Efavirenz Side Effects

Brand Names: Sustiva

Please note - some side effects for Efavirenz may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Side Effects of Efavirenz - for the Consumer

Efavirenz

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome when using Efavirenz:

Abnormal dreams; diarrhea; dizziness; drowsiness; headache; nausea; tiredness; trouble concentrating; trouble sleeping; upset stomach; vomiting.

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); burning, numbness, or tingling; change in personality; confusion; cough; delusions; fainting; fever, chills, or persistent sore throat; hallucinations; irregular heartbeat; memory loss; mental, mood, or behavior changes (eg, abnormal thoughts, agitation, aggression, anxiety, depression, nervousness, paranoia); mouth sores; rash with or without fever; red, swollen, blistered, or peeling skin; seizures; severe or persistent tiredness or weakness; severe stomach pain; shortness of breath; suicidal thoughts or behaviors; symptoms of liver problems (eg, dark urine, loss of appetite, pale stools, yellowing of the skin or eyes); vision changes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

Efavirenz/Emtricitabine/Tenofovir

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome when using Efavirenz/Emtricitabine/Tenofovir:

Back pain; cough; darkened skin color on the palms of hands or soles of feet; diarrhea; dizziness; drowsiness; gas or indigestion; headache; loss of appetite; mild stomach pain; muscle or joint aches; nausea; skin discoloration (small spots or freckles); stomach upset; strange dreams; stuffy or runny nose; tiredness; trouble concentrating; trouble sleeping; vomiting.

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); bone pain; change in personality; chest pain; confusion; decreased coordination; delusions; fever, chills, or persistent sore throat; hallucinations; memory loss; mental, mood, or behavior changes (eg, abnormal thoughts, agitation, aggression, anxiety, depression, nervousness, paranoia); muscle pain or weakness; numbness, burning, pain, or tingling of the hands, feet, or skin; red, swollen, blistered, or peeling skin; seizures; severe or persistent stomach pain, nausea, or vomiting; shortness of breath; suicidal thoughts or actions; symptoms of kidney problems (eg, increased or decreased urination, increased thirst); symptoms of lactic acidosis (eg, dizziness or lightheadedness; fast or difficult breathing; fast or irregular heartbeat; feeling cold, especially in the arms and legs; stomach pain with nausea and vomiting; unusual muscle pain; unusual weakness or tiredness); symptoms of liver problems (eg, dark urine; pale stools; persistent loss of appetite; yellowing of the skin or eyes).

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

Side Effects by Body System - for Healthcare Professionals

General

The most significant side effects associated with efavirenz have included nervous system symptoms, psychiatric symptoms, and rash. The most common side effects of at least moderate severity have included rash, dizziness, nausea, headache, fatigue, insomnia, and vomiting in greater than 5% of patients treated with efavirenz in combination with lamivudine-zidovudine or indinavir.

Nervous system

Nervous system symptoms generally begin the first or second day of therapy and often resolve after 2 to 4 weeks. Dosing at bedtime may improve the tolerability of these effects.

Nervous system side effects of moderate or severe intensity have included dizziness (up to 9%), headache (up to 8%), insomnia (up to 7%), impaired concentration (up to 5%), abnormal dreams (up to 3%), and somnolence (up to 2%). Nervous system symptoms of any grade and regardless of causality (52.7%) included dizziness (28.1%), insomnia (16.3%), impaired concentration (8.3%), somnolence (7%), abnormal dreams (6.2%), hallucinations (1.2%), amnesia, agitation, euphoria, depersonalization, confusion, abnormal thinking, and stupor during clinical trials of efavirenz in combination with other antiretroviral agents. These symptoms were mild in 33.3%, moderate in 17.4%, and severe in 2% of patients. Therapy was discontinued in 2.1% of patients due to these side effects. Vivid dreams, nightmares, and impaired attention span have also been reported. Abnormal coordination, ataxia, cerebellar coordination and balance disturbances, convulsions, hypoesthesia, paresthesia, neuropathy, tremor, vertigo, and tinnitus have been reported during postmarketing experience.

Psychiatric

Psychiatric side effects have included depression (moderate or severe intensity: up to 5%; any severity: up to 19%), anxiety (moderate or severe intensity: up to 4%; any severity: up to 13%), and nervousness (moderate or severe intensity: up to 2%; any severity; up to 7%). Psychiatric side effects classified as serious during controlled trials included severe depression (2.4%), suicidal ideation (0.7%), nonfatal suicide attempts (0.5%), aggressive behavior (0.4%), paranoid reactions (0.4%), and manic reactions (0.2%). One percent of patients discontinued or interrupted efavirenz treatment due to one or more of these side effects. Obsessive disorder, irritability, and mood changes have also been reported. Aggressive reactions, agitation, delusions, emotional lability, mania, neurosis, paranoia, psychosis, and suicide have been reported during postmarketing experience.

Psychiatric symptoms generally begin the first or second day of therapy and often resolve after 2 to 4 weeks. Dosing at bedtime may improve the tolerability of these effects.

Dermatologic

The median time to onset of rash in adults was 11 days. In most patients, the rash resolved within one month despite continued use of the drug. Patients who discontinue efavirenz therapy because of rash may be reinstated with the use of appropriate antihistamines and/or corticosteroids. The drug should be withdrawn if severe rash develops, such as that associated with blistering, desquamation, mucosal involvement, or fever.

There is limited experience with the use of efavirenz in patients who have previously discontinued other nonnucleoside reverse transcriptase inhibitors (NNRTIs) due to rash. In 19 such patients formerly on nevirapine, approximately half developed a mild to moderate rash, and two of them discontinued efavirenz because of the rash.

Dermatologic side effects of moderate or severe intensity have included rash (includes erythema multiforme, rash, erythematous rash, follicular rash, maculopapular rash, petechial rash, pustular rash, urticaria, macules, papules, erythema, redness, inflammation, allergic rash, welts, hives, and itchy; up to 16%) and pruritus (up to 9%). Skin rash of any grade (26.3%) included Grade 1 rash (erythema, pruritus; 10.7%), Grade 2 rash (diffuse maculopapular rash, dry desquamation; 14.7%), Grade 3 rash (vesiculation, moist desquamation, ulceration; 0.8%), and Grade 4 rash (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, necrosis requiring surgery, exfoliative dermatitis; 0.1%) during clinical trials. Treatment was discontinued in 1.7% of patients due to rash. Nail disorders, skin discoloration, and leukocytoclastic vasculitis have also been reported. Erythema multiforme, photoallergic dermatitis, and Stevens-Johnson syndrome have been reported during postmarketing experience.

Gastrointestinal

Gastrointestinal side effects of moderate or severe intensity have included diarrhea (up to 14%), nausea (up to 10%), vomiting (up to 6%), dyspepsia (up to 4%), abdominal pain (up to 3%), and anorexia (up to 2%). Pancreatitis has been reported, although causality was not determined. Burning mouth syndrome has also been reported. Constipation and malabsorption have been reported during postmarketing experience.

A 42-year-old HIV-positive woman's saquinavir in her highly active antiretroviral therapy was replaced with efavirenz to increase compliance. Two weeks following efavirenz initiation, the patient reported severe and constant burning in her tongue, gums, and oral mucosa and was diagnosed with burning mouth syndrome (BMS). Efavirenz therapy was discontinued and the BMS resolved within a week.

Hepatic

Isolated elevations of GGT in patients receiving efavirenz may reflect the enzyme inducing effects of the drug not associated with liver toxicity.

Some of the postmarketing reports of hepatic failure occurred in patients with no preexisting liver disease or other identifiable risk factors.

Hepatic side effects have included increased ALT (greater than 5 times ULN; up to 8%), AST (greater than 5 times ULN; up to 8%), and GGT (greater than 5 times ULN; up to 8%). During clinical trials, elevations in ALT and AST to greater than five times ULN occurred in 20% and 13%, respectively, of patients seropositive for hepatitis B and/or C treated with efavirenz. Treatment was discontinued in 3% of coinfected patients due to liver or biliary system disorders. Hepatic failure (a few reports were characterized by a fulminant course, with some cases progressing to transplantation or death), hepatic enzyme increase, and hepatitis have been reported during postmarketing experience.

Hematologic

Hematologic side effects have included neutropenia (less than 750/mm3) in up to 10% of patients. Hemolytic anemia has been reported rarely.

Other

Other side effects of moderate or severe intensity have included pain (up to 13%) and fatigue (up to 8%). Elevated amylase (greater than 2 times ULN; up to 6%), asymptomatic increases in serum amylase levels, and vitamin D deficiency have been reported. Contraceptive failure (with an implantable hormonal contraceptive) and asthenia have been reported during postmarketing experience.

Metabolic

Metabolic side effects have included increased nonfasting triglycerides (greater than or equal to 751 mg/dL; up to 11%) and increased glucose (greater than 250 mg/dL; up to 5%). Increased nonfasting serum cholesterol (up to 54%) and HDL (up to 35%) have been reported, although the clinical significance of these elevations is unknown. Redistribution and accumulation of body fat including central obesity, dorsocervical fat enlargement, peripheral wasting, facial wasting, breast enlargement, and "cushingoid appearance" have been observed in patients receiving antiretroviral therapy. Hypercholesterolemia and hypertriglyceridemia have been reported during postmarketing experience.

Cardiovascular

Cardiovascular side effects have included flushing and palpitations during postmarketing experience. QT interval prolongation and torsades de pointes have been reported.

Hypersensitivity

Hypersensitivity side effects have included skin rash, eosinophilia, and systemic involvement (lymphadenopathy, interstitial nephritis, pneumonia, pulmonary infiltration, hepatitis, fever, rigor, myalgia, and arthralgias). Allergic reactions have been reported during postmarketing experience.

Musculoskeletal

Musculoskeletal side effects have included arthralgia, myalgia, and myopathy during postmarketing experience. Osteomalacia due to efavirenz-induced vitamin D deficiency has been reported.

Immunologic

Immunologic side effects have included immune reconstitution syndrome in patients treated with combination antiretroviral therapy, including efavirenz.

Genitourinary

Analysis of a 3 mm stone, eliminated by a 47-year-old HIV-1-infected male patient, showed a stone consisting of 60% efavirenz metabolites.

Genitourinary side effects have included rare cases of renal colic and urolithiasis.

Respiratory

Respiratory side effects have included dyspnea during postmarketing experience.

Endocrine

Endocrine side effects have included gynecomastia during postmarketing experience.

Ocular

Ocular side effects have included abnormal vision during postmarketing experience.

Renal

Renal side effects have included at least one report of podocyte damage.

Other

False positive urine drug screening test results for tetrahydrocannabinol and benzodiazepines have been reported in HIV-infected patients receiving efavirenz. False positive cannabinoid test results have been observed with the CEDIA (Cloned Enzyme Donor ImmunoAssay) DAU Multilevel THC assay and the InstaCheck multidrug Screen Panel. The Triage 8 and the Drug Screen Multi 5 have shown false-positive results for benzodiazepines and tetrahydrocannabinol.

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