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

Applies to etravirine: oral tablet.

Serious side effects of Intelence

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, itching
• hoarseness
• irritation
• joint pain, stiffness, or swelling
• muscle pain
• red skin lesions, often with a purple center
• red, irritated eyes
• redness of the skin
• 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

Incidence not known

• Dark urine
• general feeling of tiredness or weakness
• headache
• light-colored stools
• stomach pain, continuing
• swollen, painful, or tender lymph glands in the neck, armpit, or groin
• vomiting
• yellow eyes or skin

Other side effects of Intelence

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:

Less common

• Stomach pain

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, prurigo, dry skin

Uncommon (0.1% to 1%): Hyperhidrosis, 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), Stevens-Johnson syndrome (fatal cases), drug rash with eosinophilia and systemic symptoms (DRESS)^[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, abdominal distension, constipation, dry mouth, stomatitis, elevated blood amylase

Uncommon (0.1% to 1%): Pancreatitis, hematemesis, retching^[Ref]

Metabolic

Very common (10% or more): Elevated glucose levels (up to 15%)

Common (1% to 10%): Hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, hyperglycemia, diabetes mellitus, 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, somnolence, paresthesia, hypoesthesia, amnesia

Uncommon (0.1% to 1%): Convulsion, syncope, disturbance in attention, hypersomnia, tremor, vertigo, hemorrhagic stroke^[Ref]

Renal

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

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

Hematologic

Common (1% to 10%): Decreased neutrophils, decreased platelet count, decreased hemoglobin, decreased WBC count, anemia, thrombocytopenia

Frequency not reported: Hemolytic anemia^[Ref]

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]

Cardiovascular

Common (1% to 10%): Hypertension, myocardial infarction

Uncommon (0.1% to 1%): Angina pectoris, atrial fibrillation

Frequency not reported: Mild atrioventricular block^[Ref]

Psychiatric

Common (1% to 10%): Insomnia, anxiety, sleep disorders

Uncommon (0.1% to 1%): Abnormal dreams, confusional state, disorientation, nervousness, nightmares^[Ref]

Ocular

Common (1% to 10%): Blurred vision^[Ref]

Respiratory

Common (1% to 10%): Exertional dyspnea

Uncommon (0.1% to 1%): Bronchospasm^[Ref]

Hypersensitivity

Uncommon (0.1% to 1%): Drug hypersensitivity

Postmarketing reports: Severe hypersensitivity reactions (including DRESS and cases of hepatic failure)^[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, autoimmune hepatitis)^[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]