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Related to Sustiva: efavirenz, Videx, Stocrin



Pharmacologic class: Nonnucleoside reverse transcriptase inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category D


Inhibits human immunodeficiency virus (HIV) reverse transcriptase (required for transcription of HIV-1 RNA to DNA), leading to viral cell death


Capsules: 50 mg, 200 mg

Tablets: 600 mg

Indications and dosages

HIV infection (given with one or more additional antiretrovirals)

Adults and children older than age 3 and weighing more than 40 kg (88 lb): 600 mg P.O. once daily

Children weighing 32.5 to 40 kg (71.5 to 88 lb): 400 mg P.O. once daily

Children weighing 25 to 32.5 kg (55 to 71.5 lb): 350 mg P.O. once daily

Children weighing 20 to 25 kg (44 to 55 lb): 300 mg P.O. once daily

Children weighing 15 to 20 kg (33 to 44 lb): 250 mg P.O. once daily

Children weighing 10 to 15 kg (22 to 33 lb): 200 mg P.O. once daily

Dosage adjustment

• Concurrent use of rifampin or voriconazole


• Hypersensitivity to drug

• Concurrent use of astemizole, cisapride, midazolam, triazolam, ergot derivatives, voriconazole, or bepridil


Use cautiously in:

• hypercholesterolemia, hepatic impairment, concurrent use of hepatotoxic drugs, mental illness, or substance abuse

• concurrent use of St. John's wort (use not recommended)

• pregnant or breastfeeding patients

• children.


• Give on empty stomach.

• Know that drug is given with other antiretrovirals.

Adverse reactions

CNS: dizziness, drowsiness, fatigue, insomnia, abnormal dreams, hypoesthesia, depression, headache, poor concentration, nervousness, anxiety, CNS depression, suicidal ideation

CV: arrhythmias

GI: nausea, diarrhea, flatulence, abdominal pain, dyspepsia

GU: hematuria, renal calculi

Hepatic: hepatotoxicity

Respiratory: respiratory depression

Skin: rash, diaphoresis, pruritus,erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome

Other: increased appetite


Drug-drug. Azole antifungals (ketoconazole, voriconazole): decreased antifungal plasma concentration, increased efavirenz plasma concentration

Calcium channel blockers: possible decreased calcium channel blocker concentration

Clarithromycin, indinavir: reduced blood levels of these drugs

CNS depressants (including antidepressants, antihistamines, opioids): increased CNS depression

CYP450 inducers (including phenobarbital, rifabutin, rifampin): increased clearance and decreased blood level of efavirenz

CYP450 inhibitors, ergot alkaloids, estrogen, midazolam, ritonavir, triazolam: increased blood levels of these drugs, greater risk of serious adverse reactions (including arrhythmias, CNS and respiratory depression, and hepatotoxicity)

HMG-CoA reductase inhibitors: decreased plasma concentration of atorvastatin, pravastatin, and simvastatin

Hormonal contraceptives: increased ethinyl estradiol blood level

Protease inhibitors: decreased plasma level and efficacy of these drugs

Saquinavir: decreased saquinavir blood level

Warfarin: increased or decreased warfarin effects

Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, gamma-glutamyltransferase, total cholesterol, triglycerides: increased levels

Urine cannabinoid test: false-positive result

Drug-food. High-fat meal: increased drug absorption

Drug-herbs. St. John's wort: decreased efavirenz blood level and efficacy, drug resistance

Drug-behaviors. Alcohol use: increased CNS depression

Patient monitoring

• Monitor dietary intake and hepatic and lipid profile.

• Closely monitor patients with hepatic failure.

Record mood changes and stay alert for suicidal ideation or behavior.

• Be aware that drug may cause hypercholesterolemia.

• Know that amount of HIV in blood may increase if patient stops drug therapy even briefly.

Patient teaching

• Instruct patient to take with full glass of water, preferably at bedtime to improve tolerance of CNS effects. Also tell him to avoid taking drug with high-fat meals.

• Inform patient that drug must be taken in combination with other antiretrovirals.

• Tell patient that drug doesn't cure HIV or AIDS and that he can still transmit virus to others.

Advise patient to report suicidal thoughts and other psychiatric symptoms.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

Tell female patient to immediately inform prescriber if she becomes pregnant.

• Advise female patient to use adequate contraceptive measures for 12 weeks after discontinuing drug.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


(e-fa-veer-enz) ,


(trade name)


Therapeutic: antiretrovirals
Pharmacologic: non nucleoside reverse transcriptase inhibitors
Pregnancy Category: D


HIV infection (in combination with one or more other antiretroviral agents).


Inhibits HIV reverse transcriptase, which results in disruption of DNA synthesis.

Therapeutic effects

Slowed progression of HIV infection and decreased occurrence of sequelae.
Increases CD4 cell counts and decreases viral load.


Absorption: 50% absorbed when ingested following a high-fat meal.
Distribution: 99.5–99.75% bound to plasma proteins; enters CSF.
Metabolism and Excretion: Mostly metabolized by the liver.
Half-life: Following single dose—52–76 hr. Following multiple doses—40–55 hr.

Time/action profile (blood levels)

POrapid3–5 hr24 hr


Contraindicated in: Hypersensitivity;Concurrent pimozide, midazolam, triazolam, voriconazole (standard doses), St. John's wort, or ergot derivatives;Moderate to severe hepatic impairment.
Use Cautiously in: History of mental illness or substance abuse (↑ risk of psychiatric symptomatology);Mild hepatic impairment;History of seizure disorders (↑ risk of seizures); Obstetric: Use in pregnancy only if other options have been exhausted; birth defects have been reported; Lactation: Breast feeding not recommended for HIV-infected mothers; Pediatric: Children <3 mo (safety not established); ↑ incidence of rash; Geriatric: Cautious initial dosing due to ↑ incidence of renal or cardiac dysfunction.

Adverse Reactions/Side Effects

Central nervous system

  • abnormal dreams
  • depression
  • dizziness
  • drowsiness
  • fatigue
  • headache
  • impaired concentration
  • insomnia
  • nervousness
  • psychiatric symptomatology


  • hepatotoxicity (life-threatening)
  • nausea (most frequent)
  • abdominal pain
  • anorexia
  • diarrhea
  • dyspepsia
  • flatulence


  • hematuria
  • renal calculi


  • rash (most frequent)
  • sweating
  • pruritus


  • hypercholesterolemia
  • hypertriglyceridemia


  • hypoesthesia


  • fat redistribution
  • immune reconstitution syndrome


Drug-Drug interaction

↑ levels of pimozide, midazolam, triazolam, or ergot alkaloids when used concurrently; may result in potentially serious adverse reactions including arrhythmias, CNS, and respiratory depression (concurrent use contraindicated).Induces (stimulates) the hepatic cytochrome P450 3A4 enzyme system and would be expected to influence the effects of other drugs that are metabolized by this system; efavirenz itself is also metabolized by this system.↑ risk of CNS depression with other CNS depressants, including alcohol, antidepressants, antihistamines, and opioid analgesics.Concurrent use with ritonavir ↑ levels of both agents and the likelihood of adverse reactions, especially hepatotoxicity.May ↓ the effectiveness of progestin-containing hormonal contraceptives (e.g., etonogestrel, norelgestromin, levonorgestrel).Use with voriconazole significantly ↓ voriconazole levels and ↑ efavirenz levels; concurrent use with standard doses of voriconazole is contraindicated; if used together, ↑ dose of voriconazole to 400 mg q 12 hr and ↓ dose of efavirenz to 300 mg daily.May ↓ posaconazole levels (avoid concurrent use).↓ indinavir levels (indinavir dose ↑ recommended).↓ saquinavir levels (avoid using saquinavir as the only protease inhibitor with efavirenz).↓ maraviroc levels (maraviroc dose ↑ recommended).May alter the effects of warfarin.May ↓ levels of cyclosporine, tacrolimus, and sirolimus.May ↓ levels of bupropion and sertraline.Rifampin may ↓ levels (↑ dose of efavirenz)Concurrent use with other NNRTIs including etravirine, nevirapine, rilpivirine, and delavirdine may lead to ↓ effectiveness and should be avoided.May ↓ levels of raltegravir May ↓ levels of boceprevir ; avoid concurrent useConcurrent use with telaprevir may ↓ levels of telaprevir and efavirenzUse with St. John’s wort may cause ↓ levels and effectiveness, including development of drug resistance (concurrent use contraindicated).Ingestion following a high-fat meal ↑ absorption by 50%.


Oral (Adults and Children ≥40 kg) 600 mg once daily; Concurrent rifampin therapy (in patients >50 k g)—800 mg once daily.
Oral (Children ≥3 mo and 32.5–39.9 kg) 400 mg once daily.
Oral (Children ≥3 mo and 25–32.4 kg) 350 mg once daily.
Oral (Children ≥3 mo and 20–24.9 kg) 300 mg once daily.
Oral (Children ≥3 mo and 15–19.9 kg) 250 mg once daily.
Oral (Children ≥3 mo and 7.5–14.9 kg) 200 mg once daily.
Oral (Children ≥3 mo and 5–7.4 kg) 150 mg once daily.
Oral (Children ≥3 mo and 3.5–4.9 kg) 100 mg once daily.


Capsules: 50 mg, 200 mg
Tablets: 600 mg
In combination with: emtricitabine and tenofovir (Atripla) (See combination drugs).

Nursing implications

Nursing assessment

  • Assess for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy.
  • Assess for rash, especially during 1st mo of therapy. Onset is usually within 2 wk and resolves with continued therapy within 1 mo. May range from mild maculopapular with erythema and pruritus to exfoliative dermatitis and Stevens-Johnson syndrome. Occurs more often and may be more severe in children. If rash is severe or accompanied by blistering, desquamation, mucosal involvement, or fever, therapy must be discontinued immediately. Efavirenz may be reinstated concurrently with antihistamines or corticosteroids in patients discontinuing due to rash.
  • Assess patient for CNS and psychiatric symptoms (dizziness, impaired concentration, somnolence, abnormal dreams, insomnia) during therapy. Symptoms usually begin during 1st or 2nd day of therapy and resolve after 2–4 wk. Administration at bedtime may minimize symptoms. Concurrent use with alcohol or psychoactive agents may cause additive CNS symptoms.
  • Lab Test Considerations: Monitor viral load and CD4 cell count regularly during therapy.
    • Monitor liver function tests in patients with a history of hepatitis B or C or underlying liver disease. May cause ↑ serum AST, ALT, and GGT concentrations. If moderate to severe liver function test abnormalities occur, efavirenz doses should be held until levels return to normal. Discontinue if liver function abnormalities recur when therapy is resumed.
    • May cause ↑ in total cholesterol and serum triglyceride levels.
    • Obtain a pregnancy test prior to starting therapy. May cause fetal harm if administered during first trimester of pregnancy.
    • May cause false-positive urine cannabinoid results.

Potential Nursing Diagnoses

Risk for infection (Indications)
Noncompliance (Patient/Family Teaching)


  • Oral: Administer on an empty stomach, preferably at bedtime to minimize nervous 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 tsp) of food for children at least 3 mo old and weighing at least 3.5 kg and adults who cannot swallow capsules or tablets. Open capsule carefully; avoid spillage or dispersion of contents into the air. For infants receiving capsule sprinkle-infant formula mixture, gently mix entire capsule contents into 2 tsp (10 mL) of reconstituted room temperature infant formula in a medicine cup, then draw up mixture into a 10 mL oral dosing syringe for administration. Use of infant formula for mixing should only be considered for those young infants who cannot consume solid foods. For patients able to tolerate solid foods, mix entire capsule contents gently with soft food (applesauce, grape jelly, yogurt). After administration of mixture, add a small amount (2 tsp) of food or formula to empty mixing container, stir to disperse any remaining efavirenz residue, and administer to patient. Administer mixture within 30 minutes of mixing. Avoid food for 2 hr after administration.

Patient/Family Teaching

  • Emphasize the importance of taking efavirenz as directed. It must always be used in combination with other antiretroviral drugs. Do not take more than prescribed amount, and do not stop taking without consulting health care professional. Take missed doses as soon as remembered; do not double doses.
  • Instruct patient that efavirenz should not be shared with others.
  • May cause dizziness, impaired concentration, or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Instruct patient to notify health care professional immediately if rash occurs.
  • Inform patient that efavirenz does not cure AIDS or prevent associated or opportunistic 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 unknown at this time.
  • Inform patient that redistribution and accumulation of body fat may occur, causing 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, vitamins, or herbal products being taken and to consult with health care professional 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 efavirenz. 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 determine 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.
Drug Guide, © 2015 Farlex and Partners


A trademark for the drug efavirenz.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.


Efavirenz AIDS An non-nucleoside reverse transcriptase inhibitor NNRTI antiretroviral drug for treating HIV-1 infection approved for once-daily dosing in combination with other antiretroviral agents. See AIDS.
McGraw-Hill Concise Dictionary of Modern Medicine. © 2002 by The McGraw-Hill Companies, Inc.
References in periodicals archive ?
Biopharmaceutical company Bristol-Myers Squibb Company (NYSE:BMY) reported on Friday that it has received US Food and Drug Administration (FDA) approval of a supplemental new drug application (sNDA) for SUSTIVA (efavirenz), including dosing recommendations for HIV-1 infected pediatric patients three months to three years old and weighing at least 3.5 kg.
The team, led by Atlanta physician Melanie Thompson, recommends a regimen of Truvada or Epizom plus either Sustiva, Reyataz, Prezista, or Isentress.
The double-blind, active-controlled, noninferiority study randomized 563 patients to receive either 400 mg raltegravir (Isentress) twice daily or 600 mg efavirenz (Sustiva) once daily both in combination with coformulated teno-fovir and emtricitabine (Truvada), said Dr.
Sales of its AIDS drug Truvada rose 8% to $668.7 million, while sales of Atripla, which combines Truvada with Bristol-Myers Squibb Co.'s (New York) Sustiva into a single pill, rose 23% to $742.7 million.
Bristol-Meyers Squibb (BMS) markets the originator efavirenz product (sold as Sustiva in the USA, Canada and some countries in the European Union).
Baken changed Lowis' medication from Sustiva to Viramune a drug to relieve sleeplessness and resulting fatigue.
The findings are important, however, as one NNRTI (efavirenz, brand name Sustiva) can be taken just once daily, compared to some PI regimens that require taking pills four times daily.
On January 31 the FDA announced that the Sustiva (efavirenz) package insert had been changed "to include drug-drug interaction information regarding coadministration of efavirenz with rifampin, diltiazem, itraconazole, voriconazole, atorvastatin, pravastatin, simvastatin, pimozide and bepridil."
Atripla, the first one-pill product to treat HIV/AIDS, combines the active ingredients of Sustiva, Emtriva and Viread.
* Comment: The combination of the three drugs--efavirenz (Sustiva), a nonnucleoside reverse transcriptase inhibitor, and emtricitabine (Emtriva) and tenofovir (Viread), nucleoside reverse transcriptase inhibitors--was evaluated in 244 HIV-1 infected patients.
The only exception to this is efavirenz (Sustiva, Bristol-Myers Squibb), which is the only HIV medication now classified as category D because it has been linked to an increase in neural tube defects, she said.