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
Other namestenofovir disoproxil fumarate/emtricitabine/efavirenz
AHFS/Drugs.com Professional Drug Facts
License data
Pregnancy
category
Routes of
administration 		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only) [1]
  • UK: POM (Prescription only) [3]
  • US: WARNING [4] Rx-only [5]
  • EU:Rx-only [6]
  • In general: ℞ (Prescription only)
Identifiers
CAS Number
ChemSpider
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Efavirenz/emtricitabine/tenofovir, sold under the brand name Atripla among others, is a fixed-dose combination antiretroviral medication used to treat HIV/AIDS. [7] [6] It contains efavirenz, emtricitabine, and tenofovir disoproxil. [7] [6] It can be used by itself or together with other antiretroviral medications. [7] It is taken by mouth. [5] [6] [7]

Contents

Common side effects include headache, trouble sleeping, sleepiness, and unsteadiness. [5] Serious side effects may include high blood lactate levels, psychiatric symptoms, and enlargement of the liver. [5] It should not be used in children. [7] If used during the first trimester of pregnancy harm to the baby may occur. [5]

Efavirenz/emtricitabine/tenofovir was approved for medical use in the United States in 2006, [5] [8] and in the European Union in 2007. [6] It is on the World Health Organization's List of Essential Medicines. [9] Efavirenz/emtricitabine/tenofovir is available as a generic medication. [10] [11]

Medical uses

Efavirenz/emtricitabine/tenofovir is indicated for the treatment of HIV/AIDS. [5] [6]

Contraindications

People who have shown strong hypersensitivity to efavirenz, should not take efavirenz/emtricitabine/tenofovir. Drugs that are contraindicated 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. [5]

Side effects

Common side effects of efavirenz/emtricitabine/tenofovir are tiredness, dizziness, gastrointestinal distress, and skin discoloration. More severe side effects are hallucinations, sleeplessness and depression. [12]

Recommended dosage for efavirenz/emtricitabine/tenofovir is one tablet at or before bedtime. Side effects can be reduced if it is taken on an empty stomach. People with kidney or liver problems can take one 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. [13]

Interactions

Medications that should not be taken with efavirenz/emtricitabine/tenofovir include bepridil, midazolam, pimozide, triazolam, or ergot derivatives. Additionally, St. John's wort is known to reduce the effectiveness of efavirenz/emtricitabine/tenofovir, resulting in increased viral load and possible resistance to efavirenz/emtricitabine/tenofovir. [14]

Mechanism of action

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. [5]

In combination studies there were synergistic antiviral effects observed between emtricitabine and efavirenz, efavirenz and tenofovir, and emtricitabine and tenofovir. [5]

History

Efavirenz/emtricitabine/tenofovir was approved in the United States to treat HIV in 2006. The main advantage of the new drug was that it could be taken once daily and reduce the overall stress in an antiretroviral regimen. [15] 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 [16] and Merck and Co makes efavirenz available in developing countries at a reduced price. [17]

Society and culture

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. [18]

In much of the developing world marketing and distribution is handled by Merck & Co. [19]

Related Research Articles

Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some cases hepatitis B. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase that is required for replication of HIV and other retroviruses.

<span class="mw-page-title-main">Lamivudine</span> Chemical compound

Lamivudine, commonly called 3TC, is an antiretroviral medication used to prevent and treat HIV/AIDS. It is also used to treat chronic hepatitis B when other options are not possible. It is effective against both HIV-1 and HIV-2. It is typically used in combination with other antiretrovirals such as zidovudine, dolutegravir, and abacavir. Lamivudine may be included as part of post-exposure prevention in those who have been potentially exposed to HIV. Lamivudine is taken by mouth as a liquid or tablet.

<span class="mw-page-title-main">Emtricitabine</span> Antiretroviral drug used to treat HIV infection

Emtricitabine, with trade name Emtriva, is a nucleoside reverse-transcriptase inhibitor (NRTI) for the prevention and treatment of HIV infection in adults and children. In 2019, it was the 494th most commonly prescribed medication in the United States, with more than 3 thousand prescriptions.

<span class="mw-page-title-main">Tenofovir disoproxil</span> Antiviral drug used to treat or prevent HIV and hepatitis infections

Tenofovir disoproxil, sold under the trade name Viread among others, is a medication used to treat chronic hepatitis B and to prevent and treat HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for prevention of HIV/AIDS among those at high risk before exposure, and after a needlestick injury or other potential exposure. It is sold both by itself and together in combinations such as emtricitabine/tenofovir, efavirenz/emtricitabine/tenofovir, and elvitegravir/cobicistat/emtricitabine/tenofovir. It does not cure HIV/AIDS or hepatitis B. It is available by mouth as a tablet or powder.

<span class="mw-page-title-main">Efavirenz</span> Antiretroviral medication

Efavirenz (EFV), sold under the brand names Sustiva among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for prevention after a needlestick injury or other potential exposure. It is sold both by itself and in combination as efavirenz/emtricitabine/tenofovir. It is taken by mouth.

<span class="mw-page-title-main">Emtricitabine/tenofovir</span> Drug combination for HIV/AIDS prophylaxis and treatment

Emtricitabine/tenofovir, sold under the brand name Truvada among others, is a fixed-dose combination antiretroviral medication used to treat and prevent HIV/AIDS. It contains the antiretroviral medications emtricitabine and tenofovir disoproxil. For treatment, it must be used in combination with other antiretroviral medications. For prevention before exposure, in those who are at high risk, it is recommended along with safer sex practices. It does not cure HIV/AIDS. Emtricitabine/tenofovir is taken by mouth.

<span class="mw-page-title-main">Pre-exposure prophylaxis for HIV prevention</span> HIV prevention strategy using preventative medication for HIV-negative individuals

Pre-exposure prophylaxis for HIV prevention, commonly known as PrEP, is a form of medication used to prevent HIV infection, the cause of HIV/AIDS.

Integrase inhibitors (INIs) are a class of antiretroviral drug designed to block the action of integrase, a viral enzyme that inserts the viral genome into the DNA of the host cell. Since integration is a vital step in retroviral replication, blocking it can halt further spread of the virus. Integrase inhibitors were initially developed for the treatment of HIV infection, but have been applied to other retroviruses. The class of integrase inhibitors called integrase strand transfer inhibitors (INSTIs) are in established medical use. Other classes, such as allosteric integrase inhibitors (ALLINIs) or integrase binding inhibitors (INBIs), are still experimental.

<span class="mw-page-title-main">Rilpivirine</span> HIV treatment

Rilpivirine, sold under the brand names Edurant and Rekambys, is a medication, developed by Tibotec, used for the treatment of HIV/AIDS. It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs such as efavirenz.

<span class="mw-page-title-main">Cobicistat</span> Chemical compound

Cobicistat, sold under the brand name Tybost, is a medication for use in the treatment of human immunodeficiency virus infection (HIV/AIDS). Its major mechanism of action is through the inhibition of human CYP3A proteins.

Emtricitabine/rilpivirine/tenofovir is a fixed-dose combination of antiretroviral drugs for the treatment of HIV/AIDS. The drug was co-developed by Gilead Sciences and Johnson & Johnson's Tibotec division and was approved by the Food and Drug Administration in August 2011, and by the European Medicines Agency in November 2011, for patients who have not previously been treated for HIV. It is available as a once-a-day single tablet.

<span class="mw-page-title-main">Tenofovir alafenamide</span> Chemical compound

Tenofovir alafenamide, sold under the brand name Vemlidy, is an antiviral medication used against hepatitis B and HIV. It is used for the treatment of chronic hepatitis B virus (HBV) infection in adults with compensated liver disease and is given in combination with other medications for the prevention and treatment of HIV. It is taken by mouth.

Elvitegravir/cobicistat/emtricitabine/tenofovir, sold under the brand name Stribild, also known as the Quadpill, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. Elvitegravir, emtricitabine and tenofovir disoproxil directly suppress viral reproduction. Cobicistat increases the effectiveness of the combination by inhibiting the liver and gut wall enzymes that metabolize elvitegravir. It is taken by mouth.

<span class="mw-page-title-main">John C. Martin (businessman)</span>

John Charles Martin was an American billionaire businessman, and the former executive chairman (2016–2018) and CEO (1996–2016) of the American biotechnology company Gilead Sciences. He joined Gilead Sciences in 1990 as vice president for research and development. Gilead is known for developing drugs such as Atripla and commercializing Sovaldi (sofosbuvir) for the treatment of the liver virus hepatitis C. Martin is the recipient of a number of awards, including the Biotechnology Heritage Award (2017).

<span class="mw-page-title-main">Abacavir/dolutegravir/lamivudine</span> Drug combination for HIV

Abacavir/dolutegravir/lamivudine, sold under the brand name Triumeq among others, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. It is a combination of three medications with different and complementary mechanisms of action: abacavir, dolutegravir and lamivudine.

Efavirenz/lamivudine/tenofovir (EFV/3TC/TDF), sold under the brand name Symfi among others, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. It combines efavirenz, lamivudine, and tenofovir disoproxil. As of 2019, it is listed by the World Health Organization as an alternative first line option to dolutegravir/lamivudine/tenofovir. It is taken by mouth.

<span class="mw-page-title-main">Bictegravir/emtricitabine/tenofovir alafenamide</span> Fixed dose combination HIV drug

Bictegravir/emtricitabine/tenofovir alafenamide, sold under the brand name Biktarvy, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. One tablet, taken orally once daily, contains 50 mg bictegravir, 200 mg emtricitabine, and 25 mg tenofovir alafenamide.

Doravirine/lamivudine/tenofovir, sold under the brand name Delstrigo, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. It contains doravirine, lamivudine, and tenofovir disoproxil. It is taken by mouth.

Dolutegravir/lamivudine/tenofovir (DTG/3TC/TDF) is a fixed-dose combination antiretroviral medication used to treat HIV/AIDS. It is a combination of dolutegravir, lamivudine, and tenofovir disoproxil. As of 2019, it is listed by the World Health Organization (WHO) as the first line treatment for adults, with tenofovir/lamivudine/efavirenz as an alternative. It is taken by mouth.

<span class="mw-page-title-main">Lamivudine/tenofovir</span> Combination antiretroviral medication for the treatment of HIV/AIDS

Lamivudine/tenofovir disoproxil, sold under the brand name Cimduo among others, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS in adults and children weighing more than 35 kilograms (77 lb). It contains lamivudine and tenofovir disoproxil. It is taken by mouth.

References

  1. 1 2 "TGA eBS - Product and Consumer Medicine Information Licence".
  2. ↑ "Efavirenz / emtricitabine / tenofovir (Atripla) Use During Pregnancy". Drugs.com. 27 July 2018. Retrieved 31 March 2020.
  3. ↑ "Atripla 600 mg/200 mg/245 mg film coated tablets - Summary of Product Characteristics (SmPC)". (emc). 2 March 2020. Archived from the original on 10 August 2020. Retrieved 31 March 2020.
  4. ↑ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA . Retrieved 22 October 2023.
  5. 1 2 3 4 5 6 7 8 9 10 "Atripla- efavirenz, emtricitabine, and tenofovir disoproxil fumarate tablet, film coated". DailyMed. 5 November 2019. Retrieved 3 February 2020.
  6. 1 2 3 4 5 6 "Atripla EPAR". European Medicines Agency (EMA). 7 July 2008. Retrieved 31 March 2020.
  7. 1 2 3 4 5 World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. p. 160. hdl: 10665/44053 . ISBN   9789241547659.
  8. ↑ "Drug Approval Package: Atripla (Efavirenz/Emtricitabine/Tenofovir Disoproxil Fumarate) NDA #021937". U.S. Food and Drug Administration (FDA). 13 December 2006. Retrieved 25 September 2021.
  9. ↑ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl: 10665/325771 . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  10. ↑ "Office of Generic Drugs 2018 Annual Report". U.S. Food and Drug Administration (FDA). 28 January 2021. Retrieved 25 September 2021.
  11. ↑ "Efavirenz, Emtricitabine, and Tenofovir Disoproxil Fumarate: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 25 September 2021.
  12. ↑ "Possible Side Effects of Atripla". Bristol-Myers Squibb & Gilead Sciences, LLC. 2008. Retrieved 3 January 2010.
  13. ↑ "Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents" (PDF). Archived (PDF) from the original on 1 November 2016. Retrieved 19 October 2012.
  14. ↑ "Medicines You Should Not Take with Atripla". Bristol-Myers Squibb & Gilead Sciences, LLC. 2008. Archived from the original on 25 April 2010. Retrieved 3 January 2010.
  15. ↑ "HIV Medication List - AIDS Drugs". AIDS Drugs HIV Reference. aidsdrugsonline. 2009. Archived from the original on 26 December 2008. Retrieved 3 January 2010.
  16. ↑ "Medicines Patent Pool Signs Licence Agreement with Gilead to Increase Access to HIV/AIDS Medicines". Archived from the original on 19 February 2014.
  17. ↑ "HIV & AIDS Information :: Merck cuts price of efavirenz for developing countries again". 16 February 2007. Archived from the original on 19 February 2014.
  18. ↑ "Search for Tradename: Atripla". Drug Patent Watch. 2010. Archived from the original on 15 August 2011. Retrieved 3 January 2010.
  19. ↑ "Merck To Register, Lower Cost Of Antiretroviral Atripla In Developing Countries". Medical News Today. 23 February 2007. Archived from the original on 3 July 2010. Retrieved 3 January 2010.
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