir disoproxil fumarate) or tenofovir disoproxil fumarate-containing products including TRUVADA (emtricitabine/tenofovir disoproxil fumarate combination tablet), ATRIPLA (efavirenz/emtricitabine/tenofovir disoproxil fumarate combination tablet) and COMPLERA (emtricitabine/rilpivirine/tenofovir disoproxil fumarate).

Hepatotoxicity

Likehood score: E (unlikely cause of clinically apparent, idiosyncratic liver injury).

Human Toxicity Excerpts

/CASE REPORTS/ Fanconi syndrome results from generalised renal tubular toxicity and, owing to phosphate wasting can cause hypophosphatemic osteomalacia. /Investigators/ diagnosed Fanconi syndrome in conjunction with severe osteomalacia in 2 hepatitis B-positive patients on standard-dose adefovir therapy. The first patient was a 40-year-old male with a 5 month history of bone pain involving his knees, ankles, and ribs. He had been receiving adefovir dipivoxil for 27 months before the development of hypophosphataemia, urinary phosphate wasting, and aminoaciduria. These abnormalities resolved within weeks of discontinuation of adefovir dipivoxil and supplementation with elemental phosphate, calcium carbonate, and cholecalciferol. The second patient was a 53-year-old female with a 6 month h...

Drug Induced Liver Injury

References: DOI:10.1016/j.drudis.2019.09.022

Non-Human Toxicity Excerpts

/LABORATORY ANIMALS: Developmental or Reproductive Toxicity/ Animal reproduction studies were conducted in rats and rabbits with orally administered adefovir dipivoxil and intravenously administered adefovir. In rats and rabbits, no embryotoxicity or teratogenicity was shown from oral administration of adefovir dipivoxil at maternal doses producing systemic exposures approximately 23 times (rats) and 40 times (rabbits) that achieved in humans at the therapeutic dose of 10 mg/day.

Populations at Special Risk

In patients at risk of or having underlying renal dysfunction, chronic administration of adefovir may result in nephrotoxicity. These patients should be monitored closely for renal function and may require dose adjustment.

Antidote and Emergency Treatment

/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use...

Effects During Pregnancy and Lactation

◉ Effects on Lactation and Breastmilk