Sustiva Side Effects

Generic name: efavirenz

Generic Name: Efavirenz

Please note - some side effects for Sustiva may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA at http://www.fda.gov/medwatch/ or 1-800-FDA-1088 (1-800-332-1088).

Side Effects of Sustiva - for the consumer

Sustiva

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 Sustiva:

Abnormal dreams; changes in body fat; diarrhea; dizziness; drowsiness; headache; trouble concentrating; trouble sleeping.

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); bizarre behavior; change in personality, behavior, mood, or emotions; dark urine or pale stools; delusions; hallucinations; memory loss; mouth sores; paranoia; rash with or without fever; severe depression; suicidal thoughts or behaviors; unusual fatigue; vision changes; yellowing of the skin or eyes.

By body system

General side effects

The most significant adverse effects associated with efavirenz have included central nervous system (53% of patients), psychiatric (up to 19%), and dermatologic (up to 45.6%) side effects.

Nervous system side effects

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 as a whole were reported with the highest frequency (53%) during clinical trials of efavirenz in combination with other antiretroviral agents. Most were mild or moderate in severity, including dizziness (up to 10%), insomnia (up to 7%), headache (up to 6%), somnolence (up to 3%), and hypesthesia (up to 2%). These symptoms were classified as severe in 2% of patients and therapy was discontinued in 2.1% of patients due to these side effects. Amnesia, agitation, euphoria, depersonalization, vivid dreams, abnormal dreams, nightmares, confusion, abnormal thinking, impaired concentration, impaired attention span, and hallucinations have also been reported. Abnormal coordination, ataxia, cerebellar coordination and balance disturbances, convulsions, hypoesthesia, paresthesia, neuropathy, and tremor have been reported during postmarketing experience.

Psychiatric side effects

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.

Psychiatric adverse effects that were classified as serious have included depression (up to 19%), severe depression (2.4%), anxiety (up to 13%), nervousness (up to 7%), 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 efavirenz treatment due to one or more of these side effects. Obsessive disorder, irritability, and mood changes have also been reported. Aggressive reactions, delusions, emotional lability, mania, neurosis, paranoia, psychosis, and suicide have been reported during postmarketing experience.

Dermatologic side effects

Dermatologic side effects have included skin rash in 27% of adults and 40% of a small pediatric population during clinical trials. Rash tended to be more severe in children than in adults. Pruritus (up to 9%), nail disorders, skin discoloration, photoallergic dermatitis, leukocytoclastic vasculitis, and Stevens-Johnson syndrome have also been reported.

Grade 1 rash, consisting of erythema and/or pruritus, occurred in approximately 10% of all patients during clinical trials. Grade 2 rash, defined as diffuse maculopapular rash and/or dry desquamation, occurred in 16.7% of adults and 24.5% of pediatric patients. Grade 3 rash, including vesiculation, moist desquamation and ulceration, occurred in less than 1% of adults but in 3.5% of children. Grade 4 rash, the most severe and which includes erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, necrosis requiring surgery and exfoliative dermatitis, occurred in 3.5% of children. The percentage of patients who discontinued treatment due to rash was 1.7% in adults and 8.8% in pediatric patients.

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.

Gastrointestinal side effects

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.

Gastrointestinal side effects associated with efavirenz-containing regimens have included nausea (up to 10%), diarrhea (up to 14%), vomiting (up to 6%), dyspepsia (up to 4%), and abdominal pain (up to 3%). Constipation and malabsorption have been reported in postmarketing experience. Burning mouth syndrome has also been reported.

Hepatic side effects

Hepatic side effects have included increases in ALT (greater than 5 times ULN), AST (greater than 5 times ULN), GGT (greater than 5 times ULN), and amylase (greater than 2 times ULN), most often in patients with hepatitis B and/or C seropositivity. Pancreatitis has been reported, although causality was not determined. Hepatic failure and hepatitis have been reported during postmarketing experience.

During clinical trials, elevations of AST and ALT levels to greater than five times the upper limit of normal occurred in 6% and 13%, respectively, of patients seropositive for Hepatitis B and/or C treated with efavirenz, compared to 5% and 2% of their counterparts in the control group. Elevations of GGT to greater than five times the upper limit of normal were also reported more frequently in efavirenz patients. However, isolated elevations of GGT in patients receiving efavirenz may reflect the enzyme inducing effects of the drug not associated with liver toxicity.

Metabolic side effects

Metabolic side effects have included increases in nonfasting triglycerides (greater than or equal to 751 mg/dL) in up to 11% of patients and increases in nonfasting serum cholesterol in up to 54% and HDL in up to 20% of patients, although the clinical significance of these elevations is unknown.

Endocrine side effects

Endocrine side effects have included gynecomastia during postmarketing experience.

Cardiovascular side effects

Cardiovascular side effects have included postmarketing reports of flushing, palpitations, QT interval prolongation, and torsade de pointes.

Hematologic side effects

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

Hypersensitivity side effects

Hypersensitivity reactions have included skin rash, eosinophilia, and systemic involvement (lymphadenopathy, interstitial nephritis, pneumonia, pulmonary infiltration, hepatitis, fever, rigor, myalgia, and arthralgias).

Musculoskeletal side effects

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

Respiratory side effects

Respiratory side effects have included dyspnea during postmarketing experience.

Ocular side effects

Ocular side effects have included abnormal vision during postmarketing experience.

Other side effects

False positive urine cannabinoid test results have been reported in uninfected volunteers who received efavirenz. False positive test results have been observed with the CEDIA (Cloned Enzyme Donor ImmunoAssay) DAU Multilevel THC assay and the InstaCheck multidrug Screen Panel, which are used for screening, and have not been observed with other assays tested including tests used for confirmation of positive results.

Other side effects

Other side effects have included fatigue (up to 8%), pain (up to 13%), tinnitus, and vitamin D deficiency. Fever and cough has been reported primarily in children.

Other side effects

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.

Genitourinary side effects

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

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.

Renal side effects

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

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