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Intelence Side Effects

Generic Name: etravirine

Note: This document contains side effect information about etravirine. Some of the dosage forms listed on this page may not apply to the brand name Intelence.

For the Consumer

Applies to etravirine: oral tablet

Along with its needed effects, etravirine (the active ingredient contained in Intelence) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking etravirine:

More common
  • Rash
Less common
  • Blurred vision
  • burning, numbness, tingling, or painful sensations
  • dizziness
  • headache
  • nervousness
  • pounding in the ears
  • slow or fast heartbeat
  • unsteadiness or awkwardness
  • weakness in the arms, hands, legs, or feet
Rare
  • Blistering, peeling, or loosening of the skin
  • chills
  • cough
  • diarrhea
  • fever
  • hives
  • hoarseness
  • irritation
  • itching
  • joint pain, stiffness, or swelling
  • muscle pain
  • red skin lesions, often with a purple center
  • red, irritated eyes
  • redness of the skin
  • shortness of breath
  • sore throat
  • sores, ulcers, or white spots in the mouth or on the lips
  • swelling of the eyelids, face, lips, hands, or feet
  • tightness in the chest
  • trouble with breathing or swallowing
  • unusual tiredness or weakness
  • wheezing

Some side effects of etravirine may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common Less common

For Healthcare Professionals

Applies to etravirine: oral tablet

General

The safety report of this drug is based on 599 HIV-1-infected, therapy-experienced patients receiving 200 mg twice daily in combination with background regimen; the median exposure was 52.3 weeks. The most commonly reported side effects (of all intensities) were rash, diarrhea, nausea, and headache. Discontinuation due to side effects occurred in 5.2% of patients using this drug; a total of 2.2% of HIV-1-infected patients in phase 3 trials discontinued this drug due to rash.[Ref]

Hepatic

Grade 2 or higher abnormalities representing a worsening from baseline of AST, ALT, and total bilirubin have been reported in 27.8%, 25%, and 7.1%, respectively, in patients coinfected with hepatitis B and/or C virus as compared to 6.7%, 7.5%, and 1.8% reported in non-coinfected patients.

Grades 2, 3, and 4 elevated ALT have been reported in 6%, 3%, and 1% of patients, respectively. Grades 2, 3, and 4 elevated AST have been reported in 6%, 3%, and less than 1% of patients, respectively.[Ref]

Very common (10% or more): Worsening from baseline of AST (up to 27.8%), worsening from baseline of ALT (up to 25%)
Common (1% to 10%): Worsening from baseline of total bilirubin, elevated ALT, elevated AST
Uncommon (0.1% to 1%): Hepatomegaly, cytolytic hepatitis, hepatic steatosis, hepatitis
Frequency not reported: Hepatic failure[Ref]

Other

Very common (10% or more): Elevated total cholesterol (up to 20%), elevated low-density lipoprotein (up to 13%)
Common (1% to 10%): Elevated triglycerides, fatigue
Uncommon (0.1% to 1%): Sluggishness
Frequency not reported: Pyrexia

Antiretroviral therapy:
-Frequency not reported: Increased weight[Ref]

Grades 2 and 3 elevated total cholesterol have been reported in 20% and 8% of patients, respectively. Grades 2 and 3 elevated low-density lipoprotein have been reported in 13% and 7% of patients, respectively. Grades 2, 3, and 4 elevated triglycerides have been reported in 9%, 6%, and 4% of patients, respectively.[Ref]

Dermatologic

Very common (10% or more): Rash (up to 19.2%)
Common (1% to 10%): Night sweats, lipohypertrophy
Uncommon (0.1% to 1%): Prurigo, hyperhidrosis, dry skin, face swelling, angioneurotic edema, erythema multiforme, acquired lipodystrophy
Rare (0.01% to 0.1%): Stevens-Johnson syndrome
Very rare (less than 0.01%): Toxic epidermal necrolysis
Frequency not reported: Contact dermatitis, erythema, pruritus
Postmarketing reports: Toxic epidermal necrolysis (fatal cases)[Ref]

During clinical trials, rash generally was mild to moderate, occurred chiefly in the second week of therapy, and was infrequent after the fourth week. Rash usually resolved within 1 to 2 weeks on continued use of the drug. The incidence of rash was higher in women taking this drug (at least grade 2 rash: 15%) compared to men (at least grade 2 rash: 9.5%). Discontinuation due to rash occurred in 5% of women compared to 1.9% of men. Patients with a history of nonnucleoside reverse transcriptase inhibitor-related rash did not appear to be at increased risk.[Ref]

Gastrointestinal

Grades 2, 3, and 4 elevated pancreatic amylase have been reported in 7%, 7%, and 2% of patients, respectively. Grades 2, 3, and 4 elevated lipase have been reported in 4%, 2%, and 1% of patients, respectively.[Ref]

Very common (10% or more): Diarrhea (up to 18%), nausea (up to 14.9%)
Common (1% to 10%): Elevated pancreatic amylase, elevated lipase, abdominal pain, vomiting, gastroesophageal reflux disease, flatulence, gastritis
Uncommon (0.1% to 1%): Abdominal distension, pancreatitis, constipation, dry mouth, hematemesis, retching, stomatitis[Ref]

Metabolic

Very common (10% or more): Elevated glucose levels (up to 15%)
Common (1% to 10%): Hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, hyperglycemia, diabetes mellitus
Uncommon (0.1% to 1%): Anorexia, dyslipidemia

Antiretroviral therapy:
-Frequency not reported: Increased blood lipid levels, increased glucose levels[Ref]

Grades 2 and 3 elevated glucose levels have been reported in 15% and 4% of patients, respectively.[Ref]

Nervous system

Very common (10% or more): Headache (up to 10.9%)
Common (1% to 10%): Peripheral neuropathy
Uncommon (0.1% to 1%): Somnolence, paresthesia, convulsion, hypoesthesia, amnesia, syncope, disturbance in attention, hypersomnia, tremor, vertigo[Ref]

Renal

Common (1% to 10%): Elevated creatinine, renal failure[Ref]

Grades 2 and 3 elevated creatinine have been reported in 6% and 2% of patients, respectively.[Ref]

Hematologic

Grades 2, 3, and 4 decreased neutrophils have been reported in 5%, 4%, and 2% of patients, respectively. Grades 2, 3, and 4 decreased platelet count have been reported in 3%, 1%, and less than 1% of patients, respectively. Grades 2, 3, and 4 decreased hemoglobin have been reported in 2%, less than 1%, and less than 1% of patients, respectively. Grades 2, 3, and 4 decreased WBC count have been reported in 2%, 1%, and 1% of patients, respectively.[Ref]

Common (1% to 10%): Decreased neutrophils, decreased platelet count, decreased hemoglobin, decreased WBC count, anemia, thrombocytopenia
Frequency not reported: Hemolytic anemia[Ref]

Cardiovascular

Common (1% to 10%): Hypertension, myocardial infarction
Uncommon (0.1% to 1%): Angina pectoris, atrial fibrillation, hemorrhagic stroke
Frequency not reported: Mild atrioventricular block[Ref]

Psychiatric

Common (1% to 10%): Insomnia, anxiety
Uncommon (0.1% to 1%): Sleep disorders, abnormal dreams, confusional state, disorientation, nervousness, nightmares[Ref]

Hypersensitivity

Uncommon (0.1% to 1%): Drug hypersensitivity
Postmarketing reports: Severe hypersensitivity reactions (including drug rash with eosinophilia and systemic symptoms [DRESS] and cases of hepatic failure)[Ref]

Ocular

Uncommon (0.1% to 1%): Blurred vision[Ref]

Immunologic

Uncommon (0.1% to 1%): Immune reconstitution syndrome
Frequency not reported: Autoimmune disorders in the setting of immune reconstitution (e.g., Graves' disease, polymyositis, Guillain-Barre syndrome)[Ref]

Respiratory

Uncommon (0.1% to 1%): Exertional dyspnea, bronchospasm[Ref]

Endocrine

Uncommon (0.1% to 1%): Gynecomastia[Ref]

Musculoskeletal

Frequency not reported: Severe myopathy (including articular pain, muscular pain, weakness, stiffness, increased creatine kinase)
Postmarketing reports: Rhabdomyolysis

Combination antiretroviral therapy:
-Frequency not reported: Osteonecrosis[Ref]

References

1. "Etravirine: R165335, TMC 125, TMC-125, TMC125." Drugs R D 7 (2006): 367-73

2. Cerner Multum, Inc. "Australian Product Information." O 0

3. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0

4. Panel on Antiretroviral Guidelines for Adults and Adolescents "Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents Living with HIV Available from: URL: https://aidsinfo.nih.gov/contentfiles/lvguidelines/adultandadolescentgl.pdf." ([2018, Mar 27]):

5. "Drugs for HIV infection." Treat Guidel Med Lett 7 (2009): 11-22

6. "Product Information. Intelence (etravirine)." Ortho Biotech Inc, Bridgewater, NJ.

7. Cohen CJ, Berger DS, Blick G, et al. "Efficacy and safety of etravirine (TMC125) in treatment-experienced HIV-1-infected patients: 48-week results of a phase IIb trial." AIDS 23 (2009): 423-6

8. Johnson LB, Saravolatz LD "Etravirine, a Next-Generation Nonnucleoside Reverse-Transcriptase Inhbitor." Clin Infect Dis (2009):

9. "Etravirine(Intelence) for HIV infection." Med Lett Drugs Ther 50 (2008): 47-8

10. "Anti-HIV agents. Effectiveness of etravirine in treatment-experienced PHAs." TreatmentUpdate 19 (2007): 3-5

11. Peeters M, Janssen K, Kakuda TN, et al. "Etravirine Has No Effect on QT and Corrected QT Interval in HIV-Negative Volunteers (June)." Ann Pharmacother (2008):

12. Borras-Blasco J, Navarro-Ruiz A, Borras C, Castera E "Adverse cutaneous reactions associated with the newest antiretroviral drugs in patients with human immunodeficiency virus infection." J Antimicrob Chemother 62 (2008): 879-88

13. Gruzdev B, Rakhmanova A, Doubovskaya E, et al. "A randomized, double-blind, placebo-controlled trial of TMC125 as 7-day monotherapy in antiretroviral naive, HIV-1 infected subjects." AIDS 17 (2003): 2487-94

14. "Anti-HIV agents. Brain side effects not common with etravirine." TreatmentUpdate 19 (2007): 6-7

15. Tommasi C, Tempestilli M, Fezza R, et al. "A rare case of severe myopathy associated with etravirine use." AIDS 24 (2010): 1088-90

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Some side effects may not be reported. You may report them to the FDA.

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