"Nov. 27, 2012 -- Every month, 1,000 more young Americans ages 13 to 24 get an incurable infection that's deadly unless held at bay by daily doses of costly drugs -- and many of them don't even know it.
That infection is HIV, the virus"...
Sustiva Side Effects Center
Medical Editor: John P. Cunha, DO, FACOEP
Sustiva (efavirenz) is used to treat HIV, which causes the acquired immunodeficiency syndrome (AIDS). It is not a cure for HIV or AIDS. It is an antiviral medication. Common side effects include dizziness, trouble sleeping, drowsiness, unusual dreams, and trouble concentrating. These side effects may begin 1-2 days after starting this medication and usually go away in 2-4 weeks.
The recommended adult dosage of Sustiva is 600 mg orally, once daily, in combination with a protease inhibitor and/or nucleoside analogue reverse transcriptase inhibitors (NRTIs). Sustiva may interact with cyclosporine, itraconazole, sirolimus, tacrolimus, St. John's wort, voriconazole, blood thinners, cholesterol medications, antibiotics, heart or blood pressure medications, other HIV medicines, or seizure medications. Tell your doctor all medications you use. Sustiva is not recommended for use during pregnancy. It may harm a fetus, especially if taken during the first 3 months of pregnancy. Women of childbearing age should have a pregnancy test before starting this medication. Consult your doctor about using at least 2 forms of birth control (such as condoms with birth control pills) during treatment and for 3 months after the end of treatment. If you become pregnant or think you may be pregnant, tell your doctor immediately. It is unknown if Sustiva passes into breast milk. Because breast milk can transmit HIV, do not breast-feed.
Our Sustiva (efavirenz) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
What is Patient Information in Detail?
Easy-to-read and understand detailed drug information and pill images for the patient or caregiver from Cerner Multum.
Sustiva in Detail - Patient Information: Side Effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Efavirenz may cause serious psychiatric symptoms including confusion, severe depression, suicidal thoughts, aggression, extreme fear, hallucinations, or unusual behavior. Contact your doctor at once if you have any of these side effects, even if you have had them before.
Call your doctor at once if you have a serious side effect such as:
- fever, sore throat, and headache with a severe blistering, peeling, and red skin rash;
- nausea, stomach pain, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
- fever, chills, body aches, flu symptoms; or
- any other signs of new infection.
Less serious side effects may include:
- mild nausea, vomiting, or stomach pain, diarrhea or constipation;
- blurred vision;
- headache, tired feeling, dizziness, spinning sensation;
- trouble concentrating, problems with balance or coordination;
- muscle or joint pain;
- sleep problems (insomnia), unusual dreams; or
- changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).
Read the entire detailed patient monograph for Sustiva (Efavirenz) »
What is Patient Information Overview?
A concise overview of the drug for the patient or caregiver from First DataBank.
Sustiva Overview - Patient Information: Side Effects
Tiredness, headache, nausea, vomiting, and diarrhea may also occur.
If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Some people may experience worsening of a previous medical condition (such as an old infection) as their immune systems improve, or develop new conditions because their immune systems have become overactive. This reaction may occur at any time (soon after starting HIV treatment or many months later). Tell your doctor right away if you have any serious side effects, including: unexplained weight loss, persistent muscle aches/weakness, joint pain, numbness/tingling of the hands/feet/arms/legs, severe tiredness, vision changes, severe/persistent headaches, signs of infection (such as fever, chills, trouble breathing, cough, non-healing skin sores), signs of an overactive thyroid (such as irritability, nervousness, heat intolerance, fast/pounding/irregular heartbeat, bulging eyes, unusual growth in the neck/thyroid known as a goiter), signs of a certain nerve problem known as Guillain-Barre Syndrome (such as difficulty breathing/swallowing/moving your eyes, drooping face, paralysis, slurred speech).
Infrequently, serious psychiatric symptoms may occur during efavirenz treatment, although it is unclear if they are caused by efavirenz. These effects may be seen especially in people who have mental/mood conditions. Tell your doctor immediately if any of these unlikely but serious side effects occur: mental/mood changes (such as depression, rare thoughts of suicide, nervousness, angry behavior, hallucinations).
Tell your doctor immediately if any of these rare but serious side effects occur: signs of liver problems (such as persistent nausea/vomiting, stomach/abdominal pain, severe tiredness, yellowing eyes/skin, dark urine).
Changes in body fat may occur while you are taking this medication (such as increased fat in the upper back and stomach areas, decreased fat in the arms and legs). The cause and long-term effects of these changes are unknown. Discuss the risks and benefits of treatment with your doctor, as well as the possible use of exercise to reduce this side effect.
Efavirenz can commonly cause a rash that is usually not serious. A rash may occur in the first 2 weeks after starting treatment and if it is not serious, it will usually resolve in 4 weeks. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Therefore, seek immediate medical attention if you develop any rash.
A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, blisters, peeling skin, fever, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
In the US -
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
Read the entire patient information overview for Sustiva (Efavirenz)»
What is Prescribing information?
The FDA package insert formatted in easy-to-find categories for health professionals and clinicians.
Sustiva FDA Prescribing Information: Side Effects
The most significant adverse reactions observed in patients treated with SUSTIVA are:
- psychiatric symptoms [see WARNINGS AND PRECAUTIONS],
- nervous system symptoms [see WARNINGS AND PRECAUTIONS],
- rash [see WARNINGS AND PRECAUTIONS].
The most common ( > 5% in either efavirenz treatment group) adverse reactions of at least moderate severity among patients in Study 006 treated with SUSTIVA in combination with zidovudine/lamivudine or indinavir were rash, dizziness, nausea, headache, fatigue, insomnia, and vomiting.
Clinical Trials Experience in Adults
Because clinical studies are conducted under widely varying conditions, the adverse reaction rates reported cannot be directly compared to rates in other clinical studies and may not reflect the rates observed in clinical practice.
Selected clinical adverse reactions of moderate or severe intensity observed in ≥ 2% of SUSTIVA-treated patients in two controlled clinical trials are presented in Table 3.
Table 3: Selected Treatment-Emergenta Adverse Reactions
of Moderate or Severe Intensity Reported in ≥ 2% of
SUSTIVA-Treated Patients in Studies 006 and ACTG 364
|Adverse Reactions||Study 006 LAM-, NNRTI-, and Protease Inhibitor-Naive Patients||Study ACTG 364 NRTI-experienced, NNRTI-, and Protease Inhibitor-Naive Patients|
|SUSTIVAb + ZDV/LAM
(n=412) c 180 weeks
| SUSTIVAb + Indinavir
(n=415) c 102 weeks
|Indinavir + ZDV/LAM
(n=401) c 76 weeks
| SUSTIVA + Nelfinavir + NRTIs
(n=64) c 71.1 weeks
| SUSTIVA + NRTIs
(n=65) c 70.9 weeks
|Nelfinavir + NRTIs
(n=66) c 62.7 weeks
|Body as a Whole|
|Central and Peripheral Nervous System|
|Concentration impaired||5%||3%||< 1%||0||0||0|
|Anorexia||1%||< 1%||< 1%||0||2%||2%|
|Skin & Appendages|
|a Includes adverse events at least possibly related to study
drug or of unknown relationship for Study 006. Includes all adverse events
regardless of relationship to study drug for Study ACTG 364.
bSUSTIVA provided as 600 mg once daily.
cMedian duration of treatment.
dIncludes erythema multiforme, rash, rash erythematous, rash follicular, rash maculopapular, rash petechial, rash pustular, and urticaria for Study 006 and macules, papules, rash, erythema, redness, inflammation, allergic rash, urticaria, welts, hives, itchy, and pruritus for ACTG 364.
- = Not Specified.
ZDV = zidovudine, LAM = lamivudine.
Pancreatitis has been reported, although a causal relationship with efavirenz has not been established. Asymptomatic increases in serum amylase levels were observed in a significantly higher number of patients treated with efavirenz 600 mg than in control patients (see Laboratory Abnormalities).
Nervous System Symptoms
For 1008 patients treated with regimens containing SUSTIVA and 635 patients treated with a control regimen in controlled trials, Table 4 lists the frequency of symptoms of different degrees of severity and gives the discontinuation rates for one or more of the following nervous system symptoms: dizziness, insomnia, impaired concentration, somnolence, abnormal dreaming, euphoria, confusion, agitation, amnesia, hallucinations, stupor, abnormal thinking, and depersonalization [see WARNINGS AND PRECAUTIONS]. The frequencies of specific central and peripheral nervous system symptoms are provided in Table 3.
Table 4: Percent of Patients with One or More Selected
Nervous System Symptomsa,b
|Percent of Patients with:||SUSTIVA 600 mg Once Daily
|Symptoms of any severity||52.7||24.6|
|Treatment discontinuation as a result of symptoms||2.1||1.1|
|a Includes events reported regardless of causality.
bData from Study 006 and three Phase 2/3 studies.
c “Mild” = Symptoms which do not interfere with patient's daily activities.
d“Moderate” = Symptoms which may interfere with daily activities.
e “Severe” = Events which interrupt patient's usual daily activities.
Serious psychiatric adverse experiences have been reported in patients treated with SUSTIVA. In controlled trials, psychiatric symptoms observed at a frequency of > 2% among patients treated with SUSTIVA or control regimens, respectively, were depression (19%, 16%), anxiety (13%, 9%), and nervousness (7%, 2%).
For 1008 adult and 57 pediatric patients treated with regimens containing SUSTIVA and 635 patients treated with a control regimen in controlled trials, the frequency of rash by NCI grade and the discontinuation rates as a result of rash in clinical studies are provided in Table 5 [see WARNINGS AND PRECAUTIONS].
Table 5: Percent of Patients
with Treatment-Emergent Rasha,b
|Percent of Patients with:||Description of Rash Gradec||SUSTIVA 600 mg Once Daily Adults
|SUSTIVA Pediatric Patients
|Control Groups Adults
|Rash of any grade||-||26.3||45.6||17.5|
|Grade 1 rash||Erythema, pruritus||10.7||8.8||9.8|
|Grade 2 rash||Diffuse maculopapular rash, dry desquamation||14.7||31.6||7.4|
|Grade 3 rash||Vesiculation, moist desquamation, ulceration||0.8||1.8||0.3|
|Grade 4 rash||Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, necrosis requiring surgery, exfoliative dermatitis||0.1||3.5||0.0|
|Treatment discontinuation as a result of rash||-||1.7||8.8||0.3|
|a Includes events reported regardless of causality.
bData from Study 006 and three Phase 2/3 studies.
c NCI Grading System.
As seen in Table 5, rash is more common in pediatric patients and more often of higher grade (ie, more severe) [see WARNINGS AND PRECAUTIONS].
Experience with SUSTIVA in patients who discontinued other antiretroviral agents of the NNRTI class is limited. Nineteen patients who discontinued nevirapine because of rash have been treated with SUSTIVA. Nine of these patients developed mild-to-moderate rash while receiving therapy with SUSTIVA, and two of these patients discontinued because of rash.
Selected Grade 3-4 laboratory abnormalities reported in ≥ 2% of SUSTIVA-treated patients in two clinical trials are presented in Table 6.
Table 6: Selected Grade 3-4 Laboratory Abnormalities
Reported in ≥ 2% of SUSTIVA-Treated Patients in Studies 006 and
|Variable||Limit||Study 006 LAM-, NNRTI-, and Protease Inhibitor-Naive Patients||Study ACTG 364 NRTI-experienced, NNRTI-, and Protease Inhibitor-Naive Patients|
|SUSTIVAa + ZDV/LAM
(n=412) b 180 weeks
| SUSTIVAa+ Indinavir
(n=415) b 102 weeks
|Indinavir + ZDV/LAM
(n=401) b 76 weeks
| SUSTIVAa + Nelfinavir + NRTIs
(n=64 )b 71.1 weeks
| SUSTIVAa + NRTIs
(n=65) b 70.9 weeks
|Nelfinavir + NRTIs
(n=66) b 62.7 weeks
|ALT||> 5 x ULN||5%||8%||5%||2%||6%||3%|
|AST||> 5 x ULN||5%||6%||5%||6%||8%||8%|
|GGTc||> 5 x ULN||8%||7%||3%||5%||0||5%|
|Amylase||> 2 x ULN||4%||4%||1%||0||6%||2%|
|Glucose||> 250 mg/dL||3%||3%||3%||5%||2%||3%|
|Triglyceridesd||≥ 751 mg/dL||9%||6%||6%||11%||8%||17%|
|a SUSTIVA provided as 600 mg once daily.
b Median duration of treatment.
c Isolated elevations of GGT in patients receiving SUSTIVA may reflect enzyme induction not associated with liver toxicity.
ZDV = zidovudine, LAM = lamivudine, ULN = Upper limit of normal, ALT = alanine aminotransferase, AST = aspartate aminotransferase, GGT = gamma-glutamyltransferase.
Patients Coinfected with Hepatitis B or C
Liver function tests should be monitored in patients with a history of hepatitis B and/or C. In the long-term data set from Study 006, 137 patients treated with SUSTIVA-containing regimens (median duration of therapy, 68 weeks) and 84 treated with a control regimen (median duration, 56 weeks) were seropositive at screening for hepatitis B (surface antigen positive) and/or C (hepatitis C antibody positive). Among these coinfected patients, elevations in AST to greater than five times ULN developed in 13% of patients in the SUSTIVA arms and 7% of those in the control arm, and elevations in ALT to greater than five times ULN developed in 20% of patients in the SUSTIVA arms and 7% of patients in the control arm. Among coinfected patients, 3% of those treated with SUSTIVA-containing regimens and 2% in the control arm discontinued from the study because of liver or biliary system disorders [see WARNINGS AND PRECAUTIONS].
Increases from baseline in total cholesterol of 10-20% have been observed in some uninfected volunteers receiving SUSTIVA. In patients treated with SUSTIVA + zidovudine + lamivudine, increases from baseline in nonfasting total cholesterol and HDL of approximately 20% and 25%, respectively, were observed. In patients treated with SUSTIVA + indinavir, increases from baseline in nonfasting cholesterol and HDL of approximately 40% and 35%, respectively, were observed. Nonfasting total cholesterol levels ≥ 240 mg/dL and ≥ 300 mg/dL were reported in 34% and 9%, respectively, of patients treated with SUSTIVA + zidovudine + lamivudine; 54% and 20%, respectively, of patients treated with SUSTIVA + indinavir; and 28% and 4%, respectively, of patients treated with indinavir + zidovudine + lamivudine. The effects of SUSTIVA on triglycerides and LDL in this study were not well characterized since samples were taken from nonfasting patients. The clinical significance of these findings is unknown [see WARNINGS AND PRECAUTIONS].
Clinical Trial Experience in Pediatric Patients
Clinical adverse experiences observed in ≥ 10% of 57 pediatric patients aged 3 to 16 years who received SUSTIVA capsules, nelfinavir, and one or more NRTIs in Study ACTG 382 [see Use In Specific Populations] were rash (46%), diarrhea/loose stools (39%), fever (21%), cough (16%), dizziness/lightheaded/fainting (16%), ache/pain/discomfort (14%), nausea/vomiting (12%), and headache (11%). The incidence of nervous system symptoms was 18% (10/57). One patient experienced Grade 3 rash, two patients had Grade 4 rash, and five patients (9%) discontinued because of rash [see WARNINGS AND PRECAUTIONS and ADVERSE REACTIONS, Table 5)].
The following adverse reactions have been identified during postapproval use of SUSTIVA. Because these reactions are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Cardiovascular: flushing, palpitations
Liver and Biliary System: hepatic enzyme increase, hepatic failure, hepatitis. A few of the postmarketing reports of hepatic failure, including cases in patients with no pre-existing hepatic disease or other identifiable risk factors, were characterized by a fulminant course, progressing in some cases to transplantation or death.
Metabolic and Nutritional: hypercholesterolemia, hypertriglyceridemia
Special Senses: abnormal vision, tinnitus
Read the entire FDA prescribing information for Sustiva (Efavirenz) »
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