POSITIVELY AWARE MARCH/APRIL 2011
brand name: Sustiva
common name: efavirenz
class: Non-nucleoside reverse transcriptase inhibitor
(non-nucleoside, NNRTI, or non-nuke)
manufacturer: Bristol-Myers Squibb | www.sustiva.com; (800) 321-1335
Standard dose: One 600 mg tablet, once a day, typically at bedtime; on an empty stomach or with a light, low-fat snack. 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 almost time for your next dose. Do not double up on your next dose.
AWP: $663.00 / month for 600 mg tablets
Potential side effects and toxicity
Central nervous system (CNS) or psychiatric symptoms (dizziness, headache, memory loss, somnolence, hypnotic trance, confusion, insomnia, hallucinations, vivid or abnormal dreams or nightmares, depression, euphoria or mania, and agitation). These symptoms typically diminish within four weeks. Other side effects may include rash, nausea, vomiting, diarrhea, fever, and increased liver enzymes. These symptoms occur early and generally resolve within two to four weeks. A serious side effect of the NNRTI class is rash, which can be life-threatening. Rash is more common, and more severe, in children, as are low levels of some blood cells. May raise levels of triglycerides, and both “good” and “bad” cholesterol. May lead to false positive tests for use of marijuana. Women taking Sustiva should not become pregnant or breast-feed because of the risk of birth defects. 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.
Potential drug interactions
Do not take with Atripla, since Sustiva is already in Atripla. Do not take with Intelence, Rescriptor, rilpivirine, or Viramune. Do not take the following medications with Sustiva: midazolam, triazolam, ergot medications (Wigraine, Methergine, and Cafergot), St. John’s wort, Gingko biloba, pimozide, bepridil, or Biaxin. May affect Coumadin therapy. Sustiva decreases methadone levels; dosing 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 due to potential risk of liver damage. Reyataz dose should be higher and also boosted with Norvir (Reyataz 400 mg/Norvir 100 mg once daily) 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 concentrations, so maintain 600 mg once-daily dose and monitor. Rifabutin levels are decreased, so daily dose of rifabutin should be increased by 50%. When taken with anticonvulsants Dilantin, phenobarbital, or Tegretol, periodic monitoring of blood levels of anticonvulsants and Sustiva should be performed or alternative anti-seizure medications should be considered. Can affect birth control pill levels, so a second barrier contraceptive method is advised. Sustiva can lower the concentrations of Sporanox, Noxafil, immunosuppressants (including transplant drugs), Zoloft, Lipitor, pravastatin, simvastatin, and diltiazem. Dose adjustment may be needed. The maintenance dose of 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. Drug 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.
More information
According to current U.S. guidelines, when choosing an NNRTI-based regimen, Sustiva is the preferred drug. 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. However, either may make you even more groggy the next morning. If you can’t sleep (which more commonly develops later), ask about switching the timing of your dose little by little until you’re taking it in the daytime. It is usually recommended that you continue your other HIV medications for several days after stopping Sustiva to avoid developing resistance. Sustiva remains a class D drug and should not be used in women planning pregnancy or started in pregnant women during the first trimester. According to one meta-anyalysis, if women get pregnant while on Sustiva or Atripla, however, the concern for birth defects is minimal. See package insert for more complete information on potential side effects and interactions.
Doctor’s comments
Nine years after its approval in 2002, Sustiva (as well as Atripla, the combination of Sustiva, Viread, and Emtriva) has still never been beaten in clinical trials, and remains a preferred drug in all treatment guidelines. Besides its excellent potency, 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!), and excellent long-term safety. Its flaws, however, include “neuropsychiatric” side effects, (dizziness, vivid dreams or nightmares, difficulty concentrating, and mood changes) and allergic rashes, also common during the first few weeks, though they generally go away without having to stop the drug. Sustiva can cause birth defects; pregnant women should avoid it during the first trimester. Once you’re been on Sustiva for three to four weeks, it’s usually smooth sailing, though it can raise lipid levels. Some people may have persistent neurologic side effects, including depression. When starting Sustiva or Atripla, take it in the evening on an empty stomach (at least two hours after dinner) to minimize side effects. You may be dizzy. Start it on a weekend, or some 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, though if you don’t feel like your normal self after a month on Sustiva or Atripla, it’s time for a change. It’s easy to become resistant to Sustiva, so don’t stop this drug unless you’re replacing it with something else. —Joel Gallant, MD, MPH
Activist’s comments
Convenient once-daily dosing of Sustiva is counterbalanced by the side effects that range from vivid dreams to screaming nightmares and walking zombie status. For most people, these effects diminish after the first few weeks, but for some, they never go away. Add a host of drug interactions, worsening of cholesterol, triglycerides, and liver enzymes, possible osteoporosis, and the need to avoid a heavy or fatty meal to prevent making the side effects even worse, and it’s not so convenient any more. Its long half-life can be a problem if you need to stop your meds for any reason—make sure you talk to your doctor about stopping the Sustiva before your other meds and perhaps switch to another med to “cover the tail” while you still have low levels of Sustiva in your blood. And for women of childbearing age—this drug can cause birth defects, so if you have any plans to get pregnant, don’t take it. —Jeff Taylor
