Brand name: Sustiva

Common name: efavirenz (EFV)

Class: non-nucleoside analog (also called non-nucleoside reverse transcriptase inhibitor, NNRTI or non-nuke)

Standard dose: One 600 mg tablet, typically at bedtime; with a light snack or 30 minutes after food. 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 your next dose.

AWP: $473.70 / month

Manufacturer contact: Bristol-Myers Squibb, www.sustiva.com; 1 (800) 334–4486

AIDS Treatment Information Service: 1 (800) HIV–0440 (448–0440)

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) symptoms (dizziness, headache, somnolence or hypnotic trance). Psychiatric symptoms (confusion, insomnia, hallucinations, vivid dreams or nightmares, depression, euphoria or mania, agitation) are less frequent. Some people in recovery from substance use will experience flashbacks. Other side effects include rash, nausea, vomiting, diarrhea, fever, insomnia and increased liver enzymes. These symptoms occur early and generally resolve within two to four weeks. If you can’t sleep (which more commonly develops after some time on Sustiva), ask about switching the timing of your dose little by little until you’re taking it in the daytime. 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 (midazolam), Halcion (triazolam), or ergot medications (Wigraine and Cafergot), in any form—serious interactions seen with dilation during gynecological exams. Do not use with Biaxin (clarithromyocin), as levels of Biaxin are reduced. May affect Coumadin (warfarin) 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. Reyataz should also be “boosted” with Norvir (Reyataz 300 mg/Norvir 100 mg), still once daily, when taken with Sustiva. Sustiva and saquinavir (Fortovase and Invirase) should not be used in combination, because levels of saquinavir are decreased substantially. No interaction data available with Fortovase/Norvir—consider doubling Fortovase to 800 mg twice-a-day. Monitor liver enzymes closely if Sustiva and Norvir are used together due to potential risk of liver damage. With once-daily Lexiva, boost with 300 mg Norvir.

Tips: Women of child-bearing age and their male partners should consider the use of alternative contraception methods with barrier, in addition to the Pill, because of the potential for embryo heart defects. It is recommended that Sustiva be taken at bedtime to help reduce CNS symptoms, but can be taken at any time. People have described having “happy dreams” or nightmares depending on their mood or types of movies (Disney movie or horror movie, for example) or television shows they viewed before sleep. Avoid driving or operating heavy machinery for a few hours after dose. Side effects may linger. 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 experiencing 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. Some people develop sleeplessness and increased energy after taking Sustiva. If this happens, you may try taking it when you wake up. 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 your side effects—was seen more often in African Americans than in whites (20% vs. 3%).