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1 Use Cautiously in: Concurrent use of antiarrhythmics, anticonvulsants, antifun-

gals, clarithyromycin, rifabutin, diazepam, dexamethasone, HMG CoA reductase in-
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etravirine (e-tra-veer-een) hibitors (statins), immunusuppressants; Geri: Consider age-relatedpin organ func-
Intelence tion and body mass, concurrent disease states and medications; OB, Lactation:
Safety not established, breast feeding not recommended in HIV-infected women;
Classification
Pedi: Children ⬍6 yr (safety not established).
Therapeutic: antiretrovirals
Pharmacologic: non-nucleoside reverse transcriptase inhibitors Adverse Reactions/Side Effects
Pregnancy Category B CNS: SEIZURES, anxiety, confusion, fatigue, headache, insomnia, sleep disorders.
EENT: blurred vision, vertigo. CV: MYOCARDIAL INFARCTION, angina pectoris, atrial
fibrillation, hypertension. GI: HEPATIC FAILURE, nausea, abdominal pain, anorexia,
Indications dry mouth, hepatitis, stomatitis, vomiting. GU: renal failure. Endo: gynecomastia,
HIV-1 infection (with other antiretrovirals) in treatment-experienced patients who
hyperglycemia, hyperlipidemia. Hemat: anemia, hemolytic anemia. Derm: ERY-
have evidence of viral replication and HIV-1 strains resistant to a non-nucloside re-
THEMA MULTIFORME, STEVENS JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS, rash.
verse transcriptase inhibitor (NNRTI) and other antiretrovirals.
Metab: fat redistribution. Neuro: peripheral neuropathy. MS: hemarthrosis.
Action Misc: DRUG RASH WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), immune re-
Binds to the enzyme reverse transcriptase, which results in disrupted viral DNA syn- constitution syndrome.
thesis. Therapeutic Effects: Evidence of decreased viral replication and reduced
viral load with slowed progression of HIV and its sequelae. Interactions
Drug-Drug: Etravirine is a substrate of the CYP3A4, CYP2C9, and CYP2C19 en-
Pharmacokinetics zyme systems; other medications that induce or inhibit these systems may be expected
Absorption: Well absorbed following oral administration. Food enhances absorp- to alter the response to etravirine. Etravirine is an inducer of CYP3A4 and an inhibi-
tion. tor of CYP2C9 and CYP2C19. The effects of medications that are substrates of these
Distribution: Unknown. enzyme systems may be altered by concurrent use. Concurrent use with other
Protein Binding: 99.9%. NNRTIs including efavirenz, nevirapine, rilpivirine, and delavirdine may lead
Metabolism and Excretion: Mostly metabolized by the liver (CYP3A4, CYP2C9, topeffectiveness and should be avoided. Concurrent use with protease inhibitors
and CYP2C19 enzyme systems); minimal renal excretion; mostly eliminated in feces (PIs) including, nelfinavir and indinavir may lead to altered plasma levels and
as unchanged drug and metabolites. should be untertaken with concurrent low dose ritonavir. Concurrent use with
Half-life: 41 hr. higher dose ritonavir, combination tipranavir/ritonavir, fosamprenavir/rito-
TIME/ACTION PROFILE (blood levels) navir, atazanavir/ritonavir alter levels and effectiveness of etravirine and should
be avoided. Concurrent use with lopinavir/ritonavir mayplevels. Concurrent use
ROUTE ONSET PEAK DURATION of the combination saquinavir/ritonavir should be undertake cautiously.pblood
PO unknown 2.5–4 hr 12 hr levels and effectiveness of antiarrhythmics including amiodarone, disopyram-
ide, flecainide, lidocaine, mexiletine, quinidine, propafenone, and quini-
Contraindications/Precautions dine; blood level monitoring recommended. Blood levels and effects may bepby an-
Contraindicated in: Concurrent use with other NNRTIs, rifampin, rifapentine, St. ticonvulsants including carbamazepine, phenobarbital, and phenytoin.
John’s wort. Concurrent use with voriconazole voriconazole mayqlevels of both drugs;plev-
⫽ Canadian drug name. ⫽ Genetic Implication. CAPITALS indicate life-threatening, underlines indicate most frequent. Strikethrough ⫽ Discontinued.
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2 ● May causeqpancreatic amylase and lipase.

● May causeqin total cholesterol, low density lipoprotein, serum triglyceride, and
els of itraconazole and ketoconazole (dose adjustments may be necessary). Con- glucose levels. PDF Page #2
current use with fluconazole mayqlevels. May alter levels and response to clarith- ● May causeqserum creatinine.
romycin; other agents should be considered. Rifampin and rifapentinepblood ● May causepneutrophils,pplatelet count, anemia and hemolytic anemia.
levels and effectiveness and should be avoided; rifabutin should only be used with-
out a protease inhibitor/ritonavir combination. Mayqblood levels and sedation from Potential Nursing Diagnoses
diazepam, monitor for effects. Levels and effectiveness may bepby dexametha- Risk for infection (Indications)
sone use cautiously and consider alternatives. May alter blood levels and effects of Noncompliance (Patient/Family Teaching)
fluvastatin, lovastatin, and simvastatin(dose adjustments may be necessary. May Implementation
alter blood levels and effects of cyclosporine, sirolimus, and tacrolimus; careful ● PO: Administer tablets twice daily following a meal; type of food does not matter.
monitoring required. Maypthe antiplatelet effects of clopidogrel. Maypbupren- Swallow tablet whole, do not break, crush, or chew. If patient has difficulty swal-
orphine levels. Mayplevels of artemether/lumefantrine and telaprevir. lowing, may disperse tablet in 5 mL (1 teaspoon) of water, or at least enough liq-
Drug-Natural Products: St. John’s wort maypblood levels and effectiveness; uid to cover the medication, stir well until water looks milky. Add more water or
avoid concurrent use. orange juice or milk (do not place tablets in orange juice or milk without first add-
ing water). Avoid grapefruit juice, warm, or carbonated beverages. Once dis-
Route/Dosage
persed, patient should stir well and drink immediately; rinse glass with water and
PO (Adults): 200 mg twice daily.
drink several times to ensure entire dose is consumed.
PO (Children 6– 17 yr and ⱖ30 kg): 200 mg twice daily.
PO (Children 6– 17 yr and 25– 29 kg): 150 mg twice daily. Patient/Family Teaching
PO (Children 6– 17 yr and 20– 24 kg): 125 mg twice daily. ● Emphasize the importance of taking etravirine as directed, at the same time each
PO (Children 6– 17 yr and 16– 19 kg): 100 mg twice daily. day. 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
NURSING IMPLICATIONS health care professional. Take missed doses following a meal if remembered
Assessment within 6 hr of the time its usually taken, then return to regular schedule. If more
● Assess for change in severity of HIV symptoms and for symptoms of opportunistic than 6 hr from time dose is usually taken, omit dose and resume dosing schedule;
infections during therapy. do not double doses.
● Assess patient for rash (mild to moderate rash usually occurs in the 2nd ● Instruct patient that etravirine should not be shared with others.
wk of therapy and resolves within 1– 2 wk of continued therapy). If rash ● Inform patient that etravirine does not cure AIDS or prevent associated or oppor-
is severe (extensive erythematous or maculopapular rash with moist tunistic infections. Etravirine does not reduce the risk of transmission of HIV to
desquamation or angioedema) or accompanied by systemic symptoms others through sexual contact or blood contamination. Caution patient to use a
(serum sickness-like reaction, Stevens-Johnson syndrome, toxic epi- condom and to avoid sharing needles or donating blood to prevent spreading the
dermal necrolysis), therapy must be discontinued immediately. AIDS virus to others. Advise patient that the long-term effects of etravirine are un-
● Lab Test Considerations: Monitor viral load and CD4 cell count regularly dur- known at this time.
ing therapy. ● May cause dizziness, impaired concentration, or drowsiness. Caution patient to
● Monitor liver function tests periodically during therapy. May causeqse- avoid driving or other activities requiring alertness until response to medication is
rum AST, ALT concentrations. known.
䉷 2015 F.A. Davis Company CONTINUED
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etravirine
● Instruct patient to notify health care professional immediately if rash,
signs of hypersensitivity (fever, generally ill feeling, extreme tiredness,
muscle or joint aches, blisters, oral lesions, eye inflammation, facial
swelling), signs and symptoms of liver problems (yellowing of skin or
whites of eyes, dark or tea colored urine, pale colored stools/bowel
movements, nausea, vomiting, loss of appetite, or pain, aching or sensi-
tivity on right side below ribs), or signs of Immune Reconstitution Syn-
drome (signs and symptoms of an infection) occur.
● Advise patient to notify health care professional of all Rx or OTC medications, vita-
mins, or herbal products being taken and to consult with health care professional
before taking other medications, especially St. John’s wort.
● Inform patient that changes in body fat (increased fat in upper back and neck,
breast, and around back, chest, and stomach area, loss of fat from legs, arms, and
face) may occur.
● Advise patients taking oral contraceptives to use a nonhormonal method of birth
control during etravirine therapy and to notify health care professional if they be-
come pregnant or plan to breast feed while taking etravirine.
● 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.