Efavirenz/emtricitabine/tenofovir

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Efavirenz/emtricitabine/tenofovir disoproxil
Efavirenz, emtricitabine and tenofovir disoproxil.svg
Combination of
Efavirenz non-nucleoside reverse transcriptase inhibitor
Emtricitabine nucleoside analog reverse transcriptase inhibitor
Tenofovir disoproxil nucleotide analog reverse transcriptase inhibitor
Clinical data
Trade names Atripla, Viraday, others
AHFS/Drugs.com Professional Drug Facts
Pregnancy
category
  • US: D (Evidence of risk)
Routes of
administration
by mouth
ATC code
Legal status
Legal status
Identifiers
CAS Number
ChemSpider
  • none
KEGG
NIAID ChemDB
  (verify)

Efavirenz/emtricitabine/tenofovir, sold under the trade name Atripla among others, is a medication used to treat HIV/AIDS. It is a fixed-dose combination of efavirenz, emtricitabine, and tenofovir disoproxil. It can be used by itself or together with other antiretroviral medications. It is taken by mouth once a day.[1]

Common side effects include headache, trouble sleeping, sleepiness, and unsteadiness. Serious side effects may include high blood lactate levels, psychiatric symptoms, and enlargement of the liver.[2] It should not be used in children.[1] If used during the first trimester of pregnancy harm to the baby may occur.[2]

Efavirenz/emtricitabine/tenofovir was approved for medical use in the United States in 2006.[2] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[3] The wholesale cost in the developing world is about 10.71 to 14.19 USD per month as of 2014.[4] The wholesale cost in the United States is about 2308.20 USD a month as of 2016 while in the United Kingdom it costs the NHS GB£532.87 per month as of 2015.[5][6]

Medical uses[edit]

Combining the three drugs into a single, once-daily pill reduces pill burden and simplifies dosing schedules, and therefore has the potential to increase adherence to antiretroviral therapy.

Contraindications[edit]

People who have shown strong hypersensitivity to efavirenz, a constituent of Atripla, should not take Atripla. Drugs that are contraindicated in the intake of Atripla are: voriconazole, ergot derivative drugs, benzodiazepines midazolam and triazolam, calcium channel blocker bepridil, cisapride, pimozide and St. John’s wort (Hypericum perforatum). Breastfeeding is also contraindicated.[7]

Side effects[edit]

Common side effects of Atripla are tiredness, dizziness, gastrointestinal distress, and skin discoloration. More severe side effects are hallucinations, sleeplessness and depression.[8]

Recommended dosage for Atripla is 1 tablet at or before bedtime. Side effects can be reduced if Atripla is taken on an empty stomach. For people with kidney or liver problems can take 1 tablet by mouth once a day. However, people whose CrCl levels are less than 50ml/min should not follow this dosage. Instead, patients should be prescribed drug components of the fixed-dose combinations while adjusting TDF and FTC doses according to the patient’s CrCl levels.[9]

Interactions[edit]

Medications that should not be taken with Atripla are Vascor (bepridil), Versed (midazolam), Orap (pimozide), Halcion (triazolam), or ergot derivatives (for example, Wigraine and Cafergot)." Discuss any other HIV or hepatitis medications you are taking with your doctor to avoid complications. Additionally, St. John's wort is known to reduce the effectiveness of Atripla, resulting in increased viral load and possible resistance to Atripla.[10]

Mechanism of action[edit]

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) of HIV-1.Tenofovir is a nucleotide reverse transcriptase inhibitor of HIV-1, and it can be classified as an NtRTI. These three drugs work in combination to target the HIV reverse transcriptase protein in three ways, which reduces the virus’s capacity to mutate.[7]

In combination studies there were synergistic antiviral effects observed between emtricitabine and efavirenz, efavirenz and tenofovir, and emtricitabine and tenofovir.[7]

History[edit]

Atripla was approved as a once daily tablet to treat HIV in 2006. The main advantage of the new drug Atripla was that it could be taken once daily and reduces the overall stress in an antiretroviral regimen.[11] There is currently no generic version of Atripla available in the United States. An equivalent two pill regimen is available in developing countries at a price of about US$1.00 per day, as Gilead Sciences has licensed the patents covering emtricitabine/tenofovir to the Medicines Patent Pool[12] and Merck and Co makes efavirenz available in developing countries at a reduced price.[13]

Society and culture[edit]

It is the first multi-class antiretroviral drug available in the United States and represents the first collaboration between two U.S. pharmaceutical companies to combine their patented anti-HIV drugs into one product.[14]

In North America and Europe, Atripla is marketed jointly by Gilead Sciences and Bristol-Myers Squibb, but in much of the developing world, marketing and distribution is handled by Merck & Co.[15]

Cost[edit]

The wholesale cost in the developing world is about 10.71 to 14.19 USD per month as of 2014.[4]

Appearance[edit]

Atripla is a pink, film-coated tablet with "123" impressed on one side.

References[edit]

  1. ^ a b WHO Model Formulary 2008 (PDF). World Health Organization. 2009. p. 160. ISBN 9789241547659. Retrieved 8 December 2016. 
  2. ^ a b c "Atripla". www.drugs.com. April 2016. Retrieved 12 December 2016. 
  3. ^ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Retrieved 8 December 2016. 
  4. ^ a b "Efavirenz + Emtricitabine + Tenofovir Df". International Drug Price Indicator Guide. Retrieved 28 November 2016. 
  5. ^ "NADAC as of 2016-12-07 | Data.Medicaid.gov". Centers for Medicare and Medicaid Services. Retrieved 12 December 2016. 
  6. ^ British National Formulary (BNF) 69 (69 ed.). Pharmaceutical Press. 2015. p. 423. ISBN 9780857111562. 
  7. ^ a b c Atripla [package insert]. Wallingford Center, CT: Bristol-Myers Squibb and Gilead Sciences, LLC; 2011 Sep., .
  8. ^ "Possible Side Effects of ATRIPLA". Bristol-Myers Squibb & Gilead Sciences, LLC. 2008. Retrieved 2010-01-03. 
  9. ^ "Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents." (PDF). Retrieved 19 October 2012. 
  10. ^ "Medicines You Should Not Take with ATRIPLA". Bristol-Myers Squibb & Gilead Sciences, LLC. 2008. Retrieved 2010-01-03. 
  11. ^ "HIV Medication List - AIDS Drugs:". AIDS Drugs HIV Reference. aidsdrugsonline. 2009. Archived from the original on December 26, 2008. Retrieved 2010-01-03. 
  12. ^ "Medicines Patent Pool Signs Licence Agreement with Gilead to Increase Access to HIV/AIDS Medicines". 
  13. ^ "HIV & AIDS Information :: Merck cuts price of efavirenz for developing countries again". 
  14. ^ "Search for Tradename: Atripla". Drug Patent Watch. 2010. Retrieved 2010-01-03. 
  15. ^ "Merck To Register, Lower Cost Of Antiretroviral Atripla In Developing Countries". Medical News Today. 23 February 2007. Archived from the original on 2010-07-03. Retrieved 2010-01-03. 

External links[edit]