Names and pronunciation
(ef-ah-veer′enz) Sustiva
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Individual generic drug information
Extracted information for efavirenz only.
(ef-ah-veer′enz) Sustiva
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Func. class.: Antiretroviral
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Chem. class.: Nonnucleoside reverse transcriptase inhibitor (NNRTI)
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ACTION: Binds directly to reverse transcriptase and blocks RNA, DNA poly- merase, thus causing a disruption of the enzyme’s site
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USES: HIV-1 in combination with at least 2 other antivirals
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Unlabeled uses: HIV prophylaxis
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Extracted information for efavirenz only.
CONTRAINDICATIONS: Preg- nancy, hypersensitivity, moderate/severe hepatic disease Precautions: Breastfeeding, children <3 yr, renal/hepatic disease, myelosup- pression, depression, seizures
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SIDE EFFECTS CNS: Fatigue, impaired cognition, insomnia, abnormal dreams, depres- sion, headache, dizziness, anxiety, drowsiness, odd feeling, suicidal thoughts/behaviors GI: Diarrhea, abdominal pain, nausea, vomiting, hepatotoxicity GU: Hematuria, kidney stones INTEG: Rash, Stevens-Johnson syn- drome, toxic epidermal necrolysis, exfoli- ative dermatitis SYST: Immune reconstitution syndrome MISC: Fat accumulation/redistribution ENDO: Hyperlipidemia CV: QT prolongation
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INTERACTIONS • Avoid use with boceprevir, delavir- dine, rilpivirine; dosage change may be needed if given with telaprevir • Do not give together with benzodiaze- pines, ergots, midazolam, triazolam, pimo- zide Increase: CNS depression—alcohol, antidepressants, antihistamines, opioids Increase: levels of both products— ritonavir, estrogens, anticonvulsants Increase: levels of warfarin, statins (except pravastatin, fluvastatin) Decrease: levels of indinavir, amprena- vir, lopinavir, oral contraceptives, ketoconazole, itraconazole, posacon- azole, voriconazole, saquinavir, cyclo- sporine, tacrolimus, sirolimus, buPRO- Pion, sertraline Decrease: metabolism of CYP2B6 inhibi- tors, CYP2C19 substrates, CYP3A4 substrates Decrease: efavirenz metabolism—CYP3A4 inhibitors (conivaptan, ambrisentan, SORAfenib) Decrease: efavirenz effect—CYP3A4 inducers (carBAMazepine, rifamycins) Drug/Herb Decrease: efavirenz level—St. John’s wort; do not use together Drug/Food Increase: absorption—high-fat foods Drug/Lab Test Increase: ALT False positive: cannabinoids
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Extracted information for efavirenz only.
DOSAGE AND ROUTES • Adult and child ≥3 mo and >40 kg: PO 600 mg/day at bedtime • Child ≥3 mo, 32.5-39.9 kg: PO 400 mg/day at bedtime • Child ≥3 mo, 25-32.4 kg: PO 350 mg/ day at bedtime • Child ≥3 mo, 20-24.9 kg: PO 300 mg/ day at bedtime • Child ≥3 mo, 15-19.9 kg: PO 250 mg/ day at bedtime • Child ≥3 mo, 7.5-14.9 kg: PO 200 mg/day at bedtime • Child ≥3 mo, 5-<7.5 kg: PO 150 mg/ day at bedtime • Child ≥3 mo, 3.5-#5 kg: PO 100 mg/ day at bedtime
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Available forms: Capsules 50-, 200- mg; 600-mg tablets
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Administer: • Give on empty stomach; give at bed- time to decrease CNS side effects • Capsules may be opened, added to grape jelly to disguise peppery taste or sprinkled on food, may be mixed in for- mula, do not cut/break tablets
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Extracted information for efavirenz only.
Assess: • HIV: monitor CBC with differential, plasma HIV RNA, absolute CD4+/CD8+ cell counts/%, serum β2 microglobu- lin, serum ICD+24 antigen levels, cholesterol, hepatic enzymes, blood glucose, pregnancy test, bilirubin, uri- nalysis • Assess for suicidal thoughts/behaviors, poor concentration, dizziness, inability to sleep, usually resolves after 4 wk, give at bedtime • Bowel pattern prior to, during treat- ment; if severe abdominal pain with bleeding occurs, product should be discontinued; monitor hydration • Serious skin reactions: Stevens- Johnson syndrome, toxic epidermal necrolysis, usually occurs during first 2 wk, mild rash may resolve within 30 days; severe skin reactions including blistering, fever, product should be dis- continued immediately and corticoste- roids started • Signs of toxicity: severe nausea/ vomiting, maculopapular rash • Hepatotoxicity: LFTs in those with liver disease, hold if LFTs are moder- ately elevated; if severe or if LFTs in- crease after product is restarted, discontinue permanently, do not breast- feed • Pregnancy/breastfeeding: rule out pregnancy prior to starting treatment; use contraception, oral/nonhormonal contraceptives are decreased, use bar- rier methods also. Avoid use in first tri- mester (particular caution in first 8 wk of pregnancy) and in females of child- bearing potential. Register pregnant women with Antiretroviral Pregnancy Registry (800-258-4263)
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Evaluate: • Therapeutic response: increased CD4 cell counts; decreased viral load; slowing progression of HIV
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take as prescribed; if dose is missed, to take as soon as remem- bered; not to double dose; to take with water, juice; to take on empty stomach at bedtime; to take at same time of day; not to break tablets; to use with other antiretrovirals • To make sure health care provider knows all medications, supplements, OTC products taken • To notify health care provider if se- vere rash occurs; that adverse reactions (rash, dizziness, abnormal dreams, in- somnia) lessen after 1 mo, not to stop E taking • To avoid hazardous activities if dizzi- ness, drowsiness occur • That product does not cure disease but controls symptoms; that HIV can be transmitted to others even while taking this product; to continue with safe-sex practices, that opportunistic infections can occur • To report all adverse reactions, in- somnia, poor concentration, but usually are less in 2-4 wk • That CNS side effects of feeling “stoned” or “drunk” usually abate in several months • Pregnancy/breastfeeding: Identify if pregnancy is planned or suspected or if breastfeeding; not to breastfeed or be- come pregnant if taking this product; to use nonhormonal contraception because serious birth defects have occurred, to use barrier method for ≥12 wk after last dose
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Extracted information for efavirenz only.
PHARMACOKINETICS Peak 3-5 hr, duration up to 24 hr, well absorbed, metabolized by liver; half- life 40-76 hr; >99% protein binding, excreted in urine, feces; concentra- tions higher in females and in those of African, Asian, and Hispanic descent
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Filter the extracted dose blocks for this individual drug.
• Adult and child ≥3 mo and >40 kg: PO 600 mg/day at bedtime
Candidate age grouping · source page 448