"The number of pregnant and breastfeeding women in Malawi with HIV who started life-saving antiretroviral treatment increased by more than 700 percent in one year, according to a study in CDC's Morbidity and Mortality Weekly Report. The "...
Intelence Side Effects Center
Medical Editor: John P. Cunha, DO, FACOEP
Intelence (etravirine) is used with other medications to treat HIV, which causes the acquired immunodeficiency syndrome (AIDS). This drug is not a cure for HIV or AIDS, and it is usually given after other antiviral drugs have been tried unsuccessfully. It is an antiviral medication. Common side effects include nausea, or mild rash.
The recommended adult oral dose of Intelence is 200 mg (one 200 mg tablet or two 100 mg tablets) taken twice daily following a meal. Pediatric dose is based on body weight. Intelence may interact with blood thinners, clopidogrel, darunavir, lopinavir/ritonavir, dexamethasone, diazepam, cyclosporine, cholesterol medications, maraviroc, methadone, sildenafil, sirolimus, tacrolimus, antibiotics, antifungals, or heart rhythm medications. Many other medicines can interact with Intelence, or make it less effective. Tell your doctor all medications and supplements you use. During pregnancy, Intelence should be used only when prescribed. It is unknown if this medication passes into breast milk. Because breast milk can transmit HIV, do not breastfeed.
Our Intelence (etravirine) 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.
Intelence 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.
In rare cases, etravirine can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness especially if you also have fever, unusual tiredness, and dark colored urine.
Stop taking etravirine and call your doctor at once if you have a serious side effect such as:
- fever, chills, muscle weakness, joint or muscle pain, mouth sores, feeling very tired, or any other signs of new infection;
- chest pain, feeling short of breath;
- confusion, seizure;
- urinating less than usual or not at all, swelling, rapid weight gain;
- rapid heart rate, increased sweating, tremors, sleep problems (insomnia), feeling anxious or irritable;
- severe diarrhea, unexplained weight loss, menstrual changes, impotence, loss of interest in sex;
- swelling in your neck or throat (enlarged thyroid);
- weakness or prickly feeling in your fingers or toes;
- problems with balance or eye movement, trouble speaking or swallowing;
- severe lower back pain, loss of bladder or bowel control;
- nausea, upper stomach pain, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
- the first sign of any type of skin rash, no matter how mild; or
- severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.
Less serious side effects may include:
- numbness or tingly feeling in your hands or feet;
- dizziness, drowsiness;
- blurred vision;
- upset stomach, constipation, heartburn, dry mouth;
- 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 Intelence (Entravirine Tablets) »
What is Patient Information Overview?
A concise overview of the drug for the patient or caregiver from First DataBank.
Intelence Overview - Patient Information: Side Effects
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).
Tell your doctor right away if any of these unlikely but serious side effects occur: increased thirst/urination, change in the amount of urine, mental/mood changes (e.g., nervousness, confusion), seizures.
Get medical help right away if any of these rare but very serious side effects occur: chest/jaw/left arm pain, persistent nausea/vomiting, severe stomach/abdominal pain, dark urine, yellowing eyes/skin.
Changes in body fat may occur while you are taking this medication (e.g., 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 role of exercise to reduce this side effect.
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
Etravirine can commonly cause a mild rash that is usually not serious. The rash usually occurs during the second week of treatment and goes away in 1 to 2 weeks. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe allergic reaction. Therefore, get medical help right away if you develop any rash, especially with symptoms such as fever, tiredness, muscle/joint pain, blisters, mouth sores, or red/swollen eyes.
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 Intelence (Entravirine Tablets)»
What is Prescribing information?
The FDA package insert formatted in easy-to-find categories for health professionals and clinicians.
Intelence FDA Prescribing Information: Side Effects
The following adverse reactions are described in greater detail in other sections:
- Severe skin and hypersensitivity reactions [see WARNINGS AND PRECAUTIONS].
Clinical Trials Experience: Adults
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The safety assessment is based on all data from 1203 subjects in the Phase 3 placebo-controlled trials, TMC125C206 and TMC125-C216, conducted in antiretroviral treatment-experienced HIV-1-infected adult subjects, 599 of whom received INTELENCE® (200 mg twice daily). In these pooled trials, the median exposure for subjects in the INTELENCE® arm and placebo arm was 52.3 and 51.0 weeks, respectively. Discontinuations due to adverse drug reactions (ADRs) were 5.2% in the INTELENCE® arm and 2.6% in the placebo arm.
The most frequently reported ADR at least Grade 2 in severity was rash (10.0%). Stevens-Johnson syndrome, drug hypersensitivity reaction and erythema multiforme were reported in less than 0.1% of subjects during clinical development with INTELENCE® [see WARNINGS AND PRECAUTIONS]. A total of 2.2% of HIV-1-infected subjects in Phase 3 trials receiving INTELENCE® discontinued due to rash. In general, in clinical trials, rash was mild to moderate, occurred primarily in the second week of therapy, and was infrequent after Week 4. Rash generally resolved within 1 to 2 weeks on continued therapy. The incidence of rash was higher in women compared to men in the INTELENCE® arm in the Phase 3 trials (rash ≥ Grade 2 was reported in 9/60 [15.0%] women versus 51/539 [9.5%] men; discontinuations due to rash were reported in 3/60 [5.0%] women versus 10/539 [1.9%] men). Patients with a history of NNRTI-related rash did not appear to be at increased risk for the development of INTELENCE®related rash compared to patients without a history of NNRTI-related rash.
Common Adverse Reactions
Clinical ADRs of moderate intensity or greater (greater than or equal to Grade 2) and reported in at least 2% of subjects treated with INTELENCE® and occurring at a higher rate compared to placebo (excess of 1%) are presented in Table 1. Laboratory abnormalities considered ADRs are included in Table 2.
Table 1: Treatment-Emergent Adverse Reactions* of at
least Moderate Intensity† (Grades 2 to 4) in at least 2% of Adult
Subjects in the INTELENCE® Treatment Groups and at a higher rate compared to
placebo (excess of 1%)
|System Organ Class, Preferred Term, %||Pooled TMC125-C206 and TMC125-C216 Trials|
|INTELENCE® + BR
|Placebo + BR
|Nervous System Disorders|
|Skin and Subcutaneous Tissue Disorders|
|N=total number of subjects per treatment group, BR=background
* Includes adverse reactions at least possibly, probably, or very likely related to the drug.
† Intensities are defined as follows: Moderate (discomfort enough to cause interference with usual activity); Severe (incapacitating with inability to work or do usual activity).
Less Common Adverse Reactions
Treatment-emergent ADRs occurring in less than 2% of subjects (599 subjects) receiving INTELENCE® and of at least moderate intensity (greater than or equal to Grade 2) are listed below by body system:
Ear and Labyrinth Disorders: vertigo
Eye Disorders: blurred vision
General Disorders and Administration Site Conditions: sluggishness
Hematologic Disorders: hemolytic anemia
Immune System Disorders: drug hypersensitivity, immune reconstitution syndrome
Psychiatric Disorders: anxiety, sleep disorders, abnormal dreams, confusional state, disorientation, nervousness, nightmares
Renal and Urinary Disorders: acute renal failure
Reproductive System and Breast Disorders: gynecomastia
Respiratory,Thoracic and Mediastinal Disorders: exertional dyspnea, bronchospasm
Additional ADRs of at least moderate intensity observed in other trials were acquired lipodystrophy, angioneurotic edema, erythema multiforme and haemorrhagic stroke, each reported in no more than 0.5% of subjects.
Laboratory Abnormalities in Treatment-Experienced Patients
Selected Grade 2 to Grade 4 laboratory abnormalities that represent a worsening from baseline observed in adult subjects treated with INTELENCE® are presented in Table 2.
Table 2: Selected Grade 2 to 4 Laboratory
Abnormalities Observed in Treatment-Experienced Subjects
|Laboratory Parameter Preferred Term, %||DAIDS Toxicity Range||Pooled TMC125-C206 and TMC125-C216 Trials|
|INTELENCE® + BR
|Placebo + BR
|Grade 2||> 1.5-2 x ULN||7%||8%|
|Grade 3||> 2-5 x ULN||7%||8%|
|Grade 4||> 5 x ULN||2%||1%|
|Grade 2||> 1.5-3 x ULN||4%||6%|
|Grade 3||> 3-5 x ULN||2%||2%|
|Grade 4||> 5xULN||1%||< 1%|
|Grade 2||> 1.4-1.8 x ULN||6%||5%|
|Grade 3||> 1.9-3.4 x ULN||2%||1%|
|Grade 4||> 3.4 x ULN||0%||< 1%|
|Grade 2||90-99 g/L||2%||4%|
|Grade 3||70-89 g/L||< 1%||< 1%|
|Grade 4||< 70 g/L||< 1%||< 1%|
|White blood cell count|
|Grade 4||< 1,000/mm³||1%||< 1%|
|Grade 4||< 500/mm³||2%||3%|
|Grade 4||< 25,000/mm³||< 1%||< 1%|
|LIPIDS AND GLUCOSE|
|Grade 2||> 6.20-7.77 mmol/L 240-300 mg/dL||20%||17%|
|Grade 3||> 7.77 mmol/L > 300 mg/dL||8%||5%|
|Low density lipoprotein|
|Grade 2||4.13-4.9 mmol/L 160-190 mg/dL||13%||12%|
|Grade 3||> 4.9 mmol/L > 190 mg/dL||7%||7%|
|Grade 2||5.65-8.48 mmol/L 500 -750 mg/dL||9%||7%|
|Grade 3||8.49-13.56 mmol/L 751 - 1200 mg/dL||6%||4%|
|Grade 4||> 13.56 mmol/L > 1200 mg/dL||4%||2%|
|Elevated glucose levels|
|Grade 2||6.95-13.88 mmol/L 161-250 mg/dL||15%||13%|
|Grade 3||13.89-27.75 mmol/L 251 - 500 mg/dL||4%||2%|
|Grade 4||> 27.75 mmol/L > 500 mg/dL||0%||< 1%|
|Alanine amino transferase|
|Grade 2||2.6-5 x ULN||6%||5%|
|Grade 3||5.1-10 x ULN||3%||2%|
|Grade 4||> 10 x ULN||1%||< 1%|
|Aspartate amino transferase|
|Grade 2||2.6-5 x ULN||6%||8%|
|Grade 3||5.1-10 x ULN||3%||2%|
|Grade 4||> 10 x ULN||< 1%||< 1%|
|ULN=Upper Limit of Normal, BR=background regimen|
Patients co-infected with hepatitis B and/or hepatitis C virus
In Phase 3 trials TMC125-C206 and TMC125-C216, 139 subjects (12.3%) with chronic hepatitis B and/or hepatitis C virus co-infection out of 1129 subjects were permitted to enroll. AST and ALT abnormalities occurred more frequently in hepatitis B and/or hepatitis C virus co-infected subjects for both treatment groups. Grade 2 or higher laboratory abnormalities that represent a worsening from baseline of AST, ALT or total bilirubin occurred in 27.8%, 25.0% and 7.1% respectively, of INTELENCE®-treated co-infected subjects as compared to 6.7%, 7.5% and 1.8% of non-co-infected INTELENCE®-treated subjects. In general, adverse events reported by INTELENCE®treated subjects with hepatitis B and/or hepatitis C virus co-infection were similar to INTELENCE®-treated subjects without hepatitis B and/or hepatitis C virus co-infection.
Clinical Trials Experience: Pediatric Subjects (6 years to less than 18 years of age)
The safety assessment in children and adolescents is based on the Week 24 analysis of the single-arm, Phase 2 trial TMC125-C213 in which 101 antiretroviral treatment-experienced HIV-1 infected subjects 6 years to less than 18 years of age and weighing at least 16 kg received INTELENCE in combination with other antiretroviral agents [see Clinical Studies]. The frequency, type and severity of adverse drug reactions in pediatric subjects were comparable to those observed in adult subjects, except for rash which was observed more frequently in pediatric subjects. The most common adverse drug reactions in at least 2% of pediatric subjects were rash and diarrhea. Rash was reported more frequently in female subjects than in male subjects (rash ≥ Grade 2 was reported in 13/64 [20.3%] females versus 2/37 [5.4%] males); discontinuations due to rash were reported in 4% of subjects (4/64 [6.3%] females versus 0/37 [0%] males). Rash (greater than or equal to Grade 2) occurred in 15% of pediatric subjects. In the majority of cases, rash was mild to moderate, of macular/papular type, and occurred in the second week of therapy. Rash was self-limiting and generally resolved within 1 week on continued therapy. The safety profile for subjects who completed 48 weeks of treatment was similar to the safety profile for subjects who completed 24 weeks of treatment.
The following events have been identified during postmarketing use of INTELENCE®. Because these events 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.
Immune System Disorders: Severe hypersensitivity reactions including DRESS and cases of hepatic failure have been reported [see WARNINGS AND PRECAUTIONS].
Musculoskeletal and Connective Tissue Disorders: rhabdomyolysis
Skin and Subcutaneous Tissue Disorders: Fatal cases of toxic epidermal necrolysis have been reported [see WARNINGS AND PRECAUTIONS].
Read the entire FDA prescribing information for Intelence (Entravirine Tablets) »
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