Emtricitabine/tenofovir/efavirenz
| Combination of | |
|---|---|
| Tenofovir | Nucleotide analogue reverse transcriptase inhibitor |
| Emtricitabine | Nucleoside reverse transcriptase inhibitor |
| Efavirenz | Non-nucleoside reverse transcriptase inhibitor |
| Clinical data | |
| Pregnancy cat. | D (US) |
| Legal status | POM (UK) ℞-only (US) |
| Routes | Oral |
| Identifiers | |
| CAS number | 731772-50-2  |
| ATC code | J05AR06 |
| NIAID ChemDB | 026223 |
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Emtricitabine/tenofovir/efavirenz (INNs, trade name Atripla) is a fixed-dose combination drug for the treatment of HIV infection. It combines Gilead Sciences's tenofovir and emtricitabine (already available in the anti-HIV combination Truvada) with Bristol-Myers Squibb's efavirenz into a fixed-dose pill. 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.
Atripla 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.[1] The drug retails in the United States for US$1,850 for a one-month supply. As of 2007, annual cost in India is US$1,344, and US$528 in Africa. It was approved by the U.S. FDA on July 12, 2006. In the UK, the drug cost to the NHS is GB£620 per month.
Atripla is a fixed dose combination of 600 mg efavirenz, 300 mg tenofovir, and 200 mg emtricitabine. In adults, it is taken once daily on an empty stomach. Dosing at bedtime is recommended to improve tolerability of nervous system symptoms. Atripla is not recommended for patients under 18 years of age.
Atripla is a pink, capsule-shaped tablet with "123" impressed on one side.
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.[2] Cipla released its own version of Atripla in India, called Viraday. In Argentina, Atripla is marketed by Laboratorios Gador.
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[edit] Background
Atripla was approved as a once daily tablet to treat HIV in 2006. The main advantage of the new drug Atripla was that could be taken once daily and reduces the overall stress in an antiretroviral regimen.[3] There is currently no generic version of Atripla available in the United States, but countries like Brazil and India are involved with compulsory licensing. The main advantage for these countries in producing a generic Atripla (Viraday) is they can sell it domestically at a radically lower cost than the price of the United States version. India is currently a signatory to TRIPS and consequently there will be a drop in the amount of generic HIV medicines available.
[edit] Mechanism of Action
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRT) of HIV-1. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) of HIV-1.Tenofovir is a nucleotide reverse transcriptase inhibitor of HIV-1, but it can be classified as a NRTI. These three drugs work in combination to target HIV at different point in its life cycle and it reduces the virus’s capacity to mutate.[4]
Antiviral activity In combination studies there were synergistic antiviral effects observed between emtricitabine and efavirenz, efavirenz and tenofovir, and emtricitabine and tenofovir.[4]
[edit] Side effects
Common side effects of Atripla are tiredness, dizziness, gastrointestinal distress, and skin discoloration. More severe side effects are hallucinations, sleeplessness and depression.[5]
[edit] Interactions
Medications that should not be taken with Atripla are "Hismanal (astemizole), Vascor (bepridil), Propulsid (cisapride), 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.[6]
[edit] Contraindications
Patients 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.[6]
[edit] References
- ^ "Search for Tradename: Atripla". Drug Patent Watch. 2010. http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=Atripla. Retrieved 2010-01-03.
- ^ "Merck To Register, Lower Cost Of Antiretroviral Atripla In Developing Countries". Medical News Today. 23 February 2007. http://www.medicalnewstoday.com/articles/63612.php. Retrieved 2010-01-03.
- ^ "HIV Medication List - AIDS Drugs:". AIDS Drugs HIV Reference. aidsdrugsonline. 2009. http://www.aidsdrugsonline.com/index.php?option=com_content&view=article&id=50&Itemid=27. Retrieved 2010-01-03. [dead link]
- ^ a b Atripla [package insert]. Wallingford Center, CT: Bristol-Myers Squibb and Gilead Sciences, LLC; 2011 Sep., .
- ^ "Possible Side Effects of ATRIPLA". Bristol-Myers Squibb & Gilead Sciences, LLC. 2008. http://www.atripla.com/Content.aspx?bmscontentpg=atripla-side-effects. Retrieved 2010-01-03.
- ^ "Medicines You Should Not Take with ATRIPLA". Bristol-Myers Squibb & Gilead Sciences, LLC. 2008. http://www.atripla.com/Content.aspx?bmscontentpg=hiv-medications. Retrieved 2010-01-03.
[edit] External links
- Atripla.com managed by Gilead Sciences and Bristol-Myers Squibb
- Atripla article on The Body, an HIV reference site
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