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tenofovir (TDF)

Indications: - HIV/AIDS (FDA approved 2001) - acceptable alternative for use during pregnancy [10] - 1% tenofovir gel used intravaginally before & after sex reduces incidence of - HIV1 by up to 54% [6] - not so in VOICE trial: (see Clinical trials below) - HSV2 by ~ 50% [12] - chronic hepatitis B Dosage: - 300 mg PO QD 1% tenofovir gel Storage: - store in orginal container - original container (tabs, oral powder) has a desiccant [11] Monitor: renal function Adverse effects: 1) reportedly fewer adverse effects that with other nucleoside reverse transcriptase inhibitors 2) tenofovir associated with fewer cardiovascular deaths than avacavir [5] 3) nephrotoxicity* (tubulointerstitial disease) due to mitochondrial damage within renal tubular cells a) associated with tenofovir disoproxil fumarate* b) renal tubular acidosis type 2 c) glycosuria despite normal serum glucose (Fanconi syndrome) d) mild proteinuria e) discontinue tenofovir 1] recovery of renal function within weeks to months 2] chronic renal failure possible e) Fanconi syndrome [8] 4) decreased bone mineral density* 5) nausea [8] * novel formulation tenofovir alafenamide, component of Genvoya may be associated with less nephrotoxicity & less effects on bone mineral density [13] Drug interactions: - reportedly fewer drug interactions that with other nucleoside reverse transcriptase inhibitors Laboratory: - tenofovir in serum/plasma Mechanism of action: 1) nucleoside reverse transcriptase inhibitor 2) reportedly less likely than other nucleoside reverse transcriptase inhibitors to develop resistance 3) report of effectiveness in resistant HIV [2] 4) has activity against hepatitis B virus [8] Clinical trials: - VOICE trial: tenofovir gel did no better than placebo in preventing sexual transmission of HIV in women [7] Manufacturer: Gilead Sciences

Interactions

drug interactions drug adverse effects of antiretroviral agents

Related

Acquired Immuno-Deficiency Syndrome (HIV infection stage 3, AIDS)

Specific

tenofovir disoproxil fumarate (Viread)

General

nucleoside reverse transcriptase inhibitor (NRTI)

Properties

MISC-INFO: elimination route KIDNEY

Database Correlations

PUBCHEM correlations

References

  1. Prescriber's Letter 8(12):70 2001
  2. Journal Watch 23(20):158, 2003 Squires K et al, Ann Intern Med 139(Sep 2):313, 2003
  3. Department of Veterans Affairs, VA National Formulary
  4. Centers for Disease Control CDC trials of daily oral tenofovir for preventing HIV infection http://www.cdc.gov/hiv/PUBS/TenofovirFactSheet.htm
  5. Martin A et al Simplification of antiretroviral therapy with t enofovir-emtricitabine or abacavir-lamivudine: A randomized, 96-week trial. Clin Infect Dis 2009 Nov 15; 49:1591. PMID: 19842973
  6. Abdool KQ et al, Effectiveness and safety of tenofovir gel, an antiretroviral microbicide, for the prevention of HIV infection in women. Science 2010 Jul 19 PMID: 20643915 http://www.sciencemag.org/cgi/content/abstract/science.1193748v1
  7. Sax PE HIV and ID Observations Journal Watch Blogs Massachusetts Medical Society http://blogs.jwatch.org
  8. Medical Knowledge Self Assessment Program (MKSAP) 16, 17, 18. American College of Physicians, Philadelphia 2012, 2015, 2018.
  9. Izzedine H, Harris M, Perazella MA. The nephrotoxic effects of HAART. Nat Rev Nephrol. 2009 Oct;5(10):563-73 PMID: 19776778
  10. Zuger A Use of Antiretroviral Drugs in Pregnancy. Physician's First Watch, April 22, 2014 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. 2014. AIDSinfo. Clinical Guidelines Portal. March 28, 2014. http://aidsinfo.nih.gov/Guidelines/HTML/3/perinatal-guidelines/0 (corresponding NGC guideline withdrawn March 2016)
  11. Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: 300622 (subscription needed) http://www.prescribersletter.com
  12. Abdool Karim SS et al Tenofovir Gel for the Prevention of Herpes Simplex Virus Type 2 Infection. N Engl J Med 2015; 373:530-539. August 6, 2015 PMID: 26244306 http://www.nejm.org/doi/full/10.1056/NEJMoa1410649
  13. FDA News Release. November 5, 2015 FDA approves new treatment for HIV http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm471300.htm
  14. Tourret J, Deray G, Isnard-Bagnis C. Tenofovir effect on the kidneys of HIV-infected patients: a double-edged sword? J Am Soc Nephrol. 2013 Oct;24(10):1519-27. Review. PMID: 24052632 Free PMC Article

Component-of

bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy, Symtuza) cobicistat/darunavir/emtricitabine/tenofovir cobicistat/elvitegravir/emtricitabine/tenofovir (Quad, Stribild, Genvoya) doravirine/lamivudine/tenofovir efavirenz/emtricitabine/tenofovir (Atripla) efavirenz/lamivudine/tenofovir emtricitabine/rilpivirine/tenofovir DF (FTC/RPV/TDF, TAF/FTC/RPV, Complera, Odefsey) emtricitabine/tenofovir (Truvada, TDF/FTC, Descovy)