Brand name: Sustiva
Generic name: efavirenz, or EFV
Class: Non-nucleoside reverse transcriptase inhibitor (non-nucleoside, NNRTI, or non-nuke)
Manufacturer: Bristol-Myers Squibb, www.sustiva.com, (800) 321-1335
AWP: $729.99/month for 600 mg tablets
Standard Dose: One 600 mg tablet, once a day, typically at bedtime, on an empty stomach or with a light, low-fat snack. Is also available in smaller 50 mg and 200 mg capsules. Approved for children 3 years and older. Strawberry/mint flavored solution available for children under expanded access program. Take missed dose as soon as possible, unless it is closer in time to your next dose. Do not double up on your next dose.
Potential side effects and toxicity: Central nervous system (CNS) or psychiatric symptoms (dizziness, insomnia, impaired concentration, drowsiness, abnormal dreams, hallucinations, severe depression, suicidal thoughts or actions, aggressive behavior, paranoid reactions, and manic reactions). These symptoms typically diminish within four weeks. Patients with a history of drug or alcohol use, psychiatric illness, or who are taking psychiatric medications may be at an increased risk for these reactions. Other side effects may include rash, nausea, vomiting, diarrhea, fever, and increased liver enzymes. These symptoms may occur early and generally resolve within two to four weeks. Rash is more common, and more severe, in children, as are low levels of some blood cells. May raise levels of triglycerides and cholesterol. May lead to false positive urine tests for use of marijuana, but more specific tests can differentiate between marijuana and Sustiva. Women taking Sustiva should not become pregnant or breast-feed. See "More information." Increases in liver enzymes in people with hepatitis B and/or C can occur and should be monitored. Use with caution in people with mild liver impairment; not recommended for people with moderate or severe liver impairment. See chart for potential drug class side effects.
Potential drug interactions: Non-nukes interact with many other drugs. See package insert for the most complete list. Tell your provider or pharmacist about all medications, herbs, and supplements you are taking or thinking of taking, prescribed or not. Do not take with Atripla, Complera, Edurant, Intelence, Rescriptor, or Viramune. Do not take the following medications with Sustiva: midazolam, triazolam, pimozide, bepridil, or Biaxin, or the herbs St. John's wort and Gingko biloba. Sustiva may affect Coumadin (warfarin) levels. Sustiva decreases methadone levels; dose adjustment may be necessary to avoid withdrawal symptoms. Increase Kaletra to three tablets twice daily with food (recommended) when taken with Sustiva in treatment-experienced people. Kaletra cannot be taken once daily with Sustiva. Monitor liver enzymes closely if Sustiva and Norvir are used together. Reyataz once-daily dose should be higher (400 mg) and also boosted with Norvir when taken with Sustiva, but treatment-experienced people should not take this combination at all. With once-daily Lexiva, boost with 300 mg Norvir. Rifampin decreases Sustiva levels, so increase the Sustiva dose to 800 mg once daily for people weighing 110 pounds or more. Rifabutin can be used as an alternative to rifampin but double the dose. When taken with anticonvulsants Dilantin, phenobarbital, or Tegretol, periodic monitoring of blood levels of anticonvulsants and Sustiva should be done or alternative anti-seizure medications considered. Effectiveness of birth control pills may be decreased; consider the use of additional or alternative contraceptive method. The maintenance dose of Noxafil, Sporanox, and Vfend should be increased to 400 mg every 12 hours and the Sustiva dose should be decreased to 300 mg once daily using the capsule formulation. Levels of immunosuppressants (used in transplants, specific types of arthritis, and autoimmune conditions) can be decreased and should be monitored when starting or stopping Sustiva. When taking Sustiva with Zoloft, Lipitor, pravastatin, simvastatin, and diltiazem, their doses may need to be adjusted. The levels of bupropion and sertraline are lowered; titrate dose based on clinical response. Sustiva can decrease levels of buprenorphine. No dose adjustment is recommended, but monitor for withdrawal symptoms. Sustiva can decrease the effects of Malarone; consider alternative drug. Avoid taking Sustiva with the hepatitis C drug Victrelis (boceprevir), as Sustiva lowers Victrelis concentrations.
More information: According to current guidelines for adults and adolescents, Sustiva is the preferred NNRTI drug for NNRTI-based regimens. Avoid driving or operating heavy machinery for a few hours after dose. Some people adjust to Sustiva by taking Ativan or Ambien to sleep for the first few weeks, though you may feel even more groggy the next morning. If you can't sleep, ask about switching the timing of your dose little by little until you're taking it in the daytime. Based on the HIV pregnancy registry, very few infants born to women who have become pregnant while on efavirenz have had birth defects. Most birth defects occurred when exposure to efavirenz was in the first trimester. See package insert for more complete information on potential side effects and interactions.
Ten years after its approval in 2002, Sustiva (as well as Atripla, the combination of efavirenz, tenofovir, and emtricitabine) remains a preferred drug in all treatment guidelines. Besides its excellent potency and long-term safety, it also has a very long half-life, which makes it forgiving of missed or delayed doses (not that you would ever miss or delay a dose!). Its flaws, however, include "neuropsychiatric" side effects (dizziness, vivid dreams or nightmares, difficulty concentrating, and mood changes) and allergic rashes, all of which are common during the first few weeks, though they generally go away without having to stop the drug. Once you're been on Sustiva for three to four weeks, it's usually smooth sailing, though it can raise lipid levels. When starting Sustiva or Atripla, take it in the evening on an empty stomach (at least two hours after dinner) to minimize side effects. Start it on a weekend or on an evening when you have nothing important to do for the next few mornings. In most cases, things get better with each dose, so stick with it. But if you don't feel like your normal self after a month on Sustiva or Atripla, it's time for a change. Some people may have persistent neurologic side effects, including depression. It's easy to become resistant to Sustiva, so don't stop this drug unless you're replacing it with something else. Sustiva can cause birth defects; pregnant women should avoid it during the first trimester.
-- Joel Gallant, M.D., M.P.H.
Sustiva is the king of the non-nukes! This powerhouse has major benefits and major downsides. Convenient once-daily dosing of Sustiva has been studied more than any other drug, and has beaten the best of them in terms of durability and effectiveness. All is not rosy though, as the downside is pretty scary for those with side effects. It can cause vivid dreams, nightmares, depression, out of range levels for lipids, cholesterol, and even risk of possible bone problems down the road make this drug not suitable for everyone. It has meal restrictions and definitely cannot be taken by women who are pregnant or thinking about having children.
-- Joey Wynn