Standard DoseOne 600 mg tablet once daily, preferably on an empty stomach at bedtime. Must be taken in combination with another antiretroviral(s) that does not contain this medication or medication from the same drug class. Lower 400 mg dose available in the single-tablet regimen Symfi Lo (where it is combined with tenofovir DF and lamivudine; see Symfi Lo page).
Approved for adults and children 3 months and older weighing at least 7.7 pounds (3.5 kg). DHHS guidelines, however, do not recommend use for children aged 3 months up to three years or weighing less than 28.5 pounds (13 kg), due to issues with drug levels; see pediatric guidelines. For children weighing less than 88 pounds (40 kg), the dose is based on weight. See package insert for specific weight-based dosing. For children weighing at least 88 pounds, use the standard adult dose. For those who can’t swallow capsules, administer by capsule sprinkle method. See drug label for instructions or watch the video at sustiva.com.
Take missed dose as soon as possible, unless it is closer to the time of your next dose. Do not double up on your next dose. Also available in 50 mg and 200 mg capsules.
Use with caution in mild liver impairment; not recommended with moderate or severe liver impairment.
- See package insert for more complete information on potential side effects and interactions.
AWPSustiva 600 mg, 30 tablets: $1,176.74/month
generic: 600 mg, 30 tablets: $1,073.18/month
generic: 200 mg, 90 tablets: $1,059.07/month
generic: 50 mg, 30 tablets: $88.31/month
Potential Side Effects and Toxicity
Central nervous system (CNS) side effects (dizziness, insomnia, impaired concentration, abnormal or vivid dreams, and hallucinations) are most common at the start of treatment and usually diminish in two to four weeks. Bedtime dosing on an empty stomach can help reduce symptoms. Less common psychiatric symptoms (catatonia, depression, suicidal thoughts or actions, aggression, paranoid/manic reactions) may also occur. A 2014 study reviewed four previously published AIDS Clinical Trials Group (ACTG) studies regarding efavirenz and suicidal ideation and re-emphasized efavirenz has an association with suicidality (reported suicidal ideation or attempted or completed suicide), and should be used with caution in people with severe or uncontrolled depression and/or a history of suicidality. It is recommended for anyone on a regimen containing efavirenz to be regularly screened for depression and suicidality. Additional side effects may include rash (incidence of up to 26% of adults and 32% of pediatric patients), nausea, vomiting, diarrhea, fever, and gynecomastia (breast development in men). Rash among children is more common and more severe. Efavirenz may raise levels of triglycerides (fat in the blood) and cholesterol. Efavirenz can cause a false positive for marijuana on certain drug tests. A more specific confirmatory test can be done. A link to birth defects in humans was not supported by meta-analyses. Individuals in their first trimester of pregnancy are recommended to continue taking efavirenz as long as their viral load remains undetectable; however, efavirenz should only be used if the potential benefit outweighs the potential risk, as when other treatment options are not available. Because of the association with suicidality and neuropsychiatric effects, it is also recommended to screen for antenatal and postpartum depression in women with HIV who are taking a regimen containing efavirenz. Regular monitoring for increased liver enzyme levels is recommended initially and during treatment for people with hepatitis B/C or liver disease.
Potential Drug Interactions
Do not take with midazolam, pimozide, ergot derivatives, St. John’s wort, or triazolam. May affect warfarin levels. Can decrease levels of buprenorphine and methadone—monitor for withdrawal. Increase Kaletra to two 200/50 mg tablets plus one 100/25 mg tablet twice daily (total 500/125 mg twice daily) (or 520/130 mg twice daily for oral solution) with food when taken with Sustiva. Kaletra cannot be taken once daily with Sustiva. When taken with Tivicay, increase the Tivicay dose to 50 mg twice daily. Treatment-experienced people should not take Reyataz with Sustiva, but for treatment-naïve people, Reyataz once-daily dose should be 400 mg boosted with Norvir. Increase Selzentry to 600 mg twice daily. Increase the Sustiva dose to 800 mg once daily with rifampin for people weighing 110 pounds (50 kg) or more. Rifabutin can be used as an alternative, but dose adjustment is needed. Should not be used with abacavir and lamivudine in people with baseline HIV viral load over 100,000 copies/mL due to increased risk for virologic failure in this group. When taken with carbamazepine, phenobarbital, or phenytoin, periodic monitoring of anticonvulsant and Sustiva levels should be done or alternative antiseizure drugs, such as levetiracetam, should be considered. May decrease effectiveness of birth control pills; consider the use of other contraceptives. Closer monitoring and dose adjustments may be required with posaconazole (avoid unless benefit outweighs potential risk) and itraconazole. The dose of voriconazole should be increased to 400 mg every 12 hours and the Sustiva dose should be decreased to 300 mg once daily using capsules; tablets should not be broken. Monitor effectiveness of clarithromycin or consider using azithromycin instead. Levels of immunosuppressants should be monitored when starting or stopping Sustiva. Cardizem, Lipitor, Pravachol, and Zocor doses may need to be adjusted. Titrate dose of bupropion and sertraline based on clinical response. Should not be taken with other medications that prolong QT interval or medications with a known risk for torsades de pointes. No dose adjustment with Harvoni. Don’t take with Epclusa or Zepatier. Tell your provider or pharmacist about all medications, herbals, and supplements you are taking or thinking of taking, prescribed or not, as there are other drug interactions that are not listed here.
If you can’t sleep, ask your doctor about gradually adjusting the timing of your dose until it’s taken during the day. A rare genetic trait affecting drug metabolism of Sustiva, leading to a higher rate of side effects, occurs more in African Americans. In pediatric HIV guidelines, Sustiva was downgraded in 2017 from “preferred” to an “alternative” component of an initial regimen for children ages 3–12 years. For individuals with HIV-2, commonly found in some other countries, an NNRTI would not be recommended as HIV-2 is inherently resistant to NNRTIs. Efavirenz is found in the single-tablet regimens Atripla, Symfi, and Symfi Lo (see those pages).
Dr. Melanie Thompson:
Efavirenz-based regimens are no longer recommended for initial therapy due to multiple side effects, many of them affecting the central nervous system (see Atripla, Symfi and Symfi Lo). It also raises cholesterol and triglycerides, and has substantial drug-drug interactions that must be managed. Also, efavirenz should be taken on an empty stomach for best absorption. When used, it should only be given with TDF or TAF + FTC or 3TC. There is little rationale for prescribing efavirenz-based regimens at this time, although it is still recommended during pregnancy.
Activist Michael Broder:
Sustiva breathed new life into the NNRTI class when it was on life support in the wake of bad pharmacology (delavirdine) and bad marketing (nevirapine). But it causes serious neurologic side effects such as nightmares, depression, and suicidal ideation that can make it difficult to tolerate. It must be taken on an empty stomach, meaning one hour before a meal, or two hours after a meal. Given other available options, Sustiva is not an obvious first choice for most people nowadays. If your provider recommends Sustiva, they may have a good reason, but make sure they tell you what it is.