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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, 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 your next dose.
AWP: $479.45 / month for thirty 600 mg tablets
Manufacturer contact: Bristol-Myers Squibb,
www.sustiva.com; 1 (800) 334–4486
AIDSInfo:1 (800) HIV–0440 (448–0440), www.aidsinfo.nih.gov
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| 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. 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.
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| Potential drug interactions: |
| You cannot take the following medications with Sustiva: Versed, Halcion, or ergot medications (Wigraine, Methergine, and Cafergot), Sporonox or Vfend. Do not use with 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 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, phenobarbital, or Tegretol, periodic monitoring of blood levels of anticonvulsants and Sustiva should be performed or alternative anti-seizure medications should be considered. 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. Avoid driving or operating heavy machinery for a few hours after dose. High-fat food and alcohol 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.
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| Doctor |
| Efavirenz (EFV) has emerged in both studies and clinical practice as the gold standard drug for combination with two RTIs. Due to its ease of administration (once a day), general tolerability, and potency, use of EFV with AZT plus 3TC evolved to be the triple combination of first choice through 2005. EFV performs even better when matched with better tolerated drugs with similar half-lives, such as tenofovir and emtricitabine. The Achilles heal of EFV is the low threshold for resistance, which is perhaps magnified when used with drugs with shorter half-lives (e.g., ZDV/3TC) and diminished when all three drugs have a similar half-life (e.g., tenofovir plus FTC). EFV can cause a rash (usually manageable) and significant central nervous side effects (such as sleep disturbances, nightmares, dizziness), particularly during the first four weeks. Dosing on an empty stomach is recommended, while use with high fat meals can increase EFV levels and exacerbate side effects. African Americans may experience a higher rate of side effects due to genetic differences in drug metabolism. EFV has been linked to fetal abnormalities (it is classified as a Category D drug), so use in pregnancy is to be avoided (a serious concern when used in women of childbearing age interested in having children). It is available in a co-formulation that allows for a one pill a day regimen (Atripla), though my own practice is to generally use components separately during the initial four to eight weeks until it is clear that all of the drugs in the regimen are being well tolerated. Use can result in a false positive test for cannabinoids. No dose adjustment is necessary for renal dysfunction. Drug interactions are important considerations, including frequently decreasing the levels of concurrently used protease inhibitors even when using ritonavir boosting.—Keith Henry, MD |
| Activist |
| This is one of those “love it or hate it” drugs. Sustiva is a potent non-nuke that has been around for a while and still competes well with drugs from the PI class. Taken once a day (best at bedtime) with a small meal or snack it is convenient and has less of the lipo issues that some of the PIs have. The problem is, this is not a drug for everyone or everybody. It is well-known for its central nervous system side effects which can range anywhere from suicidal ideation and general depression to incredibly fabulous technicolor psychedelic sex dreams. I was on Sustiva for two years and never had any noticeable side effects myself. In fact, I was kind of disappointed when I missed out…on the hot dreams part. It just goes to show you, everyone is individual and we have to think about treatment that way. Sustiva can be a great anchor drug for the right person. The only people who should never use this drug are women who are considering pregnancy or actively attempting to become pregnant. Sustiva has been shown to cause birth defects in women who were taking it during pregnancy. If you are a woman of child-bearing age who may become pregnant (even by accident), you need to think twice before using this drug. But otherwise, don’t judge this drug by the negative (or positive) comments you may hear in support groups. Give it a fair chance.—Cathy Olufs |
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