Potential side effects and toxicity: 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. If you experience blistering, mouth lesions, conjunctivitis (redness or inflammation of eye, which if untreated may result in permanent vision loss), swelling, muscle or joint aches, fever or general malaise (general ill feeling), stop taking Sustiva and seek immediate medical attention. 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.
Potential drug interactions: You cannot take the following medications with Sustiva: Versed, Halcion, or ergot medications (Wigraine, Methergine, and Cafergot), in any form—serious interactions seen with dilation during gynecological exams. Do not use with Biaxin, as levels of Biaxin are reduced. May affect Coumadin therapy. Dosing adjustment may be necessary for people on methadone due to withdrawal symptoms. When taken with Sustiva, Crixivan should be increased to 1,000 mg every eight hours or it should be boosted with Norvir, and increase Kaletra to four capsules twice daily when taken 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, because levels of Invirase are decreased substantially. With once-daily Lexiva, boost with 300 mg Norvir. Rifampin decreases Sustiva concentrations, so it should be avoided. Rifabutin levels are decreased by Sustiva, 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 should be performed. Sporanox or Vfend should not be taken with Sustiva. Avoid St. John’s wort, as it can reduce Sustiva levels. Sustiva can decrease birth control pill levels, so a second barrier contraceptive method is advised.
Tips: Sustiva taken at bedtime helps reduce CNS symptoms, but it can be taken at any time. People have described having “happy dreams” or nightmares depending on their mood or types of movies or television shows they viewed before sleep. Avoid driving or operating heavy machinery for a few hours after dose. Taking Sustiva with high-fat food may increase the body’s uptake of Sustiva, and alcohol may increase blood concentrations—both could up the risk of side effects. 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. Shown to penetrate lymphoid tissue, a hiding place for HIV. A genetic predisposition to having Sustiva clear out of your body more slowly—and thereby increasing risks of side effects—was seen more often in African Americans than in whites (20% vs. 3%).
Doctor
Efavirenz (EFV) is the most widely used non-nuke. It is potent, durable, and convenient (dosed once daily). Many studies have shown long-term suppression of the virus when used in combination with Combivir. Treatment guidelines recommend Sustiva as the anchor drug in combination therapy (unless a protease inhibitor is used). Its main side effects include a rash when starting therapy (which is rarely severe and does not require discontinuation of treatment) and central nervous system effects. This can include drowsiness or sleep disturbance, “bizarre” dreams, the sensation of being intoxicated, and dizziness. These effects usually subside in most people within a few weeks but persist in some. Sustiva may also have longer term effects such as raising cholesterol levels. An important recent labeling change classifies Sustiva as “Pregnancy Category D,” meaning it should not be used during pregnancy unless the benefits far outweigh the risks. For this reason, this drug should be used with great caution in women of child-bearing age. A highly anticipated co-formulation with Truvada is anticipated to be available sometime in 2006, once formulation issues are resolved. This will allow for an entire three-drug regimen to be taken as one pill once a day.—Chad J. Zawitz, MD
Activist
One of the “preferred drugs” in the DHHS guidelines due to its very good efficacy. It was the first drug to be approved for once-a-day dosing, so everyone jumped on it. Some people seem to get over the nightmares and fatigue in the first 2-3 weeks, but others seem not so lucky. Sustiva put a stop to my life for four months due to depression and fatigue, so I have my biases. But I have met many people who love it and are doing great on it. Also, unlike Viramune, Sustiva can increase lipids just like most protease inhibitors. I am waiting to see when BMS and Gilead will successfully co-formulate Truvada with Sustiva, since I think that will revolutionize the market with a convenient once-a-day pill to treat HIV with three meds. This will probably shift the paradigm in the industry to collaborate to improve patient adherence and pill burden. I just hope these two companies do the right thing and make that combo available to developing countries at low cost.—Nelson Vergel
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