Class: non-nucleoside analog (also called non-nucleoside reverse transcriptase inhibitor, NNRTI or non-nuke)
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, 100 mg and 200 mg capsules. Dose can be split up. Approved for children 3 years and older. Strawberry/mint flavored solution available to children under expanded access program. Take missed dose as soon as possible, but do not double up on next dose.
Because Sustiva penetrates so readily into the brain, up to 50% of patients experience some kind of central nervous system (CNS) or psychiatric symptoms (dizziness, headache, memory loss, somnolence or hypnotic trance, confusion, insomnia, hallucinations, vivid or abnormal dreams or nightmares, depression, euphoria or mania, and agitation). These symptoms typically diminish within four weeks. 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. Some people in recovery from substance use will experience flashbacks. Other side effects 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 is diarrhea, fever, and low levels of some blood cells. May raise levels of triglycerides and the good cholesterol (HDL). 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.
Potential drug interactions:
You cannot take the following medications with Sustiva: midazolam, triazolam, or ergot medications (Wigraine, Methergine, and Cafergot), or Vfend, St. John's wort, and bepridil. Do not use with Biaxin. May affect Coumadin (warfarin) 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 people who previously took HIV drugs, especially protease inhibitors. 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 should also be "boosted" with Norvir (Reyataz 300 mg/Norvir 100 mg once daily) when taken with Sustiva. Sustiva and Invirase should not be used in combination. With once-daily Lexiva, boost with 300 mg Norvir. Rifampin decreases Sustiva concentrations, so it should be avoided. Rifabutin levels are decreased, so daily dose of rifabutin should be increased by 50%. When taken with anticonvulsants Dilantin (phenytoin), phenobarbital, or Tegretol (carbamazepine), 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 (itraconazole), Zoloft, Lipitor, pravastatin, simvastatin, and diltiazem. Dose adjustment may be needed when co-administering these drugs with Sustiva. Do not take with Atripla, since Sustiva is already in Atripla.
Tips:
Sustiva taken at bedtime helps reduce CNS symptoms, but it can be taken at any time. Avoid driving or operating heavy machinery for a few hours after dose. High-fat food and alcohol could up the risk of side effects; this is why taking it on an empty stomach is recommended. Some people adjust to Sustiva when taking Ativan or Ambien to sleep for the first few weeks, but either may make you even more groggy the next morning. Women who can become pregnant need to use appropriate birth control, as Sustiva can affect the effectiveness of the Pill (see Interactions above) and increase the risk of birth defects. Please see package insert for more complete potential side effects and interactions.
Doctor
Efavirenz is now not only the "gold standard" NNRTI; it's simply the "gold standard" ... period. In trial after trial, no drug has ever done better at suppressing viral load and keeping it suppressed. It works at high viral loads and at low CD4 counts, has little long-term toxicity, and is the key component of the first one-pill, once-a-day combination, Atripla. This is the drug I use for first-line therapy unless I can think of a reason not to. But there are reasons not to use efavirenz: It can cause birth defects, so women who want to get pregnant or who aren't preventing pregnancy should avoid it. If your baseline genotype shows NNRTI mutations, you should take something else. It sticks around for a long time in the blood, so it's forgiving of the occasional late or skipped dose, but this is not a drug for people who are prone to stopping therapy altogether: resistance occurs easily as drug levels begin to fall. Finally, it has some early side effects that can be a problem for some people. Vivid dreams, dizziness, and mental "fogginess" are common during the first few days -- sometimes weeks -- of therapy, and for a small fraction, those side effects are deal breakers. My advice when starting Sustiva or Atripla:
Start it on a weekend, when you have a few days (and especially mornings) with nothing important to do;
Get out of bed slowly;
Read or watch something funny ... or sexy ... before you go to bed, not something scary -- you may have wild dreams, so you might as well enjoy them!;
If you're dreaming too much and not feeling rested the next day, talk to your doctor about using a sleeping pill until things get better;
Remember, the side effects tend to improve with each dose. If you've been on Sustiva or Atripla for 3 to 4 weeks and still don't like the way it makes you feel, it's probably time for a switch.
Sustiva can also cause a rash, usually within the first few weeks of treatment. The rash can be itchy and annoying, but it usually goes away on its own and is rarely a reason to stop the drug. -- Joel Gallant, M.D.
Activist
Sustiva is the big shot of the non-nucleoside field. It's a very potent drug with a very long half life in the blood, which makes it tolerate the occasional skipped dose better than most drugs. But it takes only a single mutation for HIV to develop resistance, and when resistance occurs, it also knocks out the other drugs of this class. A new drug (Intelence) has finally solved that problem. For those who don't have mental disturbances, Sustiva has proven to be an excellent drug with virtually no other continuing or long term side effects. -- Martin Delaney
