Tenofovir

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Information about Tenofovir

Tenofovir disoproxil fumarate is an acyclic nucleotide analogue of adenosine used in combination with other agents in the therapy of the human immunodeficiency virus (HIV) and as single agent in hepatitis B virus (HBV) infection.

Liver safety of Tenofovir

Tenofovir does not appear to be a significant cause of drug induced liver injury.

Mechanism of action of Tenofovir

Tenofovir (ten of' oh vir) is an acyclic nucleotide analogue of adenosine, but is poorly absorbed orally. For this reason, the prodrug–tenofovir disoproxil fumarate–is used, which is well absorbed from the intestines, rapidly hydrolyzed to tenofovir intracellularly and then phosphorylated to the active form, tenofovir diphosphate. Tenofovir diphosphate is a competitive inhibitor of the HIV reverse transcriptase (and the HBV polymerase) and is also incorporated into the nascent DNA strand causing chain termination.

FDA approval information for Tenofovir

Tenofovir was approved for use in HIV infection in the United States in 2001 and for use in hepatitis B in 2008. Clinical indications include treatment and prevention of HIV infection, usually in combination with other reverse transcriptase or protease inhibitors. Tenofovir is also approved for use in chronic hepatitis B as a single agent.

Dosage and administration for Tenofovir

Tenofovir is available under the brand name Viread in 300 mg oral tablets. Tenofovir is also available in various fixed combinations with other antiviral agents for use in treatment of HIV infection, usually in a single oral daily dose: with emtricitabine as Truvada in 300/200 mg oral tablets; with emtricitabine and efavirenz as Atripla in 300/200/600 mg oral tablets; with emtricitabine and rilpivirine as Complera in 300/200/25 mg oral tablets; and, with emtricitabine, elvitegravir and cobicistat as Stribild in 300/200/150/150 mg oral tablets. The recommended dose of tenofovir in adults is 300 mg once daily.

Side effects of Tenofovir

Side effects are uncommon; they include asthenia, diarrhea, flatulence, nausea and vomiting, renal dysfunction and rash.

Antiviral agents

Drugs for HIV Infection, in the Subclass Antiretroviral Agents

Drugs for Hepatitis B

Drugs for Hepatitis C

HCV NS5A Inhibitors

HCV NS5B (Polymerase) Inhibitors

HCV Protease Inhibitors

Combination Therapies

Drugs for Herpes Virus Infections (HSV, CMV, others)

Drugs for Influenza

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