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1 fected mothers; Pedi: Children ⬍3 mo (safety not established);qincidence of rash;


Geri: Cautious initial dosing due toqincidence of renal or cardiac dysfunction.
PDF Page #1
efavirenz (e-fa-veer-enz) Adverse Reactions/Side Effects
Sustiva CNS: abnormal dreams, depression, dizziness, drowsiness, fatigue, headache, im-
Classification paired concentration, insomnia, nervousness, psychiatric symptomatology. GI: HEP-
Therapeutic: antiretrovirals ATOTOXICITY, nausea, abdominal pain, anorexia, diarrhea, dyspepsia, flatulence. GU:
Pharmacologic: non-nucleoside reverse transcriptase inhibitors hematuria, renal calculi. Derm: rash, sweating, pruritus. Endo: hypercholesterol-
emia, hypertriglyceridemia. Neuro: hypoesthesia. Misc: fat redistribution, immune
Pregnancy Category D reconstitution syndrome.

Indications Interactions
HIV infection (in combination with one or more other antiretroviral agents).
Drug-Drug: qlevels of pimozide, midazolam, triazolam, or ergot alka-
loids when used concurrently; may result in potentially serious adverse reactions in-
Action cluding arrhythmias, CNS, and respiratory depression (concurrent use contraindi-
Inhibits HIV reverse transcriptase, which results in disruption of DNA synthesis. cated). Induces (stimulates) the hepatic cytochrome P450 3A4 enzyme system and
Therapeutic Effects: Slowed progression of HIV infection and decreased occur- would be expected to influence the effects of other drugs that are metabolized by this
rence of sequelae. Increases CD4 cell counts and decreases viral load. system; efavirenz itself is also metabolized by this system.qrisk of CNS depression
with other CNS depressants, including alcohol, antidepressants, antihista-
Pharmacokinetics mines, and opioid analgesics. Concurrent use with ritonavirqlevels of both
Absorption: 50% absorbed when ingested following a high-fat meal. agents and the likelihood of adverse reactions, especially hepatotoxicity. Maypthe
Distribution: 99.5– 99.75% bound to plasma proteins; enters CSF. effectiveness of progestin-containing hormonal contraceptives (e.g. etonoges-
Metabolism and Excretion: Mostly metabolized by the liver. trel, norelgestromin, levonorgestrel). Use with voriconazole significantlypvori-
Half-life: Following single dose— 52– 76 hr. Following multiple doses— 40– conazole levels andqefavirenz levels; concurrent use with standard doses of vori-
55 hr. conazole is contraindicated; if used together,qdose of voriconazole to 400 mg q 12
hr andpdose of efavirenz to 300 mg daily. Maypposaconazole levels (avoid con-
TIME/ACTION PROFILE (blood levels) current use).pindinavir levels (indinavir doseqrecommended).psaquinavir
ROUTE ONSET PEAK DURATION levels (avoid using saquinavir as the only protease inhibitor with efavirenz).pmara-
viroc levels (maraviroc doseqrecommended). May alter the effects of warfarin.
PO rapid 3–5 hr 24 hr
Mayplevels of cyclosporine, tacrolimus, and sirolimus. Mayplevels of bupro-
pion and sertraline. Rifampin mayplevels (qdose of efavirenz). Concurrent use
Contraindications/Precautions with other NNRTIs including etravirine, nevirapine, rilpivirine, and delavir-
Contraindicated in: Hypersensitivity; Concurrent pimozide, midazolam, triazo- dine may lead topeffectiveness and should be avoided. Mayplevels of raltegravir.
lam, voriconazole (standard doses), St. John’s wort, or ergot derivatives; Moderate to Mayplevels of boceprevir; avoid concurrent use. Concurrent use with telaprevir
severe hepatic impairment. mayplevels of telaprevir and efavirenz.
Use Cautiously in: History of mental illness or substance abuse (qrisk of psychi- Drug-Natural Products: Use with St. John’s wort may causeplevels and effec-
atric symptomatology); Mild hepatic impairment; History of seizure disorders (qrisk tiveness, including development of drug resistance (concurrent use contraindi-
of seizures); OB: Use in pregnancy only if other options have been exhausted; birth cated).
defects have been reported; Lactation: Breast feeding not recommended for HIV-in- Drug-Food: Ingestion following a high-fat mealqabsorption by 50%.
⫽ Canadian drug name. ⫽ Genetic Implication. CAPITALS indicate life-threatening, underlines indicate most frequent. Strikethrough ⫽ Discontinued.
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2 ● May causeqin total cholesterol and serum triglyceride levels.


● Obtain a pregnancy test prior to starting therapy. May cause fetal harm if adminis-
Route/Dosage tered during first trimester of pregnancy. PDF Page #2
PO (Adults and Children ⱖ40 kg): 600 mg once daily; Concurrent rifampin ● May cause false-positive urine cannabinoid results.
therapy (in patients ⬎50 k g)— 800 mg once daily.
PO (Children ⱖ3 mo and 32.5– 39.9 kg): 400 mg once daily. Potential Nursing Diagnoses
PO (Children ⱖ3 mo and 25– 32.4 kg): 350 mg once daily. Risk for infection (Indications)
PO (Children ⱖ3 mo and 20– 24.9 kg): 300 mg once daily. Noncompliance (Patient/Family Teaching)
PO (Children ⱖ3 mo and 15– 19.9 kg): 250 mg once daily.
PO (Children ⱖ3 mo and 7.5– 14.9 kg): 200 mg once daily. Implementation
PO (Children ⱖ3 mo and 5– 7.4 kg): 150 mg once daily. ● PO: Administer on an empty stomach, preferably at bedtime to minimize nervous
PO (Children ⱖ3 mo and 3.5– 4.9 kg): 100 mg once daily. system side effects Avoid taking with a high-fat meal. Do not break tablets.
● Capsule may be opened and contents sprinkled on a small amount (1 to 2 tea-
NURSING IMPLICATIONS spoons) of food for children at least 3 months old and weighing at least 3.5 kg and
Assessment adults who cannot swallow capsules or tablets. Open capsule carefully; avoid spill-
● Assess for change in severity of HIV symptoms and for symptoms of opportunistic age or dispersion of contents into the air. For infants receiving capsule sprinkle-
infections during therapy. infant formula mixture, gently mix entire capsule contents in to 2 teaspoons (10
● Assess for rash, especially during 1st mo of therapy. Onset is usually
mL) of reconstituted room temperature infant formula in a medicine cup, then
within 2 wk and resolves with continued therapy within 1 mo. May range
draw up mixture into a 10 mL oral dosing syringe for administration. Use of infant
from mild maculopapular with erythema and pruritus to exfoliative der-
matitis and Stevens-Johnson syndrome. Occurs more often and may be formula for mixing should only be considered for those young infants who cannot
more severe in children. If rash is severe or accompanied by blistering, consume solid foods. For patients able to tolerate solid foods, mix entire capsule
desquamation, mucosal involvement, or fever, therapy must be discon- contents gently with soft food (applesauce, grape jelly, yogurt). After administra-
tinued immediately. Efavirenz may be reinstated concurrently with anti- tion of mixture, add a small amount (2 teaspoons) of food or formula to empty
histamines or corticosteroids in patients discontinuing due to rash. mixing container, stir to disperse any remaining efavirenz residue, and administer
● Assess patient for CNS and psychiatric symptoms (dizziness, impaired concentra- to patient. Administer mixture within 30 minutes of mixing. Avoid food for 2 hours
tion, somnolence, abnormal dreams, insomnia) during therapy. Symptoms usu- after administration.
ally begin during 1st or 2nd day of therapy and resolve after 2– 4 wk. Administra-
tion at bedtime may minimize symptoms. Concurrent use with alcohol or
Patient/Family Teaching
psychoactive agents may cause additive CNS symptoms. ● Emphasize the importance of taking efavirenz as directed. It must always be used
● Lab Test Considerations: Monitor viral load and CD4 cell count regularly dur- in combination with other antiretroviral drugs. Do not take more than prescribed
ing therapy. amount, and do not stop taking without consulting health care professional. Take
● Monitor liver function tests in patients with a history of hepatitis B or C missed doses as soon as remembered; do not double doses.
or underlying liver disease. May causeqserum AST, ALT, and GGT con- ● Instruct patient that efavirenz should not be shared with others.
centrations. If moderate to severe liver function test abnormalities oc- ● May cause dizziness, impaired concentration, or drowsiness. Caution patient to
cur, efavirenz doses should be held until levels return to normal. Dis- avoid driving or other activities requiring alertness until response to medication is
continue if liver function abnormalities recur when therapy is resumed. known.
䉷 2015 F.A. Davis Company CONTINUED
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PDF Page #3
CONTINUED
efavirenz
● Instruct patient to notify health care professional immediately if rash oc-
curs.
● Inform patient that efavirenz does not cure AIDS or prevent associated or oppor-
tunistic infections. Efavirenz does not reduce the risk of transmission of HIV to
others through sexual contact or blood contamination. Caution patient to use a
condom and to avoid sharing needles or donating blood to prevent spreading the
AIDS virus to others. Advise patient that the long-term effects of efavirenz are un-
known at this time.
● Inform patient that redistribution and accumulation of body fat may occur, caus-
ing central obesity, dorsocervical fat enlargement (buffalo hump), peripheral
wasting, breast enlargement, and cushingoid appearance. The cause and long-
term effects are not known.
● Instruct patient to notify health care professional of all Rx or OTC medications, vi-
tamins, or herbal products being taken and to consult with health care profes-
sional before taking other medications.
● Advise patients taking oral contraceptives to use a nonhormonal method of birth
control during efavirenz therapy and for at least 12 wk following discontinuation
and to notify health care professional if they become pregnant while taking efavi-
renz. Encourage patients who become pregnant during therapy to join the registry
by calling 1-800-258-4263.
● Emphasize the importance of regular follow-up exams and blood counts to deter-
mine progress and monitor for side effects.
Evaluation/Desired Outcomes
● Delayed progression of AIDS and decreased opportunistic infections in patients
with HIV.
● Decrease in viral load and increase in CD4 cell counts.
Why was this drug prescribed for your patient?

⫽ Canadian drug name. ⫽ Genetic Implication. CAPITALS indicate life-threatening, underlines indicate most frequent. Strikethrough ⫽ Discontinued.

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