Updated April 2010
Sustiva, Stocrin (outside the U.S.) – brand names
efavirenz – generic name
Sustiva belongs to a class of HIV drugs called non-nucleoside reverse transcriptase inhibitors (NNRTIs), also known as non-nucleoside analogs or “non-nukes.”
The NNRTIs block reverse transcriptase, a protein that HIV needs to make more copies of itself. This may slow down HIV disease.
The Food and Drug Administration (FDA) has approved Sustiva for use in combination with other HIV drugs for the treatment of HIV infection in adults and children over three years old.
Sustiva comes in:
- 50 milligram (mg) and 200 mg capsules
- 600 mg tablets
- A liquid formulation is being developed for children and is available through an expanded access program from the manufacturer; a health care provider can enroll a child in the program by calling 877-372-7097
The usual dose for adults is one 600 mg tablet once daily.
Check with your child’s health care provider for children’s dosing.
Sustiva must be used along with other HIV medications.
A combination tablet containing Sustiva and other HIV drugs is also available:
Atripla: Viread (tenofovir), Emtriva (emtricitabine or FTC), and
Take Sustiva on an empty stomach at bedtime to reduce side effects. Sustiva should not be taken with a high fat meal because this increases the chances of side effects. High-fat food and alcohol could increase the risk of side effects.
If you miss your dose of Sustiva, take it as soon as possible. If it is
almost time for your next dose, do not take the missed dose. Instead, take the
next dose at its regular time
Speak to your health care provider if you:
- Have liver problems
- Have mental health issues (such as depression)
- Are using street drugs or alcohol
- Have a history of seizures
- Are pregnant, planning on becoming pregnant, or not consistently using birth control other than birth control pills
It can take two to three weeks for Sustiva to be eliminated from your body after you stop taking it. Most of the other HIV drugs are eliminated much faster. This means that if you stop taking a regimen that contains Sustiva and other HIV drugs, the Sustiva will stay in your body longer than the other drugs. This can lead to the development of resistance. Careful planning with your health care provider is needed if you stop taking a drug regimen that contains Sustiva, especially if you do not immediately switch to another drug regimen.
Sustiva is one of the easiest HIV drugs to take because you only have to take one pill, once a day. Once-daily drugs dosing is convenient but you have to make sure to take Sustiva exactly as prescribed. Missing or skipping doses can cause your blood levels of Sustiva to fall too low and resistance can develop. This may cause Sustiva and other drugs you may be taking to stop working.
Sustiva can be used if you’re just starting HIV treatment.
Sustiva can also be used if you’ve been on treatment before. However, it will not work well for people whose HIV virus is already resistant to other NNRTIs like Rescriptor (delavirdine) and Viramune (nevirapine).
You and your health care provider should use resistance testing and your treatment history to help guide the use of Sustiva and to determine which drugs will work best for you.
Sustiva seems to cross the blood-brain barrier (which protects the brain and spinal cord), so it may be able to fight HIV in the brain.
If your virus develops resistance to Sustiva then it may stop working or not work as well for you. You are also not likely to benefit from the other NNRTIs.
Sometimes taking more than one medication can cause drug interactions. This can lead to the drugs not working as well or an increased risk of side effects.
Taking certain drugs with Sustiva can change the amount of each drug in your body. Your health care provider may need to adjust the doses of your drugs to avoid under- or overdosing.
Sustiva should not be combined with:
- Antifungals: Noxafil (posaconazole), standard doses of Vfend (voriconazole)
- Antipsychotic: Orap (pimozide)
- Acid reflux/heartburn drug: Propulsid (cisapride)
- Heart drug: Vascor (bepridil)
- Sedatives: Versed (midazolam), Halcion (triazolam)
- Antimigraine drugs: Wigraine, Cafergot (ergot medications)
- Herbs: St. John's wort
- HIV drugs: Atripla (because it contains Sustiva)
If you are taking any of the following medications, speak to your health care provider as your doses may need to be adjusted:
- HIV drugs: Crixivan (indinavir), Reyataz (atazanavir), Kaletra (lopinavir/ritonavir), Lexiva (fosamprenavir), Viracept (nelfinavir), Norvir (ritonavir), Invirase (saquinavir), Selzentry (maraviroc)
- Erectile disfunction drugs: Viagra (sildenafil), Levitra (vardenafil)
- Drugs to prevent blood clots: Coumadin (warfarin)
- Antihistimine: Hismanal (astemizole)
- Immunosuppressant drugs: cyclosporine (Gengraf, Neoral, Sandimmune, and others) Prograf (tacrolimus), Rapamune (sirolimus)
- Drugs to treat fungal and bacterial infections: Biaxin (clarithromycin), Rifadin (rifampin), Sporanox (itraconazole), Mycobutin (rifabutin)
- Antidepressant: Zoloft (sertraline)
- Drugs to treat convulsions: Carbatol, Tegretol (carbamazepine)
- Cholesterol-lowering drugs: Lipitor (atorvastatin), Pravachol (pravastatin), Zocor (simvastatin)
- Calcium channel blockers: Cardizem or Tiazac (diltiazem), Covera HS or Isoptin SR (verapamil)
- Methadone doses may need to be increased
- Sustiva deceases the effectiveness of birth control pills and possibly hormonal implants, so other birth control methods (such as barrier contraceptives) should be used
This is not a complete list of medications. Because there are many possible drug interactions with Sustiva, be sure your health care provider knows about all the medications you are taking (including over-the-counter, prescription, street drugs, and herbs), even if you only use them occasionally.
For more information and additional resources to check interactions between the particular drugs you are taking, see our info sheet on drug interactions or go to:
Sustiva side effects usually happen in the first two to four weeks of treatment and generally improve as your body adjusts to the medication. In some cases, side effects may continue for longer than the first month.
Many of the side effects associated with Sustiva affect the brain or central nervous system (CNS):
- Insomnia (trouble sleeping)
- Trouble concentrating
- Vivid dreams
- Changes in mood
Other side effects include:
- Skin rash (rash may be a serious problem in some children)
- Fatigue (unusual tiredness)
Many people find that they can handle the side effects better if they take Sustiva at bedtime. Your health care provider can help you manage Sustiva side effects. If the side effects do not go away or become intolerable, call your health care provider for advice. Don’t just stop taking your medication.
More serious side effects:
- Although rare, some people experience clinical depression, paranoia, and thoughts of suicide. These problems tend to occur more often in people with a history of mental illness.
- Sustiva is less likely to cause a rash than other NNRTI drugs, but in rare cases it has caused a life-threatening hypersensitivity reaction (Stevens-Johnson syndrome). Symptoms may include a severe rash, blisters, mouth sores, swelling, fever, and weakness
- Liver toxicity: this may be indicated by abnormal liver blood tests or yellowing of the skin and eyes (jaundice). Increases in liver enzymes in people with hepatitis B and/or C can occur and should be monitored
- Lipodystrophy, which may include elevated blood sugar (glucose), elevated lipid levels (cholesterol and triglycerides), and fat gain or loss in certain areas. The exact causes of lipodystrophy are not known, but may include HIV and/or HIV drugs. It is unclear if Sustiva will cause or impact symptoms of lipodystrophy. For more information, see our info sheet on lipodystrophy.
Call your health care provider right away if you are experiencing any of the more serious side effects.
Sustiva has been studied in many women. Studies of Sustiva pharmacokinetics
(how the drug is processed by the body) showed that the drug behaves similarly
in the bodies of women and men, but some research indicates that Sustiva may
reach higher levels in women. The drug manufacturer does not recommend any dose
adjustments based on weight or sex.
- Study DMP266-006 compared Retrovir (zidovudine or AZT) plus Epivir (lamivudine or 3TC) plus Sustiva to Retrovir plus Epivir plus Crixivan to Sustiva plus Crixivan in people who had not taken NNRTIs or protease inhibitors before. This study included 17 percent women, or about 215 women out of 1,266 total participants. After 48 weeks, more people taking Retrovir plus Epivir plus Sustiva had undetectable viral loads than those taking either Retrovir plus Epivir plus Crixivan or Sustiva plus Crixivan. More people in the Crixivan groups stopped treatment due to side effects (although more people in the Sustiva group developed a rash or nervous system side effects). At 72 weeks, Retrovir plus Epivir plus Sustiva still worked better, but at three years, the rates of treatment failure in the Sustiva and Crixivan groups were similar.
- Study ACTG 364 compared Sustiva to Viracept (nelfinavir) to Sustiva plus Viracept in treatment-experienced people who were also taking nucleoside reverse transcriptase inhibitors (NRTIs). This trial included 12 percent women, or about 23 women out of 196 total participants. In this study, people taking Sustiva plus Viracept plus NRTIs or Sustiva plus NRTIs were more likely to achieve undetectable viral loads than those taking Viracept plus NRTIs.
- Study DMP-020 found that Sustiva plus Crixivan plus NRTIs worked better than Crixivan plus NRTIs without Sustiva. This trial included about 17 percent women, or 55 women out of 327 total participants.
- Study AI424-034 compared Retrovir plus Epivir plus Sustiva to Retrovir plus Epivir plus Reyataz in people who had not used HIV drugs before. This study included 35 percent women, or about 280 women out of 805 total participants. In this study Sustiva and Reyataz worked equally well against HIV, but Reyataz did not increase blood fat levels as much as Sustiva.
- ACTG 384, a large study comparing six different drug combinations, found that Retrovir plus Epivir plus Sustiva was one of the best first regimens in terms of effectiveness and side effects.
- The 2NN study compared Zerit (stavudine or d4T) plus Epivir plus Sustiva versus Zerit plus Epivir plus Viramune to Zerit plus Epivir plus Sustiva plus Viramune in people who had not taken HIV drugs before. This trial included 37 percent women, or about 449 women out of 1,216 total participants. In this study, Sustiva and Viramune worked about equally well overall, but Sustiva appeared to work better in people with high viral loads. People who took both Sustiva and Viramune did worse than those who took only one NNRTI, since more stopped treatment due to side effects.
- Study ACTG 5095 found that drug regimens containing Sustiva worked better than the all-NRTI combination of Retrovir plus Epivir plus Ziagen (abacavir); these three drugs are in the Trizivir combination pill. This study included 19 percent women, or about 218 women out of 1,147 total participants.
- Several studies have looked at people switching from PIs to NNRTIs (for example, study DMP266-049, which included 10 percent women, or about 22 women out of 226 total participants). Overall, these studies have found that people who switch from a PI to Sustiva have a similar or better response to treatment, as well as increased levels of HDL (“good”) cholesterol, lower levels of LDL (“bad”) cholesterol and lower levels of triglycerides, all of which may protect against heart disease.
In terms of side effects, studies show that Sustiva can cause a skin rash or nervous system side effects. In study DMP266-006 (described above), 34 percent of participants taking Sustiva developed a rash, and 58 percent developed nervous system side effects. These side effects were most likely during the first month of treatment. Studies do not seem to indicate that women taking Sustiva experience more or different side effects than men. But we know that in general depression and mood disorders are more common in women, so more research is needed on nervous system side effects in women taking this medication.
Studies have shown that pregnant women who use HIV drugs can greatly reduce the risk of passing HIV on to their babies. There have been no formal studies on the use of Sustiva during pregnancy. However, Sustiva has been linked to birth defects in humans causing the FDA to recommend that Sustiva not be used during pregnancy. Because of this, pregnant women should not use Sustiva, and women who are taking the drug should use effective birth control. (Since Sustiva decreases the effectiveness of birth control pills, a barrier contraceptive method should be used.)
An Antiretroviral Pregnancy Registry has been established to collect
information on pregnant women who take HIV drugs, including Sustiva. If you are
pregnant and taking Sustiva or other HIV drugs, your health care provider can
register you by calling 1-800-258-4263 or going to www.apregistry.com.
It is not known whether Sustiva passes into breast milk. HIV+ women should not breast-feed because their babies could be infected with HIV through the breast milk.
Check with your health care provider about the best treatment options for you and your baby if you are thinking of getting pregnant.
Click this link for more information on pregnancy.
Sustiva may cause a false positive result if you are given a drug test for marijuana.
People who are starting HIV treatment for the first time may develop Immune Reconstitution Syndrome or IRS (also called Immune Reconstitution Inflammatory Syndrome or IRIS). IRS can happen as a result of the immune system getting stronger and responding to an HIV-related infection such as Mycobacterium avium infection (MAC), cytomegalovirus (CMV), Pneumocystis jirovecii pneumonia (PCP), or tuberculosis (TB). People may have been treated for these infections in the past or not even know they have them. If you notice any unusual symptoms soon after starting HIV drugs for the first time, let your health care provider know right away so you can be evaluated and, if necessary, treated.