Efavirenz/emtricitabine/tenofovir, sold under the brand name Atripla among others, is a

fixed-dose combination A combination drug or a fixed-dose combination (FDC) is a medicine that includes two or more active ingredients combined in a single dosage form. Terms like "combination drug" or "combination drug product" can be common shorthand for a FDC pr ...

antiretroviral medication Antiviral drugs are a class of medication used for treating viral infections. Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. Unlike most antibiotics, antiviral drugs do n ...

used to treat

HIV/AIDS Human immunodeficiency virus infection and acquired immunodeficiency syndrome (HIV/AIDS) is a spectrum of conditions caused by infection with the human immunodeficiency virus (HIV), a retrovirus. Following initial infection an individual ...

. It contains efavirenz,

emtricitabine Emtricitabine (commonly called FTC, systematic name 2',3'-dideoxy-5-fluoro-3'-thiacytidine), with trade name Emtriva (formerly Coviracil), is a nucleoside reverse-transcriptase inhibitor (NRTI) for the prevention and treatment of HIV infection i ...

, and

tenofovir disoproxil 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 preven ...

. It can be used by itself or together with other antiretroviral medications. It is taken

by mouth Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are i ...

. 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. It should not be used in children. If used during the

first trimester Pregnancy is the time during which one or more offspring develops ( gestates) inside a woman's uterus (womb). A multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occurs by sexual intercourse, but ...

pregnancy Pregnancy is the time during which one or more offspring develops (gestation, gestates) inside a woman, woman's uterus (womb). A multiple birth, multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occur ...

harm to the baby may occur. Efavirenz/emtricitabine/tenofovir was approved for medical use in the United States in 2006, and in the European Union in 2007. It is on the

World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health s ...

. Efavirenz/emtricitabine/tenofovir is available as a generic medication.

Medical uses

Efavirenz/emtricitabine/tenofovir is indicated for the treatment of

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.

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. 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.

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.

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

History

Efavirenz/emtricitabine/tenofovir was approved in the United States as a once-daily tablet 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. 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 The Medicines Patent Pool (MPP) is a Unitaid-backed international organisation founded in July 2010, based in Geneva, Switzerland. Its public health driven business model aims to lower the prices of HIV, tuberculosis and hepatitis C medicines and ...

and Merck and Co makes efavirenz available in developing countries at a reduced price.

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

Appearance

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

References

External links

* {{DEFAULTSORT:Efavirenz Emtricitabine Tenofovir Disoproxil Bristol Myers Squibb Fixed dose combination (antiretroviral) Gilead Sciences Hepatotoxins World Health Organization essential medicines Wikipedia medicine articles ready to translate